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BisoprololSystematic (IUPAC) namemethyl}phenoxy)propyl](propan-2-yl)amineIdentifiersCAS number66722-44-9ATC codeC07AB07PubChem2405DrugBankAPRD00257ChemSpider2312Chemical dataFormulaC18H31NO4 Mol. mass325.443 g/molSMILESeMolecules & PubChemPharmacokinetic dataBioavailability>90%Protein binding30%Metabolism50% HepaticHalf life10–12 hoursExcretion ?Therapeutic considerationsLicence dataUS FDA:linkPregnancy cat.C(AU) C(US)Legal status℞ Prescription onlyRoutesoralBisoprolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type β1 adrenergic receptor blocker.// Pharmacology and biochemistry β1 SelectivityBisoprolol has a higher degree of β1-selectivity compared to other β1-selective β-blockers such as atenolol, metoprolol and betaxolol. However Nebivolol is approximately 3.5 times more β1-selective.BOO Antihypertensive effectBisoprolol has a stronger antihypertensive effect than propranolol. CardioprotectionBisoprolol in animal models has been shown to be cardioprotective. Renin-angiotensin systemBisoprolol inhibits renin secretion by about 65% and tachycardia by about 35%. Pharmacology of side-effectsIn animal testing bisoprolol compared to propranolol has shown less sedative effects and only slightly reduced glucose tolerance. Clinical UsesBisoprolol is a beta-adrenoceptor blocking drug (beta-blocker).Many beta-blockers are now available and in general they are all equally effective. There are, however, differences between them which may affect choice in treating particular diseases or individual patients.Beta-blockers with a relatively short duration of action have to be given two or three times daily. Many of these are, however, available in modified-release formulations so that administration once daily is adequate for hypertension. For angina twice-daily treatment may sometimes be needed even with a modified-release formulation. Some beta-blockers such as atenolol, bisoprolol, carvedilol, celiprolol, and nadolol have an intrinsically longer duration of action and need to be given only once daily. CautionsBeta-blockers can precipitate asthma and this effect can be dangerous. Beta-blockers should be avoided in patients with a history of asthma or bronchospasm; if there is no alternative, a cardioselective beta-blocker can be used with extreme caution under specialist supervision. Atenolol, bisoprolol, metoprolol, nebivolol, and (to a lesser extent) acebutolol, have less effect on the beta2 (bronchial) receptors and are, therefore, relatively cardioselective, but they are not cardiospecific. They have a lesser effect on airways resistance but are not free of this side-effect. Side effectsBeta-blockers are also associated with fatigue, coldness of the extremities (may be less common with those with ISA, see above), and sleep disturbances with nightmares (may be less common with the water-soluble beta-blockers, see above). DoseHypertension and angina, usually 10 mg once daily (5 mg may be adequate in some patients); max. 20 mg dailyAdjunct in stable moderate to severe heart failure, initially 1.25 mg once daily (in the morning) for 1 week then, if well tolerated, increased to 2.5 mg once daily for 1 week, then 3.75 mg once daily for 1 week, then 5 mg once daily for 4 weeks, then 7.5 mg once daily for 4 weeks, then 10 mg once daily; max. 10 mg daily IndicationsBisoprolol (Concor, Zebeta, Concore, Monocor) can be used to treat cardiovascular diseases such as hypertension, coronary heart disease, arrhythmias, ischemic heart diseases and treatment of myocardial infarction after the acute event. Patients with compensated congestive heart failure may be treated with Bisoprolol as a comedication (usually together with an ACE inhibitor, a diuretic and a digitalis-glycosid, if indicated). In patients with congestive heart failure, it reduces the need for and the consumption of oxygen of the heart muscle. It is very important to start with low doses, as bisoprolol reduces also the muscular power of the heart, which is an undesired effect in congestive heart failure.The drug is also used to treat other conditions, including dysautonomia, anxiety and hyperthyroidism (over active thyroid gland).Bisoprolol will give a positive result in doping tests.
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