BISOPROLOL FUMERATE

Indications & Dose:

Hypertension Angina 

• BY MOUTH

Adult: 5–10 mg once daily; maximum 20 mg per day

Adjunct in heart failure

• BY MOUTH

Adult: Initially 1.25 mg once daily for 1 week, dose to be taken in the morning, then increased if tolerated to 2.5 mg once daily for 1 week, then increased if tolerated to 3.75 mg once daily for 1 week, then increased if tolerated to 5 mg once daily for 4 weeks, then increased if tolerated to 7.5 mg once daily for 4 weeks, then increased if tolerated to 10 mg once daily; maximum 10 mg per day

Contraindications:

Cardiogenic shock, heart block (2nd, 3rd degree), sinus bradycardia, overt cardiac failure

Side Effects:

CNS: Catatonia, depression, dizziness, drowsiness, fatigue, hallucinations, headache, insomnia, lethargy, memory loss, mental changes, peripheral neuropathy, strange dreams, vertigo

CV: Bradycardia, CHF, cold extremities, postural hypotension, profound hypotension, 2nd or 3rd degree heart block, ventricular dysrhythmias

EENT:. Dry burning eyes, rhinitis, sinusitis, sore throat

GI: Diarrhea, flatulence, gastric pain, gastritis, increased AST/ALT (1-2 times normal in 4%), ischemic colitis, mesenteric arterial thrombosis, nausea, vomiting

GU: Decreased libido, impotence

HEME: Purpura

METAB: Azotemia, hyperglycemia, hyperkalemia, hypertriglyceridemia, hyperuricemia, increased hypoglycemic response to insulin

MS: Arthralgia, joint pain

RESP: Bronchospasm, cough, dyspnea, wheezing

SKIN: Alopecia, fever, pruritus, rash, sweating

MISC: Decreased exercise tolerance, edema, facial swelling, weight gain

Cautions:

Precautions:

Anesthesia/surgery (myocardial depression), avoid abrupt withdrawal; bronchospastic airways, congestive heart failure, diabetes mellitus, hyperthyroidism/thyrotoxicosis (bisoprolol, unlike propranolol, does not decrease T3 levels), concurrent clonidine (discontinue bisoprolol several days prior to withdrawal of clonidine), peripheral vascular disease, renal disease

Interaction:

Drugs

Adenosine: Additive bradycardia

Alpha-1 adrenergic blockers:Potential enhanced first dose response [marked initial drop in blood pressure, particularly on standing (especially prazocin)]

Amiodarone: Increased bradycardia effect of bisoprolol

Antidiabetic: Reduced response to hypoglycemia (sweating persists)

Barbiturates: Enhanced bisoprolol metabolism

Cimetidine: Plasma levels of ß-blocker may be elevated

Cocaine: Bisprolol potentiates cocaine-induced coronary vasoconstriction

Contrast media: Increased risk for anaphylaxis

Digoxin, digitoxin: Potentiation of bradycardia; additive prolongation of atrioventricular (AV) conduction time

Dipyridamole: Additive bradycardia

Disopyramide: Additive decreases in cardiac output

Fluoxetine: Fluoxetine inhibits CYPD26, partially responsible for bisoprolol metabolism; increased ßblocker effects

Lidocaine: ß-blocker-induced reductions in cardiac output and hepatic blood flow may yield increased lidocaine concentrations

Neostigmine: Additive bradycardia s

Neuroleptics: Decreased bisoprolol metabolism; decreased neuroleptic metabolism

NSAIDs: Reduced antihypertensive effect

Physostigmine: Additive bradycardia

Prazosin: Enhanced 1st-dose response to prazosin.

Rifampin: Increases clearance by 51%, reduced ß-blocker effects

Tacrine: Additive bradycardia

Theophylline: Bisoprolol reduces clearance of theophylline; antagonistic pharmacodynamics

Warnings:

Adverse Effects:

Lactations:

Similar drug, atenolol frequently used in the third trimester for treatment of hypertension (many studies of efficacy and safety of atenolol in pregnancy-induced hypertension); long-term use has been associated with intrauterine growth retardation; excreted into breast milk; observe for signs of beta-blockade

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: