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Brand names,
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Analogs
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Brand Names Mixture
- Ziac (bisoprolol + hydrochlorothiazide)
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Chemical_Formula
C18H31NO4
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RX_link
http://www.rxlist.com/cgi/generic3/bisoprolol.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
R. Jonas et al.;U.S. pat. 4,258,062 (1978,1981)
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Molecular Weight
325.443 g/mol
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Melting Point
100 oC
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H2O Solubility
2240 mg/L
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State
Solid
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LogP
3.185
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Dosage Forms
Tablets (5 and 10 mg)
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Indication
For the management of hypertension and prophylaxis treatment of angina pectoris and heart failure.
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Pharmacology
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.
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Absorption
80%
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side effects and Toxicity
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.
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Patient Information
Patients especially those with coronary artery disease should be warned about discontinuing use of ZEBETA without
a physician's supervision. Patients should also be advised to consult a physician if any difficulty in breathing
occurs, or if they develop signs or symptoms of congestive heart failure or excessive bradycardia.
Patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents
should be cautioned that beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia,
and bisoprolol fumarate should be used with caution. Patients should know how they react to this medicine before they
operate automobiles and machinery or engage in other tasks requiring alertness.
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Organisms Affected
Humans and other mammals