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贝络纳、枸橼酸莫沙必利(Ballona, mosapride citrate)
贝络纳、枸橼酸莫沙必利(Ballona, mosapride citrate)
Mosapride
[name of drug]
Generic name: Chinese Mosapride
English Name: Mosapride
Other name: Ballona, mosapride citrate, Garth, Rui Qi, Xinluona, Mosapride Citrate
[clinical application]
Mainly used for functional dyspepsia with heartburn, belching, nausea, vomiting, early satiety, abdominal bloating and other gastrointestinal symptoms; also can be used for gastric dysfunction of gastroesophageal reflux disease, diabetic gastroparesis and gastric resection.
[pharmacology]
1. the pharmacodynamics of this medicine for 4 5- selective serotonin (5-HT4) receptor agonist, can promote the release of acetylcholine, stimulation of the gastrointestinal tract and exert prokinetic effect, so as to improve the functional dyspepsia patients with gastrointestinal symptoms, but does not affect the secretion of gastric acid. The drug has no affinity for dopamine D2 receptors, adrenergic alpha 1 receptors, 5-HT1 and 5-HT2 receptors on the synaptic membrane of brain neurons, so it does not cause extrapyramidal syndromes and cardiovascular adverse effects.
Animal experiments showed that this drug and promote gastric emptying function rather than cisapride, metoclopramide; gastric emptying function duration and dose of cisapride, than metoclopramide long. This medicine on colon affinity than other gastrointestinal sites, while the effect of cisapride on gastrointestinal tract of all parts of the similar.
2., the pharmacokinetics of oral absorption rapidly, in the gastrointestinal tract and liver, kidney, local tissue concentration higher, followed by plasma, the brain almost no distribution. Healthy subjects taking the drug 5mg, blood concentration peak time (Tmax) for 0.8 hours, the peak plasma concentration (Cmax) of 30.7ng/mL, the half-life of 2 hours, the area under the curve (AUC) was 67 (NG, H) /mL, the apparent volume of distribution (Vd) of 3.5L/kg, plasma protein with the rate of 99%, the total removal rate of 80L/h. The medicine in the l
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