Quentiax pills 200mg №60

Trade name

1 pill contains
CORE: Active substance:
Quetiapine fumarate (quetiapine hemifumarate) 115.13 mg, 230.26 mg, 345.39 mg, which corresponds to 100, 200, 300 mg of quetiapine.

Excipients are listed in section 6.1.

Clinical data

Therapeutic indications

• Treatment of acute and chronic psychosis, including schizophrenia;
• Treatment of manic episodes in bipolar disorder.

Dosage and administration

 Inside, 2 times a day, regardless of the meal.
Treatment of acute and chronic psychosis, including schizophrenia:
The daily dose in the first 4 days is: 1st day - 50 mg; 2nd day - 200 mg; 3rd day - 200 mg and 4th day - 300 mg. Starting from the fourth day, the daily dose is recommended: 300 mg. Depending on the clinical effect and tolerability of the drug, its dose may individually vary from 150 mg / day to 750 mg / day. The maximum daily dose for the treatment of schizophrenia is 750 mg.
Treatment of manic episodes in bipolar disorder: Quetiapine is recommended as monotherapy or as adjuvant therapy to stabilize mood.
The daily dose in the first 4 days is: 1st day - 100 mg; 2nd day 200mg; 3rd day - 300 mg and 4th day - 400 mg. The increase in the daily dose in the future may be 200 mg per day and by the 6th day of therapy is 800 mg.Depending on the clinical effect and tolerability of the drug, its dose may individually vary from 200 mg / day to 800 mg / day. As a rule, the effective dose ranges from 400 to 800 mg / day. The maximum daily dose for this indication is 800 mg.
Elderly age: Since plasma clearance of quetiapine in the elderly is reduced by 30-50%, the drug should be prescribed with caution, especially at the beginning of therapy. The starting dose is 25 mg / day, followed by an increase of 25-50 mg to achieve an effective dose.
Kidney and liver failure: In patients with renal and hepatic insufficiency, it is recommended to begin therapy with 25 mg / day. In the future, it is recommended to increase the dose daily by 25-50 mg to achieve an effective dose.

Contraindications

• Hypersensitivity to quetiapine or other components of the drug;
• Breastfeeding period;
• Children and adolescents under 18 years of age (efficacy and safety have not been established).

Special instructions and precautionary measures

 Carefully: patients with cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, congenital increase in the QT interval on an electrocardiogram (ECG) or in the presence of conditions potentially capable of increasing the QT interval (simultaneous prescription of drugs that prolong the QT interval, congestive heart failure, hypocaloria, hypomagnesemia), old age, liver failure, epilepsy, history of convulsive seizures, pregnancy. With abrupt cancellation of high doses of antipsychotic drugs, the following acute reactions may occur. ("Withdrawal syndrome") - nausea, vomiting, rarely insomnia. Cases of exacerbation of psychotic symptoms and the appearance of involuntary movement disorders (akathisia, dystonia, dyskinesia) have been reported. In this connection, it is recommended to discontinue the drug gradually. When prescribing quetiapine simultaneously with drugs that extend the QT interval, care must be taken, especially in the elderly. With congestive heart failure, with hypokalemia and hypomagnesaemia. Given that quetiapine affects the central nervous system, the drug should be used with caution in combination with other drugs that have a depressant effect on the central nervous system. It is recommended to abstain from alcohol. When symptoms appear tardive dyskinesia reduce dosage or discontinue use of quetiapine. Convulsive seizures.In controlled clinical trials, no differences in the incidence of seizures between quetiapine and placebo were established. However, just as with other antipsychotic medications, caution is advised when treating patients with a history of convulsive seizures. Malignant neuroleptic syndrome. Malignant neuroleptic syndrome may be associated with ongoing antipsychotic medication. Clinical manifestations of the syndrome include: hyperthermia, altered mental status, muscular rigidity, instability of the autonomic nervous system, an increase in the level of creatine phosphokinase.With the development of this syndrome, quetiapine should be canceled and appropriate treatment carried out.

Interaction with other drugs

Quetiapine does not cause induction of liver enzyme systems involved in metabolism phenazone and lithium.
Simultaneous administration of quetiapine with drugs that potentially inhibit hepatic enzymes, such as carbamazepine or phenytoin, as well as with barbiturates, rifampicin, Plasma concentrations of quetiapine may be decreased, which may require an increase in the dose of Quentiax, depending on the clinical effect. This also needs to be considered when canceling phenytoin or Carbamazepine, or another inducer of the liver enzyme system, or replacing it with a drug that does not induce microsomal liver enzymes (for example, valproic acid).The main enzyme responsible for the metabolism of quetiapine cytochrome P450 is CYP3A4. The pharmacokinetics of quetiapine does not change with simultaneous use as citimidine (P450 inhibitor) or fluoxetine (inhibitor of CYP3A4 and CYP2D6), antidepressant imipramine (CYP2D6 inhibitor). It is recommended to be careful when using quetiapine and systemic use of CYP3A4 inhibitors {antifungal agents of the azole group and macrolide antibiotics), because Quetiapine plasma concentrations may increase. Therefore, lower doses of quetiapine should be used. Special attention should be paid to elderly and debilitated patients.The pharmacokinetics of quetiapine did not change significantly with simultaneous administration with antipsychotics - risperidone or haloperidone. However, simultaneous reception of quetiapine with thioridazine led to increased clearance of quetiapine. Medicinal products depressing central nervous system (CNS) and ethanolincrease the risk of side effects.

