LABETALOL HYDROCHLORIDE tablet film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Labetalol Hydrochloride (UNII: 1GEV3BAW9J) (LABETALOL - UNII:R5H8897N95)

Available from:

McKesson Contract Packaging

INN (International Name):

Labetalol Hydrochloride

Composition:

Labetalol Hydrochloride 200 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

LABETALOL HYDROCHLORIDE- LABETALOL HYDROCHLORIDE TABLET, FILM COATED
MCKESSON CONTRACT PACKAGING
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LABETALOL HYDROCHLORIDE TABLETS USP
RX ONLY
DESCRIPTION
Labetalol HCl USP tablets are adrenergic receptor blocking agents that
have both selective alpha -
adrenergic and non-selective beta-adrenergic receptor blocking actions
in a single substance.
Labetalol HCl USP is a racemate, chemically designated as
5-[1-Hydroxy-2-[(1-methyl-3-
phenylpropyl)amino]ethyl] salicylamide monohydrochloride, and it has
the following structural formula:
C
H N O •HCl M.W. 364.87
Labetalol HCl USP has two asymmetric centers and therefore exists as a
molecular complex of two
diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up
25% of racemic labetalol.
Labetalol HCl USP is a white or off-white crystalline powder, soluble
in water.
Each tablet, for oral administration, contains 100 mg, 200 mg, or 300
mg of labetalol hydrochloride,
USP. In addition, each tablet contains the following inactive
ingredients: corn starch, hypromellose,
lactose monohydrate, magnesium stearate, polyethylene glycol,
polysorbate 80, sodium starch
glycolate, titanium dioxide and colorants (100 mg: D&C yellow #10
aluminum lake and FD&C yellow
#6 aluminum lake; and 300 mg: D&C yellow #10 aluminum lake, FD&C
yellow #6 aluminum lake and
FD&C blue #1 aluminum lake).
CLINICAL PHARMACOLOGY
Labetalol HCl combines both selective, competitive alpha
-adrenergic blocking and nonselective,
competitive beta-adrenergic blocking activity in a single substance.
In man, the ratios of alpha-to beta-
blockade have been estimated to be approximately 1:3 and 1:7 following
oral and intravenous (IV)
administration, respectively. Beta - agonist activity has been
demonstrated in animals with minimal
beta -agonist (ISA) activity detected. In animals, at doses greater
than those required for alpha- or beta-
adrenergic blockade, a membrane-stabilizing effect has been
demonstrated.
PHARMACODYNAMICS
The capacity of labetalol HCl to block alpha receptors in man has been