Skip to main content
UploadLanguage (EN)Support
BusinessMobileSocial MediaMarketingTechnologyArt & PhotosCareerDesignEducationPresentations & Public SpeakingGovernment & NonprofitHealthcareInternetLawLeadership & ManagementAutomotiveEngineeringSoftwareRecruiting & HRRetailSalesServicesScienceSmall Business & EntrepreneurshipFoodEnvironmentEconomy & FinanceData & AnalyticsInvestor RelationsSportsSpiritualNews & PoliticsTravelSelf ImprovementReal EstateEntertainment & HumorHealth & MedicineDevices & HardwareLifestyle
Diksha Kumari, profile picture
Uploaded byDiksha Kumari
PPTX, PDF35,487 views

ACE Inhibitors

This presentation discusses angiotensin-converting enzyme (ACE) inhibitors, which are used to treat hypertension and other cardiovascular conditions. It describes the structure and function of ACE, the drug classification of ACE inhibitors based on their zinc-binding groups, and the structure-activity relationships that determine ACE inhibitor potency. Examples of commonly used ACE inhibitors are provided, along with their chemical nature, bioavailability, time to peak action, elimination, dosing, and adverse effects. Clinical uses and drug interactions of ACE inhibitors are also summarized.

Health & Medicine◦
Downloaded 556 times
presentation by- Diksha Kumari 18601911022 B.pharm, 3rd year,6th semester
kininogen kallidin bradikinin Inactive fragments /kinins kallikrein Amino-peptidase (+)
Important structural points- 1. Positive amino group in active site 2. Zinc(2+) ion, 2 amino acids away from cationic center. 3. Hydrophobic centers for stabilizing the incoming substrate 4. Protruding hydrogen’s to stabilize the carbonyl bond of peptide bond next to the labile peptide.
Drug classification(based on groups which interact with zinc ion of ACE- 1. Sulfhydryl group containing drugs Eg. Captopril 2. Dicarboxylate group containing drugs Eg. Enalapril, lisinopril 3. Phosphonate group containing drugs Eg. Fosinopril
Structure activity relationship •The N ring must contain a carboxylic acid to mimic the C-terminal carboxylate of ACE substrate. •Large hydrophobic heterocyclic rings(i.e., the N-ring) increases potency and after pharmacokinetic factors. •The zinc binding groups can be either sulfhydryl(A), a carboxylic acid(B), or a phosphinic acid(C). •X is usually methyl to mimic the side chain of alanine within the di- carboxylate series, when X= n-butyl amine it produces an orally active drug. •Optimum activity occurs when stereochemistry of inhibitor is consistent with L-amino acids stereochemistry present in normal substrate.
captopril enalapril lisinopril fosinopril perindopril ramipril Chemical nature Sulfhydryl Carboxyl Carboxyl Phosphina te Carboxyl carboxyl Activity status Active Prodrug Active Prodrug Prodrug Prodrug Bio- availability( as active form) 70% 50% 25% 30% 20% 60% Time to peak action 1hr 4-6hr 6-8hr 3-5hr 6hr 3-6hr Elimination 2hr 11hr 12hr 12hr 25-30hr 8-48hr Mode of excretion Renal Renal Renal Renal/ hepatic Renal Renal Duration of action 6-12hr 24hr >=24hr 24hr >24hr >24hr Daily dose(mg) 25-150 2.5-40 5-40 10-40 2-8 1.25-10
1-Treatment of hypertension. 2-Treatment of heart failure. 3-Secondry prevention after myocardial infarction. 4-Diabetic nephropathy in insulin-dependent diabetes mellitus. Clinical use- Adverse effects- •Hypotension •Hyperkalamia •Cough •Rashes •Angio-edema •Foetopathic •Headache •Dizziness •Acute renal failure
Drug interactions- • Antacids decrease the bio-availability of ACE inhibitors •With diuretics they cause potential excessive deduction in blood pressure •With NSAIDs they show decreased hypotensive effects •With potassium sparing diuretics they cause hyperkalamia •On administration with iron salts there are reduction in efficacy of the drugs •With allupurinol there is increased risk of hypersensitivity.
Reference- 1) Tripathi K.D,Essentials of medical pharmacology. Sixth edition.480- 87 2)Williams, David A, Lemke, Thomas L. Foyes principles of medicinal chemistry. 6th edition. 739-52