Expiration date: 08/2025

Structure and Composition:

Film-coated tablets. One tablet contains sertindole 4 mg

Excipients: corn starch, lactose monohydrate, magnesium MCC giproloza stearate Croscarmellose sodium

shell: Hypromellose Macrogol 400 Titanium dioxide (E171) iron oxide yellow (E172)

in blisters of 10 pieces. a stack of cardboard packaging 2 or 3.

Film-coated tablets. One tablet contains sertindole 12 mg

Excipients: corn starch, lactose monohydrate, magnesium MCC giproloza stearate Croscarmellose sodium

shell: Hypromellose Macrogol 400 Titanium dioxide (E171) iron oxide yellow (E172), iron oxide red (E172)

in blisters of 14 pieces. In the paper cartons 1, 2 or 4 packaging.

Film-coated tablets. One tablet contains sertindole 16 mg

Excipients: corn starch, lactose monohydrate, magnesium MCC giproloza stearate Croscarmellose sodium

Excipients: corn starch, lactose monohydrate, magnesium MCC giproloza stearate Croscarmellose sodium

shell: Hypromellose Macrogol 400 Titanium dioxide (E171) Iron oxide red (E172)

in blisters of 14 pieces. In the paper cartons 1, 2 or 4 packaging.

Film-coated tablets. One tablet contains sertindole 20 mg

Excipients: corn starch, lactose monohydrate, magnesium MCC giproloza stearate Croscarmellose sodium

shell: Hypromellose Macrogol 400 Titanium dioxide (E171) iron oxide yellow (E172), iron oxide red (E172), black iron oxide (E172)

in blisters of 14 pieces. In the paper cartons 1, 2 or 4 packaging.

Description pharmaceutical form:

4 mg tablets: pale yellow, oval, biconcave, c symbol «S4» on one side.

12 mg Tablets: pale brownish-yellow, oval, biconcave, c symbol «S12» on one side.

Tablets 16 mg: brownish-pink color, oval, biconcave, with the symbol «S16» on one side.

Tablets 20 mg: pale pink color, oval, biconcave, with the symbol «S20» on one side.

Pharmacokinetics:

Suction

After oral administration sertindole well absorbed from the intestines, while Cmax is reached after 10 hours. The reception simultaneously with food has no effect on the absorption process.

Distribution

Binding to plasma proteins - 99.5%. The apparent volume of distribution - about 20 l / kg. It penetrates through the BBB 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.

breeding

T1 / 2 - about 3 days. Sertindole and its metabolites are excreted primarily in the feces and urine partially.

Description of the pharmacological actions:

Atypical antipsychotics, phenylindole derivative. Selectively affects the limbic structures. It has an antipsychotic effect. Neuropharmacological profile of sertindole selective blockade caused by the mesolimbic dopaminergic neurons and balanced inhibitory effect on central dopamine D2-receptor and serotonin 5-HT2-receptors, as well as adrenergic receptors & alpha1-.

Antipsychotic drugs increase levels of prolactin in the blood serum of the blockade of dopamine receptors. Patients taking Serdolect with short-term therapy and during long-term treatment (one year), prolactin levels remained in the normal range.

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

Indications:

Schizophrenia.

Contraindications:

• Hypersensitivity to the drug
  
• uncorrectable hypokalemia or hypomagnesemia
  
• expressed cardiovascular disease (including history)
  
• congestive heart failure
  
• myocardial hypertrophy
  
• arrhythmia
  
• bradycardia (<50 bpm. / min)
  
• congenital syndrome of elongated interval QT (including family history)
  
• Acquired extended interval QT (> 450 msec in males and 470 msec in females)
  
• the simultaneous use of drugs prolonging the interval the QT, including antiarrhythmics class IA and III (quinidine, sotalol, amiodarone, dofetilide), antipsychotics (thioridazine), macrolide antibiotics (erythromycin) antibiotics quinolone series (gatifloxacin), antihistamines (terfenadine, astemizole ) and cisapride, lithium preparations
  
• Simultaneous use of drugs that inhibit CYP3A isozymes, including antifungal agents from the group of azoles (itraconazole, ketoconazole), some macrolide antibiotics (erythromycin, clarithromycin), a HIV-protease inhibitors (indinavir), some CCBs (verapamil, diltiazem), cimetidine
  
• severe hepatic insufficiency
  
• pregnancy
  
• lactation (breastfeeding)
  
• childhood and adolescence to 18 years (safety and efficacy not established).
  

Application of pregnancy and breastfeeding:

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

Appointment during pregnancy is contraindicated.

If necessary, use Serdolect during lactation should stop breastfeeding.

Side effect:

The respiratory system: rhinitis, difficulty in nasal breathing, shortness of breath.

CNS: dizziness, paresthesia, rarely - syncope, seizures, movement disorders (including tardive dyskinesia), in some cases - neuroleptic malignant syndrome. Extrapyramidal disorders in patients receiving sertindole having the same frequency as that of placebo.

Cardio-vascular system: postural hypotension (is transient and occurs at the beginning of therapy), peripheral edema, rarely QT prolongation - paroxysmal ventricular tachycardia (including arrhythmia "pirouette" type).

From the urinary system: sometimes - leucocyturia, hematuria.

Other: sometimes - dry mouth, weight gain, decrease in the volume of ejaculate rarely - hyperglycemia.

