| ACEIs |
|---|
Benazepril
(Lotensin) |
- -
After oral administration, peak plasma concentrations reached within 0.5–1 hr. - -
Effective half-life in adults following multiple dosing 10–12 hr. - -
Cleared predominantly by renal excretion in subjects with normal renal function.
| Treatment of hypertension. May be used alone or in combination with thiazide diuretics. | Initial dose for adults not receiving a diuretic is 10 mg once daily. Usual maintenance range is 20–40 mg per day in a single or two equal doses. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
In patients with renal insufficiency (creatinine clearance ≤30 mL/min/1.73 m²) peak levels and initial half-life increase, time to steady state may be delayed. Recommended initial dose in such patients is 5 mg once daily. Dosage may be titrated upward until BP is controlled or to a maximum total daily dose of 40 mg.
|
Captopril
(Capoten) |
- -
After oral administration, peak plasma concentrations reached in 1 hr. Presence of food reduces absorption by 30–40%. - -
In adults, effective half-life < 3 hr (accurate determination of half-life not possible). - -
In a 24–hr period, 95% of observed dose eliminated in the urine. - -
Reduction of BP maximum at 60–90 minutes after oral administration, duration of effect dose-related. - -
Reduction in BP may be progressive.
|
Treatment of hypertension. Treatment of congestive heart failure. To improve survival following MI in clinically stable patients.
| Should be taken 1 hr before meals, dosage must be individualized. Initial dose is 25 mg twice per day or three times per day. Dosage may be increased to 50 mg twice per day or three times per day. Usual dose range is 25–150 mg twice per day or three times per day. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
Patients with renal impairment: initial daily dose should be reduced, smaller increments should be utilized for titration, and minimal effective dose should be calculated.
|
Enalapril
(Vasotec) |
- -
After oral administration, peak serum concentrations occur within 1 hr. - -
Primarily renal, 94% of dose is recovered in the urine and feces. - -
Effective half-life following multiple doses is 11 hr. - -
With GFR ≤ 30 mL/min, time to peak concentration and steady state delayed.
| Treatment of hypertension. | 10–40 mg per day in a single or two divided doses. Daily dose should not exceed 50 mg. Dosage reduction and/or discontinuation may be required for some patients who develop increases in blood urea and serum creatinine. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. Enalapril has been detected in human breast milk. - -
Dose selection for elderly patients should be cautious, usually starting at the low end of the dosing range.
|
Fosinopril
(Monopril) |
- -
After oral administration, peak concentrations achieved in 3 hr. - -
Terminal elimination half-life is 12 hr. - -
Cleared predominantly by renal excretion in subjects with normal renal function.
|
Treatment of hypertension. May be used alone or with thiazide diuretics. For heart failure as adjunctive therapy when added to conventional therapy, including diuretics with or without digitalis.
| Initial dosage is 10 mg once daily, both as monotherapy and when the drug is added to a diuretic. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
In children, doses between 0.1 and 0.6 mg/kg. For children weighing more than 50 kg, dosage is 5–10 mg once daily. - -
For heart failure patients, an initial dose of 5 mg can be increased over a several-week period but not exceeding 40 mg once daily.
|
Lisinopril
(Prinivil; Zestril) |
- -
Reaches peak serum concentrations within 7 hr. - -
On multiple doses, effective half-life accumulation is 12 hr. - -
Excreted primarily through the kidneys.
|
Treatment of hypertension. As adjunctive therapy in the management of heart failure not responding to diuretics and digitalis. Acute MI – for the treatment of hemodynamically stable patients, to improve survival.
| Initial dose is 10 mg once daily, usual dose range 20–40 mg daily in a single dose. Patients on a diuretic dosage should be adjusted according to BP response, and the diuretic should ideally be discontinued. For patients with creatinine clearance ≤ 10 mL/min, recommended initial dose is 2.5 mg, can be titrated upward up to a maximum of 40 mg daily. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
Dose selection for elderly patients should start at the low end of dosing range.
|
Moexipril
(Univasc) |
- -
Bioavailability of oral drug is 13% compared to IV; markedly affected by food. - -
After oral administration, 7% appears in urine (vs. 40% of IV dose), 52% in feces (vs. 20% of IV dose).
| Treatment of hypertension. | Initial dose in patients not receiving diuretics is 7.5 mg 1 hr prior to meals, once daily. Recommended dose range is 7.5–30 mg daily in one or two divided doses. Diuretic therapy should ideally be discontinued or an initial dose of 3.75 mg should be used with medical supervision. For patients with creatinine clearance ≤ 40 mL/min/1.73 m², the recommended initial dose is 3.75 mg once daily, can be titrated to a maximum daily dose of 15 mg. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
Dosage should be adjusted for populations with decreased renal function, mild to moderate cirrhosis and in elderly patients.
|
Perindopril
(Aceon) |
- -
After oral administration, peak plasma concentrations occur at approximately 1 hr. - -
Mean half-life 0.8–1.0 hr. - -
Clearance almost exclusively renal.
|
Treatment of hypertension. May be used alone or in combination with thiazide diuretics. Stable coronary artery disease: to reduce risk of cardiovascular mortality or nonfatal MI.
