CONCORE Bisoprolol Fumarate 5mg Film-Coated Tablet 1's
RXDRUG-DRP-6628-1pc
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Concore 2.5 mg Tablet: Treatment of stable chronic heart failure with reduced systolic left ventricular function in addition to ACE inhibitors and diuretics, and optionally cardiac glycosides.
Concore 5 mg Tablet and Concore 10 mg Tablet: Treatment of high blood pressure (hypertension); Treatment of coronary heart disease (angina pectoris); Treatment of stable chronic heart failure with reduced systolic left ventricular function in addition to ACE inhibitors and diuretics, and optionally cardiac glycosides.
Concore 5 mg Tablet and Concore 10 mg Tablet: Treatment of high blood pressure (hypertension); Treatment of coronary heart disease (angina pectoris); Treatment of stable chronic heart failure with reduced systolic left ventricular function in addition to ACE inhibitors and diuretics, and optionally cardiac glycosides.
Dosage/Direction for Use
Bisoprolol (Concore) tablets are taken in the morning with or without food. They are swallowed with some liquid and are not to be chewed.
Treatment of hypertension or angina pectoris: In all cases, the dosage is adjusted individually, in particular according to the pulse rate and therapeutic success.
The usual initial dose is 5 mg bisoprolol fumarate (1 tablet of Concore 5 mg) once daily. If necessary, the dose may be increased to 10 mg bisoprolol fumarate (1 tablet of Concore 10 mg) once daily.
The maximum recommended dose is 20 mg bisoprolol fumarate once daily.
Bisoprolol (Concore) must be used with caution in patients with hypertension or angina pectoris and accompanying heart failure.
Treatment of stable chronic heart failure: Standard treatment of CHF consists of an ACE inhibitor (or an angiotensin receptor blocker in case of intolerance to ACE inhibitors), a beta-blocker, diuretics, and when appropriate cardiac glycosides. Patients should be stable (without acute failure) when bisoprolol (Concore) treatment is initiated.
It is recommended that the treating physician be experienced in the management of chronic heart failure.
The treatment of stable chronic heart failure with bisoprolol (Concore) has to be initiated with a special titration phase.
The recommended starting dose is 1.25 mg bisoprolol fumarate once daily. Depending on individual tolerance the dose is increased to 2.5 mg, 3.75 mg, 5 mg, 7.5 mg, and 10 mg once daily in intervals of two weeks or longer.
If a dose increase is not well tolerated, treatment may be maintained at a lower dose.
The maximum recommended dose is 10 mg bisoprolol fumarate once daily.
Close monitoring of vital signs (blood pressure, heart rate) and symptoms of worsening heart failure is recommended during the titration phase.
Treatment modification: If the maximum recommended dose is not well tolerated gradual dose reduction may be considered.
In case of transient worsening of heart failure, hypotension or bradycardia, reconsideration of the dosage of the concomitant medication is recommended. It may also be necessary to temporarily lower the dose of bisoprolol (Concore) or to consider discontinuation.
The reintroduction and/or uptitration of bisoprolol (Concore) should always be considered when the patient becomes stable again.
Duration of treatment for all indications: Treatment with bisoprolol (Concore) is generally a long-term therapy.
Especially in patients with ischemic heart disease, treatment must not be discontinued suddenly, unless clearly indicated because this might lead to a transitory worsening of heart condition. If discontinuation is necessary, the daily dose is gradually decreased.
Special Populations: Renal or hepatic impairment: Treatment of hypertension or angina pectoris: In patients with liver or kidney function disorders of mild to moderate severity, no dosage adjustment is normally required. In patients with severe renal impairment (creatinine clearance < 20 mL/min) and in patients with severe hepatic impairment, a daily dose of 10 mg bisoprolol fumarate must not be exceeded.
Experience with the use of bisoprolol (Concore) in renal dialysis patients is limited; however, there is no evidence that the dosage regimen needs to be altered.
Treatment of stable chronic heart failure: There is no information regarding pharmacokinetics of bisoprolol (Concore) in patients with chronic heart failure and concomitant hepatic or renal impairment. Titration of the dose in these populations should therefore, be made with particular caution.
Elderly: No dosage adjustment is required.
