Enalapril is an anti-hypertension "prodrug" (i.e, a drug precursor)that is inactive until the ethyl ester (arrow in figure) is hydrolyzed byesterases present in blood plasma. The active drug is the dicarboxylicacid ("enalaprilat") that results from this hydrolysis reaction.(a) Enalapril is administered in pill form, but enalaprilat must beadministered intravenously. Why do you suppose enalapril works asa pill, but enalaprilat does not?EtOOC-NHCH3HOOCEnalapril(b) Enalaprilat is a competitive inhibitor of the angiotensin-convertingenzyme (ACE), which cleaves the blood-pressure regulating peptideangiotensin. ACE has a KM = 12 µM for angiotensin, which ispresent in plasma at a concentration of 75 µM. When enalaprilat ispresent 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?

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Curren'S Math For Meds: Dosages & Sol

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Chapter9: Parenteral Medication Labels And Dosage Calculation

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Enalapril is an anti-hypertension “pro-drug” (i.e., a drug precursor) that isinactive 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? (b) Enalaprilat is a competitive inhibitor of the angiotensin-convertingenzyme (ACE), which cleaves the blood-pressure regulating peptideangiotensin I. ACE has a KM = 52 μM for angiotensin I, which is presentin plasma at a concentration of 75 μM. When enalaprilat is presentat 2.4 nM, the activity of ACE in plasma is 10% of its uninhibitedactivity. What is the value of K1 for enalaprilat?
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A pentapeptide was found to have the composition Ala Arg Gly Pro Trp. Reaction of the pentapeptide with Sanger’s reagent, followed by hydrolysis, gave the DNP derivative of proline. Treatment of the pentapeptide with carboxypeptidase initially produced alanine. Treatment of the pentapeptide with trypsin gave a tetrapeptide which, when treated with chymotrypsin, produced a tripeptide. What is the sequence of the pentapeptide? (note: trypsin cleaves after basic amino acids) *
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