Acute & maintenance treatment of schizophrenia & related psychoses where positive symptoms (e.g. delusions, hallucinations, disordered thinking, hostility & suspiciousness), acute manic or mixed episodes in bipolar disorder.
Thienodiazepine; Atypical Antipsychotic
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; adrenergic A1; 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.
The recommended starting dose for Deprex is 10 mg/day, administered as a single daily dose without regard to meals.
Drugs that induce CYP1A2 or glucoronyl transferase enzymes (omeprazole, rifampicin), inhibitor of CYP1A2 (fluvoxamine), centrally acting drugs, antihypertensive agents.
Hypersensitivity, narrow-angle glaucoma, prostatic hypertrophy, or paralytic ileus & related conditions. Neuroleptic Malignant Syndrome (NMS): unexplained high fever without additional clinical manifestations of NMS, all antipsychotic medicines, including olanzapine must be discontinued. Olanzapine should be used cautiously in patients whohave a history of seizures or have conditions associated with seizures.
Frequent: somnolence & weight gain. Occasional: dizziness, asthenia, akathisia, increased appetite, peripheral oedema, orthostatic hypotension, & mild, transient anticholinergic Effects including constipation & dry mouth; transient, asymptomatic elevations of hepatic transaminases, ALT, AST.
Because of limited experience in humans, olanzapine should be used in pregnancy only when potential benefit justifies potential risk to the fetus. Maternal doses of olanzapine up to 20 mg daily produce low levels in milk and undetectable levels in the serum of breastfed infants. In most cases, short-term side effects have not been reported, but sedation has occurred. Limited long-term follow-up of infants exposed to olanzapine indicates that infants generally developed normally. A systematic review of second-generation antipsychotics concluded that olanzapine seemed to be the first-line agent during breastfeeding. Monitor the infant for drowsiness and developmental milestones, especially if other antipsychotics are used concurrently.
In premarketing trials involving more than 3100 patients and/or normal subjects, accidental or intentional acute overdosage of olanzapine was identified in 67 patients. In the patient taking the largest identified amount, 300 mg, the only symptoms reported were drowsiness and slurred speech. In the limited number of patients who were evaluated in hospitals, including the patient taking 300 mg, there were no observations indicating an adverse change in laboratory analytes or ECG. Vital signs were usually within normal limits following overdoses. In postmarketing reports of overdose with olanzapine alone, symptoms have been reported in the majority of cases. In symptomatic patients, symptoms with ≥10% incidence included agitation/aggressiveness, dysarthria, tachycardia, various extrapyramidal symptoms, and reduced level of consciousness ranging from sedation to coma. Among less commonly reported symptoms were the following potentially medically serious reactions: aspiration, cardiopulmonary arrest, cardiac arrhythmias (such as supraventricular tachycardia and 1 patient experiencing sinus pause with spontaneous resumption of normal rhythm), delirium, possible neuroleptic malignant syndrome, respiratory depression/arrest, convulsion, hypertension, and hypotension. Eli Lilly and Company has received reports of fatality in association with overdose of olanzapine alone. In 1 case of death, the amount of acutely ingested olanzapine was reported to be possibly as low as 450 mg of oral olanzapine; however, in another case, a patient was reported to survive an acute olanzapine ingestion of approximately 2 g of oral olanzapine.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.