OLANZA - 10
Tablets

Antidepressants

  • Chemical Composition

    Olanzapine 10mg

  • Packing

    30Coated Tablets

  • Medical Id

    T51

  • License Number

    350/2006

  • License date

    15/10/2006

Mechanism Of Action Olanzapine is a selective monoaminergicantagonist with high affinity binding to the following receptors: serotonin 5HT2, dopamine D1-4, muscarinic M1-5, histamine H1, and adrenergic α1 receptors. Olanzapine binds weakly to GABAA, BZD, and β adrenergic 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 serotonintype 2 (5HT2) antagonism.Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of olanzapine. Olanzapine’s antagonism of muscarinic M1-5 receptors may explain its anticholinergic effects. Olanzapine’s antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Olanzapine’s antagonism of adrenergic α1 receptors may explain the orthostatichypotension observed with this drug.
INDICATIONS • Schizophrenia OLANZA is indicated for the treatment of schizophrenia. • Bipolar Disorder Acute Monotherapy:OLANZA is indicated for the treatment of acutemixed or manic episodes associated with Bipolar I Disorder. Maintenance Monotherapy :The benefit of maintaining bipolar patients on monotherapy with OLANZA after achieving a responder status for an averageduration of two weeks was demonstrated in a controlled trial. The physician who elects to use OLANZA for extended periods should periodically re-evaluate the long-term usefulness of the drug for the individual patient. Combination Therapy: The combination of OLANZA with lithium or valproate is indicated for the short-term treatment of acute manic episodes associated with Bipolar I Disorder.
CONTRAINDICATIONS OLANZA is contraindicated in patients with a known hypersensitivity to the product
Side EFFECTS Although side effects from olanzapine are not common, they can occur. The most common adverse effects associated with OLANZA include headache, agitation, dizziness, drowsiness, constipation, dry mouth, weight gain, upset stomach, vomiting, and diarrhea. The more serious side effects include seizures, uncontrollable jerking movements, fever, extrapyramidal symptoms, very stiff muscles, excess sweating, and fast or irregular heartbeat.
WARNINGS Patients with an established diagnosis of diabetes mellitus, who are started on atypical antipsychotics, including olanzapine, should be monitored regularly for worsening of glucose control. Olanzapine is not approved for the treatment of patients with dementia-related psychosis. A potentially fatalsymptomcomplex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with administration of antipsychotic drugs, including olanzapine. Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, altered mentalstatus and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis and cardiac dysrhythmia). Additional signs may include elevated creatinine phosphokinase, myoglobinuria (rhabdomyolysis), and acuterenal failure. The management of NMS should include: 1-immediate discontinuation of antipsychotic drugs and other drugs not essential to concurrent therapy. 2-intensivesymptomatictreatment and medical monitoring. 3- treatment of any concomitant serious medical problems for which specific treatments are available. 4- Orthostatic hypotension may occur, particularly in elderly, the blood pressure in such patients should be monitored regularly. If signs and symptoms of tardivedyskinesia appear in a patient on olanzapine, drug discontinuation should be considered. However, some patients may require treatment with olanzapine despite the presence of the syndrome. Olanzapine should be used with particular caution in patients with known cardiovasculardisease, cerebrovascular disease, and conditions which would predispose patients to hypotension (dehydration, hypovolemia, and treatment with antihypertensive medications). Olanzapine should be used cautiously in patients with a history of seizures or with conditions that potentially lower the seizure threshold, e.g., Alzheimer’s dementia. Conditions that lower the seizurethreshold may be more prevalent in a population of 65years or older. Caution should be exercised in patients with signs and symptoms of hepatic impairment, in patients with pre-existing conditions associated with limited hepaticfunctional reserve, and in patients who are being treated with potentially hepatotoxic drugs. Periodic assessment of transaminases is recommended in patients with significanthepaticdisease. Since olanzapine has the potential to impair judgment, thinking, or motor skills, patients should be cautioned about operating hazardous machinery, including automobiles, until they are reasonably certain that olanzapine therapy does not affect them adversely. Appropriate care is advised when prescribing olanzapine for patients who will be experiencing conditions which may contribute to an elevation in corebodytemperature, e.g., exercising strenuously, exposure to extreme heat, receiving concomitantmedication with anticholinergic activity, or being subject to dehydration. Olanzapine and other antipsychotic drugs should be used cautiously in patients at risk for aspiration pneumonia. The possibility of a suicide attempt is inherent in schizophrenia and in bipolar disorder, and close supervision of high-risk patients should accompany drug therapy. Olanzapine should be used with caution in patients with clinically significantprostatic hypertrophy, narrow angle glaucoma, or a history of paralytic ileus. Because of the risk of orthostatichypotension with olanzapine, caution should be observed in cardiac patients.
DRUG INTERACTIONS Given the primary CNS effects of olanzapine, caution should be used when olanzapine is taken in combination with other centrally acting drugs and alcohol. Because of its potential for inducing hypotension, olanzapine may enhance the effects of certain antihypertensive agents. Olanzapine may antagonize the effects of levodopa and dopamine agonists. Agents that induce CYP1A2 or glucuronyltransferase enzymes, such as carbamazepine, omeprazole, and rifampin, may cause an increase in olanzapine clearance. Inhibitors of CYP1A2, such as Fluvoxamine, could potentially inhibit olanzapine clearance. Although olanzapine is metabolized by multipleenzyme systems, induction or inhibition of a single enzyme may appreciably alter olanzapine clearance. Therefore, a dosage increase (for induction) or a dosage decrease (for inhibition) may need to be considered with specific drugs. The co-administration of either diazepam or ethanol with olanzapine may potentiate the orthostatic hypotension observed with olanzapine. Drug \ Clinical Laboratory Test Interactions: Olanzapine therapy may be associated with asymptomatic increases in SGPT, SGOT, and GGT. Olanzapine administration is also associated with increases in serum prolactin, with an asymptomatic elevation of the eosinophilcount, and with an increase in CPK.
Pregnancy And lactations OLANZA should be given during pregnancy only if the potential benefit justifies the potentialrisk to the fetus. OLANZA should not be used during breast-feeding.
Dosage And Administration • Schizophrenia Usual Dose :Olanzapine should be administered on a once-a-day schedule without regard to meals, generally beginning with 5-10 mg initially, with a targetdose of 10 mg/day within several days. An increase to a dose greater than the targetdose of 10 mg/day (i.e., to a dose of 15 mg/day or greater) should generally occur gradually, and it is recommended only after clinical assessment. Dosing in Special Populations : The recommended starting dose is 5 mg in patients who are debilitated, who have a predisposition to hypotensive reactions, who otherwise exhibit a combination of factors that may result in slower metabolism of olanzapine (e.g., nonsmoking female patients 65 years of age), or who may be more pharmacodynamicallysensitive to olanzapine. When indicated, dose escalation should be performed with caution in these patients. Maintenance Treatment :While there is no body of evidence available to answer the question of how long the patient treated with olanzapine should remain on it, the effectiveness of oral olanzapine, 10 mg/day to 20 mg/day, in maintaining treatmentresponse in schizophrenic patients who had been stable on OLANZA for approximately 8 weeks and were then followed for a period of up to 8 months has been demonstrated in a placebo-controlled trial. Patients should be periodically reassessed to determine the need for maintenance treatment with appropriate dose. • Bipolar Disorder Usual Monotherapy Dose:Olanzapine should be administered on a once-a-day schedule without regard to meals, generally beginning with 10 or 15 mg. Dosage adjustments, if indicated, should generally occur at intervals of not less than 24 hours, reflecting the procedures in the placebo-controlled trials. When dosage adjustments are necessary, dose increments/decrements of 5mg QD are recommended. Short-term (3-4 weeks) antimanicefficacy was demonstrated in a doserange of 5 mg to 20 mg/day in clinical trials. The safety of doses above 20mg/day has not been evaluated in clinical trials. Dosing in Special Populations — The recommended starting dose is 5 mg in patients who are debilitated, who have a predisposition to hypotensive reactions, who otherwise exhibit a combination of factors that may result in slower metabolism of olanzapine (e.g., nonsmoking female patients 65 years of age), or who may be more pharmacodynamicallysensitive to olanzapine. When indicated, dose escalation should be performed with caution in these patients. Maintenance Monotherapy:The benefit of maintaining bipolar patients on monotherapy with OLANZA at a dose of 5 to 20 mg/day, after achieving a responder status for an averageduration of two weeks, was demonstrated in a controlled trial. The physician who elects to use OLANZA for extended periods should periodically re-evaluate the long-term usefulness of the drug for the individual patient. Bipolar Mania Usual Dose in Combination with Lithium or Valproate:When administered in combination with lithium or valproate, olanzapine dosing should generally begin with 10mg once-a-day without regard to meals. Short-term (6 weeks) antimanicefficacy was demonstrated in a doserange of 5 mg to 20 mg/day in clinical trials. The safety of doses above 20mg/day has not been evaluated in clinical trials.
OVERDOSE The reported symptoms of overdosage (more than 300 mg) are drowsiness, slurred speech, agitation, aggressiveness, dysarthria, tachycardia, various extrapyramidal symptoms, and reduced level of consciousness ranging from sedation to coma. Among less commonly reported symptoms are the following potentially medically serious events: aspiration, cardiopulmonary arrest, cardiac arrhythmias, delirium, respiratory depression/arrest, convulsion, hypertension, hypotension, and possible neurolepticmalignant syndrome. Overdosage Management The possibility of multipledrug involvement should be considered. Incase of acuteoverdosage, establish and maintain an airway and ensure adequate oxygenation and ventilation, which may include intubation. Gastric lavage and administration of activated charcoal together with a laxative should be considered. Cardiovascular monitoring should commence immediately and should include continuous electrocardiographic monitoring to detect possible arrhythmias. There is no specificantidote to olanzapine. Therefore, appropriate supportive measures should be initiated. Hypotension and circulatory collapse should be treated with appropriate measures such as intravenous fluids and/or sympathomimetic agents. (Do not use epinephrine, dopamine, or other sympathomimetics with beta-agonist activity, since betastimulation may worsen hypotension in the setting of olanzapine-induced alpha blockade.) Close medical supervision and monitoring should continue until the patient recovers.
Storage Conditions Store below 30 C Keep out of reach of children Prescription only medicine