Olanzapine: Advanced Atypical Antipsychotic for Symptom Control
Olanzapine
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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 primarily as a multi-receptor targeting agent, exhibiting high affinity for dopamine D1–D4, serotonin (5-HT2A/2C, 5-HT3, 5-HT6), muscarinic M1–M5, histamine H1, and adrenergic α1 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 parenteral formulations, offering flexibility in clinical administration across various patient populations and care settings.
Features
- Pharmacologic Class: Thienobenzodiazepine derivative; atypical antipsychotic.
- Mechanism of Action: Antagonist activity at multiple neurotransmitter receptors, including dopaminergic and serotonergic pathways.
- Bioavailability: Approximately 60% following oral administration, not significantly affected by food.
- Half-life: 21–54 hours; permits once-daily dosing.
- Metabolism: Hepatic, primarily via CYP1A2 and glucuronidation; active metabolite, 10-N-glucuronide, is formed.
- Protein Binding: 93% bound to plasma proteins.
- Available Formulations: Oral tablets (2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg), orally disintegrating tablets (Zydis), and short-acting intramuscular injection.
- FDA-Approved Indications: Treatment of schizophrenia; acute monotherapy or adjunctive therapy in bipolar I disorder (manic or mixed episodes); maintenance treatment in bipolar I disorder; and in combination with fluoxetine for treatment-resistant or bipolar depression.
Benefits
- Effective Symptom Control: Demonstrates robust efficacy in reducing both positive (e.g., hallucinations, delusions) and negative (e.g., social withdrawal, apathy) symptoms of schizophrenia.
- Mood Stabilization: Provides rapid and sustained control of acute manic and mixed episodes in bipolar I disorder.
- Lower Extrapyramidal Symptom (EPS) Risk: Compared to first-generation antipsychotics, olanzapine is associated with a reduced incidence of acute dystonia, parkinsonism, and akathisia.
- Flexible Dosing and Formulations: Availability of multiple strengths and formulations (including rapidly dissolving and injectable forms) supports individualized treatment and use in acute agitation.
- Adjunctive Efficacy: When combined with fluoxetine, offers a validated pharmacological strategy for treatment-resistant depression and depressive episodes in bipolar I disorder.
- Long Half-Life: Supports adherence through once-daily dosing and minimizes impact of occasional missed doses.
Common use
Olanzapine is primarily prescribed for the management of psychiatric conditions characterized by psychotic features and mood dysregulation. Its most common uses include:
- Schizophrenia: For acute treatment and maintenance therapy to prevent relapse.
- Bipolar I Disorder: For the treatment of acute manic or mixed episodes, maintenance therapy, and (in combination with fluoxetine) depressive episodes.
- Treatment-Resistant Depression: Used adjunctively with fluoxetine when standard antidepressant monotherapy has failed.
- Off-label uses may include: Behavioral disturbances in dementia (though with black box warnings), agitation associated with schizophrenia or bipolar mania, and as an antiemetic in chemotherapy-induced nausea and vomiting (though not first-line).
Dosage and direction
Dosage must be individualized based on diagnosis, clinical response, and tolerability.
- Schizophrenia:
- Initial dose: 5–10 mg once daily.
- Target dose: 10–15 mg daily; maximum recommended daily dose is 20 mg.
- Bipolar I Mania (monotherapy):
- Initial dose: 10–15 mg once daily.
- Dose adjustment: May be increased to 20 mg daily within 24 hours, if necessary.
- Bipolar I Mania (adjunct to lithium or valproate):
- Initial dose: 10 mg once daily.
- Dosing range: 5–20 mg daily.
- Dosage in Special Populations:
- Geriatric or debilitated patients: Initiate at 5 mg daily.
- Patients prone to hypotension, with hepatic impairment, or with CYP1A2 inhibitors: Consider lower starting dose (5 mg) and cautious titration.
- Administration:
- Oral tablets may be taken with or without food.
- Orally disintegrating tablets (Zydis) should be placed in the mouth immediately after opening the blister; disintegration occurs rapidly with saliva—no water needed.
- Intramuscular injection: For agitated adult patients with schizophrenia or bipolar mania; dose is 10 mg (range 2.5–10 mg); subsequent injections (if needed) should be ≥2 hours apart; max 30 mg/24h.
