Serdollect, 4 mg 30 pcs

Cardoleptic is an atypical neuroleptic, phenylindole derivative, selectively acting on limbic structures. It has antipsychotic effect.

Pharmacodynamics

. The neuropharmacological profile of sertindole as an antipsychotic is due to selective blockade of mesolimbic dopaminergic neurons and a balanced inhibitory effect on central dopamine D₂ receptors and serotonin 5-HT₂ receptors as well as α₁ -adrenergic receptors.

Antipsychotics increase serum prolactin levels due to blockade of dopamine receptors. In patients taking Seardolect on short-term therapy and during long-term treatment (1 year), prolactin levels remained within normal limits.
Sertindol has no effect on muscarinic and histamine H₁ receptors, which is confirmed by the absence of anticholinergic and sedative effects that are associated with effects on these receptors.

Pharmacokinetics

Sertindol is well absorbed from the gut, with maximum concentration reached approximately 10 hours after ingestion. Food intake has no effect on the speed and magnitude of absorption.

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

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 feces and partially in the urine.

Indications

Treatment of schizophrenia.

Sertindol is not recommended for emergency treatment of acute psychotic disorders.

Active ingredient

Sertindol

Composition

active ingredient:

sertindol 4 mg.

inauxiliary substances

– corn starch,

lactose monohydrate, <

microcrystalline cellulose,

hyprolose, magnesium stearate,

sodium croscarmellose.

coating -hypromellose,

titanium dioxide (E171),

Macragol 400 and iron oxide yellow (E172)

How to take, the dosage

Cardolec is prescribed orally once a day, regardless of meals.

The treatment with Ceardolect should be started in all patients with 4 mg per day. The daily dose should be increased by 4 mg every 4 to 5 days until the optimal dose in the range of 12 to 20 mg/day is reached. The maximum dose is 24 mg/day.

The maximum dose is prescribed in exceptional cases because of the risk of QT interval prolongation with increasing dose.

Elderly patients:
Prescribing Ceardolect should be preceded by a thorough cardiovascular evaluation. Slower dose escalation is required and lower doses should be used.

Decreased renal function: Ceardolect may be used in usual dosages in patients with renal insufficiency. Hemodialysis does not affect the pharmacokinetics of the drug.

Decreased liver function: Slower dose escalation and lower doses should be used in patients with mild to moderate hepatic impairment.

Reappointment of Cardolect after a break in treatment: If less than a week has elapsed since stopping Cardolect, gradual dose escalation is not necessary (the previous dosage may be prescribed). In other cases, the dosage should be increased to the optimal dosage gradually by titration, and an ECG study should be performed before titration.

Transition from another neuroleptic: Treatment with Ceardolect may begin with the recommended gradual dose escalation at the same time as discontinuation of another oral neuroleptic. For patients on depot neuroleptic treatment, Cerdolect is prescribed instead of the next depot injection.

Interaction

The risk of QT interval prolongation increases with concomitant treatment with drugs that prolong the QT interval or inhibit the metabolism of sertindole. The use of Cserdolect concomitantly with such drugs is prohibited. Sertindol is metabolized by the cytochromes P₄₅₀ 2D6 and P₄₅₀ 3A.

Plasma concentrations of sertindol are increased when concomitantly administered with drugs that inhibit cytochrome P₄₅₀ 2D6 (fluoxetine, paroxetine, quinidine, etc.). It may be necessary to prescribe a lower maintenance dose, and an ECG examination before and after changing the dose of these drugs.

In turn, sertindol and its major metabolites have a weak inhibitory effect on the activity of cytochrome P₄₅₀2D6, through which β-adrenoblockers, antiarrhythmic agents, some hypotensive agents, a large number of antipsychotic drugs and antidepressants are metabolized.

The concomitant use of sertindol and macrolide antibiotics (erythromycin) and calcium channel blockers (diltiazem, verapamil) may result in a slight increase (4502D6. Because it is difficult to establish these patients routinely, concomitant use of sertindol and drugs that inhibit cytochrome P₄₅₀ 3A is contraindicated, as this may lead to a significant increase in plasma sertindol concentrations.

The metabolism of sertindol can be significantly increased, leading to a decrease in its plasma concentrations, under the influence of the following drugs – rifampicin, carbamazepine, phenytoin, phenobarbital. Decreased antipsychotic activity of sertindol in such cases may require increasing its dose.

Special Instructions

Because of the precautions associated with QT interval prolongation and ECG monitoring, sertindol should be prescribed in cases where at least one other antipsychotic is already intolerant.
The risk of QT interval prolongation is greater with higher doses (20-24 mg/day). QT interval prolongation while taking a number of drugs may lead to the development of paroxysms of ventricular tachycardia and sudden death.
Blood pressure monitoring is necessary during dose titration and at the beginning of maintenance therapy.

The cardiovascular system
An ECG study should be performed prior to prescribing Cardolect. If the QT interval exceeds 450 msec in men and 470 msec in women, Ceardolect should not be prescribed.
An ECG study should be performed before prescribing the drug, when equilibrium concentrations are reached approximately 3 weeks after initiation or a daily dose of 16 mg, and 3 months after initiation of treatment. During maintenance therapy, an ECG study should be performed every 3 months.
During maintenance treatment, ECG studies should be performed before and after increasing the sertindole dose or after joining/increasing the dose of a drug that may increase the blood concentration of sertindole.
If QT interval prolongation exceeds 500 msec, sertindol should be stopped.
If a patient presents with symptoms such as palpitations, seizures, fainting, indicating a possible arrhythmia, the treating physician should immediately begin an examination of the patient, including an ECG.
The ECG examination should preferably be performed in the morning.

