[BRL 43694A--a 5-hydroxytryptamine receptor blocker as an antiemetic in cytostatic therapy].
An open study of the new antiemetic BRL 43694A, a 5-hydroxytryptamine-3-receptor antagonist, was performed in 29 patients undergoing highly emetogenic cancer chemotherapy (25 patients received cisplatin in a dose greater than or equal to 50 mg/m2). Patients received BRL 43694A as a 30-minute infusion one hour after the administration of chemotherapy. 7 patients were treated with 40 micrograms/kg and 13 patients with 100 micrograms/kg BRL 43694A; the last 9 patients received an initial dose of 40 micrograms/kg with a provision for two additional interventional doses over 24 hours in the event of prolonged nausea or vomiting. 14 patients experienced no vomiting (48%) and 13 patients (45%) had 1-5 vomiting episodes over 24 hours following administration of the cytostatic agents. BRL 43694A did not cause major side effects. Based on our preliminary experience the new 5-HT3-receptor antagonist BRL 43694A is a potent antiemetic drug for the treatment of chemotherapy-induced nausea and vomiting.
Joss
R
R
Institut für Medizinische Onkologie, Inselspital Bern.
Rohrbach
D
D
Buser
K
K
Pirovino
M
M
Karde
C
C
Brunner
K
K
D000328:Adult; D000368:Aged; D000932:Antiemetics / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000009:adverse effects*; D004341:Drug Evaluation; D005260:Female; D017829:Granisetron; D006801:Humans; D007191:Indazoles / Q000008:administration & dosage / Q000627:therapeutic use*; D008297:Male; D008875:Middle Aged; D011720:Pyrazoles / Q000627:therapeutic use*; D012702:Serotonin Antagonists / Q000627:therapeutic use*; D014839:Vomiting / Q000139:chemically induced / Q000517:prevention & control*
D000932:Antiemetics; D000970:Antineoplastic Agents; D017829:Granisetron; D007191:Indazoles; D011720:Pyrazoles; D012702:Serotonin Antagonists
BRL 43694A--ein 5-Hydroxytryptamin-Rezeptoren-Blocker als Antiemetikum in der Zytostatika-Therapie.