Сердолект

General characteristics. Structure:

Active ingredient: 4 mg, 12 mg, 16 mg or 20 mg of a sertindol.

Excipients: corn starch, lactoses monohydrate, microcrystallic cellulose, hypro rod, magnesium stearate, sodium of a kroskarmeloz.

Cover: a gipromelloza, titanium dioxide (E171), макрагол 400 and 4 mg - ferrous oxide yellow (E172), 12 mg - ferrous oxide yellow (E172), ferrous oxide red (E172), 16 mg - ferrous oxide red (E172), 20 mg - ferrous oxide yellow (E172), ferrous oxide red (E172), ferrous oxide black (E172).

Сердолект is the atypical neuroleptic derivative of a fenilindol selectively influencing limbic structures. Possesses antipsychotic action.

Pharmacological properties:

Pharmacodynamics. A neuropharmacological profile of a sertindol as antipsychotic means, it is caused by the selection blockade of mesolimbic dofaminergichesky neurons and the balanced inhibiting effect on the central dopamine D2 receptors and serotoninovy 5-HT2 receptors, and also on α1 - adrenergic receptors.

Anti-psychotics increase prolactin level in blood serum because of blockade of dopamine receptors. At the patients accepting Serdolekt at short-term therapy and during prolonged treatment (1 year), the level of prolactin remained within norm.

Sertindol does not influence muskarinovy and histamine H1 receptors that is confirmed by lack of anticholinergic and sedative effects which are connected with impact on these receptors.

Pharmacokinetics. Sertindol is well absorbed from intestines, the maximum concentration is reached approximately in 10 hours after reception. Meal does not render on the speed and size of absorption of influence.

The seeming volume of distribution of a sertindol after repeated use - about 20 l/kg. Sertindol for 99,5% contacts proteins of a blood plasma. Sertindol gets through hematoencephalic and placental barriers.

It is metabolized sertindol in a liver with the participation of tsitokhrom of P450 2D6 and P450 3A. Metabolites have no antipsychotic activity. The elimination half-life makes about 3 days. Sertindol and his metabolites are allocated, generally with a stake and, partially, with urine.

Indications to use:

Treatment of schizophrenia. Sertindol is not recommended to appoint in emergency situations for stopping of acute psychotic frustration.

Route of administration and doses:

Сердолект it is appointed inside once a day, regardless of meal. It is necessary to begin treatment by Serdolekt by all patient with 4 mg a day. The daily dose has to increase by 4 mg each 4 - 5 days before achievement of an optimum dose in the range from 12 to 20 mg/days. The maximum dose makes 24 mg/days. The maximum dose is appointed in exceptional cases owing to risk of lengthening of QT of an interval with increase in a dose.

Elderly patients. Careful inspection of cardiovascular system has to precede Serdolekt's appointment. Slower building of a dosage is required, lower doses have to be used.

Depression of function of kidneys. Сердолект it can be applied in usual dosages at patients with a renal failure. The hemodialysis does not influence drug pharmacokinetics.

Liver depression of function. Slower building of a dosage and lower doses have to be used at patients with a slight or moderate liver failure.

Repeated appointment of Serdolekt after a break in treatment. If from the moment of the termination of reception of Serdolekt passed less than a week, then gradual increase in a dosage is not obligatory (possibly purpose of a former dosage). In other cases it is necessary to increase a dosage to optimum gradually, by a titration method, at the same time before titration the ECG needs to conduct a research.

Transition from reception of other neuroleptic. Treatment by Serdolekt can begin with the recommended gradual building of a dose along with the termination of reception of other orally applied neuroleptic. For the patients who are on treatment by neuroleptics depots, Serdolekt is appointed instead of the following injection of depot.

Features of use:

Owing to the precautionary measures connected with increase in QT of an interval and monitoring of an ECG сертиндол it has to be appointed in cases where there is already an intolerance of at least one other anti-psychotic.

Danger of lengthening of QT of an interval is more at reception of higher doses (20-24 mg/days). Lengthening of QT of an interval at reception of a number of drugs can lead to development of paroxysms of ventricular tachycardia and sudden death.

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

Cardiovascular system. Before Serdolekt's appointment the ECG needs to conduct a research. At QT an interval at men and 470 ms at women of Serdolekt it is not necessary to appoint over 450 ms.

The research has to be conducted by an ECG before purpose of drug, at achievement of equilibrium concentration approximately in 3 weeks after the beginning of reception or a daily dose of 16 mg, and also in 3 months after an initiation of treatment. During a maintenance therapy of an ECG a research it is necessary to spend each 3 months.

During the ECG supporting treatments a research it has to be conducted before increase in a dose of a sertindol or after accession/increase in a dose of drug which can increase concentration of a sertindol in blood.