Children: There is no experience with bisoprolol (Concore) in children, therefore its use cannot be recommended for children.
Treatment of hypertension or angina pectoris: In all cases, the dosage is adjusted individually, in particular according to the pulse rate and therapeutic success.
The usual initial dose is 5 mg bisoprolol fumarate (1 tablet of Concore 5 mg) once daily. If necessary, the dose may be increased to 10 mg bisoprolol fumarate (1 tablet of Concore 10 mg) once daily.
The maximum recommended dose is 20 mg bisoprolol fumarate once daily.
Bisoprolol (Concore) must be used with caution in patients with hypertension or angina pectoris and accompanying heart failure.
Treatment of stable chronic heart failure: Standard treatment of CHF consists of an ACE inhibitor (or an angiotensin receptor blocker in case of intolerance to ACE inhibitors), a beta-blocker, diuretics, and when appropriate cardiac glycosides. Patients should be stable (without acute failure) when bisoprolol (Concore) treatment is initiated.
It is recommended that the treating physician be experienced in the management of chronic heart failure.
The treatment of stable chronic heart failure with bisoprolol (Concore) has to be initiated with a special titration phase.
The recommended starting dose is 1.25 mg bisoprolol fumarate once daily. Depending on individual tolerance the dose is increased to 2.5 mg, 3.75 mg, 5 mg, 7.5 mg, and 10 mg once daily in intervals of two weeks or longer.
If a dose increase is not well tolerated, treatment may be maintained at a lower dose.
The maximum recommended dose is 10 mg bisoprolol fumarate once daily.
Close monitoring of vital signs (blood pressure, heart rate) and symptoms of worsening heart failure is recommended during the titration phase.
Treatment modification: If the maximum recommended dose is not well tolerated gradual dose reduction may be considered.
In case of transient worsening of heart failure, hypotension or bradycardia, reconsideration of the dosage of the concomitant medication is recommended. It may also be necessary to temporarily lower the dose of bisoprolol (Concore) or to consider discontinuation.
The reintroduction and/or uptitration of bisoprolol (Concore) should always be considered when the patient becomes stable again.
Duration of treatment for all indications: Treatment with bisoprolol (Concore) is generally a long-term therapy.
Especially in patients with ischemic heart disease, treatment must not be discontinued suddenly, unless clearly indicated because this might lead to a transitory worsening of heart condition. If discontinuation is necessary, the daily dose is gradually decreased.
Special Populations: Renal or hepatic impairment: Treatment of hypertension or angina pectoris: In patients with liver or kidney function disorders of mild to moderate severity, no dosage adjustment is normally required. In patients with severe renal impairment (creatinine clearance < 20 mL/min) and in patients with severe hepatic impairment, a daily dose of 10 mg bisoprolol fumarate must not be exceeded.
Experience with the use of bisoprolol (Concore) in renal dialysis patients is limited; however, there is no evidence that the dosage regimen needs to be altered.
Treatment of stable chronic heart failure: There is no information regarding pharmacokinetics of bisoprolol (Concore) in patients with chronic heart failure and concomitant hepatic or renal impairment. Titration of the dose in these populations should therefore, be made with particular caution.
Elderly: No dosage adjustment is required.
Children: There is no experience with bisoprolol (Concore) in children, therefore its use cannot be recommended for children.
Overdosage
Symptoms: The most common signs expected with overdose of a beta-blocker are slow heart rate (bradycardia), marked drop in blood pressure (hypotension), bronchospasm, acute cardiac insufficiency and hypoglycemia.
There is a wide inter-individual variation in sensitivity to one single high dose of bisoprolol and patients with heart failure are probably very sensitive.
Management: In general, if overdose occurs, discontinuation of bisoprolol treatment and supportive and symptomatic treatment is recommended.
Based on the expected pharmacologic actions and recommendations for other beta-blockers, the following general measures may be considered when clinically warranted.
Bradycardia: Administer intravenous atropine. If the response is inadequate, isoprenaline or another agent with positive chronotropic properties may be given cautiously. Under some circumstances, transvenous pacemaker insertion may be necessary.
Hypotension: Intravenous fluids and vasopressors should be administered. Intravenous glucagon may be useful.
