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ACE inhibitors

Angiotensin-converting-enzyme inhibitor
Drug class
Captopril skeletal.svg
Captopril, the first synthetic ACE inhibitor
Class identifiers
Use Hypertension
ATC code C09A
Biological target Angiotensin-converting enzyme
Clinical data
Drugs.com Drug Classes
Consumer Reports Best Buy Drugs
WebMD MedicineNet  RxList
External links
MeSH D000806

An angiotensin-converting-enzyme inhibitor (ACE inhibitor) is a pharmaceutical drug used primarily for the treatment of hypertension (elevated blood pressure) and congestive heart failure.

This group of drugs causes relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart. They inhibit the angiotensin-converting enzyme, an important component of the renin–angiotensin system.

Frequently prescribed ACE inhibitors include zofenopril, perindopril, trandolapril, captopril, enalapril, lisinopril, and ramipril.

ACE inhibitors were initially approved for the treatment of hypertension and can be used alone or in combination with other antihypertensive medications. Later, they were found useful for other cardiovascular and kidney diseases including:

In treating heart disease, ACE inhibitors are usually used with other medications. A typical treatment plan often includes an ACE inhibitor, a beta blocker, a long-acting nitrate, and a calcium channel blocker, in combinations that are adjusted to the individual patient's needs. There are fixed-dose combination drugs, such as ACE inhibitor and thiazide combinations.

ACE inhibitors have also been used in chronic kidney failure and kidney involvement in systemic sclerosis (hardening of tissues, as scleroderma renal crisis).


ACE inhibitors dosages for hypertension
Dosage
Note: bid = two times a day, tid = three times a day, d = daily
Drug dosages from Drug Lookup, Epocrates Online.
Name Equivalent daily dose Start Usual Maximum
Benazepril 10 mg 10 mg 20–40 mg 80 mg
Captopril 50 mg (25 mg bid) 12.5–25 mg bid-tid 25–50 mg bid-tid 450 mg/d
Enalapril 5 mg 5 mg 10–40 mg 40 mg
Fosinopril 10 mg 10 mg 20–40 mg 80 mg
Lisinopril 10 mg 10 mg 10–40 mg 80 mg
Moexipril 7.5 mg 7.5 mg 7.5–30 mg 30 mg
Perindopril 4 mg 4 mg 4–8 mg 16 mg
Quinapril 10 mg 10 mg 20–80 mg 80 mg
Ramipril 2.5 mg 2.5 mg 2.5–20 mg 20 mg
Trandolapril 2 mg 1 mg 2–4 mg 8 mg

  • Vasoconstriction (narrowing of blood vessels) and vascular smooth muscle hypertrophy (enlargement) induced by AII may lead to increased blood pressure and hypertension. Further, constriction of the efferent arterioles of the kidney leads to increased perfusion pressure in the glomeruli.
  • It contributes to ventricular remodeling and ventricular hypertrophy of the heart through stimulation of the proto-oncogenes c-fos, c-jun, c-myc, transforming growth factor beta (TGF-B), through fibrogenesis and apoptosis (programmed cell death).
  • Stimulation by AII of the adrenal cortex to release aldosterone, a hormone that acts on kidney tubules, causes sodium and chloride ions retention and potassium excretion. Sodium is a "water-holding" ion, so water is also retained, which leads to increased blood volume, hence an increase in blood pressure.
  • Stimulation of the posterior pituitary to release vasopressin (antidiuretic hormone, ADH) also acts on the kidneys to increase water retention. If ADH production is excessive in heart failure, Na+ level in the plasma may fall (hyponatremia), and this is a sign of increased risk of death in heart failure patients.
  • A decrease renal protein kinase C
  • Previous angioedema associated with ACE inhibitor therapy
  • Hypersensitivity to ACE inhibitors
  • Fosinopril (Fositen/Monopril) is the only member of this group
  • Casokinins and lactokinins, breakdown products of casein and whey, occur naturally after ingestion of milk products, especially cultured milk. Their role in blood pressure control is uncertain.
  • The lactotripeptides Val-Pro-Pro and Ile-Pro-Pro produced by the probiotic Lactobacillus helveticus or derived from casein have been shown to have ACE-inhibiting and antihypertensive functions.
  • A comprehensive resource on anti-hypertensive peptides is available in form of a database. It contains around 1700 unique antihypertensive peptides
  • Arfalasin (HOE 409) is angiotensin antagonist. U.S. Patent 4,013,791
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Wikipedia

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