Risperidone od. Risperidone: Comprehensive Guide to Uses, Side Effects, and Dosage Forms
What are the primary uses of Risperidone. How does Risperidone work in treating mental health disorders. What are the common side effects of Risperidone. How is Risperidone administered and what dosage forms are available. What precautions should be taken when using Risperidone. How does Risperidone compare to other antipsychotic medications. What should patients know about Risperidone overdose and potential risks.
Understanding Risperidone: An Overview of the Antipsychotic Medication
Risperidone is a widely prescribed antipsychotic medication used primarily in the treatment of schizophrenia and bipolar disorder. As a second-generation antipsychotic, it offers a unique mechanism of action that sets it apart from older medications in its class. Risperidone works by balancing the levels of certain neurotransmitters in the brain, particularly dopamine and serotonin, which play crucial roles in regulating mood, behavior, and thought processes.
The medication is available in various forms, including tablets, oral solution, and orally disintegrating tablets, allowing for flexibility in administration based on patient needs and preferences. Risperidone’s efficacy in managing symptoms of psychosis and mood disorders has made it a valuable tool in psychiatric care, but like all medications, it comes with potential side effects and considerations that patients and healthcare providers must carefully weigh.
The Mechanism of Action: How Risperidone Affects the Brain
Risperidone’s effectiveness in treating mental health disorders stems from its unique pharmacological profile. As a serotonin-dopamine antagonist, it primarily targets two key neurotransmitter systems in the brain:
- Dopamine receptors: Risperidone blocks D2 receptors, which helps reduce excessive dopamine activity associated with psychotic symptoms.
- Serotonin receptors: It also antagonizes 5-HT2A receptors, contributing to its mood-stabilizing effects and potentially reducing certain side effects associated with dopamine blockade alone.
This dual action on both dopamine and serotonin systems is believed to contribute to Risperidone’s efficacy in treating a range of symptoms associated with schizophrenia and bipolar disorder, including hallucinations, delusions, and mood disturbances. The medication’s ability to modulate these neurotransmitter systems helps restore balance in brain chemistry, potentially leading to improved mental health outcomes for patients.
Indications and Uses: When Is Risperidone Prescribed?
Risperidone is FDA-approved for several psychiatric conditions, showcasing its versatility in mental health treatment. The primary indications for Risperidone include:
- Schizophrenia in adults and adolescents (13 years and older)
- Acute manic or mixed episodes associated with Bipolar I Disorder
- Irritability associated with autistic disorder in children and adolescents
Beyond these approved uses, healthcare providers may prescribe Risperidone off-label for other conditions, such as:
- Obsessive-compulsive disorder (OCD)
- Post-traumatic stress disorder (PTSD)
- Severe behavioral problems in children with developmental disabilities
The decision to prescribe Risperidone is based on a careful evaluation of the patient’s symptoms, medical history, and potential risks and benefits of the medication. Healthcare providers consider factors such as the severity of symptoms, previous treatment responses, and the patient’s overall health profile when determining if Risperidone is an appropriate treatment option.
Dosage Forms and Administration: Tailoring Treatment to Patient Needs
Risperidone is available in several dosage forms, allowing for personalized treatment approaches based on individual patient needs and preferences. The various formulations include:
- Oral tablets: Available in strengths ranging from 0.25 mg to 4 mg
- Oral solution: A liquid form that can be easily measured for precise dosing
- Orally disintegrating tablets (ODT): Dissolve rapidly in the mouth, beneficial for patients who have difficulty swallowing
- Long-acting injectable suspension: Administered by a healthcare professional every two weeks
The choice of dosage form depends on factors such as the patient’s age, the condition being treated, and individual response to the medication. For example, the orally disintegrating tablets may be preferred for children or elderly patients who have trouble swallowing pills, while the long-acting injectable form can improve medication adherence in patients who struggle with daily oral dosing.
Dosing schedules vary based on the specific indication and patient characteristics. Generally, treatment begins with a low dose that is gradually increased to achieve the optimal therapeutic effect while minimizing side effects. Regular monitoring and follow-up with healthcare providers are essential to ensure the medication’s effectiveness and safety throughout the treatment course.
Side Effects and Safety Considerations: Navigating Potential Risks
While Risperidone can be highly effective in managing symptoms of mental health disorders, it’s important for patients and healthcare providers to be aware of potential side effects. Common side effects of Risperidone may include:
- Weight gain and increased appetite
- Drowsiness or fatigue
- Dizziness
- Constipation or diarrhea
- Dry mouth
- Increased prolactin levels, which can lead to sexual dysfunction or breast enlargement
More serious, but less common, side effects can include:
- Extrapyramidal symptoms (EPS) such as muscle stiffness, tremors, or involuntary movements
- Tardive dyskinesia (a potentially irreversible movement disorder)
- Neuroleptic malignant syndrome (a rare but serious condition characterized by fever, muscle rigidity, and altered mental status)
- Increased risk of stroke in elderly patients with dementia-related psychosis
Is Risperidone safe for long-term use? While many patients take Risperidone for extended periods without significant issues, long-term use requires careful monitoring. Regular check-ups, blood tests, and assessments of metabolic parameters are important to ensure the medication’s ongoing safety and efficacy. Patients should be educated about potential side effects and encouraged to report any unusual symptoms to their healthcare provider promptly.
Risperidone in Special Populations: Considerations for Vulnerable Groups
The use of Risperidone in certain populations requires special consideration and careful monitoring:
Elderly Patients
Older adults may be more sensitive to the effects of Risperidone and at higher risk for certain side effects, particularly orthostatic hypotension and falls. Lower starting doses and more gradual dose adjustments are typically recommended for this population.
Children and Adolescents
While Risperidone is approved for use in some pediatric populations, careful consideration of the risks and benefits is crucial. Growth and development should be closely monitored in young patients taking Risperidone.
Pregnant and Breastfeeding Women
The safety of Risperidone during pregnancy and breastfeeding is not fully established. Healthcare providers must carefully weigh the potential risks to the fetus or infant against the benefits of treatment for the mother.
Patients with Comorbid Medical Conditions
Individuals with pre-existing medical conditions, such as cardiovascular disease or diabetes, may require additional monitoring and dose adjustments when taking Risperidone.
How does Risperidone affect these special populations differently? The medication’s effects can vary significantly among different groups due to factors such as altered metabolism, increased sensitivity to side effects, and potential interactions with other medical conditions or treatments. Tailored treatment plans and close follow-up are essential to ensure safe and effective use of Risperidone in these vulnerable populations.
Comparing Risperidone to Other Antipsychotics: Advantages and Disadvantages
Risperidone belongs to the second-generation or atypical antipsychotics, a class of medications that generally offer some advantages over first-generation antipsychotics. When comparing Risperidone to other antipsychotic medications, several factors come into play:
Efficacy
Risperidone has shown comparable efficacy to other atypical antipsychotics in treating schizophrenia and bipolar disorder. Some studies suggest it may be particularly effective in managing positive symptoms of schizophrenia, such as hallucinations and delusions.
Side Effect Profile
Compared to first-generation antipsychotics, Risperidone generally has a lower risk of extrapyramidal symptoms. However, it may carry a higher risk of weight gain and metabolic disturbances compared to some other atypical antipsychotics.
Versatility
Risperidone’s approved indications for use in children and adolescents with autism-related irritability set it apart from some other antipsychotics, making it a valuable option in pediatric psychiatry.
Cost and Availability
As a generic medication, Risperidone is often more affordable than newer, brand-name antipsychotics, potentially improving access to treatment for many patients.
What factors should be considered when choosing between Risperidone and other antipsychotics? The decision to prescribe Risperidone or another antipsychotic medication depends on various factors, including the specific symptoms being treated, the patient’s medical history and risk factors, potential drug interactions, and individual response to treatment. Healthcare providers must carefully weigh these factors to determine the most appropriate medication for each patient.
Managing Risperidone Treatment: Tips for Patients and Caregivers
Successful treatment with Risperidone involves more than just taking the prescribed dose. Patients and caregivers can take several steps to maximize the benefits of treatment and minimize potential risks:
- Adherence to the prescribed regimen: Taking Risperidone consistently as directed is crucial for maintaining its therapeutic effects.
- Regular monitoring: Keeping up with scheduled appointments and recommended tests helps ensure the medication’s ongoing safety and effectiveness.
- Lifestyle modifications: Adopting a healthy diet and regular exercise routine can help manage potential side effects like weight gain.
- Open communication: Patients should feel comfortable discussing any concerns or side effects with their healthcare provider.
- Avoiding alcohol and certain medications: Alcohol and some drugs can interact with Risperidone, potentially altering its effects or increasing side effects.
How can patients effectively communicate with their healthcare providers about Risperidone treatment? Keeping a symptom diary, noting any side effects or changes in mood or behavior, and preparing questions before appointments can facilitate productive discussions with healthcare providers. This open dialogue is essential for optimizing treatment outcomes and addressing any concerns promptly.
Risperidone Uses,Images & Side effects
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Delayed Respiratory Depression After Risperidone Overdose : Anesthesia & Analgesia
Antipsychotic drugs, also called major tranquilizers and neuroleptics, are used to treat schizophrenia and other types of psychoses. Toxicity of these drugs may result from suicidal overdose or from adverse reactions after therapeutic administration. Risperidone overdose is rare but life-threatening. All antipsychotics produce extrapyramidal side effects (EPS), such as acute dystonic reactions, which can cause respiratory difficulty by pharyngeal and laryngeal muscle spasm. The introduction of drugs that produce minimal EPS and of atypical antipsychotics (e.g., risperidone) has allowed separation of antipsychotic from neuroleptic effects and prevents the interchange of terms. The serotonin-dopamine antagonist concept contends that antipsychotics that are more potent at 5-hydroxytryptamine 2A receptors than at D2 receptors (e.g., risperidone) have a low EPS liability (1).
Case Report
A 26-yr-old woman who had been treated with risperidone for 3 mo was found unconscious on the street. The patient was admitted to a state hospital where it was determined that she had ingested 30 mg of risperidone (a suicide attempt after an argument with her husband) rather than her usual amount of 6 mg/d. Her medical history included long-term schizophrenia.
On Day 3 (after 52 h), respiratory distress developed, and the patient was transferred to our university hospital. On admission, she was hypotensive, with an arterial blood pressure (BP) of 80/50 mm Hg, and she had a Glasgow Coma Scale (GCS) score of 8 of 15. A chest radiograph showed no abnormality. Serum electrolytes and her electrocardiogram were normal (heart rate, 50 bpm). The slow heart rate and BP responded initially to treatment that included IV fluids and a single dose of 0.5 mg of atropine.
Two hours after arrival in the intensive care unit (ICU), the patient’s respiratory drive began failing, and she started gasping. The blood gas analysis at this time, under O2 6 L/min with face mask, showed a pH value of 7.39, Po2 of 51 mm Hg, Pco ovid.com/mrws/1.0″>2 of 54 mm Hg, and HCO3 of 24.3 mmol/L, with a respiratory rate of 5 breaths/min. After 10 min, the patient had a respiratory arrest and was endotracheally intubated and ventilated. Sedation was maintained by propofol infusion. A computed tomography scan of the head was performed and showed no abnormalities. There were no other causes of respiratory depression, and she was not receiving any other respiratory depressant drugs. The patient remained hemodynamically stable, and laboratory tests were normal.
The patient started to make respiratory efforts on Day 5. Her reported GCS was 13. After 6 h, she managed to breathe spontaneously with a continuous positive airway pressure mode. She was tracheally extubated on Day 6 and discharged from the ICU on Day 8.
Discussion
Toxicity of antipsychotic drugs results from unintentional or intentional overdose or from adverse reactions after therapeutic administration. EPS are a result of basal ganglia dopamine D2 receptor blockade and consist of four main drug-induced syndromes. These can be divided into reversible syndromes, which occur within days to weeks of the onset of antipsychotic therapy (acute dystonia, parkinsonism, and akathisia) and a potentially irreversible syndrome that occurs after months to years of therapy (tardive dyskinesia).
Acute dystonic reactions (dyskinesias) consist of intermittent spasmodic or sustained involuntary contractions of muscles in the face, neck, trunk, and occasionally the extremities. Resulting clinical manifestations include trismus, tongue protrusion, torticollis, opisthotonos, and respiratory difficulty. Pharyngeal and laryngeal muscle spasm may produce respiratory distress and asphyxia (2,3).
Reported side effects of risperidone are lethargy, dystonia, hypotension, tachycardia, dysrhythmia, impaired concentration, and abnormal temperature regulation (4–7). The recommended dose is 2 mg on Day 1, 4 mg on Day 2, and 6 mg on Day 3; however, in the elderly (or in patients with hepatic or renal failure), the dose is 0.5 mg up to 2 mg on Day 3. This patient was under treatment with risperidone for three months, and her usual medication was 6 mg/d.
Delayed respiratory failure has not been a prominent feature in overdose cases. Rassam and Srinivasa (8) reported a 72-year-old patient with respiratory depression after accidental risperidone overdose, and Acri and Henretig (9) reported cases of impaired respiration when risperidone was given concomitantly with other respiratory depressant drugs resulting in no additive side effects.
