Chemical formula: C₁₈H₃₁NO₄ Molecular mass: 325.443 g/mol PubChem compound: 2405
Bisoprolol interacts in the following cases:
Monoamine oxidase inhibitors (except MAO-B inhibitors): Enhanced hypotensive effect of the beta-blockers but also risk for hypertensive crisis.
NSAIDs may reduce the hypotensive effect of bisoprolol.
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 liver function disorders it is recommended that a daily dose of 10 mg bisoprolol fumarate is not exceeded. Experience with the use of bisoprolol in renal dialysis patients is limited; however, there is no evidence that the dosage regimen needs to be altered.
There is no information regarding pharmacokinetics of bisoprolol in patients with chronic heart failure and with impaired hepatic or renal function. Titration of the dose in these populations should therefore be made with particular caution.
Intensification of blood sugar lowering effect. Blockade of beta-adrenoreceptors may mask symptoms of hypoglycaemia (for example tachycardia).
Reduction of heart rate, increase of atrio-ventricular conduction time.
Class-I antiarrhythmic drugs (e.g. disopyramide, quinidine, lidocaine, phenytoin; flecainide, propafenone): Effect on atrio-ventricular conduction time may be potentiated and negative inotropic effect increased.
Class-III antiarrhythmic drugs (e.g. amiodarone): Effect on atrio-ventricular conduction time may be potentiated.
Centrally acting antihypertensive drugs (e.g. clonidine, methyldopa, moxonidine, rilmenidine): Concomitant use of centrally acting antihypertensive drugs may further decrease the central sympathetic tonus (and may thus lead to a reduction of heart rate and cardiac output, and to vasodilation). Abrupt withdrawal, particularly if prior to beta-blocker discontinuation, may increase risk of “rebound hypertension”.
Concomitant use of bisoprolol with parasympathomimetic drugs may increase atrio-ventricular conduction time and the risk of bradycardia.
Topical beta-blockers (e.g. eye drops for glaucoma treatment) may add to the systemic effects of bisoprolol.
Calcium antagonists of the dihydropyridine type such as nifedipine: 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.
β-sympathomimetic agents (e.g. isoprenaline, dobutamine): Combination with bisoprolol may reduce the effect of both agents.
Increased risk of bradycardia.
Sympathomimetics that activate both β- and α-adrenoceptors (e.g. noradrenaline, adrenaline): Combination with bisoprolol may unmask the α-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.
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 atrio-ventricular block.
Bisoprolol must be used with caution in strict fasting.
Bisoprolol must be used with caution in in patients with first degree AV block.
In patients with phaeochromocytoma bisoprolol must not be administered until after alpha-receptor blockade.
Bisoprolol must be used with caution in ongoing desensitisation therapy. As with other beta-blockers, bisoprolol may increase both the sensitivity towards allergens and the severity of anaphylactic reactions. Adrenaline treatment does not always give the expected therapeutic effect.
Bisoprolol must be used with caution in patients with peripheral arterial occlusive disease. Intensification of complaints may occur especially when starting therapy.
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, Concor may be used with caution. In bronchial asthma or other chronic obstructive lung diseases, which may cause symptoms, bronchodilating therapy should be given concomitantly. Occasionally an increase of the airway resistance may occur in patients with asthma, therefore the dose of beta2-stimulants may have to be increased.
Bisoprolol must be used with caution in bronchospasm (bronchial asthma, obstructive airways diseases).
In patients undergoing the general anaesthesia beta-blockade reduces the incidence of arrhythmias and myocardial ischemia during induction and intubation, and the post-operative period. It is currently recommended that maintenance beta-blockade be continued peri-operatively. The anaesthesist must be aware of beta-blockade because of the potential for interactions with other drugs, resulting in bradyarrhythmias, attenuation of the reflex tachycardia and the decreased reflex ability to compensate for blood loss. If it is thought necessary to withdraw beta-blocker therapy before surgery, this should be done gradually and completed about 48 hours before anaesthesia.
Bisoprolol must be used with caution in patients with diabetes mellitus showing large fluctuations in blood glucose values. Symptoms of hypoglycaemia can be masked.
Bisoprolol must be used with caution in 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.
Patients with psoriasis or with a history of psoriasis should only be given beta-blockers (e.g. bisoprolol) after carefully balancing the benefits against the risks.
Under treatment with bisoprolol the symptoms of a thyrotoxicosis may be masked.
Bisoprolol has pharmacological effects that may cause harmful effects on pregnancy and/or the fetus/newborn. In general, β-adrenoceptor blockers reduce placental perfusion, which has been associated with growth retardation, intrauterine death, abortion or early labour. Adverse effects (e.g. hypoglycaemia and bradycardia) may occur in the fetus and newborn infant. If treatment with β-adrenoceptor blockers is necessary, β1-selective adrenoceptor blockers are preferable.
Bisoprolol is not recommended during pregnancy unless clearly necessary. If treatment is considered necessary, monitoring of the uteroplacental blood flow and 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 hypoglycaemia and bradycardia are generally to be expected within the first 3 days.
There are no data on the excretion of bisoprolol in human breast milk or the safety of bisoprolol exposure in infants. Therefore, breastfeeding is not recommended during administration of bisoprolol.
In a study of coronary heart disease patients, bisoprolol did not impair driving performance. However, depending on the individual patient’s response to treatment, the ability to drive a vehicle or to use machines may be impaired. This should be considered particularly at the start of treatment and upon change of medication or in conjunction with alcohol.
The following definitions apply to the frequency terminology used hereafter: Very common (≥1/10), Common (≥1/100, <1/10), Uncommon (≥1/1,000, <1/100), Rare (≥1/10,000, <1/1,000), Very rare (<1/10,000).
Uncommon: sleep disorders, depression.
Rare: nightmares, hallucination.
Common: dizziness*, headache*.
Rare: syncope.
Rare: reduced tear flow (to be considered if the patient uses lenses).
Very rare: conjunctivitis.
Rare: hearing disorders.
Very common: bradycardia (in patients with chronic heart failure).
Common: worsening of pre-existing heart failure (in patients with chronic heart failure).
Uncommon: AV-conduction disturbances; worsening of pre-existing heart failure (in patients with hypertension or angina pectoris); bradycardia (in patients with hypertension or angina pectoris).
Common: feeling of coldness or numbness in the extremities, hypotension especially in patients with heart failure.
Uncommon: orthostatic hypotension.
Uncommon: bronchospasm in patients with bronchial asthma or a history of obstructive airways disease.
Rare: allergic rhinitis.
Common: gastrointestinal complaints such as nausea, vomiting, diarrhoea, constipation.
Rare: hepatitis.
Rare: hypersensitivity reactions such as pruritus, flush, rash and angioedema.
Very rare: alopecia, beta-blockers may provoke or worsen psoriasis or induce psoriasis-like rash.
Uncommon: muscular weakness, muscle cramps.
Rare: erectile dysfunction
Common: asthenia (in patients with chronic heart failure), fatigue*.
Uncommon: asthenia (in patients with hypertension or angina pectoris).
Rare: increased triglycerides, increased liver enzymes (ALAT, ASAT).
No data are available.
applies only to hypertension or angina pectoris:
* These symptoms especially occur at the beginning of the therapy. They are generally mild and often disappear within 1 to 2 weeks.
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