II. Indications

III. Mechanism

  1. See Beta Adrenergic ReceptorAntagonist
  2. Selective Beta Antagonist that primarily inhibits B1 activity by blocking B1 Receptors
    1. Reduces Myocardial Contractility, Blood Pressure, myocardial oxygen demand
    2. Also Antiarrhythmic and slows ventricular response in Atrial Fibrillation
  3. Contrast with non-selective Beta Blockers (e.g. Propranolol)
    1. Non-selective Beta Blockers also act at B2 Receptors (bronchoconstriction) and B3 Receptors (block lipolysis)

IV. Adverse Effects

V. Drug Interactions

VI. Metabolism

  1. Bioavailability 90%
    1. Low first pass hepatic metabolism
  2. Primarily excreted by the liver
  3. Lipophilic

VII. Dosing

  1. Start: 10 mg orally daily
    1. Start at 5 mg in older patients or with renal Impairment
  2. Maximum: 20 mg/day

VIII. Safety

  1. Pregnancy Category C
  2. Unknown Safety in Lactation

X. References

  1. (2019) Presc Lett, Resource #350503, Comparison of Oral Beta Blockers
  2. (2020) Med Lett Drugs Ther 62(1598): 73-80
  3. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 66-7
  4. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Related Studies

Cost: Medications

betaxolol (on 6/22/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
BETAXOLOL 10 MG TABLET Generic $0.58 each
BETAXOLOL HCL 0.5% EYE DROP Generic $9.32 per ml

Ontology: Betaxolol (C0005320)

Definition (NCI) A racemic mixture and selective beta-1 adrenergic receptor antagonist with antihypertensive and anti-glaucoma activities and devoid of intrinsic sympathomimetic activity. Betaxolol selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure. When applied topically in the eye, this agent reduces aqueous humor secretion and lowers the intraocular pressure (IOP). In addition, betaxolol prevents the release of renin, a hormone secreted by the kidneys that causes constriction of blood vessels.
Definition (MSH) A cardioselective beta-1-adrenergic antagonist with no partial agonist activity.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D015784
SnomedCT 349900007, 409276006
LNC LP70622-3
English Betaxolol, 2-Propanol, 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-, Betaxolol [Chemical/Ingredient], 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-propanol, betaxolol, BETAXOLOL, Betaxolol (product), Betaxolol (substance)
Swedish Betaxolol
Czech betaxolol
Finnish Betaksololi
Russian BETAKSOLOL, БЕТАКСОЛОЛ
Japanese 塩酸ベタキシソロール, ベタキール, ベトプティック, タルロング, ベタキソン, ベトキソロール, ケルロング, ケフナン, アロング, ベタキソロール
Polish Betaksolol
Spanish betaxolol (producto), betaxolol, betaxolol (sustancia), Betaxolol
French Bétaxolol
German Betaxolol
Italian Betaxololo
Portuguese Betaxolol