PROCARDIA XL
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PROCARDIA XL (PROCARDIA XL).
| Breastfeeding | Nifedipine is excreted into breast milk in concentrations similar to maternal plasma (M/P ratio approximately 1.0). In clinical studies, no adverse effects in nursing infants have been reported, but caution is advised, especially in neonates with compromised cardiac function. |
| 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. |
■ 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 component","Cardiogenic shock","Concurrent use with strong CYP3A4 inducers (e.g., rifampin) due to decreased efficacy"]
| 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"] |
Loading safety data…
| 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. |