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Buspirone what is it. Comprehensive Guide to Buspirone: Uses, Side Effects, and More

What is buspirone? How does it work? What are the potential side effects of taking buspirone? Discover the answers to these and more in our detailed guide.

Understanding Buspirone: An Overview

Buspirone is an anxiolytic medication primarily used to treat anxiety disorders. It works by modulating the activity of serotonin, a neurotransmitter in the brain that plays a crucial role in regulating mood, emotions, and behavior. Unlike benzodiazepines, which provide immediate relief but carry the risk of dependence and withdrawal, buspirone is considered a non-addictive alternative for managing anxiety.

Buspirone: Approved Uses and Indications

Buspirone is FDA-approved for the treatment of generalized anxiety disorder (GAD). It has also been used off-label for other conditions, such as:

  • Anxiety associated with depression
  • Premenstrual syndrome (PMS)
  • Alcohol withdrawal
  • Nicotine withdrawal
  • Irritable bowel syndrome (IBS)

However, it’s important to note that the use of buspirone for these off-label indications is considered an “unlabeled” or “unapproved” use, and healthcare providers should carefully weigh the risks and benefits before prescribing it for these conditions.

Mechanism of Action: How Does Buspirone Work?

Buspirone is classified as a serotonin 1A (5-HT1A) receptor agonist. It works by binding to and activating these receptors, which are primarily found in the limbic system and raphe nuclei of the brain. This interaction leads to a modulation of serotonin neurotransmission, which can help reduce anxiety and improve mood.

Unlike benzodiazepines, which work by enhancing the effects of gamma-aminobutyric acid (GABA), buspirone does not have a direct effect on the GABA system. This unique mechanism of action contributes to its non-addictive properties and reduced risk of dependence and withdrawal symptoms compared to benzodiazepines.

Buspirone Dosage and Administration

Buspirone is available in various tablet strengths, including 5 mg, 7.5 mg, 10 mg, 15 mg, and 30 mg. The typical starting dose for the treatment of anxiety is 7.5 mg taken three times daily. The dosage may be gradually increased based on the patient’s response and tolerance, up to a maximum of 60 mg per day, typically divided into three or four doses.

It’s important to note that buspirone may take several weeks to achieve its full therapeutic effect, and patients should be advised to continue taking the medication as prescribed, even if they don’t feel immediate relief.

Potential Side Effects of Buspirone

Buspirone is generally well-tolerated, but like any medication, it can cause side effects. Some of the most common side effects associated with buspirone include:

  • Dizziness
  • Headache
  • Nausea
  • Nervousness
  • Lightheadedness
  • Insomnia

These side effects are often mild and tend to improve over time as the body adjusts to the medication. Patients should report any persistent or severe side effects to their healthcare provider.

Interactions and Contraindications

Buspirone may interact with certain medications, including:

  • Antidepressants (e.g., fluoxetine, paroxetine)
  • Antifungal medications (e.g., itraconazole, ketoconazole)
  • Antibiotics (e.g., erythromycin, clarithromycin)
  • Antiseizure drugs (e.g., phenytoin, carbamazepine)

Patients should inform their healthcare provider about all medications they are taking, including over-the-counter drugs, supplements, and herbal products, to ensure that buspirone is safe and appropriate for their individual circumstances.

Buspirone is generally not recommended for use in pregnant or breastfeeding women, as the potential risks to the developing fetus or nursing infant are not fully understood.

Transitioning from Benzodiazepines to Buspirone

For patients who are switching from benzodiazepines to buspirone, it’s important to work closely with their healthcare provider to ensure a safe and gradual transition. Abruptly stopping benzodiazepines can lead to withdrawal symptoms, so the healthcare provider may recommend a tapering schedule to gradually reduce the benzodiazepine dose while introducing buspirone.

During this transition period, patients may experience increased anxiety or other withdrawal symptoms, and close monitoring by the healthcare provider is essential to manage these effects and ensure a successful transition.

