Nisoldipine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Syscor; Belgium: Sular, Syscor; Finland: Syscor; Germany: Baymycard; Greece: Syscor; Hungary: Baymycard; Italy: Syscor; Luxembourg: Syscor; Spain: Sular, Syscor.

North America

USA: Nisoldipine, Sular.

Latin America

Brazil: Syscor.

Asia

Japan: Baymycard, Nikameal, Ninobarucin, Nisoldipine, Riohard.

Drug combinations

Chemistry

Nisoldipine: C~20~H~24~N~2~O~6~. Mw: 388.41. (1) 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, methyl 2-methylpropyl ester, (±)-; (2)(±)-Isobutyl methyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-pyridinedicarboxylate. CAS-63675-72-9 (1981).

Pharmacologic Category

Calcium-Channel Blocking Agents; Dihydropyridines. (ATC-Code: C08CA07).

Mechanism of action

As a dihydropyridine calcium channel blocker, structurally similar to nifedipine, nisoldipine impedes movement of calcium ions into vascular smooth muscle and cardiac muscle. Dihydropyridines are potent vasodilators and not as likely to suppress cardiac contractility and slow cardiac conduction as other calcium antagonists such as verapamil and diltiazem. Nisoldipine is 5-10 times as potent vasodilator as nifedipine.

Therapeutic use

Management of hypertension, alone or in combination with other antihypertensive agents.

Pregnancy and lactiation implications

Animal studies demonstrated fetotoxic but not teratogenic effects. There are no adequate, well-controlled studies in pregnant women. Use during pregnancy only if potential benefit to mother outweighs potential risk to fetus. Excretion in breast milk unknown (not recommended in nursing women).

Unlabeled use

Contraindications

Hypersensitivity to nisoldipine, any component of the formulation, or other dihydropyridine calcium channel blockers.

Warnings and precautions

Increased angina and/or MI occurred with initiation or dosage titration of calcium channel blockers. Symptomatic hypotension with or without syncope can rarely occur. Most common side-effect is peripheral edema. Use with caution in severe aortic stenosis, in heart failure, in severe hepatic impairment, and in HCM and outflow tract obstruction since reduction in afterload may worsen symptoms associated with this condition.

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