LABETALOL HYDROCHLORIDE injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Hospira, Inc.

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Labetalol HCl injection is indicated for control of blood pressure in severe hypertension. Labetalol HCl injection is 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 injection, USP 5 mg/mL, is supplied in: Store at 20 to 25° C (68 to 77° F). [See USP Controlled Room Temperature.] Protect from freezing and light. Distributed by Hospira, Inc., Lake Forest, IL 60045 USA Novaplus is a registered trademark of Vizient, Inc. LAB-1225-2.0 Revised: 04/2018

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

LABETALOL HYDROCHLORIDE- LABETALOL HYDROCHLORIDE INJECTION, SOLUTION
HOSPIRA, INC.
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LABETALOL HYDROCHLORIDE
Injection, USP
Rx only
DESCRIPTION
Labetalol hydrochloride is an adrenergic receptor blocking agent that
has both selective alpha - and
nonselective beta-adrenergic receptor blocking actions in a single
substance.
Labetalol HCl is a racemate, chemically designated as
5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)
amino] ethyl]-salicylamide monohydrochloride, and has the following
structural formula:
Labetalol hydrochloride has the molecular formula C
H N O • HCl and a molecular weight of
364.87. 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 hydrochloride is a white or off-white crystalline powder,
soluble in water.
Labetalol hydrochloride injection is a clear, colorless to light
yellow aqueous sterile isotonic solution
for intravenous injection. It has a pH range of 3.0 to 4.5. Each mL
contains 5 mg labetalol
hydrochloride, USP, 45 mg anhydrous dextrose, 0.1 mg edetate disodium;
0.8 mg methylparaben and 0.1
mg propylparaben as preservatives; citric acid monohydrate and sodium
hydroxide, as necessary, to
bring the solution into the pH range.
CLINICAL PHARMACOLOGY
Labetalol 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
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 to block alpha-receptors in man has been
demonstrated by attenuation of the
presser effect of pheny