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OBJECTIVES: To assess the cardiovascular safety, tolerability and efficacy of high doses of granisetron for the treatment of nausea and vomiting in patients undergoing highly emetogenic chemotherapy. METHODS: Patients with histologically confirmed malignant disease were given an intravenous infusion of granisetron, 160 microg/kg, over 30 min, starting 15 min after highly emetogenic chemotherapy. Patients underwent cardiac monitoring for 24 h following the granisetron infusion. Pulse, blood pressure and electrocardiogram (lead II and ambulatory) measurements were taken, and routine clinical chemistry and haematology tests performed. Blood samples for pharmacokinetic analysis were taken before the granisetron infusion, and at intervals afterwards. Adverse events were self-assessed using a symptom checklist. Self-assessment categorical rating scales were used to evaluate patient nausea, vomiting and retching. RESULTS: Ten patients (eight females and two males; average age 41.5 years) completed the trial and were included in the safety and efficacy assessments. No clinically relevant changes in electrocardiogram, pulse rate, blood pressure or laboratory parameters were observed. Furthermore, in the 7 days following dosing there were no serious adverse events leading to withdrawal from the trial. A complete response (no vomiting, retching or, at most, mild nausea) was experienced by five patients. Six patients had no, or mild, nausea and an additional two patients vomited on a maximum of two occasions. Additional antiemetic rescue medication was given to three patients during the 24-h trial period. Despite considerable interpatient variability, C(max) and AUC parameters were proportionally greater than values reported for lower doses of granisetron. CONCLUSIONS: Granisetron administered at four times the upper recommended dose demonstrated good efficacy and tolerability with no clinically important cardiac effects.

Original publication

DOI

10.1007/s00280-003-0689-6

Type

Journal article

Journal

Cancer Chemother Pharmacol

Publication Date

02/2004

Volume

53

Pages

123 - 128

Keywords

Adult, Antiemetics, Antineoplastic Agents, Area Under Curve, Cardiovascular Diseases, Electrocardiography, Female, Granisetron, Half-Life, Humans, Male, Middle Aged, Nausea, Neoplasms, Vomiting