Betaxolol

Source: Wikipedia, the free encyclopedia.
Betaxolol
Clinical data
Trade namesKerlone
AHFS/Drugs.comMonograph
MedlinePlusa609023
Pregnancy
category
  • AU: C
Routes of
administration		By mouth, ocular
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability89%
MetabolismLiver
Elimination half-life14–22 hours
ExcretionKidney (20%)
Identifiers
  • (RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-
    phenoxy}-3-(isopropylamino)propan-2-ol
JSmol)
ChiralityRacemic mixture
  • O(CCc1ccc(OCC(O)CNC(C)C)cc1)CC2CC2
  • 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
  (verify)

Betaxolol is a selective

aqueous humor) within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with elevated intraocular pressure due to glaucoma
.

It was patented in 1975 and approved for medical use in 1983.[3]

Medical uses

Hypertension

Betaxolol is most commonly ingested orally alone or with other medications for the management of essential hypertension.[4] It is a cardioselective beta blocker, targeting beta-1 adrenergic receptors found in the cardiac muscle. Blood pressure is decreased by the mechanism of blood vessels relaxing and improving the flow of blood.[5][6]

Glaucoma

Ophthalmic betaxolol is an available treatment for

primary open angle glaucoma (POAG) and optical hypertension. Betaxolol effectively prevents the increase of intracellular calcium, which leads to increased production of the aqueous humor. In the context of open angle glaucoma, increased aqueous humor produced by ciliary bodies increases intraocular pressure, causing degeneration of retinal ganglion cells and the optic nerve.[7]

Furthermore, betaxolol is additionally able to protect retinal neurones following topical application from

ischemia-reperfusion, providing a neuroprotective effect. This is thought to be attributed to its capacity to attenuate neuronal calcium and sodium influx.[8] Betaxolol is also an effective treatment for Intraocular pressure[9]

Paronychia

One study showed that topical betaxolol can be used in treating relapsed paronychia.[10]

Contraindications

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

Side effects

The adverse side-effects of betaxolol can be categorized into local and systemic effects.[7] The local effects include:

  • transient irritation (20-40% of patients)
  • burning
  • pruritus
    , or general itching
  • punctate keratitis
  • blurry vision[11]

Systemically, patients taking betaxolol might experience:

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.

Society and culture

Brand names

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

See also

References

  1. S2CID 46962082
    .
  2. ^ "Google Scholar". scholar.google.com. Retrieved 2023-12-26.
  3. ISBN 9783527607495
    .
  4. PMID 32491793
    , retrieved 2023-12-26
  5. ^ "Betaxolol: MedlinePlus Drug Information". medlineplus.gov. Retrieved 2023-01-12.
  6. ^ "Betaxolol: MedlinePlus Drug Information". medlineplus.gov. Retrieved 2023-12-26.
  7. ^
    PMID 32491793
    . Retrieved 2023-01-12.
  8. PMID 12634114
    .
  9. PMID 7619450
    – via Google Scholar.
  10. S2CID 39861588
    .
  11. S2CID 46962082
    .

External links
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