SULAR
Clinical safety rating
cautionComprehensive clinical and safety monograph for SULAR (SULAR).
Nisoldipine is a dihydropyridine calcium channel blocker that inhibits the influx of calcium ions through L-type calcium channels in vascular smooth muscle and cardiac muscle. This leads to vasodilation, reduced peripheral vascular resistance, and decreased myocardial oxygen demand.
| Metabolism | Extensively metabolized in the liver via CYP3A4; undergoes first-pass metabolism. Metabolites are inactive. |
| Excretion | Renal: 50-60% as metabolites, 10% as unchanged drug; Fecal: ~35%; Biliary: <5% |
| Half-life | Terminal half-life of 24-50 hours, mean ~34 hours; extended in elderly and hepatic impairment, dose adjustment may be needed |
| Protein binding | >95% bound to plasma proteins (albumin and alpha-1-acid glycoprotein) |
| Volume of Distribution | 3-10 L/kg; extensive tissue distribution, slow equilibration |
| Bioavailability | Oral: 65-90% (first-pass metabolism); extended-release formulation provides consistent absorption |
| Onset of Action | Oral: 30-60 minutes; peak effect at 6-12 hours |
| Duration of Action | 24 hours (once-daily dosing); sustained effect due to extended-release formulation |
| Molecular Weight | 454.5 Da |
10-20 mg orally once daily; maximum 60 mg/day.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | No adjustment for GFR ≥30 mL/min. For GFR <30 mL/min, initiate at 5 mg once daily. |
| Liver impairment | Child-Pugh A: 5 mg once daily. Child-Pugh B: 2.5 mg once daily. Child-Pugh C: not recommended. |
| Pediatric use | Safety and efficacy not established; no approved dosing. |
| Geriatric use | Initiate at 5 mg once daily; titrate cautiously due to increased sensitivity and risk of hypotension. |
| 1st trimester | Avoid use; associated with fetal anomalies in animal studies and potential for teratogenicity. Use only if no alternative and benefit outweighs risk. |
| 2nd trimester | Use with caution; may cause fetal hypotension, oligohydramnios, and renal impairment. Monitor fetal growth and amniotic fluid volume. |
| 3rd trimester | Avoid use; may cause neonatal hypotension, hyperkalemia, and oliguria. Contraindicated in pregnancy-induced hypertension due to risk of fetal harm. |
Clinical note
Comprehensive clinical and safety monograph for SULAR (SULAR).
| Placental transfer | Crosses placenta in humans; detected in cord blood and amniotic fluid. Animal studies show extensive transfer. |
| Breastfeeding | Excreted into breast milk in low amounts; case reports show no adverse effects in infants. However, due to limited data, use with caution; monitor infant for hypotension and electrolyte disturbances. |
| Lactation Rating | L3 (Limited Data) |
| Teratogenic Risk | Pregnancy Category C. First trimester: No adequate studies; potential for fetal harm based on animal data. Second and third trimesters: Risk of fetal hypotension, oligohydramnios, and neonatal renal failure. Avoid use during pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal blood pressure, fetal heart rate, and amniotic fluid volume. Consider ultrasound for fetal growth and wellbeing. |
| Fertility Effects | No human data; animal studies show no impairment of fertility. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to nisoldipine or any component of the formulationConcomitant use with strong CYP3A4 inducers (e.g., rifampin, St. John's wort)Severe hypotension (systolic BP < 90 mmHg)Cardiogenic shockUnstable angina or acute myocardial infarction within 4 weeksPregnancy (particularly third trimester due to risk of fetal harm)
| Precautions | Increased angina and/or myocardial infarction upon initiation or dose titration; caution in patients with heart failure, aortic stenosis, or significant left ventricular dysfunction; may cause hypotension; caution in patients with hepatic impairment; grapefruit juice increases nisoldipine levels and should be avoided; drug interactions with CYP3A4 inhibitors and inducers. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they increase nisoldipine serum concentrations by inhibiting CYP3A4 metabolism. Concomitant intake of high-fat meals (e.g., >50% fat) can increase the rate and extent of absorption; advise taking consistently with or without food. St. John's wort may reduce efficacy due to CYP3A4 induction. |
| Clinical Pearls | Nisoldipine (Sular) is a dihydropyridine calcium channel blocker with high vascular selectivity; avoid use in patients with unstable angina or recent MI due to reflex tachycardia risk. Do not administer with grapefruit juice as it significantly increases drug exposure. Monitor for peripheral edema, especially in the elderly. Use cautiously in patients with severe aortic stenosis or hepatic impairment. May be taken without regard to meals, but avoid high-fat meals which can increase absorption. |
| Patient Advice | Take exactly as prescribed; do not crush or chew extended-release tablets. · Avoid grapefruit and grapefruit juice while taking this medication. · Do not stop abruptly without consulting your doctor; may worsen chest pain or blood pressure. · You may experience dizziness or lightheadedness; rise slowly from sitting or lying positions. · Notify your doctor if you develop swelling in your ankles or feet, rapid heartbeat, or severe dizziness. · Avoid alcohol as it can increase the risk of low blood pressure and dizziness. |
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