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

➢ All adequately but incompletely ➢ Orally ➔ only once-a-day dosing.
absorbed Orally, should be taken on an ➢ Losartan ➔ first approved

empty stomach ➔ Because the presence member of the class, differs from
of food may decrease absorption the others in that it undergoes
➢ All are prodrugs [require activation by extensive first-pass hepatic

hydrolysis via hepatic enzymes]➔
metabolism, including conversion
Pharmacokinetics ➢ Renal elimination ➔ except being to its active metabolite.
Except for captopril
[Other drugs have inactive

metabolites]
Fosinopril (for patients with renal
dysfunction)
➢ Plasma half-lives of active compounds
compounds occur in urine and
vary from 2 to 12 hr. ➔ inhibition of ➢ Elimination of metabolites, parent
feces.
ACE may be much longer.
➢ [ramipril and Fosinopril]➔ only once- ➢ Highly plasma protein bound (>
90%) except for candesartan
a-day dosing. (more patient compliance) (↑↑ volumes of distribution)

Susceptible to Drug-Drug Interaction

1) Single-agent therapy ➔in mild dyspnea
on exertion, do not show signs or

symptoms of volume overload (edema).
 [Patients with the lowest ejection

fraction]➔↑ response to ACE-I
2) in patients with all stages of left

ventricular failure.
Indications digoxin, and aldosterone antagonists.
3) ACE inhibitors + diuretics +, β-blockers,

(In HF, depending on the disease
severity)

4) Long term ACE-inhibitor therapy➔ in
recent myocardial infarction (localized
death in heart ➔ release FR on long term

➔ -ve effect on heart) also benefit from
(Recommended initiated immediately
after myocardial infarction.)

Has antioxidant effect

NOTE

✓ ↑ angiotensin II, aldosterone ➔ direct detrimental effects on the cardiac
muscle ➔remodeling, fibrosis, inflammatory changes

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