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Olanzapine | Zyprexa among others, is an atypical anti-psychotic primarily used to treat schizophrenia and bipolar disorder.

Therapeutic Class

Atypical neuroleptic drugs

Pharmacology

Olanzapine is an antipsychotic agent and has affinities for serotonin 5HT2A/2C, 5HT3, 5HT6; dopamine D1, D2, D3, D4, D5; cholinergic muscarinic receptors M1-M5; α1 adrenergic; and histamine H1 receptors.

The mechanism of action of Olanzapine, as with other drugs having efficacy in schizophrenia, is unknown. However, it has been proposed that this drug’s efficacy in schizophrenia is mediated through a combination of dopamine and

serotonin type 2 (5HT2) antagonism. Olanzapine is well absorbed after oral administration, reaching peak plasma concentrations within 5 to 8 hours. The absorption is not affected by food. Olanzapine is not mutagenic or clastogenic as well as not carcinogenic.

Dosage & Administration

The recommended starting dose for Olanzapine/Zyprexa is 10 mg/day, administered as a single daily dose without regard to meals. Daily dosage may subsequently be adjusted based on individual clinical status within the range of 5-20 mg daily.

An increase to a dose greater than the routine therapeutic dose of 10 mg/day i.e. to a dose of 15 mg/day or greater, is recommended only after appropriate clinical reassessment.

When more than one factor is present which might result in slower metabolism (female gender, geriatric age, non-smoking status), consideration should be given to decreasing the starting dose. Dose escalation, when indicated, should be conservative in such patients.

Interaction

Drugs that induce CYP1A2 or glucoronyl transferase enzymes (omeprazole, rifampicin), inhibitor of CYP1A2 (fluvoxamine), centrally acting drugs, antihypertensive agents.

Contraindications

Olanzapine/Zyprexa is contraindicated in those patients with a known hypersensitivity to any ingredient of the product as well as in patients with known risk for narrow-angle glaucoma.

Side Effects

Frequent: somnolence and weight gain.

Occasional: dizziness, asthenia, akathisia, increased appetite, peripheral oedema, orthostatic hypotension, and mild, transient anticholinergic effects including constipation and dry mouth; transient, asymptomatic elevations of hepatic transaminases, ALT, AST.

Rare: Photosensitivity reaction and bradycardia.

Pregnancy & Lactation

Olanzapine/Zyprexa should be used in pregnancy only if the potential benefits justify the potential risk to the fetus. So, patients should be advised to notify their physician if they become pregnant or intend to become pregnant during treatment with Olanzapine.

There is no report to show teratogenicity. Patients should not breast feed if they are taking Olanzapine/Zyprexa.

Precautions & Warnings

Before taking olanzapine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver problems, seizures, difficulty swallowing, low white blood cell count, dementia, difficulty urinating (for example, due to enlarged prostate), glaucoma (narrow angle),

stomach/intestinal problems (such as blockage, chronic constipation, paralytic ileus), smoking, personal or family history of diabetes, heart disease, high cholesterol/triglyceride levels, breathing trouble during sleep (sleep apnea).

This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

This medication may make you sweat less, making you more likely to get heat stroke. Avoid doing things that may cause you to overheat, such as hard work or exercise in hot weather, or using hot tubs. When the weather is hot, drink a lot of fluids and dress lightly.

If you overheat, quickly look for a place to cool down and rest. Get medical help right away if you have a fever that does not go away, mental/mood changes, headache, or dizziness.

Use in Special Populations

Children: Olanzapine/Zyprexa has not been studied in subjects under 18 years of age.

Elderly patients (age 65 and over): starting dose 5 mg/day

Patients with hepatic, renal impairment: starting dose 5 mg/day

Storage Conditions

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.