Sertindol
Lundbeck AS
1391 Items
2019-09-19
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Clinical Pharmacology
Serdolect is an atypical neuroleptic, a derivative of phenylindole, selectively acting on limbic structures. It has antipsychotic action.
Pharmacodynamics
The neuropharmacological profile of sertindole as an antipsychotic agent is due to the selective blockade of mesolimbic dopaminergic neurons and a balanced inhibitory effect on central dopamine D2 receptors and serotonin 5-HT2 receptors as well as on α1 - adrenergic receptors.
Antipsychotics increase the level of prolactin in the serum due to the blockade of dopamine receptors. In patients taking Serdolect with short-term therapy and during long-term treatment (1 year), the level of prolactin remained within the normal range.
Sertindol does not affect muscarinic and histamine H1 receptors, as evidenced by the absence of anticholinergic and sedative effects that are associated with effects on these receptors.
Pharmacokinetics
Sertindol is well absorbed from the intestines, the maximum concentration is reached approximately 10 hours after administration. Food intake at the speed and magnitude of absorption has no effect.
The apparent volume of distribution of sertindole after repeated use is about 20 l / kg. Sertindol is 99.5% bound to plasma proteins. Sertindol penetrates the blood-brain and placental barriers.
Sertindol is metabolized in the liver with the participation of cytochromes P450 2D6 and P450 3A.
Metabolites do not have neuroleptic activity.
The half-life is about 3 days.
Sertindol and its metabolites are mainly excreted in feces and, in part, with urine.
Indications
Treatment of schizophrenia.
Sertindol is not recommended in emergency situations for the relief of acute psychotic disorders.
Composition
1 coated tablet contains:
active substance: sertindol 4 mg.
Excipients - corn starch, lactose monohydrate, microcrystalline cellulose, hyprolosis, magnesium stearate, croscarmelose sodium.
shell: hypromellose, titanium dioxide (E171), macrogol 400 and 4 mg - iron oxide yellow (E172), 12 mg - iron oxide yellow (E172), iron red oxide (E172), 16 mg - iron red oxide (E172), 20 mg - iron oxide yellow (E172), iron oxide red (E172), iron oxide black (E172).
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Dosage and Administration
Serdolect is administered orally once a day, regardless of the meal.
All patients should begin treatment with Serdolect with 4 mg per day. The daily dose should be increased by 4 mg every 4 to 5 days until the optimum dose in the range from 12 to 20 mg / day is reached. The maximum dose is 24 mg / day.
The maximum dose is prescribed in exceptional cases due to the risk of prolongation of the QT interval with an increase in dose.
Elderly patients:
The appointment of Serdolect should be preceded by a thorough examination of the cardiovascular system. A slower dosage increase is required, lower doses should be used.
Reduced kidney function: Serdolect can be used in usual dosages in patients with renal insufficiency. Hemodialysis does not affect the pharmacokinetics of the drug.
Decreased liver function: Slower dosage buildup and lower doses should be used in patients with mild or moderate liver failure.
Re-appointment of Serdolect after a break in treatment: If less than a week has passed since the termination of taking Serdolect, then a gradual increase in dosage is not necessary (it is possible to prescribe the previous dosage). In other cases, the dosage should be increased to the optimum gradually, using a titration method, while an ECG study should be carried out before titration.
The transition from taking another neuroleptic: Treatment with Serodect can begin with the recommended gradual increase in dose simultaneously with the discontinuation of taking another oral antipsychotic. For patients undergoing treatment with neuroleptic depot, Serdolect is prescribed instead of the next depot injection.
Adverse reactions
The following side effects are observed (in order of decreasing incidence): rhinitis and difficulty breathing through the nose, reducing the volume of ejaculate, dizziness, dry mouth, postural hypotension, weight gain, peripheral edema, shortness of breath, paresthesia, prolongation of the QT interval, leukocyturia and hematuria, hyperglycemia , syncopal states, convulsive disorders, motor disorders, including tardy dyskinesia, paroxysmal ventricular tachycardia (such as & "torsade de pointes &").
Extrapyramidal symptoms in patients receiving sertindole occur with the same frequency as when using placebo.
Malignant neuroleptic syndrome is very rare.
Some side effects, such as postural hypotension, are transient in nature and occur at the beginning of therapy.
Drug interactions
The risk of increasing the QT interval is increased with concomitant treatment with drugs that prolong the QT interval or inhibit serindol metabolism. Using Serdolect simultaneously with such drugs is prohibited.
Sertindole is metabolized by cytochrome P450 2D6 and P450 3A.
The concentration of sertindole in plasma increases with simultaneous use with drugs that inhibit cytochrome P450 2D6 (fluoxetine, paroxetine, quinidine, etc.). You may need a lower maintenance dose, as well as 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 P450 2D6, which metabolizes β-blockers, antiarrhythmics, some antihypertensive drugs, a large number of antipsychotic drugs and antidepressants.
The simultaneous use of sertindole and macrolide antibiotics (erythromycin) and calcium channel blockers (diltiazem, verapamil) can lead to a slight increase (& 450 2D6. Since it is difficult to establish these patients in a planned manner, the simultaneous use of sertindole and cytochrome P inhibiting drugs450 3A is contraindicated, as it can lead to a significant increase in sertindole plasma levels.
Sertindole metabolism can significantly increase, leading to a decrease in its concentration in the blood plasma, under the influence of the following drugs - rifampicin, carbamazepine, phenytoin, phenobarbital. Reducing the antipsychotic activity of sertindole in such cases may require an increase in its dose.