In this case, we evaluated whether acute dystonic reaction contributed to the clinical course of our patient, who demonstrated lethargy, tongue protrusion, and pharyngeal-laryngeal muscle spasm, all of which were related to respiratory dysfunction.
Experience with risperidone overdose is limited and the clinical presentation difficult to predict after an overdose. Therefore, patients who are being treated for risperidone overdose should be monitored for hypotension, sedation, and respiratory depression. It should be noted that respiratory depression may be seen as late as the third day after risperidone overdose.
References
1. Huttunen M. The evolution of the serotonin-dopamine antagonist concept. J Clin Psychopharmacol 1995;15:4–8.
2. Rupniak NMJ, Jenner P, Marsden CD. Acute dystonia induced by neuroleptic drugs. Psychopharmacology (Berl) 1986;88:403–5.
3. Sweet C. Drug-induced dystonia. Am J Psychiatry 1975;132:532–7.
4. Himstreet JE, Daya M. Hypotension and orthostasis following a risperidone overdose. Ann Pharmacother (United States) 1998;32:267–70.
5. Brown K, Levy H, Brenner C, et al. Overdose of risperidone. Ann Emerg Med 1993;22:1908–10.
6. Vecchio FL, Hamilton RJ, Hoffman RJ. Risperidone overdose. Am J Emerg Med 1996;14:95–6.
7. British Medical Association and the Royal Pharmaceutical Society of Great Britain. Risperidone. British National Formulary 2001;41:182–9.
8. Rassam S, Srinivasa R. Respiratory depression after accidental risperidone overdose. Am J Emerg Med 2002;20:570–4.
9. Acri AA, Henretig FM. Effects of risperidone in overdose. Am J Emerg Med 1998;16:498–501.
What you need to know about Risperdal (risperidone)!
What is Risperdal?
Risperdal is a medication known as an atypical antipsychotic that is used to treat symptoms of schizophrenia in teenagers and adults. The medication is also sometimes used to treat symptoms of bipolar disorder.
When did the U.S. Food and Drug Administration (FDA) approve the medication?
Risperdal was first approved by the FDA in 1993.
Is there a generic version of Risperdal?
Yes, risperidone is the generic version of Risperdal and is available in the United States.
Are there any major differences between Risperdal and other antipsychotics used to treat Risperdal?
Risperdal belongs to the class of medications known as atypical antipsychotics or second generation psychotics. The drug is also used to treat symptoms of bipolar disorder and irritability associated with autistic disorder in children. The medication comes in tablet, oral solution, and orally disintegrating tablet forms. Talk to your doctor about what might work best for you and the costs and benefits of taking the medication. Some people may need to try several different antipsychotics before they find the most effective with the fewest side effects.
Can children take Risperdal?
Risperdal has been approved for treatment of schizophrenia for children ages 13-17 years, for Bipolar I disorder in children ages 10-17 years, and for irritability associated with autistic disorder for children ages 5-16 years.
Are there potential interaction issues for people taking Risperdal and any other drugs?
There are hundreds of other drugs which are known to interact with Risperdal in major, moderate, or mild ways. Some of these include antidepressants, carbamazepine, cimetidine, clozapine, dopamine agonists, anxiety medication, high blood pressure medication, seizure medication, paroxetine, phenobarbital, phenytoin, quinidine, ranitidine, rifampin, sedatives, sleep medications, tranquilizers, and valproic acid. Let your doctor know what other prescription and nonprescription medications you are taking before you begin taking the medication.
Are there any other medical conditions that would make someone ineligible for Risperdal therapy?
Talk to your doctor about other medical conditions before you take Risperdal, such as diabetes, dementia, seizures, low white blood cell count, Parkinson’s disease, high cholesterol, high or low blood pressure, a history of heart attack or stroke, breast cancer, heart disease, kidney, disease, or liver disease. Also, talk to your doctor if you have a history of substance abuse or any other mental health issues.
What is the typical starting dose that would be prescribed to someone taking Risperdal?
The FDA recommends a starting dosage of 2mg a day for the treatment of schizophrenia in adults. Safety and efficacy have not been established beyond a dosage of 16mg a day. Dosage may differ when treating other conditions.
What do I do if I miss a dose?
Take the dose of Risperdal when you remember, but skip the missed dose if it’s almost time for your next dose. You should never take extra doses of the medication to make up for missed doses.
Can Risperdal cause side effects?
Common side effects of Risperdal can include:
- Weight gain
- Restlessness
- Agitation
- Dry mouth
- Increased saliva
- Nausea
- Vomiting
- Diarrhea
- Constipation
- Trouble urinating
- Stomach pain
- Vision problems
- Muscle or joint paint
- Heartburn
- Increased appetite
- Anxiety
- Trouble sleeping
- Breast enlargement
- Late or missed menstrual periods
- Decreased sexual ability
- Dry or discolored skin.
Doctors recommend that you not drink alcohol while on the medication. It also is recommended that you wait to drive or operate machinery until you know how the medication affects you. Report major side effects to your doctor immediately, which can include faintness, unusual body movements, sweating, fever, stiff muscles, fever, seizures, hives, itching, shuffling walk, difficulty breathing or swallowing, and long-lasting and pain erection. You can also report side effects to the FDA at 1-800-FDA-1088 or online.
What are the potential long-term effects of taking Risperdal?
Your doctor should monitor for progression of potential long-term side effects of Risperdal, which can include changes in heart rhythm, weight gain, high blood sugar, and tardive dyskinesia.
Is it safe for a woman who is pregnant, about to become pregnant, or nursing to take Risperdal?
There have been no controlled human pregnancy studies on the effects of Risperdal. The drug can be transferred via human breast milk, and patients are advised not to breastfeed while taking the medication. Before you take Risperdal, talk to your doctor if you are pregnant, planning to become pregnant, or are nursing.
Can symptoms occur if Risperdal is discontinued?
It’s important not to discontinue use of the drug if you feel better. Withdrawal symptoms may include dizziness, nausea, sleepiness, and the return of symptoms of schizophrenia. Maintain contact with your doctor and seek medical attention if necessary when discontinuing the drug, and talk to your doctor about how to mitigate potential withdrawal symptoms.
What should I do if I overdose on Risperdal?
Seek immediate help or call the Poison Help Line at 1-800-222-1222 if you overdose, as it can be fatal. Symptoms may include fainting, blurred vision, drowsiness, fast or irregular heartbeat, dizziness, and seizures.
Is Risperdal habit-forming?
Risperdal has no habit-forming potential, but it is not recommended that you discontinue use of the drug before talking with your doctor, as withdrawal symptoms can occur.
How much does Risperdal cost?
According to goodrx.com, 30 tablets of 1mg Risperdal cost approximately $300. 30 tablets of 1mg generic risperidone cost approximately $14.
Are there any disadvantages to Risperdal?
The biggest disadvantages of Risperdal are the potential long-term side effects, which can include tardive dyskinesia, increased blood sugar, high triglycerides, and weight gain.
DISCLAIMER: The information contained herein should NOT be used as a substitute for the advice of an appropriately qualified and licensed physician or other health care provider. This article mentions drugs that were FDA-approved and available at the time of publication and may not include all possible drug interactions or all FDA warnings or alerts. The author of this page explicitly does not endorse this drug or any specific treatment method. If you have health questions or concerns about interactions, please check with your physician or go to the FDA site for a comprehensive list of warnings.
Article Sources
Last Updated: Feb 21, 2018
Risperidone toxicity • LITFL • Toxicology Library Toxicants
Risperidone is an atypical antipsychotic agent associated with tachycardia and acute dystonic reactions.
Toxic Mechanism:
Risperidone antagonises the mesolimbic dopamine (D2), serotonin and alpha 1 + 2 receptors. Compared with other antipsychotics it has a low affinity for histamine the muscarninic receptors, meaning less CNS depression and anticholinergic features.
Toxicokinetics:
- Rapidly absorbed
- Moderate volume of distribution 1.5 L/kg
- Highly protein bound
- Metabolised in the liver and excreted in the urine
Resuscitation:
Risk Assessment
- Dose related risk assessment is poorly defined
- Children: >1 mg is associated with clinical features. Acute dystonic reactions are more common in children.
- Clinical features should manifest within 4 hours and resolve by 24 hours
- Sinus tachycardia 50%
- Acute dystonia 10%
- Mild sedation
- QT prolongation but no reports of Torsades de pointes
- CNS depression is rare
Supportive Care
Investigations
- Screening: 12 lead ECG, BSL, Paracetamol level
- Specific:
- ECG at presentation and 4 hours (if normal no further ECGs required)
- Sinus tachycardia is common
- Reports of minor QT prolongation but no Torsades de pointes.
Decontamination:
Enhanced Elimination
Antidote
- Benztropine for acute dystonic reactions.
- Over 3 yrs 0.02 mg/kg IM or IV.
- Adults 1mg.
- May repeat in 15 minutes.
Disposition
- Children who are symptomatic all need review
- Patients who are well with a normal baseline ECG can be medically cleared at 4 hours post ingestions
- Symptomatic patients need supportive care until toxicity resolves
- Patients should be warned that extrapyramidal movements may occur up to 3 days later.
References:
Dr Neil Long BMBS FACEM FRCEM FRCPC. Emergency Physician at Burnaby Hospital in Vancouver. Loves the misery of alpine climbing and working in austere environments. Supporter of FOAMed, toxicology, tropical medicine, sim and ultrasound
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Risperidone overdose – wikidoc
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overdosage topics
Human experience
Management of overdosage
Human experience
Pre-marketing experience
Premarketing experience included eight reports of acute Risperidone overdosage with estimated doses ranging from 20 to 300 mg and no fatalities. In general, reported signs and symptoms were those resulting from an exaggeration of the drug’s known pharmacological effects, i.e., drowsiness and sedation, tachycardia and hypotension, and extrapyramidal symptoms. One case, involving an estimated overdose of 240 mg, was associated with hyponatremia, hypokalemia, prolonged QT, and widened QRS. Another case, involving an estimated overdose of 36 mg, was associated with a seizure. Return to top
Post-marketing experience
Postmarketing experience includes reports of acute Risperidone overdosage, with estimated doses of up to 360 mg. In general, the most frequently reported signs and symptoms are those resulting from an exaggeration of the drug’s known pharmacological effects, i.e., drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms. Other adverse events reported since market introduction which were temporally (but not necessarily causally) related to Risperidone overdose, include torsade de pointes, prolonged QT interval, convulsions, cardiopulmonary arrest, and rare fatality associated with multiple drug overdose. Return to top
Management of overdosage
In case of acute overdosage, establish and maintain an airway and ensure adequate oxygenation and ventilation. Gastric lavage (after intubation, if patient is unconscious) and administration of activated charcoal together with a laxative should be considered. Because of the rapid disintegration of Risperdal® M-TAB®Orally Disintegrating Tablets, pill fragments may not appear in gastric contents obtained with lavage.
The possibility of obtundation, seizures, or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis. Cardiovascular monitoring should commence immediately and should include continuous electrocardiographic monitoring to detect possible arrhythmias. If antiarrhythmic therapy is administered, disopyramide, procainamide, and quinidine carry a theoretical hazard of QT-prolonging effects that might be additive to those of risperidone. Similarly, it is reasonable to expect that the alpha-blocking properties of bretylium might be additive to those of risperidone, resulting in problematic hypotension.
There is no specific antidote to Risperidone. Therefore, appropriate supportive measures should be instituted. The possibility of multiple drug involvement should be considered. Hypotension and circulatory collapse should be treated with appropriate measures, such as intravenous fluids and/or sympathomimetic agents (epinephrine and dopamine should not be used, since beta stimulation may worsen hypotension in the setting of risperidone-induced alpha blockade). In cases of severe extrapyramidal symptoms, anticholinergic medication should be administered. Close medical supervision and monitoring should continue until the patient recovers. Return to top
Adapted from the FDA Package Insert.
Tricyclic antidepressants and tetracyclic antidepressants
Tricyclic antidepressants and tetracyclic antidepressants
Tricyclic and tetracyclic antidepressants affect brain chemicals to ease depression symptoms. Explore their possible side effects and whether one of these antidepressants may be a good option for you.
By Mayo Clinic Staff
Tricyclic and tetracyclic antidepressants, also called cyclic antidepressants, are among the earliest antidepressants developed. They’re effective, but they’ve generally been replaced by antidepressants that cause fewer side effects. However, cyclic antidepressants may be a good option for some people. In certain cases, they relieve depression when other treatments have failed.
Cyclic antidepressants are designated as tricyclic or tetracyclic, depending on the number of rings in their chemical structure — three (tri) or four (tetra).
How cyclic antidepressants work
Cyclic antidepressants ease depression by affecting chemical messengers (neurotransmitters) used to communicate between brain cells. Like most antidepressants, cyclic antidepressants work by ultimately effecting changes in brain chemistry and communication in brain nerve cell circuitry known to regulate mood, to help relieve depression.
Cyclic antidepressants block the reabsorption (reuptake) of the neurotransmitters serotonin (ser-o-TOE-nin) and norepinephrine (nor-ep-ih-NEF-rin), increasing the levels of these two neurotransmitters in the brain. Cyclic antidepressants also affect other chemical messengers, which can lead to a number of side effects.
