Granisetron Hydrochloride CAS 107007-99-8

Granisetron hydrochloride

CAS 107007-99-8

Granisetron hydrochloride has high receptor selectivity. Its affinity with 5-HT3 receptor is 4000-10000 times of that with other receptors such as 5-HT1, 5-HT2, dopamine D1, D1, histamine H1, benzodiazepine and opioid receptor, while the difference of ondansetron is only 1000 times. The antiemetic rate of granisetron hydrochloride was 93%, 96% and 100% in three dose groups: 2 × 0.005, 2 × 0.05 and 2 × 0.5mg/kg (IV), while that of ondansetron 2 × 2.5mg/kg was 89%. According to the toxicity study, granisetron hydrochloride can achieve a good antiemetic effect at a small dose, with little side effect. The cardiovascular system was abnormal at high dose. As the clinical recommended dose of granisetron hydrochloride is very small (3mg / D), it is only the lowest dose used in animal experiments (< 1mg / kg = L / 25), so the clinical application is very safe. The pharmacokinetic study showed that the half-life (T1 / 2) of granisetron hydrochloride in patients was 9h, that in healthy people was 4h, that in the elderly was 7.7h, and that in young people was 4.9h. Granisetron hydrochloride is mainly metabolized in the liver. It is excreted in the form of 7-hydroxygranisetron hydrochloride and other metabolites through feces and urine. The plasma clearance rate of liver function damaged or liver metastasis cancer decreased, and the clearance rate of renal insufficiency was 1 / 4 of that of normal. A high first pass metabolism was observed by oral administration, with an absolute bioavailability of 60%.

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