B Adrenergic Receptor Antagonists

b Adrenergic receptor antagonists inhibit the interaction of NE, Epi, and sympathomimetic drugs with b receptors. Detailed knowledge of autonomic tone, localization of b receptor subtypes, effector-response coupling, and the multiplicity of possible actions of these drugs is essential for understanding their pharmacological effects and therapeutic uses (see Tables 6-1, 6-6, 6-7, 6-8, 10-2, 10-6, and Figure 10-3). Effects of b adrenergic antagonists may be predicted from the consequences of b receptor stimulation (generally equivalent to the effects of elevated cyclic AMP). Effects of b antagonists at a particular site depend on the level of receptor stimulation, or tone, at that site. Effects of antagonists are more prominent when receptor stimulation by agonist is high.

b antagonists can be distinguished by: relative specificity for b1 over b2 receptors, intrinsic sym-pathomimetic activity, capacity to block b receptors, differences in lipid solubility, capacity to induce vasodilation, and pharmacokinetic properties. b Adrenergic antagonists may be classified as Non-Subtype Selective (First Generation), ^-Selective (Second Generation), and Antagonists with Additional Cardiovascular Actions (Third Generation). Table 10-4 summarizes pharmacological and pharmacokinetic properties of b receptor antagonists.

Blood Pressure Health

Blood Pressure Health

Your heart pumps blood throughout your body using a network of tubing called arteries and capillaries which return the blood back to your heart via your veins. Blood pressure is the force of the blood pushing against the walls of your arteries as your heart beats.Learn more...

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