Serdolekt (sertindole) tablets 12 mg. №28

Description

Serdolekt (sertindole) coated tablets 12 mg. №28

Composition

active substance: sertindole;

1 tablet contains sertindol 4 mg or 12 mg;

auxiliary substances: corn starch; lactose, monohydrate; hydroxypropyl cellulose, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, hypromellose, macrogol 400, titanium dioxide (E 171); for 4 mg tablets – iron oxide yellow (E 172); for 12 mg tablets – iron oxide yellow (E 172), iron oxide red (E 172).

Medicinal form

Coated tablets.

The main physical and chemical properties:

• 4 mg: oval, yellow biconvex tablets marked “S4”;
• 12 mg: oval, beige biconvex tablets marked “S12”.

Pharmacotherapeutic group

Selective antipsychotics.
ATX code N05A E03.

Pharmacological properties

The neuropharmacological profile of the antipsychotic effect of sertindole is due to the selective blockade of mesolimbic dopaminergic neurons and a balanced inhibitory effect on central dopamine D2 and serotonin 5HT2 receptors, as well as on a1-adrenergic receptors. In pharmacological studies in animals, sertindole inhibited spontaneously active dopamine neurons in the ventral mesolimbic region of the brain with a selectivity factor greater than 100 compared to dopamine neurons in the substantia nigra pars compacta (SNC). Inhibition of SNC activity is thought to be involved in motor side effects (MSEs) associated with many antipsychotics. It is known that antipsychotic drugs increase the level of prolactin in blood plasma due to dopamine blockade. The level of prolactin in patients taking sertindole remains within the normal range both during the short and long-term (1 year) course of treatment. However, cases of hyperprolactinaemia and prolactin-related reactions have been occasionally reported during the post-marketing period of sertindole. Sertindole does not affect m-cholinergic receptors and histamine H1 receptors. This is proven by the absence of anticholinergic and sedative effects associated with these receptors.

Indications

Serdolekt tablets is a medicine designed to treat psychotic disorders.
It is mainly used to treat schizophrenia. It is not prescribed in emergency situations for the elimination of acute mental disorders.

Contraindications

Serdolekt tablets is contraindicated for allergies to components, low levels of potassium and / or magnesium in the blood, severe cardiovascular diseases, an increase in the size of the heart muscle (myocardial hypertrophy), heart rhythm disturbances (arrhythmia, bradycardia, long QT syndrome), liver dysfunction.
Do not prescribe Serdolect together with drugs that lengthen the QT interval (antiarrhythmics, some antipsychotics, antibiotics, antiallergic drugs, etc.), drugs that inhibit the liver enzyme cytochrome P450 3A (antifungal agents, antibiotics-macrolides, HIV proteinase inhibitors, calcium channel blockers and etc.).
The safety of Serdolect for children has not been established.

Application during pregnancy and lactation

Does not apply during these periods.

Method of administration and dosage

Serdolekt tablets is prescribed internally. The tablet is taken regardless of food.
All patients begin treatment with Serdolect with a dose of 4 mg x 1 time per day. Then the daily dose is increased by 4 mg every 4–5 days until the desired medicinal effect is achieved (the optimal dose is 12–20 mg / day). The maximum dose that can be taken per day is 24 mg. The maximum dose is used in exceptional cases, since there is a risk of a decrease in the electrical conductivity of the heart (lengthening of the QT interval) with increasing doses.
When prescribing Serdolect, older people need a preliminary examination of the cardiovascular system. The dose of the drug in this case is chosen lower and increased slowly.
Lower doses should also be used in patients with moderate liver failure (in severe cases, the drug is prohibited).
When the dose is increased, it is necessary to conduct an ECG study.

Overdose

Overdose signs: slurred speech, drowsiness, drop in blood pressure, temporary increase in the QT interval on the ECG. Perhaps the development of attacks of rapid and strong heartbeat – ventricular tachycardia (“torsade de pointes”).
Overdose treatment: immediate discontinuation of the drug, measures to maintain a sufficient level of oxygen in the blood, ensuring airway patency, immediate ECG examination and monitoring of the heart. If necessary, gastric lavage is performed, sorbents (activated carbon), laxatives are prescribed.
There is no specific antidote. The drug Serdolect cannot be withdrawn by dialysis.

Side effects

Runny nose, nasal breathing difficulties, fainting, decreased semen volume, dizziness, decreased pressure, dry mouth, weight gain, swelling, shortness of breath, creeping sensations on the skin, ECG changes (lengthening of the QT interval), changes in blood tests and urine (leukocyturia, hematuria, hyperglycemia), convulsions, movement disorders, bouts of rapid heartbeat.