Medicine form
Pills.
Main physical and chemical authorities:
5 mg tablets:
white or slightly white, round, chamfered tablets with engraved stylistic lettering E and the numbers 151 on one side and on the other side, odorless or with a faint characteristic odor;
10 mg tablets:
white or slightly white, round, bevelled tablets, engraved with stylistic letters E and the numbers 152 on one side and on the other side, odorless or with a faint characteristic odor.
There is a risk of serving less for breaking the tablets with the method of easier puncturing, and not for dividing them at the same dose.
Pharmacological authorities
Pharmacodynamics.
Buspiron has an anxiolytic effect and is used to treat anxious conditions of various movements, especially neuroses, which are accompanied by anxiety, restlessness, tension, and restlessness. The mechanism of the anxiolytic effect of buspirone and other similar azaspirodecandiones is similar to the mechanism of action of benzodiazepines. The smell does not affect the benzodiazepine-GABA-chloride-ionophore receptor complex; However, some of the smells are partial agonists of 5-HT1A receptors, they act as modulation of the serotonergic system. This effect leads to a suppression of 5-HT renewal and a decrease in the frequency of firing of 5-HT neurons in the dorsal raphe nuclei. Buspirone exhibits high affinity for presynaptic 5-HT1A receptors and is a partial agonist of postsynaptic 5-HT1A receptors in the central nervous system. Buspirone has been found to have effects typical of anxiolytics and antidepressants.
Buspirone does not exhibit significant activity at benzodiazepine receptors and does not interact with GABA binding. When substituted with benzodiazepines, buspirone does not exhibit muscle relaxant or anti-inflammatory properties. When used as a substitute for benzodiazepines, buspirone does not cause tolerance or persistence, and after completion of the treatment course, withdrawal symptoms do not develop. The action of buspirone develops step by step. The therapeutic effect begins to appear between 7 and 14 days of therapy, and the maximum effect is achieved after only 4 treatments.
Pharmacokinetics.
After oral administration, the drug is completely absorbed through the intestinal tract. Buspirone undergoes intensive metabolism after first passing through the liver. Therefore, invariably, low concentrations of resin are detected in the systemic bloodstream, which may have significant individual differences.
Bioavailability becomes 4%. The maximum concentration in blood plasma is achieved 60-90 weeks after taking the drug. The main metabolite is inactive, the dealkylated metabolite is active. Its anxiolytic activity is lower in 4-5 times, lower in the coba pharyngeal tract, and its level in blood plasma is higher and the period of replenishment is approximately 2 times longer, lower in buspirone. Approximately 29-63% of buspirone is visible after 24 years, mainly in the form of metabolites. Approximately 18-38% of the administered dose is excreted in feces. The period of replacement with blood plasma is approximately 2-3 years.
One-hour administration of hedgehogs enhances the absorption of buspirone from the herbal tract.
The equivalent concentration in blood plasma is achieved approximately 2 hours after repeated dosing of the drug.
Buspirone passes into breast milk. Data on the penetration of buspirone across the placenta every day.
An increase in the blood plasma AUC value equal to buspirone, as well as a prolonged dosing period, can be avoided in case of impaired liver function. Once you see the unchanged half of the heat in the plasma levels of buspirone, another peak may appear. Patients with cirrosis of the liver should take lower individual doses or the same doses, or less.
Nircov deficiency may reduce buspirone clearance by 50%. Patients with nicotine deficiency should be prescribed buspirone with caution and in reduced doses. In elderly patients, the pharmacokinetics of buspirone does not change.
Side effects of Spitomina
“Spitomin” does not always receive a positive review, and this is due to its ability to cause some unwanted reactions in the body. Usually the drug is well tolerated by the patient, but sometimes side effects may occur. If they develop, this usually happens at the very beginning of therapy; side effects disappear on their own. A reduction in the prescribed dosage is rarely required.
