What are the effects of a cyclobenzaprine high. How dangerous is abusing this muscle relaxant. What treatment options are available for cyclobenzaprine misuse. What are the risks of combining cyclobenzaprine with other substances.

Understanding Cyclobenzaprine: Uses and Mechanism of Action

Cyclobenzaprine, commonly known by its brand name Flexeril, is a muscle relaxant prescribed to alleviate muscle-related pain, tenderness, and spasms resulting from strains and other muscle injuries. Despite being classified as a low-risk substance by the Drug Enforcement Administration (DEA), cyclobenzaprine abuse has become a growing concern.

How does cyclobenzaprine work? This medication functions by blocking pain signals transmitted from nerves to the brain, both key components of the central nervous system (CNS). Unlike some muscle relaxants, cyclobenzaprine does not directly impact the muscles themselves. This mechanism of action leads to wide-ranging side effects that can affect respiratory, cardiovascular, and gastrointestinal functions.

Onset and Duration of Effects

The effects of cyclobenzaprine typically manifest within 20 to 40 minutes after ingestion. For immediate-release tablets, these effects can last 4-6 hours, while extended-release formulations may produce effects for up to 24 hours. It’s important to note that cyclobenzaprine has a long half-life, which increases the risk of habit formation and potential toxic build-up with prolonged use.

The Potential for Cyclobenzaprine to Induce a High

Can cyclobenzaprine get you high? While cyclobenzaprine is generally considered to have minimal risks when used as prescribed, it does possess sedative properties. Misuse of this drug, such as taking excessive doses, crushing or chewing capsules instead of swallowing them whole, or using it without a prescription, can indeed result in a cyclobenzaprine high.

What does a cyclobenzaprine high feel like? Users typically report feelings of sedation and mild euphoria. However, it’s crucial to understand that these effects come with significant dangers, particularly when cyclobenzaprine is combined with other substances.

Heightened Risks of Polydrug Use

The dangers of a cyclobenzaprine high are significantly amplified when the drug is combined with other substances, especially central nervous system depressants like alcohol, benzodiazepines, and barbiturates. This combination can lead to intense and debilitating consequences affecting cognition, consciousness, and basic bodily functions.

Side Effects and Risks of Cyclobenzaprine Abuse

Cyclobenzaprine abuse can lead to a range of side effects, from common and relatively mild to severe and potentially life-threatening. Understanding these risks is crucial for anyone considering misusing this medication.

Common Side Effects

• Constipation
• Dizziness
• Drowsiness
• Dry mouth
• Extreme fatigue
• Heartburn
• Headache
• Increased heart rate
• Nausea

Uncommon Side Effects

• Chest pain
• Difficulty breathing
• Fast or irregular heartbeat
• Hives or skin rash
• Swelling of tongue or face

Serious Side Effects

• Agitation
• Diarrhea
• Fast heartbeat
• Fever
• Hallucinations
• Loss of coordination
• Muscle stiffness
• Slurred speech
• Shivering
• Sweating
• Twitching
• Vomiting

Dangerous Drug Interactions with Cyclobenzaprine

What are the risks of combining cyclobenzaprine with other substances? The potential for adverse effects significantly increases when cyclobenzaprine is used in conjunction with other drugs. This polydrug use can lead to severe consequences, including an elevated risk of overdose and the development of life-threatening complications.

Interactions with Depressants

When mixed with central nervous system depressants such as alcohol, benzodiazepines, or barbiturates, cyclobenzaprine can amplify their effects. This combination can result in severe CNS depression, extreme drowsiness, and a significantly increased risk of cyclobenzaprine overdose.

Interactions with Stimulants and Antidepressants

Surprisingly, cyclobenzaprine can also be harmful when combined with stimulants or antidepressants. Even over-the-counter migraine medications can pose a risk. These combinations can potentially lead to a condition known as serotonin syndrome, characterized by an excess of serotonin in the body.

Serotonin Syndrome: A Serious Risk

What is serotonin syndrome? This potentially life-threatening condition occurs when there’s an excessive accumulation of serotonin in the body. Symptoms can manifest within hours of taking the medication and range from mild to severe. In extreme cases, serotonin syndrome can be fatal.

Recognizing Cyclobenzaprine Overdose

Understanding the signs of a cyclobenzaprine overdose is crucial for preventing potentially life-threatening situations. While overdose on cyclobenzaprine alone is rare, it becomes a significant risk when the drug is combined with other substances, particularly CNS depressants.