When lengthening QT of an interval over 500 ms сертиндол should be cancelled.

At emergence in the patient of such symptoms as heartbeat, spasms, faints, pointing to a possibility of existence of arrhythmia, the attending physician has to begin immediately inspection of the patient, including an ECG.

It is preferable to conduct an ECG a research in the morning.

Electrolytic disturbances. At patients with risk of development of the expressed electrolytic disturbances it is necessary to measure by Serdolekt before an initiation of treatment the level of potassium and magnesium in blood serum. The hypopotassemia and a hypomagnesiemia should be corrected prior to use of a sertindol. Control of potassium concentration in a blood plasma at patients with vomiting and diarrhea, at the patients accepting kaliyvyvodyashchy diuretics is recommended and also at other electrolytic disturbances.

Parkinson's disease. Antipsychotic means can inhibit effects of dopamine agonists. Сердолект it has to be used with care at patients with Parkinson's disease.

Reduced function of a liver. At insignificant or moderate degree of an abnormal liver function careful observation of a condition of the patient is necessary. Slower building of a dosage and a smaller maintenance dose is recommended.

Convulsive attacks. Сердолект it has to be appointed with care at patients with convulsive attacks in the anamnesis.

Late dyskinesia. Prolonged use of antipsychotic drugs, especially in high doses, is connected with risk of development of late dyskinesia. If against the background of reception of a sertindol there are its symptoms, then it is necessary to reduce a dosage or to absolutely cancel drug.

Malignant Antipsychotic Syndrome (MAS). In cases of development of ZNS immediate drug withdrawal is necessary.

Withdrawal. At sharp cancellation of anti-psychotics there can be nausea, vomiting, the increased sweating, sleeplessness. Return of psychotic symptoms and emergence of involuntary motive frustration (an akathisia, dystonia, dyskinesia) is also possible. Gradual drug withdrawal is necessary.

Excipients. Tablets contain monohydrate of lactose. To patients with hereditary intolerance of a galactose, insufficiency of lactase or disturbance of absorption of glucose and a galactose drug should not be appointed.

Pregnancy and feeding by a breast. As Serdolekt's safety at pregnancy at the person was not studied, this drug should not be appointed pregnant. Safety of use of Serdolekt for the nursing women was not studied. In cases where use of a sertindol is recognized as necessary, it is necessary to stop breastfeeding.

Children's and youthful age (up to 18 years). Safety and Serdolekt's efficiency at children and young men was not studied therefore drug should not be used at children's and youthful age.

Influence on ability to drive the car or other mechanisms. Though Serdolekt does not possess sedative action, patients are not recommended to drive against the background of its reception the car or other mechanisms until individual portability of drug is established.

Side effects:

The following side effects are observed (as reduction of frequency of emergence): rhinitis and difficulty of breath by a nose, reduction of volume of an ejaculate, dizziness, dryness in a mouth, postural hypotension, increase in weight, peripheral hypostases, short wind, paresthesias, lengthening of QT of an interval, a leukocyturia and a hamaturia, a hyperglycemia, syncopal states, convulsive frustration, motive disturbances, including late dyskinesia, paroxysms of ventricular tachycardia ("torsade de pointes" type).

Extrapyramidal symptoms against the background of reception of a sertindol arise with the same frequency, as when using placebo.

Malignant antipsychotic syndrome - it is very rare.

Some side effects, for example, postural hypotension, have tranzitorny character and arise at the beginning of therapy.

Interaction with other medicines:

The risk of increase in QT of an interval increases at the accompanying treatment by the drugs extending QT an interval or inhibiting metabolism of a sertindol. Serdolekt's use along with such drugs is forbidden.

Sertindol is metabolized by means of tsitokhrom of P450 2D6 and P450 3A.

Concentration of a sertindol in plasma increases at a concomitant use with drugs which inhibit P450 2D6 cytochrome (fluoxetine, пароксетин, quinidine, etc.). Purpose of lower maintenance dose, and also carrying out an ECG of inspection before change of a dose of these drugs can be required.

In turn, сертиндол and its main metabolites make the weak inhibiting impact on activity of P450 2D6 cytochrome by means of which β-adrenoblockers, antiaritmik, some antihypertensives, a large number of antipsychotic drugs and antidepressants are metabolized.

Simultaneous use of a sertindol and antibiotics macroleads (erythromycin) and blockers of calcium channels (diltiazem, verapamil) can lead to insignificant increase (<25%) concentration of a sertindol in plasma. However extent of increase can be higher at patients with weak activity of P450 2D6 cytochrome. As to establish in a planned order of these patients rather difficult, simultaneous use of a sertindol and the drugs inhibiting P450 3A cytochrome contraindicated as it can lead to substantial increase of level of concentration of a sertindol in plasma.

