Optimal features of a new beta-blocker.
Therapeutics involves the careful balance between treatment disadvantages and advantages--the so-called risk-benefit ratio. Even after 20 years beta-blockers must be selected carefully to suit the patient's needs. This review examines several problems associated with beta-blockade. Generally, beta1-cardioselectivity is considered advantageous, but properties such as partial agonist activity, which limits receptor up-regulation, might be of greater value in reducing the adverse effects associated with abrupt drug withdrawal. Beta-Blockers, either lipophilic or hydrophilic agents, have specific problems: lipophilic drugs provoke adverse central nervous system effects and need careful dose titration; variable gastrointestinal absorption is common with hydrophilic agents, whereas extra care is needed in patients with renal impairment. For most patients, especially those with asymptomatic conditions, once-daily dosing is preferred. For many, the quality of life is of overriding clinical importance. Despite significant pharmacokinetic and pharmacodynamic advances, the final criteria depend largely on a clinical assessment, improvement in the quality of life, and patient preference. We still await the discovery of an ideal beta-adrenoceptor blocking agent; some of the newer beta-blockers, however have many of the properties that clinicians value.
D000318:Adrenergic beta-Agonists / Q000494:pharmacology; D000319:Adrenergic beta-Antagonists / Q000009:adverse effects / Q000627:therapeutic use; D000818:Animals; D006801:Humans; D006973:Hypertension / Q000188:drug therapy; D011943:Receptors, Adrenergic, beta / Q000187:drug effects; D012307:Risk Factors
D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D011943:Receptors, Adrenergic, beta