| Initial dose is 4 mg once daily. May be titrated upward until BP is controlled to a maximum of 16 mg per day. Usual dose range is 4–8 mg as single daily dose. May be given in two divided doses. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
Dose selection for elderly patients should start at the low end of dosing range. - -
Patients with renal impairment: initial daily dose should be reduced.
|
Quinapril
(Accupril) |
- -
After oral administration, peak plasma concentrations reached within 1 hr. - -
After multiple oral dosing, effective half-life within 2 hr. - -
Cleared predominantly by renal excretion in subjects with normal renal function.
|
Treatment of hypertension. May be used alone or with thiazide diuretics. Management of heart failure as adjunctive therapy when added to conventional therapy, including diuretics and/or digitalis.
| Initial dosage for patients not on diuretics is 10–20 mg once daily. Dosage adjusted according to BP measured at peak and trough. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
Patients with renal impairment and heart failure: initial daily dose should be reduced. - -
Recommended dosage for elderly patients is 10 mg once daily followed by titration to the optimal response.
|
Ramipril
(Altace) |
- -
After oral administration, peak plasma concentrations reached within 1 hr. - -
Cleared predominantly by renal excretion in subjects with normal renal function.
|
Treatment of hypertension. May be used alone or in combination with thiazide diuretics. Reduction in risk of MI, stroke, and death from cardiovascular causes for patients 55 years or older at high cardiovascular risk.
| Initial dose for patients not receiving a diuretic is 2.5 mg once daily. Dosage adjustment according to BP response. Usual maintenance dosage is 2.5–20 mg once daily in a single dose or divided equally into two doses. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
Patients with renal impairment: initial daily dose should be reduced, smaller increments should be utilized for titration and minimal effective dose should be calculated.
|
Trandolapril
(Mavik) |
- -
After oral administration under fasting conditions, peak concentrations occur within 1 hr. - -
Effective half-life approximately 6 hr. - -
Cleared predominantly by renal excretion in subjects with normal renal function.
|
Treatment of hypertension. May be used alone or with other antihypertensive medication. Heart failure post-MI or LV dysfunction post-MI. Used to decrease risk of death and heart failure-related hospitalization.
| Initial dosage in patients not receiving a diuretic is 1 mg once daily in patients who are not black and 2 mg in black patients. Dosage adjusted according to BP. |
- -
When used in pregnancy during the second and third trimesters, ACEIs can cause injury and even death to the developing fetus. - -
Patients with renal impairment: initial daily dose should be reduced, smaller increments should be utilized for titration and minimal effective dose should be calculated.
|
| ARBs |
|---|
Candesartan cilexetil
(Atacand) |
- -
After oral administration, peak serum concentrations reached after 3–4 hr. - -
Elimination of half-life is approximately 9 hr. - -
Excreted in urine and feces.
|
Treatment of hypertension. May be used alone or in combination with other antihypertensive agents. Heart failure: used in patients with LV systolic dysfunction to reduce risk of cardiovascular death and heart failure hospitalization.
| Initial dose is 16 mg once daily. Can be given once or twice daily with doses ranging from 8–32 mg. Effect is usually present within 2 weeks, and maximal BP reduction occurs within 4–6 weeks. |
- -
When used in pregnancy during the second and third trimesters, drugs that act directly on the renin angiotensin system can cause injury and even death to the developing fetus. - -
Lower dose for patients with moderate hepatic impairment or depletion of intravascular volume.
|
Eprosartan
(Teveten) |
- -
After oral administration, plasma concentrations peak around 1–2 hr in the fasted state. - -
Mean terminal elimination half-life following multiple doses of 600 mg was 20 hr. - -
Eliminated primarily by biliary and renal excretion.
| Treatment of hypertension. May be used alone or in combination with other antihypertensives, such as diuretics and calcium channel blockers. | Initial dose is 600 mg once daily. Can be given once or twice daily with doses ranging 400 mg to 800 mg. |
- -
When used in pregnancy during the second and third trimesters, drugs that act directly on the rennin-angiotensin system can cause injury and even death to the developing fetus. - -
Elderly, hepatically impaired, or renally impaired patients should not exceed 600 mg daily.
|
Irbesartan
(Avapro) |
- -
After oral administration, peak plasma concentrations reached at 1.5–2 hr. - -
Average terminal elimination of half-life is 11–15 hr. - -
Eliminated primarily by biliary and renal excretion.
|
Treatment of hypertension. May be used alone or with other antihypertensive agents. Nephropathy in type 2 diabetic patients. Indicated for treatment of patients with an elevated serum creatinine and proteinuria > 300 mg/day). Reduces rate of progression of nephropathy.
| Initial dose is 150 mg once daily. Patients who require more reduction in BP should be titrated to 300 mg once daily. |
- -
When used in pregnancy during the second and third trimesters, drugs that act directly on the rennin-angiotensin system can cause injury and even death to the developing fetus. - -
Nephropathy in type 2 diabetic patients: maintenance dose is 300 mg once daily. - -
Children (6–12 years): initial dose of 75 mg, up to 150 mg once daily. Ages 13–16: initial 150 mg once daily, can be titrated to 300 mg once daily, higher doses not recommended. - -
Lower initial dose for patients with depletion of intravascular volume or salt.