Buspirone Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

buspirone 10 mg tablet

Color: whiteShape: barrelImprint: Logo and 91

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 5 mg tablet

Color: whiteShape: barrelImprint: Logo and 79

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 15 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 15 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

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buspirone 5 mg tablet

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buspirone 5 mg tablet

Color: whiteShape: roundImprint: 091 logo

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buspirone 15 mg tablet

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buspirone 30 mg tablet

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buspirone 30 mg tablet

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buspirone 7.5 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 10 mg tablet

Color: whiteShape: rectangularImprint: 10

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buspirone 15 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 10 mg tablet

Color: whiteShape: rectangular (rounded end)Imprint: B 3

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 15 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 5 mg tablet

Color: whiteShape: rectangularImprint: 5

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 15 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 5 mg tablet

Color: whiteShape: rectangular (rounded end)Imprint: B 1

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 10 mg tablet

Color: whiteShape: roundImprint: 092 logo

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 15 mg tablet

Color: whiteShape: rectangularImprint: A 0 5 5 5

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 10 mg tablet

Color: whiteShape: roundImprint: AA 65

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buspirone 10 mg tablet

Color: whiteShape: ovalImprint: WAT SON 658

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 30 mg tablet

Color: whiteShape: oblongImprint: Y 54

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 15 mg tablet

Color: whiteShape: oblongImprint: 1 00 5 5 5

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 7.5 mg tablet

Color: whiteShape: oblongImprint: 107

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buspirone 5 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 10 mg tablet

Color: whiteShape: oblongImprint: ZE 37

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 30 mg tablet

Color: whiteShape: rectangularImprint: U 247

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 10 mg tablet

Color: whiteShape: roundImprint: 245 U U

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 5 mg tablet

Color: whiteShape: roundImprint: 244 U U

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 5 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 30 mg tablet

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buspirone 15 mg tablet

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buspirone 7.5 mg tablet

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buspirone 7.5 mg tablet

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buspirone 10 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 7.5 mg tablet

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buspirone 30 mg tablet

Color: whiteShape: oblongImprint: 10 10 10 ZE 39

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buspirone 10 mg tablet

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buspirone 7.5 mg tablet

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buspirone 15 mg tablet

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buspirone 7.5 mg tablet

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buspirone 7.5 mg tablet

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buspirone 10 mg tablet

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buspirone 10 mg tablet

Color: whiteShape: roundImprint: TEVA 54

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buspirone 15 mg tablet

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This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 10 mg tablet

Color: whiteShape: roundImprint: logo and 84

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 7.5 mg tablet

Color: whiteShape: ovalImprint: AA 64

This medicine is a white, barrel, scored, tablet imprinted with “Logo and 91”.

buspirone 30 mg tablet

Color: whiteShape: oblongImprint: 1 01 10 10 10

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buspirone 5 mg tablet

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Buspar (buspirone): Side effects, dosage, uses

Buspar is a discontinued brand name version of the drug buspirone, which treats anxiety. Although Buspar is no longer available on the market, people can instead take the generic form, which is chemically identical. A person should only take buspirone as their doctor directs, as it can have side effects.

Buspirone may help individuals with anxiety feel more relaxed, think more clearly, and worry less. The medication may also help with feelings of irritability and other anxiety-related symptoms, such as an increased heartbeat, sweating, and difficulty sleeping.

The Food and Drug Administration (FDA) approved Buspar for the treatment of generalized anxiety disorder (GAD) in 1986. A doctor can diagnose a person with GAD if they have been experiencing excessive anxiety and worry on most days over a period of at least 6 months.

Although Buspar is no longer available, the FDA confirmed that its withdrawal from the market was not due to concerns regarding safety or effectiveness.

In this article, we provide more information on buspirone, including how to take it, common side effects, and whether it can make anxiety worse.

Buspirone belongs to a class of medications called anxiolytics, or anti-anxiety medications. Doctors prescribe it to treat symptoms of anxiety disorders or the disorders themselves in the short term.

Buspirone works by changing the amounts of certain natural substances in the brain. It is not an antidepressant, but older research suggests that it may enhance the action of antidepressant medication.

The drug does not have a link to other anti-anxiety medications, such as barbiturates or benzodiazepines.

People take buspirone by mouth, usually in tablet form, and they will generally need to take it twice a day. Although a person can take the drug with or without food, they should be consistent across doses and take it the same way each time.

It is important to take buspirone according to the instructions on the label and as a doctor has directed. A person should not take buspirone more or less often than their prescription states.

A doctor may start a person on a low dosage of buspirone and gradually increase it. It may take several weeks to determine the most effective dosage for a person.

The National Alliance on Mental Illness notes that a person should not operate heavy machinery or drive a vehicle until they know how the medication affects them, as it may cause dizziness or tiredness. They should also avoid the use of alcohol, which can increase these symptoms.

It may take 3–4 weeks before a person starts to feel the benefits of buspirone, so they should not stop taking the medication without speaking with their doctor first.

If a person misses a dose, they should take it as soon as they remember. However, if it is almost time for the next dose, they should skip the missed dose and continue with their regular schedule. A person should not double dose to make up for a missed tablet.

Buspirone may cause several side effects. A person should speak with their doctor if the symptoms do not go away or are severe. Side effects can include:

  • headaches
  • dizziness
  • nausea
  • confusion
  • diarrhea
  • fatigue
  • nervousness
  • weakness
  • increased sweating
  • difficulty falling or staying asleep
  • excitement
  • feelings of anger or hostility
  • lightheadedness
  • numbness

Certain side effects can be serious, and they may sometimes be cause for concern. A person should speak with their doctor if they experience:

  • swelling by the mouth, throat, lips, tongue, or eyes
  • a rash
  • itching
  • a fast or irregular heartbeat
  • blurred vision
  • uncontrollable shaking
  • hives
  • agitation
  • fever
  • severe muscle stiffness or twitching
  • hallucinations
  • loss of coordination
  • vomiting

A person needs to take buspirone continuously for several weeks for it to be fully effective.

If a person misses doses or abruptly stops taking the medication without consulting a doctor, they may feel more anxious.

There are no known problems associated with the long-term use of buspirone, and doctors consider it a safe and effective medication when a person uses it according to their prescription.

A person should seek immediate medical care if they or someone else has overdosed on buspirone.

It is also essential to call 911 immediately if a person:

  • has collapsed
  • is having trouble breathing
  • has had a seizure
  • is unresponsive to attempts to wake them

If someone has chest pain, changes in blood pressure, fainting, or muscle cramps, they should see a doctor as soon as possible. A person should also contact their doctor if they experience any serious or persistent side effects or notice symptoms of an allergic reaction. These symptoms might include swelling in the face or throat.

It is advisable for people to discuss all other medications that they are taking with their doctor, as certain medications, such as monoamine oxidase inhibitors, may interact with buspirone.

People should also seek medical advice before taking buspirone when pregnant or breastfeeding, as the drug may carry potential risks for them or the baby.

Buspar is a discontinued branded version of buspirone, an anxiolytic medication that treats anxiety disorders.

A person may need to take buspirone for 3–4 weeks before they feel the benefits of it. They should not stop taking the medication without consulting a professional.

Common side effects of the drug include headaches, fatigue, dizziness, and nausea. Serious side effects may include a rash, hallucinations, uncontrollable shaking, and swelling around the mouth, throat, or eyes.

A person should contact a doctor if they overdose on buspirone or experience serious or persistent side effects or an allergic reaction.

Buspirone does not generally make anxiety worse, but missing doses or abruptly stopping the medication may have adverse effects.

Buspiron instructions, price in pharmacies of Ukraine

Dosage

  • Buspirone: 5 mg/tablet (1)
  • Buspirone: 10 mg/tablet (1)

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Creation date: 04/27/2021
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  • tab. 5 mg blister, № 20
  • Buspirone 5 mg
  • tab. 10 mg blister, № 20
  • Buspirone 10 mg

Pharmacological activity

Pharmacodynamics. Buspirone – an anxiolytic drug zasib, zastosovyatsya for exaltation of anxious states of various walks, especially neuroses, which are accompanied by feelings of anxiety, restlessness, tension, drama. The mechanism of action of buspirone has not been established, but it is known that it is responsible for the mechanism of action of benzodiazepines and other anxiolytic effects.

Buspirone is highly potent as a presynaptic 5HT1A receptor and as a frequent agonist of postsynaptic 5HT1A receptors in the CNS. In preclinical studies, experimental models showed that buspiron had powers characteristic of anxiolytics and antidepressants. In the presence of benzodiazepines, buspirone does not show anticonvulsant and muscle relaxant effects, does not cause a chirp, and after completion of the course of treatment, no symptoms develop. Diya buspironu develop step by step. The therapeutic effect begins to appear between the 7th and 14th days of therapy, and the maximum effect is reached only after about 4 days after the cob of treatment.

Pharmacokinetics. After ingestion, the preparation is fast and may be absorbed again from the intestinal tract. Equally important plasma concentrations may be reached after approximately 2 doses after the cob of regular ingestion of the drug.

Buspirone is subject to intensive first pass metabolism through the liver. Systemic bioavailability to become 4%. Cmax of drug metabolism in blood plasma is also reached after 60-90 minutes.

close 9Buspirone 5% binds to plasma proteins. T½ of blood plasma becomes 2-3 years. Pharmacological parameters of the drug do not change when taking the drug without interruption (cumulative daily).

The main pharmacologically active metabolite of buspiron is (1-[2-pyrimidinil]-piperazine (1-PP). qia in blood plasma more i T½ in

Approximately 29-63% of buspirone and its metabolites are excreted in the stool for 24 years, 18-38% are excreted in the feces. spirone and yoga metabolites are reduced

Indications

symptomatic relief of anxiety states with dominant symptoms: anxiety, internal restlessness, stress state.

Dosing

doses are determined by the drug individually for the skin patient in case of illness. On the cob of therapy, 5 mg of buspiron hydrochloride is prescribed 2-3 times a day. To achieve the maximum therapeutic effect, the additional dose should be incrementally increased to 15-30 mg of buspirone, subdivided into five doses.

The maximum single dose should not exceed 30 mg.

The maximum supplementary dose should not exceed 45 mg.

Tablets should be taken at the same time, dobi, not rotting, drinking a small amount of rind, directly from the patient.

If necessary, place the tablet half-and-half in two halves on a hard surface with the risk of burning and press lightly with your thumb.

Special patient groups. With a decrease in the function of the liver, one / the user should stop the minimum possible dose.

Trivality of glee. Tranquilizers cannot be stopped without control over a prolonged period. If it is necessary to administer the drug (≤6 mіs), then further medical monitoring should be carried out. Next memory about the conduct of psychotherapeutic and sociotherapeutic visits in parallel with the treatment of buspirone.

Contraindications

increased sensitivity to Buspirone or to one of the components of the drug; gostra congestive glaucoma; malignant mastonia; important dysfunction of the liver; heavy nirkov deficiency; epilepsy; period of breastfeeding; century to 18 years.

Side effects

from the side of the cardiovascular system: often – non-specific pain in the chest; inodі – timchasova vtrata svіdomosti, arterial hypotension and/or hypertension, tachycardia / apparently heartbeat; rarely – damage to cerebral circulation, heart failure, myocardial infarction, cardiomyopathy, bradycardia.

On the side of the blood system: rarely – changes in blood tests (eosinophilia, leukopenia, thrombocytopenia).

On the side of the psyche: often – nightmares, drowsiness, sleeplessness, confusion, nervousness, decreased concentration of respect, emotional agitation, drastically, divination, confusion, depression; rarely – depersonalization, discomfort, pathological spontaneity of loud sounds, euphoria, hyperkinesia, restlessness, impaired associative spontaneity, hallucinations, suicidal thoughts, epileptic attacks; rіdko – sharp change in mood, claustrophobia, stupor, unrecognizable language, psychosis, problems to go through memory, serotonin syndrome.

From the side of the central nervous system: sometimes – names, paresthesia (for example, shaking, feeling pain), impaired coordination, tremor; Rarely, spontaneous collapse, galvanism, extrapyramidal symptoms, including early and late dyskinesia, impaired tone, parkinsonism, akathisia.

On the side of the organ: often – cloudy eyes; inodі – chervonіnnya i sverbіzh in the region of eyes, conjunctivitis; rіdko – photophobia, vіdchuttya vnutrіshnoochnogo vice, bіl in the eyes, the field of dawn sounded.

To the side of the hearing organ: often – noise in the ears.

On the side of the dichal system: often – sore throat, stuffy nose; inodi – sooner dihannya, zadishka, bіl in the region of the heart; rarely – nose bleeding.

From the side of the intestinal tract: often – nudity, xerostomia, epigastric dilatation, diarrhea; sometimes – flatulence, loss of appetite, increased appetite, hypersalivation, colon teasing syndrome, bleeding from the rectum, constipation, vomiting.

On the side of the slitting system: sometimes – often slashing, cutting slitting; rarely – enuresis, no sechoviprosy.

To the side of the coats: sometimes – swelling, croup, hyperemia, hematomas, oblisinnya, dryness of the coats, eczema, swelling, swelling; rarely – allergic reactions, ecchymosis, acne, thinning of the nails.

To the side of the musculoskeletal apparatus: sometimes – spasm and stiffness of the tongue, myalgia, arthralgia; rarely – myasthenia.

On the side of the endocrine system: rarely – galactorrhea, gynecomastia, dysfunction of the thyroid gland.

Head injuries: often – headache, asthenia; inodі – zbіlshennya masi tіla, fever, zvіn na golovі, zmenshennya masi tіla, unsickness, increased stomlyuvanіst, impaired scent and gustatory smells, increased sweating, hot flushes, cold hyperesthesia; rarely – skhilnist to malice with alcohol, blood coagulation disorder, loss of voice, hooting, glossalgia.

From the side of the hepatobiliary system: rarely – an increase in liver enzymes.

