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Clinical pharmacy 2024/2025 Level 3 Pharm D Pharmacology 1 (PO 502)

3- ACEIs (Angiotensin converting enzyme –Inhibitors)

ex: Enalapril & lisinopril

➢ recommended when preferred first line agent (diuretics, β-blocker) are C.I or ineffective

or if there are compelling MOA reasons to use them such as D.M.
1. ↓ peripheral resistance without affects COP or contractility

2. Block the ACE that:
Actions
(affect blood a) convert angiotensin I into potent vasoconstrictor Angiotensin II
vessels) b) Breakdown of bradykinin:
• Potent inflammatory mediators involved in dry non-reproductive cough
• ↑ production of Both N.O & prostacyclin are potent V. D

1) Inhibition conversion of angiotensin I to angiotensin II
Mechanism 2) Formation of N.O (nitric oxide)

3) Formation of prostacyclin
1. Alone ➔Most effective in hypertensive patients who are white and
young
Effectiveness 2. In heart disease to ↓ Heart load

3. In combination with diuretics ➔ effectiveness is similar in white &
black patients with hypertension.

1. Vasodilation of both arterioles and venous occurs as result of the
combined effect of
• lowering vasoconstriction by decreasing level of angiotensin II &
• potent vasodilation effect of bradykinin
Effect on Arterioles ➔ Afterload Venous ➔preload.
heart
 ACEIs ➔↓ preload and Afterload ➔ ↓ cardiac work.
2. Reducing circulating Angiotensin II ➔↓ secretion of Aldosterone
+
➔Na & water retention (Intrinsic Natriuretic effect) ➔ no need
for diuretic combination (except in black patient)
1- Dry non-reproductive cough ➔ due to bradykinin in pulmonary tree ➔

10% of patients stop the therapy
2- Angioedema (excess swelling in body and tongue like anaphylactic

shock) is rare, but potential life-threatening reaction and may also be
due to high level of bradykinin
S/E 3- 1 dose syncope (sever hypotension in first time of administration) ➔
st
under supervision when taken 1st time
4- Reversible renal failure can occur in patients with severe bilateral real
artery stenosis. (Creatinine Clearance increase)
5- Fetotoxicity
6- K level must be monitored
+

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