BLOCATENSCopy

• DRUGBANK - Bisoprolol
• indication:

  For the management of hypertension and prophylactic treatment of angina pectoris and heart failure.

• pharmacology:

• mechanism:

  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.

• toxicity:

  Oral, mouse: LD<sub>50</sub> = 100 mg/kg; Skin, rabbit: LD<sub>50</sub> = 200 mg/kg; Skin, rat: LD<sub>50</sub> = 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.

• absorprion:

  80%

• halflife:

  9-12 hours

• roouteelimination:

  The plasma elimination half-life is 9 to 12 hours and is slightly longer in elderly patients, in part because of decreased renal function in that population. Less than 2% of the dose is excreted in the feces.

• volumedistribution:

• clearance: