Olanzapine: Advanced Atypical Antipsychotic for Symptom Control
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Synonyms | |||
Olanzapine is a second-generation (atypical) antipsychotic medication indicated for the treatment of schizophrenia and bipolar I disorder. It functions as a multi-receptor targeting agent, demonstrating high affinity for serotonin, dopamine, muscarinic, histamine, and adrenergic receptors. Its pharmacodynamic profile underpins its efficacy in managing both positive and negative symptoms of psychotic disorders, as well as acute manic or mixed episodes. This agent is available in oral (standard and orally disintegrating tablets) and intramuscular formulations, providing flexibility in clinical administration across various treatment settings and patient needs.
Features
- Active pharmaceutical ingredient: Olanzapine
- Pharmacologic class: Thienobenzodiazepine derivative; Atypical antipsychotic
- Mechanism of Action: Antagonist activity at serotonin 5-HT2A/2C, dopamine D1-4, muscarinic M1-5, histamine H1, and adrenergic α1 receptors
- Available formulations: Oral tablets (2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg), Orally disintegrating tablets (Zydis), Short-acting intramuscular injection
- Bioavailability: Approximately 60%, not significantly affected by food
- Peak plasma concentration (Tmax): 6 hours for oral administration
- Protein binding: 93% primarily to albumin and α1-acid glycoprotein
- Metabolism: Extensive first-pass metabolism primarily via direct glucuronidation and cytochrome P450-mediated oxidation (primarily CYP1A2)
- Elimination half-life: 21-54 hours (mean 30 hours)
- Excretion: Approximately 57% in urine, 30% in feces
Benefits
- Provides effective control of both positive (e.g., hallucinations, delusions) and negative (e.g., social withdrawal, apathy) symptoms associated with schizophrenia.
- Demonstrates rapid efficacy in the acute treatment of manic or mixed episodes associated with bipolar I disorder, either as monotherapy or in combination with mood stabilizers.
- Offers a favorable neurological side effect profile compared to first-generation antipsychotics, with a lower propensity for causing extrapyramidal symptoms (EPS) and tardive dyskinesia.
- Available in multiple formulations, including a rapidly disintegrating oral tablet for enhanced patient compliance and a short-acting intramuscular injection for rapid tranquilization in agitated patients.
- May improve overall patient functioning and quality of life by reducing the severity of psychotic and mood symptoms.
- Can be used as part of a maintenance treatment regimen to prolong time to relapse in stabilized patients.
Common use
Olanzapine is FDA-approved for the treatment of schizophrenia and the acute treatment of manic or mixed episodes associated with bipolar I disorder. It is also approved for maintenance monotherapy of bipolar I disorder. Furthermore, it is used in combination with fluoxetine (as Symbyax) for the treatment of treatment-resistant depression and depressive episodes associated with bipolar I disorder. Off-label uses may include the treatment of behavioral and psychological symptoms of dementia (BPSD)—though with a significant warning for increased mortality in elderly patients with dementia-related psychosis—as well as adjunctive treatment in certain anxiety disorders, and for the prevention of chemotherapy-induced nausea and vomiting (CINV).
Dosage and direction
Schizophrenia:
- Initial dose: 5-10 mg orally once daily.
- Target dose: 10 mg/day within several days of initiation.
- Dosage range: 5-20 mg/day. Dose adjustments should generally occur at intervals of not less than 1 week.
Bipolar I Mania (Monotherapy):
- Initial dose: 10-15 mg orally once daily.
- Dosage range: 5-20 mg/day.
Bipolar I Mania (Adjunctive to Lithium or Valproate):
- Initial dose: 10 mg orally once daily.
- Dosage range: 5-20 mg/day.
Dosing in Special Populations:
- Non-smoking females: Likely have a lower clearance of olanzapine. A lower starting dose (5 mg) should be considered.
- Renal impairment (dialysis): No dosage adjustment is recommended. The recommended starting dose is 5 mg.
- Hepatic impairment: A lower starting dose (5 mg) is recommended. Dose escalation should be performed with caution.
- Elderly: A lower starting dose (5 mg) is recommended for debilitated patients, those predisposed to hypotensive reactions, or patients with pharmacogenomic factors suggesting reduced metabolism.
- Administration: Can be taken with or without food. Orally disintegrating tablets (Zydis) should be placed in the mouth immediately after opening the blister; the tablet disintegrates rapidly with saliva and may be swallowed with or without liquid.
Precautions
- Elderly Patients with Dementia-Related Psychosis: Olanzapine is not approved for this use. Patients treated with atypical antipsychotic drugs are at an increased risk of death, primarily from cardiovascular or infectious events.
- Metabolic Changes: Atypical antipsychotics, including olanzapine, have been associated with metabolic adverse effects, including hyperglycemia, dyslipidemia, and weight gain. Baseline and periodic monitoring of fasting blood glucose, HbA1c, and lipid profiles is mandatory.
- Neuroleptic Malignant Syndrome (NMS): A potentially fatal symptom complex characterized by hyperpyrexia, muscle rigidity, altered mental status, autonomic instability, and elevated CPK has been reported with antipsychotic drugs. Immediate discontinuation and intensive symptomatic treatment are required.
- Tardive Dyskinesia (TD): Although the risk is believed to be lower than with first-generation antipsychotics, olanzapine may cause TD, a syndrome of potentially irreversible, involuntary, dyskinetic movements. The risk appears to be greatest in the elderly, especially elderly women.
- Orthostatic Hypotension: Can occur, especially during initial dose titration. Use with caution in patients with known cardiovascular or cerebrovascular disease.
- Leukopenia/Neutropenia/Agranulocytosis: Has been reported temporally related to antipsychotic agents. Patients with a pre-existing low WBC or a history of drug-induced leukopenia/neutropenia should be monitored frequently during the first few months of therapy.
- Seizures: Should be used cautiously in patients with a history of seizures or with conditions that lower the seizure threshold.
- Dysphagia: Esophageal dysmotility and aspiration have been associated with antipsychotic drug use. Use with caution in patients at risk for aspiration pneumonia.
- Hyperprolactinemia: As with other drugs that antagonize dopamine D2 receptors, olanzapine can elevate prolactin levels.
Contraindications
Olanzapine is contraindicated in patients with a known hypersensitivity to the drug or any components of the formulation. Reactions have included anaphylaxis, angioedema, pruritus, and/or urticaria.
Possible side effect
Very common (>10%) and common (1-10%) adverse reactions include:
- Metabolic: Weight gain, increased appetite, hyperglycemia, dyslipidemia.
- Nervous System: Somnolence, sedation, dizziness, akathisia, parkinsonism.
- Gastrointestinal: Constipation, dry mouth, dyspepsia.
- Cardiovascular: Orthostatic hypotension, tachycardia.
- Hepatic: Transient, asymptomatic elevations of hepatic transaminases.
- Musculoskeletal: Arthralgia, back pain, extremity pain.
- Other: Fatigue, asthenia, blurred vision, prolactin elevation.
Less common but serious side effects include Neuroleptic Malignant Syndrome (NMS), tardive dyskinesia, leukopenia/neutropenia/agranulocytosis, seizures, and QT prolongation.
Drug interaction
- CNS Depressants (e.g., alcohol, benzodiazepines, opioids): Concomitant use can potentiate sedation and orthostatic hypotension.
- CYP1A2 Inhibitors (e.g., fluvoxamine, ciprofloxacin): May significantly increase olanzapine plasma concentrations. A dose reduction of olanzapine should be considered.
- CYP1A2 Inducers (e.g., carbamazepine, omeprazole, smoking): May increase the clearance of olanzapine and decrease its plasma concentration. A dose increase of olanzapine may need to be considered.
- Antihypertensive Agents: May potentiate hypotensive effects.
- Levodopa and Dopamine Agonists: Olanzapine may antagonize their effects.
- Drugs that Prolong the QT Interval: Concomitant use with other drugs known to prolong the QTc interval (e.g., certain antiarrhythmics, antibiotics) should be avoided due to the potential for additive effects.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is close to the time of the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Doubling the dose to make up for a missed one is not recommended.
Overdose
Signs and Symptoms: Drowsiness, sedation, tachycardia, hypotension, extrapyramidal symptoms, agitation, delirium, coma. Other reported manifestations include convulsions, respiratory depression, and cardiopulmonary arrest. Fatalities have been reported in acute overdose. Management: There is no specific antidote. Establish and maintain a patent airway and ensure adequate oxygenation and ventilation. Cardiovascular monitoring is essential. Gastric lavage and administration of activated charcoal may be considered. Provide aggressive supportive care and symptomatic treatment. Hemodialysis is unlikely to be beneficial due to high protein binding.
Storage
Store at controlled room temperature, 20°-25°C (68°-77°F). Protect from light and moisture. Keep the blister packages sealed until the time of use. Keep out of reach of children.
Disclaimer
This information is for educational and professional medical reference purposes only and does not constitute medical advice. It is not a substitute for the professional judgment of a qualified healthcare provider in diagnosing and treating patients. The content is derived from the manufacturer’s prescribing information but may not be exhaustive. Dosage, indications, and safety profiles are subject to change. The prescriber should always rely on the most current official prescribing information and their own clinical judgment when making treatment decisions for an individual patient.
Reviews
- “Olanzapine remains a cornerstone in our formulary for acute psychosis and agitation. Its efficacy is robust, though the metabolic profile demands vigilant monitoring. The availability of the Zydis formulation is invaluable for ensuring adherence in our inpatient population.” — Head of Psychiatry, Academic Medical Center
- “From a clinical pharmacology standpoint, olanzapine’s broad receptor affinity explains its wide efficacy but also its side effect burden. It is a powerful tool, but its use must be carefully balanced against the risks of significant weight gain and metabolic derangement, particularly for long-term maintenance therapy.” — Clinical Pharmacologist, Research Institute
- “In my practice specializing in treatment-resistant mood disorders, the olanzapine-fluoxetine combination (Symbyax) has provided a critical option for patients who have failed multiple other antidepressant regimens. The response can be dramatic, but it necessitates a structured monitoring protocol for metabolic parameters.” — Consulting Psychiatrist, Mood Disorders Clinic