Bioavailability and Elimination Half-Life
A 2015 systematic comparison of all clinically used angiotensin-converting enzyme (ACE) inhibitors found that most ACE inhibitors are rapidly absorbed with maximum bioavailability being reached within 30 minutes to six hours, depending on the specific ACE inhibitor and dose.1 Elimination half-life ranges from about two to 24 hours.
|
ACE Inhibitor
|
tmax
h
|
t1/2
h
|
|
Benazepril/Benazeprilat
|
0.5/1.5
|
10
|
|
Captopril
|
1-1.5
|
<2
|
|
Enalapril/Enalaprilat
|
1/3-4
|
11
|
|
Fosinopril/Fosinoprilat
|
2.8
|
11
|
|
Lisinopril
|
7
|
13
|
|
Moexipril/Moexiprilat
|
1/1.5
|
2-9
|
|
Perindopril/Perindoprilat
|
2/2.4
|
10
|
|
Quinapril
|
0.63
|
2
|
|
Ramipril/Ramiprilat
|
0.7/2.1
|
17
|
|
Trandolapril/Trandolaprilat
|
0.5/6
|
24
|
Table 1: ACE inhibitor maximum bioavailability and elimination half-life1
Time to Maximal Effect
Most of the antihypertensive effects of benazepril and quinapril occur within the first one to two weeks of dosing.2,3
Some ACE inhibitors may take several weeks of treatment to reach maximal blood pressure response, including captopril, enalapril, fosinopril, lisinopril, perindopril, and rampipril.4-9
The antihypertensive effects of moexipril reach maximal reduction after four weeks.10
The maximum reduction of blood pressure was reached within one week for all doses of trandolapril.11
The antihypertensive effect of all ACE inhibitors has been shown to continue during long-term therapy for at least two years.2-11
References
- Regulski M, Regulska K, Stanisz BJ, et al. Chemistry and pharmacology of angiotensin-converting enzyme inhibitors. Curr Pharm Des 2015; 21 (13): 1764-1775.
- Accupril [package insert]. New York, NY: Parke Davis, Pfizer; 2017.
- Lotensin [package insert]. Parsippany, NJ: Validus Pharmaceuticals LLC; 2014.
- Capoten [package insert]. Spring Valley, NY: Par Pharmaceutical Companies, Inc.; 2012.
- Vasotec [package insert]. Bridgewater, NJ: Valeant Pharmaceuticals North America LLC; 2015.
- Altace [package insert]. New York, NY: Pfizer Laboratories; 2017.
- Aceon [package insert]. North Chicago, IL: Abbot Laboratories; 2011.
- Fosinopril sodium [package insert]. Miami, FL: Ciplo USA Inc; 2015.
- Prinivil [package insert]. Whitehouse Station, NJ: Merck Sharp & Dohme Corp.; 2016.
- Moexipril hydrochloride [package insert]. Teva Pharmaceuticals USA Inc; 2016.
- Trandolapril [package insert]. Laurelton, NY: Epic Pharma, LLC; 2017.
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