Brands, Medical Use, Clinical Data
- Antihypertensive Agents
- Adrenergic Agents
Brands / Synonyms
Bisoprolol; Bisoprolol and Hydrochlorothiazide; Bisoprolol Fumarate; Bisoprolol fumerate; Bisoprolol Hemifumarate; Bisoprolol, Hemifumarate; Cardicor; Concor; Condyline; Condylox; Detensiel; Emconcor; Emcor; Euradal; Isoten; Monocor; Soloc; Soprol; Zebeta; Zebeta
For the management of hypertension and prophylaxis treatment of angina pectoris and heart failure.
Bisoprolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Bisoprolol is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. Activation of beta(1)-receptors (located mainly in the heart) by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Drugs such as Bisoprolol that block these receptors therefore have the reverse effect: they lower the heart rate and blood pressure and hence are used in conditions when the heart itself is deprived of oxygen. They are routinely prescribed in patients with ischemic heart disease. In addition, beta(1)-selective blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. Bisoprolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity.
Mechanism of Action
Bisoprolol selectively blocks catecholamine stimulation of beta(1)-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Bisoprolol can also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles, causing bronchospasm.
Oral, mouse: LD50 = 100 mg/kg; Skin, rabbit: LD50 = 200 mg/kg; Skin, rat: LD50 = 500 mg/kg. Symptoms of overdose include congestive heart failure (marked by sudden weight gain, swelling of the legs, feet, and ankles, fatigue, and shortness of breath), difficult or labored breathing, low blood pressure, low blood sugar, and slow heartbeat.
Biotrnasformation / Drug Metabolism
ZEBETA is contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV
block, and marked sinus bradycardia.
ZEBETA should not be combined with other beta-blocking agents. Patients receiving catecholamine-depleting drugs,
such as reserpine or guanethidine, should be closely monitored, because the added beta-adrenergic blocking action of
ZEBETA may produce excessive reduction of sympathetic activity. In patients receiving concurrent therapy with
clonidine, if therapy is to be discontinued, it is suggested that ZEBETA be discontinued for several days before the
withdrawal of clonidine.
ZEBETA should be used with care when myocardial depressants or inhibitors of AV conduction, such as certain
calcium antagonists (particularly of the phenylalkylamine [verapamil] and benzothiazepine [diltiazem] classes), or
antiarrhythmic agents, such as disopyramide, are used concurrently.
Concurrent use of rifampin increases the metabolic clearance of ZEBETA, resulting in a shortened elimination
half-life of ZEBETA. However, initial dose modification is generally not necessary. Pharmacokinetic studies document
no clinically relevant interactions with other agents given concomitantly, including thiazide diuretics, digoxin, and
cimetidine. There was no effect of ZEBETA on prothrombin time in patients on stable doses of warfarin.
Risk of Anaphylactic Reaction: While taking beta-blockers, patients with a history of severe anaphylactic reaction
to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic.
Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reactions.