Classifications: beta-adrenergic antagonist; antihypertensive; Therapeutic: antihypertensive; beta-adrenergic antagonist
Pregnancy Category: C
5 mg, 10 mg tablets
Long-acting cardioselective (beta1) adrenoreceptor blocking agent. To maintain beta1 cardioselectivity, the lowest effective dose is necessary. Bisoprolol decreases heart rate, blood pressure, contractile
force, and cardiac workload, which reduces myocardial oxygen consumption and increases blood flow to myocardium.
Bisoprolol has antianginal properties, especially improving exercise tolerance. It reduces both systolic and diastolic blood
pressure at rest and with exercise.
History of hypersensitivity to bisoprolol, severe sinus bradycardia, second- and third-degree AV block, overt cardiac failure,
cardiogenic shock; pulmonary edema; pregnancy (category C).
Asthma or COPD, peripheral vascular disease, diabetes mellitus, Prinzmetal's angina; hyperthyroidism, renal or hepatic insufficiency,
cerebrovascular disease, stroke; lactation, anesthetic use.
Route & Dosage
Adult: PO 2.55 mg once daily, may increase to 20 mg/d if necessary
- Note: The half life of the drug is increased in those with significant liver dysfunction; usual initial dose is 2.5 mg and may
be carefully titrated upward if necessary.
- Discontinue drug gradually over a period of 12 wk to avoid rebound, withdrawal angina, or hypertension.
- Store at room temperature, 15°30° C (59°86° F).
Adverse Effects (≥1%)CNS:
, tiredness, vertigo, anxiety, headache, sleep disturbances. CV:
Bradycardia, orthostatic hypotension, rebound/withdrawal angina or hypertension following abrupt discontinuation, may exacerbate
intermittent claudication. Endocrine:
levels of VLDL-C and decreases levels of HDL-C lipoproteins, may cause slight rise in serum
Abdominal pain, dyspepsia, nausea, vomiting, constipation
. Respiratory: Asthma
, bronchospasm, cough, dyspnea
, pharyngitis, sinusitis
, pruritus, eczema
. Other: Arthralgia
may cause significant bradycardia; beta blockers
may reduce glucose
tolerance, inhibit insulin
secretion, alter rate of recovery from hypoglycemia
, reduce peripheral circulation, and suppress hypoglycemic symptoms
decreases bisoprolol blood levels.
Readily from GI tract; 8294% reaches systemic circulation. Peak:
Therapeutic effect 24 wk. Duration:
24 h. Distribution:
50% in liver by CYP3A4. Elimination:
5060% unchanged in urine. Half-Life:
Assessment & Drug Effects
- Monitor for therapeutic effectiveness. Time required to achieve optimum antihypertensive effect varies from a few days to
- Monitor BP frequently during periods of dose adjustment or drug withdrawal.
- Monitor for activity-induced angina both during therapy and following discontinuation of drug.
- Monitor for and report severe hypotension and bradycardia. Dosage adjustment may be required.
- Monitor for bronchospasms in patients with a history of asthma or COPD.
- Monitor diabetics for loss of glycemic control.
- Lab tests: Periodic CBC, electrolytes, renal function, liver function, lipid profile.
Patient & Family Education
- Report orthostatic hypotension and dizziness to physician.
- Do not discontinue drug abruptly unless specifically instructed to do so.
- Note: Drug-induced nightmares and unpleasant dreams are possible when taking this drug.
- Monitor blood glucose for loss of glycemic control.
- Report cold extremities and development of symptoms of intermittent claudication to physician.