Buspirone - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Dopaminomimetics

Anxiolytics

Included in the formulation

Spitomin®

pills inwards

EGIS ZAO Pharmaceutical Plant Hungary

АТХ:

N.05.B.E Derivatives of azaspirodekanedione

N.05.B.E.01 Buspirone

Pharmacodynamics:

A selective partial agonist of serotonin receptors of subtype 1A (5-HT1A). Reduces the synthesis and release of serotonin, the activity of serotonergic neurons, incl. in the dorsal nucleus of the suture. Selective blockade of pre- and postsynaptic dopamine receptors, an increase in the rate of excitation of dopamine neurons in the midbrain.

Unlike classic anxiolytics, it does not have anti-epileptic, sedative, hypnotic and miorelaxing effects. Does not cause the development of drug dependence and the syndrome of "withdrawal".

Pharmacokinetics:

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract and subjected to extensive presystemic metabolism. At the "first pass" through the liver is hydroxylated and dealkylated (bioavailability - 4%). After taking a dose of 20 mg, the maximum concentration in the blood plasma is reached after 40-90 minutes and is 1-6 ng / ml. Binding to plasma proteins - 95%. Simultaneous food intake reduces the rate of absorption, but increases the amount of unchanged drug that has reached the systemic blood flow.It is excreted by the kidneys (29-63%) in the form of metabolites and unchanged (1%), as well as the gastrointestinal tract (18-38%). The half-life of buspirone is 2-3 hours, the half-life of the active metabolite is 4.8 hours.

The effect develops gradually, manifests itself after 7-14 days and reaches a maximum after 4 weeks.

Indications:Generalized anxiety disorder, panic disorder, autonomic dystonia syndrome, alcohol abstinence syndrome (adjuvant therapy), depression (ancillary therapy).

ICD-10

V.F10-F19.F10.3 Mental and behavioral disorders caused by alcohol use - withdrawal symptoms

V.F40-F48.F40.0 Agoraphobia

V.F40-F48.F41.0 Panic disorder [episodic paroxysmal anxiety]

V.F40-F48.F41.1 Generalized anxiety disorder

V.F40-F48.F42 Obsessive-compulsive disorder

V.F40-F48.F45 Somatoform disorders

Contraindications:Hypersensitivitysevere impairment of renal and hepatic function, glaucoma, gravis gravis, pregnancy, breast-feeding, age under 18, simultaneous use of monoamine oxidase inhibitors.

Carefully:When used simultaneously with neuroleptics, antidepressantsand, by cardiac glycosides, antihypertensiveand antidiabeticoral contraceptives. With renal and hepatic insufficiency of mild and moderate severity, cirrhosis of the liver is prescribed in smaller doses and under the strict supervision of a physician. During the treatment should be excluded from drinking alcohol. At the beginning of treatment with caution to apply during work drivers of vehicles and people whose profession is associated with increased concentration of attention.

Pregnancy and lactation:

Recommendations Food and Drug Administration (US Food and Drug Administration) category B. Adequate and controlled studies in humans have not been conducted. In studies on rats and rabbits, the use of a dose 30 times higher than the maximum recommended for humans did not cause birth defects.

Buspirone is excreted in breast milk. Complications in people are not registered. Nursing mothers should avoid taking this medication.

Dosing and Administration:Inside. The recommended initial dose is 5 mg 3 times a day, if necessary, it can be increased by 5 mg every 2-3 days. The average daily dose is 20-30 mg. The maximum single dose is 30 mg, the daily dose is 60 mg.

Side effects:

From the nervous system and sensory organs: dizziness, drowsiness, headache, nervousness, fatigue, sleep disturbance, decreased ability to concentrate; extrapyramidal disorders; confusion or depression, weakness, numbness; neurologic symptoms (muscle weakness, tingling, pain or weakness in the hands or feet, uncontrolled movements of the trunk).

From the cardiovascular system: tachycardia / strong palpitations.

On the part of the organs of the gastrointestinal tract: nausea, dry mouth, diarrhea; vomiting, constipation; a decrease in appetite.

From the senses: tinnitus, laryngitis, swelling of the nasal mucosa, blurred vision, itchy eyes, red eyes.

On the part of the endocrine system: galactorrhea and thyroid damage.

Other: myalgia, spasms, muscle cramps or stiffness, rash, sweating.

Overdose:

Nausea, vomiting and other gastrointestinal disorders, dizziness, miosis, drowsiness.

Treatment: gastric lavage, the appointment of activated charcoal, symptomatic therapy. Dialysis is ineffective.

Interaction:

Grapefruit juice - an increase in the concentration of buspirone in the blood.

Monoamine oxidase inhibitors are incompatible; treatment with buspirone should be started no earlier than 14 days after the abolition of monoamine oxidase inhibitors. Possible hypertensive crisis.

Inductors CYP3A4 (carbamazepine, rifampicin, phenytoin and others) - acceleration of metabolism and a decrease in the effect of buspirone.

Simultaneous use of other antipsychotic, hypotensive, hypoglycemic agents, antidepressants, cardiac glycosides and hormonal contraceptives requires caution.

Special instructions:

Does not have a negative effect on psychomotor functions, does not cause tolerance, drug dependence and withdrawal symptoms. Does not enhance the effect of alcohol. Studies have shown the efficacy of buspirone in autism, obsessive-compulsive disorders, premenstrual syndrome, sexual dysfunction, and the easing of symptoms upon cessation of smoking.

Buspirone is not used to treat anxiety and reduce stress associated with the stresses of everyday life.

It should not be used in patients with epilepsy or with a history of a tendency to develop seizures.

Use with caution in patients with impaired hepatic and / or renal function.

Patients who abuse drugs or have a history of drug dependence during the treatment period need careful monitoring to identify the development of buspirone tolerance or dependence.

In controlled trials, it has been established that buspirone is not effective for long (more than 3-4 weeks) treatment of anxiety. However, when applied for several months, no side effects were found. If buspirone apply for a long time, then its effectiveness should be checked at regular intervals.

During the period of treatment, the patient should refrain from activities related to the need to concentrate attention and high speed of psychomotor reactions.

The safety and efficacy of buspirone in children and adolescents under the age of 18 years have not been established.

Instructions

Buspirone (Buspironum)