NICARDIPINE HYDROCHLORIDE injection

Nazione: Stati Uniti

Lingua: inglese

Fonte: NLM (National Library of Medicine)

Principio attivo:

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

Commercializzato da:

Emcure Pharmaceuticals Ltd.

INN (Nome Internazionale):

NICARDIPINE HYDROCHLORIDE

Composizione:

NICARDIPINE HYDROCHLORIDE 2.5 mg in 1 mL

Via di somministrazione:

INTRAVENOUS

Tipo di ricetta:

PRESCRIPTION DRUG

Indicazioni terapeutiche:

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.

Stato dell'autorizzazione:

Abbreviated New Drug Application

Scheda tecnica

NICARDIPINE HYDROCHLORIDE - NICARDIPINE HYDROCHLORIDE INJECTION
EMCURE PHARMACEUTICALS LTD.
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RX ONLY
DESCRIPTION:
Nicardipine 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:
C
H
N O •HCl
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 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:
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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 pro