Betaxolol

Betaxolol
Names
Pronunciationbe tax' oh lol[1]
Trade namesKerlone[1]
IUPAC name
  • (RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-
    phenoxy}-3-(isopropylamino)propan-2-ol
Clinical data
Drug classCardioselective beta blocker[1]
Main usesHigh blood pressure, glaucoma[1]
Side effectsBy mouth: Slow heart rate, low blood pressure, tiredness, dizziness, depression, trouble sleeping, memory loss, sexual dysfunction[1]
Eye drop: Eye irritation[2]
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Pregnancy
category
  • AU: C
    Routes of
    use    		By mouth, eye drop
    Typical dose10 to 40 mg OD[1]
    External links
    AHFS/Drugs.comSystemic: Monograph
    Eye: Monograph
    MedlinePlusa609023
    Legal
    Legal status
    • In general: ℞ (Prescription only)
    Pharmacokinetics
    Bioavailability89%
    MetabolismLiver
    Elimination half-life14–22 hours
    ExcretionKidney (20%)
    Chemical and physical data
    FormulaC18H29NO3
    Molar mass307.434 g·mol−1
    3D model (JSmol)
    ChiralityRacemic mixture
    SMILES
    • O(CCc1ccc(OCC(O)CNC(C)C)cc1)CC2CC2
    InChI
    • InChI=1S/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3 checkY
    • Key:NWIUTZDMDHAVTP-UHFFFAOYSA-N checkY

    Betaxolol, sold under the brand name Kerlone among others, is a medication used to treat glaucoma and high blood pressure.[1] It reduces eye pressure by about 30%.[3] It is not a first line treatment for blood pressure.[4] It is take by mouth or used as an eye drop.[1]

    Common side effects by mouth include slow heart rate, low blood pressure, tiredness, dizziness, depression, trouble sleeping, memory loss, and sexual dysfunction.[1] At high doses it can induce bronchospasm.[1] Common side effects from the eye drops include eye irritation.[2] Safety in pregnancy is unclear.[4] It is a selective beta1 receptor blocker.[1] As an eye drop it is thought to work by reducing the production of aqueous humor within the eye.[3]

    Betaxolol was patented in 1975 and approved for medical use in 1983.[5] It is available as a generic medication.[1] In the United Kingdom a 5 ml bottle of eye drops costs the NHS about £2 as of 2021.[2] In the United States this amount costs about 21 USD.[6]

    Medical uses

    • Oral: for the management of hypertension
    • Ophthalmic: for the management of glaucoma
    • the drug seems to have an effect of neuroprotection in glaucoma treatment

    Dosage

    By mouth it is usually started at a dose of 10 mg once per day, which may be increased up to 40 mg per day.[1]

    The eye drops are applied twice per day.[2]

    Contraindications

    • Hypersensitivity to the drug
    • Patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure

    Side effects

    See also: Beta blocker

    History

    Betaxolol was approved by the U.S. Food and Drug Administration (FDA) for ocular use as a 0.5% solution (Betoptic) in 1985 and as a 0.25% solution (Betoptic S) in 1989.

    Brand names

    Brand names include Betoptic, Betoptic S, Lokren, Kerlone.

    See also

    References

    1. 1 2 3 4 5 6 7 8 9 10 11 12 13 "Betaxolol". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. 2012. Archived from the original on 15 May 2021. Retrieved 10 January 2022.
    2. 1 2 3 4 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1224. ISBN 978-0857114105.
    3. 1 2 "Betaxolol (EENT) Monograph for Professionals". Drugs.com. Archived from the original on 24 January 2021. Retrieved 10 January 2022.
    4. 1 2 "Betaxolol (Systemic) Monograph for Professionals". Drugs.com. Archived from the original on 6 August 2021. Retrieved 10 January 2022.
    5. ↑ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495. Archived from the original on 2017-09-08. Retrieved 2021-03-21.
    6. ↑ "Betaxolol Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 6 October 2016. Retrieved 10 January 2022.
    Identifiers:
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