Granisetron: relating pharmacology to clinical efficacy.
The 5-HT(3)-receptor antagonists, which are regarded as the 'antiemetic gold-standard', are used for prophylaxis against chemotherapy- and radiotherapy-induced emesis. At equally effective doses, the 5-HT(3)-receptor antagonists have been shown to demonstrate broadly equivalent clinical antiemetic activity and safety. However, the pharmacology of granisetron suggests that it may have an improved side-effect and tolerability profile, a lower risk of drug interactions and a longer duration of action than other 5-HT(3)-receptor antagonists. The high affinity of granisetron, coupled with the insurmountable antagonism displayed at 5-HT(3) receptors, is thought to underlie its good clinical efficacy.
Blower
Peter R
PR
Poole House, Great Yeldham, Essex, CO9 4HP, United Kingdom. peter@rblower.freeserve.co.uk
D000932:Antiemetics / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000009:adverse effects*; D004347:Drug Interactions; D017829:Granisetron / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000532:radiotherapy; D011878:Radiotherapy / Q000009:adverse effects; D014839:Vomiting / Q000188:drug therapy / Q000209:etiology* / Q000517:prevention & control*
D000932:Antiemetics; D000970:Antineoplastic Agents; D017829:Granisetron