SULAR
Clinical safety rating: caution
Comprehensive 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 |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SULAR (SULAR).
| Breastfeeding | Excreted in human milk; M/P ratio unknown. Effects on infant unknown. Use with caution, especially in preterm infants or those with compromised renal function. |
| 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 |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to nisoldipine or any dihydropyridine calcium channel blocker; concomitant administration with strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir).
| 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. |
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| 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. |