On the side of the reproductive system: sometimes – disruption of the menstrual cycle, change or increase in libido; rarely – amenorrhea, inflammation of the secretory organs, decreased ejaculation, impotence.

Particular indications ovanim.

Buspirone is not indicated for the treatment of withdrawal symptoms, benzodiazepine congestion, or other sedative/sedative drug conditions. That is why it is necessary to step-by-step administer the injection of these preparations to the cob with buspirone. This is especially important for patients, for example, they take medications that detract from the central nervous system. Do not prescribe buspirone to patients with a history of epilepsy attacks.

We are ill with impaired functions of the liver and liver in history.

Buspiron Sandoz is lactose-resistant, which has not been reported in patients with mild galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

Congestion during pregnancy and breastfeeding. Given the ingestion of buspirone during the period of pregnancy during the day, the drug can only be considered in that period, if the measles for the mother is cited, it outweighs the potential risk for the fetus. Buspirone penetrates into breast milk;

Children. Do not administer buspirone to children due to the lack of safety and efficacy.

The ability to increase the speed of the reaction when caring for vehicles or robots with other mechanisms. The hour of leniency should be minimized by transport means or by other mechanisms, shards can lead to side reactions from the side of the central nervous system and psyche.

Interaction

in connection with the lack of good clinical data on the recent congestion of buspirone with antihypertensive, neuroleptic drugs, antidepressants, antidiabetic drugs, anticoagulant ntami, oral contraceptives and cardiac glycosides can only be used in the minds of suvoromedical control. Buspirone GEXAL ® should not be co-administered with benzodiazepines and other sedative drugs.

Combination with MAO inhibitors is not recommended in conjunction with the risk of hypertensive crisis.

Oxils of buspirone are primarily metabolized by cytochrome P450, inhibition of the inhibitory enzyme may increase the bioavailability of buspirone.

Nefazodon. One-hour ingestion of buspirone and nefazodone to increase Cmax of buspirone in blood plasma by 20 times and AUC by 50 times.

Erythromycin. One-hour ingestion of buspirone and erythromycin can lead to an increase in Cmax of buspirone by 5 times and AUC by 6 times.

Itraconazole. Overnight administration of buspirone and itraconazole resulted in a 13-fold increase in buspirone Cmax and 19-fold increase in AUCrazіv.

Diltiazem. One-hour infusion of buspirone and diltiazem leads to an increase in Cmax of buspirone by 4 times and AUC by 5.3 times.

Verapamil. An overnight dose of buspirone and verapamil should result in a 3. 4-fold increase in Cmax and AUC for buspirone.

Cimetidine. Odnochasno zastosuvanya buspirone and cimetidine lead to an increase in the Cmax of buspirone by 40%, Tmax – 2 times, but the AUC practically does not change.

If buspirone is ingested at the same time due to medical advice, the therapeutic effect and toxicity of buspirone increase, so it is recommended to reduce the dose of buspirone (for example, 2.5 mg 2 times per dose).

Rifampicin. An overnight dose of buspirone and rifampicin should result in a change in Cmax for buspirone by 83.9% and AUC by 89.6%.

Inhibitor and inducer of CYP 3A4. Ketoconazole and ritonavir inhibit the metabolism of buspiron and increase blood plasma levels. If buspirone is administered concomitantly with a CYP 3A4 inhibitor, a lower dose is recommended. CYP 3A4 inducers, such as dexamethasone, phenytoin, phenobarbital, or carbamazepine, may increase the metabolic rate of buspiron. In this case, it is necessary to increase the dose of buspirone to preserve its anxiolytic efficacy.

Serotonin ingestion inhibitor. In clinical studies, there was no relapse of unsafe ingestion of buspirone concomitantly with antidepressants, selective serotonin ingestion inhibitors. Boulli okremі vodomlennya pro viniknennya podadіv ї їkh trivalno zastosuvanni podednanny z buspironom.

Haloperidol. Overnight exposure to buspirone and haloperidol led to an increase in the concentration of haloperidol in the blood serum.

Trazodone. It was reported that in some patients with one-hour ingestion of trazodone with buspirone, AST activity increased by 3 times. However, such an increase in hepatic transaminases has not been confirmed by clinical evidence.

Diazepam. With one-hour instillation of diazepam and buspiron, rhubarb in the blood plasma rises, and can also cause side effects: confusion, headache, boredom.

The first hour of drinking with buspirone will soon disappear from the introduction of alcoholic drinks.