AV block (second or third degree): Patients should be carefully monitored and treated with isoprenaline infusion or temporary pacing.
Acute worsening of heart failure: Administer i.v. diuretics, inotropic agents, vasodilating agents.
Bronchospasm: Administer bronchodilator therapy such as isoprenaline, beta2-sympathomimetic drugs and/or aminophylline.
Hypoglycemia: Administer i.v. glucose.
Limited data suggest that bisoprolol is hardly dialyzable.
There is a wide inter-individual variation in sensitivity to one single high dose of bisoprolol and patients with heart failure are probably very sensitive.
Management: In general, if overdose occurs, discontinuation of bisoprolol treatment and supportive and symptomatic treatment is recommended.
Based on the expected pharmacologic actions and recommendations for other beta-blockers, the following general measures may be considered when clinically warranted.
Bradycardia: Administer intravenous atropine. If the response is inadequate, isoprenaline or another agent with positive chronotropic properties may be given cautiously. Under some circumstances, transvenous pacemaker insertion may be necessary.
Hypotension: Intravenous fluids and vasopressors should be administered. Intravenous glucagon may be useful.
AV block (second or third degree): Patients should be carefully monitored and treated with isoprenaline infusion or temporary pacing.
Acute worsening of heart failure: Administer i.v. diuretics, inotropic agents, vasodilating agents.
Bronchospasm: Administer bronchodilator therapy such as isoprenaline, beta2-sympathomimetic drugs and/or aminophylline.
Hypoglycemia: Administer i.v. glucose.
Limited data suggest that bisoprolol is hardly dialyzable.
Administration
May be taken with or without food: Take in the morning. Swallow w/ some liqd, do not chew.
Contraindications
Bisoprolol (Concore) is contraindicated in patients with: acute heart failure or during episodes of heart failure decompensation requiring i.v. inotropic therapy; shock induced by disorders of cardiac function (cardiogenic shock); severe disturbances of atrioventricular conduction (second or third degree AV block) without a pacemaker; sick sinus syndrome; sinoatrial block; slowed heart rate, causing symptoms (symptomatic bradycardia); decreased blood pressure, causing symptoms (symptomatic hypotension); severe bronchial asthma; severe forms of peripheral arterial occlusive disease or Raynaud's syndrome; untreated tumors of the adrenal gland (pheochromocytoma); metabolic acidosis; hypersensitivity to bisoprolol or to any of the excipients.
Special Precautions
Bisoprolol (Concore) must be used with caution in: diabetes mellitus with extremely fluctuating blood glucose levels: symptoms of markedly reduced blood glucose (hypoglycemia) such as tachycardia, palpitations or sweating can be masked; strict fasting; ongoing desensitization therapy; mild disturbances of atrioventricular conduction (first degree AV block); Prinzmetal's angina; Cases of coronary vasospasm have been observed. Despite its high beta1-selectivity, angina attacks cannot be completely excluded when bisoprolol is administered to patients with Prinzmetal's angina. Utmost caution must be exercised; peripheral arterial occlusive disease. Aggravation of symptoms may occur especially when starting therapy.
Beta-blockers, including bisoprolol (Concore), may increase the sensitivity to allergens and the severity of anaphylactic reactions because the adrenergic counter-regulation under beta-blockade may be alleviated. Treatment with epinephrine may not always yield the expected therapeutic effect.
Patients with psoriasis or with a history of psoriasis should only be given beta-blockers (e.g. bisoprolol) after a careful balancing of benefits against risks.
Under treatment with bisoprolol (Concore), symptoms of a thyroid hyperfunction (thyrotoxicosis) may be masked.
In patients with a tumor of the adrenal gland (pheochromocytoma), bisoprolol (Concore) must not be administered until after alpha-receptor blockade.
In patients undergoing general anesthesia, the anesthetist must be aware of beta-blockade. If it is thought necessary to withdraw bisoprolol (Concore) before surgery, this should be done gradually and completed about 48 hours prior to anesthesia.
Although cardioselective (beta1) beta-blockers may have less effect on lung function than non-selective beta-blockers, as with all beta-blockers, these should be avoided in patients with obstructive airways diseases, unless there are compelling clinical reasons for their use. Where such reasons exist, bisoprolol (Concore) may be used with caution. In bronchial asthma or other chronic obstructive pulmonary diseases, which may cause symptoms, concomitant bronchodilating therapy is recommended. Occasionally, an increase of the airway resistance may occur in patients with asthma, therefore the dose of beta2-stimulants may have to be increased.
