Nicardipine Hydrochloride (Page 2 of 5)

Electrophysiologic Effects

In general, no detrimental effects on the cardiac conduction system were seen with the use of nicardipine.

Nicardipine increased the heart rate when given intravenously during acute electrophysiologic studies, and prolonged the corrected QT interval to minor degree. The sinus node recovery times and SA conduction times were not affected by the drug. The PA, AH, and HV intervals* and the functional and effective refractory periods of the atrium were not prolonged by nicardipine and the relative and effective refractory periods of the His-Purkinje system were slightly shortened after intravenous nicardipine.

*PA = conduction time from high to low right atrium, AH = conduction time from low right atrium to His bundle deflection, or AV nodal conduction time, HV = conduction time through the His bundle and the bundle branch-Purkinje system

Renal Function

There is a transient increase in electrolyte excretion, including sodium. Nicardipine does not cause generalized fluid retention, as measured by weight changes, although 7 to 8% of the patients experience pedal edema.

Effects in Angina Pectoris

In controlled clinical trials of up to 12 weeks duration in patients with chronic stable angina, nicardipine increased exercise tolerance and reduced nitroglycerin consumption and the frequency of anginal attacks. The antianginal efficacy of nicardipine hydrochloride (20 to 40 mg) has been demonstrated in four placebo-controlled studies involving 258 patients with chronic stable angina. In exercise tolerance testing, nicardipine significantly increased time to angina, total exercise duration and time to 1 mm ST segment depression. Included among these four studies was a dose-definition study in which dose-related improvements in exercise tolerance at one and four hours post-dosing and reduced frequency of anginal attacks were seen at doses of 10, 20 and 30 mg TID. Effectiveness at 10 mg TID was, however, marginal. In a fifth placebo-controlled study, the antianginal efficacy of nicardipine was demonstrated at 8 hours post-dose (trough). The sustained efficacy of nicardipine has been demonstrated over long-term dosing. Blood pressure fell in patients with angina by about 10/8 mmHg at peak blood levels and was little different from placebo at trough blood levels.

Effects in Hypertension

Nicardipine produced dose-related decreases in both systolic and diastolic blood pressure in clinical trials. The antihypertensive efficacy of nicardipine administered three times daily has been demonstrated in three placebocontrolled studies involving 517 patients with mild to moderate hypertension. The blood pressure responses in the three studies were statistically significant from placebo at peak (1 hour post-dosing) and trough (8 hours post-dosing) although it is apparent that well over half of the antihypertensive effect is lost by the end of the dosing interval. The results from placebo controlled studies of nicardipine given three times daily are shown in the following table:

SYSTOLIC BP (mmHg) DIASTOLIC BP (mmHg)
Dose

Number

of

Mean

Peak

Mean

Trough

Trough/

Dose

Number

of

Mean

Peak

Mean

Trough

Trough/

20 mg 50 -10.3 -4.9 48% 20 mg 50 -10.6 -4.6 43%
52 -17.6 -7.9 45% 52 -9.0 -2.9 32%
30 mg 45 -14.5 -7.2 50% 30 mg 45 -12.8 -4.9 38%
44 -14.6 -7.5 51% 44 -14.2 -4.3 30%
40 mg 50 -16.3 -9.5 58% 40 mg 50 -15.4 -5.9 38%
38 -15.9 -6.0 38% 38 -14.8 -3.7 25%

The responses are shown as differences from the concurrent placebo control group. The large changes between peak and trough effects were not accompanied by observed side effects at peak response times. In a study using 24 hour intra-arterial blood pressure monitoring, the circadian variation in blood pressure remained unaltered, but the systolic and diastolic blood pressures were reduced throughout the whole 24 hours.

When added to beta-blocker therapy, nicardipine further lowers both systolic and diastolic blood pressure.

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 betablockers.

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 it is important to be aware of the relatively large peak to trough differences in blood pressure effect. (See DOSAGE AND ADMINISTRATION.)

CONTRAINDICATIONS

Nicardipine hydrochloride is contraindicated in patients with hypersensitivity to the drug.

Because part of the effect of nicardipine is 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.

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