Enalapril is an anti-hypertension "prodrug" (i.e, a drug precursor) that is inactive until the ethyl ester (arrow in figure) is hydrolyzed by esterases present in blood plasma. The active drug is the dicarboxylic acid ("enalaprilat") that results from this hydrolysis reaction. (a) Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but enalaprilat does not? EtOOC -NH CH3 HOOC Enalapril (b) Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide angiotensin. ACE has a KM = 12 µM for angiotensin, which is present in plasma at a concentration of 75 µM. When enalaprilat is present at 2.4 nM, the activity of ACE in plasma is 10% of its uninhib- ited activity. What is the value of K; for enalaprilat?
Enalapril is an anti-hypertension "prodrug" (i.e, a drug precursor) that is inactive until the ethyl ester (arrow in figure) is hydrolyzed by esterases present in blood plasma. The active drug is the dicarboxylic acid ("enalaprilat") that results from this hydrolysis reaction. (a) Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but enalaprilat does not? EtOOC -NH CH3 HOOC Enalapril (b) Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide angiotensin. ACE has a KM = 12 µM for angiotensin, which is present in plasma at a concentration of 75 µM. When enalaprilat is present at 2.4 nM, the activity of ACE in plasma is 10% of its uninhib- ited activity. What is the value of K; for enalaprilat?
Chapter9: Parenteral Medication Labels And Dosage Calculation
Section: Chapter Questions
Problem 6.4P
Related questions
Question
Expert Solution
This question has been solved!
Explore an expertly crafted, step-by-step solution for a thorough understanding of key concepts.
This is a popular solution!
Trending now
This is a popular solution!
Step by step
Solved in 2 steps
Recommended textbooks for you