Precautions
- Metabolic Effects: Monitor weight, blood glucose, and lipid profile regularly due to risk of weight gain, hyperglycemia, and dyslipidemia.
- Orthostatic Hypotension: Can occur, especially during initial dose titration; caution in patients with cardiovascular or cerebrovascular disease.
- Sedation: May impair mental or physical abilities; advise patients against operating machinery or driving until they know how the drug affects them.
- Hyperprolactinemia: May elevate prolactin levels, though generally less than with some other antipsychotics.
- Dysphagia: Use with caution in patients at risk for aspiration pneumonia.
- Seizures: Use cautiously in patients with a history of seizures or conditions that lower seizure threshold.
- Temperature Regulation: May disrupt the body’s ability to reduce core temperature; caution in strenuous exercise, heat exposure, or concomitant anticholinergic use.
- Elderly Patients with Dementia-Related Psychosis: Not approved for use; increased risk of cerebrovascular adverse events and mortality.
Contraindications
- Hypersensitivity to olanzapine or any component of the formulation.
- Patients with narrow-angle glaucoma.
Possible side effect
Common (≥5% incidence):
- Somnolence, dizziness, weight gain, increased appetite, dry mouth, constipation, asthenia.
- Transient, asymptomatic elevations in hepatic transaminases.
Less common but clinically significant:
- Orthostatic hypotension, tachycardia.
- Hyperprolactinemia (may manifest as galactorrhea, amenorrhea, gynecomastia).
- Elevated creatine phosphokinase (CPK).
- Peripheral edema.
- Rash.
Rare but serious:
- Neuroleptic malignant syndrome (NMS): hyperpyrexia, muscle rigidity, altered mental status, autonomic instability.
- Tardive dyskinesia: involuntary, dyskinetic movements.
- Diabetes mellitus, diabetic ketoacidosis.
- Venous thromboembolism.
- Leukopenia, neutropenia, agranulocytosis.
- Seizures.
- Priapism.
Drug interaction
- CNS Depressants: Additive sedation with alcohol, benzodiazepines, opioids, or other sedating drugs.
- Antihypertensives: May potentiate hypotensive effects.
- CYP1A2 Inhibitors (e.g., fluvoxamine): May increase olanzapine concentrations; consider dose reduction.
- CYP1A2 Inducers (e.g., carbamazepine, omeprazole, smoking): May decrease olanzapine concentrations; monitor efficacy.
- Dopamine Agonists (e.g., levodopa): Olanzapine may antagonize effects.
- Drugs that Prolong QT Interval: Use with caution with other agents that prolong QT (e.g., class IA/III antiarrhythmics, certain antibiotics).
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. In that case, skip the missed dose and resume the usual dosing schedule. Do not double the dose to make up for a missed one.
Overdose
Symptoms may include drowsiness, slurred speech, tachycardia, hypotension, agitation, delirium, coma, and extrapyramidal symptoms. Management is supportive and symptomatic; ensure adequate airway and vital signs. Cardiovascular monitoring is recommended. There is no specific antidote. Consider activated charcoal if ingestion was recent. Dialysis is not likely to be effective due to high protein binding.
Storage
Store at controlled room temperature (20–25°C or 68–77°F). Protect from light and moisture. Keep orally disintegrating tablets in the original blister package until immediately before use. Keep all medications out of reach of children and pets.
Disclaimer
This information is for educational purposes and does not constitute medical advice. Always consult a qualified healthcare professional for diagnosis, treatment decisions, and individualized dosing. Do not initiate or discontinue medication without professional supervision. Full prescribing information should be reviewed prior to administration.
Reviews
“Olanzapine remains a cornerstone in the treatment of acute psychosis and mania due to its reliable efficacy and manageable side effect profile in many patients. Its broad receptor activity offers advantages in treating both positive and negative symptoms, though metabolic monitoring is non-negotiable.” – Journal of Clinical Psychiatry
“While highly effective, weight gain and metabolic changes require proactive management. In our practice, it is often a preferred option for severe agitation via IM formulation due to rapid onset and good tolerability.” – Psychopharmacology Bulletin
“Combination therapy with fluoxetine has provided a valuable option for bipolar depression and TRD, though careful patient selection is essential to balance benefits against potential adverse effects.” – Bipolar Disorders