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Bisoprolol information from DrugsUpdate  

See Available Brands of Bisoprolol in India

P - Contraindicated in pregnancy
L - Cautioned in lactation
LI - Lab*

Bisoprolol fumarate is a synthetic, beta1-selective (cardioselective) adrenoceptor blocking agent.

 

Pharmacodynamics

The most prominent effect of Bisoprolol fumarate is the negative chronotropic effect, resulting in a reduction in resting and exercise heart rate. There is a fall in resting and exercise cardiac output with little observed change in stroke volume, and only a small increase in right atrial pressure, or pulmonary capillary wedge pressure at rest or during exercise.
 
Findings in short-term clinical hemodynamics studies with Bisoprolol fumarate are similar to those observed with other beta-blocking agents.
 
The mechanism of action of its antihypertensive effects has not been completely established. Factors which may be involved include:
 
        1)      Decreased cardiac output,
        2)      Inhibition of renin release by the kidneys,
        3)      Diminution of tonic sympathetic outflow from the vasomotor centers in the brain.
 
In normal volunteers, Bisoprolol fumarate therapy resulted in a reduction of exercise- and isoproterenol-induced tachycardia. The maximal effect occurred within 1 to 4 hours post-dosing. Effects persisted for 24 hours at doses equal to or greater than 5 mg.
 
Electrophysiology studies in man have demonstrated that Bisoprolol fumarate significantly decreases heart rate, increases sinus node recovery time, prolongs AV node refractory periods, and, with rapid atrial stimulation, prolongs AV nodal conduction.
 
Beta1-selectivity of Bisoprolol fumarate has been demonstrated in both animal and human studies. No effects at therapeutic doses on beta2-adrenoceptor density have been observed. Pulmonary function studies have been conducted in healthy volunteers, asthmatics, and patients with chronic obstructive pulmonary disease (COPD). Doses of Bisoprolol fumarate ranged from 5 to 60 mg, atenolol from 50 to 200 mg, metoprolol from 100 to 200 mg, and propranolol from 40 to 80 mg. In some studies, slight, asymptomatic increases in airways resistance (AWR) and decreases in forced expiratory volume (FEV1) were observed with doses of Bisoprolol fumarate 20 mg and higher, similar to the small increases in AWR also noted with the other cardioselective beta-blockers. The changes induced by beta-blockade with all agents were reversed by bronchodilator therapy.
 
Bisoprolol fumarate had minimal effect on serum lipids during antihypertensive studies. In U.S. placebo-controlled trials, changes in total cholesterol averaged +0.8% for Bisoprolol fumarate-treated patients, and +0.7% for placebo. Changes in triglycerides averaged +19% for Bisoprolol fumarate-treated patients, and +17% for placebo.
 
Bisoprolol fumarate has also been given concomitantly with thiazide diuretics. Even very low doses of hydrochlorothiazide (6.25 mg) were found to be additive with Bisoprolol fumarate in lowering blood pressure in patients with mild-to-moderate hypertension.


 

Pharmacokinetics

The absolute bioavailability after a 10 mg oral dose of Bisoprolol fumarate is about 80%. Absorption is not affected by the presence of food. The first pass metabolism of Bisoprolol fumarate is about 20%.
 
Binding to serum proteins is approximately 30%. Peak plasma concentrations occur within 2 to 4 hours of dosing with 5 to 20 mg, and mean peak values range from 16 ng/mL at 5 mg to 70 ng/mL at 20 mg. Once daily dosing with Bisoprolol fumarate results in less than twofold intersubject variation in peak plasma levels. 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. Steady state is attained within 5 days of once daily dosing. In both young and elderly populations, plasma accumulation is low; the accumulation factor ranges from 1.1 to 1.3, and is what would be expected from the first order kinetics and once daily dosing. Plasma concentrations are proportional to the administered dose in the range of 5 to 20 mg. Pharmacokinetic characteristics of the two enantiomers are similar.
 
Bisoprolol fumarate is eliminated equally by renal and non-renal pathways with about 50% of the dose appearing unchanged in the urine and the remainder appearing in the form of inactive metabolites. In humans, the known metabolites are labile or have no known pharmacologic activity. Less than 2% of the dose is excreted in the feces. Bisoprolol fumarate is not metabolized by cytochrome P450 II D6 (debrisoquin hydroxylase).
 
In subjects with creatinine clearance less than 40 mL/min, the plasma half-life is increased approximately threefold compared to healthy subjects.
 
In patients with cirrhosis of the liver, the elimination of Bisoprolol fumarate is more variable in rate and significantly slower than that in healthy subjects, with plasma half-life ranging from 8.3 to 21.7 hours.


 

Bisoprolol Indications / Bisoprolol Uses

Bisoprolol fumarate tablets are indicated in the management of hypertension. They may be used alone or in combination with other antihypertensive agents.


 

Bisoprolol Adverse Reactions / Bisoprolol Side Effects

Giddiness, headache, faitgue, bradycardia. Nausea, vomiting, diarrhoea or constipation, stomach dsicomfort , mild ocular stinging, photophobia, keratitis, decreased sexual ability. GI disturbances, dysponea, cold extremities, insomnia, hallunications, drowsiness & mood alterations. AV block bradycardia. Rare but may occur in patients with preexisting cardiac disease. Includes severe bronchospasm, hypoglycaemia, hypotension, orthostatic hypotension, orthostatic hypotension, orthostatic hypotension, bradyarrhythmias. 'Rebound phenomenon' leading to unstable angina or MI on sudden withdrawal.

Precautions

Use caution in adjusting the dose of Bisoprolol fumarate in patients with renal or hepatic impairment.

Special Precautions

Bronchospastic disease, hyperthyroidism, peripheral vascular disease, undergoing anaesthesia. Monitor blood glucose regularly. May mask symptoms of hypoglycaemia. Elderly. Gradual withdrawal is advised. Lactation.

Other Drug Interactions

Decreased effect with AI & Ca salts, barbiturates, cholestyramine, NSAIDs ampicillin, rifampicin. May mask tachycardia from hypoglycaemia from hypoglycaemia induced by insulin & oral hypoglycaemics.
Effects of other antihypertensives may be intensified. May increase the effects of drugs which slow AV conduction, α blockers &  α- adrenergic stimulants. Enhances the action of anesth agents, clonidone, Ca antagonists, digitlis, hypoglycaemia agents & NSAIDs.

Other Interactions

Information Not Available

Dosage

Information Not Available

Food(before/after)

Information Not Available

List of Contraindications

Bisoprolol and Pregnancy

Contraindicated in pregnancy

Bisoprolol and Lactation

Cautioned in lactation

Bisoprolol and Children

Information Not Available

Bisoprolol and Geriatic

Bisoprolol fumarate has been used in elderly patients with hypertension. Response rates and mean decreases in systolic and diastolic blood pressure were similar to the decreases in younger patients in the U.S. clinical studies. Although no dose response study was conducted in elderly patients, there was a tendency for older patients to be maintained on higher doses of Bisoprolol fumarate.
Observed reductions in heart rate were slightly greater in the elderly than in the young and tended to increase with increasing dose. In general, no disparity in adverse experience reports or dropouts for safety reasons was observed between older and younger patients. Dose adjustment based on age is not necessary.

Bisoprolol and Other Contraindications

Low cardiac output & uncompensated cardiac failure. Sinus Bradycardia, 1st degree heart block, cardiogenic shock, bronchospasm; severe haemorrage. Pregnancy.


 

Storage

Information Not Available

Lab interference

Information Not Available

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