Quetiapine - instructions for use, reviews, analogs and formulations (tablets 25 mg, 100 mg, 150 mg, 200 mg and 300 mg Stade, SZ) drugs of neuroleptics for the treatment of schizophrenia and other psychoses in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Quetiapine. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of neuroleptic Quetiapine in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Quetiapine in the presence of existing structural analogues. Use for the treatment of schizophrenia, delusional disorders and other psychoses in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Quetiapine antipsychotic agent (antipsychotic). Has a higher affinity for serotonin 5HT2 receptors, compared to dopamine D1 and D2 receptors in the brain. It also has a high affinity for histamine and alpha-1 receptors and less pronounced for alpha2 receptors. Has no affinity for m-holinoretseptoram and benzodiazepine receptors.

Quetiapine in a dose effectively blocking dopamine D2 receptors causes only weak catalepsy. Selectively reduces the activity of mesolimbic A10-dopamine neurons compared to A9-nigrostriatal neurons involved in motor function.

Does not cause a prolonged increase in the level of prolactin.

In accordance with the results of positron emission tomography, the action of quetiapine on serotonin 5HT2- and dopamine D2 receptors continues up to 12 hours.

Composition

Quetiapine + auxiliary substances.

Pharmacokinetics

After oral administration, it is well absorbed from the digestive tract. Eating does not significantly affect the bioavailability of quetiapine. The pharmacokinetics of quetiapine is linear. Binding to plasma proteins is about 83%. Exposed to intensive metabolism.In studies, it has been established that the key enzyme for the metabolism of quetiapine is CYP3A4. The main metabolites, determined in blood plasma, do not have a pronounced pharmacological activity. Less than 5% of quetiapine is excreted unchanged by the kidneys or through the intestines. Approximately 73% of metabolites are excreted by the kidneys and 21% by the intestine.

Indications

• acute and chronic psychoses (including schizophrenia).

Forms of release

Tablets coated with 25 mg, 100 mg, 150 mg, 200 mg and 300 mg (producers of Stade, North Star - NW).

Instructions for use and dosage

Inside, 2 times a day, regardless of food intake.

Treatment of acute and chronic psychoses, including schizophrenia. The daily dose for the first 4 days of therapy: 50 mg - the first day, 100 mg - the second day, 200 mg - the third day, 300 mg - the 4th day. Starting from the 4th day, the dose should be selected up to an effective dose ranging from 300 to 450 mg per day. Depending on the clinical effect and tolerability of the drug, the dose may vary from 150 to 750 mg per day.

Treatment of manic episodes in bipolar disorder. The daily dose for the first 4 days of therapy is: the 1st day - 100 mg, the second day - 200 mg, the third day - 300 mg, the 4th day - 400 mg. Further, within 6 days, the daily dose is increased to 800 mg, but not more than 200 mg per day.Depending on the clinical effect and the tolerability of the drug, the dose may vary from 200 to 800 mg per day. The effective dose is 400 to 800 mg per day.

Elderly age. The plasma clearance of quetiapine in elderly people is reduced by 30-50% compared to young patients, so prescribe the drug with caution, especially at the beginning of treatment. The starting dose is 25 mg per day, followed by an increase of 25-50 mg per day, until the effective dose is achieved.

Renal and hepatic insufficiency. In renal and / or liver failure, quetiapine should be treated with 25 mg per day, followed by a daily increase of 25-50 mg, until an effective dose is reached.

Side effect

• headache;
• drowsiness;
• dizziness;
• anxiety;
• malignant neuroleptic syndrome (CNS);
• orthostatic hypotension;
• tachycardia;
• arterial hypertension;
• constipation, diarrhea;
• dry mouth;
• dyspepsia;
• transient increase in activity of hepatic enzymes (ALT, AST, GGT);
• stomach ache;
• asymptomatic leukopenia and / or neutropenia, eosinophilia;
• myalgia;
• rhinitis;
• skin rash;
• dry skin;
• earache;
• urinary tract infections;
• a slight increase in the content of cholesterol and triglycerides in the blood;
• a small dose-dependent reversible decrease in thyroid hormone levels (in particular, total and free T4);
• asthenia;
• low back pain;
• increase in body weight;
• fever;
• pain in the chest.

Contraindications

• hypersensitivity to quetiapine.

Application in pregnancy and lactation

In pregnancy and lactation, the application is possible in cases where the expected benefit to the mother exceeds the potential risk to the fetus. It is not known whether quetiapine is excreted in breast milk. If it is necessary to use lactation, breastfeeding should be discontinued.

In experimental animal studies, no mutagenic and clastogenic effects of quetiapine were identified. There was no evidence of quetiapine's influence on fertility (decreased male fertility, pseudopregnancy, an increase in the period between two estrus, an increase in the precoital interval and a decrease in the frequency of pregnancy), but one can not directly transfer the obtained data to humans. there are specific differences in the hormonal control of reproduction.

Use in children

The safety and efficacy of the drug in children and adolescents have not been investigated.

Application in elderly patients

Use with caution in the elderly, especially with the simultaneous use of drugs that extend the QT interval.

special instructions

Use with caution in patients with cardiovascular diseases and other conditions associated with risk of hypotension, especially at the beginning of treatment and in the elderly; with instructions in an anamnesis for seizures.

Quetiapine is subject to active metabolism in the liver. In patients with impaired liver and kidney function, quetiapine clearance is reduced by approximately 25%. Therefore, quetiapine should be used with caution in patients with impaired hepatic and / or renal function.

With caution apply simultaneously with drugs that extend the QT interval (especially in the elderly); with drugs that exert a depressant effect on the central nervous system, as well as with ethanol; with potential inhibitors of the isoenzyme CYP3A4 (including with ketoconazole, erythromycin).

When developing against the backdrop of ZNS treatment, quetiapine should be discontinued and appropriate treatment should be prescribed.

With prolonged use, there is a chance of developing tardive dyskinesia. In such cases, it is necessary to reduce the dose of Quetiapine or to cancel it.

Use with caution in combination with other drugs that affect the activity of the central nervous system, as well as with ethanol (alcohol)

In experimental studies in the study of the carcinogenicity of Quetiapine, there was an increase in the incidence of adenocarcinoma of the mammary gland in rats (at doses of 20, 75 and 250 mg / kg per 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 adenomas from thyroid follicular cells, which was associated with a known, rodent-specific mechanism for increasing hepatic clearance of thyroxin.

Impact on the ability to drive vehicles and manage mechanisms

Quetiapine can cause drowsiness, so patients are not recommended to perform work related to the need for concentration of attention and high speed of psychomotor reactions (including driving).

Drug Interactions

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.

With simultaneous use with phenytoin, carbamazepine, barbiturates, rifampicin, the clearance of quetiapine increases, and its concentration in the blood plasma decreases.

With simultaneous use with thioridazine, the clearance of quetiapine may be increased.

Analogues of the drug Quetiapine

Structural analogs for the active substance:

• Victor;
• Quentiaks;
• Quetiapin Canon;
• Quetiapin Canon Prolong;
• Quetiapine Sun;
• Quetiapin Stade;
• Quetiapine Vial;
• Quetiapine C3;
• Quetiapine hemifumarate;
• Quetiapine fumarate;
• Quetitex;
• Ketiap;
• Ketilept;
• Koumental;
• Kutipin;
• Lakvel;
• Nantarid;
• The servicer;
• Seroquel;
• Seroquel Prolong.

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