VELORIN Film-coated tablet Ref.[28201] Active ingredients: Atenolol

Source: Υπουργείο Υγείας (CY)  Revision Year: 2019  Publisher: Remedica Ltd, Aharnon Str., Limassol Industrial Estate, 3056 Limassol, Cyprus

5.1. Pharmacodynamic properties

Pharmacotherapeutic group: Beta blocking agents
ATC code: C07AB03

Mechanism of action

Atenolol is a beta–blocker which is beta1-selective (i.e. acts preferentially on beta1-adrenergic receptors in the heart). Selectivity decreases with increasing dose.

Atenolol is without intrinsic sympathomimetic and membrane stabilising activities and as with other beta-blockers, has negative inotropic effects (and is therefore contraindicated in uncontrolled heart failure).

As with other beta-blockers, the mode of action of atenolol in the treatment of hypertension is unclear.

It is probably the action of atenolol in reducing cardiac rate and contractility which makes it effective in eliminating or reducing the symptoms of patients with angina.

It is unlikely that any additional ancillary properties possessed by S (-) atenolol, in comparison with the racemic mixture, will give rise to different therapeutic effects.

Clinical efficacy and safety

Velorin is effective and well-tolerated in most ethnic populations although the response may be less in black patients.

Velorin is effective for at least 24 hours after a single oral dose. The drug facilitates compliance by its acceptability to patients and simplicity of dosing.

Velorin is compatible with diuretics, other hypotensive agents and antianginals (see section 4.5).

5.2. Pharmacokinetic properties

Absorption

Absorption of Atenolol following oral dosing is consistent but incomplete (approximately 40-50%) with peak plasma concentrations occurring 2-4 hours after dosing. The Atenolol blood levels are consistent and subject to little variability. There is no significant hepatic metabolism of atenolol and more than 90% of that absorbed reaches the systemic circulation unaltered.

Distribution

Atenolol penetrates tissues poorly due to its low lipid solubility and its concentration in brain tissue is low. Plasma protein binding is low (approximately 3%).

Elimination

The plasma half-life is about 6 hours but this may rise in severe renal impairment since the kidney is the major route of elimination.

5.3. Preclinical safety data

Atenolol is a drug on which extensive clinical experience has been obtained. Relevant information for the prescriber is provided elsewhere in the Summary of Product Characteristics.

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