There is no therapeutic experience of bisoprolol treatment in heart failure in patients with the following diseases and conditions: insulin dependent type 1 diabetes mellitus; severely impaired renal function; severely impaired hepatic function; restrictive cardiomyopathy; congenital heart disease; hemodynamically significant organic valvular disease; myocardial infarction within the last 3 months.
Effects on the ability to drive and use machines: In a study with patients suffering from coronary heart disease, bisoprolol did not affect the driving performance of the patients. However, depending on the individual patient's response to treatment, the ability to drive a vehicle or to use machines may be impaired. This needs to be considered particularly at the start of treatment, upon change of medication, or in conjunction with alcohol.
Beta-blockers, including bisoprolol (Concore), may increase the sensitivity to allergens and the severity of anaphylactic reactions because the adrenergic counter-regulation under beta-blockade may be alleviated. Treatment with epinephrine may not always yield the expected therapeutic effect.
Patients with psoriasis or with a history of psoriasis should only be given beta-blockers (e.g. bisoprolol) after a careful balancing of benefits against risks.
Under treatment with bisoprolol (Concore), symptoms of a thyroid hyperfunction (thyrotoxicosis) may be masked.
In patients with a tumor of the adrenal gland (pheochromocytoma), bisoprolol (Concore) must not be administered until after alpha-receptor blockade.
In patients undergoing general anesthesia, the anesthetist must be aware of beta-blockade. If it is thought necessary to withdraw bisoprolol (Concore) before surgery, this should be done gradually and completed about 48 hours prior to anesthesia.
Although cardioselective (beta1) beta-blockers may have less effect on lung function than non-selective beta-blockers, as with all beta-blockers, these should be avoided in patients with obstructive airways diseases, unless there are compelling clinical reasons for their use. Where such reasons exist, bisoprolol (Concore) may be used with caution. In bronchial asthma or other chronic obstructive pulmonary diseases, which may cause symptoms, concomitant bronchodilating therapy is recommended. Occasionally, an increase of the airway resistance may occur in patients with asthma, therefore the dose of beta2-stimulants may have to be increased.
There is no therapeutic experience of bisoprolol treatment in heart failure in patients with the following diseases and conditions: insulin dependent type 1 diabetes mellitus; severely impaired renal function; severely impaired hepatic function; restrictive cardiomyopathy; congenital heart disease; hemodynamically significant organic valvular disease; myocardial infarction within the last 3 months.
Effects on the ability to drive and use machines: In a study with patients suffering from coronary heart disease, bisoprolol did not affect the driving performance of the patients. However, depending on the individual patient's response to treatment, the ability to drive a vehicle or to use machines may be impaired. This needs to be considered particularly at the start of treatment, upon change of medication, or in conjunction with alcohol.
Use In Pregnancy & Lactation
Pregnancy: Bisoprolol (Concore) is not recommended during pregnancy unless clearly necessary. If treatment is considered necessary, monitoring of the uteroplacental blood flow and the fetal growth is recommended. In case of harmful effects on pregnancy or the fetus, consideration of alternative treatment is recommended. The newborn infant must be closely monitored. Symptoms of hypoglycemia and bradycardia are generally to be expected within the first 3 days.
Lactation: There are no data on the excretion of bisoprolol (Concore) in human breast milk or the safety of bisoprolol (Concore) exposure in infants. Therefore, breastfeeding is not recommended during administration of bisoprolol (Concore).
Lactation: There are no data on the excretion of bisoprolol (Concore) in human breast milk or the safety of bisoprolol (Concore) exposure in infants. Therefore, breastfeeding is not recommended during administration of bisoprolol (Concore).
Adverse Reactions
The undesirable effects described as follows are sorted according to system organ classes. Frequencies are classified as follows: Very common (≥ 10%), Common (≥ 1% and < 10%), Uncommon (≥ 0.1% and < 1%), Rare (≥ 0.01% and < 0.1%), Very rare (< 0.01%), frequency not known (cannot be estimated from the available data) (See table.)
