Seroquel pills 25 mg 60 pcs
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Active ingredients
Quetiapine
Release form
Pills
Composition
Active ingredient: Quetiapine (Quetiapine) Active ingredient concentration (mg): 100
Pharmacological effect
Antipsychotic (neuroleptic). Shows higher affinity for serotonin 5HT2 receptors, compared with dopamine D1 and D2 receptors in the brain. It also has a high affinity for histamine and α1 receptors and less pronounced for α2 receptors. It has no affinity for m-cholinergic receptors and benzodiazepine receptors. Quetiapine, in a dose that effectively blocks dopamine D2 receptors, causes only weak catalepsy. Selectively decreases the activity of mesolimbic A10-dopamine neurons compared to A9-nigrostriatal neurons involved in motor function. It does not cause a prolonged increase in prolactin level. According to the results of positron emission tomography, quetiapine acts on serotonin 5HT2 and dopamine D2 receptors to continue .
Pharmacokinetics
After ingestion is well absorbed from the gastrointestinal tract. Eating does not have a significant effect on the bioavailability of quetiapine. Quetiapine pharmacokinetics is linear. Plasma protein binding is about 83%. It is subjected to intensive metabolism. In vitro studies have established that CYP3A4 is a key enzyme in the metabolism of quetiapine. The major metabolites, which are detected in blood plasma, do not have a pronounced pharmacological activity. T1 / 2 is about 7 hours. Less than 5% of quetiapine is excreted unchanged by the kidneys or through the intestines. Approximately 73% of metabolites excreted by the kidneys and 21% through the intestines. The average clearance of quetiapine in elderly patients is 30-50% less than that observed in patients aged 18 to 65. The average plasma clearance of quetiapine was approximately 25% less in patients with severe renal impairment (CC less than 30 ml / min / 1.73 m2) and in patients with liver damage (alcoholic cirrhosis in the compensation stage), but individual clearance levels were within the limits corresponding to healthy people.
Indications
For the treatment of acute and chronic psychosis, including schizophrenia. For the treatment of manic episodes in the structure of bipolar disorder.
Contraindications
Hypersensitivity to any of the components of the drug.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
In pregnancy and lactation, use is possible in cases where the expected benefit to the mother outweighs the potential risk to the fetus. It is not known whether quetiapine is excreted in breast milk. If necessary, use during lactation, breastfeeding should be discontinued. In experimental animal studies, no mutagenic and clastogenic action of quetiapine was detected. No effect of quetiapine on fertility (reduced male fertility, pseudo-pregnancy, an increase in the period between two estrus, an increase in the precoital interval, and a decrease in the frequency of pregnancy), but the data obtained cannot be directly transferred to a person, because There are specific differences in the hormonal control of reproduction.
Dosage and administration
Seroquel is administered 2 times a day inside, regardless of the meal. Adults Treatment of acute and chronic psychosis, including schizophrenia. The daily dose for the first 4 days of therapy is: Day 1 - 50 mg, Day 2 - 100 mg, Day 3 - 200 mg, the 4th day - 300 mg. Starting from the 4th day, the dose should be adjusted to the effective dosage, usually in the range of 300 to 450 mg / day. Depending on the clinical effect and individual tolerance of the patient, the dose may vary from 150 to 750 mg / day. Treatment of manic episodes in the structure of bipolar disorder Seroquel is used as monotherapy or as an adjuvant therapy to stabilize mood. Daily dose for the first 4 The days of therapy are: 1st day - 100 mg, 2nd day - 200 mg, 3rd day - 300 mg, 4th day - 400 mg. In the future, by the 6th day of therapy, the daily dose of the drug can be increased to 800 mg. The increase in the daily dose should not exceed 200 mg per day. Depending on the clinical effect and individual tolerance, the dose can vary from 200 to 800 mg / day. The effective dose usually ranges from 400 to 800 mg / day. For the treatment of schizophrenia, the maximum recommended daily dose of Seroquel is 750 mg, and for treatment of manic episodes in the structure of bipolar disorder, the maximum recommended daily dose of Seroquel is 800 mg / day. Older patients in elderly patients have an initial dose of Seroquel 25 mg / day.The dose should be increased daily by 25-50 mg to achieve an effective dose, which is likely to be less than in young patients. Patients with renal and hepatic insufficiency In patients with renal or hepatic insufficiency, it is recommended to begin Seroquel therapy with 25 mg / day. It is recommended to increase the dose daily by 25-50 mg to achieve an effective dose. Children and adolescents The safety and effectiveness of Seroquel in children and adolescents has not been studied.
