Cardiovascular Medicine Book

Congestive Heart Failure

Coronary Artery Disease

Electrocardiogram

Examination

Hyperlipidemia

Hypertension

Miscellaneous

Pericardial Disorders

Obstetrics Chapter related topics

http://www.fpnotebook.com/

ACE InhibitorAka: Angiotensin Converting Enzyme Inhibitor, Accupril, Ramipril, Captopril, Altace, Trandopril, Mavik, Capoten, Lisinopril, Prinivil, Zestril, Monopril, Enalapril, Vasotec, Fosinopril, Benzapril, Lotensin, Moexipril, Univasc, Perindopril, Aceon, Quinapril

Advertisement

  1. See Also
    1. Angiotensin Receptor Blocker
  2. Contraindications
    1. Absolute Contraindications
      1. Angioneurotic edema: even if not due to ACE inhibitor
      2. Pregnancy
      3. Renal Artery Stenosis
      4. ACE Inhibitor related Allergic Reaction
    2. Relative Contraindications
      1. Aortic Stenosis
      2. Hypertrophic Cardiomyopathy
  3. Indications
    1. Hypertension
      1. Useless in low renin patients (esp. Black ethnicity)
      2. Low renin patients respond better to Diuretics
    2. Myocardial Infarction
      1. Early ACE inhibitor in acute Myocardial Infarction
        1. Started within 24 hours of Anterior MI
        2. Significant reduction in CHF and death
        3. Significantly lower mortality at 1 year
      2. Reference
        1. Ambrosioni (1995) N Engl J Med 332:80
        2. Stenestrand (2001) JAMA 285:430
    3. Congestive Heart Failure
      1. Left ventricle Systolic Dysfunction
    4. Diabetic Nephropathy
    5. Renal insufficiency
  4. Mechanism
    1. Renin-Angiotensin System
  5. Preparations (Choose once daily dosing if possible)
    1. Captopril (Capoten)
      1. Hypertension: 25 mg PO bid-tid (maximum 450 mg/day)
      2. CHF: 6.25 - 12.5 mg PO tid (maximum 450 mg/day)
    2. Enalapril (Vasotec)
      1. Hypertension: 5 mg PO qd (maximum 40 mg/day)
      2. CHF: 2.5 mg PO qd-bid (maximum 40 mg/day)
      3. IV: 1.25 mg IV q6h
    3. Lisinopril (Prinivil, Zestril)
      1. Hypertension: 10 mg PO qd (target 20-40 mg/day)
      2. CHF: 5 mg PO qd (target 20 mg/day)
      3. Acute MI: 5 mg PO qd for 2 days then 10 mg qd
      4. Maximum 40 mg/day
    4. Fosinopril (Monopril)
      1. Hypertension: 10 mg PO qd (target 40 mg/day)
      2. CHF: 10 mg PO qd (target 20-40 mg/day)
      3. Maximum: 80 mg/day
    5. Benzapril (Lotensin)
      1. Hypertension: 10 mg PO qd (target 20-40 mg/day)
      2. Maximum: 80 mg/day
    6. Moexipril (Univasc): Take one hour before meals
      1. Hypertension: 7.5 mg PO qd (maximum 30 mg/day)
    7. Perindopril (Aceon)
      1. Hypertension: 4 mg PO qd (target 4-8 mg/day)
      2. Maximum 16 mg/day
    8. Quinapril (Accupril)
      1. Hypertension: 10 mg PO qd (target 20-40 mg/day)
      2. CHF: 5 mg PO bid, titrating weekly to 20-40 mg/day
      3. Maximum: 80 mg/day
    9. Ramipril (Altace)
      1. Hypertension: 2.5 mg PO qd (target 2.5-20 mg qd)
      2. CHF: 2.5 mg PO bid (target 5 mg bid)
      3. Maximum 20 mg/day
    10. Trandopril (Mavik)
      1. Hypertension: 1 mg PO qd (target 2 to 4 mg qd)
      2. CHF: 1 mg PO qd (target 4 mg qd)
      3. Maximum: 8 mg/day
  6. Adverse Effects
    1. Cough (dry and irritating)
      1. Characteristics
        1. Occurs in 5 to 20% of patients
          1. More common in women
          2. More common in black patients
        2. Not dose related
        3. Stops within 4 days of medication cessation
      2. Alternative medications
        1. Angiotensin Receptor Blocker (e.g. Losartan)
      3. Inhalers may relieve cough
        1. Tilade 2 puffs inhaled qid
        2. Cromolyn 20 mg inhaled qid
    2. Hyperkalemia (5% of patients)
      1. See Drug Interactions below
      2. Asociated with renal insufficiency, Diabetes Mellitus
    3. Teratogenicity in second or third trimester
      1. Fetal injury or death
      2. Pregnancy Class C if discontinued in first trimester
    4. Renal Insufficiency
      1. Renal Artery Stenosis (see monitoring below)
      2. No Creatinine level is absolute contraindication
      3. Baseline Serum Creatinine <3.0 mg/dl is safe
    5. Hypotension
      1. Restart ACE Inhibitor at half prior dose
      2. Decrease or hold dose of any concurrent Diuretic
    6. Rare Adverse Reactions
      1. Angioedema
      2. Rash
      3. Agranulocytosis
      4. Neutropenia
        1. Associated with comorbid renal insufficiency
        2. Associated with comorbid collagen vascular disease
  7. Drug Interactions
    1. Increases Lithium levels (follow levels)
    2. Decreased ACE Inhibitor levels with concurrent antacids
    3. Decreased Renal Function with concurrent NSAID use
    4. Agents predisposing to Hyperkalemia
      1. Bactrim
      2. Potassium supplements or salt substitute
      3. Beta Blockers
      4. NSAIDs
      5. Potassium sparing Diuretics
        1. Triamterene
        2. Spironolactone
  8. Monitoring
    1. Serum Potassium (if patient at risk)
    2. Serum Creatinine
      1. Timing
        1. Baseline
        2. Recheck in 4 days to 2 weeks
      2. Expect an increase in Chronic Kidney Disease
        1. Despite this, renal protective effect outweighs mild to moderate Creatinine increase
      3. Indication to consider stopping ACE Inhibitor
        1. Serum Creatinine increased >20% in 4 days
      4. Additional precautions when increasing dose
        1. Serum Creatinine should not increase >30%
  9. References
    1. (1987) N Engl J Med 316(23):1429
    2. Bicket (2002) Am Fam Physician 66(3):461
    3. Pfeffer (1992) N Engl J Med 327(10):669
    4. Yeun (2001) Postgrad Med 110(5):39