A person may experience sleep problems, a significant increase in nervous excitability and headaches. In very rare cases, extrapyramidal disorder may occur. Changes in the functioning of the digestive system are possible, these are various dyspeptic phenomena, for example, nausea with vomiting, poor appetite.
In case of an overdose of the drug "Spitomin", the review of many specialists confirms the need to perform gastric lavage and provide therapy aimed at eliminating this condition. There is no antidote, there is no effect from dialysis.
Contraindicated
Increased sensitivity to buspirone or other components of the drug. Gostra congestive glaucoma, myasthenia gravis
, severe liver disease, severe liver failure (prothrombin hour more than 18 seconds); severe nitric deficiency (glomerular filtration rate less than 10 ml/h), epilepsy, acute intoxication with alcohol, drugs, analgesics and antipsychotics.
Concomitant treatment with monoamine oxidase (MAO) inhibitors for 14 days after the replacement of the non-circulating MAO inhibitor or for 1 day after the replacement of the circulating MAO inhibitor.
Interactions with other medicinal drugs and other types of interactions
Due to the lack of reliable clinical data, the combination of buspirone with antihypertensive, antipsychotic drugs, antidepressants, antidiabetic drugs, anticoagulants, oral contraceptives and cardiac glycosides may also be considered. corporal medical care. Buspirone cannot be combined with benzodiazepines or other sedatives.
Combination with MAO inhibitors is not recommended due to the risk of hypertensive crisis. The fragments of buspirone are primarily metabrized by cytochrome P450, a strong inhibitor of this enzyme can increase the bioavailability of buspirone.
Nefazodone.
Simultaneous administration of buspirone and nefazodone resulted in an increase in the maximum concentration of buspirone in blood plasma (Cmax) in 20 times and an area under the concentration-hour curve (AUC) in 50 times.
Erythromycin.
Simultaneous administration of buspirone and erythromycin resulted in an increase in Cmax of buspirone in 5 times and AUC in 6 times.
Itraconazole
Simultaneous administration of buspirone and itraconazole resulted in an increase in buspirone Cmax in 13 cases and AUC in 19 cases.
Diltiazem.
Simultaneous administration of buspirone and diltiazem resulted in an increase in buspirone Cmax by 4 times and AUC by 5.3 times.
Verapamil
Immediate administration of buspirone and verapamil resulted in a 3.4-fold increase in Cmax and AUC of buspirone.
Cimetidine.
Simultaneous administration of buspirone and cimetidine resulted in an increase in Cmax of buspirone by 40%, tmax in both patients, but AUC practically did not change.
When buspirone is administered simultaneously with essential drugs, the therapeutic effect and toxicity of buspirone increases, it is recommended to reduce the dose of buspirone (for example, 2.5 mg 2 times per dose).
Rifampicin.
Simultaneous administration of buspirone and rifampicin resulted in a change in Cmax of buspirone by 83.9% and AUC by 89.6%.
Inhibitors and inducers of CYR3A4.
Ketoconazole or ritonavir inhibit the metabolism of buspirone and increase its plasma levels.
If buspirone is administered simultaneously with a CYR3A4 inhibitor, it is recommended to change the dose.
CYR3A4 inducers, such as dexamethasone, phenytoin, phenobarbital or carbamazepine, may increase the fluidity of buspirone metabolism. In this case, it is necessary to increase the dose of buspirone to preserve its anxiolytic effectiveness.
Inhibitors of serotonin secretion
There was no evidence of unsafe use of buspirone in combination with antidepressants or selective inhibitors of renal neuronal uptake of serotonin. There were reports about the occurrence of attacks when they were taken together with buspirone.
Haloperidol
Simultaneous administration of buspirone and haloperidol led to an increase in the concentration of haloperidol in the serum.
Trazodone.
It was reported that in some patients, with a one-hour infusion of trazodone with buspirone, ALT activity increased 3 times. However, such elevation of liver transaminases has not been confirmed by clinical studies.
Diazepam.