Cyclic antidepressants approved to treat depression
The Food and Drug Administration (FDA) approved these tricyclic antidepressants to treat depression:
- Amitriptyline
- Amoxapine
- Desipramine (Norpramin)
- Doxepin
- Imipramine (Tofranil)
- Nortriptyline (Pamelor)
- Protriptyline
- Trimipramine
The FDA approved the tetracycline antidepressant maprotiline to treat depression.
Sometimes cyclic antidepressants are used to treat conditions other than depression, such as obsessive-compulsive disorder, anxiety disorders or nerve-related (neuropathic) pain.
Possible side effects and cautions
Because of the different ways cyclic antidepressants work, side effects vary somewhat from medication to medication. Some side effects may go away after a time, while others may lead you and your doctor to try a different medication. Side effects may also be dependent on the dose, with higher doses often causing more side effects.
Some common possible side effects include:
- Drowsiness
- Blurred vision
- Constipation
- Dry mouth
- Drop in blood pressure when moving from sitting to standing, which can cause lightheadedness
- Urine retention
Other possible side effects include:
- Weight loss
- Increased appetite leading to weight gain
- Excessive sweating
- Tremor
- Sexual problems, such as difficulty achieving an erection, delayed orgasm or low sex drive
Generally speaking:
- Amitriptyline, doxepin, imipramine and trimipramine are more likely to make you sleepy than other tricyclic antidepressants are. Taking these medications at bedtime may help.
- Amitriptyline, doxepin, imipramine and trimipramine are more likely to cause weight gain than other tricyclic antidepressants are.
- Nortriptyline and desipramine appear to have better tolerated side effects than other tricyclic antidepressants do.
For antidepressants that cause sleepiness, be careful about doing activities that require you to be alert, such as driving a car, until you know how the medication will affect you.
Which antidepressant is best for you depends on a number of issues, such as your symptoms and any other health conditions you may have. Ask your doctor and pharmacist about the most common possible side effects for your specific antidepressant and read the patient medication guide that comes with the prescription.
Safety issues
Some tricyclic antidepressants are more likely to cause side effects that affect safety, such as:
- Disorientation or confusion, particularly in older people when the dosage is too high
- Increased or irregular heart rate
- More-frequent seizures in people who have seizures
Other issues to discuss with your doctor before you take a cyclic antidepressant:
- Antidepressants and pregnancy. Talk to your doctor about the risks and benefits of using specific antidepressants. Some antidepressants may harm your baby if you take them during pregnancy or while you’re breast-feeding. If you’re taking an antidepressant and you’re considering getting pregnant, talk to your doctor or mental health professional about the possible risks. Don’t stop taking your medication without contacting your doctor first, as stopping might pose risks for you.
- Drug interactions. When taking an antidepressant, tell your doctor about any other prescription or over-the-counter medications, herbs or other supplements you’re taking. Some antidepressants can cause dangerous reactions when combined with certain medications or herbal supplements.
- Serotonin syndrome. Rarely, an antidepressant can cause high levels of serotonin to accumulate in your body. Serotonin syndrome most often occurs when two medications that raise the level of serotonin are combined. These include other antidepressants, certain pain or headache medications, and the herbal supplement St. John’s wort.
- Signs and symptoms of serotonin syndrome include anxiety, agitation, high fever, sweating, confusion, tremors, restlessness, lack of coordination, major changes in blood pressure and a rapid heart rate.
- Seek immediate medical attention if you have any of these signs and symptoms.
- Safety and blood tests. Your doctor may recommend blood levels to determine the most effective dose. Some side effects and benefits of cyclic antidepressants depend on the dose. Overdose of cyclic antidepressants can be dangerous.
- Chronic health conditions. Cyclic antidepressants can cause problems in people with certain health conditions. For example, if you have glaucoma, an enlarged prostate, heart problems, diabetes, liver disease or a history of seizures, talk to your doctor about whether a cyclic antidepressant is a safe choice for you.
Suicide risk and antidepressants
Most antidepressants are generally safe, but the FDA requires that all antidepressants carry black box warnings, the strictest warnings for prescriptions. In some cases, children, teenagers and young adults under 25 may have an increase in suicidal thoughts or behavior when taking antidepressants, especially in the first few weeks after starting or when the dose is changed.
Anyone taking an antidepressant should be watched closely for worsening depression or unusual behavior. If you or someone you know has suicidal thoughts when taking an antidepressant, immediately contact your doctor or get emergency help.
Keep in mind that antidepressants are more likely to reduce suicide risk in the long run by improving mood.
Stopping treatment with cyclic antidepressants
Cyclic antidepressants aren’t considered addictive. However, stopping antidepressant treatment abruptly or missing several doses can cause withdrawal-like symptoms. Symptoms may vary depending on how the drug works. This is sometimes called discontinuation syndrome. Work with your doctor to gradually and safely decrease your dose.
Withdrawal-like symptoms can include:
- Agitation, irritability or anxiety
- Nausea
- Sweating
- Flu-like symptoms, such as chills and muscle aches
- Insomnia
- Lethargy
- Headache
Finding the right antidepressant
People may react differently to the same antidepressant. For example, a particular drug may work better — or not as well — for you than for another person. Or you may have more, or fewer, side effects from taking a specific antidepressant than someone else does.
Inherited traits may play a role in how antidepressants affect you. In some cases, where available, results of special blood tests may offer clues about how your body may respond to a specific antidepressant. However, other variables besides genetics can affect your response to medication.
When choosing an antidepressant, your doctor takes into account your symptoms, any health problems, other medications you take, and what’s worked for you in the past.
Typically, it may take several weeks or longer before an antidepressant is fully effective and for initial side effects to ease up. Your doctor may recommend dose adjustments or different antidepressants, but with patience, you and your doctor can find a medication that works well for you.
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Show references
- Depression: FDA-approved medications may help. U.S. Food and Drug Administration. https://www.fda.gov/consumers/consumer-updates/depression-fda-approved-medications-may-help. Accessed Aug. 13, 2019.
- Depression basics. National Institute of Mental Health. https://www.nimh.nih.gov/health/publications/depression/index.shtml. Accessed Aug. 13, 2019.
- Revisions to product labeling. U.S. Food and Drug Administration. https://www.fda.gov/media/77404/download. Accessed Aug. 13, 2019.
- Mental health medications. National Institute of Mental Health. https://www.nimh.nih.gov/health/topics/mental-health-medications/index.shtml#part_149856. Accessed Aug. 13, 2019.
- Gabriel M, et al. Antidepressant discontinuation syndrome. Canadian Medical Association Journal. 2017; doi:10.1503/cmaj.160991.
- What is pharmacogenomics? Genetics Home Reference. https://ghr.nlm.nih.gov/primer/genomicresearch/pharmacogenomics. Accessed Aug. 13, 2019.
- Hirsch M, et al. Tricyclic and tetracyclic drugs: Pharmacology, administration, and side effects. https://www.uptodate.com/contents/search. Accessed Aug. 19, 2019.
- Tricyclic antidepressants. Facts& Comparisons eAnswers. http://www.wolterskluwercdi.com/facts-comparisons-online/. Accessed Aug. 19, 2019.
- Tetracyclic antidepressants. Facts& Comparisons eAnswers. http://www.wolterskluwercdi.com/facts-comparisons-online/. Accessed Aug. 19, 2019.
- Ritter J, et al. Antidepressant drugs. In: Rang and Dale’s Pharmacology. 9th ed. Elsevier; 2020.
- Amitriptyline (prescribing information). Accord Healthcare Inc.; 2018. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1e6d2c80-fbc8-444e-bdd3-6a91fe1b95bd. Accessed Aug. 19, 2019.
- Amoxapine (prescribing information). Actavis Pharma Inc.; 2015. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a16297df-3158-48db-85e5-5cd506885556. Accessed Aug. 19, 2019.
- Norpramin (prescribing information). Validus Pharmaceuticals LLC; 2018. https://dailymed.nlm.nih.gov/dailymed/drugInfo. cfm?setid=70b562ea-9f21-4e4a-b3ed-0590b2892f6a. Accessed Sept. 12, 2019.
- Doxepin (prescribing information). Amneal Pharmaceuticals NY LLC; 2017. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=20bfb8af-7933-4e5c-a2b5-010659d9125b. Accessed Aug. 19, 2019.
- Tofranil (prescribing information). SpecGx LLC; 2017. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1827a5aa-733a-49d9-89d9-48ea0367b230. Accessed Sept.12, 2019.
- Pamelor (prescribing information). Mallinckrodt Inc.; 2019. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e17dc299-f52d-414d-ab6e-e809bd6f8acb. Accessed Aug. 19, 2019.
- Protriptyline (prescribing information). West-Ward Pharmaceuticals Corp.; 2016. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=700abc58-9362-4ef5-9d7a-dd3c4d364d0a. Accessed Aug. 26, 2019.
- Trimipramine (prescribing information). Breckenridge Pharmaceutical, Inc.; 2019. https://dailymed.nlm.nih.gov/dailymed/drugInfo. cfm?setid=4f31df66-7dc2-1f04-e054-00144ff88e88. Accessed Aug. 20, 2019.
- Maprotiline (prescribing information). Mylan Pharmaceuticals Inc.; 2014. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c3ca69e6-1ea0-4c2c-abcb-7264b2e79a87. Accessed Sept. 12, 2019.
- Krieger CA (expert opinion). Mayo Clinic. Sept. 11, 2019.
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Long-acting risperidone for schizophrenia
Review question
Risperidone is a new antipsychotic drug that was first available as a depot injection. The review analyzes the clinical effects of depot-risperidone in the treatment of patients with schizophrenia.
Relevance
People with schizophrenia often hear voices, see different things (visual hallucinations) and have strange beliefs (delusional beliefs, delusions). Patients can also become withdrawn, socially isolated, tired, and apathetic. The main treatment for these symptoms of schizophrenia is the use of antipsychotic medications (neuroleptics). However, these drugs can cause serious side effects such as weight gain, uncontrolled shaking of the whole body, tremors, cramping, and fatigue (tiredness). A common consequence of these side effects is that patients stop taking their medication (non-compliance), which can lead to an exacerbation of the disease.
Research characteristics
The review was updated in 2015 to include 12 studies involving 5723 people who received depot-risperidone along with other treatments (placebo, conventional oral antipsychotics, oral risperidone, oral quetiapine, oral aripiprazole, oral olanzapine, non-standard / new depot neuroleptics , earlier depot antipsychotics).
Highlights
Based on the review, it is difficult to conclude that depot-risperidone is more effective in treating the symptoms of schizophrenia than placebo or other treatments. In the case of patients who prefer oral administration of drugs, depot-risperidone has shown approximately the same results as oral risperidone. Patients taking oral risperidone can continue with depot-risperidone without the need for pills. However, in high doses, depot-risperidone can cause serious side effects, especially movement disorders, uncontrolled shaking, spasms and tremors. Depo-risperidone can be used in patients who stop taking oral risperidone, which may reduce the risk of an exacerbation with a small risk of increased side effects.
Quality of evidence
The quality of the evidence presented is generally low or moderate at best. There is a need for a large, long-term and well-documented study of the efficacy of depot-risperidone treatment of schizophrenia. Depot injections are often used to treat refusals. Such individuals are difficult to include in research.
Written by a consumer (Ben Gray, Senior Research Fellow, McPean Foundation). http://mcpin.org
VED List
Vital and Essential Medicines (VED; until 2011 – Vital and Essential Medicines) is a list of medicinal products approved by the Government of the Russian Federation for the purpose of state regulation of prices for medicines. The task of state regulation of prices for medicines is to increase the availability of medicines for the population and medical institutions.
The VED List contains a list of medicines under international nonproprietary names and covers almost all types of medical care provided to citizens of the Russian Federation under state guarantees, in particular, emergency medical care, inpatient care, specialized outpatient and inpatient care, and also includes includes a significant amount of medicines sold in the commercial sector.In addition, the List of Vital and Essential Drugs serves as the basis for the development of regional lists of constituent entities of the Russian Federation and formulary lists of drugs of inpatient medical organizations.
It is formed using the international Anatomical Therapeutic Chemical Classification System (ATC).
