Zyprexa

Zy·prex·a (z-prks)

A trademark for the drug olanzapine.

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olanzapine

Zyprexa, Zyprexa IntraMuscular, Zyprexa Zydis

Pharmacologic class: Thienobenzodiazepine

Therapeutic class: Antipsychotic

Pregnancy risk category C

FDA Boxed Warning

• Elderly patients with dementia-related psychosis are at increased risk for death. Over course of 10-week controlled trial, death rate in drug-treated patients was about 4.5%, compared to about 2.6% in placebo group. Although causes of death varied, most appeared to be cardiovascular or infectious. Don't give drug to patients with dementia-related psychosis.

Action

Unknown. Thought to antagonize dopamine and serotonin type 2 in CNS. Also antagonizes muscarinic receptors in respiratory tract, causing cholinergic activation.

Availability

Solution for injection: 10-mg vials

Tablets: 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg

Tablets (orally disintegrating): 5 mg, 10 mg, 15 mg, 20 mg

⊘Indications and dosages

➣ Schizophrenia

Adults: Initially, 5 to 10 mg P.O. daily; may increase q week by 5 mg/day (not to exceed 20 mg/day)

➣ Psychotic disorders, including acute manic episodes

Adults: Initially, 10 to 15 mg P.O. daily; may increase q 24 hours by 5 mg/day (not to exceed 20 mg/day). Or 10 mg I.M.; maximum dosage is three 10-mg doses given I.M. 2 to 4 hours apart.

➣ Maintenance treatment of bipolar disorder

Adults: 12.5 mg P.O. daily

Dosage adjustment

• Elderly or debilitated patients
• Patients predisposed to hypotensive reactions

Off-label uses

• Borderline personality disorder (with oral use)

Contraindications

• Hypersensitivity to drug

Precautions

Use cautiously in:
• hepatic impairment, cardiovascular or cerebrovascular disease, diabetes mellitus, prostatic hypertrophy, angle-closure glaucoma, phenylketonuria (with orally disintegrating tablets)
• history of seizures, paralytic ileus, or suicide attempt
• elderly patients
• pregnant or breastfeeding patients
• children younger than age 18 (safety not established).

Administration

• Give without regard to meals.
• To remove orally disintegrating tablet from package, peel back foil; don't push tablet through foil.
• Reconstitute for I.M. injection with 2.1 ml of sterile water for injection only, into single-packaged vial.
• After reconstitution, withdraw total contents of vial for 10-mg dose; 1.5 ml for 7.5-mg dose; 1 ml for 5-mg dose, or 0.5 ml for 2.5-mg dose.
• Use solution for I.M. injection within 1 hour of reconstitution.
• Don't combine in syringe with diazepam, lorazepam, or haloperidol.
• Be aware that total daily dosages above 30 mg P.O. or 10 mg I.M. given more often than 2 hours after initial dose and 4 hours after second dose aren't recommended.

Route	Onset	Peak	Duration
P.O.	Unknown	6 hr	Unknown
I.M.	Rapid	15-45 min	Unknown

Adverse reactions

CNS: dizziness, headache, weakness, fatigue, restlessness, sedation, insomnia, mood changes, agitation, personality disorder, impaired speech, tardive dyskinesia, dystonia, tremor, extrapyramidal effects, neuroleptic malignant syndrome, coma

CV: orthostatic hypotension, chest pain, tachycardia

EENT: amblyopia, rhinitis, pharyngitis

GI: nausea, constipation, abdominal pain, increased salivation, dry mouth

GU: urinary incontinence, urinary tract infection

Hematologic: leukopenia

Metabolic: goiter, increased thirst, severe hyperglycemia

Musculoskeletal: hypertonia, joint pain

Respiratory: cough, dyspnea

Skin: ecchymosis, photosensitivity

Other: increased appetite, weight gain or loss, fever, flulike symptoms, impaired body temperature regulation, death

Interactions

Drug-drug. Antihypertensives: additive hypotension

Carbamazepine, omeprazole, rifampin: decreased olanzapine effects

CNS depressants: additive CNS depression

Dopamine agonists, levodopa: antagonism of these drugs' effects

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, glucose, creatinine phosphokinase, gamma-glutamyltransferase: elevated levels

Platelets: decreased count

Drug-behaviors. Alcohol use: additive CNS depression

Smoking: increased drug clearance

Sun exposure: increased risk of photosensitivity

Patient monitoring

• Assess patient's mental status during therapy.
• Monitor vital signs during dosage adjustment periods.
• Make sure patient takes drug and doesn't hoard it.
☞ Watch for signs and symptoms of neuroleptic malignant syndrome (fever, respiratory distress, tachycardia, seizures, diaphoresis, hypertension or hypotension, tiredness, severe muscle stiffness, loss of bladder control).
• Evaluate patient for onset of akathisia, tardive dyskinesia, and extrapyramidal effects.
☞ Watch for signs of increasing depression.
☞ Monitor blood glucose level closely, especially in patient with diabetes mellitus. Severe hyperglycemia, coma, and death may occur.
• Watch for orthostatic hypotension before I.M. injection. Keep patient recumbent if drowsiness or dizziness follows injection.

Patient teaching

• Tell patient he may take without regard to meals.
• Instruct patient to remove orally disintegrating tablet from package by peeling back foil - not by pushing tablet through foil. Instruct him to remove tablet from foil using dry hands, and place entire tablet in mouth. Tell him tablet will disintegrate with or without liquid.
• Tell patient drug may cause extrapyramidal symptoms, akathisia, and tardive dyskinesia leading to involuntary movements, tremors, rigidity, muscle contractions, and restlessness.
☞ Caution patient with diabetes mellitus to monitor blood glucose closely.
• Tell patient to move slowly when sitting up or standing to avoid dizziness. Advise him to dangle legs briefly before getting out of bed.
• Advise patient to avoid smoking, alcohol, or other CNS depressants.
• Tell patient to exercise in moderation and to avoid overly hot baths and showers, because drug impairs body temperature regulation.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

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Zyprexa®

Olanzapine Psychiatry An antipsychotic. See Antipsychotic.