With one-hour ingestion of diazepam and buspirone, the level of blood plasma increases significantly, and side effects may also occur: confusion, headache, boredom.
At the hour of treatment with buspirone, the traces of alcoholic drinks are eliminated.
Patients are not recommended to drink grapefruit juice in large quantities during bathing ,
The fragments may lead to an increase in the level of buspirone in blood plasma and an increase in the frequency and severity of side effects.
Features of good stagnation
Pechinkov's lack of availability.
Buspirone is characterized by intensive metabolism in the liver. In the pharmacokinetic study, the administration of buspirone in a single dose of 30 mg in patients with liver cirrhosis was similar to buspirone in blood plasma, the AUC value increased and the period of administration of buspirone was prolonged. The increase in excretion of speech in females may differ from the peak in the concentration of buspirone in the blood plasma. The use of the drug is contraindicated for those suffering from severe liver failure. Patients with liver cirrosis should be prescribed the drug at lower doses or at the same doses, rather than at a shorter interval.
Nirkova lack of availability.
In mild or severe nitric deficiency, buspirone clearance may be reduced by 50%. The drug has contraindications: we suffer from severe nitric deficiency (glomerular filtration rate (GFR) ˂ 10 ml/xv). In case of mild (GFR = 30 ml/xv) and moderate (GFR = 10-30 ml/xv) nitric deficiency, buspirone can be prescribed, but in this case it is necessary to reduce the dose.
Summer age patients.
There is no need to specify the dose, however, caution must be exercised when stagnating the drug (for example, due to possible decreased function of the liver and/or liver and increased sensitivity to side effects of the drug). Patients should be prescribed the lowest effective dose, and the patient should be closely monitored as the dose increases.
Patients should be advised not to eat grapefruit or drink grapefruit juice during bathing hours, as these products may increase the level of buspirone in blood plasma and increase the frequency of either severity of side effects.
Transferring patients from benzodiazepines to buspirone. Buspirone cannot relieve symptoms of benzodiazepine withdrawal. If a patient is transferred to buspirone therapy after a previous benzodiazepine therapy, buspirone should be started only after the benzodiazepine dose reduction period has been completed.
Buspirone does not interfere with the use of the drug, however, its administration to patients with known or suspected sensitivity to medication will require careful medical supervision.
Although the anxiolytic effect of the drug appears after 7-14 days of stagnation, and the final therapeutic effect develops after approximately 4 days, patients with severe anxiety will require close medical supervision at the initial stage of therapy.
The continuation of the course of treatment with buspirone will lead to the elimination of the addiction to alcoholic beverages.
In patients with lactose intolerance and a complex diet, take the tablets instead of lactose (55.7 mg for 5 mg tablets and 111.4 mg for 10 mg tablets).
The drug Spitomin® is lactose-absorbent and should not be prescribed to patients with rare spasmodic forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
Clinical and experimental studies have not revealed any sign that buspirone may lead to a risk of accumulation or retention, but the drug may be priming.
Buspirone is not indicated for the treatment of withdrawal symptoms associated with benzodiazepines or other sedatives/drugs. Therefore, before starting treatment with buspirone, gradually begin to stagnate these drugs. This is especially problematic for patients who are taking medications that depress the central nervous system.
The combination of buspirone with MAO inhibitors is not recommended. There was information about the displacement of arterial pressure during one-hour ingestion of these drugs.
Patients with a history of epilepsy attacks should not be prescribed buspiron.
Long-term toxicity
. The fragments of the mechanism of action are completely unrelated, the toxic influx into the central nervous system and other organ systems cannot be transferred.
Suspension during pregnancy or breastfeeding.
Given that buspirone has been used during pregnancy during the day, the drug can be prescribed only when the vaginal cortex has been extracted and the potential sac for the fetus has been increased. Buspirone passes into breast milk, so it should be applied to the breast during the bathing period.
This is due to the fluidity of the reaction during treatment with vehicles or other mechanisms.
