Spitomin
Spitomin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Spitomin
ATX code: N05BE01
Active ingredient: buspirone (buspirone)
Producer: EGIS Pharmaceuticals PLC (Hungary)
Description and photo update: 2018-27-07
Prices in pharmacies: from 616 rubles.
Buy
Spitomin is a drug with antidepressant, anxiolytic action.
Release form and composition
The dosage form of Spitomin's release is tablets: almost white or white, round flat shape, chamfer and engraving "E 151" or "E 152" (5 or 10 mg, respectively) on one side, risk on the other; with a weak characteristic odor or without it (in a cardboard box 6 blisters of 10 pcs.).
Composition of 1 tablet:
- active substance: buspirone hydrochloride - 5 or 10 mg;
- auxiliary components: lactose monohydrate, microcrystalline cellulose, anhydrous colloidal silicon dioxide, sodium carboxymethyl starch, magnesium stearate.
Pharmacological properties
Pharmacodynamics
Spitomin is an anxiolytic drug (tranquilizer) of the non-benzodiazepine series, which also has an antidepressant effect. It differs from classical anxiolytics in the absence of antiepileptic, sedative, hypnotic and muscle relaxant effects.
The mechanism of action of buspirone is associated with its effect on the dopaminergic and serotonergic systems. Selectively increases the rate of excitation of dopamine neurons in the midbrain and blocks presynaptic dopamine receptors.
Buspirone is also one of the selective partial agonists of 5-HT 1A serotonin receptors. Anxiolytic activity is approximately equal to benzodiazepines.
Spitomin does not have a significant effect on benzodiazepine receptors. Does not affect the binding of GABA, does not cause tolerance, withdrawal syndrome and drug dependence, does not have a negative effect on psychomotor functions, does not potentiate the effect of alcohol.
The development of the therapeutic effect of Spitomin occurs gradually (after 7-14 days from the start of use), the maximum effect is observed after 4 weeks of treatment.
Pharmacokinetics
After oral administration, Buspirone is almost completely and rapidly absorbed from the gastrointestinal tract. During the first passage through the liver, the substance undergoes intensive metabolism, therefore, unchanged, it is found in the systemic circulation in a small concentration (has a significant individual variability). Bioavailability is 4%. The time to reach C max (maximum concentration) in blood plasma is 60–90 minutes after taking the drug. Buspirone has a linear (dose-proportional) pharmacokinetics (clinical trials were carried out at a dose of 10–40 mg). Pharmacokinetic parameters in elderly patients do not change. Plasma concentration after a single dose of 20 mg of buspirone is 1–6 ng / ml.
The absorption of the substance when taken simultaneously with food slows down, but due to a decrease in the pre-systemic clearance (first-pass effect), the bioavailability of buspirone increases significantly. After ingestion, the AUC value (area under the concentration-time curve) increases by 84%, C max - by 16%.
The binding of the substance to blood plasma proteins is about 95% (86% binds to plasma albumin, the rest - to acidic α 1 -glycoprotein).
C ss (steady-state concentration) in blood plasma is reached approximately 2 days after the start of regular intake. The apparent V d (volume of distribution) is 5.3 l / kg.
There are no data on the penetration of buspirone through the placental barrier. Excreted in breast milk.
The oxidative metabolism of buspirone occurs with the participation of CYP3A4 isoenzymes with the formation of various hydroxylated metabolites. The main metabolite (5-OH-buspirone) is not active. The dealkylated metabolite [1- (2-pyrimidinyl) -piperazine, 1-PP] is active. Its anxiolytic activity is 4-5 times lower than that of the parent substance, but its plasma blood level is higher and T 1/2 (half-life) is about 2 times longer than that of buspirone.
It is excreted in the urine for 24 hours, mainly in the form of metabolites. Approximately 18–38% of the dose is excreted in the feces. T 1/2 of the initial substance after a single dose of 10-40 mg is about 2-3 hours, and T 1/2 of the active metabolite is 4.8 hours.
In case of impaired liver function, an increase in T 1/2 and a plasma increase in buspirone concentration and AUC values are possible. Due to the release of unchanged substance into bile, a second peak in the plasma concentration of buspirone in the blood can be observed. In case of liver cirrhosis, it is necessary to prescribe Spitomin in lower doses or to increase the interval between single doses.
