Betaxolol

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Betoptic; Belgium: Betoptic, Kerlone; Bulgaria: Betaxa, Betoptic, Lokren; Cyprus: Betac, Betoptic; Czech Republic: Betalmic, Betamed, Betaxa, Betoptic, Lokren; Denmark: Betoptic; Estonia: Betoptic S; Finland: Betoptic, Kerlon; France: Betoptic, Kerlone; Germany: Kerlone; Greece: Betoptic, Kerlone; Hungary: Betoptic, Lokren; Ireland: Betoptic; Italy: Betoptic, Kerlon; Luxembourg: Betoptic, Kerlone; Netherlands: Betoptic, Kerlon; Poland: Betabion-Bioton SP., Betoptic, Lokren, Optibetol; Portugal: Bertocil, Betoptic, Davixolol; Romania: Betac, Betaxolol, Betoptic, Lokren, Optipres; Slovakia: Betac, Betalmic, Betaxa, Betoptic, Lokren; Slovenia: Betoptic S; Spain: Betaxolol, Betoptic; Sweden: Betoptic; UK: Betoptic.

North America

Canada: Betoptic, Betaxolol; USA: Betoptic S, Kerlone.

Latin America

Argentina: Betasel; Brazil: Betaxolol, Betoptic, Presmín; Mexico: Betoptic, BTX-HA Ofteno.

Asia

Japan: Along, Betakyl, Betaxolol, Betaxon, Betoptic, Kefnan, Kerlong, Tarlong.

Drug combinations

Chemistry

Betaxolol Hydrochloride: C~18~H~29~NO~3~ HCl. Mw: 343.89. (1) 2-Propanol, 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-, hydrochloride, (±)-; (2)(±)-1-[p-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)-2-propanol hydrochloride. CAS-63659-19-8; CAS-63659-18-7 (betaxolol)(1983).

Pharmacologic Category

EENT Preparations; Antiglaucoma Agents; β-Adrenergic Blocking Agents; β~1~-Selective β-Blockers. Cardiovascular Drugs; β-Adrenergic Blocking Agents. (ATC-Code: C07AB05; S01ED02).

Mechanism of action

Competitively blocks β~1~-receptors, with little or no effect on β~2~-receptors (bronchial and vascular smooth muscle; only at high doses). No intrinsic sympathomimetic activity and little or no membrane-stabilizing effect (local anesthetic) on the heart. Reduces blood pressure by decreasing cardiac output, decreasing sympathetic outflow from the CNS, and/or suppressing renin release. Reduces intraocular pressure by reducing the production of aqueous humor (may block endogenous catecholamine-stimulated increases in cyclic adenosine monophosphate concentrations within the ciliary processes and subsequent formation of aqueous humor).

Therapeutic use

Reduction of elevated intraocular pressure in chronic open-angle glaucoma and ocular hypertension (has been used effectively in glaucoma following laser trabeculoplasty). Reduction of systemic hypertension. Initial management of hypertension in heart failure, postmyocardial infarction, high coronary disease risk, and/or diabetes mellitus.

Pregnancy and lactiation implications

Should be used during pregnancy only when clearly needed and should be used with caution in nursing women. It is unlikely that clinically important doses of the drug would be ingested by breast-fed infants during ophthalmic use of usual betaxolol dosages in the woman.

Unlabeled use

Contraindications

Hypersensitivity to betaxolol or any component of the formulation. Sinus bradycardia. Heart block greater than first-degree (except in patients with a functioning artificial pacemaker). Cardiogenic shock. Uncompensated cardiac failure.

Warnings and precautions

Caution with history of severe anaphylaxis to allergens. In general, patients with bronchospastic disease should not receive β-blockers, but betaxolol, with β~1~ selectivity, has been used cautiously with close monitoring (caution in reactive airway disease on pulmonary function testing or excessive restriction of pulmonary function). Caution in history of cardiac failure or heart block. Caution in patients on concurrent verapamil or diltiazem (bradycardia or heart block can occur). Caution in cerebrovascular insufficiency (hypotension and decreased heart rate may reduce cerebral blood flow). Caution in diabetes mellitus (may potentiate and/or mask signs and symptoms of hypoglycemia). May mask signs of hyperthyroidism (e.g. tachycardia). Caution in myasthenia gravis and myasthenic symptoms (may potentiate myasthenia-related muscle weakness, including diplopia and ptosis). May precipitate or aggravate symptoms of arterial insufficiency in peripheral vascular disease and Raynaud’s disease. In case of pheochromocytoma adequate α-blockade is required prior to use of any β-blocker. Caution in history of psychiatric illness (may cause or exacerbate CNS depression). Caution in renal impairment. Caution in patients receiving anesthetic agents which decrease myocardial function due to decreased ability of the heart to respond to reflex β-adrenergic stimuli. β-Blocker therapy should not be withdrawn abruptly (particularly in coronary artery disease). Ophthalmic suspension contains benzalkonium chloride, which may be absorbed by contact lenses. Should not be used alone in angle-closure glaucoma (has no effect on pupillary constriction). Choroidal detachment reported with aqueous suppressant therapy after filtration procedures. Oral betaxolol may interfere with glaucoma screening tests. May be absorbed systemically following topical application to the eye, especially in excessive restriction of pulmonary function. Severe respiratory and cardiac reactions, including death resulting from bronchospasm in asthma and, rarely, death associated with cardiac failure, reported following topical (ocular) β-adrenergic blocking agents. In addition, topical betaxolol and a systemic β-adrenergic blocking agent may add effects on intraocular pressure and/or systemic effects of β-adrenergic blockade. Ophthalmic betaxolol should also be used with caution in patients subject to spontaneous hypoglycemia or with diabetes mellitus. Patients having or suspected of developing thyrotoxicosis should be monitored closely during ophthalmic betaxolol therapy.

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