Spitomin 10mg 60 tablets — Made in Hungary — Free Delivery

Pharmacological properties

Pharmacodynamics. Buspirone is an anxiolytic agent and is used to treat anxiety states of various origins, especially neuroses, accompanied by feelings of anxiety, anxiety, tension, irritability.

The mechanism of the anxiolytic effect of buspirone and other azaspirodecandione derivatives differs from that of benzodiazepines. Buspirone does not act on the benzodiazepine-GABA-chloride-ionophore receptor complex; however, since it is a partial agonist of 5-HT1A receptors, it acts by modulating the serotonergic system. This effect leads to inhibition of 5-HT renewal and a decrease in the frequency of inflammation of 5-HT neurons in the dorsal suture nuclei. Buspirone exhibits a high affinity for presynaptic 5-HT1A receptors and is a partial agonist of postsynaptic 5-HT1A receptors in the central nervous system. The presence in buspirone of properties typical of anxiolytics and antidepressants was established.

Buspirone does not show significant activity against benzodiazepine receptors and does not affect the binding of GABA. Unlike benzodiazepines, buspirone does not have muscle relaxant or anticonvulsant properties. Unlike benzodiazepines, buspirone does not induce tolerance or dependence, and withdrawal symptoms do not develop after completion of treatment. The action of buspirone develops gradually. The therapeutic effect begins to manifest itself between the 7th and 14th day of therapy, and the maximum effect is achieved only after 4 weeks of treatment.

Pharmacokinetics. After oral administration, the preparation is rapidly and almost completely absorbed in the digestive tract. Buspirone undergoes intensive first pass metabolism through the liver. Therefore, the unchanged substance is detected in the systemic circulation at a low concentration.

Bioavailability is 4%. Cmax in blood plasma is achieved within 60–90 minutes after taking the preparation. The main metabolite is inactive, the dealkylated metabolite is active. Its anxiolytic activity is 4–5 times lower than that of the original substance, but its level in blood plasma is higher and T½ is about 2 times longer than that of buspirone. About 29–63% of buspirone is excreted in the urine within 24 hours, mainly in the form of metabolites. About 18–38% of the dose taken is excreted in the feces. T½ from blood plasma is about 2-3 hours.

Simultaneous food intake slows down the absorption of buspirone in the digestive tract.

Equilibrium concentration in blood plasma is achieved 2 days after repeated use of the preparation.

Buspirone passes into breast milk. There are no data on the penetration of buspirone through the placenta.

Elevated levels of buspirone in blood plasma and AUC value, as well as an increase in T½ can be observed with impaired liver function. Due to the release of unchanged compound with bile, a second peak may appear in the plasma levels of buspirone. Patients with cirrhosis of the liver should receive lower individual doses or the same dose, but less frequently.

Renal failure can reduce buspirone clearance by 50%. In patients with renal insufficiency, buspirone should be prescribed with caution and in reduced doses.

In elderly patients, the pharmacokinetics of buspirone does not change.

Indications

Symptomatic treatment of anxiety states with dominant symptoms: anxiety, inner anxiety, tension.

Application

Doses are determined by the doctor individually for each patient, depending on the course of the disease. at the beginning of therapy, 5 mg of buspirone hydrochloride is prescribed 2-3 times a day. to achieve the maximum therapeutic effect, the daily dose is gradually increased to 20-30 mg of buspirone, distributed over several separate doses.

The maximum single dose should not exceed 30 mg.

The maximum daily dose should not exceed 60 mg.

Food increases the bioavailability of buspirone. The tablets should be taken at the same time of the day, without chewing, with a small amount of liquid, after meals or with or without food.

If it is necessary to distribute the tablet into two halves, place it on a hard surface with a notch up and press lightly with your thumb.

If buspirone is used together with a potent inhibitor of CYP 3A4, its initial dose should be reduced and gradually increased only after a medical examination of the patient.

Special patient groups. The available data do not indicate the advisability of changing the dosage regimen depending on the age and gender of the patient.

Renal failure

In case of mild and moderate renal failure (creatinine clearance 20–49 ml / min / 1.72 m2), a single use of buspirone causes an increase in its level in blood plasma without an increase in T½. For these patients, it is recommended to use buspirone with caution and in smaller doses, take 2 times a day. The patient's response to treatment and symptoms must be carefully monitored before increasing the dose. In patients with anuric syndrome, a single use of the preparation leads to an increase in the level of the metabolite 1-pyrimidine / piperazine (1-PP) in the blood, in them dialysis had no effect on the content of either buspirone or 1-PP. Buspirone should not be used in patients with a creatinine clearance of 20 ml / min / 1.72 m2, especially with anuric syndrome, due to the possibility of an increase in the level of buspirone and its metabolites.