The clearance of buspirone in renal failure can be reduced by 2 times, in this regard, Spitomin should be prescribed under medical supervision in reduced doses.
Indications for use
- alcohol withdrawal syndrome (as adjuvant therapy);
- generalized anxiety disorder;
- autonomic dysfunction syndrome;
- panic disorder;
- depressive disorders (as an auxiliary therapy, Spitomin is not prescribed as monotherapy).
Contraindications
Absolute:
- severe renal failure (glomerular filtration rate <10 ml / min);
- severe hepatic impairment (prothrombin time> 18 sec);
- myasthenia gravis;
- glaucoma;
- combination therapy with MAO (monoamine oxidase) inhibitors, or a period of 1 day after discontinuation of a reversible MAO inhibitor, or a period of 14 days after discontinuation of an irreversible MAO inhibitor;
- age up to 18 years;
- pregnancy or suspicion of it, lactation period;
- individual intolerance to the components of the drug.
Relative (Spitomin tablets are prescribed under medical supervision):
- renal failure;
- cirrhosis of the liver;
- elderly age.
Instructions for the use of Spitomin: method and dosage
Spitomin tablets are taken orally before or after meals. To avoid significant fluctuations in the plasma concentration of buspirone in the blood throughout the day, the drug must always be taken at the same time of the day.
Spitomin should not be used sporadically for the treatment of anxiety, since the therapeutic effect develops only after repeated administration and does not appear earlier than on the 7-14th day of therapy.
The scheme for using Spitomin is determined by the doctor individually. The daily dose is taken in 2-3 doses.
It is recommended to start treatment with 15 mg per day, every 2-3 days the dose can be increased by 5 mg. The maximum single dose should not exceed 30 mg. The daily dose is: usual - from 20 to 30 mg, maximum - 60 mg.
In case of impaired renal / liver function, Spitomin should be used with caution and in reduced doses (a decrease in a single dose or an increase in the interval between doses is shown).
Side effects
In most cases, Spitomin is well tolerated. Adverse reactions usually appear at the beginning of the course of admission and then disappear on their own. Some patients may need dose reduction.
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):
- laboratory parameters: infrequently - increased serum alanine aminotransferase and aspartate aminotransferase activity; rarely - leukopenia, eosinophilia, thrombocytopenia;
- skin and subcutaneous tissues: infrequently - dry skin, edema, hot flashes, itching, hair loss, skin fragility, facial swelling, rash;
- nervous system: often - sleep disturbances, headache, dizziness, increased nervous irritability; infrequently - depersonalization, dysphoric reactions, increased sensitivity to noise, dysphoria, euphoria, hyperkinesis, suicidal thoughts, fear, apathy, hallucinations, confusion, epileptic seizures, prolonged reaction time, impaired coordination of movements, paresthesia, tremor; rarely - psychotic disorders, stupor, claustrophobia, cold intolerance, extrapyramidal disorders, stuttering;
- cardiovascular system: often - chest pain; infrequently - arterial hypertension, arterial hypotension, fainting; rarely - bradycardia, decompensation of heart failure, cerebrovascular accident, myocardiopathy, myocardial infarction;
- respiratory system: often - swelling of the nasal mucosa, laryngitis; infrequently - lack of air, hyperventilation, a feeling of heaviness in the chest; rarely - nosebleeds;
- sense organs: often - tinnitus; infrequently - itchy eyes, blurred vision, conjunctivitis, redness of the eyes, impaired olfactory / taste sensations; rarely - photophobia, eye pain, inner ear disorders, increased intraocular pressure;
- endocrine system: rarely - galactorrhea, thyroid gland damage;
- musculoskeletal system: infrequently - muscle stiffness, muscle spasms, arthralgia; rarely - pain in bones and muscles, muscle weakness;
- urinary system: infrequently - dysuria (including urinary retention, urinary frequency); rarely - bedwetting;
- digestive system: infrequently - anorexia, nausea, flatulence, salivation, increased appetite, intestinal bleeding; rarely - burning of the tongue, diarrhea;
- reproductive system: infrequently - decreased sex drive, menstrual irregularities; rarely - pelvic inflammatory disease, amenorrhea, delayed ejaculation, impotence;
- others: fever, weight gain / loss; rarely - loss of voice, alcohol abuse, hiccups, tinnitus.
Overdose
The main symptoms are: depression of consciousness of varying severity, gastrointestinal disturbances, vomiting, nausea, dizziness and drowsiness.