During the hour of treatment, the traces should be avoided due to treatment by motor transport or robots with other mechanisms, as there may be adverse reactions on the side of the central nervous system and psyche (div. section “Adverse reactions” ї").
Method of congestion and dosage
The dosage is determined by the doctor individually for the skin patient who is about to become ill. For initial therapy, prescribe 5 mg buspirone hydrochloride 2-3 times per dose. To achieve the maximum therapeutic effect, the additional dose should be incrementally increased to 20-30 mg of buspirone, divided into smaller doses.
The maximum single dose is 30 mg.
The maximum additional dose is 60 mg.
It increases the bioavailability of buspirone. The tablets should be taken each time at the same hour of the day, without being chewed, washed down with a small amount of ripe, before or after taking it.
If necessary, divide the tablets into two halves, place them on a hard surface at risk of burning, and press lightly with your thumb.
If buspirone is administered simultaneously with a strong CYP3A4 inhibitor, its initial dose should be changed and gradually increased after the patient is under medical restraint (section “Interactions with other doctors”) in any way and other types of mutual relations").
Special groups of patients.
Obvious data do not indicate the usefulness of changing the dosing regimen depending on the age and status of the patient.
Nirkova lack of availability
In case of low-grade hyperthyroidism of the lung and middle stage (creatinine clearance 20-49 ml/xw/1.72 m2), a single dose of buspirone causes an increase in the level of blood plasma without increasing the recovery period . For these patients, it is recommended to take buspirone with caution and in smaller doses, take 2 times per dose. The patient's response to treatment and symptoms must be carefully monitored before increasing the dose. In patients with anuric syndrome, a one-time dose of the drug causes an increase in the level of metabolite 1-pyrimidine/piperazine (1-PP) in the blood; in them, dialysis did not reveal a fluid influx on either buspirone or 1 -RR. Buspirone should not be used in patients with creatinine clearance less than 20 ml/xv/1.72 m2, especially in patients with anuric syndrome, due to the possibility of shifting the level of buspirone and its metabolites.
Pechinkova deficiency
The use of drugs such as buspirone for the treatment of patients with reduced liver function demonstrates a change in the effect of the first passage of fluids through the liver. In case of liver cirrhosis, one-time administration of buspirone causes an increase in the level of its unchanged form in the blood plasma due to an increased period of recovery. For these patients, it is recommended to administer buspirone with caution and after individual dosage titration to reduce the risk of serious adverse reactions that may occur with high-dose administration of buspirone. Dose adjustments can be seen after a close examination of the patient and only 4-5 days after the previous dose has been instilled.
The thrill of rejoicing.
Tranquilizers cannot be used without control for three hours. The duration of treatment with buspirone 5 mg or 10 mg should not last for 4 months. The dosage is determined by the doctor individually for the skin patient who is about to become ill. If it is necessary to continue drug administration (up to 6 months), close medical monitoring should be carried out.
Remember about psychotherapeutic and sociotherapeutic approaches in parallel with buspirone treatment.
Children.
Buspirone should not be prescribed to children due to the safety and effectiveness of administration.
pharmachologic effect
According to doctors' reviews, the drug "Spitomin" can be classified as a non-benzodiazepine drug; its action is defined as antidepressant. The medicine has some differences from the classic versions of anxiolytics. The effect that the drug has is associated with the effect of buspirone on the human body. It affects the activity of the dopaminergic and serotonergic systems. Buspirone, acting on presynaptic dopamine receptors, blocks them and increases the rate of activation of dopamine neurons located in the midbrain.
The active component does not have a negative effect on the implementation of psychomotor functions, it does not lead to the development of tolerance. The use of "Spitomin" eliminates the occurrence of withdrawal syndrome and dependence on this drug. The use of the drug "Spitomin" instructions for use, reviews are not associated with a negative impact on the effect that ethanol has on the body. To obtain the necessary therapeutic effect, it is necessary to be treated for 1-2 weeks; the maximum possible effect can be seen only a month after the start of therapy.
