Serdollect pills 16mg, 28pcs

Composition

1 coated tablet contains:

Active ingredient:

sertindol 16 mg

. excipients

-corn starch,

lactose monohydrate,

microcrystalline cellulose,

hyprolose,

magnesium stearate,

sodium croscarmelose.

shell:

hypromellose,

titanium dioxide (E 171),

macrogol 400 and 4 mg – iron oxide yellow (E 172),

12 mg – iron oxide yellow (E 172),

iron oxide red (E 172),

16 mg – iron oxide red (E 172),

20 mg – iron oxide yellow (E 172),

iron oxide red (E 172),

iron oxide black (E 172).

Pharmacological action

Serdolect is an atypical antipsychotic derived from phenylindole, which selectively affects limbic structures. It has an antipsychotic effect.

Pharmacodynamics

The neuropharmacological profile of sertindol as an antipsychotic agent is determined by the selective blockade of mesolimbic dopaminergic neurons and a balanced inhibitory effect on central_{dopamine D2} receptors and serotonin 5-HT2 receptors, as well as on_α1 – adrenergic receptors.

Antipsychotics increase serum prolactin levels due to blockage of dopamine receptors. In patients taking Serdolect during short-term therapy and during long-term treatment (1 year), prolactin levels remained within the normal range. Sertindol does not affect muscarinic and histamine_H1 receptors, which is confirmed by the absence of anticholinergic and sedative effects that are associated with exposure to these receptors.

Pharmacokinetics

Sertindol is well absorbed from the intestines, with a maximum concentration reached approximately 10 hours after ingestion. Food intake does not affect the rate and amount of absorption.

The apparent volume of distribution of sertindol after repeated use is about 20 l / kg. Sertindol is 99.5% bound to plasma proteins. Sertindol penetrates the blood-brain and placental barriers.

Sertindol is metabolized in the liver with the participation of cytochromes P₄₅₀ 2D6 and P₄₅₀ 3A.

The metabolites have no neuroleptic activity.

The elimination half-life is about 3 days.

Sertindol and its metabolites are excreted mainly in the faeces and partly in the urine.

Indications

Treatment of schizophrenia. Sertindol is not recommended to be prescribed in emergency situations for the relief of acute psychotic disorders.

Use during pregnancy and lactation

The safety of using Serdolect during pregnancy and lactation has not been studied.

Appointment during pregnancy is contraindicated.

If it is necessary to use Serdolect during lactation, stop breastfeeding.

Contraindications

• Serdolect is contraindicated in patients with uncorrected hypokalemia or hypomagnesemia.
• Serdolect should not be prescribed if patients have a history or status of severe cardiovascular diseases, congestive heart failure, myocardial hypertrophy, arrhythmia, or bradycardia (less than 50 beats per minute).
• The drug should not be prescribed to patients with congenital long QT syndrome or in the presence of this syndrome in relatives of the patient, as well as in cases of acquired long QT interval (over 450 msec in men and 470 msec in women).
• Serdolect should not be prescribed together with drugs that prolong the QT interval: class IA and III antiarrhythmics (quinidine, sotalol, amiodarone, dofetilide, etc. ), some antipsychotics (thioridazine), some macrolide antibiotics (erythromycin) and quinolone antibiotics (gatifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium, and other drugs that increase the QT interval.
• You should also assign Serdolect in conjunction with drugs that inhibit cytochrome P₄₅₀ 3A: “asalouye” antifungals (ketoconazole, Itraconazole), antibiotics–macrolides (erythromycin, clarithromycin), an HIV protease inhibitors (indinavir), certain calcium channel blockers (verapamil, diltiazem), as well as cimetidine and other drugs that are inhibitors of cytochrome P₄₅₀ 3A.
• Serdolect is contraindicated in patients with severe hepatic insufficiency. Pregnancy, lactation, age up to 18 years (safety and efficacy of the drug in these groups of patients have not been established).

Side effects

The following side effects are observed (in order of decreasing frequency of occurrence): : rhinitis and difficulty breathing through the nose, decreased ejaculate volume, dizziness, dry mouth, postural hypotension, weight gain, peripheral edema, shortness of breath, paresthesia, prolongation of the QT interval, leukocyturia and hematuria, hyperglycemia, syncopal states, convulsive disorders, motor disorders, including tardive dyskinesia, paroxysms of ventricular tachycardia (such as”torsade de pointes”).