Drug Interactions
Combinations not recommended: Treatment of stable chronic heart failure: Class-I antiarrhythmic drugs (e.g. quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone): Effect on atrio-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 effect on contractility and atrio-ventricular conduction. Intravenous administration of verapamil in patients on beta-blocker treatment may lead to profound hypotension and atrio-ventricular block.
Centrally-acting antihypertensive drugs (such as clonidine, methyldopa, moxonidine, rilmenidine): Concomitant use of centrally-acting antihypertensive drugs may further decrease the central sympathetic tonus and may thus lead to reduction of heart rate and cardiac output and to vasodilatation. Abrupt withdrawal, particularly if prior to beta-blocker discontinuation, may increase the risk of 'rebound hypertension'.
Combinations to be used with caution: Treatment of hypertension or coronary heart disease (angina pectoris): Class-I antiarrhythmic drugs (e.g. quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone): Effect on atrio-ventricular conduction time may be potentiated and negative inotropic effect increased.
All indications: Calcium antagonists of the dihydropyridine type (e.g. felodipine and amlodipine): Concomitant use may increase the risk of hypotension. 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 drugs (e.g. amiodarone): Effect on atrio-ventricular conduction time may be potentiated.
Topical beta-blockers (e.g. eye drops for glaucoma treatment) may add to the systemic effects of bisoprolol (Concore).
Parasympathomimetic drugs: Concomitant use may increase atrio-ventricular conduction time and the risk of bradycardia.
The blood sugar lowering effect of insulin or oral anti-diabetic drugs may be increased. Blockade of beta-adrenoceptors may mask symptoms of hypoglycemia - especially accelerated heart rate (tachycardia).
Anesthetic agents: Attenuation of the reflex tachycardia and increase of the risk of hypotension (for further information on general anesthesia see Precautions).
Cardiac glycosides (digitalis): Increase of atrio-ventricular conduction time, reduction in heart rate.
Non-steroidal anti-inflammatory drugs (NSAIDs) may reduce the hypotensive effect of bisoprolol (Concore).
Beta-sympathomimetics (e.g. isoprenaline, dobutamine) used in combination with bisoprolol (Concore) may reduce the effect of both agents.
A combination of bisoprolol (Concore) with sympathomimetics that activate both beta- and alpha-adrenoceptors (e.g. norepinephrine, epinephrine) may unmask the alpha-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 beta-blockers.
Concomitant use with antihypertensive agents as well as with other drugs with blood pressure lowering potential (e.g. tricyclic antidepressants, barbiturates, phenothiazines) may increase the risk of hypotension.
Combinations to be considered: Mefloquine may increase the risk of decelerating the heart rate (bradycardia), if used in combination with bisoprolol (Concore).
Monoamine oxidase inhibitors (except MAO-B inhibitors) may enhance the hypotensive effect of the beta-blockers. Concomitant use may also be a risk for hypertensive crisis.
Rifampicin: Slight reduction of the half-life of bisoprolol (Concore) possible due to the induction of hepatic drug-metabolizing enzymes. Normally no dosage adjustment is necessary.
Ergotamine derivatives: Exacerbation of peripheral circulatory disturbances.
All indications: Calcium antagonists of the verapamil type and to a lesser extent of the diltiazem type: Negative effect on contractility and atrio-ventricular conduction. Intravenous administration of verapamil in patients on beta-blocker treatment may lead to profound hypotension and atrio-ventricular block.
Centrally-acting antihypertensive drugs (such as clonidine, methyldopa, moxonidine, rilmenidine): Concomitant use of centrally-acting antihypertensive drugs may further decrease the central sympathetic tonus and may thus lead to reduction of heart rate and cardiac output and to vasodilatation. Abrupt withdrawal, particularly if prior to beta-blocker discontinuation, may increase the risk of 'rebound hypertension'.
Combinations to be used with caution: Treatment of hypertension or coronary heart disease (angina pectoris): Class-I antiarrhythmic drugs (e.g. quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone): Effect on atrio-ventricular conduction time may be potentiated and negative inotropic effect increased.
