Nisoldipine

Nisoldipine is a member of the dihydropyridine class of calcium channel antagonists (calcium ion antagonists or slow channel blockers) that inhibit the transmembrane influx of calcium into vascular smooth muscle and cardiac muscle. It reversibly competes with other dihydropyridines for binding to the calcium channel.

• SULAR is indicated for the treatment of hypertension. It may be used alone or in combination with other anti-hypertensive agents.ICD-10: I10

• SULAR is contraindicated in patients with known hypersensitivity to dihydropyridine calcium channel blockers.contraindicated

The dosage of SULAR must be adjusted to each patient's needs. Therapy usually should be initiated with 17 mg orally once daily, then increased by 8.5 mg per week or longer intervals, to attain adequate control of blood pressure. Usual maintenance dosage is 17 to 34 mg once daily. Blood pressure response increases over the 8.5 - 34 mg daily dose range but adverse event rates also increase. Doses beyond 34 mg once daily are not recommended. SULAR has been used safely with diuretics, ACE inhibitors, and beta-blocking agents. Patients over age 65, or patients with impaired liver function, are expected to develop higher plasma concentrations of nisoldipine. Their blood pressure should be monitored closely during any dosage adjustment. A starting dose not exceeding 8.5 mg daily is recommended in these patient groups. SULAR tablets should be administered orally once daily. SULAR should be taken on an empty stomach (1 hour before or 2 hours after a meal). Grapefruit products should be avoided before and after dosing. SULAR is an extended release dosage form and tablets should be swallowed whole, not bitten, divided or crushed.

Increased angina and/or myocardial infarction in patients with coronary artery disease: Rarely, patients, particularly those with severe obstructive coronary artery disease, have developed increased frequency, duration and/or severity of angina, or acute myocardial infarction on starting calcium channel blocker therapy or at the time of dosage increase. The mechanism of this effect has not been established. In controlled studies of SULAR in patients with angina this was seen about 1.5% of the time in patients given nisoldipine, compared with 0.9% in patients given placebo.

ADVERSE EXPERIENCES More than 6000 patients world-wide have received nisoldipine in clinical trials for the treatment of hypertension, either as the immediate release or the SULAR extended release formulation. Of about 1,500 patients who received SULAR in hypertension studies, about 55% were exposed for at least 2 months and about one third were exposed for over 6 months, the great majority at doses equivalent to 17 mg and above. SULAR is generally well-tolerated. In the U.S. clinical trials of SULAR in hypertension, 10.9% of the 921 SULAR patients discontinued treatment due to adverse events compared with 2.9% of 280 placebo patients. The frequency of discontinuations due to adverse experiences was related to dose, with a 5.4% and 10.9% discontinuation rate at the lowest and highest daily dose, respectively. The most frequently occurring adverse experiences with SULAR are those related to its vasodilator properties; these are generally mild and only occasionally lead to patient withdrawal from treatment. The table below, from U.S. placebo-controlled parallel dose response trials of SULAR using doses across the clinical dosage range in patients with hypertension, lists all of the adverse events, regardless of the causal relationship to SULAR, for which the overall incidence on SULAR was both >1% and greater with SULAR than with placebo.

Pregnancy Nisoldipine was neither teratogenic nor fetotoxic at doses that were not maternally toxic. Nisoldipine was fetotoxic but not teratogenic in rats and rabbits at doses resulting in maternal toxicity (reduced maternal body weight gain). In pregnant rats, increased fetal resorption (postimplantation loss) was observed at 100 mg/kg/day and decreased fetal weight was observed at both 30 and 100 mg/kg/day. These doses are, respectively, about 5 and 16 times the MRHD when compared on a mg/m 2 basis. In pregnant rabbits, decreased fetal and placental weights were observed at a dose of 30 mg/kg/day, about 10 times the MRHD when compared on a mg/m 2 basis. In a study in which pregnant monkeys (both treated and control) had high rates of abortion and mortality, the only surviving fetus from a group exposed to a maternal dose of 100 mg nisoldipine/kg/day (about 30 times the MRHD when compared on a mg/m 2 basis) presented with forelimb and vertebral abnormalities not previously seen in control monkeys of the same strain. There are no adequate and well controlled studies in pregnant women. SULAR should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.

Metabolism

and Metabolism Nisoldipine pharmacokinetics are independent of the dose across the clinical dosage range of 17 to 51 mg, with plasma concentrations proportional to dose. Nisoldipine accumulation, during multiple dosing, is predictable from a single dose.

There is no experience with nisoldipine overdosage. Generally, overdosage with other dihydropyridines leading to pronounced hypotension calls for active cardiovascular support including monitoring of cardiovascular and respiratory function, elevation of extremities, judicious use of calcium infusion, pressor agents and fluids. Clearance of nisoldipine would be expected to be slowed in patients with impaired liver function. Since nisoldipine is highly protein bound, dialysis is not likely to be of any benefit; however, plasmapheresis may be beneficial.

