Index of drugs

Treatment of schizophrenia. For cardiovascular safety, serticol should only be used in patients who can not tolerate at least one other antipsychotic medication. The preparation should not be used in emergency situations, in order to quickly relieve symptoms in patients with acute disorders.

1 tabl powl. contains 4 mg, 12 mg or 16 mg serticol. The tablets contain lactose.

An antipsychotic drug. The mechanism of action is based on the selective inhibition of dopaminergic neurons of the mesolimbic system and on the balanced inhibition of central dopaminergic D₂, 5-HT serotonergic receptors₂ and α receptors₁adrenergic. Following oral administration, serticol is well absorbed. The maximum concentration in the blood reaches after about 10 h. The drug is bound to plasma proteins in about 99.5%. It penetrates into red blood cells, easily penetrates the blood-brain barrier and the placental barrier. It is eliminated by hepatic metabolism. Medium T_0,5 is about 3 days. Sertndol and its metabolites are excreted very slowly, within 50 days 50-60% of the dose is excreted. About 4% of the dose is excreted in the urine as parent drug and metabolites. Faecal excretion is the main route of excretion of the parent drug and metabolites.

Hypersensitivity to the components of the preparation. Identified decompensated hypokalaemia or diagnosed hypomagnesaemia. Clinically important cardiovascular disease, congestive heart failure, hypertrophic cardiomyopathy, arrhythmias or bradycardia (<50 beats per minute). Congenital long QT syndrome or family history of this syndrome or recognized acquired QT interval prolongation (corrected QT interval (QTc)> 450 milliseconds in men and 470 milliseconds in women). Severe liver dysfunction. Concomitant use of drugs that significantly prolong the QT interval: class I and III antiararials (eg, quinidine, Amiodarone, sotalol, dofetilide), some antipsychotics (e.g. thioridazine), some macrolide antibiotics (eg erythromycin), some antihistamines ( e.g. terfenadine, astemizole), some quinoline antibiotics (e.g., gatofoxacin, moxifloxacin). The above list is not complete and single drugs that cause significant QT interval prolongation (eg cisapride, lithium compounds) are contraindicated. Simultaneous use of drugs with known strong inhibitory effects on cytochrome P450 3A enzymes: anti-fungal azole medicines (eg ketoconazole, itraconazole), some macrolide antibiotics (eg Erythromycin, clarithromycin), HIV protease inhibitors (e.g. indinavir), some Calcium channel blockers (e.g. diltiazem, verapamil). The above list is not complete and single drugs with known strong inhibitory effects on CYP3A enzymes (eg cimetidine) are contraindicated.

Serotonin prolongs the QT interval to a greater extent than other antipsychotics. The mean QT prolongation is greater when dosing at the upper limit of the recommended dose range (20 mg and 24 mg). Therefore, it should only be used in patients who can not tolerate at least one of the other antipsychotics. The prescribing physician should fully comply with the required safety measures: ECG examination should be performed before starting treatment, after reaching steady state after approximately 3 weeks of treatment or after reaching 16 mg, and then after 3 months of treatment, during maintenance treatment every 3 months, during the ECG maintenance period, should be performed before and after each dose escalation, ECG is recommended if you add or increase the dose of concomitant medication that may lead to increased serumindole levels; sertindol is contraindicated when the QTc interval, before starting treatment, is over 450 milliseconds in men or 470 milliseconds in women; when the QTc interval is above 500 milliseconds during treatment, discontinuation of therapy is recommended; if you experience symptoms such as palpitations, seizures or fainting that may indicate that you are having an arrhythmia, the doctor should immediately check the patient, including ECG; ECG testing is best performed in the morning, and QTc should be calculated using the Bazette or Frideric formula. The risk of QT prolongation is increased in patients who simultaneously take drugs that prolong the QT interval or inhibit the metabolism of sertindole.Serum potassium and Magnesium in patients at risk for significant electrolyte disturbances and low serum potassium and magnesium should be measured prior to initiation of serticol therapy. Regular monitoring of serum potassium is recommended in patients who are vomiting, diarrhea, treated with diuretics that cause potassium loss, or in patients with other electrolyte disturbances. Because sertindol blocks α-receptors₁ in the initial dose setting period orthostatic hypotension may occur. Patients treated with antipsychotics have reported cases of venous thromboembolism (VTE). Because the use of acquired risk factors for VTE is often seen in people taking antipsychotics, before and during treatment with sertindole, all possible risk factors for this disease should be identified and preventive measures should be taken. Antipsychotics may inhibit the action of Dopamine agonists. It should be used in combination with some SSRIs ( Fluoxetine, paroxetine) with particular caution and only if the potential benefit outweighs the risks. Sertindole may be required at a lower maintenance dose and ECG monitoring must be monitored before and after the dose is determined. Use with caution in patients with Parkinson's disease, with low CYP2D6 metabolised and in patients with a history of seizures. Due to the risk of hyperglycaemia or worsening of diabetes mellitus, it is recommended to monitor the clinical status of patients with diabetes or who have diabetes development factors. The preparation is not indicated for the treatment of psychoses associated with dementia and / or disorders and for the treatment of elderly patients with dementia. Elderly patients should be cautious with risk factors predisposing to stroke; treatment with sertindol should be started after careful examination of the cardiovascular system. Patients with mild or moderate hepatic impairment should be closely monitored. If signs of tardive dyskinesia appear, a reduction of sertindole dose or discontinuation of treatment should be considered. In the event of symptoms indicating a neuroleptic malignant syndrome, the antipsychotic should be discontinued immediately. Due to the lactose content, the preparation should not be given to patients with rare congenital galactose intolerance, Lapp lactase deficiency or poor absorption of Glucose and galactose. The use of the preparation is not recommended in children under 18 years of age, due to the lack of data on its safety and efficacy in this group of patients.

