No

Antipsychotic Agent, Thienobenzodiaepine

Treatment of the manifestations of psychotic disorders; short-term treatment of acute manic episodes associated with bipolar I disorder

C

Hypersensitivity to olanzapine or any component

Moderate to highly sedating, use with caution in disorders where CNS depression is a feature. Use with caution in Parkinson's disease. Caution in patients with hemodynamic instability; bone marrow suppression; predisposition to seizures; subcortical brain damage; severe cardiac, hepatic, renal, or respiratory disease. Esophageal dysmotility and aspiration have been associated with antipsychotic use - use with caution in patients at risk of pneumonia (ie, Alzheimer's disease). Caution in breast cancer or other prolactin-dependent tumors (may elevate prolactin levels). May alter temperature regulation or mask toxicity of other drugs due to antiemetic effects. Life-threatening arrhythmias have occurred with therapeutic doses of some neuroleptics. Significant weight gain may occur.

May cause extrapyramidal reactions, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions is very low relative to other neuroleptics). May be associated with neuroleptic malignant syndrome (NMS).

>10%: Central nervous system: Headache, somnolence, insomnia, agitation, nervousness, hostility, dizziness

1% to 10%:

Cardiovascular: Postural hypotension, tachycardia, hypotension, peripheral edema

Central nervous system: Dystonic reactions, parkinsonian events, amnesia, euphoria, stuttering, akathisia, anxiety, personality changes, fever

Dermatologic: Rash

Gastrointestinal: Xerostomia, constipation, abdominal pain, weight gain, increased appetite

Genitourinary: Premenstrual syndrome

Neuromuscular & skeletal: Arthralgia, neck rigidity, twitching, hypertonia, tremor

Ocular: Amblyopia

Respiratory: Rhinitis, cough, pharyngitis

<1%: Tardive dyskinesia, neuroleptic malignant syndrome, seizures, priapism

CYP1A2 enzyme substrate, CYP2C19 enzyme substrate (minor), and CYP2D6 enzyme substrate (minor)

Effects may be potentiated with CYP1A₂ inhibitors such as fluvoxamine

Increased sedation with alcohol or other CNS depressants, increased risk of hypotension and orthostatic hypotension with antihypertensives

Olanzapine may antagonize the effects of levodopa and dopamine agonists

Activated charcoal decreased the C_max and AUC of olanzapine by 60%

Store at room temperature (20°C to 25°C); protect from light

Olanzapine is a thienobenzodiazepine neuroleptic; thought to work by antagonizing dopamine and serotonin activities. It is a selective monoaminergic antagonist with high affinity binding to serotonin 5HT2 _A and 5HT2_C, dopamine D_1-4, muscarinic M_1-5, histamine H₁ and alpha₁-adrenergic receptor sites. Olanzapine binds weakly to GABA-A, BZD, and beta-adrenergic receptors.

Onset of effect: greater than or equal to 1 week

Absorption: Oral: Readily absorbed

Protein binding: 93%

Metabolism: Extensive in the liver

Half-life: 21-54 hours

Elimination: 40% removed via first-pass metabolism, 57% eliminated renally, and 30% in feces

Adults >18 years: Oral: Usual starting dose: 5-10 mg once daily; increase to 10 mg once daily within 5-7 days, thereafter adjust by 5 mg/day at 1-week intervals, up to a maximum of 20 mg/day; doses of 30-50 mg/day have been used

Orally-disintegrating tablets: Remove from foil blister by peeling back (do not push tablet through the foil); place tablet in mouth immediately upon removal; tablet dissolves rapidly in saliva and may be swallowed with or without liquid

No information available to require special precautions

No effects or complications reported

Use exactly as directed (do not increase dose or frequency); may cause physical and/or psychological dependence. It may take 2-3 weeks to achieve desired results; do not discontinue without consulting prescriber. Avoid excess alcohol or caffeine and other prescription or OTC medications not approved by prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience excess drowsiness, restlessness, dizziness, or blurred vision (use caution driving or when engaging in tasks requiring alertness until response to drug is known); or constipation (increased exercise, fluids, or dietary fruit and fiber may help). Report persistent CNS effects (eg, trembling fingers, altered gait or balance, excessive sedation, seizures, unusual movements, anxiety, abnormal thoughts, confusion, personality changes); unresolved constipation or gastrointestinal effects; vision changes; difficulty breathing; unusual cough or flu-like symptoms; or worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Tablet: 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg

Tablet, orally-disintegrating: 5 mg, 10 mg, 15 mg, 20 mg

Goldberg RJ, "Managing Psychosis-Related Behavioral Problems in the Elderly," Consult Pharm, 1997, 12(Suppl C):4-10.

Littrell K, Peabody CD, and Littrell SH, "Olanzapine: A New Atypical Antipsychotic," J Psychosoc Nurs Ment Health Serv, 1996, 34(8):41-6.

"Olanzapine for Schizophrenia," Med Lett Drugs Ther, 1997, 39(992):5-6.

Tollefson GD, Beasley CM Jr, Tran PV, et al, "Olanzapine Versus Haloperidol in the Treatment of Schizophrenia and Schizoaffective and Schizophreniform Disorders: Results of an International Collaborative Trial," Am J Psychiatry, 1997, 154(4):457-65.