Peringatan Keamanan

The toxicity symptoms of olanzapine are known to include somnolence, mydriasis, blurred vision, respiratory depression, hypotension, extrapyramidal symptoms and anticholinergic effects. The overdosage effects in children are generally associated with more significant side effects.A177059

The maximum registered dosage of olanzapine in clinical trials was of 300 mg and it was reported to present drowsiness and slurred speech. However, on post-marketing surveillance, a wide range of symptoms have been presented including agitation, dysarthria, tachycardia, extrapyramidal symptoms, and reduced consciousness. One case of overdosage-driven death was reported after ingestion of 450 mg of olanzapine. In the cases of acute overdosage, the establishment of adequate oxygenation and ventilation, gastric lavage and administration of activated charcoal with a laxative is recommended.FDA label

In carcinogenesis studies, olanzapine was showed to present an increase in the incidence of liver hemangiomas and hemangiosarcomas as well as mammary gland adenomas, and adenocarcinomas. On fertility studies, there was solely found impairment in male mating performance and delays in ovulation. There is no evidence of mutagenic, genotoxic potential not adverse events on fertility.FDA label

Olanzapine

DB00334

small molecule approved investigational

Deskripsi

Olanzapine is a thienobenzodiazepine classified as an atypical or second-generation antipsychotic agent.A176996 The second-generation antipsychotics were introduced in the 90s and quickly gained traction due to their impressive efficacy, reduced risk for extrapyramidal side effects and reduced susceptibility to drug-drug interactions.A177011 Olanzapine very closely resembles clozapine and only differs by two additional methyl groups and the absence of a chloride moiety.T554 It was discovered by scientists at Eli Lilly and approved to be marketed in the US in 1996.T548

Struktur Molekul 2D

Berat 312.432
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Olanzapine presents a half-life ranging between 21 to 54 hours with an average half-life of 30 hours.[A177014]
Volume Distribusi The volume of distribution of olanzapine is reported to be of 1000 liters which indicate a large distribution throughout the body.[A177014]
Klirens (Clearance) The mean clearance rate of olanzapine is of 29.4 L/hour however, some studies have reported an apparent clearance of 25 L/h.[T554]

Absorpsi

Olanzapine presents a linear pharmacokinetic profile and, after daily administration, it reaches steady-state in about a week.A177014 Under the administration of a normal dosage of olanzapine, the steady-state plasma concentration does not seem to exceed 150 ng/ml with an AUC of 333 ng/h/ml.A177059, T554 The absorption of olanzapine is not affected by the concomitant administration of food. The pharmacokinetic profile of olanzapine is characterized by reaching peak plasma concentration of 156.9 ng/ml approximately 6 hours after oral administration.T548

Metabolisme

Olanzapine is greatly metabolized in the liver, which represents around 40% of the administered dose, mainly by the activity of glucuronide enzymes and by the cytochrome P450 system. From the CYP system, the main metabolic enzymes are CYP1A2 and CYP2D6.A177014 As part of the phase I metabolism, the major circulating metabolites of olanzapine, accounting for approximate 50-60% of this phase, are the 10-N-glucuronide and the 4'-N-desmethyl olanzapine which are clinically inactive and formed by the activity of CYP1A2.T548 On the other hand, CYP2D6 catalyzes the formation of 2-OH olanzapine and the flavin-containing monooxygenase (FMO3) is responsible for N-oxide olanzapine.T551 On the phase II metabolism of olanzapine, UGT1A4 is the key player by generating direct conjugation forms of olanzapine.T551

Rute Eliminasi

Olanzapine is mainly eliminated through metabolism and hence, only 7% of the eliminated drug can be found as the unchanged form. It is mainly excreted in the urine which represents around 53% of the excreted dose followed by the feces that represent about 30%.A177014

Farmakogenomik

1 Varian
HTR1A (rs6295)

The presence of this polymorphism in HTR1A may indicate a higher level of efficacy in improving negative symptoms of schizophrenia when treated with olanzapine.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol may potentiate CNS adverse effects and orthostatic hypotension.
  • 2. Take with or without food. The absorption of olanzapine is unaffected by food.

