Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0042963 (vomiting)
 31,883 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Ramosetron hydrochloride as a 5-HT3 receptor antagonist-type antiemetic, which was developed in Japan. It has an indole ring which is the mother nucleus of serotonin (5-HT) and a tetrahydrobenzimidazol radical. These components are linked by a carbonyl radical. It was reported in non-clinical studies that ramosetron hydrochloride exhibited more potent and sustained antagonistic activities against 5-HT3 receptors than existing 5-HT3 receptor antagonist-type antiemetics. It was also reported that ramosetron hydrochloride inhibited vomiting by anticancer drugs in a potent and sustained manner. The phase I trial was initiated in May, 1991. Phase II and phase III trials were then conducted in a total of 357 patients at 121 institutions in Japan. The symptoms targeted in these trials were nausea and vomiting induced by anticancer drugs, such as cisplatin. Based on the results of the phase II trial, it was recommended that ramosetron hydrochloride be infected once daily at a dose of 0.3 mg. In phase III trial, a placebo-controlled double-blind study and an open trial was performed. The utility of the drug seemed to be confirmed by the results of these studies. Ramosetron hydrochloride shown an efficacy rate of 79.8% (178/223 patients) against nausea and vomiting induced by anticancer drugs, such as cisplatin when administered at a dose of 0.3 mg. The efficacy rate was 85.1% (40/47 patients) when given at a dose of 0.3 mg before the administration of anticancer drugs, such as cisplatin. The incidence of adverse effects was 2.0% (7/352 patients). Main adverse effects reported were feeling of heat, headache, and heavy feeling in the head. These adverse effects were of no clinical importance.
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PMID:[A new antiemetic ramosetron hydrochloride]. 905 Nov 43

Suppositories are the preferable dosage form for patients at home or experiencing nausea. Serotonin (5-HT(3))-receptor antagonists are used to treat vomiting in intravenous or oral administration but not suppository form. Ramosetron hydrochloride (RAM) is a new 5-HT(3) antagonist which effectively inhibits vomiting, and we prepared RAM suppositories using Witepsol((R)) H-15 (H-15) containing Carbopol((R)) 934P (CP). The viscosity of suppository base and RAM release properties from suppositories were examined. Plasma RAM concentrations after administration of suppositories to rabbits were estimated and irritation of rectal tissues were observed. Antiemetic effects of suppositories were studied using ferrets. The base viscosity increased with addition of CP. Suppositories containing CP exhibited better absorption in rabbits compared to H-15 suppositories, correlated with release behavior. Suppositories containing 2% CP had 2.5 times larger AUC(0-24 h) than H-15 suppositories, and the MRT was prolonged by 5.8 h compared with i.v. administration. 10% CP suppositories administered to rabbits for 5 days did not irritate the tissues. Antiemetic studies indicated that 2% CP suppository of RAM might have the same effect as i.v. administration. These results suggest that RAM suppositories containing CP are safe and useful in once-a-day dosage form for treatment of chemotherapy-induced nausea.
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PMID:Mucoadhesive suppositories of ramosetron hydrochloride utilizing Carbopol. 1060 83