Country: Կանադա
language: անգլերեն
source: Health Canada
BISOPROLOL FUMARATE
PRO DOC LIMITEE
C07AB07
BISOPROLOL
5MG
TABLET
BISOPROLOL FUMARATE 5MG
ORAL
100
Prescription
BETA-ADRENERGIC BLOCKING AGENTS
Active ingredient group (AIG) number: 0122418001; AHFS:
APPROVED
2008-04-03
1 PRODUCT MONOGRAPH PR PRO-BISOPROLOL – 5 PR PRO-BISOPROLOL – 10 BISOPROLOL FUMARATE TABLETS USP 5 MG, 10 MG Β-ADRENOCEPTOR BLOCKING AGENT PRO DOC LTÉE 2925, boul. Industriel Laval, Quebec H7L 3W9 SUBMISSION CONTROL NUMBER: 233100 DATE OF REVISION: November 18, 2019 Bisoprolol EN PM Pg. 1 2 PRODUCT MONOGRAPH PR PRO-BISOPROLOL – 5 PR PRO-BISOPROLOL – 10 BISOPROLOL FUMARATE TABLETS USP 5 AND 10 MG PHARMACOLOGICAL CLASSIFICATION Β-ADRENOCEPTOR BLOCKING AGENT ACTION AND CLINICAL PHARMACOLOGY Bisoprolol fumarate is a synthetic β 1 -selective (cardioselective) adrenoceptor blocking agent without significant membrane stabilizing activity or intrinsic sympathomimetic activity in its therapeutic dosage range. This preferential effect is not absolute, however, and at higher doses bisoprolol may also inhibit β 2 - adrenoceptors, located chiefly in the bronchial and vascular musculature. PHARMACODYNAMICS The most prominent effect of bisoprolol is the negative chronotropic effect, resulting in a reduction in resting and exercise heart rate. There is a fall in resting and exercise cardiac output with little observed change in stroke volume, and only a small increase in right atrial pressure, or pulmonary capillary wedge pressure at rest or during exercise. The mechanism of action of its antihypertensive effects has not been completely established. Factors which may be involved include: 1) Antagonism of β-adrenoceptors to decreased cardiac output 2) Inhibition of renin release by the kidneys 3) Diminution of tonic sympathetic outflow from the vasomotor centers in the brain In normal volunteers, bisoprolol therapy resulted in a reduction of exercise and isoproterenol- inducted tachycardia. The maximal effect occurred with 1 -4 hours post-dosing. Effects persisted for 24 hours at doses equal to or greater than 5 mg. Electrophysiology studies in man have demonstrated that bisoprolol significantly decreases heart rate, increases sinus node recovery time, prolongs AV node refractory periods, and with rapid atrial stimu read_full_document