BISOPROLOL FUMARATE
| BISOPROLOL FUMARATE (bis-o-pro'lol fum'a-rate) Zebeta Classifications: beta-adrenergic antagonist; antihypertensive; Therapeutic: antihypertensive; beta-adrenergic antagonist Prototype: Propranolol Pregnancy Category: C |
Availability
5 mg, 10 mg tablets
Action
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.
Therapeutic Effect
Bisoprolol has antianginal properties, especially improving exercise tolerance. It reduces both systolic and diastolic blood pressure at rest and with exercise.
Uses
Hypertension.
Unlabeled Uses
Angina.
Contraindications
History of hypersensitivity to bisoprolol, severe sinus bradycardia, second- and third-degree AV block, overt cardiac failure, cardiogenic shock; pulmonary edema; pregnancy (category C).
Cautious Use
Asthma or COPD, peripheral vascular disease, diabetes mellitus, Prinzmetal's angina; hyperthyroidism, renal or hepatic insufficiency, cerebrovascular disease, stroke; lactation, anesthetic use.
Route & Dosage
| Hypertension, Angina Adult: PO 2.5–5 mg once daily, may increase to 20 mg/d if necessary |
Administration
Oral- 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 1–2 wk to avoid rebound, withdrawal angina, or hypertension.
- Store at room temperature, 15°–30° C (59°–86° F).
Adverse Effects (≥1%)
CNS: Dizziness, fatigue, tiredness, vertigo, anxiety, headache, sleep disturbances. CV: Bradycardia, orthostatic hypotension, rebound/withdrawal angina or hypertension following abrupt discontinuation, may exacerbate intermittent claudication. Endocrine: Increases serum levels of VLDL-C and decreases levels of HDL-C lipoproteins, may cause slight rise in serum potassium. GI: Abdominal pain, dyspepsia, nausea, vomiting, constipation, diarrhea. Respiratory: Asthma, bronchospasm, cough, dyspnea, pharyngitis, sinusitis. Skin: Rash, acne, pruritus, eczema. Other: Arthralgia.Interactions
Drug: Amiodarone 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; rifampin decreases bisoprolol blood levels.Pharmacokinetics
Absorption: Readily from GI tract; 82–94% reaches systemic circulation. Peak: Therapeutic effect 2–4 wk. Duration: 24 h. Distribution: Some CNS penetration. Metabolism: 50% in liver by CYP3A4. Elimination: 50–60% unchanged in urine. Half-Life: 10–12.4 h.Nursing Implications
Assessment & Drug Effects
- Monitor for therapeutic effectiveness. Time required to achieve optimum antihypertensive effect varies from a few days to several weeks.
- 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.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug