Pharmacological action of Azasetron hydrochloride

Azasetron hydrochloride to choose the 5-HT3 receptor antagonist, the study of the affinity of 5-HT3 receptor in rat cerebral cortex showed that the affinity of Azasetron hydrochloride was 410 times times stronger than that of metoclopramide, 2-4 times of Ondansetron. Animal experiments show that Azasetron hydrochloride 0.1mg/kg intravenous injection can inhibit cisplatin-induced vomiting in rabbit dogs: 0.3g/kg can completely inhibit adriamycin and cyclophosphamide-induced blood mink vomiting. The clinical results showed that the Azasetron hydrochloride intravenous injection of 10mg could inhibit the nausea and vomiting caused by anticancer drugs such as cisplatin.

Absorption, distribution, elimination

According to the literature report, the healthy male volunteers static note this product 10mg after 3 minutes the plasma of the prototype drug concentration is 190.5UG/ML, its pharmacokinetics is linear. This product is eliminated bi-directional, the half cycle is 0.13h and 4.3h respectively. For patients undergoing cisplatin treatment of malignant tumors, intravenous injection of 10mg after the end half-life of 7.3 1 ± 2h, compared to healthy adults. Prototype drug 24 by urine excretion of 64.3 ± 15%.


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