CARDENE SR
Clinical safety rating
cautionComprehensive clinical and safety monograph for CARDENE SR (CARDENE SR).
Nicardipine is a dihydropyridine calcium channel blocker that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. It produces relaxation of coronary vascular smooth muscle and dilation of coronary arteries, and also dilates peripheral arteries, reducing systemic vascular resistance and blood pressure.
| Metabolism | Primarily hepatic via cytochrome P450 (CYP3A4) isoenzyme. |
| Excretion | Renal: 60% (metabolites, unchanged drug <1%); Biliary/Fecal: 35% |
| Half-life | Terminal elimination half-life 8.6 hours (range 6-15 hours). Clinical context: No accumulation at steady state with TID dosing. |
| Protein binding | 95-98%, primarily to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 0.3-0.7 L/kg. Clinical meaning: Indicates extensive tissue distribution. |
| Bioavailability | Oral: 35% (first-pass metabolism); Food does not significantly affect bioavailability. |
| Onset of Action | Oral immediate release: 20-30 minutes; Sustained release: 1-2 hours |
| Duration of Action | Oral immediate release: 8-12 hours; Sustained release: 12 hours. Clinical notes: Antihypertensive effect persists for 12 hours with SR formulation. |
| Molecular Weight | 515.99 Da (as hydrochloride salt) |
Initial: 30 mg orally twice daily (SR capsules). Titrate up to 60 mg twice daily. Usual maintenance: 30-60 mg twice daily.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | No specific GFR-based dose adjustment provided by manufacturer; use with caution in renal impairment, especially if concurrent hepatic impairment. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B/C: Consider starting at 15 mg twice daily and titrate slowly due to increased bioavailability. |
| Pediatric use | Not established; safety and efficacy in pediatric patients have not been determined. |
| Geriatric use | Start at lower initial dose (15 mg twice daily) and titrate cautiously due to increased bioavailability and slower elimination. |
| 1st trimester | Avoid; may cause fetal bradycardia and growth restriction. No adequate human studies; use only if benefit outweighs risk. |
| 2nd trimester | Avoid; use with caution if clearly needed. May reduce uteroplacental blood flow. |
| 3rd trimester | Avoid; may inhibit labor and cause fetal hypotension. |
Clinical note
Comprehensive clinical and safety monograph for CARDENE SR (CARDENE SR).
| Placental transfer | Crosses placenta in rats and likely in humans; degree not quantified. |
| Breastfeeding | Nicaradipine is excreted in human milk in low amounts; however, effects on the nursing infant are unknown. Caution is advised, especially in pre-term or low birth weight infants. |
| Lactation Rating | L3 (Moderately Safe) – limited data, no adverse effects reported in most cases |
| Teratogenic Risk | Nifedipine, the active ingredient in Cardene SR, is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. In animal studies, nifedipine has been shown to cause embryotoxicity, placentotoxicity, and fetotoxicity at doses several times the maximum recommended human dose. First trimester: Risk cannot be ruled out; potential for teratogenic effects based on animal data. Second and third trimesters: May cause maternal hypotension and fetal distress due to placental hypoperfusion; use only if benefit outweighs risk. Case reports of fetal distress, perinatal asphyxia, and cesarean delivery associated with use in preterm labor. |
| Fetal Monitoring | Monitor maternal blood pressure and heart rate closely, especially during dose initiation and titration. Fetal heart rate monitoring may be indicated, particularly if used for tocolysis (off-label). Assess for signs of maternal hypotension, which may reduce uteroplacental perfusion. In preterm labor, monitor for inhibition of labor and potential side effects like pulmonary edema (if used with beta-agonists). |
| Fertility Effects | Nifedipine has been associated with reversible impairment of male fertility in animal studies (decreased spermatogenesis). In humans, case reports suggest possible erectile dysfunction, but no controlled studies on fertility effects. Women: No significant impact on female fertility reported, but data are limited. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to nicardipine or any componentAdvanced aortic stenosisSevere hypotension (systolic BP < 90 mmHg)Cardiogenic shockConcurrent use with rifampin
| Precautions | Use caution in patients with coronary artery disease; may cause increased angina or acute myocardial infarction upon initiation or dose titration. Also caution in patients with congestive heart failure, hepatic impairment, or renal impairment. Monitor blood pressure during titration. |
| Food/Dietary | Grapefruit and grapefruit juice increase nicardipine serum concentrations by inhibiting CYP3A4 metabolism. Avoid concurrent use. High-fat meals may increase absorption; take consistently with regard to meals. Alcohol may enhance hypotensive effects; limit intake. |
| Clinical Pearls | CARDENE SR (nicardipine) is a dihydropyridine calcium channel blocker used for hypertension. Avoid in advanced aortic stenosis due to risk of reduced coronary perfusion. Monitor for peripheral edema, especially in elderly. Use caution in heart failure with reduced ejection fraction due to negative inotropic effects (though less than verapamil). May increase cyclosporine levels; monitor levels. For IV use (not SR), titrate rapidly for hypertensive emergency. Do not crush or chew SR capsules. |
| Patient Advice | Take exactly as prescribed, usually twice daily. Swallow SR capsules whole; do not crush or chew. · Avoid grapefruit and grapefruit juice as they can increase drug levels and side effects. · May cause dizziness or lightheadedness; avoid driving until you know how you react. Rise slowly from sitting or lying. · Notify your doctor if you experience swelling in ankles or feet, rapid heartbeat, or shortness of breath. · Do not stop abruptly; sudden withdrawal may worsen chest pain or blood pressure. · Keep a daily blood pressure log to track effectiveness. |
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