Source: Υπουργείο Υγείας (CY) Revision Year: 2014 Publisher: HEXAL AG, Industriestraße 25, D-83607 Holzkirchen Telephone: +49 (0) 80 24/908-0 Telefax: +49 (0) 80 24/908-1290 e-mail: service@hexal.de Distributor in Cyprus: P.T.Hadjigeorgiou Co Ltd, P.O.Box 53158-3301, ...
Atenolol is a hydrophilic beta-adrenergic blocking agent with relative β1-selectivity (“cardiac selectivity”) without intrinsic sympathomimetic activity (ISA) and without membrane-stabilizing efficacy.
The drug lowers frequency and contractility of the heart, AV conduction velocity and plasma renin activity in dependence of the level of the sympatheticotonus. Atenolol may cause a stimulation of the tone of smooth musculature due to inhibition of β2-receptors.
After oral administration, atenolol is resorbed from the gastrointestinal tract at approx. 50%. As atenolol does not undergo first pass-metabolism, the systemic bioavailability is also approx. 50%. Maximum plasma levels are reached after 2-4 hours. Plasma protein binding is approx. 3%, relative distribution volume 0.7 l/kg.
Atenolol is metabolized to a very small extent. No active metabolites with clinical relevance develop.
Approx. 90% of the systemically available atenolol are excreted in an unchanged form via the kidneys within 48 hours. Elimination half-life of atenolol is 6-10 hours in cases of normal renal function. In case of terminal renal insufficiency, elimination half-life may increase up to 140 hours.
A bioequivalence study conducted in 1988 with 24 volunteers showed the following results for Atehexal 100 versus the reference preparation:
| test preparation | reference preparation | |
|---|---|---|
| cmax [μg/ml] maximum serum concentration | 0.51 ± 0.19 | 0.49 ± 0.22 |
| tmax [h] time of maximum serum concentration | 2.52 ± 1.02 | 2.46 ± 0.98 |
| AUC [μg/ml*h] area under the concentration- versus-time curve from t=0 to infinite | 4.81 ± 1.45 | 4.51 ± 1.99 |
The values are calculated as mean values and range of scatter (standard deviation).
see point 4.9 “Overdose”.
Rats and dogs receiving atenolol in different dosages over a longer-term period (3-12 months) did not show any significant biochemical, morphologic and haematologic alterations. An increase in the myocardial and splenic weight were determined in connection with very high doses.
Atenolol has not been subject to detailed mutagenicity tests. In vitro and in vivo tests have clearly been negative to date.
Long-term trials in rats and mice did not reveal any evidence of a tumorigenic potential of atenolol.
The embryotoxic potential of atenolol was investigated in two animal species (rat and rabbit). Foetal resorptions occurred with doses below the maternal-toxic range. Malformations were not observed. A disadvantageous effect on fertility could not be ascertained.
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.
