Drug information of Nicardipine

Nicardipine

Drug group:

A potent calcium channel blockader with marked vasodilator action.

Mechanism of effect

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.

Pharmacodynamic

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.

Pharmacokinetics

Bioavailability: 35%

Onset: PO, 0.5-2 hr; IV, 10-20 min

Duration: Immediate release and IV, 8 hr; extended release, 8-12 hr

Peak plasma time: Immediate release, 0.5-2 hr; extended release, 2-4 hr

Protein bound: 95%

Vd: 8.3 L/kg

Metabolism

Metabolized in liver by CYP3A4 (first pass)

Metabolites: Pyridine analogue (inactive)

Half-life: 2-4 hr

Dialyzable: HD, no

Total plasma clearance: IV, 0.3-0.9 L/hr/kg; PO, 1.62-7.86 L/hr/kg

Excretion: Urine (60%), feces (35%)

Drug indications

Hypertension

Dosage

Adult

Hypertension

PO: 20-40 mg (conventional) q8hr or 30-60 mg (extended release) q12hr

IV: 5 mg/hr by slow infusion (50 mL/hr) initially; may be increased by 2.5 mg/hr every 15 minutes; not to exceed 15 mg/hr

IV as substitute for conventional PO

  • PO dose: 20 mg q8hr; equivalent IV infusion: 0.5 mg/hr
  • PO dose: 30 mg q8hr; equivalent IV infusion: 1.2 mg/hr
  • PO dose: 40 mg q8hr; equivalent IV infusion: 2.2 mg/hr
  • If transitioning to PO nicardipine, initiate PO dosing 1 hr before discontinuance of IV

Chronic Stable Angina

20-40 mg (conventional) PO q8hr

Start at 20 mg, and allow 3 days between dose increases to achieve steady-state plasma drug concentration; usual dosage range, 60-120 mg/day

Pediatric

Hypertension (Off-label)

Not approved by FDA; limited data available

0.5-3 mcg/kg/min IV

Drug contraindications

Aortic Stenosis

Alerts

May cause symptomatic hypotension or tachycardia; titrate slowly to avoid systemic hypotension and possible negative inotropic effects with congestive heart failure (CHF), angina, and left ventricular dysfunction (particularly during treatment initiation, after dose increase, or after withdrawal of beta blocker)

To reduce possibility of venous thrombosis, phlebitis, and vascular impairment, do not use small veins, such as those on dorsum of hand or wrist; avoid intraarterial administration or extravasation

Caution should be exercised when using the drug in congestive heart failure patients, particularly in combination with a beta-blocker; nicardipine gives no protection against dangers of abrupt beta-blocker withdrawal; any such withdrawal should be by gradual reduction of dose of beta-blocker, preferably over 8 to 10 days

Closely monitor response in patients with angina, congestive heart failure, impaired hepatic function, portal hypertension, and renal impairment and pheochromocytoma

Peripheral edema may occur

Exacerbation of angina or MI reported with dosage titration of dihydropyridine calcium-channel blockers

With acute cerebral infarction or hemorrhage, titrate slowly to avoid systemic hypotension

Use with caution in patients with hypertrophic cardiomyopathy and mild-to-moderate aortic stenosis

Use with caution in hepatic or renal impairment; lower doses may be required

Use with caution in hypertension associated with pheochromocytoma and portal hypertension when administering IV

Change infusion site every 12 hr to minimize risk of peripheral venous irritation

Blood pressure starts to fall within min of infusion; calcium channel blockers, may occasionally produce symptomatic hypotension; caution is advised to avoid systemic hypotension when administering drug to patients who have sustained acute cerebral infarction or hemorrhage

Extended-release form not recommended for angina

Points of recommendation

Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose. Use the medicine exactly as directed.

Do not crush, chew, break, or open an extended-release capsule. Swallow it whole.

You may have more severe or more frequent episodes of angina when you first start taking nicardipine, or whenever your doses are changed.

Your blood pressure will need to be checked often.

Do not stop using any of your medications suddenly. Stopping suddenly may make your condition worse.

Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

Pregnancy level

C


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