It is not recommended for patients to drink grapefruit juice in significant quantities, but it can lead to an increase in the level of buspiron in the blood plasma to an increase in the frequency or severity of side effects .

Overdose

Symptoms: nausea, vomiting, constipation, exhaustion, miosis and dysfunction of the mucosal-intestinal tract. More important complications in humans have not been reported with daily doses up to 2400 mg.

Likuvania is more symptomatic; flushing of the hose. As in times of overdosing with other medications, it is necessary to monitor the functions of the dichal system, heart rate and AT. Specific antidote daily. Hemodialysis is not effective.

Wash off

at temperatures below 25 °C.

Buspirone Instructions

BUSPIRONE SANDOS®
(UA/9598/01/01)

Release form:

5 mg tablets; 10 tablets in a blister; 2 blisters in a cardboard box; 20 tablets in a blister; 1 blister in a cardboard box

Stock:

1 tablet vengeance buspirone hydrochloride 5 mg

Manufacturer:

Nіmechchina

BUSPIRONE SANDOS®
(UA/9598/01/02)

Release form:

10 mg tablets; 10 tablets in a blister; 2 blisters in a cardboard box

Stock:

1 tablet vengeance buspirone hydrochloride 10 mg

Manufacturer:

Nіmechchina

Buspirone price in Pharmacy 911

Name Price
Buspirone tab. 10mg tab №20 305.60 UAH
Buspirone tab. 5mg pack №20 UAH 211.00

Buspirone Sandoz tab. 10mg №20

The appearance of the product may differ from that shown in the photo

International nonproprietary name: buspirone

Dosage form: tablets

Composition: 5 mg or 10 mg of buspirone hydrochloride in each tablet. Excipients: lactose monohydrate (55.7 mg in tablets of 5 mg and 111.4 mg in tablets of 10 mg), microcrystalline cellulose, sodium carboxymethyl starch, magnesium stearate, silica colloidal anhydrous

Description : Tablets 5 mg: White or almost white, round, flat tablets with a bevel, engraved with “E 151” on one side and with a score on the other side; odorless or with a slight characteristic odor. Tablets 10 mg: White or almost white, round, flat tablets with a bevel, engraved with “E 152” on one side and with a notch on the other side; odorless or with a slight characteristic odor.

Pharmacotherapeutic group: Anxiolytic agent (tranquilizer). ATX code: N05B E01

Pharmacodynamics.
Anxiolytic (tranquilizing) agent of the non-benzodiazepine series, also has an antidepressant effect. Unlike classical anxiolytics, it does not have antiepileptic, sedative, hypnotic and muscle relaxant effects.
The mechanism of action is associated with the effect of buspirone on the serotonergic and dopaminergic systems. Selectively blocks presynaptic dopamine receptors and increases the rate of excitation of dopamine neurons in the midbrain. In addition, buspirone is a selective partial agonist of 5-HT1A serotonin receptors. Buspirone does not have a significant effect on benzodiazepine receptors and does not affect the binding of GABA, does not have a negative effect on psychomotor functions, does not cause tolerance, drug dependence and “withdrawal” syndrome. Does not potentiate the effect of alcohol. According to anxiolytic activity, buspirone is approximately equal to benzodiazepines. The therapeutic effect develops gradually and is observed after 7-14 days from the start of treatment, the maximum effect is recorded after 4 weeks.

