Each film-coated tablet contains: Bisoprolol Fumarate USP 5 mg.
Pharmacology: Bisoprolol is a potent, highly β1-selective adrenoreceptor blocking agent devoid of intrinsic sympathomimetic activity and without relevant membrane stabilising activity.
As with other β1-blocking agents, the mode of action in hypertension is not clear but it is known that bisoprolol markedly depresses plasma renin levels.
In patients with angina, the blockade of β1-receptors reduces heart action and thus reduces oxygen demand. Hence, bisoprolol is effective in eliminating or reducing the symptoms.
Pharmacokinetics: Bisoprolol is almost completely absorbed from the gastrointestinal tract and undergoes only minimal first-pass metabolism resulting in an oral bioavailability of about 90%. Peak plasma concentrations are reached 2 to 4 hours after oral doses. Bisoprolol is about 30% bound to plasma proteins. It has a plasma elimination half-life of 10 to 12 hours. Bisoprolol is moderately lipid-soluble. It is metabolized in the liver and excreted in urine, about 50% as unchanged drug and 50% as metabolites.
Bisoprolol is given in the management of hypertension and angina pectoris. It is also used as an adjunct to standard therapy in patients with stable chronic heart failure.
Hypertension or Angina Pectoris: 5 to 10 mg orally as a single dose.
Maximum recommended dose: 20 mg daily.
Stable chronic heart failure: 1.25 mg once daily initially.
Standard treatment of CHF consists of an ACE inhibitor (or an angiotensin receptor blocker in case of intolerance to ACE inhibitors), a beta-blocking agent, diuretics, and when appropriate cardiac glycosides. Patients should be stable (without acute failure) when bisoprolol treatment is initiated.
It is recommended that the treating physician should be experienced in the management of chronic heart failure.
Titration phase: The treatment of stable chronic heart failure with bisoprolol requires a titration phase.
The treatment with bisoprolol is to be started with a gradual uptitration according to the following steps: 1.25 mg once daily for 1 week, if well tolerated increase to 2.5 mg once daily for a further week, if well tolerated increase to 3.75 mg once daily for a further week, if well tolerated increase to 5 mg once daily for the 4 following weeks, if well tolerated increase to 7.5 mg once daily for the 4 following weeks, if well tolerated increase to 10 mg once daily for the maintenance therapy.
The maximum recommended dose is 10 mg once daily.
Or as prescribed by the physician.
Bisoprolol is contraindicated in: acute heart failure or during episodes of heart failure decompensation requiring i.v. inotropic therapy; cardiogenic shock; AV block of second or third degree; sick sinus syndrome; sinoatrial block; symptomatic bradycardia; symptomatic hypotension; severe bronchial asthma or severe chronic obstructive pulmonary disease; severe forms of peripheral arterial occlusive disease or severe forms of Raynaud's syndrome; untreated pheochromocytoma; metabolic acidosis; hypersensitivity to the active substance or to any of the excipients.
Beta blockers should not be given to patients with bronchospasm or asthma or to those with a history of obstructive airway disease. This contraindication generally applies even to those beta blockers considered to be cardioselective. However, cardioselective beta blockers may be used with extreme caution when there is no alternative treatment. Other contraindications include metabolic acidosis, cardiogenic shock, hypotension, severe peripheral arterial disease, sinus bradycardia, and second- or third-degree AV block; caution should be observed in first-degree block. Although beta blockers are used in the management of heart failure, they should not be given to patients with uncontrolled heart failure and treatment should be begun with great care, starting with a low dose and cautiously titrating upwards. Patients with pheochromocytoma should not be given beta blockers without alpha-adrenoceptor blocking therapy as well.
Beta blockers may mask the symptoms of hyperthyroidism and of hypoglycemia. They may unmask myasthenia gravis. Psoriasis may be aggravated. Beta blockers may increase the number of attacks of chest pain in patients with Prinzmetal's angina; this occurs especially with non-cardioselective beta blockers, which should be avoided. Beta blockers increase sensitivity to allergens and also the severity of anaphylactoid reactions; patients with a history of anaphylaxis to an antigen may be more reactive to repeated challenge with the antigen while taking beta blockers.
Use in Pregnancy: Bisoprolol should not be used during pregnancy unless clearly necessary. If treatment with bisoprolol is considered necessary, the uteroplacental blood flow and the fetal growth should be monitored. In case of harmful effects on pregnancy or the fetus alternative treatment should be considered. The newborn infant must be closely monitored. Symptoms of hypoglycemia and bradycardia are generally to be expected within the first 3 days.
Use in Lactation: It is not known whether this drug is excreted in human milk. Therefore, breastfeeding is not recommended during administration of bisoprolol.
Use in Pregnancy: Bisoprolol should not be used during pregnancy unless clearly necessary. If treatment with bisoprolol is considered necessary, the uteroplacental blood flow and the fetal growth should be monitored. In case of harmful effects on pregnancy or the fetus alternative treatment should be considered. The newborn infant must be closely monitored. Symptoms of hypoglycemia and bradycardia are generally to be expected within the first 3 days.
