Olanzapine

Olanzapine may be found in some form under the following brand names:

• Symbyax

• Zyprexa

• Zyprexa Relprevv

• Zyprexa Zydis

Olanzapine is part of the drug class:

• Diazepines, oxazepines, thiazepines and oxepines

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• diazepam (Valium)
• alcohol
• carbamazepine (Tegretol)
• fluvoxamine (Luvox)
• fluoxetine (Prozac, Symbax)
• levodopa
• lorazepam
• antidepressants
• antihistamines
• medicines for anxiety
• medicines for high blood pressure

This is not a complete list of olanzapine drug interactions. Ask your doctor or pharmacist for more information.

Before starting olanzapine, tell your doctor if you have or had:

• heart problems
• seizures
• diabetes or high blood sugar levels (hyperglycemia)
• high cholesterol or triglyceride levels in your blood
• liver problems
• low or high blood pressure
• strokes or “mini-strokes” also called transient ischemic attacks (TIAs)
• Alzheimer's disease
• narrow-angle glaucoma
• enlarged prostate in men
• bowel obstruction
• phenylketonuria, because the dissolvable tablet form of olanzapine contains phenylalanine
• breast cancer
• thoughts of suicide or hurting yourself
• any other medical condition

Tell your doctor if you are pregnant or breastfeeding

Tell your doctor if you exercise a lot or are in hot places often.

The symptoms of bipolar I disorder, treatment resistant depression, or schizophrenia may include thoughts of suicide or of hurting yourself or others. If you have these thoughts at any time, tell your doctor or go to an emergency room right away.

Tell your doctor about all the medicines that you take, including prescription and nonprescription medicines, vitamins, and herbal supplements. Olanzapine and some medicines may interact with each other and may not work as well, or cause possible serious side effects. Your doctor can tell you if it is safe to take olanzapine with your other medicines. Do not start or stop any medicine while taking olanzapine without talking to your doctor first.

Tell your doctor if you are breastfeeding or plan to breastfeed. Olanzapine may be excreted in human breast milk. It may harm your nursing baby.

If you take too much olanzapine, call your local Poison Control Center or seek emergency medical attention right away.

• Store olanzapine at room temperature, between 68°F to 77°F (20°C to 25°C).
• Keep olanzapine away from light.
• Keep olanzapine dry and away from moisture.
• Protect olanzapine for Injection from light, do not freeze.

Keep olanzapine and all medicines out of the reach of children.

In the U.S.

• ZyPREXA
• ZyPREXA Zydis

Available Dosage Forms:

• Tablet
• Tablet, Disintegrating

Therapeutic Class: Antipsychotic

Chemical Class: Thienobenzodiazepine

Olanzapine is a second generation thienobenzodiazepine antipsychotic which displays potent antagonism of serotonin 5-HT2A and 5-HT2C, dopamine D1-4, histamine H1, and alpha1-adrenergic receptors. Olanzapine shows moderate antagonism of 5-HT3 and muscarinic M1-5 receptors, and weak binding to GABA-A, BZD, and beta-adrenergic receptors. Although the precise mechanism of action in schizophrenia and bipolar disorder is not known, the efficacy of olanzapine is thought to be mediated through combined antagonism of dopamine and serotonin type 2 receptor sites.

Absorption

Oral: Well absorbed; not affected by food; tablets and orally disintegrating tablets are bioequivalent

Short-acting injection: Rapidly absorbed

Distribution

Vd: Extensive, 1000 L

Metabolism

Highly metabolized via direct glucuronidation and cytochrome P450 mediated oxidation (CYP1A2, CYP2D6); 40% removed via first pass metabolism

Excretion

Urine (57%, 7% as unchanged drug); feces (30%)

Clearance: Oral:

Children (10 to 18 years; n=8): Apparent: 9.6 ± 2.4 L/hour (Grothe 2000)

Adults: Apparent: 25 L/hour [12 to 47 L/hour (5th to 95th percentile)]; 40% increase in olanzapine clearance in smokers; 30% decrease in females

Within 1 to 2 weeks for control of aggression, agitation, insomnia; 3 to 6 weeks for control of mania and positive psychotic symptoms. Adequate trial: Typically 6 weeks at maximum tolerated doses

Time to Peak

Maximum plasma concentrations after IM administration are 5 times higher than maximum plasma concentrations produced by an oral dose.

Extended-release injection: ~7 days

Short-acting injection: 15 to 45 minutes

Oral: Children (10 to 18 years; n=8): 4.7 ± 3.7 hours (Grothe 2000); Adults: ~6 hours

Half-Life Elimination

Oral and IM (short-acting): Children: (10 to 18 years; n=8): 37.2 ± 5.1 hours (Grothe 2000); Adults: 30 hours [21 to 54 hours (5th to 95th percentile)]; approximately 1.5 times greater in elderly

Extended-release injection: ~30 days

Protein Binding

Plasma: 93%, bound to albumin and alpha1-glycoprotein

There are no contraindications listed in the manufacturer’s labeling.

Canadian labeling: Hypersensitivity to olanzapine or any component of the formulation

Commonly reported side effects of olanzapine include: asthenia, dizziness, drowsiness, extrapyramidal reaction, hyperkinesia, akinesia, cogwheel rigidity, drug-induced parkinson's disease, dyspepsia, mask-like face, and xerostomia. Other side effects include: abnormal gait, back pain, constipation, fever, orthostatic hypotension, weight gain, myoclonus, and personality disorder. See below for a comprehensive list of adverse effects.

Olanzapine is an atypical antipsychotic (atypical means it is less likely than older antipsychotics to cause side effects, and more likely to be effective in the treatment of symptoms such as motivation and social withdrawal). Experts aren't exactly sure how olanzapine works but suggest it has effects on neurotransmitters such as dopamine and serotonin in the brain.

Substance Name

Olanzapine

CAS Registry Number

132539-06-1

Drug Class

Antipsychotic Agents