Chemotherapy-associated nausea and vomiting, prevention
藥理
Antiemetic; Selective 5-HT3 Receptor Antagonist
Selective 5-HT3-receptor antagonist, blocking serotonin, both peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone.
藥動學
1.Onset of action: IV: 1 to 3 minutes.
2.Duration: Oral, IV: Generally up to 24 hours.
3.Distribution: Vd: 2 to 4 L/kg; widely throughout body.
4.Protein binding: ~65%.
5.Metabolism: Hepatic via CYP1A1 and CYP3A4 N-demethylation, oxidation, and conjugation; some metabolites may have 5-HT3 antagonist activity.
6.Half-life elimination: Oral: 6 hours; IV: Mean range: 5 to 9 hours; SUBQ (extended release): ~24 hours.
7.Excretion: Urine (11% to 12% as unchanged drug, 48% to 49% as metabolites); feces (34% to 38% as metabolites)
禁忌症
Hypersensitivity to granisetron or any component of the formulation or to other 5-HT3 receptor antagonists.
懷孕分類
Available evidence is inconclusive or inadequate for determining fetal risk when used in pregnant women.
哺乳分類
Infant risk cannot be ruled out.
副作用
Asthenia, Headache, Somnolence, Fever
劑量和給藥方法
Chemotherapy-associated nausea and vomiting, prevention
IV: 10 mcg/kg within 30 minutes prior to chemotherapy; only on the day(s) chemotherapy is administered.