Source: Υπουργείο Υγείας (CY) Revision Year: 2014 Publisher: MEDOCHEMIE LTD, 1-10 Constantinoupoleos street, 3011 Limassol, Cyprus
Pharmacotherapeutic group: Beta blocking agents, selective, Beta Blocking Agents
ATC code: C07AB03
It is a beta-adrenoceptor blocking drug which acts preferentially on beta1-adrenergic receptors in the heart, it is beta1-selective. Selectivity decreases with increasing dose. It has no intrinsic sympathomimetic or membrane stabilizing properties and has negative inotropic effects.
The mode of action in the treatment of hypertension is unclear; in angina it is probably the effect of atenolol in reducing cardiac rate and contractility that make it effective.
Absorption of atenolol following oral administration is consistent, with some subject variability, but incomplete, being some 40-50%, with peak plasma concentrations occurring 2-4 hours post dose. The blood levels of atenolol are consistent and have little variability. Hepatic metabolism is not significant and about 90% of the absorbed atenolol reaches the systemic circulation unaltered. Plasma half life is about 6 hours, as the kidney is the main route of elimination this can be prolonged in renal impairment. As would be predicted from the chemistry, atenolol is poorly lipid soluble and brain tissue concentration is low. It has low plasma protein binding, about 3%. It crosses the placenta and is found in breast milk of lactating women.
As atenolol is a well established drug, and no novel pharmaceutical excipients are used in this formulation, there is no additional preclinical safety data.
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