Spitomin pills 10 mg 60 pcs
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Active ingredients
Buspirone
Release form
Pills
Composition
Buspirone hydrochloride 10 mg. Excipients: lactose monohydrate - 111.4 mg, microcrystalline cellulose, sodium carboxymethyl starch, magnesium stearate, anhydrous colloidal silicon dioxide.
Pharmacological effect
Anxiolytic drug (tranquilizer) 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 has no 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 the syndrome of "cancellation." Does not potentiate the effect of alcohol. By anxiolytic activity, buspirone is approximately equal to benzodiazepines. The therapeutic effect develops gradually and is noted after 7-14 days from the start of treatment, the maximum effect is recorded after 4 weeks.
Pharmacokinetics
Absorption After oral administration, buspirone is rapidly and almost completely absorbed from the gastrointestinal tract. Buspirone is extensively metabolized during the "first pass" through the liver. Therefore, an unchanged substance is found in the systemic circulation in a small concentration, which has significant individual differences. Bioavailability is 4%. Cmax in plasma is reached in 60-90 minutes after taking the drug. In healthy volunteers, buspirone had a linear (dose-proportional) pharmacokinetics after taking 10-40 mg. Similar pharmacokinetic parameters were found in elderly patients. After a single dose of the drug in a dose of 20 mg, its concentration in the blood plasma ranged from 1 to 6 ng / ml. Simultaneous ingestion slows down the absorption of buspirone, but due to the decrease in pre-system clearance (the “first pass” effect), the bioavailability of buspirone is significantly increased.After ingestion with food, the AUC value of buspirone is increased by 84%, and its Cmax is increased by 16%. Distribution Binding of buspirone to plasma proteins is approximately 95% (86% with plasma albumin, the rest with acid α1-glycoprotein). Css in blood plasma can be reached approximately 2 days after the start of regular intake. The apparent Vd is 5.3 l / kg. Buspirone is excreted in breast milk. Data on the penetration of the drug through the placental barrier are not available. Metabolism Buspirone undergoes oxidative metabolism mainly with the participation of CYP3A4 isoenzymes. Various hydroxylated metabolites are formed. The main metabolite (5-OH-buspirone) is inactive. The dealkylated metabolite (1- (2-pyrimidinyl) piperazine, 1-PP) is active. Its anxiolytic activity is 4-5 times lower than that of the original substance, but its plasma level is higher and T1 / 2 is approximately 2 times longer than that of buspirone. Withdrawal After a single injection of 14C-labeled buspirone, 29-63% of the radioactivity is excreted in the urine within 24 hours, mostly 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 T1 / 2 of the initial substance in a dose of about 2-3 hours, and T1 / 2 of the active metabolite is 4.8 hours. Pharmacokinetics in special clinical situations. If the liver function is abnormal, plasma concentrations of buspirone and AUC values may increase. and T1 / 2 elongation. In connection with the release of an unchanged substance in the bile, a second peak of buspirone concentration in the blood plasma is possible. Patients with cirrhosis of the liver should be prescribed the drug in lower doses or in the same doses with extended intervals. In renal failure, clearance of buspirone can be reduced by 50%. In renal insufficiency, buspirone should be administered with caution and in reduced doses. The pharmacokinetics of buspirone in elderly patients is not changed.
Indications
- Generalized anxiety disorder (GAD); - panic disorder; - autonomic dysfunction syndrome; - alcohol withdrawal syndrome (as an adjuvant therapy); - adjuvant therapy of depressive disorders (the drug is not prescribed for monotherapy of depression).
Contraindications
- Hypersensitivity to the drug; - renal failure severedegree (GFR <10 ml / min); - severe liver failure (prothrombin time> 18 sec); - glaucoma; - myasthenia gravis; - children and adolescents under 18 years of age (safety and efficacy of buspiron for this age group have not been proven); - simultaneous use of MAO inhibitors or a 14-day period after discontinuation of an irreversible MAO inhibitor or 1 day after discontinuation of a reversible MAO inhibitor; - lactation period (breastfeeding); - pregnancy or suspected pregnancy. With care: cirrhosis, a renal failure.
Use during pregnancy and lactation
Due to the lack of properly controlled clinical data, the use of buspirone during pregnancy is possible only when the expected benefit of therapy for the mother justifies the possible risk to the fetus. Women of childbearing age during the course of treatment with buspirone should use adequate methods of contraception, since the safety of buspirone during pregnancy has not been proven. Buspirone is excreted in breast milk. Data from clinical studies on the use of buspirone during breastfeeding are not enough; therefore, the drug should not be administered to nursing mothers.
