Pharmacological effects of Aprepitant

  • Author:Kathy
  • Release on :2016-05-19

1. The product Aprepitant is in 2003, the FDA approved the first neural excitation peptide 1 (NK 1) receptor blockers, with NK 1 receptor (primary central nervous system and peripheral) to block the effect of substance P. This product can be through the blood brain barrier, occupation of NK 1 receptor in the brain, with high selectivity and affinity, and the NK - 2 and NK - 3 receptor affinity is very low. At the same time, this product for other used in the treatment of chemotherapy induced nausea and vomiting symptoms of drug targets (such as dopamine receptor, 5 - HT receptor) affinity function is low, its reduce nausea and vomiting is better than other drugs.

2. This product with serotonin (5 - HT) 3 receptor blockers and dexamethasone treatment of serious cause vomiting symptoms caused by chemotherapy of standard method, can improve chemotherapy induced acute and delayed complete response rate of nausea and vomiting.

3. This product plasma protein combined rate of 95%, the steady state when the average apparent volume of distribution (V) is 70 L, and can be through the placenta of rats and rabbits, and the blood brain barrier.


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