Angiotensin-Converting Enzyme Inhibitors (C0003015)

Definition (MSH)A class of drugs whose main indications are the treatment of hypertension and heart failure. They exert their hemodynamic effect mainly by inhibiting the renin-angiotensin system. They also modulate sympathetic nervous system activity and increase prostaglandin synthesis. They cause mainly vasodilation and mild natriuresis without affecting heart rate and contractility.
Definition (CSP)class of antihypertensive agents which act by inhibiting the proteolytic activation of angiotensin.
Definition (NCI)A class of agents that target at angiotensin-converting enzyme (ACE), which catalyzes conversion of angiotensin I to angiotensin II. As a result these inhibitors cause vasodilation and mild natriuresis. In addition, ACE inhibitors induce prostaglandin synthesis, which also plays a role in their antihypertensive effects.
ConceptsPharmacologic Substance (T121)
EnglishACE INHIB, ACE inhibitor, ACE Inhibitors, ANGIOTENSIN CONVERTING ENZYME ANTAG, Angiotensin Converting Enzyme Antagonists, angiotensin converting enzyme inhibitor, Angiotensin Converting Enzyme Inhibitors, ANGIOTENSIN I CONVERTING ENZYME INHIB, Angiotensin I Converting Enzyme Inhibitors, ANTAG ANGIOTENSIN CONVERTING ENZYME, ANTAG KININASE II, INHIB ACE, INHIB ANGIOTENSIN CONVERTING ENZYME, INHIB KININASE II, KININASE II ANTAG, Kininase II Antagonists, KININASE II INHIB, Kininase II Inhibitors
Spanishagente inhibidor de la enzima convertidora de angiotensina, droga inhibidora de la enzima convertidora de angiotensina, IECA, inhibidor de la convertasa, inhibidor de la ECA
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Captopril (C0006938)

Definition (MSH)A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.
Definition (CSP)potent and specific inhibitor of peptidyl dipeptidase A; it acts to suppress the renin-angiotensin system and inhibits blood pressure responses to exogenous angiotensin.
Definition (NCI)A drug used to lower high blood pressure. It belongs to the family of drugs called ACE inhibitors.
Definition (PDQ)A sulfhydryl-containing analog of proline with antihypertensive activity and potential antineoplastic activity. Captopril competitively inhibits angiotensin converting enzyme (ACE), thereby decreasing levels of angiotensin II, increasing plasma renin activity, and decreasing aldosterone secretion. This agent may also inhibit tumor angiogenesis by inhibiting endothelial cell matrix metalloproteinases (MMPs) and endothelial cell migration. Captopril may also exhibit antineoplastic activity independent of effects on tumor angiogenesis. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=37824&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=37824&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C340" NCI Thesaurus)
Definition (NCI)A sulfhydryl-containing analog of proline with antihypertensive activity and potential antineoplastic activity. Captopril competitively inhibits angiotensin converting enzyme (ACE), thereby decreasing levels of angiotensin II, increasing plasma renin activity, and decreasing aldosterone secretion. This agent may also inhibit tumor angiogenesis by inhibiting endothelial cell matrix metalloproteinases (MMPs) and endothelial cell migration. Captopril may also exhibit antineoplastic activity independent of effects on tumor angiogenesis. (NCI04)
ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishCaptopril, CAPTOPRIL PREPARATION, CPT
Spanishcaptopril, captoprilo
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Enalapril (C0014025)