Drug Interactions:

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

When used together with sertindole drugs that inhibit CYP2D6 (fluoxetine, paroxetine, quinidine), sertindole may increase the plasma concentration (it may require dose reduction, as well as conducting an ECG examination before and after the dose of these drugs).

Sertindole and its metabolites may have a weak inhibitory effect on CYP2D6, which is involved in the metabolism of beta-blockers, antiarrhythmics, antihypertensives some, many antipsychotics and antidepressants.

Concomitant use of sertindole and macrolide antibiotics (erythromycin) and CCBs (diltiazem, verapamil) may result in a slight increase (<25%) in sertindole plasma concentrations. The degree of increase may be higher in patients with low activity of CYP2D6. So how to identify these patients are routinely difficult enough, the simultaneous use of sertindole and drugs that inhibit CYP3A is contraindicated. 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 increase in the metabolism of sertindole, which leads to a significant reduction in neuroleptic plasma concentrations. In such cases, decrease antipsychotic activity of sertindole may require increasing the dose.

Dosage and administration:

Inside, regardless of meals, 1 time per day.

Starting dose - 4 mg / day. The daily dose is increased to 4 mg every 4-5 days until optimal doses ranging from 12 to 20 mg / day. In exceptional cases (due to risk of QT interval elongation with increasing dose) it is possible to use the drug in a maximum dose - 24 mg / day.

Elderly patients before prescribing Serdolect necessary to conduct a thorough examination of the cardiovascular system. Increasing the dose should be done slowly, using a lower dose.

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

Patients with mild to moderate hepatic impairment should increase more slowly and apply the drug dosage at lower doses.

If the re-appointment Serdolect after discontinuation was less than 1 week, then gradually increase the dose is not necessary (possible use of the drug at the same dose). In other cases, increasing the dose until the optimum should be carried out gradually, by titration, while prior to titration is required to conduct an ECG study.

When changing from another oral antipsychotic treatment Serdolect can start with the recommended dose of a gradual build-up at the same time with the abolition of the previous drug. When you go to the reception Serdolect after using antipsychotics in depot form of the first reception Serdolect appointed instead next injection depot.

Overdose:

Symptoms: drowsiness, slurred speech, tachycardia, decreased blood pressure, transient elongation of the QT interval. Perhaps the development of paroxysmal ventricular tachycardia (arrhythmia "pirouette" type), especially when used together with sertindole medications that can cause this kind of side effects.

Treatment: drug should be discontinued, set in / catheter to gastric lavage, administration of activated charcoal and laxatives should be taken to maintain the airway and adequate oxygenation. No specific antidote and the drug can not be removed by dialysis. Therefore, supportive treatment should be instituted. It is necessary to immediately begin ECG monitoring and control of key physical parameters. When extending the QT interval of ECG monitoring is carried out to the normalization of this index, however, note T1 / 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, because stimulation of adrenergic & beta-simultaneous antagonistic effect of sertindole on adrenergic receptors & alpha1-can lead to a marked reduction in blood pressure. When using antiarrhythmic drugs should be borne in mind that quinidine, procainamide, disopyramide may cause prolongation of the interval QT.

With the development of severe extrapyramidal disorders should be prescribed anticholinergic drugs.

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

Special instructions:

Due to the precautionary measures associated with an increase in the QT interval and ECG monitoring, Serdolect should be prescribed only in cases where there is already a intolerance to at least one other antipsychotic.

Risk increased QT interval elongation when receiving sertindole at higher doses (20-24 mg / day). Lengthening of the QT interval that occurs when the application of a number of drugs that can lead to the development of paroxysmal ventricular tachycardia and sudden death.

Blood pressure control is necessary during the dose titration period at the beginning and maintenance therapy.

ECG monitoring should be carried out prior to treatment and during therapy: upon reaching equilibrium (after about 3 weeks from the start of therapy) or 16 mg daily dose, and 3 months after starting treatment. During maintenance therapy ECG studies should be performed every 3 months before and after the change in dose or sertindole accession / increase the dose capable to increase the concentration of sertindole in plasma.

When extending the QT interval of more than 500 ms sertindole should be abolished. When the patient's heartbeat, seizures, fainting or other symptoms indicating the possibility of arrhythmia, the patient should be evaluated immediately (including ECG). ECG study is preferably carried out in the morning.

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

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

When mild or moderate hepatic dysfunction should be closely monitored for the condition of the patient is recommended to increase the dose more slowly and less maintenance dose.

Not recommended to prescribe in emergencies for the relief of acute psychotic disorders.

Precautions should be prescribed Serdolect patients with seizures in history.

Prolonged use of antipsychotics (especially in high doses) increases the risk of tardive dyskinesia. When the symptoms of tardive dyskinesia during treatment with Serdolect should reduce the dose or cancel it altogether.

With the development of congestive heart failure require immediate removal of the drug.

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

The tablets contain lactose monohydrate. It should not be prescribed to patients with hereditary galactose intolerance, lack of lactase, or violation of the 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 have not been studied, the purpose of this category Serdolect contraindicated patients.

Effects on ability to drive vehicles and management mechanisms

Although Serdolect does not have a sedative effect, patients are not recommended to engage in potentially hazardous activities that require attention as long as the individual response to the drug is established.