Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P46098 (5-HT3 receptor)
2,290 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The paper is devoted to review literature data on intravenous and oral antiemetic effectivity of granisetron (GRAN) a selective 5HT3 antagonist and to determine the optimal dose for the prophylaxis of chemotherapy-induced acute emesis. The drug was put on the market in the injectable form in 1994 and in the oral form in 1995, so a sufficient number of reports have been published for the evaluation. According to the summarized data on 6095 patients treated with intravenous GRAN, on average 66% antiemetic complete response (CR) rate was reached (i.e. no vomiting in the first 24 hours of chemotherapy). Best results were observed with the dose of 40 microg/kg intravenous GRAN, on average 70% CR (range 47-93%) were achieved in 4182 of the 6095 patients with this dose. In 942 patients treated with the mostly applied oral dose of GRAN (1 mg twice daily), on average 61% CR (range 52-82%) were reported. Side effects were weak and transient, mostly headache and constipation were observed. Headache appeared in 13% with the use of 40 microg/kg intravenous dose GRAN and in 18% with 1 mg oral dose twice daily Constipation was observed in 5.3% and 17% with the injection and oral dose, respectively.
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PMID:About the antiemetic effectivity of granisetron in chemotherapy-induced acute emesis: a comparison of results with intravenous and oral dosing. 1046 29

Postoperative nausea and vomiting (PONV) and post-discharge nausea and vomiting (PDNV) are frequent unpleasant complaints that patients and clinicians report after surgery. PONV and PDNV have been associated with postoperative complications and hospital discharge delays. Despite the extensive evidence describing the use of several regimens in different surgical populations, the ideal regimen has not been established. Several antiemetic drugs have been evaluated in more than 1000 clinical controlled trials for management of this complex emetogenic pathway, including the 5-hydroxytryptamine (5-HT3) receptor antagonists, dopamine receptor antagonists, neurokinin-type receptor antagonists, antihistaminics, anticholinergics, and corticosteroids, with the 5-HT3 receptor antagonists being the most commonly used for PONV prophylaxis. Because of the complex emetogenic pathway and multifactorial etiology of PONV, a multimodal approach using two or more drugs that act at different neuro-receptor sites is suggested in patients with one or more risk factors to successfully address PONV and reduce its incidence. Nevertheless, the most studied regimens in randomized clinical trials (RCTs) are the combination of serotonin 5-HT3 receptor antagonists with dexamethasone or dopamine receptor antagonists (droperidol). Therefore, the safest and more effective combination regimen appears to be the use of serotonin 5-HT3 receptor antagonist antiemetic drugs with dexamethasone.
Best Pract Res Clin Anaesthesiol 2020 Dec
PMID:What is the ideal combination antiemetic regimen? 3328 20