1. Means for anesthesia
Dinitrogen oxide /
Halothane
Ketamine
Gamma hydroxybutyric acid
Sodium thiopental
Diethyl ether
Propofol
Sevoflurane
2.Sleeping pills
Flunitrazepam
Nitrazepam
Zopiclone
Zolpidem
3. Anticonvulsants
Benzobarbital
Carbamazepine
Valproic acid
Clonazepam
Lamotrigine
Topiramate
Ethosuximide
Phenobarbital
4. Antipsychotics
Haloperidol
Droperidol
Sulpirides
Thioridazine
Chlorpromazine
Amisulpride
Zuclopenthixol
Quetiapine
Clozapine
Levomepromazine
Olanzapine
Peritsiazine
Risperidone
Sertindole
Trifluoperazine
Flupentixol
Fluphenazine
Chlorprothixene
Alimemazin
5. Tranquilizers
Medazepam
Diazepam
Bromodihydrochlorophenylbenzodiazepine
Oxazepam
Chlordiazepoxide
Tofisopam
Morpholinoethylthioethoxybenzimidazole
Hydroxyzine
Diazepam + Cyclobarbital
Alprazolam
6. Sedatives
Valerian
Sodium bromide
Peppermint oil + phenobarbital + ethyl bromisovalerianate
Oregano oil + peppermint oil + phenobarbital + ethyl bromisovalerianate
An alcoholic infusion of leaves and flowers of motherwort ordinary
7.Psychostimulants
Caffeine
8. Antidepressants
Amitriptyline hydrochloride
Fluoxetine
Amitriptyline + Chlordiazepoxide
Venlafaxine
Imipramine
Clomipramine
Lithium carbonate
Maprotiline
Mianserin
Milnacipran
Paroxetine
Pipofezin
Pirlindol
Trazodone
Fluvoxamine
Citalopram
Escitalopram
Sertraline
Agomelatine
nine. Opiate antagonists
Naloxone
Naltrexone
10. Nootropics
Nicotinoyl-gamma-aminobutyric acid
Piracetam
Cerebrolysin
Cattle brain hydrolyzate
Nicergoline
Meldonium
Glycine
Noopept
Betahistine
Piracetam + Vinpocetine
Piracetam + Cinnarizine
Sulbutiamine
Phenylpiracetam
Livestock cerebral cortex polypeptides
Ipidacrine
Citicoline
Hopantenic acid
eleven.Analeptics
Dopamine
Niketamide
12. Antiparkinsonian drugs
Trihexyphenidil
Galantamine
Memantine
Piribedil
Pramipexole
13. Narcotic analgesics
Morphine hydrochloride
Trimeperidine
Fentanyl
Morphine + Codeine + Narcotine + Papaverine + Thebaine
Fentanyl
fourteen. Non-narcotic analgesics and NSAIDs
Acetaminophen
Acetylsalicylic acid
Acetylsalicylic acid + Magnesium hydroxide
Diclofenac sodium
Ibuprofen
Indomethacin
Tenoxicam
Ketorolac
Ketoprofen
Lornoxicam
Metamizole sodium
Tramadol hydrochloride
Nimesulide
Metamizole sodium + Triacetonamine-4-toluenesulfonate
Salicylic acid
Metamizole sodium + Pitofenone + Fenpiverinium bromide
Butorphanol
Nalbuphin
Meloxicam
Choline salicylate
Choline Salicylate + Cetalkonium Chloride
Sumatriptan
15.Local irritants
Levomenthol solution in menthil isovalerate
Ammonia
Camphor
16. Holinotropic drugs
Azamethonium bromide
Articaine + Epinephrine
Atropine
Galantamine
Neostigmine methyl sulfate
Dystigmine bromide
Pilocarpine
Pyridostigmine bromide
Platyphyllin
Methocinia iodide
17. Muscle relaxants
Pipecuronium bromide
Suxamethonium iodide
Tolperisone
Atracuria besilat
Tizanidine
Baclofen
Flupirtine
Rocuronium bromide
18. Adrenomimetics
Naphazoline
Oxymetazoline
Norepinephrine
Phenylephrine
Epinephrine
Ephedrine
Dobutamine
19.Adrenergic blockers
Timolol
Butylaminohydroxypropoxyphenoxymethyl methyloxadiazole
Terazosin
Doxazosin
Tamsulosin
20. Antiallergic drugs
Diphenhydramine
Chloropyramine
Mebhydrolin
Loratadin
Fexofenadine
Ketotifen
Dimethindene
Ebastin
Cromoglycic acid
21.Local anesthetics
Lidocaine
Procaine
Tetracaine
Bupivacaine hydrochloride
Chlorhexidine + lidocaine
Ropivacaine
22. Expectorants and antitussives
Acetylcysteine
Bromhexine
Thermopsis lancent herb + sodium bicarbonate
Codeine + terpine hydrate + sodium bicarbonate
Ambroxol
Butamirat
Bromhexine + Guaifenesin + Salbutamol
23.Bronchodilators
Ipratropium bromide
Tiotropium bromide
Salbutamol
Salmeterol
Salmeterol + fluticasone
Formoterol + Budesonide
Fenoterol hydrobromide
Fenoterol hydrobromide + ipratropium bromide
Theophylline
24. Cardiac glycosides
Digoxin
Strofantin K
Lily of the valley leaf glycoside
25.Antiarrhythmic drugs
Amiodarone
Procainamide
Propranolol
Quinidine
Sotalol
Propafenone
26. Antianginal drugs
Atenolol
Metoprolol
Metoprolol succinate
Nebivolol
Bisoprolol
Betaxolol
Verapamil hydrochloride
Molsidomin
Diltiazem
Isosorbide dinitrate
Isosorbide mononitrate
Nitroglycerine
Ivabradin
27. Means that improve cerebral circulation
Vinpocetine
Nimodipine
Choline alfoscerate
Ethylmethylhydroxypyridine succinate
Livestock cerebral cortex polypeptides
28. Antispasmodics
Bendazole
Papaverine hydrochloride
Pinaveria bromide
Drotaverin
Aminophylline
Theophylline
Cistenal
Spasmotsistenal
Bencyclan
Drotaverine + nicotinic acid
Mebeverin
29.Antihypertensive drugs
Amlodipine
Nifedipine
Clonidine
Rilmenidine
Captopril
Enalapril
Enalapril + Hydrochlorothiazide
Ramipril
Lisinopril
Lisinopril + Hydrochlorothiazide
Perindopril
Fosinopril
Telmisartan
Felodip
Amlodipine + perindopril
Indapamide + Perindopril
Enalapril + indapamide
Losartan
Irbesartan
Candesartan cilexetil
Valsartan
Aliskiren
Moxonidine
thirty. Diuretics
Acetazolamide
Hydrochlorothiazide
Indapamide
Mannitol
Spironolactone
Furosemide
Triamterene + hydrochlorothiazide
Torasemid
Eplerenone
31. Uricosuric funds
Allopurinol
32. Antiulcer drugs
Aluminum hydroxide
Algeldrate + Magnesium hydroxide
Omeprazole
Ranitidine
Famotidine
Sucralfate
Bismuth tripotassium dicitrate (Colloidal bismuth subcitrate)
Pantoprazole
Esomeprazole
Plantain leaf extract
Fennel ordinary fruit
33.Drugs affecting gastrointestinal motility
Loperamide
Simethicone
Microlax
34. Emetics and antiemetics
Metoclopramide
Domperidone
Ondansetron
Itoprid
35. Laxatives
Bisacodyl
Castor oil
Sennoside A + B
Fortrans
36. Hepatotropic drugs
Milk thistle fruit extract
Ursodeoxycholic acid
Essential phospholipids
Bile + Pancreas Powder + Small Intestine Mucosa Powder
Lactulose
Ornithine
Ademetionine
Ropren
Glycyrrhizic acid + phospholipids
Field artichoke leaf extract
37.Enzymes and antienzyme drugs
Aprotinin
Pancreatin
Trypsin
Chymotrypsin
Trypsin + Chymotrypsin
Fibrinolysin
Somatostatin
Octreotide
38. Uterine funds
Oxytocin
Fenoterol
Hexoprenaline
Dihydrogesterone
39. Drugs affecting hematopoiesis
Folic acid
Calcium folinate
Epoetin alfa
Epoetin beta
Filgrastim
Iron sulfate
Iron (III) hydroxide sucrose complex
Iron (III) hydroxide polymaltose
Iron (II) chloride
40. Drugs affecting hemostasis
Heparin sodium
Enoxaparin sodium
Nadroparin calcium
Dalteparin sodium
Fenindion
Warfarin
Dipyridamole
Pentoxifylline
Aminocaproic acid
Etamsilat
Tranexamic acid
Sulodexide
Clopidogrel
Clotting factor IX
Clotting factor VIII
Eptacog alpha (activated)
Alprostadil
Streptokinase
Alteplaza
Tenekteplaza
Rivaroxaban
Fondaparinux sodium
Prourokinase
Urokinase
Dabigatran etexilate
41.Hormones, their analogues and antihormonal agents
Beclomethasone
Budesonide
Dexamethasone
Hydrocortisone
Prednisone
Mazipredon
Methylprednisolone aceponate
Betamethasone
Methylprednisolone
Mometasone
Triamcinolone
Fluticasone
Fluticasone furoate
Flumethasone
Fludrocortisone
Bromocriptine
Chorionic gonadotropin
Nandrolone
Norethisterone
Progesterone
Sinestrol
Testosterone
Estron
Ethinylestradiol
Calcitonin
Proktoven
Dexamethasone + framycetin + gramicidin C
Cinacalcet
42. Thyroid-stimulating agents
Dihydrotachysterol
Levothyroxine
Thiamazole
Potassium iodide
Triiodothyronine
Levothyroxine sodium + liothyronine + potassium iodide
Levothyroxine sodium + liothyronine
43. Biogenic stimulants
Dioxomethyltetrahydropyrimidine
Hyaluronidase
Prostate extract
Chondroitin sulfate
44.Means for the treatment of sugar
diabetes and diabetes insipidus
Desmopressin
Glibenclamide
Gliclazide
Insulin – isophane
Insulin detemir
Insulin lispro
Insulin aspartate biphasic
Insulin glargine
Biphasic insulin
Insulin soluble
Insulin aspart
Metformin
Glickvidone
Glimepiride
Acarbose
Repaglinide
Glibenclamide + Metformin
Adiurecrin
Exenatid
Glucagon
Vildagliptin
Vildagliptin + Metformin
45. Vaccines, serums and other biological products
Vaccines
Immunoglobulins
Gangrenous antitoxin
Anti-snake specific serum
Diphtheria antitoxin
Tetanus toxoid
Bifidobacterium bifidum
Lactobacillus acidophilus
Lactobacillus acidophilus + Kefir fungi
Coli
Linex
Bactisubtil
Coliprotein bacteriophage
Staphylococcal bacteriophage
Enterol
46.Vitamins and their analogues
Ascorbic acid
Thioctic acid
Nicotinic acid
Nicotinamide
Menadione sodium bisulfite
Pyridoxine
Riboflavin
Thiamine
Tocopherol acetate
Cyanocobalamin
Pyridoxine + Thiamine + Cyanocobalamin + Lidocaine
Calcium carbonate + colecalciferol
Alfacalcidol
47 – 48.Preparations for the correction of water-salt
and acid-base balance
Potassium and magnesium asparaginate
Calcium carbonate
Potassium chloride
Calcium chloride
Magnesium sulfate
Sodium bicarbonate
Sodium chloride
Sodium acetate + Sodium chloride
Potassium chloride + Sodium acetate + Sodium chloride
Potassium chloride + Calcium chloride + Magnesium chloride + Sodium lactate + Sodium chloride
Sodium chloride solution complex
Amino acids for parenteral nutrition + other drugs
Human albumin
Dextran
Dextrose + Sodium Hydrocitrate
Gelatin
Hydroxyethyl starch
49. Preparations for parenteral and enteral nutrition
Amino acids for parenteral nutrition + other preparations
Dipeptive
Nutrizone
Enpit
Nutricomp
Nutriflex
Berlamin modular
Ketosteril
Lipofundin
Lipovenosis
Diazon
Glucose
Sorbitol
Amino acids for parenteral nutrition
Osmolite
Oxepa
50.Statins and various medicines,
stimulating metabolic processes
Actovegin
Solcoseryl
Atorvastatin
Atorvastatin + amlodipine
Rosuvastatin
Simvastatin
Ezetimibe
Trimetazidine
Taurine
Troxerutin
Adenosine + Nicotinamide + Cytochrome C
Methylethylpyridinol
Hesperidin + Diosmin
Dioxomethyltetrahydropyrimidine + sea buckthorn buckthorn oil + sulfaetidol
Olazol
Zinc sulfate
Dexrazoxane
Inosine + nicotinamide + riboflavin + succinic acid
51. Immunotropic drugs
Azathioprine
Tyrosyl-D-alanyl-glycyl-phenylalanyl-leucyl-arginine diacetate
Human interleukin-2, recombinant
Interferon alpha
Human immunoglobulin normal
Azoximer bromide
Meglumine Acridone Acetate
Iodophenazone
Arginyl-alpha-aspartyl-lysyl-valyl-tyrosyl-arginine
Penicillamine
Leflunomide
Crocus splendid alkaloid
Tiloron
Cyclosporine
Mycophenolic acid
Mitoxantrone
52.Antibacterial medicines
Pipemidic acid
Nitroxoline
Nitrofurantoin
Nifuroxazide
Furazolidone
Intetrix
Bacterial lysate mixture
Fosfomycin
Furazidine
53. Antibiotics
Ampicillin
Ampicillin + sulbactam
Amoxicillin
Amoxicillin + sulbactam
Amoxicillin + clavulanic acid
Benzylpenicillin
Benzathine benzylpenicillin
Daptomycin
Linezolid
Oxacillin
Cefazolin
Cefuroxime
Cefotaxime
Ceftriaxone
Ceftazidime
Cefoperazone
Cefoperazone + sulbactam
Cefepim
Cefixime
Imipenem + cilastatin
Meropenem
Ertapenem
Vancomycin
Amikacin
Fosfomycin
Gentamicin
Azithromycin
Clarithromycin
Erythromycin
Clindamycin
Doxycycline
Tetracycline
Lincomycin
Ciprofloxacin
Norfloxacin
Pefloxacin
Ofloxacin
Levofloxacin
Moxifloxacin
Tigecycline
Piperacillin + tazobactam
Chloramphenicol
Rifaximin
Netilmicin
54. Sulfanilamide medicines
Co-trimoxazole
Sulfasalazine
Mesalazine
Sulfacetamide
55. Antiviral medicines
Acyclovir
Famciclovir
Dioxotetrahydroxytetra hydronaphthalene
Lamivudine
Zanamivir
Oseltamivir
Idoxuridine
Ganciclovir
Valacyclovir
56.Antiprotozoal drugs
Metronidazole
Chloroquine
Ornidazole
57. Antifungal medicines
Amphotericin B
Voriconazole
Posaconazole
Caspofungin
Fluconazole
Ketoconazole
Nystatin
Clotrimazole
Nitrofungin
58. Anthelmintic drugs
Praziquantel
Mebendazole
Pirantel
59.Disinfectants and antiseptics
Ahdez
Dimethyl sulfoxide
Methenamine
Methylthionine chloride
Brilliant green
Hydroxymethylquinoxylindoxide
Potassium permanganate
Lysoformin
Hydrogen peroxide
Formic acid
Ethanol
Septocide
Furacilin
Boric acid
Xeroform
Iodine
Combined drug
Chlorhexidine bigluconate
Chlorine antiseptics
Silver preparation
Diamond
Wapusan 2000R
Samarovka
Laina
Liquid soap
Silver nitrate, colloidal silver
Disinfectants
Formaldehyde
Povidone iodine
Miramistin
Polyhexanide
Medilok
Hexetidine
60. Insecticides
Permethrin
Benzyl benzoate
61. Antidotes and chelators
Methionine
Sodium thiosulfate
Protamine sulfate
Activated carbon
Unitiol
Cytochrome C
Hemosorbent
Deferoxamine
Enterosorbent
Enterodesis
Acetylcysteine
Dioctahedral smectin
Hydrolytic lignin
Sugammadex
62.Diagnostic tools
Barium sulfate
Yogeksol
Sodium amidotrizoate
Indigocarmine
Yoversol
63. Anti-tuberculosis drugs
Rifampicin
Isoniazid
Kanamycin
Capreomycin
Moxifloxacin
Ofloxacin
Aminosalicylic acid
Pyrazinamide
Prothionamide
Cycloserine
Ethambutol
Ethionamide
Streptomycin
