SERDOLEKT

Active material: Sertindole
When ATH: N05AE03
CCF: Antipsychotic drug (anxiolytic)
ICD-10 codes (testimony): F20, F21, F22, F25
When CSF: 02.01.02.05
Manufacturer: H.LUNDBECK A/S (Denmark)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, coated pale yellow, Oval, lenticular, with symbol “S4” on one side.

Excipients: corn starch, lactose monohydrate, microcrystalline cellulose, giproloza, magnesium stearate, sodium croscarmellose.

The composition of the shell: gipromelloza, macrogol 400, Titanium dioxide (E171), iron oxide yellow (E172).

10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.

Pills, coated pale yellow-brown color, Oval, lenticular, with symbol “S12” on one side.

Excipients: corn starch, lactose monohydrate, microcrystalline cellulose, giproloza, magnesium stearate, sodium croscarmellose.

The composition of the shell: gipromelloza, macrogol 400, Titanium dioxide (E171), iron oxide yellow (E172), iron oxide red (E172).

14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
14 PC. – blisters (4) – packs cardboard.

Pills, coated brownish pink, Oval, lenticular, the symbol “S16” on one side.

Excipients: corn starch, lactose monohydrate, microcrystalline cellulose, giproloza, magnesium stearate, sodium croscarmellose.

The composition of the shell: gipromelloza, macrogol 400, Titanium dioxide (E171), iron oxide red (E172).

14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
14 PC. – blisters (4) – packs cardboard.

Pills, coated pale pink, Oval, lenticular, the symbol “S20” on one side.

Excipients: corn starch, lactose monohydrate, microcrystalline cellulose, giproloza, magnesium stearate, sodium croscarmellose.

The composition of the shell: gipromelloza, macrogol 400, Titanium dioxide (E171), iron oxide yellow (E172), iron oxide red (E172), iron oxide black (E172).

14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
14 PC. – blisters (4) – packs cardboard.

Pharmacological action

Atypical antipsychotics, phenylindole derivative. Selectively affects the limbic structures. It has antipsychotic action. Neuropharmacological profile of sertindole due to selective blockade of the mesolimbic dopaminergic neurons and balanced inhibitory effects on central dopamine D₂-receptors and serotonin 5-HT₂-receptors, as well as α₁-adrenoreceptory.

Antipsychotic drugs increase prolactin levels in the blood serum of the blockade of dopamine receptors. Patients, Serdolekt host at the short-term therapy and during prolonged treatment (1 year), prolactin levels remained within the normal range.

Sertindole has no effect on muscarinic and histamine H₁-receptors, as evidenced by the absence of anticholinergic and sedative effects, are associated with exposure to these receptors.

Pharmacokinetics

Absorption

After oral administration Sertindole is well absorbed from the gut, wherein C_max achieved through 10 no. Receiving simultaneously with food has no effect on the absorption process.

Distribution

Plasma protein binding is 99.5%. In Кажущийся_d – about 20 l / kg. Penetrates the GEB and placental barrier.

Metabolism

It is metabolized in the liver with the participation isozymes CYP2D6 and CYP3A. Metabolites of the drug did not have neuroleptic activity.

Deduction

T_1/2 is about 3 days. Sertindole and its metabolites are excreted mainly in the feces and urine partially.

Testimony

- Schizophrenia.

Do not appoint emergency for relief of acute psychotic disorders.

Dosage regimen

The drug is taken orally 1 time / day, regardless of the meal.

The initial dose is 4 mg / day. The daily dose is increased by 4 mg every 4-5 days until the optimal dose in the range of 12 mg / day to 20 mg / day. In exceptional cases, (due to the risk of QT prolongation with increasing dose) possible use of the preparation in maximum doses – 24 mg / day.

Elderly patients until the appointment Serdolekta necessary to conduct a thorough examination of the cardiovascular system. Increasing the dose should be slowly, using a lower dose.

In patients with renal insufficiency correction dosing regime is not required. Hemodialysis does not affect the pharmacokinetics of the drug.

In Patients with mild or moderate hepatic insufficiency should increase the dose more slowly and use the drug at lower doses.

