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Spitomin® [Buspirone]

Egis
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2019-09-19
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Clinical Pharmacology

Spitomin has anxiolytic, antidepressant effect.

Pharmacodynamics
The 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. 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
After oral administration, buspirone is rapidly and almost completely absorbed from the gastrointestinal tract.
Buspirone undergoes intensive first-pass metabolism 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 blood plasma is achieved 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 ingestion of 20 mg of the drug, its plasma levels range from 1 to 6 ng / ml. Approximately 95% of buspirone is bound to plasma proteins (86% is bound to plasma albumin, the rest is α1acidic glycoprotein).

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 level in the blood plasma is higher, and T1/2 about 2 times longer than that of buspirone. After a single injection 14C-labeled buspirone, 29–63% of 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 T1/2 the initial substance is about 2–3 hours, and T1/2 active metabolite is 4.8 hours.

Simultaneous food intake slows down the absorption of buspirone, but due to the decrease in pre-system clearance (first-pass effect), the bioavailability of buspirone is significantly increased. After ingestion, the AUC value of buspirone is increased by 84%, and its Cmax - by 16%.

Css blood plasma can be reached approximately 2 days after the start of regular intake.

Seeming vd is 5.3 l / kg.

Buspirone is excreted in breast milk, but there are no data on placental transmission.

Elevated plasma buspirone levels and AUC values, as well as T prolongation1/2 may occur in violation of the liver. In connection with the release of an unchanged substance in 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 case of 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 adjunctive therapy);
  • depressive disorders - adjuvant therapy (the drug is not prescribed for monotherapy of depression).

Composition

1 tablet contains:
active substance: buspirone hydrochloride 10 mg,
Excipients: lactose monohydrate 111.4 mg; MCC; sodium carboxymethyl starch; magnesium stearate; silicon dioxide colloidal anhydrous

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Spitomin® [Buspirone]

Dosage and Administration

For oral use, always at the same time of the day, before or after a meal (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 7–14 days of treatment.

The dose should be selected for each patient individually. The recommended dose is 15 mg; it can be increased to 5 mg / day every 2 or 3 days. The daily dose should be divided into 2-3 doses. The usual daily dose of 20-30 mg per day. The maximum single dose is 30 mg; The maximum daily dose should not exceed 60 mg.

Special patient groups

Elderly Sick By itself, old age does not require dose adjustment, since the pharmacokinetics of buspirone do 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.

Liver dysfunction. In case of abnormal liver function, the drug should be used with caution and in reduced doses, for which individual doses are reduced or the interval between doses is increased.

Adverse reactions

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.

To determine the frequency of side effects of the drug, the following classification is used: often (more than 1/100); infrequently (from 1/100 to 1/1000); rarely (less than 1/1000); very rarely(

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

From the side of the central 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, tremor rarely - claustrophobia, cold intolerance, stupor, stuttering, extrapyramidal disorders, psychotic disorders.

On the part of the organs of sight and hearing: often - tinnitus, laryngitis, swelling of the nasal mucosa; infrequently - blurred vision, itchy eyes, redness of the eyes, conjunctivitis, a violation of taste and olfactory sensations; rarely - disorders of the inner ear, eye pain, photophobia, increased IOP.

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

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

From the genitourinary system: infrequently - dysuric disorders (including frequent urination, urinary retention), menstrual disorders, decreased sexual desire; rarely - amenorrhea, pelvic inflammatory disease, bed-wetting, delayed ejaculation, impotence.

From the musculoskeletal system: infrequently - muscle spasms, muscle stiffness, arthralgia; rarely, muscle weakness.

On the part of the respiratory system: infrequently - hyperventilation, lack of air, feeling of heaviness in the chest; rarely - nosebleeds.

From the skin: Infrequently - swelling, itching, hot flashes, hair loss, dry skin, facial swelling, skin rash, rash.

Other: weight gain, fever, weight loss, muscle and bone pain; rarely - alcohol abuse, loss of voice, tinnitus, hiccups.

Changes in laboratory parameters: infrequently - increased serum ALT and ACT levels; rarely - eosinophilia, leukopenia, thrombocytopenia.

Contraindications

Carefully: liver cirrhosis, renal failure.

Drug interactions

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 simultaneously administered drugs; however, since buspirone has a significant therapeutic breadth, pharmacokinetic interactions do not lead to clinically significant pharmacodynamic changes.

MAO inhibitors (MAOIs). An increase in blood pressure and the occurrence of hypertensive crises after the simultaneous administration of buspirone and drugs acting on MAO (moclobemide, selegiline) have been described; therefore, buspirone cannot be combined with MAOI. After the cancellation of irreversible MAOI (for example, selegilin) ​​before the start of drug administration Spitomin® (and vice versa) at least 14 days must pass. Similarly, it should take at least 14 days after discontinuation of the drug Spitomin® before the introduction of moclobemide (reversible MAOI). However spitomin® can be given 1 day after the abolition of moclobemide.

Inhibitors and inducers of CYP3A4. Research in vitro have shown that buspirone is mainly metabolized by cytochrome P450 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 level of buspirone in the blood plasma; therefore, a dose reduction of buspirone is necessary (for example, up to 2.5 mg 2 times a day).

Strong inducers of CYP3A4 (for example rifampicin) can significantly reduce the levels of buspirone in the blood plasma and weaken its pharmacodynamic effects.

