Bisoprolol: a new beta-adrenoceptor blocking drug. 1987

B N Prichard
Department of Clinical Pharmacology, University College London, U.K.

Bisoprolol is a new highly beta 1-selective beta-adrenoceptor blocking drug; it is devoid of intrinsic sympathomimetic effects. Its haemodynamic effects are those expected from beta 1-blockade, heart rate is reduced at rest and on exercise, cardiac output falls and peripherial resistance is increased. Consequent on the beta 1-selectivity there is much greater inhibition of exercise tachycardia compared to inhibition of isoprenaline-induced falls of diastolic blood pressure, in contrast to propranolol. Studies in asthmatics confirm the selectivity of bisoprolol. Bisoprolol has similar solubility in water and organic solvents and predictably therefore about half is excreted by the kidneys unchanged, half metabolized by the liver. Estimates of half-life average about 10-12 h, this is in accord with the therapeutic efficacy of once daily administration. Therapeutic studies have demonstrated the efficacy of bisoprolol in angina pectoris, arrhythmias and hypertension. Comparative studies against atenolol and verapamil in angina suggest similar efficacy. In hypertension a similar antihypertensive effect to nifedipine has been found, while a significantly greater lowering of blood pressure was seen than that obtained with a diuretic. Some studies have also suggested more consistent antihypertensive effect from bisoprolol than atenolol 24 h after administration. This may have been a dosage phenomenon or reflects the longer plasma elimination half-life of bisoprolol, and requires confirmation. Bisoprolol has a favourable side-effect profile.

UI MeSH Term Description Entries
D011412 Propanolamines AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives. Aminopropanols
D006439 Hemodynamics The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM. Hemodynamic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000319 Adrenergic beta-Antagonists Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety. Adrenergic beta-Antagonist,Adrenergic beta-Receptor Blockader,Adrenergic beta-Receptor Blockaders,beta-Adrenergic Antagonist,beta-Adrenergic Blocker,beta-Adrenergic Blocking Agent,beta-Adrenergic Blocking Agents,beta-Adrenergic Receptor Blockader,beta-Adrenergic Receptor Blockaders,beta-Adrenoceptor Antagonist,beta-Blockers, Adrenergic,beta-Adrenergic Antagonists,beta-Adrenergic Blockers,beta-Adrenoceptor Antagonists,Adrenergic beta Antagonist,Adrenergic beta Antagonists,Adrenergic beta Receptor Blockader,Adrenergic beta Receptor Blockaders,Adrenergic beta-Blockers,Agent, beta-Adrenergic Blocking,Agents, beta-Adrenergic Blocking,Antagonist, beta-Adrenergic,Antagonist, beta-Adrenoceptor,Antagonists, beta-Adrenergic,Antagonists, beta-Adrenoceptor,Blockader, Adrenergic beta-Receptor,Blockader, beta-Adrenergic Receptor,Blockaders, Adrenergic beta-Receptor,Blockaders, beta-Adrenergic Receptor,Blocker, beta-Adrenergic,Blockers, beta-Adrenergic,Blocking Agent, beta-Adrenergic,Blocking Agents, beta-Adrenergic,Receptor Blockader, beta-Adrenergic,Receptor Blockaders, beta-Adrenergic,beta Adrenergic Antagonist,beta Adrenergic Antagonists,beta Adrenergic Blocker,beta Adrenergic Blockers,beta Adrenergic Blocking Agent,beta Adrenergic Blocking Agents,beta Adrenergic Receptor Blockader,beta Adrenergic Receptor Blockaders,beta Adrenoceptor Antagonist,beta Adrenoceptor Antagonists,beta Blockers, Adrenergic,beta-Antagonist, Adrenergic,beta-Antagonists, Adrenergic,beta-Receptor Blockader, Adrenergic,beta-Receptor Blockaders, Adrenergic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D017298 Bisoprolol A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. Bisoprolol Fumarate,Bisoprolol Fumarate (1:1) Salt, (+-)-Isomer,Bisoprolol Fumarate (2:1) Salt, (+-)-Isomer,Bisoprolol Hydrochloride,Bisoprolol Methanesulfonate Salt,Bisoprolol, (+-)-Isomer,Bisoprolol, (-)-Isomer,Bisoprolol, Fumarate (1:1) Salt,Bisoprolol, Fumarate (2:1) Salt,CL-297939,Concor,EMD-33512,CL 297939,CL297939,EMD 33512,EMD33512,Fumarate, Bisoprolol,Hydrochloride, Bisoprolol

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