Pharmacokinetics.
After oral administration, buspirone is rapidly and almost completely absorbed from the gastrointestinal tract. Buspirone undergoes extensive first pass metabolism through the liver. Therefore, the unchanged substance is found in the systemic circulation in a small concentration, which has significant individual differences.
Bioavailability is 4%. The maximum plasma concentration is reached 60-90 minutes after taking the drug. In healthy volunteers, buspirone had a linear (dose-proportional) pharmacokinetics after administration of 10-40 mg. Similar pharmacokinetic parameters were found in elderly patients. After a single oral dose of 20 mg of the drug, its plasma levels range from 1 to 6 ng / ml. Approximately 95% of buspirone binds to plasma proteins (86% to plasma albumin, the rest to a1-acid glycoprotein). Buspirone undergoes oxidative metabolism mainly with the participation of CYP3A4 isoenzymes. Various hydroxylated metabolites are formed. The main metabolite (5-OH-buspirone) is not active. The dealkylated metabolite (1-(2-pyrimidinyl)-piperazine, 1-PP) is active. Its anxiolytic activity is 4-5 times lower than that of the parent substance, but its plasma level is higher and the half-life is approximately 2 times longer than that of buspirone. After a single injection of 14C-labeled buspirone 29-63% of the radioactivity is excreted in the urine within 24 hours, mainly in the form of metabolites. Approximately 18-38% of the administered dose is excreted in the feces. After a single dose of 10-40 mg, the half-life of the parent substance is approximately 2-3 hours, and the half-life of the active metabolite is 4.8 hours.
Simultaneous ingestion of food slows down the absorption of buspirone, but due to a decrease in pre-systemic clearance (first pass effect), the bioavailability of buspirone is significantly increased. After taking with food, the AUC value of buspirone increases by 84%, and its Cmax increases by 16%.
Steady-state plasma concentration can be reached approximately 2 days after the start of regular intake.
The apparent volume of distribution is 5.3 l/kg.
Buspirone is excreted in breast milk, but data on placental transmission are not available.
Elevated plasma levels of buspirone and AUC values, as well as a prolongation of the half-life, may be observed with impaired liver function. In connection with the release of unchanged substance into the bile, a second peak in the concentration of buspirone in the blood plasma is possible. Patients with cirrhosis of the liver should be prescribed the drug at lower doses or at the same doses at longer intervals. In renal insufficiency, the clearance of buspirone can be reduced by 50%. In renal insufficiency, buspirone should be administered with caution and at reduced doses. The pharmacokinetics of buspirone in elderly patients is not changed.

Indications for use

  • Generalized anxiety disorder (GAD).
  • Panic disorder.
  • Autonomic dysfunction syndrome.
  • Alcohol withdrawal syndrome (as adjuvant therapy)
  • Adjuvant therapy of depressive disorders (the drug is not prescribed for monotherapy of depression).

Contraindications

  • Hypersensitivity to any component of the drug.
  • Severe renal failure (GFR below 10 ml/min).
  • Severe liver failure (PT more than 18 seconds).
  • Simultaneous use of MAO inhibitors or 14 days after discontinuation of an irreversible MAO inhibitor or 1 day after discontinuation of a reversible MAO inhibitor.
  • Glaucoma
  • Myasthenia gravis
  • Age up to 18 years (the safety and efficacy of buspirone in this age group has not been proven).
  • Lactation
  • Pregnancy or suspected pregnancy

Precautions: cirrhosis of the liver, renal failure (see section “Special instructions”).

Pregnancy and lactation

Due to the lack of adequately controlled data from clinical studies, the use of buspirone during pregnancy is possible only if the benefit of the drug justifies the possible risks. Women of childbearing age should use adequate contraceptive methods during the course of treatment with buspirone, since the safety of buspirone during pregnancy has not been proven.

Buspirone is excreted in breast milk. Sufficient data from clinical studies of the use of buspirone during breastfeeding are not available, so breastfeeding mothers are not recommended to take this drug.

Method of administration and doses

Tablets should always be taken at the same time of the day, before or after meals, in order to avoid significant fluctuations in the concentration of the active substance in the blood plasma throughout the day.

The drug should not be taken episodically for the treatment of anxiety, since the therapeutic effect of the drug develops only after repeated administration and does not appear earlier than after 7 – 14 days of treatment.

The dose must be adjusted for each patient individually. Recommended starting dose is 15 mg; it can be increased by 5 mg per day every 2 or 3 days. The daily dose should be divided into 2-3 doses. The usual daily dose is 20 – 30 mg per day. The maximum single dose is 30 mg; the maximum daily dose should not exceed 60 mg.

Special groups:

Elderly patients: By itself, advanced age does not require dose adjustment, since the pharmacokinetics of buspirone does not undergo age-related changes.

Impaired renal function: In case of impaired renal function, the drug should be used with caution and in reduced doses.

Impaired liver function: In case of impaired liver function, the drug should be used with caution and at reduced doses, for which the individual doses are reduced or the interval between doses is increased.

Side effects

Buspirone is generally well tolerated. Side effects, if they are observed, usually occur at the beginning of the course of treatment and then disappear, despite continued use of the drug. In some cases, a dose reduction is necessary.

Common side effects – at a frequency of 1/100, infrequent at a frequency of 1/100 to 1/1000 and rare at a frequency of less than 1/1000 .

Cardiovascular system:

Frequent: chest pain.
Uncommon: syncope, hypotension, hypertension.
Rare: cerebrovascular accident, decompensated heart failure, myocardial infarction, myocardiopathy, bradycardia.

Central nervous system:

Frequent: dizziness, headache, irritability, sleep disturbances.

