LABETALOL HYDROCHLORIDE INJECTION SOLUTION

Country: Կանադա

language: անգլերեն

source: Health Canada

active_ingredient:

LABETALOL HYDROCHLORIDE

MAH:

JUNO PHARMACEUTICALS CORP.

ATC_code:

C07AG01

INN:

LABETALOL

dosage:

5MG

pharmaceutical_form:

SOLUTION

composition:

LABETALOL HYDROCHLORIDE 5MG

administration_route:

INTRAVENOUS

units_in_package:

100

prescription_type:

Prescription

leaflet_short:

Active ingredient group (AIG) number: 0116170002; AHFS:

authorization_status:

APPROVED

authorization_date:

2023-06-26

SPC

PRODUCT MONOGRAPH
PR
LABETALOL
HYDROCHLORIDE
INJECTION
(LABETALOL HYDROCHLORIDE)
5 MG/ML
House Standard
Antihypertensive Agent
intravenous
Juno Pharmaceuticals Corp.
402-2233 Argentia Road
Mississauga, ON L5N 2X7
Date of Initial Authorization:
June 26, 2023
Control Number: 275421
_Page 2 of 19 _
PR LABETALOL HYDROCHLORIDE INJECTION
(LABETALOL HYDROCHLORIDE)
5 mg/mL
THERAPEUTIC CLASSIFICATION
Antihypertensive
ACTION AND CLINICAL PHARMACOLOGY
Labetalol hydrochloride injection is an adrenergic receptor blocking
agent possessing both
alpha
1
(post-synaptic) and beta-receptor blocking activity. Its action on
beta-receptors is four
times stronger than that on alpha-receptors. It antagonizes beta
1
- and beta
2
-receptors equally.
The mechanism of the antihypertensive action of labetalol has not been
fully established. It is
considered that labetalol lowers blood pressure by partially blocking
the alpha-adrenoreceptors
in the peripheral arterioles, thus causing vasodilation and a
resulting reduction of peripheral
resistance. At the same time, blockade of the beta-adrenoreceptors in
the myocardium prevents
reflex
tachycardia
and
subsequent
elevation
of
cardiac
output.
Peripheral
vasodilation
is
achieved with incomplete blockade of alpha-adrenoreceptors in the
arterioles and the barostatic
reflexes remain sufficiently active to reduce the incidence of
postural hypotension.
At rest, labetalol slightly reduces the heart rate, increases the
stroke volume but does not
significantly affect cardiac output. It reduces exercise-induced
increases in systolic pressure and
heart rate, again without significantly influencing cardiac output.
Following oral administration to hypertensive patients, labetalol
decreases plasma renin activity
and aldosterone levels, both at rest and during exercise, particularly
when these were elevated
prior to treatment. Labetalol is significantly more efficacious in
hypertensive patients with high
baseline plasma noradrenaline levels.
Labetalol is metabolized mostly by conjugation with glucuronic acid;