Buspiron

General characteristics. Structure:

Active ingredient: буспирон; 1 tablet contains 5 mg or 10 mg of a buspiron of a hydrochloride;
excipients: lactoses monohydrate, starch corn, calcium hydrophosphate dihydrate, kremkniya dioxide colloid anhydrous, sodium starch-glikolyat (type A), cellulose microcrystallic, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Buspiron — anxiolytic medicine, is applied to treatment of alarming conditions of a different origin, especially neurosises which are followed by feeling of alarm, concern, tension, irritability. The mechanism of action of a buspiron is not finalized, however it is known that it differs from the mechanism of effect of benzodiazepines and other anxiolytic means. Buspiron shows high likeness to presynaptic 5HT1A-receptors and is a partial agonist of postsynaptic 5HT1A-receptors of TsNS. In preclinical trials on experimental models existence at a buspiron of the properties characteristic of anxiolytics and antidepressants is established. Unlike benzodiazepines буспирон does not show anticonvulsant and myorelaxation action, does not cause accustoming, and after end of a course of treatment cancellation symptoms do not develop. Action of a buspiron develops gradually. The therapeutic effect begins to be shown between the 7th and 14th days of therapy, and the maximum effect is reached only approximately in 4 weeks after an initiation of treatment.

Pharmacokinetics. After use drug quickly and almost is completely absorbed from a GIT. Equilibrium concentration in a blood plasma can be reached approximately in 2 days after the beginning of regular use of drug.
Buspiron is exposed to intensive metabolism of the first passing through a liver. System bioavailability makes 4%. Cmax of a metabolite of drug in a blood plasma is reached also in 60–90 min.
About 95% of a buspiron contact proteins of a blood plasma. T½ makes 2–3 h of a blood plasma. Pharmacological parameters of drug do not change at continuous administration of drug (cumulation is absent).
The main pharmacological an active metabolite of a buspiron is (1-[2-pirimidinit] - piperazin (1-PP).
Its anxiolytic activity is 4-5 times lower, than at initial substance, but concentration in a blood plasma is higher also than T½ twice longer, than at a buspiron.
About 29-63% of a buspiron and its metabolites are removed with urine for 24 h, 18–38% are removed with a stake. At a renal failure and a liver elimination of a buspiron and its metabolites is reduced.

Indications to use:

Symptomatic treatment of alarming states with the dominating symptoms: alarm, internal concern, condition of tension.

Route of administration and doses:

Doses are defined by the doctor individually for each patient depending on a condition of a disease. At the beginning of therapy appoint 5 mg of a buspiron of a hydrochloride 2–3 times a day. For achievement of the maximum therapeutic effect the daily dose is gradually raised to 15–30 mg of a buspiron distributed on several separate doses.
The maximum single dose should not exceed 30 mg.
The maximum daily dose should not exceed 45 mg.
Pill should be taken at the same time days, without chewing, washing down with a small amount of liquid, irrespective of meal.
In need of division of a tablet into two half it should be put on a firm surface a hyphen up and to press slightly a thumb.
Special groups of patients. At reduced function of a liver and/or kidneys it is necessary to apply minimum possible dose.
Treatment duration. Tranquilizers cannot be applied without control throughout the long period. If long use of drug (≤6 months) is necessary, it is necessary to carry out careful medical monitoring. It is necessary to remember carrying out psychotherapeutic and sotsioterapevtichesky measures in parallel with treatment buspirony.

Features of use:

Clinical and preclinical trials did not reveal signs which demonstrate risk of accustoming or dependence to a buspiron, however purpose of drug have to be reasonable.
Buspiron do not appoint for treatment of the abstinence signs caused by use of benzodiazepines or other sedative/somnolent medicines. Therefore prior to treatment buspirony it is necessary to stop use of these drugs gradually. It especially concerns patients who accept the medicines suppressing TsNS. Do not appoint буспирон to patients with epilepsy attacks in the anamnesis.
The patient with renal failures and a liver in the anamnesis drug is used with care.
Drug Buspiron Sandoz contains lactose therefore patients should not appoint it with the most rare hereditary forms of intolerance of a galactose, deficit of lactase or a syndrome of glyukozo-galaktozny malabsorption.
Use during pregnancy and feeding by a breast. The uses of a buspiron given relatively during pregnancy is absent therefore it is possible to appoint drug only in that case when the expected advantage for mother exceeds potential risk for a fruit. Buspiron gets into breast milk therefore feeding by a breast during treatment should be stopped.
Children. To children буспирон do not appoint due to the lack of data on safety and efficiency of use.
Ability to influence speed of response at control of vehicles or work with other mechanisms. During treatment it is necessary to refrain from control of vehicles or work with other mechanisms as emergence of side reactions from TsNS and mentality is possible.

Side effects:

Frequency of side reactions: very often (≥ 1/10), it is frequent (≥ 1/100, <1/10), sometimes (≥ 1/1000, <1/100), is rare (≥ 1/10 000, <1/1000), is very rare (<1/10 000), it is unknown (frequency cannot be estimated due to the lack of data).
From cardiovascular system: often — not specific stethalgia; sometimes — a temporary loss of consciousness, arterial hypotension and/or hypertensia, a tachycardia/heart consciousness; seldom — disturbance of cerebral circulation, heart failure, a myocardial infarction, a cardiomyopathy, bradycardia.
From system of blood: seldom — changes of indicators of blood (an eosinophilia, a leukopenia, a thrombopenia).
From mentality: often — nightmares, drowsiness, sleeplessness, dizziness, nervousness, decrease in concentration of attention, contagious excitation, irritability, hostility, confusion of consciousness, a depression; seldom — depersonalization, discomfort, the pathological increased perception of usual sounds, euphoria, a hyperkinesia, concern, disturbance of associative perception, a hallucination, suicide thoughts, epileptic attacks; seldom — the sharp change of mood, claustrophobia, a stupor, the illegible speech, psychosis passing problems with memory, a serotoninovy syndrome.
From TsNS: sometimes — numbness, paresthesia (for example a pricking, feeling of pain), a lack of coordination, a tremor; seldom — the spontaneous movements, block, extrapyramidal symptoms, including early and late dyskinesia, disturbance of a tone, parkinsonism, an akathisia.
From an organ of sight: often — sight opacification; sometimes — reddening and an itch in an eye, conjunctivitis; seldom — photophobia, feeling of intraocular pressure, eye pain, the narrowed field of vision.
From an acoustic organ: often — a sonitus.
From respiratory system: often — a throat inflammation, a nose congestion; sometimes — hurried breathing, an asthma, pain in heart; seldom — nasal bleeding.
From a GIT: often — nausea, a xerostomia, pain in epigastric area, diarrhea; sometimes — a meteorism, lack of appetite, increase in appetite, hypersalivation, a syndrome of irritation of a large intestine, a proctorrhagia, a lock, vomiting.
From an urinary system: sometimes — a frequent urination, an urination delay; seldom — enuresis, a night urination.
From skin: sometimes — hypostasis, urticaria, a hyperemia, developing of hematomas, baldness, a xeroderma, eczema, a face edema, blisters; seldom — allergic reactions, an ecchymoma, an acne, thinning of nails.
From a musculoskeletal system: sometimes — a spasm and muscle tension, a mialgiya, an arthralgia; seldom — a myasthenia.
From endocrine system: seldom — a galactorrhoea, a gynecomastia, dysfunction of a thyroid gland.
General disturbances: often — a headache, an adynamy; sometimes — increase in body weight, a fever, a ring in the head, a body degrowth, an indisposition, increased fatigue, disturbance of sense of smell and flavoring feelings, the increased sweating, inflows, a cold hyperesthesia; seldom — tendency to an alcohol abuse, disturbance of blood coagulation, loss of a voice, a hiccups, a glossodynia.
From gepatobiliarny system: seldom — increase in liver enzymes.
From reproductive system: sometimes — disturbance of a menstrual cycle, reduction or increase in a libido; seldom — an amenorrhea, an inflammation of urinogenital bodies, decrease in an ejaculation, impotence.

