Nicardipine

• CARDENE I.V. is a calcium channel blocker indicated for the short-term treatment of hypertension in adults when oral therapy is not feasible.

Nicardipine 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 are more selective to vascular smooth muscle than cardiac muscle. In animal models, nicardipine produced relaxation of coronary vascular smooth muscle at drug levels which cause little or no negative inotropic effect.

• For Intravenous Use. • No further dilution is required. • When substituting for oral nicardipine therapy, use the intravenous infusion rate from the table below: Oral CARDENE Dose Equivalent I.V. Infusion Rate (0.1 mg/mL) Equivalent I.V. Infusion Rate (0.2 mg/mL) 20 mg q8h 0.5 mg/hr = 5 mL/hr 0.5 mg/hr = 2.5 mL/hr 30 mg q8h 1.2 mg/hr = 12 mL/hr 1.2 mg/hr = 6 mL/hr 40 mg q8h 2.2 mg/hr = 22 mL/hr 2.2 mg/hr = 11 mL/hr • In a patient not receiving oral nicardipine, initiate therapy at 5 mg/hr. Increase the infusion rate by 2.5 mg/hr every 5 minutes (for rapid titration) to 15 minutes (for gradual titration) up to a maximum of 15 mg/hr until desired blood pressure reduction is achieved. Conversion Table (mg/hr) Equivalent I.V.

• Do not use in patients with advanced aortic stenosis. Advanced Aortic Stenosis CARDENE I.V. is contraindicated in patients with advanced aortic stenosis because part of the effect of CARDENE I.V. is secondary to reduced afterload. Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance.

• Closely monitor response in patients with angina, heart failure, impaired hepatic function, or renal impairment. • To reduce the possibility of venous thrombosis, phlebitis, and vascular impairment, do not use small veins, such as those on the dorsum of the hand or wrist. Exercise extreme care to avoid intra-arterial administration or extravasation. • To minimize the risk of peripheral venous irritation, change the site of infusion of CARDENE I.V. every 12 hours.

Most common adverse reactions: are headache (15%), hypotension (6%), tachycardia (4%) and nausea/vomiting (5%).

• Cimetidine increases oral nicardipine plasma levels. • Oral or intravenous nicardipine may increase cyclosporine and tacrolimus plasma levels. Frequent monitoring of trough blood levels of cyclosporine and tacrolimus is recommended when co-administering CARDENE I.V.

Store at controlled room temperature 20º to 25ºC (68º to 77ºF), refer to USP Controlled Room Temperature. Protect from freezing. Protect from light, store in carton until ready to use.