NICARDIPINE HYDROCHLORIDE � nicardipine hydrochloride injection
Sun Pharma Global Inc.
Description
Nicardipine HCl is a calcium ion influx inhibitor (slow channel blocker or calcium channel blocker). Nicardipine HCl injection for intravenous administration contains 2.5 mg/mL of nicardipine hydrochloride. Nicardipine hydrochloride is a dihydropyridine derivative with 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. 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.
Nicardipine HCl injection is available as a sterile, non-pyrogenic, clear, yellow solution in 10 mL ampuls for intravenous infusion after dilution. Each mL contains 2.5 mg nicardipine hydrochloride in Water for Injection, USP with 20 mg Sorbitol, NF, buffered to pH 3.5 with 0.525 mg citric acid monohydrate, USP and 0.09 mg sodium hydroxide, NF. Additional citric acid and/or sodium hydroxide may have been added to adjust pH.
Clinical Pharmacology
MECHANISM OF ACTION
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.