64. Cytostatics
Anastrozole
Buserelin
Cyproterone
Bicalutamide
Zoledronic acid
Pamidronic acid
Treosulfan
Vinorelbin
Asparginase
Bleomycin
Busulfan
Vinblastine
Vincristine
Hydroxycarbamide
Dakarbazine
Daunorubicin
Doxorubicin
Imatinib
Colchicine
Lomustin
Melphalan
Mercaptopurine
Calcium folinate
Gemcitabine
Carboplatin
Capecitabine
Carmustin
Hydrazine sulfate
Temozolomide
Triptorelin
Oxaliplatin
Topotecan
Paclitaxel
Tegafur
Tamoxifen
Tacrolimus
Goserelin
Letrozole
Ibandronic acid
Exemestane
Methotrexate
Procarbazine
Epirubicin
Fluorouracil
Chlorambucin
Cyclophosphamide
Cytarabine
Etoposide
Fludarabine
Mycophenolate mofetil
Mitoxantrone
Cisplatin
Tretinoin
Thioguanine
Ifosfamide
Rituximab
Mesna
65. Other medicines
Sterilization controls
Vaseline medical
Water for injections
Gypsum
Glycerol
Medical gelatin
Talc
Copper sulfate
Zinc oxide
Sulfur besieged
Hydrochloric acid
Citral
Trilon-B
Desicont
Talc + starch
Silver 7.8%
Dexpanthenol
Sea buckthorn oil
66.Medical products
Subclavian catheters
Peripheral intravenous catheters
Urinary catheters
Gauze bandages
Gauze
Biopsy needle
Spinal needle
Epidural needle
Cotton wool
Adhesive plasters
Collagen hemostatic sponge
Infusion systems
Irrigoscopy system
Gloves
Condom
Rubber finger cot
Eye bath
Eye pipette
Syringe
Esmarch’s irrigator
Bed vessel
Warmer
Ice bubble
Kalopriyemnik
Urine collection
Oilcloth
Probes
Esmarch’s harness
Silicone tube
Container Gemakon 500/300/300
Wooden crutches
Esmarch Mug Tips
Cover glass, specimen
Thermometers
Endotracheal tube, tracheostomy
Syringe
Needle
Elastic bandage
Garbage bags
Medical mask
Remedies
Device for active drainage of wounds, dressings with specified healing properties (Hartmann)
Diapers, milk nipple, pacifier, sterile napkins
67. Reagents, culture media, diagnostics
and other consumables
Reagents for CDL
Reagents for PJSC
Reagents for KIL
Reagents and media for the tank. Laboratories
Reagents for OLD
Consumables for OFD
Pharmacy reagents
Consumables for hemodialysis
68. Means for prevention
Rh-conflict between mother and fetus
Resonative
CAMROW
PKB number 5 – Schizophrenia
Schizophrenia is a chronic mental illness, which is characterized by a violation of the unity of thinking processes, with a relatively preserved intellect, which is combined with significant emotional impoverishment and a decrease in will.Hallucinatory and delusional disorders often join.
The term “schizophrenia” itself is made up of two Greek words – “schizo” – I split and “freni” – reason – reason.
This term was first used by the Swiss psychiatrist Eigen Bleuler in 1908. Schizophrenia, of course, existed before, but only by the beginning of the 20th century the idea of it as a special kind of psychoses matured.
In the mass consciousness, there is an unreasonable identification of schizophrenia with a “split personality” – that is, in fact, with a very rare mental disorder, in which different “I” are alternately activated in one person.
Schizophrenia, unfortunately, is quite common. Its prevalence among the population of Russia is 35 per 10,000 people, with no significant difference between the sexes. Thus, in Russia there are at least half a million patients with this serious pathology.
Schizophrenia refers to endogenous mental illness, which means that it is an internal mental breakdown. It cannot be caused by any factors acting on the brain from the outside (trauma, intoxication, severe stress).Of course, these factors can affect the rate of development of schizophrenia, but not on its occurrence. Nevertheless, the mechanism for the development of the schizophrenic process has not yet been established with any certainty. There are several hypotheses on this score. Thus, there is evidence of a connection between schizophrenia and impaired distribution of dopamine in the central nervous system.
The role of heredity is very important. So, if one of the twins fell ill with schizophrenia, then the risk of getting sick for the other twin is 17% in the opposite pair and 48% in the identical one.However, it is believed that in half of cases, schizophrenia arises from an accidental mutation, that is, on the basis of genetic changes that were absent in the parents and appeared after conception.
Symptoms can develop at any age (possibly even in utero), but usually its onset is timed to the third pubertal crisis, that is, by the age of 12-18 years or for the next several years (approximately up to 30 years).
Most often, the disease begins with negative symptoms associated with the loss of normal functioning – a person for no apparent reason changes in character, becomes withdrawn, fenced off, loses social contacts, emotional warmth in relation to loved ones disappears. Previous interests disappear, academic performance at school or university is sharply reduced, or official duties are not fulfilled. Thus, from the very beginning of clinical manifestations, there is a very high risk of disability. In the most unfavorable variant, which is designated as simple schizophrenia, the patient can lie for days, look at the ceiling and, with clear consciousness and normal physical strength, is not able to serve himself elementarily. Even with more favorable options, thinking disorders increase, which are expressed in the influx of thoughts or in the feeling that there are no thoughts at all.Reasoning becomes unproductive, unfocused, an ambivalence is formed towards life phenomena (ambivalence). Speech is notable for its ornateness, sometimes with neologisms that the patient himself comes up with. During a conversation, there are distractions from his topic (slippage), and not on specific details and circumstances, but on the “bad” attitude of certain characters towards the patient, or on global philosophical topics. People with schizophrenia tend to be somewhat cynical about many aspects of their environment.
Patients have a painful feeling that everything around is somehow changed, devoid of naturalness, harmony (- derealization), the same sensations can arise in relation to their personality (- depersonalization). With depersonalization, the consciousness (but not the personality!) Seems to split in two: one part of it looks at what is happening from the side, and the other feels horror at the realization of the loss of control over itself.
Own thoughts and ideas begin to be perceived as alien. According to modern views, this is why verbal hallucinations (“voices”) occur in schizophrenia, and it is not surprising that the sound of “voices” inside the head is typical for this disease.For the same reason, it seems to the patient that someone controls him from the outside, up to the control of movements and the work of internal organs. Visions are less common.
Such a growing wave of unusual sensations is very painful. In many cases, internal tension is somewhat relieved due to the formation of delusional ideas (quickly – like insight – delirium crystallizes). The patient suddenly becomes “clear” that what is happening to him is, for example, the “intrigues” of some “organization”, which, with the help of modern equipment, exerts an “influence” on him from the outside (delirium of persecution, influence).There is also delirium of jealousy, damage. It is clear that the storyline of experiences is influenced by the level of development of society, including the plots of popular works of literature and cinema.
This entire clinical picture often develops acutely, in the form of an attack that lasts from several days to several months, and then may be repeated. Paroxysmal forms of schizophrenia are more favorable, in prognostic terms, than continuous ones. The intervals between attacks are very long (sometimes tens of years), and between them a person looks almost as before, before the illness.But this is rather an exception. Much more often, exacerbations of symptoms are repeated annually or several times a year, and after each new attack comes out, it turns out that the will has become even weaker and the emotions have faded even more. Gradually, over the years, hallucinatory experiences become less relevant. At the same time, but also very slowly, delirium is falling apart as a system of pseudo-logical inferences, – separate scraps of delirium remain. As a result, a defect condition develops that resembles simple schizophrenia.
Patients either do not recognize themselves as sick, or have conflicting thoughts on this score. As a rule, they negatively meet the persuasion of their relatives about the need to see a psychiatrist. There are attempts to alleviate their condition with alcohol and drugs, which only complicates the clinical picture and leads to further social maladjustment.
Under the influence of command “voices” and against the background of delusional experiences, the risk of socially dangerous actions of patients increases. For example, there are known cases of attacks on alleged “persecutors”.But much more often patients with endogenous mental pathology commit OOD by other mechanisms, including when alcohol or drug intoxication influences their behavior, which is superimposed on negative symptoms.
Schizophrenia is the most frequent illness among patients in the Moscow City Clinical Hospital No. 5.
A common diagnosis: “Paranoid schizophrenia, episodic course with a growing defect, incomplete remission.” The clinical picture with this diagnosis includes delusions and hallucinations (usually – delusions of persecution and verbal hallucinations – “voices”).
Treatment of schizophrenia includes antipsychotics, antidepressants, nootropics. The leading role belongs to antipsychotics, whose action is aimed primarily at combating delusions and hallucinations. Against the background of treatment, at first, as a rule, the patient’s affective reaction to his own experiences is dulled – he becomes calmer, psychomotor agitation passes. Then the hallucinations decrease in intensity or completely disappear. All these positive changes become noticeable already in the first days of the use of antipsychotics.But the plot (that is, the plot) of delirium can linger for a long time, although in the picture of internal experiences it fades significantly in relevance. After the relief of acute symptoms, the task comes to the fore: how to reduce negative symptoms and eliminate psychopathic (that is, as with psychopathies) behavioral disorders. This is helped by the latest generation of antipsychotics, such as olanzapine, paliperidone, risperidone. Already at this stage, it is worth thinking about the patient’s rehabilitation. Contrary to the earlier opinion, psychotherapy is indicated for these patients, and it helps to strengthen remission and resocialization.A good prognostic sign is the patient’s participation in physical labor, which, in itself, brings a significant therapeutic effect.
Although schizophrenia is a very formidable disease, it is not a death sentence. Due to the partial preservation of certain abilities (especially intellectual) and non-standard thinking, many of these patients have significant creative potential, which is evident, among other things, from the works presented at the “Ariadne’s Thread” festival of arts.
Risperdal OD – instructions for use, dosage, composition, analogs, side effects / Pillintrip
Inside. Food intake has no effect on drug absorption.
Patients who have persistent drowsiness while taking Risperidone Organica are advised to divide the daily dose into two doses.
Cancellation of the drug Risperidone Organica is recommended to be carried out gradually. Very rarely, after abrupt cessation of high doses of antipsychotic drugs, a withdrawal syndrome occurs, including nausea, vomiting, hyperhidrosis, and insomnia.
Schizophrenia
Adults. Risperidone Organic can be administered 1 or 2 times a day. The initial dose is 2 mg / day. On the second day, the dose can be increased to 4 mg / day. From this point on, the dose can either be kept at the same level, or individually adjusted (if necessary). Usually the optimal dose is 4-6 mg / day. In some cases, a slower dose increase and a lower initial and maintenance dose may be justified. Doses above 10 mg / day have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms.Due to the fact that the safety of doses above 16 mg / day has not been studied, doses above this level cannot be used.
