Each film-coated tablet of BISOLOL-5 mg and BISOLOL-10mg contains Bisoprolol fumarate 5mg and 10mg respectively. Bisoprolol fumarate is a beta-blocker drug used to lower blood pressure in people with hypertension.

Bisoprolol fumarate is a beta-adrenergic blocking agent, it inhibits beta-1-adrenergic receptors (cardioselective) and, at higher doses (≥ 20mg), it inhibits beta-2 receptors. It has no intrinsic sympathomimetic activity and no membrane-stabilizing activity in its therapeutic dose range. To retain relative selectivity, it is important to use the lowest effective dose.

Over 90% of the oral dose is absorbed. Peak plasma concentrations occur within 2-4 hours of dosing with 2.5 to 20mg of Bisoprolol fumarate, and mean peak values range from 9.0 ng/ml at 2.5mg to 70 ng/ml at 20mg. The half-life of Bisoprolol in plasma is ranging between 9-12 hours. Approximately 50% is excreted unchanged through the urine and the remainder as inactive metabolites; a small amount (less than 2%) is excreted through the feces.

BISOLOL is indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents.

BISOLOL should be avoided in patients with cardiogenic shock, overt cardiac failure; second and third degree AV block, and marked sinus bradycardia. It also should be avoided in hypersensitivity to the component.

Bisoprolol fumarate is well tolerated in most patients. Most adverse effects have been mild and transient. The most common adverse effects of Bisoprolol are a mixture of dose-dependent phenomena, such as bradycardia, diarrhea, asthenia and fatigue, and dose-independent phenomena (occasional rash).

Since Bisoprolol is selective for beta-1 receptors, it may be used with caution in patients with bronchospastic disease who do not respond to, or who cannot tolerate, other antihypertensive therapy. BISOLOL should also be used with caution in patients with impaired renal or hepatic functions, and the dose should be adjusted in such patients. Caution should also be exercised in patients with diabetes, hypoglycemia, and peripheral vascular diseases. Abrupt cessation of BISOLOL therapy should be avoided. BISOLOL is used with caution during lactation. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

 

BISOLOL should not be combined with other beta-blocking agents. Concurrent use of rifampicin increases the metabolic clearance of BISOLOL, resulting in a shortened elimination half-life of Bisoprolol. Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be closely monitored because the added beta-adrenergic blocking action of Bisoprolol fumarate may produce excessive reduction of sympathetic activity. In patients receiving concurrent therapy with clonidine, if therapy is to  be discontinued, it is suggested that Bisoprolol fumarate be discontinued for several days before the withdrawal of clonidine.

Bisoprolol fumarate should be used with caution when myocardial depressants or inhibitors of AV conduction, such as certain calcium antagonists (particularly verapamil and diltiazem), or antiarrhythmic agents, such as disopyramide, are used concurrently.

Increase in SGPT,SGOT, uric acid, creatinine, serum potassium, glucose, and phosphorus. Decrease in WBCs and platelets.

Dose must be individualized to the need of the patient. The usual starting dose is one tablet of BISOLOL-5 (5mg) once daily. In some patients (bronchospastic patients) 2.5mg/day may be an appropriate starting dose. If the 5-mg dose is inadequate, the dose may be increased to 10mg/day and then, if needed, to 20mg once daily. In patients with impaired renal or hepatic function, the initial daily dose should be 2.5mg with caution used in titrating the dose upward.

Hypotension and bradycardia may result in case of product overdose; sympathomimetic agents may be given for the treatment of these cases.

30 film-coated tablets in two blisters of BISOLOL-5mg or BISOLOL-10mg.