Extrapyramidal symptoms occur with sertindol at the same rate as with placebo. Neuroleptic malignant syndrome is very rare.

Some side effects, such as postural hypotension, are transient and occur at the beginning of therapy.

Interaction

The risk of prolongation of the QT interval increases with concomitant treatment with drugs that prolong the QT interval or inhibit sertindol metabolism. The use of Serdolect simultaneously with such drugs is prohibited.

Sertindol is metabolized by cytochromes P₄₅₀ 2D6 and P₄₅₀ 3A.

The concentration of sertindol in plasma increases when taken simultaneously with drugs that inhibit cytochrome_P450 2D6 (fluoxetine, paroxetine, quinidine, etc. ). It may be necessary to prescribe a lower maintenance dose, as well as conduct an ECG examination before and after changing the dose of these drugs.

Sertindol and its major metabolites, in turn, have a weak inhibitory effect on the activity_{of cytochrome P450} 2D6, which is used to metabolize beta-blockers, antiarrhythmics, some antihypertensive agents, a large number of antipsychotic drugs and antidepressants.

Concomitant use of sertindol and macrolide antibiotics (erythromycin) and calcium channel blockers (diltiazem, verapamil) may result in a slight increase ( & 450 2D6. Since it is quite difficult to establish these patients in a planned manner, the simultaneous use of sertindol and drugs that inhibit cytochrome P – 3A is contraindicated, since this can lead to a significant increase in the level of sertindol concentration in plasma.

Sertindol metabolism can significantly increase, leading to a decrease in its concentration in blood plasma, under the influence of the following drugs: rifampicin, carbamazepine, phenytoin, phenobarbital. A decrease in the antipsychotic activity of sertindol in such cases may require an increase in its dose.

How to take, course of use and dosage

Serdolect is prescribed orally once a day, regardless of food intake. All patients should start treatment with Serdolect with 4 mg per day. The daily dose should be increased by 4 mg every 4 to 5 days until the optimal dose is reached in the range of 12 to 20 mg / day. The maximum dose is 24 mg / day. The maximum dose is prescribed in exceptional cases due to the risk of prolongation of the QT interval with increasing dose.

Elderly patients: The appointment of Serdolect should be preceded by a thorough examination of the cardiovascular system. A slower dosage build-up is required, and lower doses should be used.

Decreased renal function: Serdolect can be used in normal dosages in patients with renal insufficiency. Hemodialysis does not affect the pharmacokinetics of the drug.

Decreased liver function: A slower dosage build-up and lower doses should be used in patients with mild to moderate hepatic insufficiency.

Repeated use of Serdolect after a break in treatment: If less than a week has passed since stopping taking Serdolect, then a gradual increase in the dosage is not necessary (the previous dosage may be prescribed). In all other cases, the dosage should be increased to the optimal one gradually, by titration, and an ECG study should be performed before titration.

Switching from another antipsychotic: Treatment with Serdolect may begin with the recommended gradual dose increase at the same time as discontinuing the other oral antipsychotic. For patients undergoing treatment with neuroleptics-depo, Serdolect is prescribed instead of the next depo injection.

Overdose

Symptoms. Drowsiness, slurred speech, tachycardia, decreased blood pressure and a transient increase in the QT interval. It is possible to develop paroxysms of ventricular tachycardia (such as”torsade de pointes”), especially in cases of using sertindol together with drugs that can cause this type of side effect.

Treatment. In case of overdose, the drug should be discontinued immediately, measures should be taken to maintain airway patency and adequate oxygenation. ECG and basic somatic parameters should be monitored immediately. In cases of an increase in the QT interval, ECG monitoring is performed until this indicator normalizes, and the half-life of sertindol (from 2 to 4 days) should be taken into account.

An intravenous catheter should be installed, gastric lavage, activated charcoal, and laxatives should be prescribed. There is no specific antidote and the drug cannot be eliminated by dialysis. Therefore, maintenance therapy should be prescribed.

