Bisoprolol (Fumarate)

Bisoprolol (Fumarate) is cardioselective beta-blocking agent. It slows the heart rate and reduces high blood pressure. Bisoprolol (Fumarate) is used in the treatment of angina (chest pain), hypertension, and arrhythmias (irregular heartbeats).


Adult Dose
Dose: 5 to 20 mg
Single Dose: 12 (12.5)
Frequency: 24 hourly
Route: PO
Instructions: Gradually Increased
Neonatal
Paedriatic
Characteristics
. It is of Synthetic origin and belongs to Phenoxypropanol. It belongs to Beta-1 adrenergic antagonist pharmacological group on the basis of mechanism of action. The Molecular Weight of Bisoprolol (Fumarate) is 384.00. Its pKa is 9.5.
Contraindications
Bisoprolol (Fumarate) is contraindicated in conditions like Bronchospasm,Heart block,Bradycardia,Severe hemorrhage,Untreated heart failure.
Effects
The severe or irreversible adverse effects of Bisoprolol (Fumarate), which give rise to further complications include Bronchospasm, Decreased cardiac performance, Cardiogenic shock, Bradycardia, AV-block, Necrosis of extremities.Bisoprolol (Fumarate) produces potentially life-threatening effects which include Severe bronchospasm, Hypoglycemia, Hypotension, Bradyarrhythmias, Rebound phenomenon. which are responsible for the discontinuation of Bisoprolol (Fumarate) therapy.The symptomatic adverse reactions produced by Bisoprolol (Fumarate) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Tiredness, Headache, Cold extremities, Sweating, Impotence, Weakness of the leg.
Indications
Bisoprolol (Fumarate) is primarily indicated in conditions like Adjunct in stable moderate to severe heart failure, Angina, Arterial hypertension, Cardiac arrhythmia, Hyperthyroidism, Ischaemic heart disease, Prophylaxis of NSAID-induced gastric and duodenal ulceration, Schizophrenia and other psychoses.
Interactions
Bisoprolol (Fumarate) is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAdrenalineSevere hypertension when beta-blockers given with Adrenaline.Amiodarone (HCl)Amiodarone may enhance the bradycardic effect of Bisoprolol. Possibly to the point of cardiac arrest.MajorMonitor increased signs and symptoms of bradycardia with Bisoprolol (possibly to the point of cardiac arrest) if amiodarone is initiated/dose increased, or decreased effects if amiodarone is discontinued/dose decreased. Ophthalmic beta-blockers are likely of little concern.Cimetidine (HCl)Clonidine (HCl)DigoxinBisoprolol may potentiate bradycardia due to Digoxin.ModerateMonitor for increased bradycardia if these two agents are used concomitantly. Ophthalmic beta-blockers are likely of little concern.Diltiazem (HCl)Severe hypotension and heart failure when beta-blockers given with Diltiazem.IndacaterolBeta-blockers may exacerbate bronchospasms in patients with COPDmonitor closelyIndomethacinNSAIDs antagonizes antihypertensive effects of beta-blockers.NaproxenNaproxen through renal prostaglandin synthesis inhibition reduces the antihypertensive activity of bisoprolol.ModerateAltered antihypertensive response is monitored whenever naproxen is introduced or discontinued in treatment.NifedipineCoadministration additively reduces in heart rate, cardiac conduction and cardiac contractility. While this combination is useful in congestive heart failure, severe hypotension and angina.ModerateDose of both agents must be adjusted and close clinical monitoring of hemodynamic response must be recommended.RifampicinMetabolism of Bisoprolol accelerated by Rifampicin (plasma concentration significantly reduced)ModerateTheophyllineBisoprolol reduces the CYP450 hepatic metabolism of theophylline and its serum levels may be increased.MajorClosely monitored the increased serum level of theophylline and decreased bronchodilatory effectiveness.Verapamil (HCl)Severe hypotension and heart failure when beta-blockers given with Verapamil.VORICONAZOLEVoriconazole may increase the serum concentration of bisoprolol by decreasing its metabolismMonitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or if doses are changed. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Bilirubin measurement by diazo method Determination of metanephrines by the Pisano Method
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Tab Store in a well closed container, Below 40°C. Protect from Sunlight and Moisture.
Warnings
Bisoprolol should be used with caution in patients with history of heart, kidney or liver diseases, asthma, bronchitis, emphysema or other lungs disease, diabetes, hyperthyroidism or any drug allergy. Before having surgery, tell the doctor or dentist about the use of the drug. This drug should be used only if clearly needed during pregnancy or lactation.
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