Elderly patients. Risperidone at a different dosage (0.5–1 mg) is recommended for starting therapy. The dosage can be individually increased by 1 mg / day. Tablets of the drug Risperidone Organica 2 mg can be prescribed to elderly patients when, as a result of titration, the maximum recommended daily dose is reached – 4 mg in 2 divided doses.
Children from 13 years old. Risperidone at a different dosage (0.5 mg) is recommended for starting therapy. If necessary, the dose can be increased no earlier than 24 hours by 0.5–1 mg / day. Tablets of the drug Risperidone Organica 2 mg can be prescribed when the daily dose reaches 2 mg as a result of titration with good tolerance. Despite the effectiveness demonstrated in the treatment of schizophrenia in adolescents with doses of risperidone 1–6 mg / day, with the appointment of doses of more than 3 mg / day, no increase in effectiveness was observed, and side effects developed more often.The use of doses above 6 mg / day has not been studied.
Manic episodes associated with bipolar disorder
Adults. The recommended initial dose of the drug is 2 mg / day in 1 dose. If necessary, this dose can be increased no earlier than 24 hours by 1 mg per day. For most patients, the optimal dose is 1–6 mg / day. The use of doses above 6 mg / day in patients with manic episodes has not been studied.
As with any other symptomatic therapy, the advisability of continuing treatment with Risperidone Organica should be regularly evaluated and confirmed.
Elderly patients. Risperidone at a different dosage (0.5–1 mg) is recommended for starting therapy. The dosage can be individually increased by 1 mg / day. Tablets Risperidone Organika 2 mg can be prescribed to elderly patients when the titration reaches the maximum recommended daily dose of 4 mg in 2 divided doses. Care must be taken due to the limited experience of use in elderly patients.
Children from 10 years old. Risperidone at a different dosage (0.5 mg) is recommended for starting therapy.If necessary, the dosage can be increased at least 24 hours later by 0.5–1 mg per day until a dose of 1–2.5 mg / day is reached with good tolerance. Risperidone Organic 2 mg tablets can be prescribed to children under 10 years of age when the titration reaches a daily dose of 2 mg. Despite the effectiveness demonstrated in the treatment of manic episodes associated with bipolar disorder in children, doses of 0.5–6 mg / day, when doses of more than 2.5 mg / day were prescribed, there was no increase in effectiveness, and side effects developed more often.The use of doses above 6 mg / day has not been studied.
Persistent aggression in patients with Alzheimer’s dementia
A different dosage of risperidone (less than 2 mg) is recommended. For persistent aggression in patients with Alzheimer’s dementia, risperidone should not be used for more than 6 weeks. During treatment, the condition of patients and the need for continuation of therapy should be regularly assessed.
Incessant aggression in the structure of behavior disorder
Children from 5 to 18 years old. For patients weighing 50 kg or more, the appointment of risperidone with a different dosage (less than 2 mg) is recommended.
For patients weighing less than 50 kg, a different dosage of risperidone (less than 1 mg) is recommended.
As with any other symptomatic therapy, the advisability of continuing treatment with risperidone should be regularly assessed and confirmed.
Use in children under 5 years of age is not recommended due to the lack of data on efficacy and safety.
Diseases of the liver and kidneys
In patients with kidney diseases, the ability to excrete the active antipsychotic fraction is reduced in comparison with other patients. In patients with liver disease, an increased concentration of the free fraction of risperidone in the blood plasma is observed. The initial and maintenance doses, in accordance with the indications, should be reduced by 2 times, the increase in the dose in patients with liver and kidney diseases should be carried out more slowly.Risperidone should be used with caution in this category of patients.
Int.
Schizophrenia. Adults and children over 15 years old: 1 or 2 times a day. The initial dose is 2 mg / day, on the second day the dose should be increased to 4 mg / day. From this point on, the dose can either be kept at the same level or individually adjusted if necessary. Usually the optimal dose is 4-6 mg / day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.Doses above 10 mg / day have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg / day has not been studied, doses above this level cannot be used. There is no data on use for the treatment of schizophrenia in children under 15 years of age.
Elderly patients and with diseases of the liver and kidneys: the initial dose is 0.5 mg per dose 2 times a day. The dosage can be individually increased to 1-2 mg 2 times a day.
Drug abuse or drug dependence: the recommended daily dose is 2–4 mg.
Behavioral disorders in patients with dementia: initial dose – 0.25 mg per dose 2 times a day. The dosage, if necessary, can be individually increased by 0.25 mg 2 times a day, not more often than every other day. For most patients, the optimal dose is 0.5 mg 2 times a day. However, some patients are shown taking 1 mg 2 times a day. When the optimal dose is reached, taking the drug once a day may be recommended.
Mania for bipolar disorder: The recommended starting dose is 2 mg per day in 1 dose. If necessary, this dose can be increased by 2 mg per day, not more often than every other day. For most patients, the optimal dose is 2–6 mg / day.
Behavioral disorders in patients with mental retardation. Patients weighing 50 kg or more: the recommended initial dose is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg per day, not more often than every other day.For most patients, the optimal dose is 1 mg per day. However, some patients prefer 0.5 mg per day, while others require an increase in dose to 1.5 mg per day.
Patients weighing less than 50 kg: the recommended initial dose is 0.25 mg once a day. If necessary, this dose can be increased by 0.25 mg per day, not more often than every other day. For most patients, the optimal dose is 0.5 mg per day. However, some patients prefer 0.25 mg per day, while some require an increase in dose to 0.75 mg per day.
Long-term use of Risperdal OD in adolescents should be carried out under constant medical supervision.
Not recommended for use in children under 15 years of age.
Int.
Rispolept ® Quiclet tablets can be taken without water or with water or other liquid, but if taken with meals, there should be no food in the mouth when the patient puts the tablet on the tongue. Rispolept ® Queklet tablets begin to disintegrate in the mouth within a few seconds and can be swallowed immediately.
Schizophrenia
Adults and children over 15 years old. Rispolept ® Kviklet can be administered 1 or 2 times a day. The initial dose of the drug Rispolept ® Kviklet – 2 mg / day. On the second day, the dose should be increased to 4 mg / day. From this point on, the dose can either be kept at the same level or individually adjusted if necessary. Usually the optimal dose is 4-6 mg / day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.
Doses above 10 mg / day do not show higher efficacy compared to lower doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg / day has not been studied, doses above this level cannot be used.
Benzodiazepines can be added to therapy with Rispolept ® if additional sedation is required.
Elderly patients. An initial dose of 0.5 mg twice a day is recommended.The dose can be individually increased by 0.5 mg 2 times a day to 1-2 mg 2 times a day.
If it is necessary to use a dose of 0.5 mg, it is recommended to prescribe the drug Rispolept ® , oral solution.
Adolescents over 13 years of age. An initial dose of 0.5 mg is recommended once a day in the morning or in the evening. If necessary, the dose can be increased at least 24 hours later by 0.5–1 mg per day to the recommended dose of 3 mg / day with good tolerance. The safety of doses above 6 mg / day has not been studied.
Patients who experience persistent drowsiness are advised to take half the daily dose 2 times a day.
If it is necessary to use a dose of 0.5 mg, it is recommended to prescribe the drug Rispolept ® , oral solution.
There is no information on the use of the drug for the treatment of schizophrenia in children under 13 years of age.
Behavioral disorders in patients with dementia
An initial dose of 0.25 mg per dose 2 times a day is recommended.The dose, if necessary, can be individually increased by 0.25 mg 2 times a day, not more often than every other day. For most patients, the optimal dose is 0.5 mg 2 times a day. However, some patients are shown taking 1 mg 2 times a day.
Upon reaching the optimal dose, it may be recommended to take the drug once a day.
If it is necessary to use doses of 0.25 or 0.5 mg, it is recommended to prescribe the drug Rispolept ® , oral solution.
Bipolar disorders in mania
Adults. The recommended initial dose of the drug is 2 or 3 mg / day at a time. If necessary, this dose can be increased at least 24 hours by 1 mg / day. For most patients, the optimal dose is 1–6 mg / day.
Adolescents and children over 10 years old. An initial dose of 0.5 mg is recommended once a day in the morning or in the evening. If necessary, the dose can be increased at least 24 hours later by 0.5–1 mg / day to the recommended dose of 2.5 mg / day with good tolerance.For most patients, the optimal dose is 0.5–6 mg / day.
If it is necessary to use a dose of 0.5 mg, it is recommended to prescribe the drug Rispolept ® , oral solution.
The safety of doses above 6 mg / day has not been studied.
Patients who experience persistent drowsiness are advised to take half the daily dose 2 times a day.
There is no information on the use of the drug for the treatment of bipolar disorders in children under 10 years of age.
Behavioral disorders
Patients weighing 50 kg or more. The recommended initial dose of the drug is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg / day no more often than every other day. For most patients, the optimal dose is 1 mg / day. However, for some patients, a dose of 0.5 mg / day is preferable, while some require an increase in the dose to 1.5 mg / day.
If it is necessary to use a dose of 0.5 mg, it is recommended to prescribe the drug Rispolept ® , oral solution.
Patients weighing less than 50 kg. The recommended initial dose of the drug is 0.25 mg once a day. If necessary, this dose can be increased by 0.25 mg / day no more often than every other day. For most patients, the optimal dose is 0.5 mg / day. However, for some patients, a dose of 0.25 mg / day is preferable, while some require an increase in dose to 0.75 mg / day.
If it is necessary to use doses of 0.25 or 0.5 mg, it is recommended to prescribe the drug Rispolept ® , oral solution.
Long-term use of the drug Rispolept ® Kviklet in adolescents should be carried out under the constant supervision of a physician.
Use in children under 5 years of age has not been studied.
Autism in children and adolescents
The dose of Rispolept ® Kviklet should be selected individually. The recommended initial dose of the drug is 0.25 mg / day for patients weighing less than 20 kg and 0.5 mg / day for patients weighing 20 kg or more.On the 4th day of admission, the dose may be increased by 0.25 mg / day for patients weighing less than 20 kg and by 0.5 mg / day per day for patients weighing 20 kg or more.
This dose should be applied until about the 14th day of treatment when an assessment of efficacy is required. A further increase in the dose is carried out only in the absence of efficacy. The dose can be increased at intervals of 2 weeks or more by 0.25 mg / day for patients weighing less than 20 kg and by 0.5 mg / day for patients weighing 20 kg or more.
In clinical studies, the maximum daily dose did not exceed 1.5 mg / day for patients weighing less than 20 kg and 2.5 mg / day for patients weighing 20 kg or more, and 3.5 mg / day for patients with a body weight of more than 45 kg.
Table
Doses of the drug Rispolept ® in the treatment of autism in children (per day)
Body weight, kg | Days 1–3, mg | Days 4–14 +, mg | Increase in dose ( if necessary) | Recommended dose, mg |
Less than 20 | 0.25 | 0.5 | +0.25 mg after 2 weeks or more | 0.5–1.5 |
20 or more | 0.5 | 1 | +0.5 mg after 2 weeks or more | 1–2.5 * |
* For patients weighing more than 45 kg, higher doses may be required, the maximum studied dose is 3.5 mg / day.
If it is necessary to use doses of 0.25 or 0.5 mg, it is recommended to prescribe the drug Rispolept ® , oral solution.
Rispolept ® Quiclet can be administered 1 or 2 times a day.
Patients who experience persistent drowsiness are advised to take a daily dose 1 time before bedtime or 2 times a day.
If consistent efficacy is observed, a decision may be made to gradually reduce the dose to achieve an optimal balance of efficacy and safety.
Use in children under 5 years of age has not been studied.
Other patient groups
Patients with liver and kidney diseases. Patients with kidney disease have a reduced ability to excrete the active antipsychotic fraction compared to other patients. In patients with liver disease, an increased concentration of the free fraction of risperidone in the blood plasma is observed.
The initial and maintenance dose in accordance with the indications should be reduced by 2 times, the dose increase in patients with liver and kidney disease should be carried out more slowly.
If it is necessary to use doses of 0.25 or 0.5 mg, it is recommended to prescribe the drug Rispolept ® , oral solution.
Rispolept ® Kviklet should be prescribed with caution in this category of patients.
V / m , once every 2 weeks, deep into the gluteus muscle, using the sterile needle attached to the syringe. Injections should be given alternately in the right and left buttocks. The drug should not be administered intravenously.
In patients who have not previously received risperidone, it is recommended to determine the tolerance of oral dosage forms of risperidone before starting treatment with Risperdal OD ® .
Adults. The recommended dose is 25 mg every 2 weeks. Some patients require higher doses of 37.5 or 50 mg. In clinical studies, no increase in efficacy was observed with the use of 75 mg. The maximum dose should not exceed 50 mg once every 2 weeks.
Within 3 weeks after the first administration of Risperdal OD ® , the patient should be taking an effective antipsychotic agent.
The dose of the drug can be increased no more than once every 4 weeks.The effect of such an increase in dose should be expected no earlier than 3 weeks after the first injection of the increased dose.
Elderly patients. The recommended dose is 25 mg every 2 weeks. Within 3 weeks after the first injection of Risperdal OD ® , the patient should be taking an effective antipsychotic agent.
Patients with impaired liver or kidney function. There is currently no data on the use of the drug Risperdal OD ® in patients with impaired liver or kidney function.
