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Bisoprolol Fumarate (bisoprolol fumarate)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Bisoprolol is a beta1-selective adrenergic blocking agent (beta-blocker).

Bisoprolol is a beta1-selective adrenergic blocking agent. Bisoprolol is related structurally to acebutolol, atenolol, and metoprolol in that the drugs contain substituents in the para position of the benzene ring; the presence of large substituents in the para position is believed to account in part for the selective beta1-adrenergic blocking effect of these drugs. The commercially available drug is a racemic mixture of the 2 optical isomers; however, only the l-isomer of bisoprolol has substantial beta-adrenergic blocking activity.

The drug does not exhibit the intrinsic sympathomimetic activity seen with pindolol or the membrane-stabilizing activity possessed by propranolol or pindolol. At low dosages, bisoprolol selectively inhibits response to adrenergic stimuli by competitively blocking cardiac beta1-adrenergic receptors, while having little effect on the beta2-adrenergic receptors of bronchial and vascular smooth muscle. At high doses (e.g., 20 mg or higher), the selectivity of bisoprolol on beta1-adrenergic receptors usually diminishes, and the drug will competitively inhibit beta1- and beta2-adrenergic receptors.

The drug is commercially available as the fumarate.

SumMon(R)(see Users Guide). For additional information on this drug until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the labeling be consulted for detailed information on the usual cautions, precautions, and contraindications.

Bisoprolol is used in the management of hypertension. The drug also has been used in the management of heart failure+.

Generic name: bisoprolol fumarate
Pronunciation: (BIS-oh-PROE-lol)

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Bisoprolol Fumarate:

  • Hypertension

Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.

Dosing

Adjustment of dosage of bisoprolol-containing therapy based solely on age does not appear to be necessary in geriatric patients, unless appreciable renal or hepatic impairment is present. (See Dosage and Administration: Dosage in Renal and Hepatic Impairment.)

Since pharmacokinetics of bisoprolol may be altered in patients with renal impairment (i.e., creatinine clearance less than 40 mL/minute) or hepatic impairment, the manufacturer states that bisoprolol fumarate should be initiated at 2.5 mg daily in such patients. If needed, dosage of bisoprolol fumarate should be increased with caution. Limited data indicate that patients with severe renal impairment (i.e., creatinine clearances less than 20 mL/minute per 1.73 m2) generally should not receive bisoprolol fumarate dosages exceeding 10 mg once daily. Since limited data suggest that the drug is not removed by dialysis, the manufacturer states that patients undergoing dialysis do not require a supplemental dose afterward. If progressive renal impairment develops in any patient receiving bisoprolol fumarate in fixed combination with hydrochlorothiazide, the manufacturer recommends that the combination be discontinued.

Drug interactions

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Contraindications

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Adverse reactions

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Precautions

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ICD codes

No ICD codes are available for this drug.

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data