LABETALOL HYDROCHLORIDE- labetalol hydrochloride injection, solution

Страна: Соединенные Штаты

Язык: английский

Источник: NLM (National Library of Medicine)

Активный ингредиент:

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

Доступна с:

Breckenridge Pharmaceutical, Inc.

Администрация маршрут:

INTRAVENOUS

Тип рецепта:

PRESCRIPTION DRUG

Терапевтические показания :

Labetalol hydrochloride injection is indicated for control of blood pressure in severe hypertension. Labetalol hydrochloride 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.

Обзор продуктов:

Labetalol hydrochloride injection, USP 5 mg/mL, is supplied in: NDC 51991-934-98, 100 mg/ 20 mL Multiple Dose Vial, Carton of 1. NDC 51991-935-98, 200 mg/ 40 mL Multiple Dose Vial, Carton of 1. Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from freezing and light.

Статус Авторизация:

Abbreviated New Drug Application

Характеристики продукта

LABETALOL HYDROCHLORIDE- LABETALOL HYDROCHLORIDE INJECTION, SOLUTION
BRECKENRIDGE PHARMACEUTICAL, INC.
----------
LABETALOL HYDROCHLORIDE INJECTION, USP
RX ONLY
DESCRIPTION
Labetalol hydrochloride injection is an adrenergic receptor blocking
agent that has 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
injection is a clear, colorless to light yellow, aqueous, sterile,
isotonic solution for intravenous (IV)
injection. It has a pH range of 3.0 to 4.5. Each mL contains 5 mg
labetalol hydrochloride, USP, 45 mg
anhydrous dextrose, 0.10 mg edetate disodium; 0.80 mg of methylparaben
and 0.10 mg of propylparaben
as preservatives; and citric acid monohydrate and sodium hydroxide, as
necessary, to bring the solution
into the pH range.
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
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