If it is necessary to treat patients with impaired liver or kidney function with Risperdal OD ® in the first week, it is recommended to take 0.5 mg orally 2 times a day, an oral dosage form of risperidone. During the second week, the patient can take 1 mg 2 times a day or 2 mg 1 time a day. If the patient tolerates an oral dose of at least 2 mg well, then he can be administered IM 25 mg of the drug Risperdal OD ® 1 time in 2 weeks.
Directions for use
The use of Risperdal OD ® requires strict adherence to the instructions for preparing the suspension in order to ensure accurate administration of the drug and avoid possible errors.
To prepare a suspension from the Risperdal OD ® extended-release microgranules in the vial, only the solvent in the pre-filled syringe can be used. The finished suspension is injected intramuscularly only into the gluteal region. The components in the package must not be replaced with any other product. To ensure that the full dose of risperidone is used, the entire contents of the vial must be injected. The introduction of part of the contents of the vial cannot ensure that the patient receives the required dose of the drug.The drug should be administered immediately after preparation of the suspension.
First, remove the package of Risperdal OD ® from the refrigerator and allow the suspension to warm to room temperature for 30 minutes before preparing the suspension.
The contents of the package are shown in the figure below:
1. Remove the colored plastic cap from the bottle. Do not remove the gray rubber plug. Wipe unopened bottle with an alcohol wipe and allow to dry.
2. Open the blister pack and remove the Alaris ™ Smart Site ® Needleless Device by holding it between the white Luer cap and the skirt. Never touch the sharp tip of the .
3. It is very important that the Smart Site ® Needleless Device is correctly installed on the vial, otherwise the solvent may leak when it enters the vial. Place the bottle on a hard surface. Hold the base of the bottle. Aim the Smart Site ® Needleless Device vertically at the vial with the sharp tip in the center of the vial rubber stopper.
Correct
Incorrect
Pushing from top to bottom, push the sharp tip of the Smart Site ® Needleless Device through the center of the vial rubber stopper until the device is securely attached to the top of the vial.
4. Before attaching the syringe to the Smart Site ® Needleless Device, hold the base of the bottle, wipe the syringe attachment point (blue circle) with an alcohol wipe and allow to dry.
5.The pre-filled syringe has a white tip with two parts: a white collar and a glossy white cap. To open the syringe, hold the syringe by the white collar and break off the glossy white cap (the white cap cannot be twisted or cut off) . Then remove the white cap together with the rubber tip inside it.
At all stages of assembly, hold the syringe only by the white collar located on the tip of the syringe.Fixing the white collar will help keep the collar from separating and ensure a good connection to the syringe. Care must be taken not to twist the components during assembly, as in this case, parts of the syringe may come off from it.
6. Holding the syringe by the white collar, insert the syringe into the blue circle of the needleless device, push and turn clockwise so that the syringe is firmly connected to the needleless device (avoid twisting).To prevent the needleless device from rotating while connecting to the syringe, hold the skirt firmly. The syringe and needleless device must be in line.
7. Introduce the entire contents of the solvent syringe into the vial.
8. Holding the syringe plunger with your thumb, shake vigorously the contents of the vial for at least 10 seconds until a homogeneous suspension is formed. After proper mixing, the suspension becomes homogeneous, thick, milky in color. Microgranules may be visible in the liquid, but there should be no dry microgranules not wetted with solvent. Do not store the vial after preparation of the suspension, as the suspension may separate.
9. Turn the bottle upside down and slowly draw the entire contents of the bottle into the syringe. Separate part of the label from the bottle along the perforation line and stick it to the syringe (for identification).
10. Holding the syringe by the white collar, disconnect the syringe from the needleless device. Dispose of the vial and needleless device in accordance with local regulations for the disposal of this type of waste.
11. Open the blister pack of the Needle-Pro ® needle. Do not touch the part of the needle that connects to the syringe. Take the needle out of the package, holding it by the transparent case.
12. To prevent the entry of germs, do not touch the luer tip of the orange needle guard Needle-Pro ® . Holding the syringe by the white collar, attach the orange needle guard Needle-Pro ® Luer-lock cannula to the syringe with a slight clockwise twist.
13. While still holding the syringe by the white collar, clamp the transparent needle sheath and secure the needle tightly to the Needle-Pro ® guard by pressing and turning clockwise. Securing the needle can ensure a safe connection between the needle and the Needle-Pro ® Needle Guard during the following steps.
14. Immediately before administration, the preparation Risperdal OD ® must be resuspended, since after preparation of the suspension in the vial, some of the microgranules may settle.Shake the syringe vigorously to resuspend the microbeads.
15. Holding the syringe by the white collar, remove the transparent case from the needle. Do not bend the case as in this case, the connection of the luer lock can be violated.
16. Tap the syringe lightly with your finger so that the air bubbles in it rise up. Slightly pushing the plunger upward, remove air bubbles from the syringe and needle, holding the syringe so that the needle is pointing straight up. Inject the entire contents of the syringe into the upper outer quadrant of the gluteal region.
The suspension must not be administered intravenously!
Caution: to avoid injury to medical personnel by the used needle:
– do not touch the Needle-Pro ® needle guard with your free hand when pressing it to a flat surface;
– do not disassemble the Needle-Pro ® needle guard;
– do not try to straighten the needle or touch the Needle-Pro ® needle guard if the needle is bent or damaged;
– Use the Needle-Pro ® needle guard only for its intended purpose, otherwise the needle may protrude from the protective cap.
17. After injection, insert the needle into the orange Needle-Pro ® needle guard with one hand. To do this, gently press the orange Needle-Pro ® needle guard against a flat surface.
18. Once the orange Needle-Pro ® needle guard is depressed, the needle should fit snugly into the Needle-Pro ® needle guard. Before discarding the needle, make sure the needle is firmly seated in the orange Needle-Pro ® needle guard.Dispose of in accordance with local regulations for the disposal of this type of waste.
Do not reuse: This device is for single use only. Any attempt at subsequent reuse may adversely affect the integrity of the device itself or result in degradation of its performance.
Sublingual. The lozenges are fragile and should not be squeezed through the foil of the packaging, becausebecause they can break. Open the package by gently pulling on the edge of the blister foil marked with a dot, remove the tablet and immediately put it on the tongue. The tablet begins to dissolve in the mouth within a few seconds and can be swallowed without water; you should also not mix the drug in the mouth with food, bite or chew.
Schizophrenia (acute and chronic) and other psychotic conditions with productive and / or negative symptoms. For adults and children over 15 years of age, the drug is prescribed 1 or 2 times a day.The initial dose is 2 mg / day. On the second day, the dose should be increased to 4 mg / day. From this point on, the dose can either be kept at the same level or individually adjusted if necessary. Usually the optimal dose is 4-6 mg / day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.
Doses above 10 mg / day do not show higher efficacy compared to lower doses and may cause extrapyramidal symptoms.Due to the fact that the safety of doses above 16 mg / day has not been studied, doses above this level should not be used.
Behavioral disorders in patients with dementia with symptoms of aggressiveness (outbursts of anger, physical violence). Mental disorders (agitation, delusions) or psychotic symptoms. The recommended initial dose is 0.25 mg 2 times a day (an adequate dosage form should be used). The dosage, if necessary, can be individually increased by 0.25 mg 2 times a day, not more often than every other day.For most patients, the optimal dose is 0.5 mg 2 times a day. However, some patients are shown taking 1 mg 2 times a day. Upon reaching the optimal dose, it may be recommended to take the drug once a day.
Mania in bipolar disorder. The recommended starting dose is 2 mg once a day. If necessary, this dose can be increased by 2 mg / day no more often than every other day. For most patients, the optimal dose is 2–6 mg / day.
Behavioral disorders in adolescents from 15 years of age and adult patients with reduced intellectual level or mental retardation. Patients weighing 50 kg or more. The recommended starting dose is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg / day, not more often than every other day. For most patients, the optimal dose is 1 mg / day. However, for some patients, a dose of 0.5 mg / day is preferable, while some require an increase in the dose to 1.5 mg / day.
Special patient groups
Elderly patients. Initial dose of 0.5 mg 2 times a day.The dosage can be individually increased by 0.5 mg 2 times a day to 1-2 mg 2 times a day.
Children. The use of the drug Torendo ® Ku-tab in children under 15 years of age is contraindicated.
Long-term use of the drug Torendo ® Ku-tab in adolescents over 15 years old requires constant medical supervision.
Renal and / or liver dysfunction. Therapy with Torendo ® Q-tab is recommended to start with 0.5 mg 2 times a day.The dose can be gradually increased by 0.5 mg of risperidone 2 times a day to 1-2 mg / day. In this group of patients, the drug Torendo ® Ku-tab should be used with caution until more complete information is obtained.
Drug abuse or drug dependence. The recommended daily dose of the drug is 2–4 mg.
Patients weighing less than 50 kg. The recommended initial dose of the drug is 0.25 mg once a day. If necessary, this dose can be increased by 0.25 mg / day, not more often than every other day.For most patients, the optimal dose is 0.5 mg / day. However, for some patients, a dose of 0.25 mg / day is preferable, while others require an increase in dose to 0.75 mg / day.
Inside, regardless of food intake.
Schizophrenia
Adults. Risperdal OD ® can be administered 1 or 2 times a day. The initial dose of Risperdal OD ® is 2 mg / day. On the second day, the dose should be increased to 4 mg / day.From this point on, the dose can either be kept at the same level or individually adjusted if necessary. Usually the optimal dose is 4-6 mg / day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.
Doses above 10 mg / day do not show higher efficacy compared to lower doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg / day has not been studied, doses above this level cannot be used.
Benzodiazepines can be added to therapy with Risperdal OD ® if additional sedation is required.
Elderly patients. An initial dose of 0.5 mg twice a day is recommended. The dose can be individually increased by 0.5 mg 2 times a day to 1-2 mg 2 times a day.
Adolescents over 13 years of age. An initial dose of 0.5 mg is recommended once a day in the morning or in the evening. If necessary, the dose can be increased at least 24 hours later by 0.5–1 mg per day to the recommended dose of 3 mg / day with good tolerance.The safety of doses above 6 mg / day has not been studied.
Patients who experience persistent drowsiness are advised to take half the daily dose 2 times a day.
There is no information on the use of the drug for the treatment of schizophrenia in children under 13 years of age.
Behavioral disorders in patients with dementia
An initial dose of 0.25 mg per dose 2 times a day is recommended. The dose, if necessary, can be individually increased by 0.25 mg 2 times a day, not more often than every other day.For most patients, the optimal dose is 0.5 mg 2 times a day. However, some patients are shown taking 1 mg 2 times a day.
Upon reaching the optimal dose, it may be recommended to take the drug once a day.
Bipolar disorders in mania
Adults. The recommended initial dose of the drug is 2 or 3 mg / day at a time. If necessary, this dose can be increased at least 24 hours by 1 mg / day. For most patients, the optimal dose is 1–6 mg / day.
Adolescents and children over 10 years old. An initial dose of 0.5 mg is recommended once a day in the morning or in the evening. If necessary, the dose can be increased at least 24 hours later by 0.5–1 mg / day to the recommended dose of 2.5 mg / day with good tolerance. For most patients, the optimal dose is 0.5–6 mg / day.
The safety of doses above 6 mg / day has not been studied.
Patients who experience persistent drowsiness are advised to take half the daily dose 2 times a day.
There is no information on the use of the drug for the treatment of bipolar disorders in children under 10 years of age.
Behavioral disorders
Patients weighing 50 kg or more. The recommended initial dose of the drug is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg / day no more often than every other day. For most patients, the optimal dose is 1 mg / day. However, for some patients, a dose of 0.5 mg / day is preferable, while some require an increase in the dose to 1.5 mg / day.
Patients weighing less than 50 kg. The recommended initial dose of the drug is 0.25 mg once a day. If necessary, this dose can be increased by 0.25 mg / day no more often than every other day. For most patients, the optimal dose is 0.5 mg / day. However, for some patients, a dose of 0.25 mg / day is preferable, while some require an increase in dose to 0.75 mg / day.
Long-term use of Risperdal OD ® in adolescents should be carried out under constant medical supervision.
Use in children under 5 years of age has not been studied.
Autism in children and adolescents
The dose of Risperdal OD ® should be selected individually. The recommended initial dose of the drug is 0.25 mg / day for patients weighing less than 20 kg and 0.5 mg / day for patients weighing 20 kg or more. On the 4th day of admission, the dose may be increased by 0.25 mg / day for patients weighing less than 20 kg and by 0.5 mg / day per day for patients weighing 20 kg or more.
This dose should be applied until about the 14th day of treatment when an assessment of efficacy is required. A further increase in the dose is carried out only in the absence of efficacy. The dose can be increased at intervals of 2 weeks or more by 0.25 mg / day for patients weighing less than 20 kg and by 0.5 mg / day for patients weighing 20 kg or more.
In clinical studies, the maximum daily dose did not exceed 1.5 mg / day for patients weighing less than 20 kg and 2.5 mg / day for patients weighing 20 kg or more, and 3.5 mg / day for patients with a body weight of more than 45 kg.
