Nifedipine

Calcium channel blocker (dihydropyridine), Antihypertensive, Antianginal, Tocolytic (off-label)

Nifedipine

Procardia, Procardia XL, Adalat CC, Afeditab CR

Experience

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Titration strategies

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Effects

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Pharmacy

Starting dose

ER 30-60 mg PO once daily; immediate-release 10 mg PO TID (now rarely used for hypertension due to reflex tachycardia)

Preparations

10, 20 mg IR capsules; 30, 60, 90 mg ER tablets

US FDA Max

120 mg/d (ER); IR not for chronic hypertension

Common uses

Classification(s)

Classes

Calcium channel blocker (dihydropyridine), Antihypertensive, Antianginal, Tocolytic (off-label)

Pharmacology

Routes

Oral; sublingual IR is discouraged (uncontrolled BP drops, MI reports)

Onset

IR 20 minutes; ER ~6 hours

Duration

IR 4-8 hours; ER 24 hours

Half-life

2-5 hours (IR); ER formulations extend functional duration via osmotic/matrix release

Bioavailability

~50% IR (extensive first-pass via CYP3A4); ER products release-rate-limited

Pregnancy

Oral nifedipine is one of the preferred agents for severe hypertension in pregnancy and for tocolysis in preterm labor.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Nifedipine is a dihydropyridine calcium channel blocker that selectively inhibits L-type voltage-gated calcium channels in vascular smooth muscle, producing peripheral and coronary arterial vasodilation; cardiac myocyte and AV nodal effects are minimal compared with non-dihydropyridines like diltiazem and verapamil.▲0▼ Immediate-release nifedipine's rapid vasodilation and reflex sympathetic activation drove the early 1990s safety concerns that led to ER-only chronic use; sublingual IR is contraindicated. CYP3A4 substrate with substantial grapefruit/itraconazole interactions.