bisoprolol fumarate
bisoprolol fumarate
Pharmacologic class: Beta1-adrenergic blocker
Therapeutic class: Antihypertensive
Pregnancy risk category C
Action
Blocks beta1-adrenergic receptors of sympathetic nervous system in heart and kidney, thereby decreasing myocardial excitability, myocardial oxygen consumption, cardiac output, and renin release from kidney. Also lowers blood pressure without affecting beta2-adrenergic (pulmonary, vascular, and uterine) receptor sites.
Availability
Tablets: 5 mg, 10 mg
Indications and dosages
➣ Hypertension
Adults: Initially, 2.5 to 5 mg P.O. daily. Dosages up to 20 mg P.O. daily have been used.
Dosage adjustment
• Renal or hepatic impairment
Contraindications
• Hypersensitivity to drug
• Sinus bradycardia
• Second- or third-degree heart block
• Cardiogenic shock
• Heart failure
• Children (safety and efficacy not established)
Precautions
Use cautiously in:
• renal or hepatic impairment, pulmonary disease, asthma, diabetes mellitus, thyrotoxicosis, peripheral vascular disease
• patients undergoing anesthesia or major surgery
• elderly patients
• pregnant or breastfeeding patients.
Administration
• Give with or without food, but be consistent to minimize variations in absorption.
• Be aware that drug may be given alone or added to diuretic therapy.
Adverse reactions
CNS: dizziness, depression, paresthesia, sleep disturbances, hallucinations, memory loss, slurred speech
CV: bradycardia, peripheral vascular insufficiency, claudication, hypotension, sinoatrial or atrioventricular (AV) node block, second- or third-degree heart block, heart failure, pulmonary edema, cerebrovascular accident, arrhythmias
EENT: blurred vision, dry eyes, conjunctivitis, tinnitus, rhinitis, pharyngitis
GI: nausea, vomiting, diarrhea, constipation, gastric pain, gastritis, flatulence, anorexia, ischemic colitis, acute pancreatitis, renal and mesenteric arterial thrombosis
GU: dysuria, polyuria, nocturia, erectile dysfunction, Peyronie's disease, decreased libido
Hematologic: eosinophilia, agranulocytosis, thrombocytopenia
Hepatic: hepatomegaly
Metabolic: hyperglycemia, hypoglycemia
Musculoskeletal: arthralgia, muscle cramps
Respiratory: dyspnea, cough, bronchial obstruction, bronchospasm
Skin: rash, purpura, pruritus, dry skin, excessive sweating
Interactions
Drug-drug. Amphetamines, ephedrine, epinephrine, norepinephrine, phenylephrine, pseudoephedrine: unopposed alpha-adrenergic stimulation
Antihypertensives: increased hypotension
Digoxin: additive bradycardia
Dobutamine, dopamine: decrease in beneficial beta1-adrenergic cardiovascular effects
General anesthetics, I.V. phenytoin, verapamil: additive myocardial depression
MAO inhibitors: hypertension (when taken within 14 days of bisoprolol)
Nonsteroidal anti-inflammatory drugs: decreased antihypertensive effect
Thyroid preparations: decreased bisoprolol efficacy
Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, blood urea nitrogen, glucose, low-density lipoproteins,
potassium, uric acid: increased levels
Antinuclear antibodies: increased titers
Insulin tolerance test: test interference
Drug-behaviors. Acute alcohol ingestion: additive hypotension
Cocaine use: unopposed alpha-adrenergic stimulation
Patient monitoring
• Closely monitor blood glucose levels in diabetic patients.
• Assess for signs and symptoms of heart failure, including weight gain.
• Stay alert for blood pressure variations. Low blood pressure may indicate overdose.
Patient teaching
• Tell patient to weigh himself daily at same time and to report gain of 3 to 4 lb/day.
• Instruct patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from blood pressure decrease.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Advise patient to restrict salt intake to help avoid fluid retention.
• Caution patient not to discontinue drug abruptly unless prescriber approves.
• Tell patient to carry medical identification stating that he's taking a beta blocker.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.