Symptoms of Cyclobenzaprine Overdose

• Severe drowsiness or loss of consciousness
• Extremely slow or shallow breathing
• Seizures
• Severe confusion or disorientation
• Rapid or irregular heartbeat
• High blood pressure
• Dilated pupils
• Muscle rigidity
• Nausea and vomiting
• Hallucinations

If you suspect someone is experiencing a cyclobenzaprine overdose, it’s crucial to seek immediate medical attention. Prompt treatment can significantly improve outcomes and prevent potentially fatal complications.

Cyclobenzaprine Addiction and Withdrawal

While cyclobenzaprine is not classified as a controlled substance, it still carries a risk of addiction, particularly when misused or used for prolonged periods. Understanding the signs of addiction and the potential withdrawal symptoms is essential for anyone using this medication.

Signs of Cyclobenzaprine Addiction

• Taking higher doses than prescribed
• Using the drug without a prescription
• Crushing or chewing tablets to intensify effects
• Combining cyclobenzaprine with other substances for enhanced effects
• Experiencing cravings for the drug
• Continuing use despite negative consequences
• Neglecting responsibilities due to drug use
• Experiencing withdrawal symptoms when not using the drug

Cyclobenzaprine Withdrawal Symptoms

When someone who has been using cyclobenzaprine regularly stops or significantly reduces their dosage, they may experience withdrawal symptoms. These can include:

• Nausea and vomiting
• Headaches
• Fatigue
• Anxiety
• Irritability
• Insomnia
• Muscle pain or spasms
• Sweating
• Tremors

The severity and duration of withdrawal symptoms can vary depending on factors such as the length of use, dosage, and individual physiology. It’s always recommended to taper off cyclobenzaprine under medical supervision rather than stopping abruptly.

Treatment Options for Cyclobenzaprine Misuse and Addiction

For individuals struggling with cyclobenzaprine misuse or addiction, there are several treatment options available. The most appropriate approach will depend on the severity of the addiction, the presence of any co-occurring disorders, and individual circumstances.

Medical Detoxification

For those physically dependent on cyclobenzaprine, medical detoxification may be the first step in treatment. This process involves gradually reducing the dosage of the drug under medical supervision to manage withdrawal symptoms safely. Medical detox can help minimize discomfort and reduce the risk of complications during the withdrawal process.

Inpatient Rehabilitation

Inpatient or residential treatment programs provide intensive, round-the-clock care for individuals with severe addiction or those who have not succeeded with outpatient treatment. These programs typically last 28 to 90 days and offer a structured environment free from triggers and temptations.

Outpatient Treatment

Outpatient programs allow individuals to receive treatment while maintaining their daily responsibilities. These programs vary in intensity, from intensive outpatient programs (IOP) that meet several times a week to standard outpatient care with weekly therapy sessions.

Cognitive Behavioral Therapy (CBT)

CBT is a widely used therapeutic approach for addiction treatment. It helps individuals identify and change negative thought patterns and behaviors associated with drug use. CBT can be particularly effective in developing coping strategies and preventing relapse.

Support Groups

Support groups such as Narcotics Anonymous (NA) or SMART Recovery can provide ongoing support and community for individuals in recovery. These groups offer a platform for sharing experiences, learning from others, and maintaining accountability in the recovery process.

Dual Diagnosis Treatment

For individuals with co-occurring mental health disorders, dual diagnosis treatment is crucial. This approach addresses both the addiction and the underlying mental health issues simultaneously, providing a more comprehensive and effective treatment plan.

Preventing Cyclobenzaprine Misuse: Safe Usage Guidelines

While cyclobenzaprine can be an effective medication when used as prescribed, it’s essential to follow safe usage guidelines to prevent misuse and potential addiction. Here are some key recommendations:

Follow Prescription Instructions

• Take cyclobenzaprine exactly as prescribed by your healthcare provider
• Do not increase your dosage without consulting your doctor
• Do not take the medication for longer than prescribed
• Never share your medication with others

Be Aware of Potential Interactions

• Inform your healthcare provider of all medications you’re taking, including over-the-counter drugs and supplements
• Avoid alcohol and other CNS depressants while taking cyclobenzaprine
• Be cautious when combining cyclobenzaprine with any other medications

Monitor for Side Effects

• Keep track of any side effects you experience
• Report severe or persistent side effects to your healthcare provider immediately
• Be aware of the signs of allergic reactions or severe adverse effects

Store and Dispose of Medication Safely

• Keep cyclobenzaprine in a secure location, out of reach of children and pets
• Dispose of unused medication properly, following FDA guidelines or local take-back programs

Regular Check-ins with Healthcare Provider

• Attend all scheduled follow-up appointments
• Discuss any concerns or changes in your condition with your healthcare provider
• Be honest about your medication use and any urges to misuse the drug

By following these guidelines, patients can maximize the benefits of cyclobenzaprine while minimizing the risks of misuse and addiction. Remember, open communication with your healthcare provider is key to ensuring safe and effective use of any medication.

The Future of Muscle Relaxant Medications: Alternatives to Cyclobenzaprine

As concerns about the potential for misuse and addiction to cyclobenzaprine grow, researchers and pharmaceutical companies are exploring alternative treatments for muscle pain and spasms. These emerging options aim to provide effective relief while minimizing the risks associated with current muscle relaxants.

Non-Pharmacological Approaches

There’s an increasing focus on non-drug therapies for managing muscle pain and spasms. These include:

• Physical therapy and targeted exercises
• Massage therapy
• Acupuncture
• Heat and cold therapy
• Transcutaneous Electrical Nerve Stimulation (TENS)
• Mindfulness and relaxation techniques

Novel Pharmacological Approaches

Researchers are also exploring new pharmacological options with improved safety profiles:

• Selective muscle relaxants that target specific muscle groups without affecting the central nervous system
• Topical formulations that provide localized relief without systemic effects
• Compounds that modulate pain signaling pathways more selectively
• Combination therapies that allow for lower doses of individual medications

Personalized Medicine Approaches

Advancements in genetic testing and biomarker identification may lead to more personalized treatment plans. This could help healthcare providers select the most effective and least risky medications for each individual patient based on their genetic profile and other factors.

As research in this field progresses, it’s likely that we’ll see a shift towards more targeted, safer, and potentially more effective treatments for muscle-related pain and spasms. However, it’s important to note that the development and approval of new medications is a lengthy process, and cyclobenzaprine will likely remain a commonly prescribed option for the foreseeable future.

In the meantime, healthcare providers and patients must work together to ensure the safe and appropriate use of cyclobenzaprine and other current muscle relaxants. This includes careful consideration of the potential risks and benefits, close monitoring for side effects and signs of misuse, and exploring alternative treatment options when appropriate.

What Does A Cyclobenzaprine High Feel Like? Is It Dangerous?

Cyclobenzaprine, better known as the brand name medication Flexeril, is a muscle relaxant used to treat muscle-related pain such as tenderness and spasms from strains and other types of muscle injuries. Despite being deemed low to no-risk by the DEA (Flexeril is not a controlled substance) cyclobenzaprine abuse is a fairly regular occurrence that is at its most dangerous when it’s combined with other substances be they legal or illicit, depressant or stimulant. 

How Does Cyclobenzaprine Work? 

Cyclobenzaprine works by blocking the pain signals sent from nerves to the brain (two key components of the central nervous system), rather than impacting the muscles directly. Like any other drug that impacts the CNS, side effects are far-reaching and affect respiratory, cardiovascular, and even gastrointestinal function. Side effects can take place within 20 to 40 minutes of ingestion and last 4-6 hours for immediate-release tablets or up to 24 hours for extended-release tablets.

Pain medication of any kind has a high potential to be habit-forming, but those with long half-lives such as cyclobenzaprine face a significant risk of doing so and causing toxic levels of medication build-up. As a result, this medication is only intended for short-term use or periods for a few weeks at a time. 

Can Cyclobenzaprine Get You High?

On its own, cyclobenzaprine has minimal risks or long-term effects. However, it does have sedative properties, and misusing this drug (taking too much, crushing or chewing a capsule rather than swallowing, using it without a prescription) can result in a cyclobenzaprine high. 

A cyclobenzaprine high causes feelings of sedation and mild euphoria. Those effects—and its dangers—are heightened when cyclobenzaprine is combined with other drugs, particularly central nervous system depressants such as alcohol, benzos, and barbiturates. 

Wherever there are drug highs to be found, there are adverse effects including the risk of overdosing, developing an addiction, and even withdrawal effects. In rare circumstances, cyclobenzaprine can even cause life-threatening complications. 

Risks & Drug Interactions

The risk of adverse side effects becomes more serious in instances when cyclobenzaprine was combined with other drugs. When mixed with depressants, it can amplify the effects of those drugs to cause intense and debilitating consequences that affect cognition, consciousness, and basic bodily functions. It also significantly increases the likelihood of a cyclobenzaprine overdose which can result in extreme drowsiness and CNS depression.

However, cyclobenzaprine can also be harmful when combined with stimulants, antidepressants, or even simple over-the-counter migraine medication. The presence of cyclobenzaprine in the body can cause a condition called serotonin syndrome; when there’s too much serotonin being present in the body. These symptoms can take effect within hours of taking a medication, ranging from mild to severe, and yes, can even result in death.

Side Effects of Cyclobenzaprine Abuse 

Common Side Effects

• Constipation
• Dizziness
• Drowsiness
• Dry mouth
• Extreme fatigue
• Heartburn
• Headache
• Increased heart rate
• Nausea

Uncommon Side Effects

• Chest pain
• Difficulty breathing
• Fast or irregular heartbeat
• Hives or skin rash
• Swelling of tongue or face

Serious Side Effects

• Agitation
• Diarrhea
• Fast heartbeat
• Fever
• Hallucinations
• Loss of coordination
• Muscle stiffness
• Slurred speech
• Shivering
• Sweating
• Twitching
• Vomiting

Struggling With Prescription Painkillers?

If you are struggling with prescription painkillers, you’re not alone. These drugs (including opioid analgesics) are the leading cause of addiction and overdose in the nation. Specialized addiction treatment centers can help individuals get through unpleasant withdrawal side effects and safely overcome any compulsive or inappropriate use of pain meds. Call today to learn more. 

Sources:

https://www.drugs.com/tips/cyclobenzaprine-patient-tips

https://medlineplus.gov/druginfo/meds/a682514.html

Treatment for Recreational Use of Flexeril

A prescription-based medication, cyclobenzaprine (known by the brand names Flexeril and Amrix) is similar to tricyclic antidepressants and being both diverted and abused, Drug Enforcement Administration (DEA) reports.

Designed for the short-term relief of limited motion and pain that may be caused by muscle spasms, cyclobenzaprine is a central nervous system muscle relaxer that may stop hyperactive nerve firings that can cause muscles to spasm.

The DEA reports that there were more than 25 million prescriptions written for cyclobenzaprine in 2011, which may be a common medication prescribed for back pain. Flexeril comes in tablet form in both immediate- and extended-release formations to be swallowed.

Who Abuses Flexeril and Why?

NIDA reports that young adults between the ages of 18 and 25 (according to 2014 data) abuse prescription drugs at the highest rates of any other age demographic. Young adults may use the Internet to access information on how to abuse Flexeril and the possible desirable effects that may come from the drug’s recreational use. Flexeril may be used to heighten the effects of alcohol or other drugs when used recreationally.

Prescription drugs are abused across almost all age, gender, race, cultural, and socioeconomic demographics, however. For example, the Substance Abuse and Mental Health Services Administration (SAMHSA) reports that prescription drug abuse is increasing for older adults in their 50s, which may be of particular concern due to the range of negative side effects that specifically impact this population group. Flexeril in particular is not even generally prescribed to the elderly population, according to the FDA, because of the high risk factors.

Additionally, individuals with a legitimate prescription to Flexeril may develop a tolerance to the drug, requiring them to take higher and more frequent doses to feel its effects. Drug dependence can develop wherein the brain becomes accustomed to the interaction of cyclobenzaprine and begins to rely on it in order to keep functioning the same way.

Dependence on cyclobenzaprine is recognized by the onset of withdrawal symptoms when the drug leaves the bloodstream. These may include fatigue, nausea, headache, and general malaise.

Understanding Drug Dependence and Addiction

The terms drug dependence and addiction are often used interchangeably; however, they are not the same thing. A dependence on a drug can occur independently of addiction. It is a physical reaction to the brain needing a particular drug to remain balanced. Drug dependence can form even when a drug is taken for medical reasons and used exactly as prescribed. Narcotic drugs, like opioids, and sedatives, like benzodiazepines and tricyclic antidepressants (which are similar in structure to cyclobenzaprine), can cause physical dependence.

Medical help is needed to stop taking a drug after a person has become dependent on it, as withdrawal symptoms and drug cravings may be significant. Instead of stopping the drug suddenly, these drugs can be tapered off slowly, or their dosage slowly reduced over a period of time to minimize withdrawal. This should only be done under medical supervision. Significant dependence, often created by the nonmedical use of drugs, is best treated with medical detox where medications may be used and medical supervision is available around the clock.

Addiction is not just physical but also behavioral. Addiction is classified as a disease by the American Society of Addiction Medicine (ASAM) that is related to changes in brain structure and chemical makeup as the result of substance abuse. The main indicator of drug addiction is a loss of control over drug use. An individual battling addiction may make multiple attempts to stop using the drug, may take more than intended at one time, or may take the drug for longer than initially desired. Individuals suffering from addiction may use drugs in situations that could potentially be hazardous and continue abusing them even when negative consequences are clear.

Signs of a Cyclobenzaprine Overdose

A drug overdose occurs when a toxin is unable to be successfully metabolized and removed from the body, and certain bodily functions are negatively affected. In the case of cyclobenzaprine, the Journal of Occupational Medicine and Toxicology reports that more than 100 mg of the drug taken in one dose can cause a toxic overdose.

The FDA publishes the following as potential overdose signs of Flexural:

• Drowsiness
• Rapid heart rate (tachycardia)
• High blood pressure (hypertension)
• Tremors
• Slurred speech
• Agitation
• Confusion
• Dizziness
• Nausea
• Vomiting
• Hallucinations
• Loss of muscle control (ataxia)
• Coma

Less common and more serious symptoms of a Flexeril overdose, according to the drug’s prescription information published by the FDA, include:

• Chest pain
• Seizures
• Extremely low blood pressure (hypotension)
• The heart stops beating (cardiac arrest)
• Irregular heart rate (cardiac dysrhythmia)
• Fever, muscle rigidity, and altered mental state (neuroleptic malignant syndrome)

A toxic overdose necessitates immediate medical attention.

The DEA reported that in 2010, there were over 10,000 mentions of cyclobenzaprine in calls to the American Association of Poison Control Centers. The Drug Abuse Warning Network (DAWN) published that in 2011, more than 11,000 people sought emergency department (ED) treatment for abuse of cyclobenzaprine.

Recovery Is Possible

If an overdose on cyclobenzaprine is suspected, call 911. Immediate medical attention is always needed in cases of overdose.

If you, or someone you love, have been struggling with Flexeril abuse, treatment is needed. With medical detox and comprehensive addiction treatment, you can leave such abuse in your past and embrace a happier, healthier future without substance abuse of any kind.

About The Contributor

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Author, American Addiction Centers

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antidepressants

Last Updated on Nov 16, 2022

Sergolin

Manufacturer: Teva

Composition and formulation:

tab. p / captivity. shell 30 mg, No. 28, No. 56

Nicergoline 30 mg

Other ingredients: lactose monohydrate, microcrystalline cellulose, magnesium stearate, crospovidone, hypromellose, propylene glycol, talc, titanium dioxide, polysorbate 80, polyethylene glycol 6000.

No. UA/8444/0 1/01 from 17.06.2008 to 06/17/2013

Pharmacological properties:

Pharmacodynamics. Nicergoline is a semi-synthetic derivative of ergot alkaloids that penetrates well into the central nervous system. It has alpha-adrenolytic, vasodilating and antiplatelet properties, improves the metabolism of the central nervous system. Nicergoline improves the dynamics of cerebral and peripheral circulation, reduces vascular resistance and increases blood flow. By inhibiting platelet aggregation, it reduces blood viscosity, reduces the formation of microclots and improves oxygen transport, especially in brain tissues. The drug has a number of neuropharmacological effects. Enhances the absorption and utilization of glucose, as well as the biosynthesis of proteins and nucleic acids in the brain tissue; affects the systems of various neurotransmitters and the mechanisms of their transformation. Nicergoline improves the cholinergic functions of the brain, increases the conversion of dopamine, especially in the mesolimbic region (by modulating dopaminergic receptors), and also improves the mechanisms of cellular signal transmission (increases the conversion of phosphoinositide and increases the translocation of calcium-dependent isoforms of protein kinase C in membrane regions). Influence on mental function. Nicergoline normalizes EEG data in both elderly and young patients with symptoms of brain hypoxia — nicergoline increases ?- and ?-activity, and also reduces ?- and ?-activity. In patients with moderate dementia of various origins (senile dementia of the Alzheimer type and vascular dementia), prolonged treatment with nicergoline (for 2-6 months) leads to positive changes in the bioelectrical activity of the brain. Pharmacokinetics. After oral administration, nicergoline rapidly and almost completely (90-100%) is absorbed and undergoes significant first pass metabolism. The main nicergoline metabolites formed during first pass metabolism are MMDL (1, dimethyl-8?-hydroxymethyl-10?-methoxy-ergoline) and MDL (methyl-8?-hydroxymethyl-10?-methoxy-ergoline). After oral administration, the maximum level of nicergoline in blood plasma is reached after 1-1.5 hours, MMDL – after 1 hour, MDL – after 4 hours. Food intake does not significantly affect the rate and completeness of absorption. More than 90% of nicergoline binds to plasma proteins, mainly to glycoproteins. The concentration of glycoproteins in blood plasma increases with age as a result of acute inflammatory processes, malignant neoplasms or stress. Such conditions cause a decrease in the concentration of nicergoline in the blood plasma. 90% of the administered dose is metabolized, mainly by hydrolysis and desmethylation. The process of desmethylation is determined by the catalytic activity of the CYP 2D6 isoenzyme. Approximately 80% of nicergoline and its metabolites are excreted in the urine, the rest in the feces. Nicergoline and MMDL undergo rapid elimination (biological T1 / 2 is 2.5 hours for nicergoline and 2-4 hours for MMDL), while MDL is excreted more slowly (biological T1 / 2 is 10-12 hours).

Readings:

Alzheimer’s disease of mild to moderate degree, vascular dementia, presenile and senile cognitive disorders, accompanied by a decrease in intelligence, emotional and behavioral disorders, amnesia, a decrease in the ability to concentrate, mood volatility, dizziness, increased fatigue, vestibular and cochlear disorders (ringing in the ears , dizziness, hearing loss). Disorders of the peripheral circulation (Raynaud’s disease).

Usage:

The usual adult dose is 30 mg nicergoline once daily. The dose may be increased to 60 mg/day in 2 doses in the morning and evening, which is the maximum dose for adults. If Sergolin is used at a dose of 30 mg once a day, it should be taken in the morning. The effect appears only after prolonged therapy, so the course of treatment with Sergolin should be long. The results of treatment are usually evaluated once every 6 months – at the end of this period, the doctor must decide on the advisability of further treatment. Elderly patients do not need dose adjustment. Reducing the dose of the drug is recommended for patients with impaired renal function. Tablets are taken before meals, without chewing, with a sufficient amount of liquid. If there are problems with digestion, the tablets can be taken with meals.

Contraindications:

hypersensitivity to the active substance or any other component of the drug, porphyria. Acute bleeding, recent myocardial infarction, severe bradycardia (heart rate <50 bpm), severe hypotension, exertional angina, severe atherosclerosis, childhood, pregnancy and lactation.

Side effects:

Most side effects are mild and temporary. Possible sensations of heartburn, skin flushing, dry mouth, fatigue, apathy, dizziness, tinnitus, headache, sleep disorders, gastrointestinal dysfunction (nausea, vomiting, diarrhea, constipation, abdominal pain), nervousness, anxiety, tachycardia , orthostatic disorders, nasal congestion, ejaculation disorders and increased levels of uric acid in the blood.

Special instructions:

the drug contains lactose, so it should not be taken by patients with congenital galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome. For the period of treatment, it is necessary to exclude the use of alcohol. Special security measures. The benefit/risk ratio of treatment should be considered for patients with cardiac arrhythmia or hyperuricemia, patients who have been treated for gout in the past or are currently receiving drugs that inhibit the metabolism and excretion of uric acid (loop diuretics, thiazide diuretics, amiloride, theophylline , cyclosporine, pyrazinamide, ethambutol, streptomycin, isotretinoin, ketoconazole, levodopa, cisplatin, cyclophosphamide, vincristine, salicylates, etc.). Pregnancy or lactation. The use of Sergolin during pregnancy is contraindicated due to insufficient experience with nicergoline treatment during this period. Nicergoline passes into breast milk. Therefore, the drug should not be taken during breastfeeding due to the possibility of developing severe side effects. Children. The safety and efficacy of treatment with Sergolin in children has not been established, therefore it should not be used in patients of this age group. The ability to influence the reaction rate when driving vehicles or working with mechanisms. No impact study was conducted. The drug can cause dizziness and increased fatigue, therefore, for the duration of treatment, you should refrain from driving vehicles and working with other mechanisms.

