Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Data on the use of intravenous grainsetron (Kytril) were collected during a surveillance exercise amongst Swiss oncologists. The data were analysed to ascertain how grainsetron was used, and to document the incidence of adverse experiences in a clinical setting. Forty-nine oncologists at 40 Swiss centres were surveyed for their use of granisetron for the prevention and treatment of chemotherapy-induced nausea and vomiting. All were advised to follow the Swiss prescribing instructions for granisetron. They were invited to return data on patient demography, chemotherapy duration, granisetron dosing and adverse experiences. From 285 patients it was deduced that the mean daily dose of granisetron was 1.3 ampoules (3.9 mg) and the median daily dose was 1 ampoule (3 mg). The average number of doses of granisetron per patient per session was 3.8. There were 44 reports of adverse experiences by 34 patients, the most common report being headache. The survey confirmed that the large majority of patients undergoing chemotherapy required only a single dose of granisetron per day, and that the adverse experience profile was good.
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PMID:Granisetron (Kytril): a survey of use in clinical practice in Switzerland. 856 52

Granisetron (Kytril, Roche) is a 5-hydroxytryptamine 3 (5-HT(3))-receptor antagonist indicated for the prevention of nausea and/or vomiting associated with initial and repeat courses of emetogenic chemotherapy, including high-dose cisplatin. Its indication expanded in August 2002, with approval from the FDA for the prevention and treatment of postoperative nausea and vomiting. Granisetron strongly and selectively binds to the 5-HT(3) receptor with a binding constant of 0.26 nM and exhibits a 4000 - 40,000 times greater binding affinity for the 5-HT(3) receptor than other binding sites, including other 5HT subtypes and adrenergic, histaminergic and opioid receptors. Its selectivity to the 5-HT(3) receptor over other receptor types is > 1000:1. Granisetron noncompetitively binds to the 5-HT(3) receptor and is associated with a long duration of action as shown by the inhibition of a 5-HT axonal response flare for up to 24 h. Granisetron is unique among the 5-HT(3)-receptor antagonists because it is not metabolised via the cytochrome P450 (CYP) 2D6 pathway and is, therefore, less susceptible to variation in patient response because of factors such as pharmacogenomic differences. Granisetron and other 5-HT(3)-receptor antagonists are first-line agents for acute chemotherapy-induced nausea and vomiting (CINV), whereas combination therapy with 5-HT(3)-receptor antagonists, dexamethasone and neurokinin (NK)-1 receptor antagonism (i.e., with the recently approved aprepitant) is an effective approach to prevent delayed CINV. Granisetron has been shown to be an effective within-class rescue antiemetic for prophylactic failures, which may be linked to its pharmacological properties including non-competitive, insurmountable binding to the 5-HT(3) receptor. As with other 5-HT(3)-receptor antagonists, granisetron is well-tolerated with adverse events of mild severity including headache, asthenia and constipation. Overall, data demonstrate that granisetron is an efficacious, safe and cost-effective member of the 5HT(3)-receptor antagonist class for the prevention of CINV.
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PMID:Granisetron: new insights into its use for the treatment of chemotherapy-induced nausea and vomiting. 1294 86