If when re-appointment Serdolekta after discontinuation passed less than a week, the gradual increase of the dose is not necessary (possible use of the drug at the same dose). In other cases, increasing the dose to the optimum should be gradual, titration, at the same time before titration is required to conduct ECG study.

At switching from another oral antipsychotic Serdolektom treatment can begin with a gradual increase of the recommended dosage at the same time with the abolition of the previous formulation. At going to the reception after Serdolekta neuroleptics in Depo-form first reception Serdolekta appointed instead next injection depot.

Side effect

The respiratory system: rhinitis, obstruction of nasal breathing, breathlessness.

CNS: dizziness, paresthesia; rarely – syncope, convulsions, movement disorders (including tardive dyskinesia); in some cases – neuroleptic malignant syndrome. Extrapyramidal disorders in patients receiving sertindole occur with the same frequency, and that with placebo.

Cardio-vascular system: postural hypotension (It is transient and occurs at the beginning of therapy), peripheral edema, QT prolongation; rarely – paroxysmal ventricular tachycardia ( incl. the type of arrhythmia “pirouette”).

From the urinary system: sometimes – leucocyturia, hematuria.

Other: sometimes – dry mouth, weight gain, decrease in the volume of ejaculate; rarely – giperglikemiâ.

Contraindications

- Uncorrectable hypokalemia or hypomagnesemia;

- Expressed cardiovascular disease (incl. history);

- Congestive heart failure;

- Myocardial hypertrophy;

- Arrhythmia;

- Bradycardia (less 50 u. / min);

- Congenital long QT syndrome (incl. family history);

- Acquired QT prolongation (more 450 ms in men and 470 msec in women);

- Simultaneous use of drugs, prolonging the QT interval, including antiarrhythmics class IA and III (quinidine, sotalol, Amiodarone, dofetilid), Some antipsychotics (tioridazin), some macrolide antibiotics (Erythromycin), some quinolone antibiotics number (gatifloxacin), Some antihistamines (terfenadine, astemizol), and cisapride, lithium preparations;

- Simultaneous use of drugs, inhibiting CYP3A isoenzymes, including antifungal agents from the group of azoles (itraconazole, ketoconazole), some macrolide antibiotics (Erythromycin, clarithromycin), HIV protease inhibitors (indinavir), Some calcium channel blockers (verapamil, diltiazem), cimetidine;

- Severe hepatic impairment;

- Pregnancy;

- Lactation (breast-feeding);

- Childhood and adolescence up 18 years (Safety and efficacy have not been established);

- Hypersensitivity to the drug.

Pregnancy and lactation

Safety of Serdolekta during pregnancy and lactation has not been studied.

Appointment during pregnancy is contraindicated.

If necessary, use Serdolekta during lactation should stop breastfeeding.

Cautions

Due precautions, associated with an increase in QT interval and ECG monitoring Serdolekt should be given only in cases, when it has an intolerance to at least one other antipsychotic.

Risk of QT prolongation increases when receiving sertindole higher doses (20-24 mg / day). QT prolongation, arising from the application of a number of drugs, can lead to the development of paroxysmal ventricular tachycardia, and sudden death.

BP control is necessary during titration and at the start of maintenance therapy.

ECG monitoring should be performed before treatment and during treatment: when the equilibrium state (approximately 3 weeks of therapy) or a daily dose 16 mg, and through 3 months after initiation of treatment. During maintenance therapy an ECG study should be carried out every 3 Months. ECG study should be conducted before and after increasing the dose of sertindole or accession / increase in dose, which may cause an increase in the concentration of sertindole in plasma.

When QT prolongation over 500 ms sertindole should be abolished. When the patient's heartbeat, seizures, fainting or other symptoms, pointing to the possibility of developing an arrhythmia, immediately examine the patient (including an electrocardiogram). ECG study is preferably carried out in the morning.

In patients with increased risk of electrolyte abnormalities before starting therapy Serdolektom should determine the concentration of potassium and magnesium in the blood serum. Hypokalemia and hypomagnesemia should be corrected prior to use of sertindole. Recommend conduct regular monitoring of the concentration of potassium in the blood serum of patients with vomiting and diarrhea, when applying kaliyvyvodyaschih diuretics and other electrolyte disorders.