Definition (MSH)One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS that is used to treat hypertension.
Definition (CSP)1-carboxy-3-phenylpropyl-L-alanyl- L-proline (as 1'-ethyl ester, maleate 1:1), is an ACE inhibitor used as an antihypertensive.
Definition (NCI)A dicarbocyl-containing peptide and angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, enalapril is converted by de-esterification into its active form enalaprilat. Enalaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Enalapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.
Definition (NCI)An antihypertensive agent that can also be used to slow or prevent the progression of heart disease in people with childhood cancer treated with drugs that may be harmful to the heart.
ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishEnalapril, ENALAPRIL PREPARATION
Spanishenalapril, enalaprilo
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Lisinopril (C0065374)

Definition (MSH)One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.
Definition (CSP)lysine derivative of the active form of enalapril; an angiotensin converting enzyme inhibitor used in the treatment of hypertension.
Definition (NCI)A synthetic peptide derivate and long-acting angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Lisinopril specifically and competitively inhibits angiotensin-converting enzyme thereby decreasing the formation of the potent vasoconstrictor angiotensin II. This leads to a diminished vasopressor activity. In addition, angiotensin II-stimulated aldosterone secretion by adrenal cortex is decreased which results in a decrease of sodium and water retention and an increase of serum potassium.
ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishLisinopril, LISINOPRIL PREPARATION, Lysinopril
Spanishlisinopril, lisinoprilo
CreditsDerived from the NIH UMLS (Unified Medical Language System)


moexipril (C0066685)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishmoexipril, MOEXIPRIL PREPARATION
Spanishmoexipril, moexiprilo
CreditsDerived from the NIH UMLS (Unified Medical Language System)


quinapril (C0072857)

Definition (NCI)A prodrug and non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Quinapril is hydrolized into its active form quinaprilat, which binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This abolishes the potent vasoconstrictive actions of angiotensin II and leads to vasodilatation. Quinapril also causes a decrease in angiotensin II-induced aldosterone secretion by the adrenal cortex, thereby promoting diuresis and natriuresis, and increases bradykinin levels.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishquinapril, QUINAPRIL PREPARATION
Spanishquinapril, quinaprilo
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Ramipril (C0072973)

Definition (MSH)A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.
Definition (NCI)A prodrug and nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Ramipril is converted in the liver by de-esterification into its active form ramiprilat, which inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This abolishes the potent vasoconstrictive actions of angiotensin II and leads to vasodilatation. This agent also causes an increase in bradykinin levels and a decrease in angiotensin II-induced aldosterone secretion by the adrenal cortex, thereby promoting diuresis and natriuresis.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishRamipril, RAMIPRIL PREPARATION
Spanishramipril, ramiprilo
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Fosinopril (C0118168)

Definition (MSH)A phosphinic acid-containing angiotensin-converting enzyme inhibitor that is effective in the treatment of hypertension. It is a prodrug that is converted to its active metabolite fosinoprilat.
Definition (NCI)A phosphinic acid-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As an ester prodrug, fosinopril is hydrolysed by esterases to its active metabolite fosinoprilat. Fosinoprilat specifically and competitively inhibits angiotensin-converting enzyme thereby decreasing the formation of the potent vasoconstrictor angiotensin II, resulting in diminished vasopressor activity. In addition, angiotensin II-mediated aldosterone secretion by adrenal cortex is decreased, which results in a decrease of sodium retention and an increase in water outflow.
ConceptsOrganophosphorus Compound (T115) , Pharmacologic Substance (T121)
EnglishFosenopril, Fosinopril, FOSINOPRIL PREPARATION
Spanishfosinopril, fosinoprilo
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Perindopril (C0136123)

Definition (MSH)An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishPerindopril, PERINDOPRIL PREPARATION, Pirindopril
Spanishperindopril, perindoprilo
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Accupril (C0244580)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAccupril
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Capoten (C0591224)

ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishCapoten
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Zestril (C0678140)

ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishZestril
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Prinivil (C0701176)

ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishPrinivil
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Lotensin (C0721436)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishCibacène, Cibacen, Lotensin, Novartis brand of benazepril hydrochloride
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Mavik (C0721596)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAbbott brand of trandolapril, Gopten, Knoll brand of trandolapril, Mavik
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Univasc (C0724125)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishMoex, Perdix, Schwarz brand of moexipril hydrochloride, Univasc
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Vasotec (C0728763)

ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishBiovail Brand of Enalaprilat Anhydrous, Merck Frosst Brand of Enalaprilat Anhydrous, Vasotec
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Monopril (C0728957)

ConceptsOrganophosphorus Compound (T115) , Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
EnglishBristol Myers Squibb Brand of Fosinopril Sodium, Fosinorm, Monopril, Newace, Staril
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Aceon (C0875950)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAceon
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Altace (C0878061)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAcovil, Altace, Astra Brand of Ramipril, Aventis Brand of Ramipril, Aventis Pharma Brand of Ramipril, Delix, Hoechst Brand of Ramipril, Monarch Brand of Ramipril, Ramace, Triatec, Tritace, Zabien
CreditsDerived from the NIH UMLS (Unified Medical Language System)



Navigation Tree