In short-term, placebo-controlled angina trials with CARDENE (an immediate release oral dosage form of nicardipine), about 7% of patients on CARDENE (compared with 4% of patients on placebo) have developed increased frequency, duration or severity of angina. Comparisons with beta-blockers also show a greater frequency of increased angina, 4% vs 1%. The mechanism of this effect has not been established.
Although preliminary hemodynamic studies in patients with congestive heart failure have shown that CARDENE reduced afterload without impairing myocardial contractility, it has a negative inotropic effect in vitro and in some patients. Caution should be exercised when using the drug in congestive heart failure patients, particularly in combination with a beta-blocker.
CARDENE is not a beta-blocker and therefore gives no protection against the dangers of abrupt beta-blocker withdrawal; any such withdrawal should be by gradual reduction of the dose of beta-blocker, preferably over 8 to 10 days.
There is currently no manufacturer warning information available for this drug.
CARDENE SR is indicated for the treatment of hypertension. CARDENE SR may be used alone or in combination with other antihypertensive drugs.
CARDENE® SR is a sustained release formulation of CARDENE®. CARDENE SR capsules for oral administration each contain 30 mg, 45 mg or 60 mg of nicardipine hydrochloride. Nicardipine hydrochloride is a calcium ion influx inhibitor (slow channel blocker or calcium entry blocker).
Nicardipine hydrochloride is a dihydropyridine derivative with the IUPAC (International Union of Pure and Applied Chemistry) chemical name (±)-2-(benzyl-methyl amino)ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate monohydrochloride, and it has the following structure:
Nicardipine hydrochloride is a greenish-yellow, odorless, crystalline powder that melts at about 169°C. It is freely soluble in chloroform, methanol and glacial acetic acid, sparingly soluble in anhydrous ethanol, slightly soluble in n-butanol, water, 0.01 M potassium dihydrogen phosphate, acetone and dioxane, very slightly soluble in ethyl acetate, and practically insoluble in benzene, ether and hexane. It has a molecular weight of 515.99.
CARDENE SR is available in hard gelatin capsules containing 30 mg, 45 mg or 60 mg nicardipine hydrochloride. All strengths contain a two component capsule fill. A powder component containing 25% of total nicardipine hydrochloride dose contains pregelatinized starch and magnesium stearate as inactive ingredients. A spherical granule component containing 75% of total nicardipine hydrochloride dose also contains microcrystalline cellulose, starch, lactose and methacrylic acid copolymer Type C as inactive ingredients.
The colorants used in the 30-mg capsules are titanium dioxide, FD&C Red No. 40 and red iron oxide, and the colorants used in the 45-mg and 60-mg capsules are titanium dioxide and FD&C Blue No. 2.