Liver failure

The use of preparations such as buspirone for the treatment of patients with impaired liver function demonstrates a reduced effect of the first passage of preparations through the liver. With cirrhosis of the liver, a single use of buspirone causes an increase in the level of its unchanged form in the blood plasma with an increase in T½. For these patients, it is recommended to use buspirone with caution and after individual titration of doses to reduce the risk of serious adverse reactions that may occur due to the use of buspirone in high doses. Increasing doses should be considered after careful examination of the patient and only 4–5 days after the previous dose.

Duration of treatment. Tranquilizers should not be used without supervision for a long time. Therefore, the duration of treatment with buspirone 5 mg and / or 10 mg should not exceed 4 months. Doses are determined individually for each patient, depending on the condition of the disease. If long-term use of the preparation is necessary (up to 6 months), careful medical monitoring should be carried out.

It should be remembered about psycho- and socio-therapeutic measures in parallel with treatment with buspirone.

Contraindications

Hypersensitivity to buspirone or other components of the preparation. acute congestive glaucoma, myasthenia gravis, severe liver disease, severe liver failure (prothrombin time 18 s), severe renal failure (glomerular filtration rate 10 ml / min), epilepsy, acute alcohol intoxication, hypnotics, analgesics and antipsychotics.

Concomitant treatment with MAO inhibitors and within 14 days after discontinuation of an irreversible MAO inhibitor or within 1 day after discontinuation of a reversible MAO inhibitor.

Side effects

Side effects usually occur at the beginning of treatment, their severity usually decreases with prolonged use. in some cases, a dose reduction is necessary. Adverse reactions from the nervous system, such as dizziness, insomnia, nervousness, drowsiness, and fainting were more common; from the digestive tract, such as nausea, as well as other unwanted effects, such as headache and increased fatigue.

Less often, anger and hostility, confusion, blurred vision, diarrhea, pain in muscles and bones, numbness, paresthesia, impaired coordination of movements, tremors and skin rashes, dry mouth, weakness, asthenia, increased sweating, clammy skin were detected.

Adverse reactions are classified by frequency of occurrence: very often (≥1 / 10); often (≥1 / 100, 1/10); infrequently (≥1 / 1000, 1/100); rarely (≥1 / 10,000, 1/1000); very rare (1/10 000); the frequency is unknown (cannot be estimated due to lack of data).

Infections and invasions: frequency unknown - fever.

From the side of the cardiovascular system: often - nonspecific chest pain; infrequently - temporary loss of consciousness, arterial hypotension and / or hypertension, tachycardia / palpitations; rarely - cerebrovascular accident, heart failure, myocardial infarction, cardiomyopathy, bradycardia, cerebrovascular disorders.

From the side of the blood system: rarely - changes in blood parameters (eosinophilia, leukopenia, thrombocytopenia).

Mental disorders: often - nightmares, drowsiness, insomnia, dizziness, nervousness, decreased concentration, emotional excitement, irritability, hostility, confusion, depression; infrequently - depersonalization, discomfort, pathologically increased perception of ordinary sounds, euphoria, hyperkinesia, anxiety, loss of interest, impaired associative perception, hallucinations, suicidal thoughts, epileptic seizures, dysphoria, fear; rarely - sudden mood swings, claustrophobia, stupor, slurred speech, transient memory problems, serotonin syndrome, psychosis.

From the nervous system: infrequently - numbness, paresthesia (for example, tingling, pain), impaired coordination, tremor, epileptic seizures, dysgeusia, dysosmia, prolonged reaction time; rarely - spontaneous movements, lethargy, extrapyramidal symptoms, including early and tardive dyskinesia, disturbances in tone, fever, parkinsonism, akathisia, noise in the head.

From the side of the organ of vision: often - blurred vision; infrequently - redness and itching in the eye area, conjunctivitis; rarely - photophobia, a feeling of pressure on the eyes, pain in the eyes, narrowed field of vision, increased intraocular pressure.

From the side of the organ of hearing: often - tinnitus; rarely - damage to the inner ear.

From the respiratory system: often - sore throat, nasal congestion; infrequently - excessive breathing, shortness of breath, tightness in the region of the heart, hyperventilation, feeling of lack of air; rarely - nosebleeds, burning sensation of the tongue.

