Description: Ramosetron Hydrochloride for Injection is used for the prevention and treatment of anti-cancer medication caused nausea, vomiting and other gastrointestinal symptoms. The main ingredients of this product of hydrochloric acid ramosetron, chemical name: (-(R-5 -[(1-methyl-1H-indole-3-ylcarbonyl]-4,5,6,7-tetrahydro-1H-benzimidazole hydrochloride 2 Cymbalta injection, excipients mannitol.This product is white or white lumps or powder .
Pharmacological effects: 1.5-HT3 receptor antagonism of 5-HT3 induced guinea pig isolated colon contraction experiment and rats, ferrets heart rate reduction the slow reflex (Bezold-Jarisch reflex) experiments, the drug 5-HT3 receptor antagonism. The anti-cancer drug-induced vomiting mechanism of inhibition of cisplatin-induced vomiting ferrets, vomiting before or after the initial vomiting give this product shows the inhibitory effect. Cisplatin and other anti-cancer drugs can - serotonin freed from chromaffin cells of the digestive tract. 5-serotonin present in the gastrointestinal mucosa afferent vagal nerve endings 5-HT3 receptor binding, thereby stimulating the vomiting center to induce vomiting. The hydrochloric acid ramosetron is through blocking this 5-HT3 receptor play an antiemetic effects. Toxicology acute toxicity of intravenous administration of animal experiments in mice, rats and dogs. mice and rats after administration seen a transient decrease in spontaneous movement, tremors and spasms of death. LD50, male mice the 90-108mg/kg, female mice were 108-130 mg / kg, 172mg/kg of male rats, female rats 151 mg / kg. dogs administered 30mg/kg seen after vomiting, shortness of breath, rapid heart rate, weight loss, does not appear to death no matter what kind of animals are no significant gender differences. subacute toxicity in rats and dogs The one-month intravenous administration of animal experiments. rats (dose: 0.1,1.0,10 mg / kg / day administration of 1 mg / kg of the GPT increased slightly (about the control group 1.2 times the weight gain when administered 10mg/kg inhibited (about 4%, but, no matter what kind of animal organs and tissues were obtained histopathological abnormalities presumed to be the maximum non-toxic dose of rat 0.1 mg / kg / day. Highest dog to Pharmacy amounted to 3 mg / kg, did not appear toxic effects, reproductive toxicity and carcinogenicity in rats and rabbits administered intravenously, the dose up to 10 mg / kg gestation / rat does not appear, does not appear teratogenic, fetal death, only born mouse weight gain was inhibited at doses up to 20 mg / kg Rabbit reduced fetal weight, delayed ossification, but no teratogenic effects 24 weeks oral administration to rats and mice showed no tumor occurred.
Pharmacokinetics: Plasma concentrations in healthy adults intravenous administration of 0.1 ~ 0.8mg, plasma the prototype drug concentration was reduced biphasic, the T1/2β is about 5 hours. AUC is directly proportional to the dose, in vivo drug dynamic changes linearly healthy adults of intravenous administration, metabolic pharmacokinetic parameters
Indications: the prevention and treatment of anti-cancer medication caused nausea, vomiting and other gastrointestinal symptoms.
Precautions: Recommendations of the goods in 15-30 minutes prior to anti-cancer therapy intravenous administration. Drug safety during pregnancy has not been established only in determining treatment for pregnant women or women who may become pregnant, usefulness is greater than the risk before administration. usually elderly patients with low physiological function, patients should be closely observed state, careful administration. timely processing of adverse reactions.
Adverse reaction: body heat, headache, heavy head. serious adverse reaction, allergy-like symptoms may occur. Those who are allergic to the chemicals, such as chest tightness, difficulty breathing, wheezing, facial flushing, redness, itching, cyanosis, lower blood pressure and even shock.
