Spitomin pills 10mg №60

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).

Dosing regimen

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 manifests itself not earlier than after 7-14 days of treatment.

The dose should be selected individually.

The recommended dose is 15 mg, it can be increased to 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.

Have elderly patients dose adjustment does not require, because The pharmacokinetics of buspirone do not depend on age.

At renal dysfunction the drug should be used with caution and in reduced doses.

At liver dysfunction the drug should be used with caution and in reduced doses, for this purpose reduce single doses or increase the interval between doses.

Side effect

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.

Cardiovascular: often - chest pain; infrequently - fainting, arterial hypotension, arterial hypertension; rarely - cerebrovascular accidents, decompensation of heart failure, myocardial infarction, myocardiopathy, bradycardia.

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.

Special 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.

Respiratory: 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, damage to the thyroid gland.

Gastrointestinal: infrequently - nausea, flatulence, anorexia, increased appetite, drooling, intestinal bleeding; rarely - diarrhea, burning in the tongue.

Urogenital: infrequently - dysuria (including frequent urination, urinary retention); rarely bedwetting.

From the reproductive system: infrequently - violations of the menstrual cycle, decreased sexual desire; rarely - amenorrhea, pelvic inflammatory disease, delayed ejaculation, impotence.

Musculoskeletal system: infrequently - muscle spasms, muscle stiffness, arthralgia; rarely, muscle weakness, pain in muscles and bones.

Dermatological: Infrequently - swelling, itching, hot flashes, hair loss, dry skin, swelling of the face, skin 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.

Contraindications

- hypersensitivity to the drug;

- renal failure severe (GFR <10 ml / min);

- severe liver failure (prothrombin time> more than 18 seconds);

- 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.

Carefully: cirrhosis of the liver, 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.

During the course of treatment with buspirone, adequate contraceptive methods should be used, 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.

Application for violations of the liver

Contraindication: severe liver failure (prothrombin time> more than 18 seconds).

Application for violations of kidney function

Contraindication: severe renal failure (GFR <10 ml / min).

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 prolongation of T_1/2 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, becauseThese 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 tablets (55.7 mg tablets 5 mg and 111.4 mg tablets 10 mg).

Influence on ability to drive motor transport and control mechanisms

The results of clinical studies have shown that buspiron monotherapy does not affect the psychomotor performance of patients. Despite this, transient undesirable effects are possible at the beginning of the course of treatment.In this connection, patients should be warned that the driving of vehicles and the control of mechanisms is possible only with full patient confidence in their psychomotor functions. The patient's ability to drive vehicles and mechanisms should be determined individually, depending on the patient's response to treatment and the use of concomitant therapy.

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 not known, dialysis is ineffective. Experience to date indicates that even extremely high doses (single intake of 375 mg) do not necessarily cause severe symptoms.

Drug interaction

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) ​​before the start of the administration of the drug Spitomin^® (and vice versa) must take at least 14 weeks. Similarly, it should take at least 14 days after discontinuation of the drug Spitomin^® before the introduction of moclobemide (reversible inhibitor of MAO). However spitomin^® can be taken 1 day after the withdrawal 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, it is necessary to reduce the dose of buspirone (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.

Preparations with a high degree of binding to proteins: 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 .

When used together cimetidine and buspirone C_max Buspirone increases by 40%, and its AUC does not change. Co-administration of these drugs requires careful medical supervision.

When used together 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: when combined, buspirone with triazolam or flurazepam does not increase the duration or 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 medicines: 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.

Terms and conditions of storage

The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 30 ° C.