Betaxolol Hcl (betaxolol HCl)

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

Betaxolol hydrochloride is a beta1-selective adrenergic blocking agent. Betaxolol is related structurally to metoprolol, differing only by the addition of a cyclopropyl group at the terminal carbon of the methoxyethyl side chain of metoprolol. The presence of large substituents in the para position is believed to account in part for the selective beta1-adrenergic blocking effect of betaxolol.

Betaxolol is one of the most potent and selective beta1-adrenergic blocking agents currently available. In vitro studies indicate that the beta1-adrenergic blocking activity of betaxolol on a molar basis is approximately the same as that of propranolol, 2-8 times that of metoprolol, and 9 times that of atenolol. The drug does not exhibit intrinsic sympathomimetic (beta1-agonist) activity and does not have substantial membrane-stabilizing (local anesthetic) activity.

At low dosages, betaxolol hydrochloride 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, the selectivity of betaxolol hydrochloride for beta1-adrenergic receptors usually diminishes, and the drug will competitively inhibit beta1- and beta2-adrenergic receptors.

USP currently states that potency of betaxolol hydrochloride preparations should be expressed both in terms of the salt and the base (''active moiety''). Commercially available tablets containing 10 or 20 mg of betaxolol hydrochloride contain 8.94 or 17.88 mg of betaxolol, respectively. Whereas dosage and potency of betaxolol hydrochloride tablets are expressed in terms of the salt, dosage of ophthalmic preparations of the drug are expressed in terms of the base.

Therefore, care should be taken to avoid confusion between labeled potencies as the salt and base and dosage of betaxolol hydrochloride.

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.

The choice of a beta-adrenergic blocking agent (beta-blocker) depends on numerous factors, including pharmacologic properties (e.g., relative beta-selectivity, intrinsic sympathomimetic activity, membrane-stabilizing activity, lipophilicity), pharmacokinetics, intended use, and adverse effect profile, as well as the patient's coexisting disease states or conditions, response, and tolerance. While specific pharmacologic properties and other factors may appropriately influence the choice of a beta-blocker in individual patients, evidence of clinically important differences among the agents in terms of overall efficacy and/or safety is limited. Patients who do not respond to or cannot tolerate one beta-blocker may be successfully treated with a different agent.

Generic name: betaxolol HCl
Pronunciation: (be-TAX-oh-lol)

The following indications are listed for Betaxolol Hcl:

• Hypertension

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

No ICD codes are available for this drug.