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).
Primary 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.
Molecular Weight: 384 · pKa: 9.5 · Solubility in Water: > 1 in 1 · Solubility in Alcohol: 1 in 20 · Non-proprietary name: Bisoprolol (Fumarate).
Pharmacokinetics
Absorption: Bisoprolol (Fumarate) has an oral bioavailability is 94.5% (±4.5%), pre-systemic (first-pass) metabolism accounts for 5% (±5%).
Distribution: Bisoprolol (Fumarate) has a volume of distribution is 3 l/kg. plasma protein binding is 30%.
Elimination: it is metabolised via Hepatic, plasma half-life is 10-12 hr, renal excretion is > 50%.
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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.
Contraindications
Bisoprolol (Fumarate) is contraindicated in conditions like Bronchospasm, Heart block, Bradycardia, Severe hemorrhage, Untreated heart failure.
Dosage
Bisoprolol (Fumarate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 12.5 mg | 12.5 mg | Every 24h | PO | Gradually Increased |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Bisoprolol (Fumarate) in overdosage may give rise to further complications which include Bradycardia , AV-block , Bronchospasm , Necrosis of extremities, Cardiogenic shock , Decreased cardiac performance .
Bisoprolol (Fumarate) produces potentially life-threatening effects which include Severe bronchospasm, Hypoglycemia , Hypotension, Bradyarrhythmias , Rebound phenomenon. Careful monitoring is needed with proper medical management.
Bisoprolol (Fumarate) is known to cause more or less tolerable side effects which are usually transient. These include Cold extremities, Dizziness, Headache, Impotence, Sweating , Tiredness , Weakness of the leg.
Warnings / Precautions
Interference in Pathology
Bisoprolol (Fumarate) may interfere in the diagnosis of Bilirubin measurement by diazo method , Determination of metanephrines by the Pisano Method .
Available Brands
Storage Conditions
Drug Classification
- 1.12.3.1 — Beta blocking agents