Nicardipine Hydrochloride

What it is and how it works

Mechanism of Action Nicardipine hydrochloride capsules are a calcium entry blocker (slow channel blocker or calcium ion antagonist) that inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle without changing serum calcium concentrations. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. The effects of nicardipine hydrochloride capsules are more selective to vascular smooth muscle than cardiac muscle.

Indications

INDICATIONS AND USAGE I. Stable Angina Nicardipine hydrochloride capsules are indicated for the management of patients with chronic stable angina (effort-associated angina). Nicardipine hydrochloride capsules may be used alone or in combination with beta-blockers. II. Hypertension Nicardipine hydrochloride capsules are indicated for the treatment of hypertension. Nicardipine hydrochloride capsules may be used alone or in combination with other antihypertensive drugs. In administering nicardipine hydrochloride it is important to be aware of the relatively large peak to trough differences in blood pressure effect (See DOSAGE AND ADMINISTRATION ).

Dosage and administration (summary)

DOSAGE AND ADMINISTRATION Angina The dose should be individually titrated for each patient beginning with 20 mg three times daily. Doses in the range of 20 to 40 mg three times a day have been shown to be effective. At least 3 days should be allowed before increasing the nicardipine hydrochloride capsuels dose to ensure achievement of steady-state plasma drug concentrations. Concomitant Use With Other Antianginal Agents Sublingual NTG may be taken as required to abort acute anginal attacks during nicardipine hydrochloride capsules therapy. Prophylactic Nitrate Therapy: nicardipine hydrochloride capsules may be safely coadministered with short- and long-acting nitrates.

Contraindications

CONTRAINDICATIONS Nicardipine hydrochloride capsules are contraindicated in patients with hypersensitivity to the drug. Because part of the effect of nicardipine hydrochloride capsules are secondary to reduced afterload, the drug is also contraindicated in patients with advanced aortic stenosis. Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance.

Warnings and precautions

WARNINGS Increased Angina About 7% of patients in short-term, placebo-controlled angina trials have developed increased frequency, duration or severity of angina on starting nicardipine hydrochloride capsules or at the time of dosage increases, compared with 4% of patients on placebo. Comparisons with beta-blockers also show a greater frequency of increased angina, 4% vs 1%. The mechanism of this effect has not been established (see ADVERSE REACTIONS ).

Pregnancy

Pregnancy Pregnancy Category C Nicardipine was embryocidal when administered orally to pregnant Japanese White rabbits, during organogenesis, at 150 mg/kg/day (a dose associated with marked body weight gain suppression in the treated doe) but not at 50 mg/kg/day (25 times the maximum recommended antianginal or antihypertensive dose in man).

Storage and supply

HOW SUPPLIED Nicardipine hydrochloride 20 mg capsules are available in light blue opaque/white opaque hard gelatin capsules imprinted “E501” in black ink on cap and body, filled with yellow powder.

Source: Nicardipine Hydrochloride (Nicardipine Hydrochloride) — US FDA prescribing information, 2019-01-07, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.