Overdose
Symptoms:
boredom, vomiting, confusion, drowsiness, increased sleepiness, miosis, disorders of the scolio-intestinal tract, loss of fluidity. Severe conditions were not affected when taking doses up to 2400 mg.
Likuvannya:
washing the schluka, monitoring breathing, pulse, arterial pressure. Symptomatic therapy. Specific antidote for daily life. Buspirone is not available for additional hemodialysis. Based on the fact that the drug has been given before it has been used, overdosing with high doses (single dose – 375 mg orally) does not necessarily cause severe symptoms.
Reviews about the use of Spitomin
Reviews from patients and doctors confirm the effectiveness of Spitomin. Negative comments are rare.
Doctors
Neurologists use Spitomin in their practice. They often prescribe this medication, noting its effectiveness and immediate action:
Kovalchuk Z.P.: “I often prescribe Spitomin as part of complex therapy, since the drug alone cannot always cope with serious disorders. I would like to note that the side effects indicated in the instructions for the medication occur rarely, which is undoubtedly a plus.”
Oleynikov E.V.: “When used and prescribed correctly, the medication is effective and easily tolerated, with the exception, of course, of individual intolerance. Most often, side effects are a consequence of self-medication.”
Side effects
Side effects occur, as a rule, at the beginning of the treatment and tend to change during dry stagnation. In some cases, a reduced dose is necessary. Most often, side reactions were observed on the side of the nervous system, such as confusion, sleeplessness, nervousness, drowsiness, fatigue, as well as on the side of the herbal tract, such as boredom, as well as other effects, for example, headache and fatigue.
In the past, one should beware of anger and witchcraft, confusion of vision, blurred vision, diarrhea, pain in the muscles and bones, numbness, paresthesia, impaired coordination of the arms, tremors and skin. irritation, dry mouth, weakness, asthenia, excessive sweating, sticky skin.
Adverse reactions are classified according to frequency: even wider (≥ 1/10); wider (≥1/100, <1/10); not wide (≥1/1000, <1/100); rarely wide (≥1/10,000, <1/1000); very rarely wide (< 1/10000); unknown (frequency cannot be estimated through the availability of data).
Infections and invasions:
the frequency of the unknown is a gap.
On the side of the cardiovascular system:
wider – non-specific pain in the breasts;
non-expanded - timely restlessness, arterial hypotension and/or hypertension, tachycardia/heart palpitations;
rarely widened - impaired cerebral blood flow, heart failure, myocardial infarction, cardiomyopathy, bradycardia, cerebrovascular damage.
On the side of the blood system:
rarely widened - changes in blood indicators (eosinophilia, leukopenia, thrombopenia).
Mental disorders:
wider - nighttime fever, drowsiness, sleeplessness, confusion, nervousness, decreased concentration of energy, emotional awakening, twitchiness, witchcraft, confusion, depression;
not widespread – depersonalization, discomfort, pathologically impaired response to sounds, euphoria, hyperkinesia, restlessness, loss of interest, impaired associative awareness, hallucinations, suicidal ideation , epileptic attacks, dysphoria, fear;
Rarely widened – sudden change in mood, claustrophobia, stupor, confusion, memory problems, serotonin syndrome, psychosis.
On the side of the nervous system:
not wide – numbness, paresthesia (for example, tingling, due to pain), poor coordination, tremor, epileptic attacks, dysgeusia, dysosmia, delayed reaction time;
Rarely widespread - spontaneous rashes, hypersensitivity, extraparametric symptoms, including early and late dyskinesia, impaired tone, fever, parkinsonism, akathisia, head noise.
From the side of the organs:
wider – dim vision;
not wide – redness and itching in the eyes, conjunctivitis;
Rarely widened - photophobia, pressure on the eyes, pain in the eyes, sound field of vision, displacement of the internal eye pressure.