Side effects
The following most common adverse reactions associated with taking the drug were noted: drowsiness (17.5%), dizziness (10%), constipation (9%), dyspepsia (6%), orthostatic hypotension and tachycardia (7%), dry mouth ( 7%), increased serum liver enzymes (6%) (including increased cholesterol and triglyceride concentrations). Seroquel can be accompanied by the development of moderate asthenia, rhinitis and dyspepsia, weight gain (mainly in the first weeks of treatment). Seroquel can cause orthostatic which hypotension (accompanied by dizziness), tachycardia, and in some patients fainting; these adverse reactions are mainly found in the initial period of dose selection (see section “Special Instructions”). In patients taking Seroquel, very rare cases of priapism and seizures occurred. In rare cases, malignant neuroleptic syndrome (hyperthermia, impaired consciousness, muscular rigidity, vegetative-vascular disorders, increase in the concentration of creatine phosphokinase), leukopenia and / or neutropenia was observed. No cases of severe neutropenia or agranulocytosis have been reported in patients taking Seroquel. When using Seroquel in the usual practice, leukopenia and / or neutropenia was resolved after discontinuation of the drug. Possible risk factors for the development of leukopenia and / or neutropenia include a decrease in the number of leukocytes before the start of therapy or a history of leukopenia and / or neutropenia, caused by medication. Cases of eosinophilia, development of peripheral edema, and allergic reactions, including angioedema, were rarely reported. There were reports of asymptomatic increases in the activity of serum transferase (alanine and aspartic ALT and ACT, respectively) or gamma-glutamyltranspeptidase (GGT) activity in patients treated with Serokol.During the treatment with Seroquel, these changes were usually reversible. During treatment with Seroquel, there may be a slight increase in the concentration of cholesterol and serum triglycerides. The therapy with Seroquel is associated with a small dose-dependent decrease in thyroid hormone levels, in particular, total T4 and free T4. The maximum decrease in total and free T4 was registered on the 2nd and 4th week of quetiapine therapy, without further reducing the concentration of hormones during prolonged treatment. In the future, there were no signs of clinically significant changes in the concentration of thyroid-stimulating hormone. In almost all cases, the concentration of total and free T4 returned to baseline after discontinuing Seroquel therapy, regardless of the duration of treatment. Seroquel may cause a prolongation of the QTC interval, no relationship has been identified between the use of Seroquel with a constant increase in QTC (see the section “Special Instructions”). The following frequent side effects (1/100) were also reported: increased blood pressure, palpitations, dysarthria, pharyngitis, cough, anorexia, and increased sweating. The causal relationship of these side effects with the reception Seroquel is not installed.
Overdose
Currently, no cases of overdose have been reported.
Interaction with other drugs
With simultaneous use with ketoconazole, erythromycin, it is theoretically possible to increase the concentration of quetiapine in the blood plasma and the development of side effects. When used simultaneously with phenytoin, carbamazepine, barbiturates, rifampicin, the clearance of quetiapine increases, its concentration in the blood plasma decreases. quetiapine.
special instructions
It is used with caution in patients with cardiovascular diseases and other conditions associated with the risk of arterial hypotension, especially at the start of treatment and in the elderly; with indications of a history of seizures. Quetiapine is actively metabolized in the liver. In patients with impaired liver and kidney function, the clearance of quetiapine is reduced by approximately 25%. Therefore, quetiapine should be used with caution in patients with impaired liver and / or kidney function. It is used with caution along with drugs that prolong the QT interval (especially in the elderly); with drugs that have a depressant effect on the central nervous system, as well as with ethanol; with potential inhibitors of an isoenzyme CYP3A4 (includingwith ketoconazole, erythromycin). When developing during the treatment of ZNS, quetiapine should be canceled and appropriate treatment should be given. With prolonged use, there is a likelihood of tardive dyskinesia. In such cases, it is necessary to reduce the dose of quetiapine or cancel it. Use with caution in combination with other drugs that affect the activity of the central nervous system, as well as ethanol. 20, 75 and 250 mg / kg / day), which is associated with prolonged hyperprolactinemia. In male rats (250 mg / kg / day) and mice (250 and 750 mg / kg / day) there was an increase in the incidence of benign animals. denomyra from thyroid follicular cells, which was associated with the well-known rodent-specific mechanism of increasing hepatic clearance of thyroxin. The effect on the ability to drive vehicles and control mechanismsKetiapin can cause drowsiness, so patients are not recommended to perform work related to the need to concentrate and high speed psychomotor reactions (including driving vehicles).