• Feb 2, 1995NDANDA020356Azurity

1. 1Nausea887.4%
2. 2Drug Ineffective796.6%
3. 3Dizziness776.4%
4. 4Headache766.4%
5. 5Fatigue746.2%
6. 6Renal Failure655.4%
7. 7Pain645.4%
8. 8Dyspnoea635.3%
9. 9Asthenia625.2%
10. 10Diarrhoea594.9%
11. 11Anxiety544.5%
12. 12Myocardial Infarction544.5%
13. 13Oedema Peripheral544.5%
14. 14Hypertension504.2%
15. 15Pruritus504.2%

Recent PubMed references pinned to Nisoldipine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• In silico Development and Characterization of Nisoldipine Analogues for Enhanced Solubility and Therapeutic Potential in the Treatment of Angina Pectoris.
  Current drug discovery technologies · 2025 · Krosuri P, Mohan M
  PMID 40257029DOI 10.2174/0115701638359244250411045740
• Exploring the binding behaviors between nisoldipine and bovine serum albumin as a model protein by the aid of multi-spectroscopic approaches and in silico.
  Journal of biomolecular structure & dynamics · 2024 · Hu ZY, Wu M, Wang WJ, et al.
  PMID 37403263DOI 10.1080/07391102.2023.2232027
• Development of Self-Microemulsifying Drug Delivery System to Improve Nisoldipine Bioavailability: Cell Line and In Vivo Evaluations : Development of Self-Microemulsifying Drug Delivery System.
  AAPS PharmSciTech · 2021 · Mundada VP, Patel MH, Mundada PK, et al.
  PMID 34676456DOI 10.1208/s12249-021-02109-4
• Enhanced bioavailability and antihypertensive activity of nisoldipine loaded nanoemulsion: optimization, cytotoxicity and uptake across Caco-2 cell line, pharmacokinetic and pharmacodynamic studies.
  Drug development and industrial pharmacy · 2020 · Mundada VP, Patel MH, Mundada PK, et al.
  PMID 32031412DOI 10.1080/03639045.2020.1724128
• On the dimorphism and the pressure-temperature state diagram of racemic m-nisoldipine, a dihydropyridine calcium ion antagonist.
  Annales pharmaceutiques francaises · 2018 · Li K, Gbabode G, Coquerel G, et al.
  PMID 29798781DOI 10.1016/j.pharma.2018.03.010
• Comparative study of nisoldipine-loaded nanostructured lipid carriers and solid lipid nanoparticles for oral delivery: preparation, characterization, permeation and pharmacokinetic evaluation.
  Artificial cells, nanomedicine, and biotechnology · 2018 · Dudhipala N, Janga KY, Gorre T, et al.
  PMID 29688077DOI 10.1080/21691401.2018.1465068
• Effects of m-nisoldipine on the activity and mRNA expression of four CYP isozymes in rats.
  Xenobiotica; the fate of foreign compounds in biological systems · 2018 · Sun Y, Liu Y, Zhang X, et al.
  PMID 28756727DOI 10.1080/00498254.2017.1358831
• Comparative evaluation of proliposomes and self micro-emulsifying drug delivery system for improved oral bioavailability of nisoldipine.
  International journal of pharmaceutics · 2016 · Nekkanti V, Rueda J, Wang Z, et al.
  PMID 27041124DOI 10.1016/j.ijpharm.2016.03.065

The 6 most recently updated of 6 ClinicalTrials.gov registrations naming Nisoldipine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• ACEI or ARB and COVID-19 Severity and Mortality in US Veterans
  Completed · Observational · 22,213 enrolled · University of Utah
  NCT04467931updated 2021-04-28
• Bioequivalence Study of Nisoldipine Extended-Release Tablets, 30 mg
  Completed · Phase 1 · Interventional · 78 enrolled · Mylan Pharmaceuticals Inc
  NCT00985660updated 2009-09-28
• Single-Dose Fed Bioequivalence Study of Nisoldipine Extended-Release Tablets (40 mg; Mylan) and Sular® Extended-Release Tablets (40 mg; First Horizon) in Healthy Volunteers
  Completed · Phase 1 · Interventional · 83 enrolled · Mylan Pharmaceuticals Inc
  NCT00979537updated 2009-09-18
• Fasting Bioequivalence Study of Nisoldipine Extended-Release Tablets 40 mg
  Completed · Phase 1 · Interventional · 48 enrolled · Mylan Pharmaceuticals Inc
  NCT00730197updated 2008-08-08
• Renin-Guided Therapeutics in the Management of Untreated, Uncontrolled, or Complicated Hypertension
  Completed · Interventional · 52 enrolled · Medical University of South Carolina
  NCT00684489updated 2008-05-26
• Renoprotective Effect of Nisoldipine and Lisinopril in Type 1 Diabetic Nephropathy
  Completed · Phase 4 · Interventional · 52 enrolled · Steno Diabetes Center Copenhagen
  NCT00311870updated 2006-04-06

Frequently asked questions

How does Nisoldipine work?

Nisoldipine is a member of the dihydropyridine class of calcium channel antagonists (calcium ion antagonists or slow channel blockers) that inhibit the transmembrane influx of calcium into vascular smooth muscle and cardiac muscle. It reversibly competes with other dihydropyridines for binding to the calcium channel.

What is Nisoldipine used for?

According to FDA labeling, Nisoldipine carries indications including: SULAR is indicated for the treatment of hypertension. It may be used alone or in combination with other anti-hypertensive agents.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Nisoldipine?

Nisoldipine is classified as Dihydropyridine derivatives, Dihydropyridine Calcium Channel Blocker, Calcium Channel Antagonists, L-Calcium Channel Receptor Antagonists, Coronary Arterial Vasodilation, Decreased Blood Pressure.

What are the brand names for Nisoldipine?

Nisoldipine is marketed under brand names including Sular.

What are the contraindications for Nisoldipine?

Nisoldipine labeling lists contraindications including: SULAR is contraindicated in patients with known hypersensitivity to dihydropyridine calcium channel blockers.. Always consult the full prescribing information and a clinician.