On the side of the hearing organs:
wider - noise in the wuhah; Rarely widened - the inner ear is strong.
On the side of the dichotomy system:
Wider – sore throat, stuffy nose;
not wide - extremely accelerated breathing, shortness of breath, constriction of the heart, hyperventilation, due to lack of wind;
Rarely widened - nosebleeds, as if the tongue is swollen.
On the side of the grass tract:
wide – tiredness, xerostomia, pain in the epigastric region, diarrhea;
indigestion – flatulence, loss of appetite, loss of appetite, hypersalivation, small bowel syndrome, bleeding from the rectum, constipation, vomiting.
On the side of the thyroid system:
not wide – often sechovypuskannaya, zatrimka sechovypuskannaya, dysuria;
Rarely enlarged – enuresis, urinary discharge.
From the side of the skin:
not wide – bumps, weeds, hyperemia, hematomas, scaling, dry skin, eczema, skin bumps, puffy skin, hot flashes, skin irritation, skin sagging, itching;
rarely widespread - allergic reactions, ecchymosis, acne, thinning of nails.
On the side of the cysto-muscular system:
non-widening – spasm and stiffness of the muscles, myalgia, arthralgia;
rarely wider – myasthenia.
On the side of the endocrine system:
rarely widespread – galactorrhea, gynecomastia, thyroid dysfunction.
Metabolic disorders:
non-broad – anorexia, loss of appetite;
unknown frequency – increased body weight, change in body weight.
Zagalni destruction:
widening – headache, asthenia; not broadened – fever, ringing in the head, uneasiness, increased sweating, impaired sense of smell and savory senses, increased sweating, hot flashes, cold hyperesthesia;
Rarely widened - predisposition to alcohol abuse, impaired blood coagulation, loss of voice, woofing, glossalgia.
On the side of the hepatobiliary system:
unexpanded – increase in liver enzymes.
On the side of the reproductive system:
not widened – disruption of the menstrual cycle, decreased or increased libido;
rarely - amenorrhea, inflammation of the sechostatic organs, decreased ejaculation, impotence.
Laboratory research:
elevated levels of transaminases in blood serum.
Overdose and side effects
If you overdose, you may experience nausea, vomiting, and drowsiness. If an overdose occurs and the dose of the drug is large, then depression of the nervous system may occur (this is the case when a severe form appears).
In order to get rid of these symptoms, it is necessary to rinse the stomach with plenty of water.
But here we need to make a reservation - even in the case of an overdose, the patient may not always develop symptoms of intoxication.
Side effects after taking the drug do occur, but the medicine is almost always very well tolerated. Typically, the negative effects of the drug on the body begin to appear immediately in the early stages of therapy.
But, as a rule, such manifestations disappear after prolonged use of the drug. It also happens that in some cases a reduction in the dosage of the drug is required.
Side effects appear as follows:
- The cardiovascular system . Most often there is chest pain, sometimes there may be fainting and high blood pressure. Sometimes patients may experience disturbances in cerebral circulation. In rare cases, heart attacks have been recorded.
- Central nervous system . Most often, dizziness is recorded, a headache appears, and the person begins to react more sharply to noise. Apathy and fear may appear, as well as hallucinations. A slower reaction is recorded, thoughts of suicide appear, as well as epileptic seizures. If a person suffered from stuttering before taking the drug, then during use the stuttering begins to intensify.
- Organs of hearing and vision . A number of patients experienced tinnitus and swelling of the mucous membrane. Deterioration of vision is recorded much less frequently. In terms of vision, conjunctivitis may appear, and the eyes may begin to turn red. There is also pain in the eyes.
- Endocrine system and gastrointestinal tract . Nausea and vomiting may occur. More rarely, diarrhea and a burning sensation in the tongue area are noted.
- Urinary system . If the drug is used, frequent urination may occur and the menstrual cycle may be disrupted in women. In some cases, bedwetting is recorded. In men, impotence may be observed during the period of use of the drug.
