Kventiax tablets 25mg, No. 60

When used in adults, the initial dose is 50 mg / day, for elderly patients - 25 mg / day. Then the dose is gradually increased according to the scheme. Depending on the clinical effect and individual sensitivity, the effective therapeutic dose may be 150-750 mg / day.

In patients with impaired liver and / or kidney function, the initial dose is 25 mg / day. The daily dose increase should be 25-50 mg until optimal effect is achieved.

Film-coated tablets of brownish-red color, round, biconvex, beveled; cross-sectional view - a white rough surface with a brownish-red shell.

1 tab.

quetiapine fumarate 28.78 mg,

which corresponds to the content of quetiapine 25 mg

Excipients: lactose monohydrate - 4.5 mg, calcium hydrogen phosphate dihydrate - 2.5 mg, microcrystalline cellulose - 18.97 mg, povidone - 1.25 mg, sodium carboxymethyl starch (type A) - 5 mg, magnesium stearate - 1.5 mg.

Hypersensitivity to quetiapine.

pharmachologic effect

Antipsychotic (neuroleptic). Shows 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 ? 1 -receptors and less pronounced - for ?2-receptors. It has no affinity for m-cholinergic receptors and benzodiazepine receptors.

Quetiapine, at a dose that effectively blocks dopamine D2 receptors, produces only mild catalepsy. Selectively reduces the activity of mesolimbic A10-dopamine neurons compared to A9-nigrostriatal neurons involved in motor function.

Does not cause prolonged increases in prolactin levels.

According to the results of positron emission tomography, the effect of quetiapine on serotonin 5HT2 and dopamine D2 receptors lasts up to 12 hours.

Pharmacokinetics

After oral administration, it is well absorbed from the gastrointestinal tract. Food intake does not significantly affect the bioavailability of quetiapine.

The pharmacokinetics of quetiapine are linear.

Plasma protein binding is about 83%.

Undergoes intensive metabolism. In vitro studies have established that the key enzyme of quetiapine metabolism is CYP3A4. The main metabolites, which are determined in blood plasma, do not have 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 are 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 years.

The mean plasma clearance of quetiapine was approximately 25% lower in patients with severely impaired renal function (CC less than 30 ml / min / 1.73 m2) and in patients with liver damage (alcoholic cirrhosis in the compensating stage), but individual clearance levels were within, appropriate for healthy people.

Side effect

From the side of the central nervous system: headache, drowsiness, dizziness, anxiety; rarely - ZNS.

From the side of the cardiovascular system: orthostatic hypotension, tachycardia, arterial hypertension.

From the digestive system: constipation, dry mouth, dyspepsia, diarrhea, transient increase in the activity of liver enzymes (ALT, AST, GGT), abdominal pain.

From the side of hematopoiesis: asymptomatic leukopenia and / or neutropenia; rarely, eosinophilia.

From the musculoskeletal system: myalgia.

From the respiratory system: rhinitis.

Dermatological reactions: skin rash, dry skin.

From the side of the organ of hearing: pain in the ear.

From the genitourinary system: urinary tract infections.

From the side of metabolism: a slight increase in the content of cholesterol and triglycerides in the blood.

From the endocrine system: a small dose-dependent reversible decrease in the level of thyroid hormones (in particular, total and free T4).

Others: asthenia, back pain, weight gain, fever, chest pain.

Application during pregnancy and lactation

During 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 studies on animals, no mutagenic and clastogenic effects of quetiapine were detected. No effect of quetiapine on fertility was found (decreased male fertility, pseudopregnancy, increased period between estrus, increased precoital interval and decreased pregnancy rate), however, the obtained data cannot be directly transferred to humans, because there are specific differences in hormonal control of reproduction.

Application for violations of liver function

Quetiapine is actively metabolized in the liver. In patients with impaired liver function, the clearance of quetiapine is reduced by approximately 25%. Therefore, quetiapine should be used with caution in patients with impaired liver function.

Application for impaired renal function

In patients with impaired renal function, the clearance of quetiapine is reduced by approximately 25%. Therefore, quetiapine should be used with caution in patients with impaired renal function.

Use in elderly patients

Use with caution in the elderly, especially while taking medications that prolong the QT interval.

special instructions

Use with caution in patients with cardiovascular diseases and other conditions associated with the risk of arterial hypotension, especially at the beginning 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 decreases by approximately 25%. Therefore, quetiapine should be used with caution in patients with impaired liver and / or kidney function.

Use with caution simultaneously with drugs that lengthen the QT interval (especially in the elderly); with drugs that have a depressing effect on the central nervous system, as well as with ethanol; with potential inhibitors of the isoenzyme CYP3A4 (including with ketoconazole, erythromycin).

If NNS develops on the background of treatment, quetiapine should be discontinued and appropriate treatment should be prescribed.

With prolonged use, there is a possibility of developing 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 with ethanol.

In experimental studies, when studying the carcinogenicity of quetiapine, an increase in the incidence of mammary adenocarcinomas in rats (at doses of 20, 75 and 250 mg / kg / day) was noted, which is associated with prolonged hyperprolactinemia.

In male rats (250 mg / kg / day) and mice (250 and 750 mg / kg / day), an increase in the incidence of benign adenomas from thyroid follicular cells was noted, which was associated with a known rodent-specific mechanism of increased hepatic clearance of thyroxine.

Influence on the ability to drive vehicles and use mechanisms

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

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, its concentration in the blood plasma decreases.

With simultaneous use with thioridazine, an increase in the clearance of quetiapine is possible.