Brimonidine

Source: Wikipedia, the free encyclopedia.
Brimonidine
Clinical data
Pronunciation/brɪˈmoʊnɪdiːn/ bri-MOH-nid-een
Trade namesAlphagan, Mirvaso, Lumify, others
AHFS/Drugs.comMonograph
MedlinePlusa601232
License data
Pregnancy
category
  • AU: B3
Routes of
administration		Topical
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismPrimarily liver
Elimination half-life3 hours (ocular), 12 hours (topical)
Identifiers
  • 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl) quinoxalin-6-amine
JSmol)
Melting point252 °C (486 °F)
  • Brc2c1nccnc1ccc2N/C3=N/CCN3
  • InChI=1S/C11H10BrN5/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8/h1-4H,5-6H2,(H2,15,16,17) checkY
  • Key:XYLJNLCSTIOKRM-UHFFFAOYSA-N checkY
  (verify)

Brimonidine is an

eye drops or applied to the skin.[1][2]

Common side effects when used in the eyes include itchiness, redness, and a dry mouth.

aqueous humor made while increasing the amount that drains from the eye.[1] When applied to the skin it works by causing blood vessels to contract.[2]

Brimonidine was patented in 1972 and came into medical use in 1996.

generic medication.[4][5] In 2021, it was the 160th most commonly prescribed medication in the United States, with more than 3 million prescriptions.[6][7]

Medical uses

Brimonidine is indicated for the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It is also the active ingredient of brimonidine/timolol along with timolol maleate.

A 2017

Cochrane review found insufficient evidence to determine if brimonidine slows optic nerve damage.[8]

In 2013, the FDA approved topical application of brimonidine 0.33% gel for persistent facial redness of rosacea.

Mechanism of action

Brimonidine is an α2 adrenergic agonist.[1]

α2 agonists, through the activation of a

adenylate cyclase. This reduces cAMP and hence aqueous humour production by the ciliary body
.

Peripheral α2 agonist activity results in vasoconstriction of blood vessels (as opposed to central α2 agonist activity that decreases sympathetic tone, as can be seen by the medication clonidine). This vasoconstriction may explain the acute reduction in aqueous humor flow. The increased uveoscleral outflow from prolonged use may be explained by increased prostaglandin release due to α adrenergic stimulation. This may lead to relaxed ciliary muscle and increased uveoscleral outflow.[9]

Society and culture

Names

It is sold under the brand names Alphagan, Alphagan-P, Mirvaso, Lumify, Brymont, and others.

Over the counter

In July 2018,

over the counter (OTC) eye drops, using brimonidine's tartrate formulation in a concentration of 0.025%, as an ophthalmic vasoconstrictor under the brand name Lumify. Intended to relieve redness in the sclerae of the eyes for periods of up to eight hours at a time through its vasoconstrictive effects, Lumify was marketed as an alternative to Visine, the brand of tetrahydrozoline hydrochloride solution most commonly used for that purpose.[citation needed
]

References

  1. ^ a b c d e f g "Brimonidine Tartrate eent Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 17 March 2019.
  2. ^ a b c d e f g "Brimonidine Tartrate topical Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 17 March 2019.
  3. ISBN 9783527607495
    .
  4. ^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 29 June 2023. Archived from the original on 29 June 2023. Retrieved 29 June 2023.
  5. ISBN 9780857113382
    .
  6. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  7. ^ "Brimonidine - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  8. PMID 28122126
    .
  9. PMID 10482088
    .

Further reading
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