Nicardipine; Uses, Contraindications, Dosage, Side Effects, Interactions

Nicardipine; Uses, Contraindications, Dosage, Side Effects, Interactions

Nicardipine is a potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardio-depressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.

Nicardipine is a synthetic derivative of nitrophenyl-pyridine and potent calcium channel blocker, Nicardipine (Nifedipine Family) blocks calcium ions from certain cell walls and inhibits contraction of coronary and peripheral arteries, resulting in lowered oxygen requirements for heart muscle and decreased arterial contraction and spasm. It is used clinically as a cerebral and coronary vasodilator.

Nicardipine is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders such as chronic stable angina, hypertension, and Raynaud’s phenomenon.

Mechanism of action of Nicardipine

Nicardipine is similar to other peripheral vasodilators. Nicardipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. 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.

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine 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 Nicardipine

Contra-Indications of Nicardipine

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Dosage of Nicardipine

Strengths: 30 mg; 45 mg; 60 mg; 20 mg; 2.5 mg/mL; 20 mg/200 mL

Hypertension

Oral, Immediate release

  • Initial dose: 20 mg orally 3 times a day
  • Maintenance dose: 20 to 40 mg orally 3 times a day

Sustained release

  • Initial dose: 30 mg orally twice a day
  • Maintenance dose: 30 to 60 mg orally twice a day

IV infusion

As substitute for oral therapy:The following IV infusion rates are required to produce an average plasma level corresponding to a given oral dose at steady state:

  • 20 mg orally every 8 hours is equivalent to 0.5 mg/hour via IV infusion
  • 30 mg orally every 8 hours is equivalent to 1.2 mg/hour via IV infusion
  • 40 mg orally every 8 hours is equivalent to 2.2 mg/hour via IV infusion

For initiation of therapy in patient not receiving oral nicardipine

  • Initial dose: 5 mg/hour by IV infusion
  • The infusion rate may be increased by 2.5 mg/hour every 5 to 15 minutes (rapid and gradual titration, respectively) up to a maximum of 15 mg/hour, until desired blood pressure reduction is achieved. The infusion rate should be decreased to 3 mg/hour following achievement of the blood pressure goal using rapid titration.
  • Maintenance dose: The rate of infusion should be adjusted as needed to maintain the desired response.

Angina Pectoris Prophylaxis

Oral: Immediate release

  • Initial dose: 20 mg orally 3 times a day
  • Maintenance dose: 20 to 40 mg orally 3 times a day

Sustained release

  • Initial dose: 30 mg orally twice a day
  • Maintenance dose: 30 to 60 mg orally twice a day

IV infusion

The following IV infusion rates are required to produce an average plasma level corresponding to a given oral dose at steady state

  • 20 mg orally every 8 hours is equivalent to 0.5 mg/hr IV infusion
  • 30 mg orally every 8 hours is equivalent to 1.2 mg/hr IV infusion
  • 40 mg orally every 8 hours is equivalent to 2.2 mg/hr IV infusion
  • Initiation of therapy: 5 mg/hour by IV infusion
  • May increase by 2.5 mg/hour every 5 to 15 minutes up to a maximum of 15 mg/hour

Congestive Heart Failure

Oral, Immediate release

  • Initial dose: 20 mg orally 3 times a day
  • Maintenance dose: 20 to 40 mg orally 3 times a day
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Sustained release

  • Initial dose: 30 mg orally twice a day
  • Maintenance dose: 30 to 60 mg orally twice a day

IV infusion
The following IV infusion rates are required to produce an average plasma level corresponding to a given oral dose at steady state

  • 20 mg orally every 8 hours is equivalent to 0.5 mg/hr IV infusion
  • 30 mg orally every 8 hours is equivalent to 1.2 mg/hr IV infusion
  • 40 mg orally every 8 hours is equivalent to 2.2 mg/hr IV infusion

Initiation of therapy: 5 mg/hour by IV infusion
May increase by 2.5 mg/hour every 5 to 15 minutes up to a maximum of 15 mg/hour

Side Effects of Nicardipine

The most common 

More common

Rare

Drug Interactions of Nicardipine

Nicardipine  may interact with the following drug, supplements, & may change the efficacy of the drug

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Pregnancy Category of Nicardipine

FDA Pregnancy Category C

Pregnancy

Nicardipine falls into category C. There are no well-controlled studies in pregnant women. Nicardipine should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.

Lactation

Studies in rats have shown that nicardipine can pass into breast milk. For this reason, it is recommended that women who wish to breastfeed should not take this drug.

References

Nicardipine

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