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Goodman & Gilman's The Pharmacological Basis of Therapeutics, 11e
| V. Drugs Affecting Renal and Cardiovascular Function > |
Inhibitors of the Renin–Angiotensin System
Sections: Inhibitors of
the Renin–Angiotensin System, Angiotensin
Converting Enzyme (ACE) Inhibitors, History, Pharmacological
Effects in Normal Laboratory Animals and Human Beings, Clinical Pharmacology, Captopril (capoten)
, Enalapril (vasotec), Enalaprilat (vasotec injection)
, Lisinopril (prinivil, zestril)
, Benazepril (lotensin)
, Fosinopril (monopril)
, Trandolapril (mavik)
, Quinapril (accupril)
, Ramipril (altace)
, Moexipril (univasc)
, Perindopril (aceon)
, Therapeutic
Uses of ACE Inhibitors and Clinical Summary, ACE Inhibitors in Hypertension , ACE Inhibitors in Left Ventricular Systolic
Dysfunction , ACE Inhibitors in Acute Myocardial Infarction
, ACE Inhibitors in Patients Who Are at High
Risk of Cardiovascular Events
, ACE Inhibitors in Chronic Renal Failure
, ACE Inhibitors in Scleroderma Renal Crisis
, Adverse Effects
of ACE Inhibitors, Hypotension
, Cough
, Hyperkalemia
, Acute Renal Failure
, Fetopathic Potential
, Skin Rash
, Proteinuria
, Angioedema
, Dysgeusia
, Neutropenia
, Glycosuria
, Hepatotoxicity
, Drug Interactions
.
Topics Discussed: angioedema; angiotensin-converting enzyme inhibitors; benazepril; captopril; cough; dysgeusia; enalapril; enalaprilat; exanthema; fosinopril; glycosuria; hydralazine; hyperkalemia; hypertension; hypotension; kidney failure, chronic; left ventricular systolic dysfunction; lisinopril; moexipril; myocardial infarction, acute; neutropenia; perindopril; proteinuria; quinapril; ramipril; renal failure, acute; renin-angiotensin system; renin-angiotensin system inhibition; scleroderma renal crisis; toxic responses of the liver; trandolapril.
Excerpt:
"Angiotensin II itself has limited therapeutic utility and is
not available for therapeutic use in the United States. Instead,
clinical interest focuses on inhibitors of the renin–angiotensin
system.In the 1960s, Ferreira and colleagues found that the
venoms of pit vipers contain factors that intensify responses to
bradykinin. These bradykinin-potentiating factors proved to be a
family of peptides that inhibit kininase II, an enzyme that inactivates
bradykinin. Erdös and coworkers established that ACE and
kininase II are the same enzyme, which catalyzes both the synthesis
of angiotensin II, a potent pressor substance, and the destruction
of bradykinin, a potent vasodilator.Captopril, the first ACE inhibitor to be marketed, is a potent
ACE inhibitor with a Ki of
1.7 nM. It is the only ACE inhibitor
approved for use in the United States that contains a sulfhydryl
moiety. Given orally, captopril is absorbed rapidly and has a bioavailability
of about 75%. Peak concentrations in plasma occur
within an hour, and the drug is cleared rapidly with a half-life
of approximately 2 hours. Most of the drug is eliminated in urine,
40% to 50%..."
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