Olazin

Each Film Coated Tablet contains: Olanzapine 5 mg or 10 mg.

Pharmacology: Pharmacokinetics: Olanzapine is well absorbed from the gastrointestinal tract after oral doses but undergoes considerably first-pass metabolism. Peak plasma concentrations are achieved about 5 to 8 hours after oral dose and about 15 to 45 minutes after an intramuscular dose. Olanzapine is about 93% bound to plasma proteins. It is extensive metabolised in the liver, primarily by direct glucuronidation and by oxidation mediated through the cytochrome P450 isoenzymes CYP1A2, and a fewer extent, CYP2D6. The 2 major metabolites, 10-N-glucuronide and 4-N-desmethyl olanzapine appears to be inactive. About 57% of a dose is excreted in the urine mainly as metabolites, and about 30% appears in the faeces. The mean plasma elimination half-life has been variously reported to be about 30 to 38 hours half-life tends to be longer in female than in male patients. Olanzapine is distributed into breast milk.

Olanzapine is a thienobenzodiazepine atypical antipsychotic. It is used for the management of schizophrenia and for the treatment of moderate to severe mania associated with bipolar disorder.

The usual initial dose for schizophrenia is 10 mg daily as a single dose by mouth, dosage adjustments may be according to response at intervals of not less than 24 hours to within the range of 5 to 20 mg daily.
For the treatment of acute mixed or manic episodes in bipolar disorder, a recommended initial dose is 10 or 15 mg daily by mouth as monotherapy or 10 mg if given as part of combination therapy; the daily dosage may be adjusted in increments or decrements of 5 mg if necessary, at intervals of not less than 24 hours to a dose of between 5 and 20 mg daily. If a response is achieved, therapy may continue at the same dosage to prevent recurrence. For prevention of recurrence in patients whose manic episodes have been responded previously to olanzapine, the recommended starting dose is 10 mg daily.
The metabolism of olanzapine might be slower in female elderly, or non-smoking patients; if more than one of these factors is present, a lower initial dose (e.g. 5 mg daily if given by mouth) and a more gradual dose escalation should be considered. The intramuscular dose should be reduced by half in the elderly.
Administration in hepatic or renal impairment: A starting dose of 5 mg daily of olanzapine by mouth or by intramuscular injection may be necessary for patients with renal or hepatic impairment; for patients with moderate hepatic insufficiency, the starting dose should only be increased with caution.

The antimuscarinic effects of olanzapine contra-indicate its use in patient with angle-closure glaucoma.

Cautions is recommended when giving olanzapine by mouth to such patients and to those with cerebrovascular disease or conditions predisposing to hypotension. It is recommended that blood pressure is periodically assessed in elderly patients.
Cautions is also advised in those with conditions such as benign prostatic hyperplasia or paralytic ileus.
Olanzapine is not recommended in Parkinson's disease since its use has commonly been associated with an increase in parkinsonian symptoms and hallucinations. It should be used with caution in patients with hepatic impairment, or a history of blood dyscrasias, bone marrow depression, or myeloproliferative disease. Seizures are rare with olanzapine but it should be use with care in those with a history of seizures or with conditions that lower the seizure threshold.
Olanzapine does not affect the performance of skilled tasks such as driving.

Olanzapine do not appear to increase the risk of fetal teratogenicity. The rate of spontaneous abortions in pregnant women exposed to olanzapine was not found to be higher than that of the general population; however this drug increased the risk of hyperglycaemia in pregnant women.
The effect of olanzapine on breast-fed infants is unknown, its use by mothers during breast-feeding, may be of concern since antipsychotic drugs do appear in breast milk and this could conceivably alter CNS function in the infant both in the short and long term.

Adverse effects of olanzapine have been seen with the classical antipsychotic but the incidence and severity of such effects may vary.
Somnolence and weight gain are the most frequent adverse effects of olanzapine. Hyperprolactinemia is also common, but usually asymptomatic. Increased appetite, dizziness, elevated plasma glucose, triglyceride, and liver enzymes values, eosinophilia, edema, orthostatic hypotension and mild transient anti-muscarinic effects such as constipation and dry mouth are also relatively common. More severe abnormalities of glucose homeostasis are uncommon. Severe hyperglycaemia or exacerbation of pre-existing diabetes, sometimes leading to ketoacidosis, coma, or death has occurred. Olanzapine is associated with low incidence of extrapyramidal effects, including tardive dyskinesia, although these effects may be more likely at high doses and in the elderly has been associated.
Tardive dyskinesia increases with long term use. Neuroleptic malignant syndrome has been reported rarely. Olanzapine-associated haemotoxicity have been reported. It was suggested that white blood cell counts should be monitored periodically during olanzapine treatment. Thrombocytopenia associated with olanzapine treatment, hypothermia, clinical hypothyroidism, acute hepatocellular cholestatic jaundice, pancreatitis, priapism, mania in both schizophrenic and bipolar patients, worsening of motor function and stuttering has been reported. There is an increased risk of weight gain, glucose intolerance and diabetes mellitus, hyperlipidaemia.

Antipsychotics

N05AH03 - olanzapine ; Belongs to the class of diazepines, oxazepines and thiazepines antipsychotics

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