There are many classes of antihypertensive drugs of which six (ACE inhibitors, ARBs, renin inhibitors, calcium channel blockers, diuretics, and beta-blockers) are suitable for initial therapy based on efficacy and tolerability. A number of considerations enter into the selection of the initial regimen for a given patient. These include the weight of evidence for beneficial effects on clinical outcomes, the safety and tolerability of the drug, its cost, demographic differences in response, concomitant medical conditions, and lifestyle issues. The specific classes of antihypertensive medications are discussed below, and guidelines for the choice of initial medications are offered.
A. Angiotensin-Converting Enzyme Inhibitors
ACE inhibitors are commonly used as the initial medication in mild to moderate hypertension (Table 11–6). Their primary mode of action is inhibition of the RAAS, but they also inhibit bradykinin degradation, stimulate the synthesis of vasodilating prostaglandins, and can reduce sympathetic nervous system activity. These latter actions may explain why they exhibit some effect even in patients with low plasma renin activity. ACE inhibitors appear to be more effective in younger white patients. They are relatively less effective in blacks and older persons and in predominantly systolic hypertension. Although as single therapy they achieve adequate antihypertensive control in only about 40–50% of patients, the combination of an ACE inhibitor and a diuretic or calcium channel blocker is potent.
Table 11–6.Antihypertensive drugs: renin and ACE inhibitors and angiotensin II receptor blockers. |Favorite Table|Download (.pdf) Table 11–6. Antihypertensive drugs: renin and ACE inhibitors and angiotensin II receptor blockers.
|Drug ||Proprietary Name ||Initial Oral Dosage ||Dosage Range ||Cost per Unit ||Cost of 30 Days of Treatment (Average Dosage)1 ||Adverse Effects ||Comments |
|Renin Inhibitors |
|Aliskiren ||Tekturna ||150 mg once daily ||150–300 mg once daily ||$8.31/150 mg ||$249.36 || |
Angioedema, hypotension, hyperkalemia.
Contraindicated in pregnancy.
|Probably metabolized by CYP3A4. Absorption is inhibited by high-fat meal. |
|Aliskiren and HCTZ ||Tekturna HCT ||150 mg/12.5 mg once daily ||150 mg/12.5 mg–300 mg/25 mg once daily ||$8.31/150 mg/12.5 mg ||$249.36 || || |
|ACE Inhibitors |
|Benazepril ||Lotensin ||10 mg once daily ||5–40 mg in 1 or 2 doses ||$1.05/20 mg ||$31.50 ||Cough, hypotension, dizziness, kidney dysfunction, hyperkalemia, angioedema; taste alteration and rash (may be more frequent with captopril); rarely, proteinuria, blood dyscrasia. Contraindicated in pregnancy. ||More fosinopril is excreted by the liver in patients with kidney dysfunction (dose reduction may or may not be necessary). Captopril and lisinopril are active without metabolism. Captopril, enalapril, lisinopril, and quinapril are approved for heart failure. |
|Benazepril and HCTZ ||Lotensin HCT ||5 mg/6.25 mg once daily ||5 mg/6.25 mg–20 mg/25 mg ||$2.07/any dose ||$62.10 |
|Benazepril and amlodipine ||Lotrel ||10 mg/2.5 mg once daily ||10 mg/2.5 mg–40 mg/10 mg ||$3.32/20 mg/10 mg ||$99.60 |
|Captopril ||Capoten ||25 mg twice daily ||50–450 mg in 2 or 3 doses ||$1.36/25 mg ||$81.60 |
|Captopril and HCTZ ||Capozide ||25 mg/15 mg twice daily ||25 mg/15 mg–50 mg/25 mg ||$2.85/25 mg/15 mg ||$171.00 |