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Kventiax (Quetiapinum, Quetiapine) - antipsychotic (neuroleptic).
Quetiapine is an atypical antipsychotic, which exhibits higher affinity for serotonin receptors (5HT2) receptors than for dopamine D1 and D2 brain. Quetiapine has affinity for histamine and alpha-1 receptors and less affinity for alpha-2 receptors. There were no appreciable affinity for cholinergic muscarinic to quetiapine and benzodiazepine receptors. The standard tests shows quetiapine antipsychotic activity.
Results of the study of extrapyramidal symptoms (EPS) in animals revealed that quetiapine causes weak catalepsy at a dose that effectively blocking dopamine D2 receptors. Quetiapine is a selective decrease in the activity-A10 mesolimbic dopaminergic neurons, compared with the A9-nigrostriatal neurones involved in motor function.
There were no differences between the use of quetiapine (at a dose of 75-750 mg / day) and placebo in the incidence of cases of extrapyramidal symptoms and concomitant use of anticholinergic preparatov.- does not cause long-term increase prolactin concentration in blood plasma.
Quetiapine prolonged supports clinical improvement in patients who have developed a positive effect at the beginning of treatment.
The duration of exposure to quetiapine 5HT2 receptors - serotonin and dopamine D2 receptors is less than 12 hours after dosing.
Absorption - high, it does not affect food intake on bioavailability. Relationship to plasma proteins - 83%.
The pharmacokinetics of quetiapine is linear and does not differ in men and women.
Extensively metabolized in the liver with the formation of pharmacologically inactive metabolites by the enzyme cytochrome P450 CYP3A4. Quetiapine and some of its metabolites are weak inhibitors of isoenzymes 1A2, 2C9, 2C19, 2D6, and human cytochrome P450 ZA4, but only at concentrations of at least 10-50 times higher than the concentration of the drug when used in effective doses ranging from 300 to 450 mg / d.
Based on the results in vitro, not to be expected that co-administration of quetiapine with other drugs will result in clinically significant inhibition of cytochrome P450 mediated metabolism of other drugs. The half-life (T½) of about 7 hours.
Report the news about 73%, and through the intestines - 21%. 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 plasma clearance of quetiapine in patients with severe renal insufficiency (creatinine clearance less than 30 mL / min / 1.73 m3) decreased by approximately 25% in patients with liver disease (stable alcoholic cirrhosis).
Treatment of acute and chronic psychosis, including schizophrenia; treatment of manic episodes in bipolar disorder.
Precautions: patients with cardiovascular and cerebrovascular disease, or other conditions predisposing to hypotension, inherent increase in the QT interval on the electrocardiogram (ECG), or under the conditions with the potential to cause an increase in the QT interval (co-administration of drugs prolonging the interval QT, congestive heart failure , hypokalemia, hypomagnesemia), advanced age, liver failure, epilepsy, seizures in history, pregnancy.
With a sharp lifting of high doses of antipsychotic drugs following acute reactions ( "withdrawal") can be observed - nausea, vomiting, insomnia rarely. It reported cases. exacerbation of psychotic symptoms and the emergence of involuntary movement disorders (akathisia, dystonia, dyskinesia). In this connection, the abolition of the drug is recommended to be made gradually.
In the appointment of quetiapine in conjunction with drugs, prolongs the QT interval, care must be taken, especially in the elderly. In congestive heart failure in hypokalemia and hypomagnesemia.
Given that quetiapine affects the central nervous system, the drug should be used with caution in combination with other drugs having inhibitory effect on the central nervous system. It is recommended to abstain from alcohol.
If symptoms of tardive dyskinesia should reduce the dose or discontinue the use of quetiapine.
In controlled clinical trials there was no difference found in the incidence of seizures between quetiapine and placebo. However, just as with other antipsychotic drug therapy is recommended caution in patients with having a history of seizures.
Neuroleptic malignant syndrome
Neuroleptic malignant syndrome may be associated with antipsychotic treatment conducted. The clinical manifestations of the syndrome include: hyperthermia, altered mental status, muscular rigidity, instability of the autonomic nervous system, increased creatine phosphokinase levels. With the development of this syndrome quetiapine should be discontinued and appropriate treatment.
Effects on ability to drive and other mechanical means: during treatment with quetiapine is recommended to use caution when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.
Inside, 2 times a day regardless of the meal.
Treatment of acute and chronic psychosis, including schizophrenia: The daily dose of the day is the first 4: 1 day - 50 mg; Day 2 - 200 mg; Day 3 -200 mg and Day 4 - 300 mg. Starting from the fourth day of the daily recommended dose of 300 mg. Depending on the clinical effect and tolerability of the dose may vary individually from 150 mg / day to 750 mg / day. The maximum daily dose for the treatment of schizophrenia - 750 mg.
Treatment of manic episodes in bipolar disorder: Quetiapine is recommended as monotherapy or as adjunctive therapy to mood stabilization.
The daily dose of the day is the first 4: 1 day - 100 mg; Day 2 200mg; Day 3 -300 mg and 4 th day - 400 mg. Increasing daily dose may subsequently 200 mg per day and the second day of treatment is 800 mg. Depending on the clinical effect and tolerability of the dose may vary individually from 200 mg / day to 800 mg / day. Typically, the effective dose is from 400 to 800 mg / day. The maximum daily dose for this indication - 800 mg.
Because plasma clearance of quetiapine in the elderly is reduced by 30-50%, should be prescribed the drug with caution, especially at the beginning of therapy. Starting dose - 25 mg / day, followed by an increase to 25-50 mg to achieve an effective dose.
Renal and hepatic insufficiency: In patients with renal and hepatic impairment is recommended to start treatment with the 25 mg / day. Further it is recommended to increase the dose of 25-50 mg daily to achieve an effective dose.
Data on overdose of quetiapine limited. Cases of quetiapine in doses exceeding '30 In most patients, side effects are not observed in the case of the development of side effects were on their own. Joined case of death when taking 13.6 grams of quetiapine. Very rarely reported cases of quetiapine overdose leads to a lengthening of the QT interval, coma or death. In patients with severe cardiovascular disease in the history of the risk of side effects may increase in overdose.
Symptoms: excessive sedation, somnolence, tachycardia, decreased blood pressure.
Treatment: symptomatic; activities aimed at the maintenance of respiratory function, cardiovascular system, adequate oxygenation and ventilation. No specific antidote.
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