CARDENE
Clinical safety rating
cautionComprehensive clinical and safety monograph for CARDENE (CARDENE).
Cardene (nicardipine) is a dihydropyridine calcium channel blocker that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. It dilates peripheral arterioles, reducing systemic vascular resistance and blood pressure, and also has coronary vasodilatory effects.
| Metabolism | Hepatic metabolism primarily via cytochrome P450 isoenzymes CYP3A4 and CYP2C8, with minor contributions from CYP2D6. |
| Excretion | Renal: 60% as metabolites, 10% unchanged; Fecal: 35% |
| Half-life | 1.5-2 hours (terminal); prolonged in hepatic impairment (up to 6-8 hours) |
| Protein binding | >95% bound to albumin and alpha-1 acid glycoprotein |
| Volume of Distribution | 0.6-1.2 L/kg (large Vd due to extensive tissue binding) |
| Bioavailability | Oral: 35-60% (first-pass metabolism; increased with hepatic disease) |
| Onset of Action | IV: 1 minute; Oral: 20-30 minutes |
| Duration of Action | IV: 30 minutes to 2 hours (dose-dependent); Oral: 6-8 hours |
| Molecular Weight | 479.53 |
20-40 mg orally three times daily.
| Dosage form | CAPSULE |
| Renal impairment | For GFR < 30 mL/min: initiate at 20 mg orally twice daily. |
| Liver impairment | Child-Pugh class B or C: reduce dose by 50% and titrate slowly. |
| Pediatric use | Not established; safety and efficacy not determined. |
| Geriatric use | Initiate at 20 mg orally twice daily; titrate cautiously. |
| 1st trimester | No adequate studies in pregnant women; use only if potential benefit justifies risk. May cause fetal harm based on animal data. |
| 2nd trimester | Use only if clearly needed. Monitor maternal blood pressure and fetal growth. Risk of fetal hypotension and hypoperfusion. |
| 3rd trimester | Use with caution; may cause fetal bradycardia, hypotension, and oligohydramnios. Avoid near term due to risk of uterine atony and postpartum hemorrhage. |
Clinical note
Comprehensive clinical and safety monograph for CARDENE (CARDENE).
| Placental transfer | Nicardipine crosses the placenta. Measurable levels in fetal plasma and amniotic fluid. Animal studies show embryotoxicity and fetotoxicity at high doses. |
| Breastfeeding | NICARDIPINE (CARDENE) is excreted in human milk in small amounts. The American Academy of Pediatrics considers it compatible with breastfeeding. However, due to potential for adverse effects in the infant, weigh benefits against risks. Monitor infant for bradycardia, hypotension, and poor feeding. |
| Lactation Rating | L2: Safer (limited data, no evidence of harm in few studies). |
| Teratogenic Risk | Cardene (nicardipine) is classified as FDA Pregnancy Category C. In animal studies, nicardipine was associated with embryotoxicity, fetotoxicity, and teratogenicity at high doses. There are no adequate and well-controlled studies in pregnant women. Use in the first trimester should be avoided if possible; in the second and third trimesters, potential benefits must outweigh risks, particularly due to possible maternal hypotension and fetal hypoxia. |
| Fetal Monitoring | Monitor maternal blood pressure and heart rate closely. Assess for signs of hypotension. Fetal heart rate monitoring is recommended during prolonged use, especially in preeclampsia. Monitor renal function and electrolytes in the mother. |
| Fertility Effects | No significant adverse effects on fertility have been reported in animal studies. In humans, no specific data are available, but calcium channel blockers may theoretically impair spermatogenesis or ovarian function; however, clinically relevant effects are unlikely. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to nicardipine or any componentAdvanced aortic stenosis (risk of hemodynamic decompensation)Severe hypotension (systolic BP < 90 mmHg)Cardiogenic shockAcute myocardial infarction within 4 weeksSecond- or third-degree AV block (unless pacemaker in place)
| Precautions | Hypotension (especially in patients with ventricular dysfunction or those receiving beta-blockers), increased angina (rare, more common with dihydropyridines), peripheral edema, congestive heart failure (use caution in patients with severe left ventricular dysfunction), hepatic impairment (reduce dose), renal impairment (monitor blood pressure), abrupt discontinuation may cause angina exacerbation. |
| Food/Dietary | Grapefruit and grapefruit juice increase nicardipine exposure and should be avoided. High-fat meals may reduce absorption; take consistently with or without food. Alcohol may enhance hypotensive effects. |
| Clinical Pearls | CARDENE (nicardipine) is a dihydropyridine calcium channel blocker used intravenously for acute hypertension. Onset is rapid (1-2 minutes), making it ideal for hypertensive emergencies. It is metabolized hepatically; reduce dose in hepatic impairment. Does not cause reflex tachycardia as prominently as other dihydropyridines. Contraindicated in advanced aortic stenosis. Can be used for hypertension during pregnancy but with caution. |
| Patient Advice | Take exactly as prescribed; do not stop abruptly. · May cause dizziness or lightheadedness; avoid driving until you know how it affects you. · Avoid grapefruit and grapefruit juice as they may increase drug levels. · Report irregular heartbeat, shortness of breath, or swelling of the ankles or feet. · Keep all appointments for blood pressure monitoring. |
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