Serdolect coated pills 16mg N28
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Sertindol
Release form
Pills
Composition
Sertindol 16 mg; Excipients: corn starch, lactose monohydrate, microcrystalline cellulose, hyprolosis, magnesium stearate, croscarmellose sodium.; Shell composition: hypromellose, macrogol 400, titanium dioxide (E171), iron red oxide (E172).
Pharmacological effect
Antipsychotic, atypical neuroleptic, phenylindole derivative. It has an antipsychotic effect due to selective blockade of mesolimbic dopaminergic neurons and a balanced inhibitory effect on the central dopamine D2 receptors and serotonin 5HT2 receptors, as well as on 1-adrenoreceptor.; Sertindol does not affect muscarinic and histamine H1-receptors. sedative effects associated with effects on these receptors. Does not affect the level of prolactin.
Pharmacokinetics
After oral administration, sertindol is well absorbed from the gastrointestinal tract. Cmax in plasma is reached 10 hours after ingestion. Plasma protein binding - 99.5%. Metabolized in the liver with the participation of CYP2D6 and CYP3A isoenzymes. Metabolites do not possess neuroleptic activity. T1 / 2 is about 3 days. Sertindol and its metabolites are excreted mainly with feces and partially with urine.
Indications
Schizophrenia (with the exception of acute psychotic disorders), with intolerance to at least one antipsychotic.
Contraindications
Hypokalemia, hypomagnesemia; severe cardiovascular diseases (including history), including congestive heart failure, myocardial hypertrophy, arrhythmia or bradycardia (less than 50 beats / min), congenital long QT syndrome, or the presence of this syndrome in relatives of the patient, acquired elongated QT interval (more than 450 msec for men and 470 msec for women); simultaneous administration of drugs that prolong the QT interval (including class I A and III antiarrhythmics, some antipsychotics, macrolide antibiotics, fluoroquinolones, antihistamines, cisapride, lithium preparations); simultaneous administration of drugs inhibiting CYP3A isoenzymes (including antifungal agents derived from azole, macrolide antibiotics, HIV protease inhibitors, cimetidine); severe liver failure; depression of the central nervous system function of various etiologies; pregnancy, lactation; children and adolescents up to 18 years; hypersensitivity to sertindole.
Use during pregnancy and lactation
Contraindicated in pregnancy, during lactation.
Dosage and administration
Is ingested 1 time / day.; Initial dose - 4 mg / day. Depending on the individual reaction, the dose can be gradually increased to 20 mg / day. If you exceed the dose of 20 mg / day, the risk of prolongation of the QT interval increases significantly. In patients with mild or moderate liver failure, as well as in elderly patients, sertindole should be used in low doses and a slower dose increase.
Side effects
On the part of the respiratory system: often - rhinitis, difficulty in nasal breathing; rarely - shortness of breath.; CNS and peripheral nervous system: rarely - dizziness, paresthesia, syncopal states, convulsive disorders, movement disorders (including tardive dyskinesia), malignant neuroleptic syndrome;; Digestive system: rarely - dry mouth .; Since the cardiovascular system: rarely - postural hypotension, an increase in the QT interval, paroxysmal ventricular arrhythmias (like "pirouette") .; From the urinary system: rarely - leukocyturia, hematuria; in: rarely - weight gain, hyperglycemia, Other:. peripheral edema, reduction of volume of ejaculate.
Overdose
Symptoms Drowsiness, slurred speech, tachycardia, lowering blood pressure and transient increase in the QT interval. The development of paroxysms of ventricular tachycardia (like & "torsade de pointes &") is possible, especially in cases of using Sertindole in conjunction with drugs that can cause this type of side effect .; Treatment. In case of overdose, the drug should be immediately discontinued, measures should be taken to maintain the airway and ensure adequate oxygenation. Monitoring of the ECG and the main somatic indicators should be started immediately. In cases of an increase in the QT interval, ECG monitoring is performed before normalization of this indicator, and the half-life of sertindole should be taken into account (from 2 to 4 days). ; Intravenous catheter should be installed, gastric lavage, activated carbon and laxatives should be prescribed. ; A specific antidote does not exist and the drug can not be bred by dialysis.Therefore, maintenance therapy should be prescribed. ; Correction of blood pressure reduction and manifestations of vascular collapse is performed using intravenous administration of solutions. If sympathomimetics are used, adrenaline or dopamine should be used with caution, since stimulation of β-adrenergic receptors together with the characteristic antagonistic effect on sertindole on 1-adrenoreceptors can lead to a pronounced decrease in blood pressure. ; If antiarrhythmic drugs are used, then it should be borne in mind that drugs such as quinidine, disopyramide, procainamide can potentially increase the QT interval. If severe extrapyramidal disorders develop, anticholinergic drugs should be prescribed. The patient must be under constant medical supervision until full recovery.
Interaction with other drugs
With simultaneous use with drugs that increase the QT interval, the risk of this effect increases. Since sertindole is metabolized with the participation of CYP2D6 and CYP3A isoenzymes, it can be increased while taking with CYP2D6 isoenzyme inhibitors (including fluoxetine, paroxetine, quinidine) sertindole plasma levels. Sertindol and its main metabolites are weak inhibitors of the activity of the CYP2D6 isoenzyme, with the participation of which beta-blockers, antiarrhythmics, some antihypertensive drugs, many antipsychotic drugs and antidepressants are metabolized. HIV proteases (macrolide antibiotics) can significantly increase sertindole concentration in the blood plasma.; Under the influence of carbamazepine, phenytoin Rapid metabolism of sertindole, which leads to a decrease in its plasma concentrations and a decrease in antipsychotic action.
special instructions
It is used with caution in patients with epilepsy, Parkinson's disease, hepatic insufficiency, in elderly patients. It is not recommended to use in emergency cases for stopping acute psychotic disorders. When taking a number of drugs, lengthening of the QT interval is associated with the development of paroxysmal ventricular tachycardia (such as " pirouette "); Because of the potential danger of prolongation of the QT interval, sertindol should be used in cases where there is already intolerance of at least one antipsychotic drug.; Monitoring ECG should be performed before the start of treatment.when the equilibrium concentration is reached (approximately 3 weeks after the start of administration) or when the dose reaches 16 mg / day. During maintenance therapy, an ECG study should be carried out before and after changing the dose of sertindole or after adding / increasing the dose of the drug, which can increase the concentration of sertindole in the blood plasma. With an increase in the QT interval of more than 500 ms, sertindol should be canceled. Blood pressure monitoring is necessary during the dose titration period and at the beginning of the maintenance therapy period. ) should immediately begin the examination of the patient, including an ECG.; Before the start of the use of sertindole, correction of hypokalemia and hypomagnesemia should be carried out. When vomiting, diarrhea, against the background of the use of diuretics, which can cause hypokalemia, with electrolyte disorders, it is recommended to monitor the concentration of potassium in the blood. in high doses, the risk of tardive dyskinesia increases. If symptoms of tardive dyskinesia or neuroleptic malignant sertindol syndrome occur, they should be discontinued; activities to determine the individual response of the patient to treatment.