olanzapine

CLINICAL USE

Schizophrenia Moderate to severe mania

DOSE IN NORMAL RENAL FUNCTION

Oral: 5–20 mg daily IM: 5–10 mg repeated after 2 hours if required; maximum 3 doses daily for 3 daysMaximum dose of combined routes: 20 mg per day

PHARMACOKINETICS

Molecular weight :312.4

%Protein binding :93

%Excreted unchanged in urine : 7 (57% as metabolites and unchanged drug)

Volume of distribution (L/kg) :

10 to 20 :

half-life – normal/ESRD (hrs) :30–38/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Initial dose 5 mg daily and titrate as necessary

10 to 20 : Initial dose 5 mg daily and titrate as necessary

<10 : Initial dose 5 mg daily and titrate as necessary

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Not dialysed. Dose as in GFR <10 mL/min

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

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

CAV/VVHD :Unknown dialysability. Dose as in GFR 10 to 20 mL/min

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

Antibacterials: concentration possibly increased by ciprofloxacin

Antidepressants: fluvoxamine increases concentration of olanzapine

Anti-epileptics: antagonism (convulsive threshold lowered); carbamazepine increases metabolism of olanzapine; increased risk of neutropenia with valproate

Antimalarials: avoid concomitant use with artemether/lumefantrine

Antivirals: concentration reduced by ritonavirAnxiolytics and hypnotics: increased sedative effects; increased risk of hypotension, bradycardia and respiratory depression with IM olanzapine and parenteral benzodiazepines

Sibutramine: increased risk of CNS toxicity – avoid concomitant use

ADMINISTRATION

Reconstition

2.1 mL water for injection

Route

Oral, IM

Rate of Administration

–

Comments

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