Interaksi Obat

1867 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Olanzapine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Olanzapine is combined with Levodopa.
Risperidone Olanzapine may increase the hypotensive activities of Risperidone.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Olanzapine.
Deferasirox The serum concentration of Olanzapine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Olanzapine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Olanzapine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Olanzapine can be decreased when it is combined with Teriflunomide.
Buprenorphine Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
Hydrocodone Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Olanzapine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Olanzapine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
Orphenadrine Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
Rotigotine Olanzapine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Olanzapine.
Sodium oxybate Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
Thalidomide Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Lorazepam The risk or severity of adverse effects can be increased when Lorazepam is combined with Olanzapine.
Halazepam The risk or severity of adverse effects can be increased when Halazepam is combined with Olanzapine.
Diazepam The risk or severity of adverse effects can be increased when Diazepam is combined with Olanzapine.
Camazepam The risk or severity of adverse effects can be increased when Camazepam is combined with Olanzapine.
Ethyl loflazepate The risk or severity of CNS depression can be increased when Olanzapine is combined with Ethyl loflazepate.
Fludiazepam The risk or severity of adverse effects can be increased when Fludiazepam is combined with Olanzapine.
1,2-Benzodiazepine The risk or severity of adverse effects can be increased when 1,2-Benzodiazepine is combined with Olanzapine.
Pinazepam The risk or severity of CNS depression can be increased when Olanzapine is combined with Pinazepam.
Loprazolam The risk or severity of adverse effects can be increased when Loprazolam is combined with Olanzapine.
Doxefazepam The risk or severity of adverse effects can be increased when Doxefazepam is combined with Olanzapine.
Nordazepam The risk or severity of CNS depression can be increased when Olanzapine is combined with Nordazepam.
Oxazepam acetate The risk or severity of adverse effects can be increased when Oxazepam acetate is combined with Olanzapine.
Cinazepam The risk or severity of adverse effects can be increased when Cinazepam is combined with Olanzapine.
Bentazepam The risk or severity of adverse effects can be increased when Bentazepam is combined with Olanzapine.
Clonazepam The risk or severity of adverse effects can be increased when Clonazepam is combined with Olanzapine.
Midazolam The risk or severity of adverse effects can be increased when Midazolam is combined with Olanzapine.
Adinazolam The risk or severity of adverse effects can be increased when Adinazolam is combined with Olanzapine.
Delorazepam The risk or severity of adverse effects can be increased when Delorazepam is combined with Olanzapine.
Aclidinium The risk or severity of adverse effects can be increased when Olanzapine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Olanzapine.
Mirabegron The risk or severity of urinary retention can be increased when Olanzapine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Olanzapine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Olanzapine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Olanzapine.
Tiotropium The risk or severity of adverse effects can be increased when Olanzapine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Olanzapine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Olanzapine is combined with Umeclidinium.
Amisulpride Olanzapine may increase the antipsychotic activities of Amisulpride.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Olanzapine.
Quinagolide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Olanzapine.
Sulpiride Olanzapine may increase the antipsychotic activities of Sulpiride.
Benzylpenicilloyl polylysine Olanzapine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Olanzapine.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Olanzapine.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Olanzapine.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Olanzapine.
Valproic acid The serum concentration of Olanzapine can be decreased when it is combined with Valproic acid.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Olanzapine.
Lithium citrate Lithium citrate may increase the neurotoxic activities of Olanzapine.
Lithium hydroxide Lithium hydroxide may increase the neurotoxic activities of Olanzapine.
Mequitazine Olanzapine may increase the arrhythmogenic activities of Mequitazine.
Dapoxetine Dapoxetine may increase the orthostatic hypotensive activities of Olanzapine.
Atazanavir Olanzapine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Olanzapine can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefditoren Olanzapine can cause a decrease in the absorption of Cefditoren resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefpodoxime Olanzapine can cause a decrease in the absorption of Cefpodoxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefuroxime Olanzapine can cause a decrease in the absorption of Cefuroxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dabrafenib Olanzapine can cause a decrease in the absorption of Dabrafenib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dasatinib Olanzapine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Delavirdine Olanzapine can cause a decrease in the absorption of Delavirdine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexmethylphenidate The therapeutic efficacy of Dexmethylphenidate can be decreased when used in combination with Olanzapine.