Dosage and administration
The drug should always be taken at the same time of the day, before or after a meal, in order to avoid significant fluctuations in the concentration of the active substance in the blood plasma during the day. The drug should not be taken sporadically for the treatment of anxiety, since the therapeutic effect of the drug Spitomin develops only after repeated administration and appears no earlier than after 7-14 days of treatment. The dose should be selected individually. The recommended initial dose is 15 mg, it can be increased by 5 mg / day every 2-3 days. The daily dose should be divided into 2-3 doses. The usual daily dose is 20-30 mg. The maximum single dose is 30 mg. The maximum daily dose is 60 mg. Elderly patients dose adjustment is not required, because The pharmacokinetics of buspirone do not depend on age. In case of impaired renal function, the drug should be used with caution and in reduced doses. In case of abnormal liver function, the drug should be used with caution and in reduced doses, for this purpose reduce single doses or increase the interval between doses.
Side effects
Buspirone is usually well tolerated. Side effects, if they occur, usually occur at the beginning of the course of treatment and then disappear, despite continuing to take the drug. In some cases, a dose reduction is necessary. Determination of the frequency of side effects: often (1/100), infrequently (from 1/100 to 1/1000), rarely (<1/1000). In many cases, in the absence of a comparator drug, the association of adverse effects with the intake of the drug could not be proven. Since the cardiovascular system: often - chest pain; infrequently - fainting, arterial hypotension, arterial hypertension; rarely - cerebrovascular accidents, decompensation of heart failure, myocardial infarction, myocardiopathy, bradycardia. On the part of the nervous system: often - dizziness, headache, increased nervous irritability, sleep disturbances; infrequently - dysphoric reactions, depersonalization, dysphoria, hypersensitivity to noise, euphoria, hyperkinesis, fear, apathy, hallucinations, confusion, prolonged reaction time, suicidal thoughts, epileptic seizures, paresthesia, poor coordination of movements, tremors; rarely - claustrophobia, cold intolerance, stupor, stuttering, extrapyramidal disorders, psychotic disorders. From the senses: often - tinnitus; infrequently - blurred vision, itchy eyes, redness of the eyes, conjunctivitis, a violation of taste and olfactory sensations; seldom - disorders of the inner ear, pain in the eyes, photophobia, increased intraocular pressure. On the part of the respiratory system: often - laryngitis, swelling of the nasal mucosa; infrequently - hyperventilation, lack of air, feeling of heaviness in the chest; rarely - nosebleeds. On the part of the endocrine system: rarely - galactorrhea, the defeat of the thyroid gland. On the part of the digestive system: rarely - nausea, flatulence, anorexia, increased appetite, drooling, intestinal bleeding; rarely - diarrhea, burning in the tongue. From the urinary system: infrequently - dysuria (including frequent urination, urinary retention); rarely bedwetting. On the part of the reproductive system: infrequently - violations of the menstrual cycle, decreased sexual desire; rarely - amenorrhea, pelvic inflammatory disease, delayed ejaculation, impotence.On the part of the musculoskeletal system: infrequently - muscle spasms, muscle stiffness, arthralgia; rarely, muscle weakness, pain in muscles and bones. On the part of the skin and subcutaneous tissues: infrequently - swelling, itching, flushing, hair loss, dry skin, swelling of the face, skin visibility, rash. Changes in laboratory parameters: infrequently - an increase in the activity of ALT and ACT in serum; rarely - eosinophilia, leukopenia, thrombocytopenia. Other: weight gain, fever, weight loss; rarely, alcohol abuse, loss of voice, tinnitus, hiccups.
Overdose
Symptoms: gastrointestinal disturbances, nausea, vomiting, dizziness and drowsiness (also in severe forms), depression of consciousness of varying severity. Treatment: gastric lavage and symptomatic therapy. The specific antidote is unknown, dialysis is ineffective. Experience to date indicates that even extremely high doses (single intake of 375 mg) do not necessarily cause severe symptoms.