Metabolism of a sertindol can amplify considerably, leading to decrease in its concentration in a blood plasma, under the influence of the following drugs - rifampicin, carbamazepine, Phenytoinum, phenobarbital. Decrease in antipsychotic activity of a sertindol in similar cases can demand increase in its dose.

Contraindications:

• Hypersensitivity to drug or its components.

• Сердолект it is contraindicated at nekorregiruyemy to a hypopotassemia or a hypomagnesiemia.

• Сердолект it should not be appointed in the presence in the status or the anamnesis of the sick expressed cardiovascular diseases, congestive heart failure, a hypertrophy of a myocardium, arrhythmia or bradycardia (it is less than 50 beats per minute).

• Drug should not be appointed by the patient with an inborn syndrome of the extended QT of an interval or in the presence of this syndrome at the patient's relatives, and also in cases of the acquired extended QT of an interval (over 450 ms is at men and women have 470 ms).

• It is not necessary to appoint Serdolekt together with the drugs extending QT an interval: antiaritmikam of IA and the III classes (quinidine, соталол, Amiodaronum, дофетилид and др), some anti-psychotics (thioridazine), some antibiotics macroleads (erythromycin) and antibiotics of a hinolonovy row (гатифлоксацин), some antihistamines (терфенадин, астемизол), and also tsizapridy, the lithium and other medicines increasing QT an interval.

• It is also not necessary to appoint Serdolekt together with the drugs inhibiting P450 3A cytochrome: "azolovy" antifungal means (кетоконазол, итраконазол), antibiotics macroleads (erythromycin, кларитромицин), proteinase HIV inhibitors (индинавир), some blockers of calcium channels (verapamil, diltiazem), and also Cimetidinum and other medicines which are inhibitors of P450 3A cytochrome.

• Сердолект it is contraindicated at the expressed liver failure.

• Pregnancy, the lactation period, age up to 18 years (safety and efficiency of drug at these groups of patients are not established).

Overdose:

Symptoms. Drowsiness, muffled speech, tachycardia, decrease in the ABP and tranzitorny increase in QT of an interval. Development of paroxysms of ventricular tachycardia ("torsade de pointes" type), especially in cases of use of a sertindol together with the drugs capable to cause this type of side effect is possible.

Treatment. In case of overdose it is necessary to cancel immediately drug, measures have to be taken for maintenance of passability of respiratory tracts and adequate oxygenation. Monitoring of an ECG and main somatic indicators has to be immediately begun. In cases of increase in QT of an interval control of an ECG is carried out before normalization of this indicator, at the same time the elimination half-life of a sertindol (from 2 to 4 days) has to be considered.

It is necessary to establish an intravenous catheter, to appoint a gastric lavage, absorbent carbon and purgatives.

The specific antidote does not exist and drug cannot be removed by dialysis. Therefore the maintenance therapy has to be appointed.

Correction of decrease in the ABP and displays of a vascular collapse is carried out with use of intravenous administration of solutions. If at the same time sympathomimetics are used, then adrenaline or dopamine should be applied with care as stimulation of β-adrenoceptors together with antagonistic influence inherent to a sertindol on α1-адренорецепторы can lead to the expressed decrease in the ABP.

If antiaritmik are applied, then it is necessary to consider that such drugs as quinidine, Disopyramidum, procaineamide can potentially increase QT an interval. In case of development of heavy extrapyramidal disturbances anticholinergic drugs have to be appointed. The patient has to be under constant medical observation to an absolute recovery.

Storage conditions:

List B. In the place protected from light at a temperature not above 25 °C. To store in places, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated 4 mg, 12 mg, 16 mg, 20 mg. Packaging: 4 mg - 20 pieces, 30 pieces. On 10 tablets in a blister strip packaging (blister) from PVC and an Al-foil. 3 blisters with the application instruction in a cardboard pack. When packaging on CJSC ZIO-Zdorovye: on 10 tablets in a blister strip packaging (blister) from PVC and an Al-foil. 2 blisters with the application instruction in a cardboard pack.
12 mg - 14 pieces, 28 pieces, 56 pieces.
16 mg - 14 pieces, 28 pieces, 56 pieces.
20 mg - 14 pieces, 28 pieces, 56 pieces.
On 14 tablets in a blister strip packaging (blister) from PVC and an Al-foil. 2 blisters with the application instruction in a cardboard pack. When packaging on CJSC ZIO-Zdorovye: on 14 tablets in a blister strip packaging (blister) from PVC and an Al-foil. 1 or 4 blisters with the application instruction in a cardboard pack.