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A highly selective serotonin (5 - HT3) 3 receptor antagonist, for nausea and vomiting caused by radiotherapy, chemotherapy and surgery has a good prevention and treatment effect. Radiotherapy with chemotherapy and surgery can cause intestinal chromaffin cells release 5 - HT, 5 - HT can activate central or vagus nerve endings 5 - HT3 receptors and cause gag reflex. Gamla SiQiong control mechanism of nausea and vomiting, hydrochloric acid by antagonism central chemical zone and the peripheral vagus nerve endings in the 5 - HT3 receptors, inhibit the occurrence of nausea and vomiting. Hydrochloric acid granite SiQiong high selectivity, without excessive extrapyramidal reactions, calm and other adverse reactions.

Healthy volunteers single oral pharmacokinetic 】 【 1 mg, peak plasma concentration is 3.63 ng/ml, plasma clearance has a half-life of 6.23 hours, distribution volume of 3.94 L/kg, serum protein combined with the rate of about 65%, the total clearance rate of 0.4 L/h/kg. The removal of the cancer patients significantly prolong half-life, 9.8 ~ 11.6 hours. Healthy volunteers in the condition of not fasting, single oral gamla SiQiong hydrochloride 10 mg, AUC (area under the curve when the medicine -) fell 5%, Cmax increased by 30%. Healthy volunteers oral gamla SiQiong hydrochloride, about 11% of the dose in 48 hours in the form of prototype drug excretion from urine, and the rest in the form of metabolism excretion, in the urinary and fecal excretion rate were 48% and 38% respectively. The absolute bioavailability of oral tablet was 90%. Gamla SiQiong hydrochloride combined with plasma protein rate is about 65%. Gamla SiQiong hydrochloric acid metabolism of particles by the liver enzyme P450 3 a mediated, and the major metabolic pathways for N - demethylation aromatic epoxidation and then combine the product.

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