Sertindole


Concise Prescribing Info
Indications/Uses
Schizophrenia.
Dosage/Direction for Use
Adult : PO For patient intolerant to at least 1 other antipsychotic agent: Initial: 4 mg once daily, increased gradually in increments of 4 mg every 4-5 days. Maintenance: 12-20 mg once daily. Max: 24 mg/day.
Dosage Details
Oral
Schizophrenia
Adult: For patient intolerant to at least 1 other antipsychotic agent: Initially, 4 mg once daily, increased gradually in increments of 4 mg every 4-5 days. Maintenance: 12-20 mg once daily. Max: 24 mg daily. Re-titrate dose if therapy is interrupted for ≥1 wk.
Elderly: Slower dose titration and lower maintenance dose.
Hepatic Impairment
Mild to moderate: Slower dose titration and lower maintenance dose. Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Known uncorrected hypokalaemia or hypomagnesaemia, known or family history of congenital long QT syndrome, known acquired QT interval prolongation [QTc >450 msec (male) and 470 msec (female)]; history of clinically significant CV disease, CHF, cardiac hypertrophy, arrhythmia or bradycardia (<50 beats/min). Severe hepatic impairment. Concomitant use w/ potent CYP3A4 inhibitors or drugs known to significantly prolong or increase QT interval.
Special Precautions
Patient w/ Parkinson's disease, history of seizures, risk factors for stroke, conditions which may contribute to an elevation of core body temp (e.g. exercising strenuously). Patient at risk for aspiration pneumonia and those who are poor CYP2D6 metabolisers. Not intended for the treatment of dementia-related psychosis. Avoid abrupt withdrawal. Mild to moderate hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
QT interval prolongation, tardive dyskinesia, convulsions, hyperglycaemia, seizures, hyperprolactinaemia, peripheral oedema, dyspnoea, rhinitis, sexual dysfunction, dizziness, dry mouth, orthostatic hypotension, wt gain, paraesthesia, insomnia, headache, nasal congestion, constipation.
Potentially Fatal: Torsade de Pointes-type arrhythmia, neuroleptic malignant syndrome.
Patient Counseling Information
May impair ability to drive or operate machinery.
MonitoringParameters
Monitor ECG prior to and periodically during treatment, BP (during titration and early maintenance treatment); baseline serum K and Mg screening.
Overdosage
Symptoms: Hypotension, tachycardia, somnolence, slurred speech, transient prolongation of QTc interval, Torsade de Pointes. Management: Supportive treatment. Establish a patent airway and maintain adequate oxygenation. Establish IV access; may consider admin of activated charcoal w/ laxative. Hypotension and circulatory collapse may be treated w/ IV fluids. Anticholinergic agents may be administered for severe extrapyramidal symptoms.
Drug Interactions
Increased plasma levels w/ potent CYP2D6 inhibitors (e.g. fluoxetine, paroxetine). Decreased plasma concentration w/ CYP inducers (e.g. rifampicin, carbamazepine, phenytoin).
Potentially Fatal: Increases in QT interval may be exacerbated by drugs known to significantly prolong or increase QT interval (e.g. quinidine, thioridazine, erythromycin, lithium). Significantly increased plasma levels w/ potent CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, indinavir, diltiazem).
Action
Description: Sertindole is an atypical antipsychotic. The exact mechanism of action is unknown but it has been proposed that its efficacy is derived from its selective inhibitory effect on mesolimbic dopaminergic neurons through a combination of central dopamine D2, serotonin 5-HT2 and α1-adrenergic receptor antagonism.
Pharmacokinetics:
Absorption: Slowly absorbed. Time to peak plasma concentration: Approx 10 hr.
Distribution: Readily crosses the blood-brain barrier and placenta. Volume of distribution: Approx 20 L/kg. Plasma protein binding: Approx 99.5% (primarily to albumin and α1-acid glycoprotein).
Metabolism: Extensively metabolised in the liver by CYP2D6 and CYP3A4 isoenzymes.
Excretion: Mainly via faeces (as unchanged drug and metabolites); urine (small amount). Terminal half-life: Approx 3 days.
Chemical Structure

Chemical Structure Image
Sertindole

Source: National Center for Biotechnology Information. PubChem Database. Sertindole, CID=60149, https://pubchem.ncbi.nlm.nih.gov/compound/Sertindole (accessed on Jan. 23, 2020)

Storage
Store between 15-30°C. Protect from light and moisture.
MIMS Class
ATC Classification
N05AE03 - sertindole ; Belongs to the class of indole derivatives antipsychotics.
References
Buckingham R (ed). Sertindole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/03/2016.

Serdolect 4 mg Film-Coated Tablets (H. Lundbeck A/S, Denmark). MHRA. https://products.mhra.gov.uk/. Accessed 08/03/2016.

Serdolect Tablets (H. Lundbeck A/S, Denmark). U.S. FDA. http://www.fda.gov/. Accessed 08/03/2016.

Disclaimer: This information is independently developed by MIMS based on Sertindole from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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