FDA Indication(s)

Pharmacokinetics

Pregnancy and Breastfeeding Risk[10]

Cost and Formulation

DIHYDROPYRIDINE

Amlodipine

Treatment of HTN; treatment of coronary artery disease (including chronic stable angina and vasospastic angina)

A: ~ 64% - 90% oral[8]

M: hepatic; 90% converted to inactive metabolites

E: renal 60% as inactive metabolites, 10% unchanged; not dialyzable

t1/2 = 30- 50 hours; increased with hepatic impairment

Pregnancy: limited human data - animal data suggest moderate risk

Breastfeeding: limited human data - probably compatible; present in breast milk

Generic available[9]

2.5 mg (30 tab): $36.32

5mg (30 tab): $37.76

10mg (30 tab): $51.49

Nifedipine (extended-release)

Treatment of HTN; treatment of chronic stable or vasospastic angina

A:90%

M: hepatic -CYP3A4 substrate, extensive first-pass metabolism

E: renal 80% as mostly inactive metabolites; fecal 20%; not dialyzable

t1/2 = 2 - 5 hrs

Category C

Pregnancy: human data suggest low risk

Breasfeeding: limited human data - probably compatible; enters breast milk (AAP considers compatible)

Generic available extended-release[9]

30 mg (30 tab): $53.52

60 mg (30 tab): $75.79

90 mg (30 tab) $83.60

Felodipine

Treatment of HTN

A: 100%

M: Hepatic - CYP3A4 substrate, extensive first-pass metabolism

E: renal 70%; 10% fecal; not dialyzable

t1/2 = 11-16 hours

Category C

Pregnancy: limited human data - animal data suggest risk

Breasfeeding: no human data - probably compatible; excretion in breast milk should be expected due to low molecular weight

Generic available[9]

2.5 mg (30 tab): $46.27

5 mg (30 tab): $48.21

10 mg (30 tab) $ 79.42

NON-DIHYDROPYRIDINE

Verapamil

Treatment of HTN, angina, atrial fibrillation (rate control), treatment and prophylaxis of supraventricular tachycardia

A: 90%

M: hepatic - extensive first-pass metabolism via multiple CYP isoenzymes

E: renal 70% as metabolites; not dialyzable

t1/2: 5-12 hours, 14-16 hours (severe hepatic impairment)

Category C

Pregnancy: compatible

Breastfeeding: limited human data - probably compatible; enters breast milk
(AAP considers compatible)

Generic available
extended release[11]

100 mg (100 tab): $195.84
120 mg (100 tab): $193.93
180 mg (100 tab): $182.86
200 mg (100 tab): $252.23
240 mg (100 tab): $206.36
300 mg (100 tab): $366.98
360 mg (100 tab): $637.50

Diltiazem

Treatment of HTN, chronic stable angina or angina from coronary spasm

A: ~93% - 95%

M: hepatic - extensive first-pass metabolism, substrate and inhibitor of CYP3A4 and P-gp

E: renal; hepatic; not dialyzable

t1/2: 4-9.5 hours

Category C

Pregnancy: human data suggest low risk

Breastfeeding: limited human data - probably compatible; enters breast milk
(AAP considers compatible)

Generic available extended release[9]

120mg(30 cap): $38.96
180mg(30 cap): $44.16
240mg(30 cap): $60.05
300mg(30 cap): $76.64

360mg(30 cap): $341.86

A = absorption; M = metabolism; E = excretion; AAP = American Academy of Pediatrics