Quentiax Coated Tablets 300mg N60
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Active ingredients
Quetiapine
Release form
Pills
Composition
Quetiapine fumarate 345.39 mg, which corresponds to the content of quetiapine 300 mg; Excipients: lactose monohydrate - 54 mg, calcium hydrogen phosphate dihydrate - 30 mg, microcrystalline cellulose - 227.61 mg, povidone - 15 mg, sodium carboxymethyl starch (type A) - 60 mg, magnesium stearate - 18 mg.; Shell composition: hypromellose - 15 mg, titanium dioxide (E171) - 6 mg, macrogol 4000 - 3 mg.
Pharmacological effect
Antipsychotic drug (neuroleptic). Quetiapine is an atypical antipsychotic drug that exhibits a higher affinity for serotonin 5HT 2 receptors than for dopamine D 1 and D 2 brain receptors. Quetiapine has an affinity for histamine and 1 -adrenoreceptors, and a lower affinity for 2 -adrenoreceptors. No significant affinity of quetiapine for cholinergic muscarinic and benzodiazepine receptors was detected .; In standard tests, quetiapine exhibits antipsychotic activity .; The results of studying extrapyramidal symptoms in animals revealed that quetiapine causes weak catalepsy at a dose that effectively blocks dopamine D 2 receptors. Quetiapine causes a selective decrease in the activity of mesolimbic A10-dopaminergic neurons, in comparison with A9-nigrostriatal neurons involved in motor functions .; 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 syndromes 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 effects of quetiapine on serotonin 5HT 2 receptors and dopamine and D 2 receptors is less than 12 hours after taking the drug.
Pharmacokinetics
Absorption - high, food intake does not affect bioavailability. Plasma protein binding - 83%; Quetiapine pharmacokinetics is linear and does not differ in men and women .; ; Metabolism; Actively metabolized in the liver to form pharmacologically inactive metabolites under the influence of CYP3A4 isoenzyme.Quetiapine and some of its metabolites are weak inhibitors of the 1A2, 2C9, 2C19, 2D6 and 3A4 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 / day.; Based on in vitro results, one should not expect the simultaneous administration of quetiapine with other drugs to result in clinically pronounced inhibition of cytochrome P450 mediated metabolism of other drugs .; Withdrawal; T1 / 2 is approximately 7 hours. About 73% is excreted by the kidneys and 21% through the intestines. Less than 5% of quetiapine is metabolized and excreted unchanged .; Pharmacokinetics in special clinical situations; 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 renal insufficiency is severe (CC less than 30 ml / min / 1.73 m 2) and in patients with liver damage (stabilized alcoholic cirrhosis) is reduced by about 25%.
Indications
- treatment of acute and chronic psychosis, including schizophrenia; - treatment of manic episodes in bipolar disorder.
Contraindications
- breastfeeding period; - children and adolescents under 18 years of age (efficacy and safety have not been established); - Hypersensitivity to quetiapine or other components of the drug. With caution, the drug should be prescribed to patients with cardiovascular and cerebrovascular diseases or other conditions that predispose to arterial hypotension, with congenital increase in the QT interval on the 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, hypokalemia, hypomagnesemia), with hepatic impairment chnosti, epilepsy, seizures in history, pregnancy, elderly patients.
Use during pregnancy and lactation
Safety and efficacy of quetiapine in pregnant women have not been established. Therefore, quetiapine can be used during pregnancy only if the expected benefit justifies the potential risk. The degree of elimination of quetiapine with mother's milk has not been established. Women should be advised to avoid breastfeeding while taking quetiapine.
Dosage and administration
The drug is administered orally, 2 times / day, regardless of the meal.; In the treatment of acute and chronic psychosis, including schizophrenia, the daily dose in the first 4 days is: Day 1 - 50 mg; 2nd day - 200 mg; 3rd day - 200 mg and 4th day - 300 mg. Starting from the 4th day, the daily dose is 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 treating schizophrenia is 750 mg. When treating manic episodes for bipolar disorder, quetiapine is recommended as monotherapy or as an adjuvant therapy to stabilize mood. Daily dose for the first 4 days is: Day 1 - 100 mg; 2nd day - 200 mg; 3rd day - 300 mg and 4th day - 400 mg. An increase in the daily dose in the future is possible at 200 mg / day and by day 6 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 mg to 800 mg / day. The maximum daily dose is 800 mg.; plasma clearance of quetiapine in elderly patients 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 until an effective dose is reached. In patients with renal and hepatic insufficiency, it is recommended to start 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.
Side effects
Classification of the incidence of side effects (WHO): very often (> 1/10), often (> 1/100, less than 1/10), infrequently (> 1/1000, less than 1/100), rarely (> 1/10 000, less than 1/1000), very rarely (less than 1/10 000, including individual reports) .; From the hemopoietic system: often - leukopenia; infrequently - eosinophilia; very rarely - neutropenia. From the side of the central and peripheral nervous system: very often - dizziness, drowsiness, headache; often - syncopal states; infrequently - anxiety, agitation, insomnia, akathisia, tremor, convulsions, depression, paresthesias; rarely - neuroleptic malignant syndrome (hyperthermia, impaired consciousness, muscle rigidity, vegetative-vascular disorders, increased concentration of CPK); very rarely - tardy dyskinesia. From the side of the cardiovascular system: often - tachycardia, orthostatic arterial hypotension, prolongation of the QT interval on an ECG.; From the side of the respiratory system: rhinitis,pharyngitis. From the digestive system: often - dry mouth, constipation, diarrhea, dyspepsia, increased levels of serum transaminases (ACT or ALT); rarely - jaundice, nausea, vomiting, abdominal pain; very rarely - hepatitis.; Allergic reactions: infrequently - skin rash, hypersensitivity reactions; very rarely - angioedema, Stevens-Johnson syndrome. On the part of the reproductive system: rarely - priapism. On the part of the endocrine system: often - an increase in body weight (mainly in the first weeks of treatment); very rarely - hyperglycemia or decompensation of diabetes mellitus. Laboratory indicators: infrequently - an increase in the serum level of GGT and the content of 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 T3 and reverse T3 / only when taking high doses of quetiapine /); Other: often - peripheral edema, asthenia; rarely - back pain, chest pain, low-grade fever, myalgia, dry skin, impaired vision.
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 the admission of 13.6 g 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 sedation, drowsiness, tachycardia, lowering blood pressure.; Treatment: symptomatic therapy is carried out, measures aimed at maintaining respiratory function, cardiovascular system, adequate oxygenation and ventilation of the lungs. There are no specific antidotes.
Interaction with other drugs
Quetiapine does not cause induction of liver enzyme systems involved in the metabolism of phenazone and lithium .; The simultaneous administration of quetiapine with drugs that potentially inhibit hepatic enzymes, such as carbamazepine or phenytoin, as well as with barbiturates, rifampicin, may decrease the plasma concentrations of quetiapine, which may require an increase in Quentiax dose, depending on the clinical effect.This should also be taken into account 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 is the CYP3A4 isoenzyme. The pharmacokinetics of quetiapine does not change with the simultaneous use of cimetidine (P450 inhibitor), fluoxetine (CYP3A4 inhibitor and CYP2D6) or imipramine antidepressant (CYP2D6 inhibitor) .; It is recommended to use caution with the simultaneous use of quetiapine and systemic use of inhibitors of CYP3A4 (antifungal agents of the azoles group and macrolide antibiotics), since 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 haloperidol. However, simultaneous taking of quetiapine with thioridazine led to an increase in clearance of quetiapine .; CNS depressant drugs and ethanol increase the risk of side effects.