País: Canadá
Língua: inglês
Origem: Health Canada
LABETALOL HYDROCHLORIDE
JUNO PHARMACEUTICALS CORP.
C07AG01
LABETALOL
5MG
SOLUTION
LABETALOL HYDROCHLORIDE 5MG
INTRAVENOUS
100
Prescription
Active ingredient group (AIG) number: 0116170002; AHFS:
APPROVED
2023-06-26
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; Leia o documento completo