Interaction with other medicines:

 Due to the insufficiency of the relevant clinical data the combined use of a buspiron with anti-hypertensive, antipsychotic medicines, antidepressants, anti-diabetic drugs, anticoagulants, oral contraceptives and cardiac glycosides perhaps only in the conditions of strictly medical control. Buspiron do not apply along with benzodiazepines and other sedatives.
The combination with MAO inhibitors is not recommended in connection with risk of developing of hypertensive crisis.
As буспирон it is mainly metabolized by P450 cytochrome, powerful inhibitors of this enzyme can increase bioavailability of a buspiron.
Nefazodon. Simultaneous use of a buspiron and nefazodon leads to increase in Cmax of a buspiron in a blood plasma by 20 times and AUC by 50 times.
Erythromycin. Simultaneous use of a buspiron and erythromycin leads to increase in Cmax of a buspiron by 5 times and AUC by 6 times.
Itrakonazol. Simultaneous use of a buspiron and itrakonazol led to increase in Cmax of a buspiron by 13 times and AUC by 19 times.
Diltiazem. Simultaneous use of a buspiron and diltiazem leads to increase in Cmax of a buspiron by 4 times and AUC by 5,3 times.
Verapamil. Simultaneous use of a buspiron and verapamil leads to increase in Cmax and AUC for a buspiron by 3,4 times.
Cimetidinum. Simultaneous use of a buspiron and Cimetidinum leads to increase in Cmax of a buspiron by 40%, Tmax — twice, but AUC practically does not change.
At use of a buspiron along with above-mentioned medicines the therapeutic effect and toxicity of a buspiron therefore it is recommended to reduce a dose of a buspiron increase (for example 2,5 mg 2 times a day).
Rifampicin. Simultaneous use of a buspiron and rifampicin leads to reduction of Cmax of a buspiron by 83,9% and AUC — for 89,6%.
Inhibitors and inductors CYP 3A4. Ketokonazol or ритонавир inhibit metabolism of a buspiron and increase its level in a blood plasma. If буспирон to apply along with CYP 3A4 inhibitor, its dose is recommended to be lowered. The inductors CYP 3A4, for example dexamethasone, Phenytoinum, phenobarbital or carbamazepine, can increase the speed of metabolism of a buspiron. In this case it is necessary to raise a dose of a buspiron for preservation of its anxiolytic efficiency.
Inhibitors of the return serotonin reuptake. In clinical trials cases of dangerous use of a buspiron along with antidepressants, the selection inhibitors of the return neyronalny serotonin reuptake were not revealed. There were separate messages on emergence of attacks at their long use combined with buspirony.
Haloperidol. Simultaneous use of a buspiron and haloperidol led to increase in concentration of a haloperidol in blood serum.
Trazodonum. There were messages that at some patients at simultaneous use of Trazodonum with buspirony activity of ASAT by 3 times increased. However such increase in hepatic transaminases was not confirmed with clinical trials.
Diazepam. At simultaneous use of diazepam and a buspiron the level of the first in a blood plasma increases, and also there can be side effects: dizziness, headache, nausea.
During treatment buspirony it is necessary to refrain from the use of alcoholic beverages.
Patients during treatment are not recommended to use in significant amounts grapefruit juice as it can lead to increase in level of a buspiron in a blood plasma and to increase in frequency or weight of side effects.

Contraindications:

Hypersensitivity to a buspiron or to one of drug components; acute congestive glaucoma; malignant myasthenia; heavy dysfunction of a liver; heavy renal failure; epilepsy; feeding period breast; age up to 18 years.

Overdose:

Symptoms: nausea, vomiting, dizziness, fatigue, miosis and dysfunction of a GIT. Heavier complications at the person did not note even at introduction daily doses to 2400 mg.
Symptomatic treatment; gastric lavage. As well as in case of overdose by other medicines, it is necessary to carry out constant observation of functions of respiratory system, ChSS and the ABP. The specific antidote is absent. The hemodialysis is inefficient.

Storage conditions:

Drug needs to be stored in the place unavailable to children, at a temperature of 15-30 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets of 5 mg blister, No. 20

Tablets of 10 mg blister, No. 20