PROCARDIA XL
Clinical safety rating
cautionComprehensive clinical and safety monograph for PROCARDIA XL (PROCARDIA XL).
Dihydropyridine calcium channel blocker that inhibits calcium ion influx across cardiac and vascular smooth muscle cells, leading to vasodilation and reduced peripheral vascular resistance.
| Metabolism | Hepatic metabolism primarily via CYP3A4 |
| Excretion | Renal: 70-80% as metabolites, <1% unchanged; Fecal: 15-20% via bile. |
| Half-life | Terminal elimination half-life: 6-11 hours; clinical context: steady-state achieved after 2-3 days of once-daily dosing. |
| Protein binding | 92-98% bound primarily to albumin. |
| Volume of Distribution | 0.78-1.6 L/kg; high Vd indicates extensive tissue distribution. |
| Bioavailability | Oral (extended-release): 65-85% due to first-pass metabolism; absolute bioavailability 45-65%. |
| Onset of Action | Oral (extended-release): onset of antihypertensive effect within 20-30 minutes; peak effect at 6 hours. |
| Duration of Action | Duration of antihypertensive effect: 24 hours; clinical notes: once-daily dosing provides consistent blood pressure control over the dosing interval. |
| Molecular Weight | 666.7 |
30-90 mg orally once daily, extended-release tablet.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | No specific dose adjustment for GFR; use with caution in renal impairment due to potential accumulation of metabolites. |
| Liver impairment | Child-Pugh A and B: reduce dose by 50%; Child-Pugh C: avoid use. |
| Pediatric use | Safety and efficacy not established; use not recommended. |
| Geriatric use | Start at lowest dose (30 mg daily) and titrate slowly; monitor for hypotension and peripheral edema. |
| 1st trimester | Associated with congenital anomalies in animal studies; human data limited. Use only if benefit outweighs risk. |
| 2nd trimester | May cause fetal hypoxia due to maternal hypotension; monitor fetal heart rate. Use only if clearly needed. |
| 3rd trimester | May cause fetal hypoxia, oligohydramnios, and neonatal hypotension. Avoid near term or during labor. |
Clinical note
Comprehensive clinical and safety monograph for PROCARDIA XL (PROCARDIA XL).
| Placental transfer | Crosses placenta; detected in cord blood. Fetal/maternal ratio not well established. |
| Breastfeeding | Minimal excretion into breast milk; unlikely to affect nursing infant. However, use with caution due to potential for hypotension. |
| Lactation Rating | L2 - Limited data; probably compatible |
| Teratogenic Risk | In animal studies, nifedipine caused embryotoxicity, fetotoxicity, and teratogenicity (skeletal anomalies, phalangeal malformations) at doses 30-100 times the maximum recommended human dose. In humans, no adequate controlled studies; however, case reports and observational studies suggest an increased risk of preterm birth and possibly fetal distress after third-trimester use. Use in the first trimester is associated with possible cardiovascular defects. Avoid in pregnancy unless benefit clearly outweighs risk. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of hypotension. Periodic blood pressure monitoring in the fetus via ultrasound to assess for placental insufficiency. Monitor for uterine contractility changes if used for tocolysis. In late pregnancy, monitor for fetal distress and neonatal outcomes. |
| Fertility Effects | Nifedipine may cause reversible impairment of fertility in males (sperm motility and morphology changes) based on animal studies. In humans, no definitive studies on fertility effects; however, transient gynecomastia has been reported. |
■ FDA Black Box Warning
Increased risk of cardiovascular events and mortality in patients with coronary artery disease when using short-acting nifedipine; use with caution.
| Serious Effects |
Hypersensitivity to nifedipine or any componentCardiogenic shockConcurrent use with rifampin
| Precautions | May cause severe hypotension, especially in patients on beta-blockers, Can exacerbate angina or cause myocardial infarction upon initiation or dose increase, Peripheral edema is common and dose-dependent, Avoid grapefruit juice which increases nifedipine levels, Use caution in patients with hepatic impairment |
| Food/Dietary | Avoid grapefruit and grapefruit juice. Grapefruit inhibits CYP3A4, increasing nifedipine plasma concentrations and risk of toxicity. High-fat meals may slightly increase absorption but no specific restriction. |
| Clinical Pearls | PROCARDIA XL (nifedipine extended-release) is a dihydropyridine calcium channel blocker used primarily for hypertension. Avoid grapefruit juice due to CYP3A4 inhibition increasing nifedipine levels. Do not crush or chew tablets; swallow whole. Monitor for peripheral edema, especially in elderly. Use with caution in patients with severe aortic stenosis or heart failure with reduced ejection fraction. Abrupt discontinuation may cause rebound hypertension. |
| Patient Advice | Take exactly as prescribed, usually once daily. · Swallow tablet whole; do not crush, chew, or split. · Avoid grapefruit and grapefruit juice while taking this medication. · May cause dizziness or lightheadedness; avoid driving until you know how you react. · Do not stop taking without consulting your doctor; sudden stop may worsen blood pressure. · Report swelling in ankles/feet, persistent cough, or irregular heartbeat. · Keep tablets in original container; protect from light and moisture. |
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