Duration: 24 hours. Distribution: 2 to 4 L/kg. Protein binding: ~65%. Metabolism: Hepatic via CYP1A1 and CYP3A4 N-demethylation, oxidation, and conjugation; some metabolites may have 5-HT3 antagonist activity. Half-life elimination: 6 hours. Excretion: Urine ; feces.
禁忌症
Hypersensitivity to granisetron or any component of the formulation or to other 5-HT3 receptor antagonists.
懷孕分類
B
哺乳分類
副作用
>10%: Constipation (3% to 22%), nausea (20%), vomiting (12%), injection site reaction, asthenia (14% to 18%), headache (9% to 21%). 1% to 10%: hypertension (1% to 2%), prolonged QT interval on ECG (1% to 3%), alopecia (3%), abdominal pain (4% to 7%), decreased appetite (6%), diarrhea (4% to 9%), dyspepsia (3% to 6%), anemia (4%), leukopenia (9%), thrombocytopenia (2%), increased serum alanine aminotransferase (3% to 6%), increased serum aspartate aminotransferase (3% to 5%),anxiety (≤2%), dizziness (3% to 5%), drowsiness (≤4%), insomnia (4% to 5%),fever (3% to 9%).
劑量和給藥方法
Chemotherapy-induced nausea and vomiting (CINV), prevention: 2 mg once a day. The first dose should be given within one hour of treatment. Radiation therapy–associated emesis, prophylaxis: 2 mg once daily administered 1 to 2 hours prior to each fraction of radiation; administer in combination with dexamethasone.
小兒調整劑量
For infants, Children, and Adolescents: 40 mcg/kg/dose every 12 hours on chemotherapy days.
腎功能調整劑量
Children ≥ 2 years and Adolescents: No dosage adjustment necessary.