Interactions:

Nicergoline enhances the effect of oral anticoagulant and antihypertensive agents. It should not be used simultaneously with ?- and ?-adrenergic receptor blockers. Combined use with sympathomimetics can lead to significant fluctuations in blood pressure. Nicergoline is metabolized by CYP 2D6, therefore, interactions with drugs that are metabolized in the same way cannot be excluded: painkillers – phenacetin, methadone, morphine, oxycodone, pethidine, tramadol; anorexigenic drugs – dexfenfluramine, fenfluramine; antiarrhythmic drugs – amiodarone, encainide, flecainide, quinidine, mexiletine, propafenone; antidepressants – amitriptyline, bupropion, citalopram, desipramine, doxepin, escitalopram, fluoxetine, fluvoxamine, imipramine, clomipramine, maprotiline, moclobemide, minaprine, nortriptyline, paroxetine, sertraline, trazodone, venlafaxine; antiemetics – metoclopramide, ondansetron; anti-inflammatory drugs – celecoxib; antihistamines – chlorpheniramine; antihypertensive agents – alprenolol, bisoprolol, bufuralol, captopril, carvedilol, debrisoquine, metoprolol, prehexilin, propranolol, mibefradil; anticoagulants – ticlopidine; antimalarials – halofantrine; antifungals – terbinafine; antitussives – dextromethorphan, hydrocodone, codeine; antiulcer drugs – cimetidine, ranitidine; antivirals – ritonavir; cytostatics – doxorubicin, tamoxifen; local anesthetics – lidocaine; muscle relaxants – cyclobenzaprine; neuroleptics – fluphenazine, haloperidol, chlorpromazine, clozapine, levomepromazine, perphenazine, risperidone, thioridazine; thymol – in the form of eye drops; oral hypoglycemic agents – phenformin; psychostimulants – donepezil and others. The hypotensive effect of nicergoline is enhanced by alcohol.

Overdose:

arterial hypotension. There is no specific antidote. Treatment is symptomatic.

Storage conditions:

below 25°C.

Sergolin analogues:

Serotonin-norepinephrine-dopamine reuptake inhibitor

Serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI ) also known as Triple Reuptake Inhibitor ( TRI ), is a type of drug , which acts as a combined reuptake inhibitor of the monoamine neurotransmitters serotonin, norepinephrine, and dopamine. It does this by simultaneously inhibiting the serotonin transporter (SERT), the norepinephrine transporter (NET), and the dopamine transporter (DAT), respectively. Inhibition of reuptake from these neurotransmitters increases their extracellular concentration and therefore leads to an increase in serotonergic, adrenergic and dopaminergic neurotransmission. The natural and potent cocaine SNDRI is widely used recreationally and often illegally due to its euphoric effect.

Other SNDRIs have been developed as potential antidepressants and treatments for other disorders such as obesity, cocaine addiction, attention deficit hyperactivity disorder (ADHD), and chronic pain. They are an extension of selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs), with the addition of a dopaminergic action thought to increase the therapeutic effect. However, increased side effects and potential for abuse are potential issues with these agents compared to their SSRI and SNRI counterparts.

SNDRIs are similar to non-selective monoamine oxidase inhibitors (MAOIs) such as phenelzine and tranylcypromine in that they increase the action of all three major monoamine neurotransmitters. They are also similar to serotonin-norepinephrine-dopamine (SNDRA) releasing agents such as MDMA (ecstasy) and α-ethyltryptamine (αET) for the same reason, although they act by a different mechanism and have different physiological and qualitative effects. .

Although their primary mechanism of action is that they are NMDA receptor antagonists, ketamine and phencyclidine are also SNDRIs and also occur as addictive drugs.

Major depressive disorder (MDD) is the main reason for the development of the SNDRI. ^{[1] [2] [3] [4] [5] [6] [7] [8]} 9 0147 [9] ^[10] According to the World Health Organization, depression is the leading cause of disability and the fourth leading cause of disability. global burden of disease in 2000. By 2020, depression is projected to be the 2nd largest DALY. ^[11]

It is estimated that about 16% of the population suffers from major depression and another 1% suffers from bipolar disorder one or more times during a person’s life.