Table
Doses of Risperdal OD ® in the treatment of autism in children (per day)
Body weight, kg | Days 1–3, mg | Days 4–14 +, mg | Dose increase (if necessary) | Recommended dose, mg |
Less than 20 | 0.25 | 0.5 | +0.25 mg after 2 weeks or more | 0.5–1.5 |
20 or more | 0.5 | 1 | +0.5 mg after 2 weeks or more | 1–2.5 * |
* Patients weighing more than 45 kg may require higher doses , the maximum studied dose is 3.5 mg / day.
Risperdal OD ® can be administered 1 or 2 times a day.
Patients who experience persistent drowsiness are advised to take a daily dose 1 time before bedtime or 2 times a day.
If consistent efficacy is observed, a decision may be made to gradually reduce the dose to achieve an optimal balance of efficacy and safety.
Use in children under 5 years of age has not been studied.
Other patient groups
Patients with liver and kidney diseases. Patients with kidney disease have a reduced ability to excrete the active antipsychotic fraction compared to other patients. In patients with liver disease, an increased concentration of the free fraction of risperidone in the blood plasma is observed.
The initial and maintenance dose in accordance with the indications should be reduced by 2 times, the dose increase in patients with liver and kidney disease should be carried out more slowly.
Risperdal OD ® should be prescribed with caution in this category of patients.
ADAPTOL | ADEPRESS | AZAPHEN |
AZAFEN MV | AKTAPAROXETIN | ALVENTA |
ALEVAL | ALEMBIK PIPZOL | AMDOAL |
AMINAZINE | AMITRIPTILINE | AMITRIPTILINE NIKOMED |
AMITRIPTILINE-AKOS | AMITRIPTILIN-GRINDEX | AMITRIPTILIN-ZENTIVA |
AMITRIPTILINE-LENS | AMITRIPTILINE-FEREINE | ANAFRANIL |
ANAFRANIL SR | ANVIFEN | ANDANTE |
APO-PAROXETIN | APO-FLUOXETIN | ARIPIPRAZOL OD-TEVA |
ARIPIPRAZOL-TEVA | ARIPRISOL | ASENTRA |
ATARAX | BRINTELLIX | BELLATAMINAL |
BETAMAX | VELAXIN | VALOCORDIN-DOXYLAMINE |
VALDOXAN | VELAFAX MV | VELAFAX |
VELAFAX | VENLAFAXIN ORGANIKA | VENLAXOR |
VENLAFAXIN | VOKSEMEL | VERO-AMITRIPTILINE |
VICTOEL | GALOPERIDOL-ACRI | HALOPERIDOL |
GALOPERIDOL DECANOAT | GALOPERIDOL-FEREINE | GALOPERIDOL-RATIOPHARM |
GALOPERIDOL-RICHTER | DEKSDOR | HYDROXISIN CANON |
GRANDAXIN | DULOXENTA | DEPREFOLT |
DIAMIDAZEPAM | ZALASTA KU-TAB | DULOXETIN CANON |
ROOM | ZIPRASIDON | ZELDOX |
ZILAXERA | ZIPSILA | ZIPREXA |
ZIPREKSA ZIDIS | INVEGA | ZOLOFT |
IKSEL | QUENTIAX SR | KALIKSTA |
QUENTIAX | QUETIAPIN CANON PROLONG | QUETIAPIN |
QUETIAPIN CANON | QUETIAPIN-VIAL | QUETIAPIN SAN |
QUETIAPIN STADA | KETILEPT | KVETIAPIN-NW |
QUETITEX | KLOPIXOL DEPOT | CLOMIPRAMINE |
CLOPIXOL | CONDILIN | KLOPIXOL-AKUFAZ |
CLOFRANEL | XEPLION | HORSE CHESTNUT EXTRACT LIQUID |
KUTIPIN | LAQUEL | KUMENTAL |
LEVOMYCETIN ALCOHOL SOLUTION FOR EXTERNAL APPLICATION 1%, 3%, 5% (YFF) | LEPTINORM | LATUDA |
LENUKSIN | LYUDIOMIL | LERIVON |
LIMIPRANIL | MELIPRAMIN | MEBIKAR |
MEBIX | MIRTAZAPIN CANON | MIRZATEN |
MIRZATEN KU-TAB. | NANTARID | MIRTAZONAL |
MODITEN DEPOT | UNULEPTED | NANTARID |
NEUROPHAZOL | NOOPHEN | NOVO-TRIPTIN |
NOXIBEL | NEWELONG | NORMAZIDOL |
NORMITON | OLANZAPIN-VIAL | OLANZAPIN |
OLANZAPIN CANON | OLANZAPIN-TL | OLANZAPIN-NW |
OLANZAPIN-TEVA | PARNASAN | RIM |
PAXIL | PIRAZIDOL | PAROXETIN |
PERICIASINE | PRAM | PLYSIL |
PLYSIL N | PROPAZINE | PRODEP |
PROZAK | CUT | PROSULPINE |
PROFLUZAK | RIDONEX | RECSETIN |
REMERON | RISDONAL | RILEPT |
RILEPTIDE | RISPERIDON | RISPAXOL |
RISPEN | RISPERIDON ORGANIKA | RISPERIDON ZENTIVA |
RISPERIDON CANON | RISPOLEPT | RISPERIDON-SZ |
RISPERIDON-TL | RISPOLUX | RISPOLEPT KVIKLET |
RISPOLEPT CONSTA | SAROTHEN RETARD | RISSET |
RISSET QUITAB | SELANK | SAFRIS |
SEDALITE | SERVER | SELECTRA |
SENORM | SERLIFT | SERDOLEKT |
SERENATA | SIZODON-SAN | SEROQUEL |
SEROQUEL PROLONG | SIRESTILL | SIMBALTA |
SYOZAM | SPERIDAN | SOLIAN |
SONAPAX | STRESAM | SPITOMIN |
STIMULOTON | TIAPRID | SULPIRIDE |
SULPIRIDE BELUPO | THIORYL | TIAPRIDAL |
THIODAZINE | TORENDO KU-TAB | TISON |
TORENDO | TREVIKTA | TORIN |
TRANQUESIPAM | TRIFTHAZIN-DARNITSA | TRITTICO |
TRIFTHAZINE | FEVARIN | TRUKSAL |
UMORAP | FENZITATE | FESANEF |
PHENAZEPAM | PHENORELAXAN | FLUWAL |
FLUNISAN | FLUOXETIN | FLUOXETIN LANNACHER |
FLUOXETIN-OBL | FLUOXETIN-ACRY | FLUOXETIN-CANON |
FLUFENAZINE | FLUANKSOL | FRAMEX |
CHLOROPHILLIPT | CHLORPROTIXEN | CHLORPROTIXEN ZENTIVA |
CYCLODINONE | CYPRALEX | TSIPRAMIL |
CIRCADIN | CITALIFT | CITALON |
CITALOPRAM | CITOL | EGLEK |
EGLONIL | EGOLANZA | ACEEPY |
ELZEPAM | ELIVEL | ELICEE |
ESPRITAL | ESCITALOPRAM | ETHAPERAZINE |
EPHEVELON | EPHEVELON RETARD |
Problems of general anesthesia while taking psychopharmacotherapy (Part II)
3
Most water-soluble injectable TAPs
(for example, haloperidol, chlorpromazine, trifluopera-
zina, etc.)) T1 / 2 and the retention time on the D2 receptor also
allows them to be used once a day (although in the case of ost-
ry states or in the process of increasing doses, as indicated above, the introduction several times a day can be
forest-like). An exception is the droperidol used in
mainly in anesthesiological practice,
T1 / 2 of which, when injected into a vein, does not exceed 2 hours,
and the main effect falls on the first 30-45
minutes, and when injected into the muscle it lengthens up to 6 hours [Fisc-
hler M et al., 1986].
Oil solutions of prolonged forms of esters
TAP have different T1 / 2 depending both on the specific
TAP and on its dose and on which etheric
residue the particular TAP is connected to. So, for zuclopenthic-
acetate salt (clopixol-akufase) the duration of
action is up to 3 days, for decanoates of haloperidol, flupen-
thixol, zuclopenthixol, perphenazine, fluorophenazine and
for palmitate 9000 depending on the dose varies from 1–2 weeks (with a minimum
dose of the depot preparation) to 4–6 weeks (with a maximum
permissible dose).In accordance with this, the schedule of
repeated administrations is also different for different de-
in the form of TAP and at different dosages.
Main side effects. It is known that many
typical antipsychotics are capable of causing extra-
ramid side effects, such as: acute dystonia,
akathisia, parkinsonism and tardive dyskinesia, prolongation of the
QT interval leading to sudden death [Attri2 JP et al
., 2012; Huyse FJ et al., 2007].
The withdrawal syndrome of typical antipsychotics
Abrupt withdrawal of TAP leads to the development of a syndrome of
mena, which can have manifold manifestations: who had psychotic
manifestations, and received TAP for other indications,
, withdrawal dyskinesia, withdrawal akathisia [Becker RA,
Bykov YV, 2016 (a)], insomnia, anxiety, tremor.
With a sharp abolition of TAP, which have a pronounced m-x –
linoleic effect, so-called. “Holi-
nergic rebound”, manifested by nausea, an-
rexia, sometimes vomiting, diarrhea, painful spasms,
mi of the gastrointestinal tract. With a sharp abolition of TAP with a pronounced alpha-ad-
renoblocking effect, against the background of cancellation,
arterial hypertension is possible.
Atypical antipsychotics
Atypical antipsychotic drugs (AAP)
are called AP, which, unlike TAP, have less ability to cause extrapyramidal syndrome
(EPS), cause less depression5 and less ability to 9000 secondary, AP-induced, negative or deficient symptoms (
NIDS – neuroleptic-induced deficiency syndrome) [Uçok A,
Gaebel W, 2008].Today, the AAP group includes
risperidone, paliperidone, iloperidone, clozapine, queti-
pin, clotiapine, olanzapine, asenapine, aripiprazole, ser-
tindol, ziprasidone, amisulpride and siprasidone. The group of
is constantly updated with new drugs.
The general property of the AAP group to cause less EPS and
secondary negative symptoms is based on the fact that they have a shorter retention time on the D2 receptor
(more quickly “release” the receptor), have a higher
selectivity to D2- receptors of the mesolimbic and me-
zocortical systems than to the D2 receptors of the nigrostri-
ary system and the prefrontal cortex (their binding to the
D2 receptor depends on the “microenvironment” of the receptor),
as well as the fact that many of these,
5-HT2A and 5-HT2C receptors are more strongly blocked than D2 receptors, which, with
, leads to a reciprocal increase in the level of dopamine in the
nigrostriatal system and in the prefrontal cortex and co-
EPS and secondary negative
phenomena [Seeman P, 2002].
Aripiprazole stands alone. Its reduced
ability to induce EPS and secondary negative
phenomena is associated with its special mechanism of action: unlike most AAPs, it is not an antagonist of
D2 receptors, but their weak partial agonist, and,
thus, its action is reduced to imitation of the effect of dopamine in those areas of the brain where its concentration is reduced
, and to blockade of the effect of dopamine in those
areas of the brain where its concentration is high [de Bartolo-
meis A et al., 2015]. In addition, aripiprazole is also a
partial agonist of 5-HT1A receptors, like beads
pyrone, and this is associated with both its antidepressant and
anxiolytic properties, as well as its ability to indirectly
but increase the dopamine system in the nigrostriatal system. and pre-
frontal cortex, which again leads to a decreased ability to cause EPS and secondary negative
symptoms [de Bartolomeis A et al., 2015].
In the lesser ability of AAP to induce EPS, compared to
as compared to TAP, their effect on M-cholinergic receptors
(especially in clozapine and olanzapine), h2-hista
min receptors, a1- adrenergic receptors and others. a1-Antago-
NISM is considered the main mechanism for decreasing EPS in
of the newest AAP iloperidone [Stahl SM, 2013 (b)].
Brief pharmacokinetics and pharmacodynamics
[Bykov Y., et al., 2013].The half-lives of dilutions of
personal AAP vary from 6-7 hours for quetiapine and zipras-
don, up to 72 hours for sertindole and almost 96 hours for aripipraz-
la. Therefore, some AADs (for example, quetiapine or zi-
prasidone) must be taken
2 times a day, while some others, for example,
risperidone or aripiprazole, can be taken once-
times a day (for aripiprazole, a regimen of
administrations every other day has even been developed, which allows its large T1 / 2).It is important to note
that even despite a significant T1 / 2 in some
representatives of the AAP class, their retention time at the
D2 receptor is short and much shorter than that of TAP. Therefore, with even a slight decrease in the concentration of AAP
in the blood, the deterioration of the mental state in patients with
psychoses can occur very quickly, much faster –
faster than in the case of TAP (often the next day
after discontinuation or dose reduction) [Stahl SM, 2013 (a)].
Main side effects. For many AAPs,
is characterized by the ability to cause weight gain, me-
tabolic disorders (hypercholesterolemia, hyperlipidemia
, hyperglycemia), the development of type 2 diabetes
, obesity and metabolic syndrome. This
is associated with their strong 5-HT2C-blocking and h2-hy-
staminoblocking properties, which leads to
increased appetite, drowsiness and weight gain and
metabolic disorders [UHok A, Gaebel W, 2008 ; Attri
JP et al.