CARDENE® SR
(nicardipine hydrochloride)
Sustained Release Capsules
DESCRIPTION:
CARDENE® SR (nicardipine hydrochloride) is a sustained release formulation of CARDENE®. CARDENE SR capsules for oral administration each contain 30 mg or 60 mg of nicardipine hydrochloride. Nicardipine hydrochloride is a calcium ion influx inhibitor (slow channel blocker or calcium entry blocker).
Indication: CARDENE SR is indicated for the treatment of hypertension. CARDENE SR may be used alone or in combination with other antihypertensive drugs.
Additional information about CARDENE® SR is available at www.cardenesr.com
Full Prescribing Information
Important Safety Information
CARDENE is contraindicated in patients with hypersensitivity to the drug.
Because part of the effect of CARDENE is secondary to reduced afterload, the drug is also contraindicated in patients with advanced aortic stenosis. Reduction of diastolic pressure by any means in these patients may worsen rather than improve myocardial oxygen balance.
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.
Because CARDENE decreases peripheral resistance, careful monitoring of blood pressure during the initial administration and titration of CARDENE is suggested. CARDENE, like other calcium channel blockers, may occasionally produce symptomatic hypotension. Caution is advised to avoid systemic hypotension when administering the drug to patients who have sustained an acute cerebral infarction or hemorrhage.
Since the liver is the major site of biotransformation and since CARDENE is subject to first-pass metabolism, CARDENE should be used with caution in patients having impaired liver function or reduced hepatic blood flow. Patients with severe liver disease developed elevated blood levels (fourfold increase in AUC) and prolonged half-life (19 hours) of CARDENE.
When 45-mg CARDENE SR bid was given to hypertensive patients with moderate renal impairment, mean AUC and Cmax values were approximately 2-fold to 3-fold higher than in patients with mild renal impairment. Doses in these patients must be adjusted. Mean AUC and Cmax values were similar in patients with mildly impaired renal function and normal volunteers. In patients with severe renal impairment undergoing routine hemodialysis, plasma levels following a single dose of CARDENE SR were not significantly different from those patients with mildly impaired renal function.
The most common adverse events are headache (6.2%), pedal edema (5.9%), vasodilatation (4.7%), palpitation (2.8%), nausea (1.9%), and dizziness (1.6%).
Cardene® is a registered trademark of EKR Therapeutics, Inc., Bedminster, NJ, USA.