Uncommon: dysphoric reactions, depersonalization, dysphoria, increased sensitivity to noise, euphoria, hyperkinesis, fear, apathy, hallucinations, confusion, prolongation of reaction time, suicidal thoughts, epileptic seizures, paresthesia, incoordination, tremor.

Rare: claustrophobia, cold intolerance, stupor, stuttering, extrapyramidal disorders, psychotic disorders.

Ophthalmic and otorhinolaryngological:

Frequent: tinnitus, laryngitis, swelling of the nasal mucosa.

Infrequent: blurred vision, itching in the eyes, redness of the eyes, conjunctivitis, impaired taste and smell.

Rare: inner ear disorders, eye pain, photophobia, increased intraocular pressure.

Endocrine:

Rare: galactorrhea and thyroid disease.

Gastrointestinal:

Uncommon: nausea, flatulence, anorexia, increased appetite, salivation, intestinal bleeding.

Rare: diarrhoea, burning tongue.

Genitourinary system:

Uncommon: dysuric disorders (including frequent urination, urinary retention), menstrual disorders, sexual desire disorders.

Rare: amenorrhea, pelvic inflammatory disease, bedwetting, delayed ejaculation, impotence.

Musculoskeletal:

Uncommon: muscle spasms, muscle stiffness, arthralgia.

Rare: muscle weakness.

From the side of the respiratory system:

Infrequent: hyperventilation, lack of air, a feeling of heaviness in the chest.

Rare: epistaxis.

Skin:

Infrequent: swelling, itching, flushing, hair loss, dry skin, swelling of the face, skin fragility, rash.

Others : Weight gain, fever, weight loss, muscle and bone pain.

Rare: alcohol abuse, loss of voice, tinnitus, hiccups.

Laboratory changes:

Uncommon: Increased serum ALT and AST levels.

Rare: eosinophilia, leukopenia, thrombocytopenia.

Overdose

Symptoms: gastrointestinal disorders, nausea, vomiting, dizziness and drowsiness (also in severe forms), depression of consciousness of varying severity.

Treatment: Gastric lavage and symptomatic therapy. No specific antidote is known, dialysis is ineffective.

Experience to date suggests that even extremely high doses (single oral dose of 375 mg) do not necessarily cause severe symptoms.

Special instructions and precautions for use.

Liver failure: Buspirone is extensively metabolized by the liver. A single administration of 30 mg to patients with cirrhosis of the liver increases the levels of buspirone in blood plasma and increases the AUC with a prolongation of the half-life of the drug. In connection with the release of unchanged substance into the bile, a second peak in the concentration of buspirone in the blood plasma is possible. The drug is contraindicated in patients with severe hepatic impairment. Patients with cirrhosis of the liver should be prescribed the drug at lower doses or at the same doses at longer intervals.

Renal insufficiency: In moderate or severe renal insufficiency, the clearance of buspirone may be reduced by 50%. The drug is contraindicated in patients with severe renal insufficiency with GFR less than 10 ml/min. In mild (GFR over 30 ml/min) and moderate (GFR 10-30 ml/min) renal failure, buspirone can be given, but caution should be exercised and reduced doses should be used.

Elderly patients: Older age alone does not require dose adjustment, but caution is advised (for example, due to a possible decrease in kidney and / or liver function and an increased likelihood of side effects). Patients should be given the lowest possible effective dose, and if the dose is increased, the patient should be closely monitored.

– The use of the drug requires special care in patients with rectangular glaucoma and myasthenia gravis.

– In the case of lactose intolerance , the lactose content of the tablets (55.7 mg in 5 mg tablets and 111.4 mg in 10 mg tablets) should be taken into account when formulating the diet.

– Patients should be advised not to eat grapefruit and not to drink large amounts of grapefruit juice as these products may increase the plasma levels of buspirone and lead to an increase in the frequency or severity of side effects.

Switching patients from benzodiazepines to buspirone: Buspirone cannot reverse benzodiazepine withdrawal symptoms. If a patient is switched to buspirone after long-term benzodiazepine therapy, buspirone should only be given after the end of the benzodiazepine taper period.

– Buspirone is not addictive, but its administration to patients with known or suspected drug dependence requires careful medical supervision.

Since the anxiolytic effect occurs after 7 to 14 days of taking the drug, and the full therapeutic effect develops in about 4 weeks, patients with severe anxiety need careful medical supervision in the initial period of therapy.

– Alcoholic beverages should be avoided throughout the course of treatment with buspirone .

Influence on the ability to drive vehicles and control mechanisms. The results of clinical studies have shown that monotherapy with buspirone does not affect the psychomotor performance of patients.