Correction of blood pressure reduction and manifestations of vascular collapse is carried out using intravenous solutions. If sympathomimetics are used, then epinephrine or dopamine should be used with caution, since the stimulation of beta-adrenergic receptors together with the antagonistic effect of sertindol_{on α1}-adrenergic receptors can lead to a pronounced decrease in blood pressure.

If antiarrhythmics are used, it should be taken into account that drugs such as quinidine, disopyramide, procainamide can potentially increase the QT interval. In case of severe extrapyramidal disorders, anticholinergic drugs should be prescribed. The patient should be under constant medical supervision until full recovery.

Special instructions

Due to the precautions associated with increasing the QT interval and ECG monitoring, sertindol should be prescribed in cases where there is already an intolerance to at least one other antipsychotic.

The risk of prolongation of the QT interval is greater when taking higher doses (20-24 mg / day). Prolongation of the QT interval when taking a number of drugs can lead to the development of paroxysms of ventricular tachycardia and sudden death.

Monitoring of blood pressure is necessary during the titration period of the dose and at the beginning of the maintenance therapy period.

Cardiovascular system Before prescribing Serdolect, it is necessary to conduct an ECG study. If the QT interval exceeds 450 msec in men and 470 msec in women, Serdolect should not be prescribed. An ECG test should be performed before prescribing the drug, when the equilibrium concentration is reached approximately 3 weeks after the start of taking or a daily dose of 16 mg, as well as 3 months after the start of treatment. During maintenance therapy, an ECG test should be performed every 3 months.

During maintenance treatment, an ECG test should be performed before and after increasing the dose of sertindol or after adding / increasing the dose of a drug that may increase the concentration of sertindol in the blood.

If the QT interval is prolonged beyond 500 ms, sertindol should be discontinued.

If the patient has symptoms such as palpitations, seizures, or fainting that indicate the possibility of an arrhythmia, the attending physician should immediately begin an examination of the patient, including an ECG. Conduct an ECG study preferably in the morning.

Electrolyte disturbances In patients at risk of developing severe electrolyte disturbances, the level of potassium and magnesium in the blood serum should be measured before starting treatment with Serdolect. Hypokalemia and hypomagnesemia should be corrected before starting sertindol. It is recommended to monitor the concentration of potassium in the blood plasma in patients with vomiting and diarrhea, in patients taking potassium-withdrawing diuretics, as well as in other electrolyte disorders.

Parkinson’s disease Antipsychotic drugs may inhibit the effects of dopamine agonists. Serdolect should be used with caution in patients with Parkinson’s disease.

Reduced liver function If there is a minor or moderate degree of liver dysfunction, careful monitoring of the patient’s condition is necessary. A slower dosage build-up and a smaller maintenance dose are recommended.

Convulsive seizures Serdolect should be administered with caution in patients with a history of convulsive seizures.

Tardive dyskinesia Long-term use of antipsychotic drugs, especially in high doses, is associated with the risk of tardive dyskinesia. If symptoms of sertindol occur while taking sertindol, then the dosage should be reduced or the drug should be completely discontinued.

Neuroleptic malignant syndrome (NMS) In cases of NMS, immediate discontinuation of the drug is necessary.

Withdrawal syndrome When antipsychotics are abruptly discontinued, nausea, vomiting, increased sweating, and insomnia may occur. The return of psychotic symptoms and the appearance of involuntary movement disorders (akathisia, dystonia, dyskinesia) are also possible. Gradual withdrawal of the drug is necessary.

Auxiliary substances Tablets contain lactose monohydrate. Patients with hereditary galactose intolerance, lactase deficiency or impaired glucose and galactose absorption should not be prescribed the drug.

Pregnancy and breast-feeding Since the safety of Serdolect during pregnancy in humans has not been studied, this drug should not be prescribed to pregnant women. The safety of using Serdolect in breast-feeding women has not been studied. In cases where the use of sertindol is considered necessary, breastfeeding should be discontinued.

Children and youth age (up to 18 years) The safety and efficacy of Serdolect in children and adolescents has not been studied, so the drug should not be used in children and adolescents.

Influence on the ability to drive a car or other mechanisms Although Serdolect does not have a sedative effect, patients are not recommended to drive a car or other mechanisms while taking it until individual tolerability of the drug is established.

Form of production

Film-coated tablets

Storage conditions

In a dark place, at a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Sertindol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets