NICARDIPINE HYDROCHLORIDE injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

NICARDIPINE HYDROCHLORIDE (UNII: K5BC5011K3) (NICARDIPINE - UNII:CZ5312222S)

Available from:

PharmaForce, Inc.

INN (International Name):

NICARDIPINE HYDROCHLORIDE

Composition:

NICARDIPINE HYDROCHLORIDE 2.5 mg in 1 mL

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Nicardipine hydrochloride injection is indicated for the short-term treatment of hypertension when oral therapy is not feasible or not desirable. For prolonged control of blood pressure, patients should be transferred to oral medication as soon as their clinical condition permits (see DOSAGE AND ADMINISTRATION). Nicardipine hydrochloride injection is contraindicated in patients with known hypersensitivity to the drug. Nicardipine hydrochloride injection is also contraindicated in patients with advanced aortic stenosis because part of the effect of nicardipine hydrochloride injection is secondary to reduced afterload. Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance.

Product summary:

Nicardipine hydrochloride injection 25 mg/10 mL (2.5 mg/mL) single dose vials are available in cartons of 10 as follows: 25 mg/10 mL (2.5 mg/mL) – NDC 40042-047-10 Store at 20ºC to 25ºC (68ºF to 77ºF) [see USP Controlled Room Temperature]. Freezing does not adversely affect the product, but exposure to elevated temperatures should be avoided. Protect from light. Store vials in carton until used. Manufactured for: PharmaForce, Inc. Columbus, OH 43229 Revised August 2009

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

NICARDIPINE HYDROCHLORIDE - NICARDIPINE HYDROCHLORIDE INJECTION,
SOLUTION
PHARMAFORCE, INC.
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NICARDIPINE HYDROCHLORIDE INJECTION
Rx Only
DESCRIPTION
Nicardipine hydrochloride is a calcium ion influx inhibitor (slow
channel blocker or calcium channel
blocker). Nicardipine hydrochloride 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 and
has the following structure:
Nicardipine hydrochloride is a greenish-yellow, odorless, crystalline
powder that melts at about 169º
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 hydrochloride injection is available as a sterile,
non-pyrogenic, clear, yellow solution in
10 mL vials for intravenous infusion after dilution. Each mL contains
2.5 mg nicardipine hydrochloride
in water for injection, USP with 48 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