Olanzapine 98% supplier in China CAS NO.132539-06-1

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1. Introduction of Olanzapine

Olanzapine (trade name Zyprexa or in combination with fluoxetine Symbyax) is an atypical antipsychotic, approved by the U.S. Food and Drug Administration (FDA) for the treatment of schizophrenia and bipolar disorder.[2] Olanzapine is structurally similar to clozapine, but is classified as a thienobenzodiazepine.

2. Properties of Olanzapine

ACD/LogP: 3.076 ACD/LogD (pH 5.5): 0.42 ACD/LogD (pH 7.4): 2.35
ACD/BCF (pH 5.5): 1.00 ACD/BCF (pH 7.4): 23.98
ACD/KOC (pH 5.5): 2.50 ACD/KOC (pH 7.4): 210.04
#H bond acceptors: 4 #H bond donors: 1
#Freely Rotating Bonds: 1 Polar Surface Area: 59.11  2
Index of Refraction: 1.709 Molar Refractivity: 92.156 cm3
Molar Volume: 235.993 cm3 Polarizability: 36.534 10-24cm3
Surface Tension: 52.015998840332 dyne/cm Density: 1.324 g/cm3
Flash Point: 241.697 °C Enthalpy of Vaporization: 73.967 kJ/mol
Boiling Point: 476.035 °C at 760 mmHg
 

3. Structure descriptors of Olanzapine

SMILES:CN1CCN(CC1)C/2=N/c4ccccc4Nc3sc(C)cc\23

Std. InChI:InChI=1S/C17H20N4S/c1-12-11-13-16(21-9-7-20(2)8-10-21)18-14-5-3-4-6-15(14)19-17(13)22-12/h3-6,11,19H,7-10H2,1-2H3

Std. InChIKey:KVWDHTXUZHCGIO-UHFFFAOYSA-N
 

4. Medical uses

Prevention of psychosis

Olanzapine has been considered as part of an early psychosis approach for schizophrenia. The Prevention through Risk Identification, Management, and Education (PRIME) study, funded by the National Institute of Mental Health and Eli Lilly, tested the hypothesis that olanzapine might prevent the onset of psychosis in people at very high risk for schizophrenia. The study examined 60 patients with prodromal schizophrenia, who were at an estimated risk of 36–54% of developing schizophrenia within a year, and treated half with olanzapine and half with placebo.[16] In this study, patients receiving olanzapine did not have a significantly lower risk of progressing to psychosis. Olanzapine was effective for treating the prodromal symptoms, but was associated with significant weight gain.

Use in elderly

Citing an increased risk of stroke, in 2004 the Committee on the Safety of Medicines (CSM) in the UK issued a warning that olanzapine and risperidone, both atypical antipsychotic medications, should not be given to elderly patients with dementia. In the U.S., olanzapine comes with a black box warning for increased risk of death in elderly patients. It is not approved for use in patients with dementia-related psychosis.However, a BBC investigation in June 2008 found that this advice was being widely ignored by British doctors.

Investigatory uses

Olanzapine has been investigated for use as an antiemetic, particularly for the control of chemotherapy-induced nausea and vomiting (CINV). A 2007 study demonstrated its successful potential for this use, achieving a complete response in the acute prevention of nausea and vomiting in 100% of patients treated with moderately and highly-emetogenic chemotherapy, when used in combination with palonosetron and dexamethasone.