PLENDIL
Clinical safety rating
cautionComprehensive clinical and safety monograph for PLENDIL (PLENDIL).
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 | Primarily hepatic via CYP3A4; undergoes extensive first-pass metabolism. |
| Excretion | Renal (approximately 70% as metabolites, <0.5% unchanged); fecal (approximately 10%) |
| Half-life | Terminal elimination half-life 2-5 hours in healthy adults; 7-12 hours in patients with hepatic impairment or advanced age |
| Protein binding | >99% bound, primarily to albumin and alpha1-acid glycoprotein |
| Volume of Distribution | 4-10 L/kg; large Vd indicates extensive tissue distribution |
| Bioavailability | Oral: 15-20% (extensive first-pass metabolism) |
| Onset of Action | Oral: 30-60 minutes |
| Duration of Action | 24 hours (due to sustained-release formulation) |
| Molecular Weight | 384.48 |
| Action Class | Calcium channel blockers- Dihydropyridines (DHP) |
Initial: 5 mg orally once daily. Maintenance: 2.5–10 mg orally once daily. Maximum: 10 mg/day.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | No adjustment required for any degree of renal impairment. |
| Liver impairment | Child-Pugh A or B: Initial dose 2.5 mg orally once daily. Child-Pugh C: Contraindicated or not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | Initial dose 2.5 mg orally once daily; titrate cautiously due to increased systemic exposure. |
| 1st trimester | Associated with fetal toxicity in animal studies; human data limited. Use only if maternal benefit outweighs risk. |
| 2nd trimester | May cause reduced uteroplacental perfusion and fetal hypoxia. Avoid use after 20 weeks gestation. |
| 3rd trimester | Contraindicated in pregnancy due to risk of fetal hypotension, oligohydramnios, and neonatal renal failure. |
Clinical note
Comprehensive clinical and safety monograph for PLENDIL (PLENDIL).
| Placental transfer | Crosses the placenta in animal studies; human data suggest transfer occurs. Degree not quantified. |
| Breastfeeding | Excreted into breast milk in small amounts. Due to potential for adverse effects in the infant (e.g., hypotension), use with caution and monitor infant for symptoms. Consider alternative antihypertensives with more safety data. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Pregnancy Category C. First trimester: No adequate studies in humans; animal studies show fetal toxicity at high doses. Second and third trimesters: Potential for fetal hypotension, hypoxia, and growth restriction due to maternal hypotension; avoid use if possible. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of hypotension. Fetal monitoring for growth, heart rate, and amniotic fluid volume if used in pregnancy. |
| Fertility Effects | Reversible fertility impairment in animal studies (reduced pregnancy rates). Human data limited; potential for decreased sperm motility in males. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to felodipine or any dihydropyridine calcium channel blockerPregnancy (especially second and third trimesters)Cardiogenic shockAcute myocardial infarction (within 4 weeks)Unstable angina pectorisSevere aortic stenosis
| Precautions | Beta-blocker withdrawal: taper gradually, Peripheral edema, Hepatic impairment, Grapefruit juice increases drug levels |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they increase felodipine plasma concentrations; take on an empty stomach or with a light meal to minimize fluctuations; high-fat meals may increase absorption. |
| Clinical Pearls | Avoid grapefruit products; titrate slowly to minimize reflex tachycardia; use with caution in severe aortic stenosis; may cause peripheral edema, more common in women; administer extended-release tablets whole, do not crush or chew. |
| Patient Advice | Swallow the tablet whole; do not crush, chew, or split. · Avoid grapefruit juice and grapefruit products while taking this medication. · Do not stop taking suddenly without consulting your physician. · May cause dizziness or lightheadedness; avoid driving if affected. · Report any persistent swelling of ankles or feet, severe dizziness, or irregular heartbeat. |
Loading safety data…