The safety of the medicine during pregnancy has not been established. The drug should not be used during pregnancy. Exposure to antipsychotics (including serticol) during the third trimester of pregnancy may result in neonatal side effects including extrapyramidal symptoms and / or withdrawal symptoms that may vary in severity and duration after birth. Cases of agitation, hypertonia, tremor, drowsiness, respiratory distress syndrome, and feeding disorders have been reported. Therefore, the condition of newborns should be carefully monitored. It is expected that sertindol is excreted in human milk. If sertindole treatment is considered necessary, discontinuation of breast-feeding should be considered.
Peri- and post-natal studies performed in rats showed a reduction in fertility in the offspring when dosages remained in the therapeutic range used in humans.

Very often: rhinitis or obstruction. Common: weight gain, prolongation of the QT interval, presence of erythrocytes in the urine, presence of leucocytes in the urine, peripheral edema, dizziness, paresthesia, dyspnea, dry mouth, orthostatic hypotension, ejaculation disorders. Not so often:torsade de pointes, fainting, convulsions, movement disorders (especially tardive dyskinesias), hyperglycemia. Rare: a neuroleptic malignant syndrome. Very rare: Venous thromboembolism (including cases of pulmonary embolism and deep vein thrombosis). Not known: withdrawal syndrome in the newborn.If you suddenly stop using antipsychotics, you may experience acute withdrawal symptoms (nausea, vomiting, sweating and insomnia); also recurrences of psychotic symptoms and the appearance of disorders - involuntary movements (akathisia, dystonia, dyskinesia).

Orally. Adults.Dose setting: all patients should start using the 4 mg daily dose. The dose should be increased by 4 mg after 4-5 days of each dose until an optimal daily maintenance dose of 12-20 mg is achieved. The initial dose of 8 mg or a rapid dose escalation is associated with a significantly increased risk of orthostatic hypotension.Maintenance treatment: depending on the patient's response to treatment, the dose may be increased to 20 mg per day. A maximum dose of 24 mg per day can only be used in exceptional cases (studies have not demonstrated a clearly higher dose effectiveness> 20 mg, and QT prolongation may be higher when doses are used at the upper end of the dose range). Dose control should be performed during the dose setting and early maintenance period. In elderly patients, treatment should only be started after a direct cardiovascular examination; in this group of patients, a slower dose setting and lower maintenance dose may be indicated. Patients with hepatic impairment require a slower dose setting and a lower maintenance dose. There is no need to change the dosage in patients with impaired renal function. Hemodialysis does not affect the pharmacokinetics of sertindole. When resuming treatment with sertindole in patients who have not received the drug for less than a week, no further dose adjustment is required and the fixed maintenance dose can be re-applied. In other cases, it is advisable to follow the recommended dose setting scheme. The ECG should be performed before re-dosing. Dosage after prior use of other antipsychotics: sertindol therapy may be started according to the recommended dose setting schedule and at the same time discontinued using other oral antipsychotics. In patients treated with sustained release antipsychotics, the first dose of sertindole should be given instead of the subsequent injection of the drug in the form of depot. In cases where a sedative effect is required, the preparation can be given in combination with benzodiazepine.
The tablets should be taken once a day, regardless of meals.