|
Losartan
(Cozaar) |
- -
After oral administration, mean peak concentrations reached in 1 hr. - -
Terminal half-life is 2 hr. - -
Eliminated primarily by biliary and renal excretion.
|
Treatment of hypertension. May be used alone or with other antihypertensive agents, including diuretics. Hypertensive patients with LV hypertrophy: reduces risk of stroke, though some evidence that this does not apply to black patients. Nephropathy in type 2 diabetic patients: reduces rate of progression of nephropathy as measured by doubling of serum creatinine or end-stage renal disease.
| Initial dose is 50 mg once daily, with 25 mg used in patients with possible depletion of intravascular volume and patients with history of hepatic impairment. May be given twice daily with total doses from 25 mg to 100 mg. |
- -
When used in pregnancy during the second and third trimesters, drugs that act directly on the rennin-angiotensin system can cause injury and even death to the developing fetus. - -
Pediatric hypertensive patients (6 years and greater): starting dose is 0.7 mg/kg once daily (up to 50 mg total) given as tablet or a suspension. - -
Hypertensive patients with LV hypertrophy: starting dose is 50 mg once daily. Based on BP response, hydrochlorothiazide 12.5 mg daily should be added and/or dose of losartan should be increased to 100 mg once daily followed by an increase of hydrochlorothiazide to 25 mg once daily.
|
Olmesartan medoxomil
(Benicar) |
- -
After oral administration, peak plasma concentrations reached after 1–2 hr. - -
Terminal elimination of half-life is 13 hr. - -
Eliminated primarily by biliary and renal excretion.
| Treatment of hypertension. May be used alone or with other antihypertensive agents. | Initial dose is 20 mg once daily. For patients requiring further reduction in BP, dose may be increased to 40 mg. |
- -
When used in pregnancy during the second and third trimesters, drugs that act directly on the rennin-angiotensin system can cause injury and even death to the developing fetus. - -
In patients with impaired renal failure, a lower starting dose should be considered.
|
Telmisartan
(Micardis) |
- -
After oral administration, peak concentrations reached within 0.5–1 hr. - -
Terminal elimination of half-life is 24 hr. - -
Eliminated mostly through feces.
| Treatment of hypertension. May be used alone or with other antihypertensive agents. | Starting dose is 40 mg once daily. BP response is dose-related over range of 20–80 mg. |
- -
When used in pregnancy during the second and third trimesters, drugs that act directly on the rennin-angiotensin system can cause injury and even death to the developing fetus. - -
Patients with depletion of intravascular volume, biliary obstructive disorders, or hepatic insufficiency should start treatment under close medical supervision.
|
Valsartan
(Diovan) |
- -
After oral administration, peak plasma concentrations reached within 2–4 hr. - -
Average elimination half-life about 6 hr. - -
Primarily eliminated in feces and urine.
|
Treatment of hypertension. May be used alone or with other antihypertensive agents. Heart failure: used in treatment of heart failure, reduces hospitalizations. Post-MI: used to reduce cardiovascular mortality.
| Initial dose is 80 mg or 160 mg once daily in patients who are not volume depleted. May be used over a dose range of 80 mg to 320 mg once daily. |
- -
When used in pregnancy during the second and third trimesters, drugs that act directly on the rennin-angiotensin system can cause injury and even death to the developing fetus. - -
Care should be given when dosing patients with hepatic or severe renal impairment.
|
| Direct renin inhibitor |
|---|
Aliskiren
(Tekturna) |
- -
Poorly absorbed (bioavailability about 2.5%) with an approximate accumulation half-life of 24 hours. - -
Steady state blood levels are reached in about 7–8 days. - -
Following oral administration, peak plasma concentrations of aliskiren are reached within 1–3 hr. - -
When taken with a high-fat meal, mean AUC and Cmax of aliskiren are decreased by 71% and 85% respectively. - -
One-fourth of the absorbed dose appears in the urine as parent drug.
| Treatment of hypertension. |
- -
May be used alone or in combination with other antihypertensive agents. - -
Use with maximal doses of ACEIs has not been adequately studied. - -
Starting dose: 150 mg once daily. - -
If blood pressure remains uncontrolled titrate up to 300 mg (available in 150 mg and 300 mg. tablets). - -
Patients should establish a routine pattern for taking aliskiren with regard to meals. High-fat meals decrease absorption substantially.
|
- -
No adjustment of the starting dose is required in elderly patients, patients with mild-to-severe renal impairment or mild to- severe hepatic insufficiency. - -
Care should be taken when dosing aliskiren in patients with severe renal impairment, as clinical experience with such patients is limited. - -
Pediatric patients: The pharmacokinetics of aliskiren have not been investigated in patients < 18 years of age. - -
Nursing mothers: It is not known whether aliskiren is excreted in human breast milk. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. - -
Race: The pharmacokinetic differences between blacks, Caucasians, and the Japanese are minimal.
|
