Serokvel 100

General characteristics. Structure:

Active agent: кветиапин 25, 100, 200 mg

Pharmacological properties:

Pharmacodynamics. Antipsychotic means (neuroleptic). Shows higher affinity to receptors of serotonin (5-HT2), than to receptors of D1 and D2 dopamine in a brain. Has tropism to histamine and to alfa1-adrenoceptors, is less active in relation to alfa2-adrenoceptors. Elective affinity to m-holino-and to benzodiazepine receptors is not revealed. Reduces activity of mesolimbic A10-dofaminergichesky neurons, in comparison with A9-nigrostriatnymi the neurons involved in motive functions. Does not cause long increase in concentration of prolactin. Communication duration with 5-HT2-serotoninovymi and D2 - dopamine receptors makes less than 12 h.

Pharmacokinetics. Absorption - high, meal does not influence bioavailability. Communication with proteins of plasma - 83%. It is actively metabolized in a liver with formation pharmacological of inactive metabolites under the influence of the CYP3A4 enzyme mediated by P450 cytochrome. Kvetiapin and some of his metabolites possess a weak inhibiting effect on enzymes of CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 cytochrome, but only in concentration, at 10-50 times exceeding those which arise at usually used dose - 300-450 mg/days. It is removed by kidneys of 73%, through intestines - 21%. T1/2 is 7 h. The average clearance at elderly patients is 30-50% less, than observed at patients aged from 18 up to 65 years. At a renal and liver failure the clearance decreases by 25%.

Indications to use:

Acute and chronic psychoses (including at schizophrenia).

Route of administration and doses:

Inside, 2 times a day, irrespective of meal. A daily dose for the first 4 days of therapy - 50 mg (1 day), 100 mg (2 day), 200 mg (3 day), 300 mg (4 day). Since 4 days, the dose has to be titrated to effective, ranging from 300 to 450 mg/days, if necessary - to 750 mg/days. At a renal and/or liver failure and elderly patients have an initial dose - 25 mg/days, with the subsequent daily increase by 25-50 mg before achievement of an effective dose.

Features of use:

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From a nervous system: drowsiness, dizziness, a headache, uneasiness, an adynamy, hostility, excitement, sleeplessness, an akathisia, a tremor, spasms, a depression, paresthesias, a malignant antipsychotic syndrome (a hyperthermia, muscular rigidity, the changed mental status, lability of the autonomic nervous system, increase in activity of KFK).

From CCC: orthostatic hypotension, tachycardia, lengthening of an interval of Q-T.

From the alimentary system: dryness of a mucous membrane of an oral cavity, nausea, vomiting, abdominal pain, diarrhea or lock, increase in activity of "hepatic" transaminases.

From respiratory system: pharyngitis, rhinitis.

Allergic reactions: skin rash, eosinophilia. Laboratory indicators: leukopenia, hypercholesterolemia, gipertriglitseridemiya, decrease in concentration of T4 (first 4 weeks).

Others: a back pain, thorax pain, subfebrile condition, increase in body weight (it is preferential in the first weeks of treatment), a mialgiya, a xeroderma, sight easing.

Interaction with other medicines:

Does not cause induction of the fermental systems of a liver involved in antipyrine metabolism. Inductors of microsomal systems of a liver (Phenytoinum, etc.), thioridazine increase clearance of a kvetiapin, inhibitors of microsomal systems of a liver - reduce; at the same time co-administration of a kvetiapin and antidepressants - Imipraminum (CYP2D6 inhibitor) or fluoxetine (CYP3A4 and CYP2D6 inhibitor) has no significant effect on its pharmacokinetics. HP, the oppressing TsNS, and ethanol increase risk of development of side effects.

Contraindications:

Hypersensitivity, pregnancy, lactation period.

Overdose:

Data on Serokvel's overdose are limited. Cases of reception of Serokvel in the dose exceeding 20 g without fatal effects are described and with a complete recovery, however there are messages on extremely exceptional cases of overdose by Serokvel leading to death and a coma. Symptoms: noted symptoms generally were a consequence of strengthening of the known pharmacological effects of drug, such as drowsiness excessive sedation, tachycardia and a lowering of arterial pressure. Treatment: there are no specific antidotes to a kvetiapin. In cases of serious intoxication it is necessary to consider the possibility of symptomatic therapy and it is recommended to hold the events directed to maintenance of function of breath, cardiovascular system, ensuring adykvatny oxygenation and ventilation. Attentive medical control and observation должо to be continued to an absolute recovery of the patient.

Storage conditions:

List B. To store at a temperature below 30 °C, in places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

tablets film coated 25, 100, 200 mg