Interaction with other drugs
Given the pharmacokinetic properties of the drug (low bioavailability, intensive metabolism in the liver, high binding to proteins), there is a high probability of the interaction of buspirone with drugs while using it simultaneously. However, since buspirone has a significant therapeutic breadth, pharmacokinetic interactions do not lead to clinically significant pharmacodynamic changes. MAO inhibitors: an increase in blood pressure and the occurrence of hypertensive crises after the simultaneous administration of buspirone and drugs acting on MAO (moclobemide, selegiline) are described; therefore, buspirone cannot be combined with MAO inhibitors. After discontinuation of an irreversible MAO inhibitor (for example, selegilin), Spitomin (and vice versa) should take at least 14 days before the introduction of the drug. Similarly, it should take at least 14 days after discontinuation of the drug Spitomin before the introduction of moclobemide (reversible MAO inhibitor). However, Spitomin can be taken 1 day after the abolition of moclobemide. Inhibitors and inducers of CYP3A4: In vitro studies have shown that buspirone is mainly metabolized by CYP3A4 isoenzymes. The simultaneous administration of buspirone and inhibitors of CYP3A4 (erythromycin, itraconazole, nefazodone, diltiazem, verapamil, and grapefruit juice) can lead to drug interactions, and with the administration of a strong inhibitor also increase the plasma plasma concentration of buspirone; therefore, a dose reduction of buspirone is necessary (for example, up to 2.5 mg 2 times / day).Strong inducers of CYP3A4 (for example, rifampicin) can significantly reduce the concentration of buspirone in the blood plasma and weaken its pharmacodynamic effects. Drugs with a high degree of protein binding: since buspirone is highly bound to plasma proteins (95%), there is always a chance of interaction with other active substances characterized by high binding to plasma proteins. In vitro studies have shown that buspirone is not able to displace drugs with strong binding (warfarin, phenytoin, propranolol) from protein binding sites, but it can replace drugs with low binding, for example, digoxin. With the combined use of cimetidine and buspirone, Cmax of buspirone increases by 40%, and its AUC does not change. Co-administration of these drugs requires careful medical supervision. With the combined use of diazepam and buspirone, the concentration of nordiazepam increases slightly, and side effects can occur: systemic dizziness, headache, nausea. Substances that inhibit the central nervous system, and alcohol: the combined use of buspirone with triazolam or flurazepam does not increase the duration or the strength of the effect of these benzodiazepines. After a single dose of 20 mg of buspirone, its effects on the CNS do not increase. The experience of joint use of buspirone and other anxiolytics or other agents acting on the central nervous system (for example, antipsychotics and antidepressants) is insufficient. Therefore, in such cases, careful medical observation is necessary. Other drugs: due to the lack of relevant clinical data, the combined use of buspirone with antihypertensive drugs, cardiac glycosides, oral contraceptives and hypoglycemic agents is possible only under careful medical supervision.
special instructions
Buspirone is extensively metabolized in the liver. With a single dose of 30 mg in patients with cirrhosis of the liver, the concentration of buspirone in the blood plasma increases and the AUC increases with the prolongation of the T1 / 2 drug. In connection with the release of an unchanged substance in the bile, a second peak of buspirone concentration in the blood plasma is possible. The drug is contraindicated in patients with severe liver failure.Patients with cirrhosis of the liver should be prescribed the drug in lower doses or in the same doses with extended intervals. In moderate to severe renal failure, clearance of buspirone can be reduced by 50%. The drug is contraindicated in patients with severe renal insufficiency with GFR less than 10 ml / min. With mild (GFR more than 30 ml / min) and moderate (GFR 10-30 ml / min) of renal failure, buspirone can be given, but care should be taken and the drug should be given in reduced doses. Elderly patients do not require dose adjustment, but the drug should be used with caution, for example, in connection with a possible reduction in renal and / or liver function and an increased likelihood of side effects. These patients should be prescribed the drug in the minimum effective doses, and in the case of increasing the dose should be carefully monitored by the patient. With extreme caution should be used in patients with angle-closure glaucoma and myasthenia. Patients should be advised not to eat grapefruit and not to drink grapefruit juice in significant quantities, because These products can increase the plasma concentration of buspirone and lead to an increase in the frequency or severity of side effects. Transfer of patients from benzodiazepines to buspirone: buspirone cannot eliminate the symptoms of benzodiazepine withdrawal. If a patient is transferred to buspirone after prolonged benzodiazepine therapy, buspirone should be given only after the period of gradual reduction of the dose of benzodiazepines is completed. Buspirone does not cause addiction to the drug, but its administration to patients with an established or suspected susceptibility to drug dependence requires careful medical monitoring. Since the anxiolytic effect appears after 7-14 days of taking the drug, and the full therapeutic effect develops in about 4 weeks, patients with strong anxiety need careful medical observation in the initial period of therapy. During the entire course of treatment with buspirone patients should avoid alcohol. In the case of lactose intolerance in the preparation of a diet should take into account the lactose content in the pills (55.7 mg pills 5 mg and 111.4 mg pills 10 mg).Effect on the ability to drive motor vehicles and control mechanisms The results of clinical studies have shown that monotherapy with buspirone does not affect the indicators of the psychomotor activity of patients. Despite this, at the beginning of the course of treatment, transient undesirable effects are possible, and therefore patients should be warned that driving vehicles and operating mechanisms is possible only with full patient confidence in their psychomotor functions. The ability of the patient to drive vehicles and mechanisms should be determined individually, depending on the patient's response to treatment and the use of concomitant therapy.