Pregnancy and Lactation
The safety of the use of the drug Serdolect during pregnancy and lactation has not been studied.
Appointment during pregnancy is contraindicated.
If necessary, use Serdolekta during lactation should stop breastfeeding.
Special instructions
Due to precautions associated with an increase in the QT interval and ECG monitoring, sertindol should be administered in cases where there is already intolerance to at least one other antipsychotic.
The risk of prolongation of the QT interval is greater when taking higher doses (20-24 mg / day). Elongation of the QT interval when taking a number of drugs can lead to the development of paroxysms of ventricular tachycardia and sudden death.
Blood pressure monitoring is necessary during the dose titration period and at the beginning of the maintenance period.
The cardiovascular system
Before the appointment of Serdolect need to conduct an ECG study. When the QT interval is above 450 msec for men and 470 msec for women, the Serdolect should not be prescribed.
ECG examination should be carried out before the appointment of the drug, when the equilibrium concentration is reached approximately 3 weeks after the start of administration or a daily dose of 16 mg, and 3 months after the start of treatment. During ECG maintenance therapy, the study should be done every 3 months.
During supportive ECG treatment, the study should be carried out before and after increasing the dose of sertindole or after adding / increasing the dose of the drug, which can increase the concentration of sertindole in the blood.
When extending the QT interval above 500 ms, sertindole should be canceled.
When the patient has symptoms such as palpitations, convulsions, fainting, indicating the possibility of arrhythmia, the attending physician should immediately begin the examination of the patient, including the ECG.
To conduct an ECG study preferably in the morning.
Electrolyte disorders
In patients at risk of developing severe electrolyte abnormalities, the level of serum potassium and magnesium should be measured before starting treatment with Serdolect. Hypokalemia and hypomagnesemia should be adjusted prior to the use of sertindole. It is recommended to control the concentration of potassium in the blood plasma in patients with vomiting and diarrhea, in patients taking potassium-diuretic diuretics, as well as other electrolyte disorders.
Parkinson's disease
Antipsychotics can inhibit the effects of dopamine agonists. Serdolect should be used with caution in patients with Parkinson's disease.
Reduced liver function
With a slight or moderate degree of abnormal liver function, careful monitoring of the patient’s condition is necessary. A slower dosage increase and lower maintenance dose are recommended.
Convulsive seizures
Serodet should be administered with caution in patients with a history of convulsive seizures.
Tardive dyskinesia
Prolonged use of antipsychotic drugs, especially in high doses, is associated with the risk of tardive dyskinesia. If the symptoms of sertindole appear on the background of taking it, then the dosage should be reduced or the drug should be completely discontinued.
Malignant Neuroleptic Syndrome (ZNS)
In cases of the development of ZNS, immediate withdrawal of the drug is necessary.
Cancellation syndrome
With the abrupt cancellation of antipsychotics, nausea, vomiting, increased sweating, and insomnia may occur.It is also possible the return of psychotic symptoms and the appearance of involuntary movement disorders (akathisia, dystonia, dyskinesia). A gradual withdrawal of the drug.
Excipients
The tablets contain lactose monohydrate. Patients with hereditary intolerance to galactose, lactase deficiency or impaired absorption of glucose and galactose should not be prescribed the drug.
Pregnancy and breastfeeding
Since the safety of Serdolect during pregnancy has not been studied in humans, this drug should not be administered to pregnant women.
The safety of Serdolect in breastfeeding women has not been studied. In cases where the use of sertindole recognized as necessary, should stop breastfeeding.
Children's and youthful age (till 18 years)
The safety and effectiveness of Serdolect in children and young men has not been studied, so the drug should not be used in childhood and adolescence.
Influence on ability to drive a car or other mechanisms
Although Serdolect does not have a sedative effect, patients are not recommended against the background of its reception to drive a car or other mechanisms until the individual tolerance of the drug is established.
Overdosage
SymptomsDrowsiness, slurred speech, tachycardia, decrease in blood pressure and transient increase in the QT interval. The development of paroxysms of ventricular tachycardia (like & "torsade de pointes &") is possible, especially in cases of using Sertindole in conjunction with drugs that can cause this type of side effect.
Treatment.In the event of an overdose, the drug should be immediately discontinued, measures should be taken to maintain the airway and adequate oxygenation. Monitoring of ECG and main somatic indicators should be started immediately. In cases of an increase in the QT interval, ECG monitoring is performed before normalization of this indicator, and the half-life of sertindole should be taken into account (from 2 to 4 days).
An intravenous catheter should be installed, gastric lavage, activated carbon and laxatives should be prescribed.
Specific antidote does not exist and the drug can not be bred by dialysis. Therefore, maintenance therapy should be prescribed.
Correction of blood pressure reduction and manifestations of vascular collapse is performed using intravenous administration of solutions. If sympathomimetics are used, adrenaline or dopamine should be used with caution, since the stimulation of β-adrenergic receptors together with the characteristic antagonistic effect of sertindole on α1-adrenoretseptory can lead to a pronounced decrease in blood pressure.
If antiarrhythmic drugs are used, then it should be borne in mind that drugs such as quinidine, disopyramide, procainamide can potentially increase the QT interval. If severe extrapyramidal disorders develop, anticholinergic drugs should be prescribed. The patient must be under constant medical supervision until complete recovery.
- Brand name: Serdolect
- Active ingredient: Sertindol
- Dosage form: Coated pills
- Manufacturer: Lundbeck AS
- Country of Origin: Denmark
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