Sertindole (Sertindolum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Neuroleptics

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    H. Lundbeck A / S     Denmark
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    N.05   Psychotherapy

    Pharmacodynamics:

    The antipsychotic effect is due to selective blockade of mesolimbic dopaminergic neurons and a balanced inhibitory effect on central dopamine D2-receptors and serotonin 5HT2-receptors, as well as α1-adrenoceptors.

    Pharmacokinetics:

    Absorption is fast. It penetrates the GEB and the placental barrier. The maximum concentration in the plasma - 10 hours after admission. Relationship with plasma proteins 99.5%. Biotransformation in the liver (CYP3A, 2D6) to inactive metabolites. The elimination half-life is about 3 days. Elimination with urine and feces.

    Indications:

    Schizophrenia (with the exception of acute psychotic disorders) with intolerance to other antipsychotic drugs.

    ICD-10

    V.F20-F29.F20.9   Schizophrenia, unspecified

    V.F20-F29.F20.8   Another type of schizophrenia

    V.F20-F29.F20.6   Simple type of schizophrenia

    V.F20-F29.F20.5   Residual schizophrenia

    V.F20-F29.F20.3   Undifferentiated schizophrenia

    V.F20-F29.F20.2   Catatonic Schizophrenia

    V.F20-F29.F20.1   Gebefrenic schizophrenia

    V.F20-F29.F20.0   Paranoid schizophrenia

    V.F20-F29.F20   Schizophrenia

    V.F20-F29   Schizophrenia, schizotypic and delusional disorders

    Contraindications:

    Hypersensitivity, hypokalemia, hypomagnesemia, decompensated diseases SSS (incl.chronic heart failure, myocardial hypertrophy, arrhythmia or bradycardia (heart rate less than 50 beats per minute), congenital syndrome of prolonged QT interval (including family history), acquired long QT interval syndrome (> 450 msec men and 470 ms in women), severe hepatic impairment, CNS depression of any etiology; simultaneous reception of drugs, extending the interval QT (incl. quinidine, sotalol, thioridazine, erythromycin, fluoroquinolones, terfenadine, cisapride, preparations of Li +) and drugs that inhibit the cytochrome P450 isoenzyme CYP3A (incl. itraconazole, erythromycin, indinavir, cimetidine); pregnancy, lactation.

    Carefully:

    Epilepsy, Parkinson's disease, hepatic insufficiency, elderly age, under 18 years of age (safety and efficacy not established).

    Pregnancy and lactation:

    Recommendation category FDA not determined.

    Contraindicated in pregnancy and during breastfeeding.

    Dosing and Administration:

    Inside, 1 time per day. The initial dose is 4 mg / day. The daily dose is increased by 4 mg every 4-5 days until the optimum dose is reached in the range of 12-20 mg / day, in exceptional cases - over 20 mg / day (significant increase in the risk of prolongation of the QT interval).In elderly patients, as well as with mild or moderate hepatic impairment, lower doses should be used and a slower dose build-up is required.

    Side effects:

    From the nervous system and sensory organs: dizziness, paresthesia, seizures, motor disorders (including late dyskinesia), extrapyramidal disorders (incidence is comparable to placebo), malignant neuroleptic syndrome.

    On the part of the respiratory system: rhinitis, difficulty in nasal breathing, dyspnea.

    On the part of the intestine: dry mouth.

    From the cardiovascular system and blood (hematopoiesis, hemostasis): postural hypotension, paroxysms of ventricular tachycardia (of the "torsade de pointes" type), prolongation of the QT interval.

    From the genitourinary system: leukocyturia, hematuria, decrease in ejaculate volume.

    Others: weight gain, peripheral edema, hyperglycemia, syncope.

    Overdose:

    Symptoms: drowsiness, slurred speech, tachycardia, decreased blood pressure and transient prolongation of the QT interval, paroxysms of ventricular tachycardia (such as "torsade de pointes"), especially in cases of concurrent admission with drugs that cause a similar side effect.

    Treatment: gastric lavage with the use of sorbent and the appointment of laxative drugs; ensuring airway patency and adequate oxygenation; ECG monitoring and basic physical indicators. In cases of increasing the QT interval, ECG monitoring is performed prior to the normalization of this parameter, and the half-life of sertindole (from 2 to 4 days) should be taken into account.

    Symptomatic therapy: with a decrease in blood pressure and the manifestation of vascular collapse, epinephrine or dopamine should be administered with caution (stimulation of beta-adrenoreceptors and antagonism with alpha-adrenergic receptors in sertindole can lead to a marked decrease in blood pressure). If it is necessary to use antiarrhythmic drugs, it should be taken into account that quinidine, disopyramide, procainamide potentially increase the QT interval. When developing severe extrapyramidal disorders, anticholinergic drugs are prescribed. There is no specific antidote.

    Interaction:

    Inhibitors of cytochrome P450 CYP2D6 (including fluoxetine, paroxetine, quinidine) and CYP3A (including H2-histamin blockers, antifungal drugs, HIV protease inhibitors, macrolides) - an increase in the concentration of sertindole, the risk of overdose.

    Antiepileptic drugs (carbamazepine, phenytoin) - a decrease in the concentration of sertindole in blood plasma.

    Sertindole and its major metabolites have a weak inhibitory effect on the activity of cytochrome P450 CYP2D6.

    Means that prolong the QT interval or inhibit the metabolism of sertindole, increase the risk of prolonging the QT interval.

    Special instructions:

    Do not use in emergency situations for relief of acute psychotic disorders.

    Control of blood pressure is necessary during the titration period and in the initial period of maintenance therapy.

    ECG monitoring should be performed before and during treatment when the equilibrium concentration is reached (approximately 3 weeks after the start of administration) or a daily dose of 16 mg. During maintenance ECG treatment, the study should be performed before and after a change in the dose of sertindole or after the addition / increase in the dose of other drugs that may increase the concentration of sertindole in the blood.

    When the QT interval is longer than 500 msec sertindole should be canceled.

    Because of the potential danger of prolonging the QT interval sertindole should be prescribed in cases where there is an intolerance of at least one other antipsychotic drug.

    The risk of prolongation of the QT interval increases with the use of doses in the range of 20-24 mg / day.

    If symptoms such as palpitations, convulsions, fainting, suggesting the possibility of arrhythmia, it is necessary to immediately begin the examination of the patient, including ECG monitoring.

    In patients with a risk of developing severe electrolyte disturbances, the serum concentration of K + and Mg2 + should be determined before starting treatment. Hypokalemia and hypomagnesemia should be corrected before starting treatment. It is recommended to monitor the concentration of K + in the blood plasma in patients with vomiting and diarrhea, in patients taking potassium-withdrawing diuretics, as well as in other electrolyte disorders.

    At a slight or moderate degree of hepatic insufficiency, careful monitoring of the patient's condition is necessary.

    When symptoms of tardive dyskinesia appear, you should reduce the dosage or cancel the drug. In cases of malignant neuroleptic syndrome, immediate withdrawal of the drug is necessary.

    Before establishing individual tolerability during the treatment period, one should refrain from engaging in potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions (including driving).

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