Use in Lactation: It is not known whether this drug is excreted in human milk. Therefore, breastfeeding is not recommended during administration of bisoprolol.
Bronchospasm, shortness of breath, and dyspnea may be precipitated, particularly in patients with a history of obstructive airways disease, due to blockade of beta
2 receptors in bronchial smooth muscle. Drugs with selectivity for beta
1-receptors or with intrinsic sympathomimetic activity at beta
2-receptors may be less likely to induce bronchospasm. Pneumonitis, pulmonary fibrosis and pleurisy have also been reported.
CNS effects include headache, depression, dizziness, hallucinations, confusion, amnesia and sleep disturbances including nightmares. Coma and convulsions have been reported after beta-blocker overdosage. Beta blockers that are lipid soluble are more likely to enter the brain and would be expected to be associated with a higher incidence of CNS adverse effects, although this is not proven.
Fatigue is a common adverse-effect of beta blockers. Paresthesia, arthralgia, and myopathies, including muscle cramps, have been reported. Reduced peripheral circulation can produce coldness of the extremities and may exacerbate peripheral vascular disease such as Raynaud's syndrome.
Adverse gastrointestinal effects include nausea and vomiting, diarrhea, constipation and abdominal cramping.
Combinations not recommended: Chronic heart failure only: Class I antiarrhythmic medicinal products (e.g. quinidine, disopyramide; lidocaine, phenytoin; flecainide, propafenone): Effect on atria-ventricular conduction time may be potentiated and negative inotropic effect increased.
All indications: Calcium antagonists of the verapamil type and to a lesser extent of the diltiazem type: Negative influence on contractility and atrio-ventricular conduction. Intravenous administration of verapamil in patients on β-blocker treatment may lead to profound hypotension and atrioventricular block.
Centrally-acting antihypertensive medicinal products such as clonidine and others (e.g. methyldopa, moxonodine, rilmenidine): Concomitant use of centrally acting antihypertensive medicinal products may worsen heart failure by a decrease in the central sympathetic tonus (reduction of heart rate and cardiac output, vasodilation). Abrupt withdrawal, particularly if prior to beta-blocking agent discontinuation, may increase the risk of "rebound hypertension".
Combinations to be used with caution: Hypertension/Angina pectoris only: Class I antiarrhythmic medicinal products (e.g. quinidine, disopyramide; lidocaine, phenytoin; flecainide, propafenone): Effect on atria-ventricular conduction time may be potentiated and negative inotropic effect increased.
All indications: Calcium antagonists of the dihydropyridine type such as felodipine and amlodipine: Concomitant use may increase the risk of hypotension, and an increase in the risk of a further deterioration of the ventricular pump function in patients with heart failure cannot be excluded.
Class-III antiarrhythmic medicinal product (e.g. amiodarone): Effect on atrio-ventricular conduction time may be potentiated.
Topical beta-blocking agents (e.g. eye drops for glaucoma treatment) may add to the systemic effects of bisoprolol.
Parasympathomimetic medicinal products: Concomitant use may increase atrio-ventricular conduction time and the risk of bradycardia.
Insulin and oral antidiabetic medicinal products: Increase of blood sugar lowering effect. Blockade of beta-adrenoceptors may mask symptoms of hypoglycemia.
Anaesthetic agents: Attenuation of the reflex tachycardia and increase of the risk of hypotension.
Digitalis glycosides: Reduction of heart rate, increase of atrio-ventricular conduction time.
Non-steroidal anti-inflammatory drugs (NSAIDs): NSAIDs may reduce the hypotensive effect of bisoprolol.
β-sympathomimetic agents (e.g. isoprenaline, dobutamine): Combination with bisoprolol , may reduce the effect of both agents.
Sympathomimetics that activate both β- and α-adrenoceptors (e.g. noradrenaline, adrenaline): Combination with bisoprolol may unmask the a-adrenoceptor-mediated vasoconstrictor effects of these agents leading to blood pressure increase and exacerbated intermittent claudication. Such interactions are considered to be more likely with nonselective β-blockers.
Concomitant use with antihypertensive agents as well as with other medicinal products with blood pressure lowering potential (e.g. tricyclic antidepressants, barbiturates, phenothiazines) may increase the risk of hypotension.
Combinations to be considered: Mefloquine: increased risk ofbradycardia.
Monoamine oxidase inhibitors (except MAO-B inhibitors): Enhanced hypotensive effect of the beta-blocking agents, but also risk for hypertensive crisis.
Rifampicin: Slight reduction of the half-life of bisoprolol possible due to the induction of hepatic drug-metabolising enzymes. Normally no dosage adjustment is necessary.
Ergotamine derivatives: Exacerbation of peripheral circulatory disturbances.
Store at temperatures not exceeding 30°C.
C07AB07 - bisoprolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
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