sertindole.txt

CLINICAL USE

Atypical antipsychotic:Schizophrenia

DOSE IN NORMAL RENAL FUNCTION

12–20 mg once daily; maximum 24 mg daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :440.9

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :99.5

%Excreted unchanged in urine &nbsp &nbsp : <1

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :20

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :72

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function. Start at low dose and increase according to response

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anaesthetics: enhanced hypotensive effect

Analgesics: increased risk of convulsions with tramadol; enhanced hypotensive and sedative effects with opioids

Anti-arrhythmics: increased risk of ventricular arrhythmias with anti-arrhythmics that prolong the QT interval; avoid concomitant use with amiodarone, disopyramide and procainamide (risk of ventricular arrhythmias)

Antibacterials: avoid concomitant use with macrolides and moxifloxacin (increased risk of ventricular arrhythmias)

Antidepressants: fluoxetine and paroxetine increase sertindole concentration; increased plasma level of tricyclics

Anti-epileptics: antagonises anticonvulsant effect; metabolism accelerated by carbamazepine and phenytoin

Antifungals: avoid concomitant use with imidazoles and triazoles

Antimalarials: avoid concomitant use with artemether/lumefantrine

Antipsychotics: increased risk of ventricular arrhythmias with amisulpride – avoid concomitant use

Antivirals: concentration increased by amprenavir, indinavir, lopinavir, nelfinavir, ritonavir and saquinavir (increased risk of ventricular arrhythmias) – avoid concomitant useAnxiolytics and hypnotics: increased sedative effects

Beta-blockers: increased risk of ventricular arrhythmias with sotalolDiuretics increased risk of ventricular arrhythmias due to hypokalaemiaIvabradine: increased risk of ventricular arrhythmias

Lithium: increased risk of ventricular arrhythmias

Sibutramine: increased risk of CNS toxicity – avoid concomitant use

Ulcer-healing drugs: increased risk of ventricular arrhythmias with cimetidine

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Available on a named patient basis Can cause peripheral oedema Associated with cardiac arrhythmias, QT interval prolongation, and sudden cardiac deathPatients should have an ECG pre and during treatment
Hypokalaemia and hypomagnesaemia should be corrected before starting therapy.

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