Antipruritic Potency of Serotonin Type 3 (5-HT3) Receptor Antagonists--a Reply

1999 ◽  
Vol 135 (5) ◽  
pp. 599-600
Author(s):  
E. Weisshaar
Keyword(s):  
2016 ◽  
Vol 8 ◽  
pp. CMT.S10240 ◽  
Author(s):  
Hiromitsu Kitayama

Serotonin-type 3 receptor antagonists have been available as intravenous and oral formulations. Recently, granisetron transdermal system has won a firm position in the antiemesis of cancer chemotherapy. Its pharmacokinetic profile has been shown by pooled population analysis incorporation data. The 52 cm2 patch, which contains 34.3 mg granisetron, releases 3.3 mg daily and reaches the maximal plasma concentration after 48 hours, maintaining a 2.2 ng/mL stable average concentration over six days. This level is similar to the one obtained with daily oral 2 mg of granisetron. Three randomized clinical studies evaluating its efficacy have been published. Transdermal granisetron showed noninferiority to other formulations of serotonin-type 3 receptor antagonists for highly and moderately emetogenic – including multiday – chemotherapy. The adverse effects were not significantly different from other formulations. The system has possible applications in oral chemotherapy, radiotherapy, dexamethasone sparing, palliative care, and refractory emesis due to benign disease.


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