From the digestive tract: often - nausea, xerostomia, pain in the epigastric region, diarrhea; infrequently - flatulence, lack of appetite, increased appetite, hypersalivation, irritable bowel syndrome, rectal bleeding, constipation, vomiting.

From the urinary system: infrequently - frequent urination, urinary retention, dysuria; rarely - enuresis, nocturnal urination.

On the part of the skin: infrequently - edema, urticaria, hyperemia, hematomas, baldness, dry skin, eczema, facial edema, pemphigus, hot flashes, skin vulnerability, skin rashes, itching; rarely - allergic reactions, ecchymosis, acne, thinning of nails.

From the musculoskeletal system: infrequently - muscle spasm and stiffness, myalgia, arthralgia; rarely - myasthenia gravis.

From the endocrine system: rarely - galactorrhea, gynecomastia, thyroid dysfunction.

Metabolic disorders: infrequently - anorexia, increased appetite; frequency unknown - increase in body weight, decrease in body weight.

General disorders: often - headache, asthenia; infrequently - fever, ringing in the head, malaise, increased fatigue, impaired sense of smell and taste, increased sweating, hot flashes, cold hyperesthesia; rarely - a tendency to abuse alcohol, blood coagulation disorders, loss of voice, hiccups, glossalgia.

From the hepatobiliary system: infrequently - an increase in hepatic enzymes.

Reproductive system disorders: infrequently - menstrual irregularities, decreased or increased libido; rarely - amenorrhea, inflammation of the genitourinary organs, decreased ejaculation, impotence.

Laboratory tests: increase in the level of transaminases in the blood plasma.

Special instructions

Liver failure. buspirone is extensively metabolized in the liver. in a pharmacokinetic study, the use of buspirone in a single dose of 30 mg to patients with liver cirrhosis increased the level of buspirone in the blood plasma, increased the auc value and lengthened t½ buspirone. due to the excretion of the substance into bile, a second peak in the concentration of buspirone in the blood plasma is possible. the use of the preparation  is contraindicated in patients with severe hepatic impairment. patients with cirrhosis of the liver should be prescribed the preparation in lower doses or at the same doses, but with an extended interval.

Renal failure In moderate or severe renal failure, the clearance of buspirone can be reduced by 50%. The preparation is contraindicated in patients with severe renal failure (GFR 10 ml / min). With mild (GFR 30 ml / min) and moderate (GFR = 10-30 ml / min) renal failure, buspirone can be prescribed, however, caution should be exercised and reduced doses should be prescribed.

Elderly patients. Dose changes are not required, however, caution should be exercised when using the preparation (for example, due to a possible decrease in renal and / or liver function and an increased sensitivity to side effects of the preparation). Patients should be prescribed the lowest effective dose, and if the dose is increased, the patient should be closely monitored.

Patients should be advised not to eat grapefruit or drink large amounts of grapefruit juice during treatment, as these products can increase the plasma level 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 benzodiazepine withdrawal symptoms. If the patient is transferred to buspirone therapy after prolonged benzodiazepine therapy, buspirone should be prescribed only after the end of the period of gradual dose reduction of benzodiazepines.

Buspirone is not addictive to the preparation, but its use in patients with known or suspected preparation dependence requires careful medical supervision.

Since the anxiolytic effect of the preparation appears after 7-14 days of use, and the full therapeutic effect develops after 4 weeks, patients with severe anxiety require careful medical supervision at the initial stage of therapy.

During the course of treatment with buspirone, alcoholic beverages should be avoided.

In patients with lactose intolerance, the diet should take into account the lactose content of the tablets (55.7 mg in 5 mg tablets and 111.4 mg in 10 mg tablets).

The preparation Spitomin contains lactose, so it should not be prescribed to patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.

Clinical and experimental studies have not revealed any signs that buspirone leads to the risk of addiction or dependence, however, the prescription of the preparation must be justified.

Buspirone is not intended to treat withdrawal symptoms associated with benzodiazepines or other sedatives / hypnotics. Therefore, before starting treatment with buspirone, the use of these preparations should be gradually discontinued. This is especially true for patients taking preparations that depress the central nervous system.

The combination of buspirone with MAO inhibitors is not recommended.

There have been reports of an increase in blood pressure with the simultaneous use of these preparations.

Do not prescribe buspirone to patients with a history of epileptic seizures.

