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Olanzapine information from DrugsUpdate  

See Available Brands of Olanzapine in India

P - Caution when used during pregnancy
L - Contraindicated in lactation

Olanzapine (trade names Zyprexa, Zyprexa Zydis, Zalasta, Zolafren, Olzapin, Rexapin or in combination with fluoxetine Symbyax) is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder. The olanzapine formulations are manufactured and marketed by the pharmaceutical company Eli Lilly and Company, whose patent for olanzapine proper expires in 2011

Pharmacodynamics

Pharmacokinetics

Olanzapine is an atypical antipsychotic with affinity for serotonin 5-HT2A/2C, dopamine, muscarinic M1-M5, histamine H1 and adrenergic α1 receptors.

Absorption

Well absorbed from the GI tract (oral); peak plasma concentrations after 5-8 hr (oral) or 15-45 min (IM).

Distribution
Protein-binding: 93%.

Metabolism
Extensively hepatic by direct glucuronidation and oxidation.

Excretion
Urine (as metabolites), faeces; 30-38 hr (elimination half-life).

Olanzapine Indications / Olanzapine Uses

Information Not Available

Olanzapine Adverse Reactions / Olanzapine Side Effects

Postural hypotension; constipation; dizziness; wt gain; agitation; insomnia; akathisia; tremor; personality disorders; oedema; somnolence; increased appetite; antimuscarinic effects; speech difficulty; exacerbation of Parkinson's disease; hallucinations; asthenia; increased body temperature; bradycardia; hyperprolactinaemia; QT prolongation (uncommon); asymptomatic elevations of hepatic transaminases.

Potentially Fatal: Exacerbation of preexisting diabetes sometimes leading to ketoacidosis. Neuroleptic malignant syndrome.

Precautions

Warnings


Increased mortality
Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death compared with those taking placebo. Although the causes of death were varied, most of the deaths appeared to be either CV (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature. Olanzapine is not approved for treatment of dementia-related psychosis.

Monitor
Assess LFTs periodically; monitor blood glucose for hyperglycemia, and assess patient for symptoms of hyperglycemia (eg, polydipsia, polyuria, polyphagia), especially in diabetic patients. In patients receiving treatment for extended time, periodically reevaluate the long-term usefulness of continued therapy. Monitor baseline and follow-up lipid levels. Regularly monitor patient's weight.


Overdosage


Symptoms: Tachycardia, agitation/aggressiveness, dysarthria, extrapyrimidal symptoms, sedation/coma. Induction of emesis is not recommended, gastric lavage and admin of activated charcoal may be effective. Monitor closely and treat symptomatically

Special Precautions

Impaired renal, hepatic, cardiovascular function; prostatic hypertrophy; paralytic ileus; DM; parkinsonism; pregnancy. History of blood dyscrasias, myelosuppression, seizures; dementia; dyslipidaemia. IM: Hypotension, bradyarrhythmia, hypoventilation; monitor BP carefully.

Other Drug Interactions

Olanzapine may antagonise the effects of levodopa and dopamine agonists. Drugs that induce CYP1A2 or glucuronyl transferase enzymes e.g. omeprazole and rifampicin, may increase olanzapine clearance. Inhibitors of CYP1A2 may potentially inhibit olanzapine elimination. Carbamazepine may increase the clearance of olanzapine. Concomitant admin of activated charcoal reduced the oral bioavailability of olanzapine by 50-60%. Caution should be taken when olanzapine is administered with centrally acting drugs and alcohol.

Other Interactions

Information Not Available

Dosage

Oral
Schizophrenia
Adult: Initially, 5-10 mg daily adjusted in steps of 5 mg, according to response. Usual range: 5-20 mg daily. Doses >10 mg should be given only after clinical reassessment. Max: 20 mg daily.
Renal impairment: Initiate at lower dose (5 mg) and increase cautiously.
Hepatic impairment: Initiate at lower dose (5 mg) and increase cautiously.

Oral
Acute mixed or manic episodes in bipolar disorder
Adult: Initially, 10 or 15 mg daily as monotherapy or 10 mg daily when used as part of combination therapy. Adjust dose in steps of 5 mg; usual range: 5-20 mg daily. For prevention of recurrence: Start with 10 mg daily.
Renal impairment: Initiate at lower dose (5 mg) and increase cautiously
Hepatic impairment: Initiate at lower dose (5 mg) and increase cautiously

Intramuscular
Rapid control of agitation and disturbed behaviour in schizophrenia or mania
Adult: Initially, 5-10 mg followed by 5-10 mg as required 2 hr later. Max: 3 inj per 24-hr period; max (including oral olanzapine): 20 mg/day. May give injections for up to 3 days but should transfer to oral therapy as soon as possible.
Hepatic impairment: Dose adjustments may be needed.

Food(before/after)

May be taken with or without food

List of Contraindications

Olanzapine and Pregnancy

Caution when used during pregnancy.


Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Olanzapine and Lactation

Contraindicated in lactatio

Olanzapine and Children

Safety and efficacy not established

Olanzapine and Geriatic

Consider a lower starting dose

Olanzapine and Other Contraindications

Angle-closure glaucoma; lactation. IM: History of CVS disease, heart surgery.

Storage

Intramuscular
Store at 15-30°C.

Oral
Store at 15-30°C.

Lab interference

Intramuscular
Store at 15-30°C.

Oral
Store at 15-30°C.

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