Drugs strongly bound by proteins. Since buspirone is strongly bound to proteins (95%), there is always a chance of interaction with other protein-bound active substances. Research in vitro have shown that buspirone cannot displace strongly bound drugs from proteins (warfarin, phenytoin, propranolol), but can replace loosely bound drugs, for example digoxin.

With co-administration cimetidine with buspirone Cmax Buspirone increases by 40%, and its AUC does not change. Co-administration of these drugs requires careful medical supervision.

With co-administration diazepam with buspirone, the level of nordiazepam increases slightly, and side effects may occur: systemic dizziness, headache, nausea.

Substances, oppressive central nervous system, and alcohol. Combined administration of 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 drugs. Due to the lack of relevant clinical data, the combined use of buspirone with antihypertensive drugs, cardiac glycosides, oral contraceptives and antidiabetic drugs is possible only under careful medical supervision.

Pregnancy and Lactation

Due to the lack of properly controlled clinical research data, the use of buspirone during pregnancy is possible only if the benefits of the drug justify the possible risks. 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. Sufficient data from clinical studies on the use of buspirone during breastfeeding are not available, so breastfeeding mothers are not recommended to take this drug.

Special instructions

Liver failure. Buspirone is extensively metabolized in the liver. A single dose of 30 mg in patients with liver cirrhosis increases plasma levels of buspirone and increases AUC with a prolonged T duration.1/2 drug. In connection with the release of an unchanged substance in 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.

Renal failure. With moderate or 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 used, but care should be taken to administer reduced doses.

Elderly patients. Older age in itself does not require dose adjustment, but caution is recommended (for example, due to the possible reduction in renal and / or liver function and an increased likelihood of side effects). Patients should be prescribed the lowest possible effective dose, and in case of a dose increase, careful monitoring of the patient should be established.

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

In case of lactose intolerance When drafting a diet, one should take into account the lactose content in tablets (55.7 mg - in tablets of 5 mg and 111.4 mg - in tablets of 10 mg).

Patients should be advised not to eat. grapefruit and do not drink grapefruit juice in significant quantities, because These products can increase the level of buspirone in the blood plasma and lead to an increase in the frequency or severity of side effects.

Transfer of patients from benzodiazepines to buspirone. Buspirone cannot eliminate benzodiazepine withdrawal symptoms. If a patient is transferred to buspirone after prolonged benzodiazepine therapy, buspirone should be administered 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, alcohol should be avoided.

Impact on the ability to drive vehicles 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, 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.

Overdosage

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

Treatment: gastric lavage and symptomatic therapy. Dialysis is ineffective.

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

  • Brand name: Spitomin
  • Active ingredient: Buspirone
  • Dosage form: Pills
  • Manufacturer: Egis
  • Country of Origin: Hungary

Studies and clinical trials of Buspirone (Click to expand)

  1. Equine metabolism of buspirone studied by high-performance liquid chromatography/mass spectrometry
  2. Anxiolytic effect of hydroxyzine: a double-blind trial versus placebo and buspirone
  3. An improved multigram synthesis of tetradeuterated buspirone
  4. Buspirone potentiation of antidepressants in the treatment of PTSD
  5. Meta-analysis of the safety and tolerability of two dose regimens of buspirone in patients with persistent anxiety
  6. Relationship between chromatographic behavior and affinity to 5-hT1A serotonin receptors of new buspirone analogues
  7. Flow Injection Analysis with Tubular Membrane Ion-Selective Electrode and Coated Wires for Buspirone Hydrochloride
  8. An Efficient Synthesis of Buspirone and its Analogues.
  9. An Efficient Synthesis of Aripiprazole, Buspirone and NAN-190 by the Reductive Alkylation of Amines Procedure
  10. The relationship between buspirone bioavailability and dose in healthy subjects
  11. Pharmacokinetics of 6-hydroxybuspirone and its enantiomers administered individually or following buspirone administration in humans
  12. Rapid high-performance liquid chromatographic measurement of buspirone in human plasma after overdose
  13. ChemInform Abstract: Novel Buspirone-Like 5-HT1A Receptor Ligands
  14. ChemInform Abstract: Facile Synthesis of Anxiolytic Buspirone (V).
  15. Effects of buspirone and alprazolam treatment on the startle-potentiated startle response
  16. Behavioral and neurochemical studies on the anticonflict actions of buspirone
  17. Changing concepts of the biochemical action of the anxioselective drug, buspirone
  18. Buspirone as a midbrain modulator: Anxiolysis unrelated to traditional benzodiazepine mechanisms
  19. Buspirone attenuates learned helplessness behavior in rats
  20. Buspirone antagonizes the expression of conditioned taste aversion in rats
  21. Drug discrimination in pentylenetetrazol-trained baboons: Generalization to buspirone and β-carboline-3-carboxylic acid ethyl ester but not lorazepam or pentobarbital
  22. Effects of buspirone in the geller-seifter conflict test with incremental shock
  23. Effects of chlordiazepoxide, buspirone, and serotonin receptor agonists and antagonists on responses of squirrel monkeys maintained under second-order schedules of intramuscular cocaine injection or food presentation
  24. Cork gnawing in the rat as a screening method for buspirone-like anxiolytics

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