Long term toxicity. Since the mechanism of action is not fully understood, long-term toxic effects on the central nervous system or other organ systems cannot be anticipated.

Use during pregnancy and lactation. There are no data on the use of buspirone during pregnancy, so the preparation can be prescribed only when the expected benefit to the pregnant woman outweighs the potential risk to the fetus. Buspirone passes into breast milk, so breastfeeding should be discontinued for the period of treatment.

Children. Buspirone is not prescribed for children due to the lack of data on safety and efficacy.

The ability to influence the reaction rate when driving or working with other mechanisms. During treatment, one should refrain from driving vehicles or working with other mechanisms, since adverse reactions from the central nervous system and psyche may occur.

Interactions

Due to the lack of relevant clinical data, the combined use of buspirone with antihypertensive, antipsychotic preparations, antidepressants, hypoglycemic agents, anticoagulants, oral contraceptives and cardiac glycosides is possible only under close medical supervision. buspirone should not be used concomitantly with benzodiazepines and other sedatives.

The combination with MAO inhibitors is not recommended due to the risk of hypertensive crisis. Since buspirone is mainly metabolized by cytochrome P450, potent inhibitors of this enzyme can increase the bioavailability of buspirone.

Nefazodone. The simultaneous use of buspirone and nefazodone led to an increase in Cmax of buspirone in blood plasma by 20 times and AUC by 50 times.

Erythromycin. The simultaneous use of buspirone and erythromycin led to an increase in buspirone Cmax by 5 times and AUC by 6 times.

Itraconazole. The simultaneous use of buspirone and itraconazole led to an increase in buspirone Cmax by 13 times and AUC by 19 times.

Diltiazem. The simultaneous use of buspirone and diltiazem led to an increase in buspirone Cmax by 4 times and AUC by 5.3 times.

Verapamil. The simultaneous use of buspirone and verapamil led to an increase in Cmax and AUC of buspirone by 3.4 times.

Cimetidine. The simultaneous use of buspirone and cimetidine led to an increase in the Cmax of buspirone by 40%, Tmax - twice, but the AUC practically did not change.

When using buspirone together with the aforementioned agents, the severity of the therapeutic effect increases and the toxicity of buspirone increases, therefore it is recommended to reduce the dose of buspirone (for example, 2.5 mg 2 times a day).

Rifampicin. The simultaneous use of buspirone and rifampicin led to a decrease in buspirone Cmax by 83.9% and AUC by 89.6%.

Inhibitors and inducers of CYP 3A4. Ketoconazole or ritonavir inhibits the metabolism of buspirone and increases its plasma levels.

If buspirone is used together with a CYP 3A4 inhibitor, it is recommended to reduce its dose.

CYP 3A4 inducers, such as dexamethasone, phenytoin, phenobarbital, or carbamazepine, can increase the metabolic rate of buspirone. In this case, it is necessary to increase the dose of buspirone to maintain its anxiolytic efficacy.

Serotonin reuptake inhibitors. Not a single case of dangerous use of buspirone with antidepressants, selective serotonin reuptake inhibitors has been identified. There have been separate reports of the occurrence of seizures during their long-term use with buspirone.

Haloperidol. The simultaneous use of buspirone and haloperidol led to an increase in the concentration of haloperidol in blood plasma.

Trazodone. It is reported that in some patients, while using trazodone with buspirone, the activity of ALT increased by 3 times. However, such an increase in hepatic transaminases has not been confirmed by clinical studies.

Diazepam. With the simultaneous use of diazepam and buspirone, the level of the former in the blood plasma increases slightly, and side effects may also occur: dizziness, headache, nausea.

During treatment with buspirone, you should refrain from drinking alcoholic beverages.

Patients are not advised to consume large amounts of grapefruit juice during treatment, as this can lead to an increase in the level of buspirone in the blood plasma and an increase in the frequency or severity of side effects.

Overdose

Symptoms: nausea, vomiting, dizziness, drowsiness, fatigue, miosis, gastrointestinal disturbances, loss of consciousness. severe complications were not noted even when taking a daily dose of up to 2400 mg.

Treatment: gastric lavage, monitoring of respiration, pulse, blood pressure. Symptomatic therapy. There is no specific antidote. Buspirone is not excreted by hemodialysis. Based on experience with the preparation, overdose with high doses (single dose of 375 mg orally) does not necessarily cause severe symptoms.

Storage conditions

At a temperature not exceeding 30 ° C in a dark place.