All indications: Calcium antagonists of the dihydropyridine type (e.g. felodipine and amlodipine): Concomitant use may increase the risk of hypotension. 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 drugs (e.g. amiodarone): Effect on atrio-ventricular conduction time may be potentiated.
Topical beta-blockers (e.g. eye drops for glaucoma treatment) may add to the systemic effects of bisoprolol (Concore).
Parasympathomimetic drugs: Concomitant use may increase atrio-ventricular conduction time and the risk of bradycardia.
The blood sugar lowering effect of insulin or oral anti-diabetic drugs may be increased. Blockade of beta-adrenoceptors may mask symptoms of hypoglycemia - especially accelerated heart rate (tachycardia).
Anesthetic agents: Attenuation of the reflex tachycardia and increase of the risk of hypotension (for further information on general anesthesia see Precautions).
Cardiac glycosides (digitalis): Increase of atrio-ventricular conduction time, reduction in heart rate.
Non-steroidal anti-inflammatory drugs (NSAIDs) may reduce the hypotensive effect of bisoprolol (Concore).
Beta-sympathomimetics (e.g. isoprenaline, dobutamine) used in combination with bisoprolol (Concore) may reduce the effect of both agents.
A combination of bisoprolol (Concore) with sympathomimetics that activate both beta- and alpha-adrenoceptors (e.g. norepinephrine, epinephrine) may unmask the alpha-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 beta-blockers.
Concomitant use with antihypertensive agents as well as with other drugs with blood pressure lowering potential (e.g. tricyclic antidepressants, barbiturates, phenothiazines) may increase the risk of hypotension.
Combinations to be considered: Mefloquine may increase the risk of decelerating the heart rate (bradycardia), if used in combination with bisoprolol (Concore).
Monoamine oxidase inhibitors (except MAO-B inhibitors) may enhance the hypotensive effect of the beta-blockers. Concomitant use may also be a risk for hypertensive crisis.
Rifampicin: Slight reduction of the half-life of bisoprolol (Concore) possible due to the induction of hepatic drug-metabolizing enzymes. Normally no dosage adjustment is necessary.
Ergotamine derivatives: Exacerbation of peripheral circulatory disturbances.
Storage
Concore 2.5 mg Film-coated Tablet: Store at temperatures not exceeding 25°C.
Concore 5 mg Film-coated Tablet: Store at temperatures not exceeding 25°C.
Concore 10 mg Film-coated Tablet: Store at temperatures not exceeding 30°C.
Description
Each Concore 2.5 mg film-coated tablet contains 2.5 mg Bisoprolol fumarate. Each Concore 5 mg film-coated tablet contains 5 mg Bisoprolol fumarate. Each Concore 10 mg film-coated tablet contains 10 mg Bisoprolol fumarate. The chemical name of Bisoprolol fumarate is (RS)-1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]propan-2-ol fumarate.
Action
Pharmacology: Pharmacodynamics: Bisoprolol, the active ingredient of Concore, is a beta1-selective-adrenoceptor blocking agent, lacking intrinsic stimulating and relevant membrane stabilizing activity. It only shows very low affinity to the beta2-receptor of the smooth muscles of bronchi and vessels as well as to the beta2-receptors concerned with metabolic regulation. Therefore, bisoprolol is generally not to be expected to influence the airway resistance and beta2-mediated metabolic effects. Its beta1-selectivity extends beyond the therapeutic dose range.
Bisoprolol has no pronounced negative inotropic effect.
Bisoprolol reaches its maximal effect 3 - 4 hours after oral administration. The plasma elimination half-life of 10 - 12 hours provides 24 hours efficacy following a once daily dosage.
The maximal antihypertensive effect of bisoprolol is generally reached after 2 weeks.
In acute administration in patients with coronary heart disease without chronic heart failure, bisoprolol reduces the heart rate and stroke volume, thus reducing cardiac output and oxygen consumption. In chronic administration the initially elevated peripheral resistance decreases. Among others, the depression of plasma renin activity is discussed as a mechanism of action underlying the antihypertensive effect of beta-blockers.
Bisoprolol depresses the response to sympathoadrenergic activity through blockade of cardiac beta-receptors. This causes a decrease in heart rate and in contractility, and thus a reduction of myocardial oxygen consumption, which is the desired effect in angina pectoris with underlying coronary heart disease.
