section name header

Pronunciation

oh-LAN-za-peen

Classifications

Therapeutic Classification: antipsychotics, mood stabilizers

Pharmacologic Classification: thienobenzodiazepines

Indications

IM: IM:

BEERS REMS


Unlabeled Use:

Action

  • Antagonizes dopamine and serotonin type 2 in the CNS.
  • Also has anticholinergic, antihistaminic, and anti–alpha1-adrenergic effects.
Therapeutic effects:
  • Decreased manifestations of psychoses.

Pharmacokinetics

Absorption: Well absorbed but rapidly metabolized by first-pass effect, resulting in 60% bioavailability. Conventional tablets and orally disintegrating tablets (Zydis) are bioequivalent. IM administration results in significantly higher blood levels (5 times that of oral).

Distribution: Extensively distributed.

Protein Binding: 93%.

Metabolism/Excretion: Primarily metabolized by the liver by the CYP1A2 isoenzyme; 7% excreted unchanged in urine.

Half-Life: 21–54 hr.

Time/Action Profile

(antipsychotic effects)

ROUTEONSETPEAK*DURATION
POunknown6 hrunknown
IMrapid15–45 min2–4 hr



*Blood levels.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: orthostatic hypotension, bradycardia, chest pain, syncope, tachycardia

Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), photosensitivity

EENT: amblyopia, rhinitis, salivation, pharyngitis

Endo: galactorrhea, goiter, gynecomastia, hyperglycemia, hyperprolactinemia

F and E: thirst

GI: liver enzymes, constipation, dry mouth, weight loss, abdominal pain, dysphagia, nausea

GU: fertility (females), libido, amenorrhea, impotence, urinary incontinence

Hemat: AGRANULOCYTOSIS, leukopenia, neutropenia

Metab: weight gain, appetite, dyslipidemia

MS: hypertonia, joint pain

Neuro: agitation, delirium, dizziness, headache, restlessness, sedation, tremor, weakness, dystonia, falls, insomnia, mood changes, NEUROLEPTIC MALIGNANT SYNDROME, personality disorder, SEIZURES, speech impairment, SUICIDAL THOUGHTS, tardive dyskinesia

Resp: aspiration, cough, dyspnea

Misc: body temperature dysregulation, fever, flu-like syndrome

Interactions

Drug-drug:

Route/Dosage

Schizophrenia

Acute Manic or Mixed Episodes Associated With Bipolar I Disorder

Maintenance Treatment of Bipolar I Disorder

Acute Agitation due to Schizophrenia or Bipolar I Mania

Depressive Episodes Associated With Bipolar I Disorder

Treatment-Resistant Depression

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

ZyPREXA, ZyPREXA Relprevv, ZyPREXA Zydis

Pill Image

olanzapine_195-8488.jpg

Code

NDC Code