[Pharmacokinetics of azasetron (Serotone), a selective 5-HT3 receptor antagonist].
5-HT3 receptor antagonists have been established in a number of clinical trials as effective agents in the management of nausea and vomiting induced by cancer chemotherapy including cisplatin. Azasetron (Serotone) is a potent and selective 5-HT3 receptor antagonist, and classified as benzamide derivative. It has a different chemical structure from indole-type 5-HT3 receptor antagonists such as granisetron, ondansetron, ramosetron and tropisetron. The major difference is found in the pharmacokinetic profiles. Approximately 60-70% of azasetron administered i.v. and orally is excreted in urine as the unmetabolized form. Also, orally-administered azasetron has shown to be absorbed and/or secreted by the saturable transport mechanism in the small intestine, resulting in good bioavailability as approximately 90%. In this report, the relationship between the structure of 5-HT3 receptor antagonists (especially azasetron) and their pharmacokinetics were described.
Cancer Chemotherapy Center, Japanese Fundation for Cancer Research.
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Tsukagoshi
D000284:Administration, Oral; D000932:Antiemetics / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D010078:Oxazines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D012702:Serotonin Antagonists / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D013329:Structure-Activity Relationship; D014840:Vomiting, Anticipatory / Q000188:drug therapy
D000932:Antiemetics; D019086:Bridged Bicyclo Compounds, Heterocyclic; D010078:Oxazines; D012702:Serotonin Antagonists; C070671:azasetron