II. Class
- Atypical Antipsychotic (Second Generation agent)
- Neuroleptic
- Thienobenzodiazepine
III. Mechanism
- Primarily Serotonin Type II Antagonist (5-HT2 antagonist)
- Also Dopamine, muscarinic Anticholinergic, alpha-1 and histamine H1 antagonist
- Chemical structure similar to Clozapine
IV. Indications
- Primary Indications
- Schizophrenia
- Acute mania phase of Bipolar Disorder
- Agitated Delirium (emergency department)
- Other Indications
- Migraine Headache
- Appears to have similar efficacy to Droperidol (Inapsine) for Migraine Headache
- Hill (2008) Acad Emerg Med 15(9):806-11 +PMID:19244630 [PubMed]
- Migraine Headache
- Avoid use in Psychosis in Dementia
- Higher risk of CVA and overall mortality in elderly
V. Dosing
- Adults
- Start: 5 to 10 mg orally daily
- Increase in 5 mg increments weekly as tolerated
- Maximum: 20 mg/day
- Elderly
- Initial: 1.25 to 2.5 mg PO qd
- Titrate up as tolerated (watch for Hypotension)
- Maximum: 10 mg/day
- Acute management of Agitation
- Dose: 10 mg IM every 4 hours (up to 30 mg/day)
- Emerging: Intravenous dosing
- Only FDA approved for oral and IM delivery
- Large HCMC ED study in 2016 demonstrated safety of IV doses (typically 5 mg)
- No serious complications including no QT Prolongation (although Hypoxia did occur)
- Martel (2016) Acad Emerg Med 23(1): 29-35 +PMID:26720055 [PubMed]
VI. Adverse Effects
- See Antipsychotics
- Weight gain (4 kg)
- Sedation
- Orthostatic Hypotension
- Seizures (nearly 1% of patients)
- Overall higher mortality in elderly
- Lowest risk of QTc Prolongation compared with other Antipsychotics
-
Hyperglycemia
- Increased risk of Diabetes Mellitus
- Koro (2002) BMJ 325:243-5 [PubMed]
- Hyperlipidemia
- Other effects
- Neuroleptic malignant sydnrome (rare, but lethal)
- Extrapyramidal Side Effects
- Increased Liver Function Tests
- Increased Creatine Kinase
- Pancreatitis
- Anticholinergic side effects
VII. Drug Interactions
- Increase Antipsychotic levels (toxicity risk): Monitor for toxicity
- Decrease Antipsychotic levels (lower efficacy)
- Cardiorespiratory depression (includes sedation, Bradycardia and Hypotension)
- Benzodiazepines (e.g. Midazolam)
- Based on warning in prescribing information since 2005
- Combination appears safe from studies in which Olanzapine was combined with Benzodiazepines
- EMA recommends separating dosing by 60 minutes
- Williams (2018) Ment Health Clin 8(5): 208–213 +PMID: 30206503 [PubMed]
- Benzodiazepines (e.g. Midazolam)
VIII. Safety
- Pregnancy Category C
- Not recommended during Lactation (found in Breast Milk)
IX. Monitoring
- See Antipsychotic
X. References
- Glauser and Peters (2016) Crit Dec Emerg Med 30(4): 17-27
Images: Related links to external sites (from Bing)
Related Studies
olanzapine (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
OLANZAPINE 10 MG TABLET | Generic | $0.19 each |
OLANZAPINE 15 MG TABLET | Generic | $0.31 each |
OLANZAPINE 2.5 MG TABLET | Generic | $0.13 each |
OLANZAPINE 20 MG TABLET | Generic | $0.34 each |
OLANZAPINE 5 MG TABLET | Generic | $0.14 each |
OLANZAPINE 7.5 MG TABLET | Generic | $0.18 each |
OLANZAPINE ODT 10 MG TABLET | Generic | $1.38 each |
OLANZAPINE ODT 15 MG TABLET | Generic | $1.44 each |
OLANZAPINE ODT 20 MG TABLET | Generic | $2.63 each |
OLANZAPINE ODT 5 MG TABLET | Generic | $1.31 each |
OLANZAPINE-FLUOXETINE 12-25 MG | Generic | $13.13 each |
OLANZAPINE-FLUOXETINE 12-50 MG | Generic | $14.19 each |
OLANZAPINE-FLUOXETINE 3-25 MG | Generic | $7.23 each |
OLANZAPINE-FLUOXETINE 6-25 MG | Generic | $7.95 each |
OLANZAPINE-FLUOXETINE 6-50 MG | Generic | $9.74 each |
zyprexa (on 6/22/2016 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ZYPREXA ZYDIS 10 MG TABLET | Generic | $1.38 each |
Ontology: olanzapine (C0171023)
Definition (CHV) | a drug used to treat schizophrenia |
Definition (NCI_NCI-GLOSS) | A drug used to treat certain mental disorders. It is also being studied in the treatment of nausea and vomiting caused by some cancer treatments. It is a type of antipsychotic and a type of monoamine antagonist. |
Definition (NCI) | A synthetic derivative of thienobenzodiazepine with antipsychotic, antinausea, and antiemetic activities. As a selective monoaminergic antagonist, olanzapine binds with high affinity binding to the following receptors: serotoninergic, dopaminergic, muscarinic M1-5, histamine H1, and alpha-1-adrenergic receptors; it binds weakly to gamma-aminobutyric acid type A, benzodiazepine, and beta-adrenergic receptors. The antinausea and antiemetic effects of this agent appear to be due to the blockade of 5-HT2 and 5-HT3 receptors for serotonin. Although its exact mechanism of action in schizophrenia is unknown, it has been proposed that olanzapine's antipsychotic activity is mediated through antagonism to dopamine D2 receptors with rapid ligand-receptor dissociation kinetics that help to minimize extrapyramidal symptoms (EPS). Olanzapine may also stimulate appetite. |
Definition (PDQ) | A synthetic derivative of thienobenzodiazepine with antipsychotic properties. As a selective monoaminergic antagonist, olanzapine binds with high affinity binding to the following receptors: serotonin, dopamine, muscarinic M1-5, histamine H1, and alpha1-adrenergic receptors; it binds weakly to gamma-aminobutyric acid type A, benzodiazepine, and beta-adrenergic receptors. Although its exact mechanism of action in schizophrenia is unknown, it has been proposed that olanzapine's antipsychotic activity is mediated through a combination of dopamine and serotonin type 2 antagonism. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=449664&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=449664&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C47639" NCI Thesaurus) |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C076029 |
SnomedCT | 108441004, 386849001 |
LNC | LP18087-4, MTHU002999 |
English | 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno(2,3-b)(1,5)benzodiazepine, olanzapine, 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno(2,3-b)(1,5)benzodiazepine, olanzapine (medication), olanzapine [Chemical/Ingredient], OLANZAPINE, olanzapine (Zyprexa), OLANZapine, Olanzapine, Olanzapine (product), Olanzapine (substance) |
Spanish | olanzapina (producto), olanzapina (sustancia), olanzapina |
Ontology: Zyprexa (C0527258)
Definition (CHV) | a kind of psychiatry drug |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C076029 |
English | Zyprexa, zyprexa, ZyPREXA, Eli Lilly brand of olanzapine, Lilly brand of olanzapine |