LABETALOL HYDROCHLORIDE- labetalol hydrochloride tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

LABETALOL HYDROCHLORIDE (UNII: 1GEV3BAW9J) (LABETALOL - UNII:R5H8897N95)

Available from:

REMEDYREPACK INC.

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Labetalol Hydrochloride Tablets are indicated in the management of hypertension. Labetalol Hydrochloride Tablets may be used alone or in combination with other antihypertensive agents, especially thiazide and loop diuretics. Labetalol Hydrochloride Tablets are contraindicated in bronchial asthma, overt cardiac failure, greater-than-first-degree heart block, cardiogenic shock, severe bradycardia, other conditions associated with severe and prolonged hypotension, and in patients with a history of hypersensitivity to any component of the product (see WARNINGS). Beta-blockers, even those with apparent cardioselectivity, should not be used in patients with a history of obstructive airway disease, including asthma.

Product summary:

Labetalol Hydrochloride Tablets, 100 mg, light orange, round, scored, film-coated tablets debossed on one side with "CL 37" and "100", bottles of 100 (NDC 43199-037-01) and bottles of 500 (NDC 43199-037-05) Labetalol Hydrochloride Tablets, 200 mg, white, round, scored, film-coated tablets debossed on one side with "CL 38" and "200", bottles of 100 (NDC 43199-038-01) and bottles of 500 (NDC 43199-038-05) Labetalol Hydrochloride Tablets, 300 mg, mid-orange, round, scored, film-coated tablets debossed on one side with "CL 39" and "300", bottles of 100 (NDC 43199-039-01). Labetalol Hydrochloride Tablets should be stored between 2° and 30°C (36° and 86°F).

Authorization status:

New Drug Application

Summary of Product characteristics

LABETALOL HYDROCHLORIDE- LABETALOL HYDROCHLORIDE TABLET
REMEDYREPACK INC.
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LABETALOL HYDROCHLORIDE TABLETS
DESCRIPTION
Labetalol Hydrochloride Tablets are adrenergic receptor blocking
agents that have both selective alpha
-adrenergic and nonselective beta-adrenergic receptor blocking actions
in a single substance.
Labetalol hydrochloride (HCl) is a racemate chemically designated as
2-hydroxy-5-[1-hydroxy-2-[(1-
methyl-3-phenylpropyl)amino]ethyl]benzamide monohydrochloride, and it
has the following structure:
Labetalol HCl has the empirical formula C
H
N
O
·HCl and a molecular weight of 364.9. It 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 is a white or off-white crystalline powder, soluble in
water.
Labetalol Hydrochloride Tablets contain 100 mg, 200 mg, or 300 mg of
labetalol HCl and are taken
orally. The tablets also contain the inactive ingredients corn starch,
FD&C Yellow No. 6 (100 mg- and
300mg tablets only), hydroxypropyl methylcellulose, lactose, magnesium
stearate, pregelatinized corn
starch, sodium benzoate (200-mg tablet only), talc (100-mg tablet
only), and titanium dioxide.
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
demonstrated by attenuation of
the pressor effect of phenylephrine and by a significant reduction