Tìm theo
Azosemide
Các tên gọi khác (1) :
  • 2-chloro-5-(1H-tetrazole-5-yl)-N^4-(2-thenyl)
Thuốc Gốc
Small Molecule
CAS: 27589-33-9
Azosemide is a loop diuretic used to treat hypertension, edema, and ascites [1,2].
Dược Lực Học : Diuretic affects upon oral administration match those of furosemide. However, upon intravenous administration azosemide displays 5.5-8 times greater effect.
Cơ Chế Tác Dụng : Azosemide is a loop diuretic used to treat hypertension, edema, and ascites [1,2]. Exact mechanism of action is unclear. However, it acts primarily on the loop of Henle, in both the medullary and cortical segments of the thick ascending limb. [1]
Dược Động Học :
▧ Absorption :
Peak plasma concentrations are achieved in 3-4 hours when azosemide is administered to healthy humans in a fasting state. There is an absorption lag time of approximately 1 hour. [1] Oral bioavailability estimated to be 20.4% [1]
▧ Volume of Distribution :
Poor affinity for human tissue. Small apparent post-pseudodistribution Vd of 0.262 l/kg. [1]
▧ Protein binding :
> 95% 4% protein binding to 4% human serum albumin at azosemide concentrations of 10-100ug/ml, using equilibrium dialysis. [1]
▧ Metabolism :
Considerable first pass metabolism which makes parentral administration more effective than oral administration. Eleven metabolites of azosemide were found in rats, but only azosemide and its glucuronide were detected in humans. [1]
▧ Route of Elimination :
Total body clearance 112ml/min. Renal clearance 41.6ml/min. Actively secreted in the renal proximal tubule of humans. This may or may not involve a nonspecific organic acid secretory pathway. [1] There is thus a potential for disease states and other organic acids such as NSAIDs which affect the organic acid transport pathway to affect the efficacy of azosemide.
▧ Half Life :
Terminal half life 2-3 hours. [1]
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08961
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