RESUMO
Neurokinin I receptor antagonist (NK1RA) fosaprepitant is a new antiemetic drug. Fosaprepitant dimeglumine was ap-proved by FDA in January 2008, while it is still in the approval stage in China. Fosaprepitant, as a prodrug of aprepitant, is rapidly converted to aprepitant after intravenous administration in vivo. The indication of fosaprepitant is the prevention of chemotherapy in-duced nausea and vomiting ( CINV) , especially the delayed CINV. Fosaprepitant as a unique intravenous preparation overcomes the drawbacks of aprepitant with oral administration only. Its bioavailability is not affected by the vomiting of patients. It is also suitable for patients with oral mucositis, who are unfavorable for oral medication. The action mechanisms, pharmacokinetics, and clinical trials of fosaprepitant were reviewed in the paper.
RESUMO
We described here blood acetate levels in aldehyde dehydrogenase 2 knockout (ALDH2 KO) male mice based on C57BL/6J strain after ethanol (EtOH) dosing (2 g/kg). Blood samples were collected at 30, 60, 90, 120 180, and 240 min after decapitation, and then EtOH, acetaldehyde (AcH) and acetate were determined by head-space gas chromatography. We found that blood acetate levels in ALDH2 KO mice were slightly lower than those in wild type (WT), whereas EtOH and AcH levels in ALDH2 KO were significantly higher than those in WT. These observations indicate that high EtOH, AcH and low acetate in the blood of ALDH2 KO are due to the deficient effect of ALDH2 enzyme activity.
