NEUROHORMONAL ANTAGONISTS

Comparison of ACEI Table (FDA approved for heart failure treatment)

ACEI
Accupril
Altace
Capoten
Mavik

Monopril
Prinivil
Vasotec
Zestril
Generic name
Quinipril
Ramipril
Captopril
Trandola
pril
Fosino
pril
Lisinopril
Enalapril
Lisino
pril
FDA Indications
HTN, CHF
HTN, CHF
HTN, CHF, Asymp LV dysfunction
HTN,
S/P MI CHF
HTN, CHF
HTN, CHF
HTN, CHF, Asymp LV dysfunction
HTN, CHF
Tablet Size
5, 10, 20, 40
1.25, 2.5. 5, 10
12.5, 25, 50, 100
1, 2, 4
10, 20
5, 10, 20, 40
2.5, 5, 10, 20
5, 10, 20, 40
Starting Dose
5 mg bid
1.25-2.5 mg qd
6.25-12.5 mg tid
1 mg qd
5 mg qd
2.5-5 mg qd
2.5 mg bid
2.5-5 mg qd
Target Dose (a)
20 mg bid
10 mg qd
50 mg tid
2-4 mg qd
20 mg qd
20 mg qd
10 mg bid
20 mg qd
Maximum Dose
40 mg bid
10 mg bid
100 mg tid
8 mg qd
40 mg qd
40 mg qd
20 mg bid
40 mg qd
Can Tablet Be Broken in Half
(b)
Capsule
(b)
(b)
(b)
(b)
(b)
(b)
(a) = average maintenance dose used in clinical trials
(b) = Tablets are in all forms and sizes. Many of them can be cut in a half with good pill cutter and do it carefully. It may save money in many preparations and dosages.

Beta Blockers with Proven Benefit in Heart Failure
Beta Blocker
Action
Starting Dose
Target Dose
FDA Approved
Carvedilol (Coreg) (a)
Beta 1; Beta 2, Alpha 1
3.125 mg bid
25 mg bid
Yes
Metoprolol Succinate CR (Toprol XL)
Beta 1 (c)
12.5 mg qd
100-200 mg qd
Yes
Metoprolol Tartrate (b)
Beta 1 (c)
6.25 mg bid
50-75 mg bid
No
Bisoprolol (Zebeta)
Beta 1 (c)
1.25 mg qd
10 mg qd
No
-  There are no proven benefit data for other Beta blockers.
-  (a) = When prescribe low dose, only Carvedilol has proven benefit. Carvedilol is superior to Metoprolol Tartrate, although dosage may not be equivalent and there is no comparison to Metoprolol Succinate CR (COMET, 2003)
-  (b) = There is no mortality benefit data for Metoprolol tartrate.
-  At target dose in clinical trials, these selective beta blocker may become non selective ones.

ARBs (Those in Heart Failure Trials)
ARB
Initial Dose
Target Dose
FDA approved
Losartan (Cozaar) (1)
25 mg qd
50 qd  (4)
No
Valsartan (Diovan) (2)
80 mg qd
160 mg bid
Yes
Irbesartan (Avapro)
75 mg qd
150 - 300 qd  (5)
No
Candesartan (Atacan) (3)
4 mg qd
32 mg qd
Yes
(1) In ELETE II, 2000.   (2) In Val-Helf, 2001 and VALIANT, 2003.   (3) In CHARM, 2003, .  (4) Dose of 100 mg qd may be better.    (5) Need to be confirmed.

Aldosterone Antagonist (FDA approved for heart failure treatment)
Aldosterone antagonist IndicationInitial dose Target dose
Spironolactone (Aldactone)
NYHA III-IV
12.5 mg 25 mg
Eplerenone (Inspra)
Post MI with heart fuilure
25 mg 50 mg