Anatomical Therapeutic Chemical Classification System
Alprenolol is a non-selective beta blocker as well as a 5-HT1A and 5-HT1B receptor antagonist, used in the treatment of angina pectoris.
Atenolol is a beta-blocker which is beta1-selective, (i.e. acts preferentially on beta1-adrenergic receptors in the heart). Atenolol is without intrinsic sympathomimetic and membrane-stabilising activities and as with other beta-blockers, has negative inotropic effects.
Betaxolol is a cardioselective Beta1 receptor blocker which, when applied topically to the eye, lowers intraocular pressure. It is thought to produce this effect by reducing the rate of production of aqueous humour.
Bisoprolol is a potent highly beta1-selective-adrenoceptor blocking agent, lacking intrinsic stimulating and without relevant membrane stabilising activity.
Carvedilol is a vasodilatory non-selective beta-blocker, which reduces the peripheral vascular resistance by selective alpha1-receptor blockade and suppresses the renin-angiotensin system through non-selective beta-blockade. Plasma renin activity is reduced and fluid retention is rare.
Celiprolol is a vasoactive beta-l selective adrenoceptor antagonist with partial beta-2 agonist activity indicated in mild to moderate hypertension. The beta-2 agonist activity is thought to account for its mild vasodilating properties. It lowers blood pressure in hypertensive patients at rest and on exercise.
Esmolol is a beta-selective (cardioselective) receptor blocking agent. At therapeutic doses esmolol has no significant intrinsic sympathicomimetic activity (ISA) or membrane stabilising activity.
Labetalol lowers the blood pressure by blocking peripheral arteriolar alphaadrenoceptors thus reducing peripheral resistance, and by concurrent betablockade, protects the heart from reflex sympathetic drive that would otherwise occur.
Metoprolol is a cardioselective beta-adrenergic blocking agent. It has a relatively greater blocking effect on beta1-receptors (ie those mediating adrenergic stimulation of heart rate and contractility and release of free fatty acids from fat stores) than on beta2-receptors, which are chiefly involved in broncho and vasodilation.
Nebivolol is a racemate of two enantiomers, SRRR-nebivolol (or d-nebivolol) and RSSS-nebivolol (or l-nebivolol). It is a competitive and selective beta-receptor antagonist and it has mild vasodilating properties due to an interaction with the L-arginine/nitric oxide pathway.
Pindolol is a potent beta-adrenoceptor antagonist (beta-blocker) with uses similar to those of propranolol. It is classified as non cardioselective. It blocks both B1- and B2-adrenoceptors for more than 24 hours after administration. It has negligible membrane-stabilising activity. Pindolol exhibits low cardiodepressant activity at therapeutic dose.
Propranolol is a competitive antagonist at both beta, and beta2-adrenoceptor, but has membrane stabilising activity at concentrations exceeding 1-3mg/litre, though such concentrations are rarely achieved during oral therapy. Competitive beta-blockade has been demonstrated in man by a parallel shift to the right in the dose-heart rate response curve to beta-agonists such as isoprenaline.
D,l-sotalol is a non-selective hydrophilic β-adrenergic receptor blocking agent, devoid of intrinsic sympathomimetic activity or membrane stabilizing activity. Sotalol has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties.
Timolol is a non-selective beta-adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anaesthetic activity. Timolol reduces intra-ocular pressure, whether or not this is associated with glaucoma.