Dialysis is ineffective; specific antidote is unknown. Symptomatic therapy and gastric lavage are indicated. According to available data, taking even very high doses of Spitomin (375 mg once) does not always lead to the development of severe symptoms.
special instructions
Due to a possible decrease in renal / liver function and an increased likelihood of developing adverse reactions, Spitomin should be used with caution in elderly patients. The drug is prescribed in the minimum effective dose; with its increase, the patient's condition should be closely monitored.
During the period of therapy, the use of grapefruit / grapefruit juice is not recommended, since this can lead to an increase in the plasma concentration of buspirone in the blood and an increase in the severity or frequency of side effects.
Patients with a suspected / established predisposition to drug dependence require careful medical supervision.
When transferring patients from benzodiazepines to Spitomin, it is necessary to take into account that buspirone cannot eliminate the symptoms of benzodiazepine withdrawal. Spitomin should be prescribed only after the end of the period of gradual dose reduction of benzodiazepines.
For the entire period of therapy, alcohol consumption should be abandoned.
In the initial period of therapy, patients with severe anxiety need careful medical supervision, since the Spitomin effect develops gradually (up to 4 weeks).
In patients with lactose intolerance, when drawing up a diet, it is necessary to take into account the lactose content in Spitomin (in tablets of 5 or 10 mg - 55.7 or 111.4 mg, respectively).
Influence on the ability to drive vehicles and complex mechanisms
The ability to drive vehicles is determined individually, depending on the use of concomitant therapy and the patient's response to Spitomin.
Application during pregnancy and lactation
According to the instructions, it is contraindicated to take Spitomin during pregnancy / lactation.
During the course of treatment, women of childbearing age should use adequate methods of contraception.
Pediatric use
Therapy with Spitomin is contraindicated in patients under 18 years of age (due to the lack of clinical experience with the drug).
With impaired renal function
Contraindication: severe renal failure (glomerular filtration rate <10 ml / min).
For violations of liver function
Contraindication: severe hepatic impairment (prothrombin time> 18 sec).
Use in the elderly
Spitomin for elderly patients should be prescribed under medical supervision.
Drug interactions
There is a high probability of interaction of Spitomin with other drugs, which is associated with low bioavailability, intense metabolism in the liver, high protein binding. However, buspirone has a significant therapeutic breadth, therefore pharmacokinetic interactions do not lead to clinically significant pharmacodynamic changes.
Combination therapy of Spitomin with MAO inhibitors, or the use of the drug within one day after discontinuation of a reversible MAO inhibitor, or a period of 14 days after discontinuation of an irreversible monoamine oxidase inhibitor is contraindicated. This is due to the likelihood of an increase in blood pressure and the occurrence of hypertensive crises.
Other possible interactions:
- CYP3A4 inhibitors (erythromycin, itraconazole, nefazodone, diltiazem, verapamil and grapefruit juice): an increase in the plasma concentration of buspirone in the blood (a decrease in the buspirone dose is required);
- strong inducers of CYP3A4 (rifampicin): a significant decrease in the plasma concentration of buspirone in the blood and a weakening of its pharmacodynamic effects;
- drugs with a low degree of binding to proteins (digoxin): their displacement by buspirone from the sites of binding to proteins;
- cimetidine: a significant increase in the C max of buspirone (careful medical supervision is required);
- diazepam: a slight increase in the concentration of nordiazepam and the appearance of the likelihood of side effects - systemic dizziness, headache, nausea;
- alcohol, central nervous system depressants, antihypertensive drugs, cardiac glycosides, oral contraceptives and hypoglycemic agents: the interaction has not been studied, therefore the combined use should be carried out under close medical supervision.
Analogs
There is no information about Spitomin's analogues.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 30 ° C. Keep out of the reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Spitomin
Reviews about Spitomin are different. In some cases, it is noted to be highly effective in the treatment of anxiety and insomnia. However, they often indicate an insufficient therapeutic effect and the development of pronounced side effects, which become the reason for drug withdrawal.
The price of Spitomin in pharmacies
The approximate price for Spitomin (60 pcs. In a package) is 581-635 rubles.
Spitomin: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Spitomin 10 mg tablets 60 pcs. RUB 616 Buy |
|
Spitomin tablets 10mg 60 pcs. 764 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
