(±)-Talinolol is a selective β1 adrenoceptor antagonist with cardioprotective and antihypertensive activity.
β adrenoceptor antagonist is a class of medications that are particularly used to manage cardiac arrhythmias, and to protect the heart from a second heart attack after a first heart attack.
By blocking β1-adrenergic receptors, (±)-talinolol delays the conduction of stimuli in the AV node, reduces the sino-atrial conduction time, and impedes the sinus node automaticity [1]. Pharmacokinetic data of the time course of plasma concentrations following intravenous infusion of 30 mg (±)-Talinolol revealed that the peak serum concentration (Cmax), the area under the serum concentration-time curve (AUC), and terminal elimination halflife (t1/2) were 631±95 ng/ml, 1433±153 ng×h/ml, and 10.6±3.3 h, respectively. Pharmacokinetic data of the time course of plasma concentrations following oral administration of 50 mg (±)-Talinolol revealed that the Cmax, the AUC, and the t1/2 were 168±67 ng/ml, 1321±382 ng×h/ml, and 11.9±2.4 h, respectively [2].
References:
[1] Abmann I. The actions of talinolol, a β1-selective beta blocker, in cardiac arrhythmia and acute myocardial infarction[J]. Current Medical Research and Opinion, 2008, 13(6): 325-342.
[2] Trausch B, Oertel R, Richter K, et al. Disposition and bioavailability of the β1‐adrenoceptor antagonist talinolol in man[J]. Biopharmaceutics & Drug Disposition, 1995, 16(5): 403-414.