Erlotinib Olanzapine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Amprenavir Olanzapine can cause a decrease in the absorption of Amprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fosamprenavir Olanzapine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gefitinib Olanzapine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Indinavir Olanzapine can cause a decrease in the absorption of Indinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Itraconazole Olanzapine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ledipasvir Olanzapine can cause a decrease in the absorption of Ledipasvir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methylphenidate The therapeutic efficacy of Methylphenidate can be decreased when used in combination with Olanzapine.
Nelfinavir Olanzapine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nilotinib Olanzapine can cause a decrease in the absorption of Nilotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pazopanib The therapeutic efficacy of Pazopanib can be decreased when used in combination with Olanzapine.
Rilpivirine Olanzapine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Risedronic acid Olanzapine can cause an increase in the absorption of Risedronic acid resulting in an increased serum concentration and potentially a worsening of adverse effects.
Saquinavir Olanzapine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Glycopyrronium The risk or severity of adverse effects can be increased when Olanzapine is combined with Glycopyrronium.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Olanzapine.
Phenindione The risk or severity of adverse effects can be increased when Olanzapine is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Olanzapine is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Olanzapine is combined with Tioclomarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Olanzapine is combined with 4-hydroxycoumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Olanzapine is combined with Ethyl biscoumacetate.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
D(1A) dopamine receptor DRD1
D(1B) dopamine receptor DRD5
D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 3A HTR3A
5-hydroxytryptamine receptor 6 HTR6
Histamine H1 receptor HRH1
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M4 CHRM4
D(1) dopamine receptor DRD1
Beta adrenergic receptor ADRB1
5-hydroxytryptamine receptor 1 HTR1A
GABA(A) Receptor Benzodiazepine Binding Site GABRA1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28503222
    Chelkeba L, Gidey K, Mamo A, Yohannes B, Matso T, Melaku T: Olanzapine for chemotherapy-induced nausea and vomiting: systematic review and meta-analysis. Pharm Pract (Granada). 2017 Jan-Mar;15(1):877. doi: 10.18549/PharmPract.2017.01.877. Epub 2017 Mar 15.
  • PMID: 26720055
    Martel ML, Klein LR, Rivard RL, Cole JB: A Large Retrospective Cohort of Patients Receiving Intravenous Olanzapine in the Emergency Department. Acad Emerg Med. 2016 Jan;23(1):29-35. doi: 10.1111/acem.12842. Epub 2015 Dec 31.
  • PMID: 28112422
    Yang T, Liu Q, Lu M, Ma L, Zhou Y, Cui Y: Efficacy of olanzapine for the prophylaxis of chemotherapy-induced nausea and vomiting: a meta-analysis. Br J Clin Pharmacol. 2017 Jul;83(7):1369-1379. doi: 10.1111/bcp.13242. Epub 2017 Mar 23.
  • PMID: 23902726
    Brunner E, Falk DM, Jones M, Dey DK, Shatapathy CC: Olanzapine in pregnancy and breastfeeding: a review of data from global safety surveillance. BMC Pharmacol Toxicol. 2013 Aug 1;14:38. doi: 10.1186/2050-6511-14-38.
  • PMID: 26266027
    Malhotra K, Vu P, Wang DH, Lai H, Faziola LR: Olanzapine-Induced Neutropenia. Ment Illn. 2015 Jun 23;7(1):5871. doi: 10.4081/mi.2015.5871. eCollection 2015 Feb 24.
  • PMID: 30422498
    Thomas K, Saadabadi A: Olanzapine .
  • PMID: 12921220
    Chue P, Singer P: A review of olanzapine-associated toxicity and fatality in overdose. J Psychiatry Neurosci. 2003 Jul;28(4):253-61.
Textbook
  • ISBN: 0-7817-5950-1
    Green W. (2001). Child & adolescent clinical psychopharmacology (3rd ed.). Lippincott Williams & Wilkins.
  • ISBN: 978-0-521-87363-5
    Ng C., Lin K., Singh B. and Chiu E. (2008). Ethno-psychopharmacology. Cambridge University Press.
  • ISBN: 978-161-5371-228
    Schatzberg A. and Nemeroff C. (2017). The american psychiatric association publishing textbook of psychopharmacology (5th ed.). American Psychiatric Association Publishing.

Contoh Produk & Brand

Produk: 1221 • International brands: 21
Produk
  • Abbott-olanzapine ODT
    Tablet, orally disintegrating • 5 mg • Oral • Canada • Generic • Approved
  • Abbott-olanzapine ODT
    Tablet, orally disintegrating • 10 mg • Oral • Canada • Generic • Approved
  • Abbott-olanzapine ODT
    Tablet, orally disintegrating • 15 mg • Oral • Canada • Generic • Approved
  • Accel-olanzapine
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Accel-olanzapine
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Accel-olanzapine
    Tablet • 7.5 mg • Oral • Canada • Generic • Approved
  • Accel-olanzapine
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Accel-olanzapine
    Tablet • 15 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 1221 produk.
International Brands
  • Aedon — G.L. Pharma
  • Amulsin — Sanitas
  • Apisco — LKM
  • Apsico — LKM
  • Arkolamyl — Mylan
  • Caprilon — Lavipharm
  • CO Olanzapine — Cobalt
  • Deprex — Square
  • Dominazol — Stein
  • Dopin — Daksh

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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