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

At low to moderate liver dysfunction should be carefully monitored for the patient's condition; It recommends a slow increase in the dose and lower maintenance dose.

Precautions should be prescribed Serdolekt patients with a history of seizures.

Long-term use of antipsychotics (especially in high doses) It increases the risk of tardive dyskinesia. When symptoms of tardive dyskinesia during treatment with Serdolekta dose should be reduced or completely cancel it.

With the development of the CSN required the immediate withdrawal of the drug.

With a sharp lifting of antipsychotics can cause nausea, vomiting, increased perspiration, insomnia. It is also possible the return of psychotic symptoms and the emergence of involuntary movement disorders (akathisia, dystonia, dyskinesia). You need gradual removal of the drug.

The tablets contain lactose monohydrate. It should not be prescribed to patients with hereditary galactose intolerance, lactase deficiency or impaired absorption of glucose and galactose.

Use in Pediatrics

The safety and efficacy of the drug in children and adolescents under the age of 18 years We have not been studied, appointment Serdolekta these patients is contraindicated.

Effects on ability to drive vehicles and management mechanisms

Although Serdolekt does not have a sedative effect, Patients are advised not to engage in potentially dangerous activities, require attention, until, until you have established an individual response to the drug.

Overdose

Symptoms: drowsiness, gibberish, tachycardia, decrease in blood pressure, transient prolongation of the interval QT. Perhaps the development of paroxysmal ventricular tachycardia (the type of arrhythmia “pirouette”), especially when used together with drugs sertindole, which can cause this type of side effects.

Treatment: the drug should be discontinued, set / catheter, to gastric lavage, administration of activated charcoal and laxatives; measures must be taken to maintain the airway and adequate oxygenation. No specific antidote and the drug can not be removed by dialysis. Therefore, it should be assigned supportive care. It is necessary to immediately begin ECG monitoring and control of key physical parameters. When QT prolongation ECG monitoring is carried out to the normalization of this index, however, note T_1/2 sertindole (from 2 to 4 days).

When the correction of blood pressure lowering and manifestations of vascular collapse in / in a solution of dopamine or epinephrine should be made with caution, tk. stimulation of β-adrenergic receptors with simultaneous antagonistic effect of sertindole for α₁-adrenergic receptors can lead to a marked decrease in blood pressure. When using antiarrhythmic drugs should be considered, Chto quinidine, prokaynamyd, disopyramide may cause QT prolongation.

With the development of severe extrapyramidal disorders should be prescribed anticholinergics.

The patient should be under constant medical supervision until complete recovery.

Drug Interactions

The risk of QT prolongation is increased by concomitant use of drugs, prolong the QT interval or inhibit the metabolism of sertindole (these combinations are contraindicated).

In a joint application with drugs sertindole, inhibitory CYP2D6 (fluoxetine, paroxetine, quinidine), may increase the concentration of sertindole in plasma (You may need to reduce the dose, as well as carrying out ECG examination before and after the doses of these drugs).

Sertindole and its metabolites may have a weak inhibitory effect on CYP2D6, which is involved in the metabolism of beta-blockers, antiaritmikov, Some antihypertensive agents, many antipsychotics and antidepressants.

The simultaneous use of sertindole and macrolide antibiotics (Erythromycin) and calcium channel blockers (diltiazem, verapamil) may lead to a slight increase (<25%) Sertindole concentration in plasma. The magnification level may be higher in patients with weak activity CYP2D6. As set routinely in these patients is difficult enough, the simultaneous use of sertindole and preparations, inhibiting CYP3A contraindicated, tk. this can lead to a significant increase in the concentration of sertindole in plasma.

In an application with carbamazepine, phenytoin, phenobarbital and rifampicin may be a significant strengthening of the metabolism of sertindole, which leads to a substantial reduction in the plasma concentration of antipsychotic blood. In such cases, the decrease antipsychotic activity of sertindole may require increasing the dose.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored in the dark, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 5 years.