METHYLDOPATE HYDROCHLORIDE injection solution

Maa: Yhdysvallat

Kieli: englanti

Lähde: NLM (National Library of Medicine)

Aktiivinen ainesosa:

METHYLDOPATE HYDROCHLORIDE (UNII: 7PX435DN5A) (METHYLDOPA ANHYDROUS - UNII:M4R0H12F6M)

Saatavilla:

American Regent, Inc.

INN (Kansainvälinen yleisnimi):

METHYLDOPATE HYDROCHLORIDE

Koostumus:

METHYLDOPATE HYDROCHLORIDE 50 mg in 1 mL

Prescription tyyppi:

PRESCRIPTION DRUG

Valtuutuksen tilan:

Abbreviated New Drug Application

Valmisteyhteenveto

METHYLDOPATE HYDROCHLORIDE- METHYLDOPATE HYDROCHLORIDE INJECTION,
SOLUTION
AMERICAN REGENT, INC.
----------
METHYLDOPATE
HCL INJECTION, USP
DESCRIPTION
Methyldopate HCl Injection, USP, is an antihypertensive agent for
intravenous use. Sterile,
nonpyrogenic.
Methyldopate hydrochloride
[levo-3-(3,4-dihydroxyphenyl)-2-methylalanine, ethyl ester
hydrochloride] is the ethyl ester of methyldopa, supplied as the
hydrochloride salt with a molecular
weight of 275.73. Methyldopate hydrochloride is more soluble and
stable in solution than methyldopa
and is the preferred form for intravenous use.
The molecular formula for Methyldopate hydrochloride is C
H NO ·HCl and the structural formula
is:
Each mL contains:
Methyldopate Hydrochloride ......... 50 mg
Citric Acid (Anhydrous) ................. 5 mg
Edetate Disodium ......................... 0.5 mg
Monothioglycerol ........................... 2 mg
Water for Injection ................q.s. to 1 mL
Methylparaben 1.5 mg and Propylparaben 0.2 mg added as preservatives,
Sodium Bisulfite 3.2 mg added
as an antioxidant. pH adjusted with Sodium Hydroxide and/or
Hydrochloric Acid.
CLINICAL PHARMACOLOGY
Methyldopate, an antihypertensive agent, is an aromatic-amino-acid
decarboxylase inhibitor in animals
and in man. Although the mechanism of action has yet to be
conclusively demonstrated, the
antihypertensive effect of methyldopa probably is due to its
metabolism to alpha-methyl-norepinephrine,
which then lowers arterial pressure by stimulation of central
inhibitory alpha-adrenergic receptors,
false neurotransmission, and/or reduction of plasma renin activity.
Methyldopa has been shown to cause
a net reduction in the tissue concentration of serotonin, dopamine,
norepinephrine, and epinephrine.
Only methyldopa, the L-isomer of alpha-methyldopa, has the ability to
inhibit dopa decarboxylase and to
deplete animal tissues of norepinephrine. In man, the antihypertensive
activity appears to be due solely
to the L-isomer. About twice the dose of the racemate
(DL-alpha-methyldopa) is required