Palonosetron hydrochloride for the prevention of chemotherapy-induced nausea and vomiting.
A large number of different 5-hydroxytryptamine (HT)(3) receptor antagonists have been marketed with the indication of preventing nausea and vomiting induced by chemotherapy--palonosetron is the most recently developed of these. Pharmacologic studies have revealed that palonosetron has a long half-life, a high affinity for 5-HT(3) receptors, exhibits allosteric binding to 5-HT(3) receptors and possess positive cooperativity. Although interesting, pharmacologic differences are only useful if they result in clinical advantages, such as an increase in efficacy and/or an improvement in tolerability. We summarize preclinical and clinical studies of palonosetron and compare the efficacy and tolerability with the other 5-HT(3) receptor antagonists, ondansetron, granisetron and dolasetron.
Ruhlmann
Christina
C
Odense University Hospital, Department of Oncology, Sdr. Boulevard 29, DK-5000 Odense C, Denmark. christina.ruhlmann@ouh.regionsyddanmark.dk
Herrstedt
Jørn
J
D000932:Antiemetics / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000009:adverse effects*; D002986:Clinical Trials as Topic; D006801:Humans; D007546:Isoquinolines / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D009325:Nausea / Q000139:chemically induced / Q000517:prevention & control*; D000077924:Palonosetron; D011812:Quinuclidines / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D014839:Vomiting / Q000139:chemically induced / Q000517:prevention & control*
D000932:Antiemetics; D000970:Antineoplastic Agents; D007546:Isoquinolines; D011812:Quinuclidines; D000077924:Palonosetron