Electrolyte disorders
Serum potassium and magnesium levels should be measured before starting treatment with CARDOLEKT in patients at risk of severe electrolyte disturbances. Hypokalemia and hypomagnesemia should be corrected before starting sertindol. Monitoring of plasma potassium concentrations is recommended in patients with vomiting and diarrhea, in patients taking potassium-eluting diuretics, and in other electrolyte disorders.

Parkinson’s disease
Antipsychotics may inhibit the effects of dopamine agonists. Cardolect should be used with caution in patients with Parkinson’s disease.

Decreased liver function
In mild to moderate cases of impaired liver function, close monitoring of the patient’s condition is necessary. A slower dose escalation and a smaller maintenance dose is recommended.

Convulsive seizures
Ceardolet should be prescribed with caution in patients with a history of seizures.

Late dyskinesia
Prolonged use of antipsychotic medications, especially in high doses, is associated with the risk of developing late dyskinesia. If symptoms of tardive dyskinesia occur while taking sertindol, the dosage should be reduced or the drug should be stopped altogether.

Malignant neuroleptic syndrome (MNS)
In cases of MNS, immediate withdrawal of the drug is necessary.

Withdrawal syndrome
Nausea, vomiting, increased sweating, and insomnia may occur if antipsychotics are abruptly withdrawn. Psychotic symptoms may also return and involuntary motor disorders (akathisia, dystonia, dyskinesia) may occur. Gradual withdrawal of the drug is necessary.

Auxiliary substances
Tablets contain lactose monohydrate. The drug should not be used in patients with hereditary galactose intolerance, lactase deficiency or impaired glucose and galactose absorption.

Pregnancy and lactation
Since the safety of Ceardolect in humans has not been studied, this drug should not be prescribed to pregnant women.
The safety of using Ceardolect in breastfeeding women has not been studied. In cases where the use of Sertindol has been found to be necessary, breastfeeding should be discontinued.

Children and adolescents (under 18 years)
The safety and effectiveness of Ceardolect has not been studied in children and adolescents, so the drug should not be used in children and adolescents.

Impact on ability to drive or operate machinery
Although Ceardolect has no sedative effect, patients are not recommended to drive or operate other machinery while taking it until individual tolerance of the drug is established.

Contraindications

• High sensitivity to the drug Ceardolect or its components.
• Ceardolect is contraindicated in unreported hypokalemia or hypomagnesemia.
• Serdolect should not be prescribed if there is a history or history of significant cardiovascular disease, congestive heart failure, myocardial hypertrophy, arrhythmia, or bradycardia (less than 50 beats per minute).
• The drug should not be administered to patients with congenital long QT interval syndrome or if relatives of the patient have this syndrome, or in cases of acquired long QT interval (over 450 msec in men and 470 msec in women).
• Do not prescribe Ceardolect 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), and cisapride, lithium and other QT interval-enhancing medications.
• Do not also prescribe Ceardolet with drugs that inhibit cytochrome P₄₅₀ 3A: “azole” antifungal agents (ketoconazole, itraconazole), macrolide antibiotics (erythromycin, clarithromycin), HIV proteinase inhibitors (indinavir), certain calcium channel blockers (verapamil, diltiazem), and cimetidine and other drugs that are cytochrome P₄₅₀ 3A inhibitors.
• Serdolect is contraindicated in severe hepatic insufficiency. Pregnancy, lactation, age under 18 years (safety and efficacy of the drug in these groups of patients has not been established).
  

Side effects

The following side effects have been observed (in decreasing order of frequency of occurrence):

• rinitis and difficulty breathing through the nose,
• decreased ejaculate volume,
• dizziness,
• dry mouth,
• postural hypotension,
• weight gain,
• peripheral edema,
• dyspnea,
• paresthesias,
long QT interval,
• leukocyturia and hematuria,
• hyperglycemia,
• syncopal conditions,
• movement disorders, including tardive dyskinesia,
• paroxysms of ventricular tachycardia (torsade de pointes type).

Extrapyramidal symptoms on sertindol occur with the same frequency as with placebo.
Malignant neuroleptic syndrome is very rare.
Some side effects, such as postural hypotension, are transient and occur at the beginning of therapy.

Overdose

Symptoms.
Drowsiness, slurred speech, tachycardia, decreased blood pressure and transient prolongation of the QT interval. Paroxysms of ventricular tachycardia (such as “torsade de pointes”) may develop, especially when using sertindol in conjunction with drugs that can cause this type of side effect.
Treatment.
In case of overdose, the drug should be stopped immediately and measures should be taken to maintain airway patency and adequate oxygenation.
Monitoring of ECG and basic somatic parameters should be started immediately. If the QT interval increases, the ECG is monitored until it is normalized, and the half-life of sertindol (2 to 4 days) must be taken into account.

The intravenous catheter should be placed, gastric lavage, activated charcoal and laxatives should be prescribed.
There is no specific antidote and the drug cannot be eliminated by dialysis. Therefore, supportive therapy should be prescribed. Correction of BP decrease and vascular collapse manifestations is carried out using intravenous injection of solutions. If sympathomimetics are used, adrenaline or dopamine should be used with caution because stimulation of β-adrenoreceptors together with the inherent antagonistic effect of sertindol on α₁-adrenoreceptors may result in a marked decrease in BP.

If antiarrhythmics are used, note that drugs such as quinidine, disopyramide, procainamide can potentially prolong the QT interval.
If severe extrapyramidal disorders develop, anticholinergic drugs should be prescribed. The patient should be under constant medical supervision until full recovery.

Pregnancy use

The safety of using the drug Ceardolet in pregnancy and lactation has not been studied.

Prescribing in pregnancy is contraindicated.

Breastfeeding should be stopped if it is necessary to use Ceardolect during lactation.