Pregnancy and breastfeeding

Safety and efficacy of quetiapine in pregnant women have not been established. Therefore, during pregnancy, quetiapine can only be used if the expected benefit justifies the potential risk. The degree of excretion of quetiapine with mother's milk has not been established. Women should be advised to avoid breastfeeding while taking quetiapine.

Influence on ability to drive a car and other mechanisms

During treatment with quetiapine, caution is recommended when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.

Adverse effects

 From the side of blood-forming organs and lymphatic system: often - leukopenia; infrequently - eosinophilia; very rarely - neutropenia.
Metabolism and nutrition disorders: often - body mass predominantly in the first weeks of treatment); very rarely - hyperglycemia or decompensation of diabetes.
From the central and peripheral nervous system: very often dizziness, drowsiness, headache; often - syncopal states; infrequently - anxiety, agitation, insomnia, akathisia, tremor, convulsions, depression, paresthesias; very rare: tardive dyskinesia.
Since the cardiovascular system: often - tachycardia, orthostatic hypotension, prolongation of the QT interval on the ECG.
On the part of the respiratory system: rhinitis, pharyngitis.
From the gastrointestinal tract: often - dry mouth, constipation, diarrhea, dyspepsia ; rarely - jaundice, nausea, vomiting, abdominal pain; very rarely - hepatitis.
Allergic reactions: infrequently - skin rash, hypersensitivity reactions; very rarely - angioedema, Stevens-Johnson syndrome.
From the reproductive system and mammary glands: rarely, priapism (painful erection).
Other: often - peripheral edema, asthenia; rarely - back pain, chest pain, subfebrile condition, myalgia, dry skin, weakening of vision, neuroleptic malignant syndrome (hyperthermia, impaired consciousness, muscular rigidity, vegetative - vascular disorders, increased concentration of creatine phosphokinase).
Laboratory values: often - the level of serum transaminases (ACT or ALT); infrequently, increased serum levels of GGT and triglycerides (not fasting), hypercholesterolemia; decrease in the level of thyroid hormones: total T4 and free T4 (in the first 4 weeks), as well as total TK and reversible TZ (only when taking high doses of quetiapine).

Overdose

Data on quetiapine overdose is limited. The cases of taking quetiapine in a dose exceeding 30 g have been described.In most patients, side effects were not observed, in cases of their development, side effects passed on their own. A fatal case has been reported with 13.6 grams of quetiapine. Extremely rare cases of quetiapine overdose have been reported, leading to prolongation of the QT interval, coma or death. In patients with a history of severe cardiovascular disease, the risk of side effects from overdose may increase. Symptoms: excessive sedapia, drowsiness, tachycardia, lowering blood pressure.
Treatment: symptomatic; measures aimed at maintaining respiratory function, cardiovascular system, adequate oxygenation and ventilation of the lungs. There are no specific antidotes.

Pharmacodynamics

Pharmacotherapeutic group: antipsychotic (neuroleptic).

Pharmacological properties.

Quetiapine is an atypical antipsychotic drug that exhibits a higher affinity for serotonin (5HT2) receptors than for dopamine D1 and D2 receptors in the brain. Quetiapine has an affinity for histamine and alpha-1 receptors, and a lower affinity for alpha-2 receptors. No significant affinity of quetiapine for cholinergic muscarinic and benzodiazepine receptors was detected. In standard tests, quetiapine exhibits antipsychotic activity. Pharmacodynamic effects The results of the study of extrapyramidal symptoms (EPS) in animals revealed that quetiapine causes weak catalepsy at a dose that effectively blocks dopamine D2 receptors. Quetiapine causes a selective decrease in the activity of mesolimbic AU-dopaminergic neurons, in comparison with A9-nigrostriatal neurons involved in motor functions. Clinical efficacy There were no differences between the use of quetiapine (at a dose of 75-750 mg / day) and placebo in the incidence of extrapyramidal symptoms and the concomitant use of anticholinergic drugs. Does not cause a prolonged increase in the concentration of prolactin in the blood plasma. Quetiapine for a long time supports clinical improvement in those patients in whom a positive effect developed at the very beginning of treatment. The duration of exposure to quetiapine at the 5HT2 receptors - serotonin and D2-dopamine receptors is less than 12 hours after taking the drug.

Pharmacokinetics

Absorption - high, food intake does not affect bioavailability. Communication with plasma proteins - 83%. The pharmacokinetics of quetiapine is linear and does not differ in men and women. Extensively metabolized in the liver to form pharmacologically inactive metabolites under the influence of the CYP3A4 enzyme cytochrome P450. Quetiapine and some of its metabolites are weak inhibitors of the 1A2, 2C9, 2C19, 2D6 and ZA4 isoenzymes of human cytochrome P450, but only in concentrations at least 10-50 times higher than the concentration of the drug when used in the effective dose range from 300 to 450 mg / daysBased on in vitro results, one should not expect that the simultaneous administration of quetiapine with other drugs will lead to a clinically pronounced inhibition of cytochrome P450 mediated metabolism of other drugs. The half-life (T1 / 2) is approximately 7 hours. Approximately 73% is excreted by the kidneys and 21% through the intestines. Less than 5% of quetiapine is not metabolized and excreted unchanged. The average clearance of quetiapine in elderly patients is 30-50% less than in patients aged 18 to 65 years. The average clearance of quetiapine plasma in patients with severe renal insufficiency (creatinine clearance <30 ml / min / 1.73 m3) is reduced by about 25% and in patients with liver damage (stabilized alcoholic cirrhosis).

Special storage conditions

Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.