Pharmacokinetics: Absorption: Bisoprolol is almost completely (>90%) absorbed from the gastrointestinal tract and, because of its small first pass metabolism of approximately 10%, it has an absolute bioavailability of approximately 90% after oral administration. The bioavailability is not affected by food intake. Bisoprolol has a linear, age-independent kinetics and the plasma concentrations are proportional to the administered dose over the dose range 5 to 20 mg. Peak plasma concentrations occur within 2-3 hours.
Distribution: Bisoprolol is extensively distributed. The volume of distribution is 3.5 L/Kg. Binding to plasma proteins is approximately 30%.
Metabolism: Bisoprolol is metabolized via oxidative pathways with no subsequent conjugation. All metabolites, being very polar, are renally eliminated. The major metabolites in human plasma and urine were found to be without pharmacological activity. In vitro data from studies in human liver microsomes show that bisoprolol is primarily metabolized via CYP3A4 (Yulex95%) with CYP2D6 having only a minor role.
Elimination: The clearance of bisoprolol is 'balanced' between renal elimination of the unchanged molecule (Yulex50%) and hepatic metabolism (Yulex50%) to metabolites which are also renally excreted. The total clearance of bisoprolol is approximately 15 L/h. Bisoprolol has a plasma elimination half-life of 10-12 hours.
Bisoprolol has no pronounced negative inotropic effect.
Bisoprolol reaches its maximal effect 3 - 4 hours after oral administration. The plasma elimination half-life of 10 - 12 hours provides 24 hours efficacy following a once daily dosage.
The maximal antihypertensive effect of bisoprolol is generally reached after 2 weeks.
In acute administration in patients with coronary heart disease without chronic heart failure, bisoprolol reduces the heart rate and stroke volume, thus reducing cardiac output and oxygen consumption. In chronic administration the initially elevated peripheral resistance decreases. Among others, the depression of plasma renin activity is discussed as a mechanism of action underlying the antihypertensive effect of beta-blockers.
Bisoprolol depresses the response to sympathoadrenergic activity through blockade of cardiac beta-receptors. This causes a decrease in heart rate and in contractility, and thus a reduction of myocardial oxygen consumption, which is the desired effect in angina pectoris with underlying coronary heart disease.
Pharmacokinetics: Absorption: Bisoprolol is almost completely (>90%) absorbed from the gastrointestinal tract and, because of its small first pass metabolism of approximately 10%, it has an absolute bioavailability of approximately 90% after oral administration. The bioavailability is not affected by food intake. Bisoprolol has a linear, age-independent kinetics and the plasma concentrations are proportional to the administered dose over the dose range 5 to 20 mg. Peak plasma concentrations occur within 2-3 hours.
Distribution: Bisoprolol is extensively distributed. The volume of distribution is 3.5 L/Kg. Binding to plasma proteins is approximately 30%.
Metabolism: Bisoprolol is metabolized via oxidative pathways with no subsequent conjugation. All metabolites, being very polar, are renally eliminated. The major metabolites in human plasma and urine were found to be without pharmacological activity. In vitro data from studies in human liver microsomes show that bisoprolol is primarily metabolized via CYP3A4 (Yulex95%) with CYP2D6 having only a minor role.
Elimination: The clearance of bisoprolol is 'balanced' between renal elimination of the unchanged molecule (Yulex50%) and hepatic metabolism (Yulex50%) to metabolites which are also renally excreted. The total clearance of bisoprolol is approximately 15 L/h. Bisoprolol has a plasma elimination half-life of 10-12 hours.
MedsGo Class
Beta-Blockers
Features
Brand
Concore
Full Details
Dosage Strength
5mg
Drug Ingredients
- Bisoprolol Fumarate
Drug Packaging
Film-Coated Tablet 1's
Generic Name
Bisoprolol Fumarate
Dosage Form
Film-Coated Tablet
Registration Number
DRP-6628
Drug Classification
Prescription Drug (RX)
View all variations as list
| CODE | Dosage Strength | Drug Packaging | Availability | Price | ||
|---|---|---|---|---|---|---|
|
RXDRUG-DRP-6628-1pc
|
In stock
|
₱3250 |
Please sign in so that we can notify you about a reply