Nisoldipine; Uses, Dosage, Side Effects, Interactions

Nisoldipine; Uses, Dosage, Side Effects, Interactions

Nisoldipine is a dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.

Nisoldipine is a dihydropyridine calcium channel blocking agent. Nisoldipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

Nisoldipine is a calcium channel blocker of the dihydropyridine class.  Nisoldipine has tropism for cardiac blood vessels. Nisoldipine is a 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction.

Mechanism of Action of Nisoldipine

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nisoldipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Indications of Nisoldipine

Contra-Indications of Nisoldipine

  • Severe Disease of the Arteries of the Heart
  • Chronic heart failure
  • Abnormally low blood pressure
  • Severely Low Blood Pressure
  • Severe liver disease
  • Allergies to Calcium Channel Blockers
  • Calcium Channel Blocking Agents-Dihydropyridines
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Dosage of Nisoldipine

Strengths: 10 mg; 20 mg; 30 mg; 40 mg; 8.5 mg; 17 mg; 25.5 mg; 34 mg

Hypertension

Slow release (old formulation)

  • Initial dose: 20 mg orally once a day
  • Maintenance dose: 10 to 60 mg orally once a day
  • Maximum dose: 60 mg/day

Controlled release (new formulation)

  • Initial dose: 17 mg orally once a day
  • Maintenance dose: 8.5 to 34 mg orally once a day
  • Maximum dose: 34 mg/day

Side Effects of Nisoldipine

The most common 

More common

Rare

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Drug Interactions of Nisoldipine

Nisoldipine  may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy Category

FDA Pregnancy Category C

Pregnancy

This medication should not be taken by women who are or may become pregnant, as nisoldipine may cause harm to the developing baby if it is taken by the mother during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

This medication should not be taken by women who are breastfeeding. The safety and effectiveness of using this medication have not been established for children.

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References

Nisoldipine

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