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Concor 5Concor 5

Active ingredient : bisoprolol hemifumarate

 

Composition

Each film-coated tablet contains 5mg bisoprolol hemifumarate as active ingredient.

Excipients : Tablet core : Silica, colloidal anhydrous; magnesium stearate, crospovidone, microcrystalline cellulose, maize starch, calcium hydrogen phosphate, anhydrous.

Film coating : Iron oxide yellow, dimethicone, macrogol 400, titanium dioxide, hypromellose.

 

Product descriptions

Yellowish white, heart-shaped, biconvex film-coated tablets, scored on both sides.

 

Properties

Pharmacodynamics

Bisoprolol, the active ingredient of Concor is a beta1-selective-adrenoceptor blocking agent, lacking intrinsic stimulating and relevant membrane stabilising 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.

 

Pharmacokinetics

Absorption. Bisoprolol is almost completely ( >90% ) absorbed from the gastrointestinal tract and, because of its small first pass metabolism of approximately 10%, has an bioavailability of approximately 90% after oral administration. The bioavailability is not affected by food intake. Bisoprolol shows linear kinetics and the plasma concentrations are proportional to the administered dose over the dose range 5 to 20mg. 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 metabolised 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 bioprolol is primarily metabolised via CYP3A4 ( ~95% ) with CYP2D6 having only a minor role.

 

Elimination. The clearance of bisoprolol is 'balanced' between renal elimination of the unchanged molecule ( ~50% ) and hepatic metabolism ( ~50% ) to metabolites which are also renally excreted. The total clearnace of bisoprolol is approximately 15 l/h. Bisoprolol has an elimination half-life of 10-12 hours.

 

Indication

* Treatment of high blood pressure ( hypertension )

* Treatment of coronary heart disease ( angina pectoris )

* Treatment of stable chronic moderate to severe heart failure with reduced systolic ventricular function ( ejection fraction ≤ 35%, based on echocardiography ) in addition to ACE inhibitors, and diuretics, and optionally cardiac glycosides.

 

Contraindications

Concor must not be used in patients with :

* acute heart failure or during episodes of heart failure decompensation requiring intravenous therapy with substances increasing the contractility of the heart,

* 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

* decreased blood pressure, causing symptoms

* severe forms of peripheral arterial occlusive disease or Raynaud's syndrome,

* untreated tumors of the adrenal gland ( phaeochromocytoma ),

* metabolic acidosis,

* hypersensitivity to bisoprolol or to any of the excipients ( see composition ).

 

Special warnings and precautions

The following section describes when Concor must be used with special caution :

* diabetes mellitus with extremely fluctuating blood glucose levels : symptoms of markedly reduced blood glucose ( hypoglycaemia ) such as tachycardia, palpitations or sweating can be masked.

* strict fasting,

* ongoing desensitisation therapy,

* mild disturbances of atrioventricular conduction ( first degree AV block ),

* disturbed blood flow in the coronary vessels due to vasospasms ( Prinzmetal's angina ),

* peripheral arterial occlusive disease ( intensification of complaints may occur especially when starting therapy ),

* patients with a personal or family history of psoriasis.

 

Respiratory system : In bronchial asthma or other symptomatic chronic obstructive pulmonary disease concomitant bronchodilator therapy is indicated. An increase in airway resistance may occasionally occur in patients with asthma, requiring a higher dose of beta2-sympathomimetics.

 

Allergic reactions : Beta-blockers, including Concor, 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 adrenaline may not always give the expected therapeutic effect.

 

General anaesthesia : In patient undergoing general anaesthesia the anaesthetist must be aware of beta-blockage. If it is thought necessary to withdraw Concor before surgery, this should be done gradually and completed about 48 hours prior to anaesthesia.

 

Phaeochromocytoma : In patients with a tumour of the adrenal gland ( phaeochromocytoma ) Concor may only be administered after previous alpha-receptor blockade.

 

Thyrotoxicosis : Under treatment with Concor the symptoms of a thyroid hyperfunction ( thyrotoxicosis ) may be masked.

 

Special populations

So far no sufficient therapeutic experience is available for Concor in patients with heart failure and concomitant insulin dependent type I diabetes mellitus, impaired kidney function ( serum creatinine ≥ 3.4 mg/dl ), impaired liver function, restrictive cardiomyopathy, congenital heart diseases or haemodynamically relevant organic valvular heart disease. No sufficient therapeutic experience is available either in patients with mild heart failure ( NYHA II ) as well as heart failure and myocardial infarction within the last 3 months.

 

There is insufficient experience with bisoprolol in children, therefore the use of Concor cannot be recommended for children.

 

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, due to individually different reactions, the ability to drive a vehicle or to operate machinery may be impaired. This needs to be considered particularly at the start of treatment, after change of dose, as well as in conjunction with alcohol.

 

Pregnancy and lactation

During pregnancy Concor should only recommended following careful assessment of benefit-to-risk ratio by the doctor. In general, beta-blockers reduce placental blood flow and may affect the development of the unborn child. Placental and uterine blood flow as well as the growth of the unborn child must be monitored and, in case of harmful effects on pregnancy or the foetus, alternative therapeutic measures considered.

 

The new born infant must be monitored closely after delivery. Symptoms of reduced blood glucose and slowed pulse rate generally may occur within the first 3 days of life.

 

There are no data on the excretion of bisoprolol in human breast milk or the safety of bisoprolol exposure in infants. Therefore administration of Concor is not recommended during breastfeeding.

 

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