o·lan·za·pine ( -l n z-p n )n. A psychotropic drug used orally and intramuscularly in the treatment of schizophrenia, bipolar disorder, and acute psychosis. |
olanzapine,
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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