Olanzapine

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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 132539-06-1
  • AHFC code: 28:16.08.04
  • Synonyms:
  • ATC Code: N05AH03
  • Chemical Formula: C11H17NO3
  • Molecular Weight: 312.432
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00334 (APRD00138)
  • SMILES: CN1CCN(CC1)C1=NC2=CC=CC=C2NC2=C1C=C(C)S2
  • InChl: KVWDHTXUZHCGIO-UHFFFAOYSA-N
  • PubChem: 4585
  • IUPAC: 5-methyl-8-(4-methylpiperazin-1-yl)-4-thia-2,9-diazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),3(7),5,8,10,12-hexaene

Additional Details

Indication:
For the acute and maintenance treatment of schizophrenia and related psychotic disorders, as well as acute treatment of manic or mixed episodes of bipolar 1 disorder. Intramuscular olanzapine is indicated for the rapid control of agitated patients.
Pharmacodynamics:
Olanzapine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, olanzapine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors.
Mode of Action:
Olanzapine's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia.
Metabolism:
Hepatic
Toxicity:
Symptoms of an overdose include tachycardia, agitation, dysarthria, decreased consciousness and coma. Death has been reported after an acute overdose of 0.45g, but also survival after an acute overdose of 1500g.
General Reference:
de Haan L, van Amelsvoort T, Rosien K, Linszen D: Weight loss after switching from conventional olanzapine tablets to orally disintegrating olanzapine tablets. Psychopharmacology (Berl). 2004 Sep;175(3):389-90. Pubmed Pollack MH, Simon NM, Zalta AK, Worthington JJ, Hoge EA, Mick E, Kinrys G, Oppenheimer J: Olanzapine augmentation of fluoxetine for refractory generalized anxiety disorder: a placebo controlled study. Biol Psychiatry. 2006 Feb 1;59(3):211-5. Epub 2005 Sep 1. Pubmed Sepede G, De Berardis D, Gambi F, Campanella D, La Rovere R, DêAmico M, Cicconetti A, Penna L, Peca S, Carano A, Mancini E, Salerno RM, Ferro FM: Olanzapine augmentation in treatment-resistant panic disorder: a 12-week, fixed-dose, open-label trial. J Clin Psychopharmacol. 2006 Feb;26(1):45-9. Pubmed Jakovljevic M, Sagud M, Mihaljevic-Peles A: Olanzapine in the treatment-resistant, combat-related PTSDãa series of case reports. Acta Psychiatr Scand. 2003 May;107(5):394-6; discussion 396. Pubmed McGlashan TH, Zipursky RB, Perkins D, Addington J, Miller TJ, Woods SW, Hawkins KA, Hoffman R, Lindborg S, Tohen M, Breier A: The PRIME North America randomized double-blind clinical trial of olanzapine versus placebo in patients at risk of being prodromally symptomatic for psychosis. I. Study rationale and design. Schizophr Res. 2003 May 1;61(1):7-18. Pubmed
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