止吐注射 (antiemetics IV) Chemotherapy-induced nausea and vomiting; Prophylaxis. Postoperative nausea and vomiting. Postoperative nausea and vomiting; Prophylaxis. Radiation-induced nausea and vomiting; Prophylaxis.
藥理
Granisetron hydrochloride is a selective antagonist of 5-hydroxytryptamine(3) (5-HT(3)) receptors present peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone. Binding results in blockade of serotonin stimulation and subsequent vomiting triggered by emetogenic stimuli. Granisetron hydrochloride has little or no affinity for other serotonin receptors, for adrenergic, for dopamine-D(2), histamine-H(1), benzodiazepine, picrotoxin or opioid receptors.
藥動學
Distribution:
Vd: (IV, cancer patients), 3.07 L/kg
Vd: (IV, 21 y to 42 y), 3.04 L/kg
Vd: (IV, 65 y to 81 y), 3.97 L/kg
Vd: (IV, adult postoperative patients), 2.42 L/kg
Metabolism:
Hepatic; extensive; P450 CYP3A; N-demethylation, oxidation followed by conjugation
Excretion:
Renal: (IV), 49% as metabolites, approximately 12% unchanged.
Elimination Half Life:
Cancer patients: (IV), 8.95 h
21 y to 42 y: (IV), 4.91 h; 65 y to 81 y: (IV), 7.69 h
Adult postoperative patients: (IV), 8.63 h
禁忌症
Hypersensitivity to granisetron or any of its components
懷孕分類
Fetal risk cannot be ruled out. (TH)
哺乳分類
Infant risk cannot be ruled out.(MDX)
副作用
Common:
Neurologic: Asthenia (oral, 14% to 18% ), Headache (8.6% to 21% ), Somnolence (up to 10% )
Other: Fever (3% to 56% )
Serious:
Cardiovascular: Prolonged QT interval
Immunologic: Hypersensitivity reaction
劑量和給藥方法
Chemotherapy-induced nausea and vomiting; Prophylaxis
Postoperative nausea and vomiting
1 mg IV
Postoperative nausea and vomiting; Prophylaxis
1 mg IV before induction of anesthesia or immediately before reversal of anesthesia
小兒調整劑量
Chemotherapy-induced nausea and vomiting; Prophylaxis:
2 years and older, 10 mcg/kg IV 30 minutes before chemotherapy