sertraline.txt

CLINICAL USE

SSRI:Antidepressant Post-traumatic stress disorder Obsessive compulsive disorder

DOSE IN NORMAL RENAL FUNCTION

25–200 mg daily depending on indication

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :342.7 (as hydrochloride)

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>98

%Excreted unchanged in urine &nbsp &nbsp : 0

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :25

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :26/Probably unchanged

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

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in normal renal function

HDF/high flux &nbsp :Unknown dialysability. Dose as in normal renal function

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

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Analgesics: increased risk of bleeding with aspirin and NSAIDs; risk of CNS toxicity increased with tramadol

Anticoagulants: effect of coumarins possibly enhanced

Antidepressants: increased risk of toxic CNS effects of MAOIs and moclobemide; sertraline and MAOIs should not be prescribed within a 2 week period of each other; avoid concomitant use with St John’s wort; possibly enhanced serotonergic effects with duloxetine; can increase tricyclics antidepressant concentration; increased agitation and nausea with tryptophan

Anti-epileptics: antagonism (lowered convulsive threshold)

Antimalarials: avoid concomitant use with artemether/lumefantrine

Antipsychotics: concentration of clozapine and pimozide increased – avoid concomitant use with pimozide

Antivirals: concentration reduced by efavirenz and darunavir; possibly increased concentration with ritonavir

Ciclosporin: may increase serotonin syndrome

Dopaminergics: increased risk of hypertension and CNS excitation with selegiline – avoid concomitant use; increased risk of CNS toxicity with rasagiline – avoid concomitant use

Dopaminergics: hypertension and CNS excitation5HT 1 agonist: increased risk of CNS toxicity with sumatriptan – avoid concomitant use; possibly increased risk of serotonergic effects with frovatriptanLinezolid: use with caution

Lithium: increased risk of CNS effects; lithium toxicity reported

Sibutramine: increased risk of CNS toxicity – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Sertraline is extensively metabolised by the liver. It can be used in renal failure at normal doses with caution.

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