Common side effects when used in the eyes include itchiness, redness, and a dry mouth.[1] Common side effects when used on the skin include redness, burning, and headaches.[2] More significant side effects may include allergic reactions and low blood pressure.[2][1] Use in pregnancy appears to be safe.[2][1] When applied to the eye it works by decreasing the amount of 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.[3] It is available as a generic medication.[4][5] In 2021, it was the 160th most commonly prescribed medication in the United States, with more than 3million prescriptions.[6][7]
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.
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 cultureedit
Namesedit
It is sold under the brand names Alphagan, Alphagan-P, Mirvaso, Lumify, Brymont, and others.
Over the counteredit
In July 2018, Bausch and Lomb began to market 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]
Referencesedit
^ abcdefg"Brimonidine Tartrate eent Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 17 March 2019.
^ abcdefg"Brimonidine Tartrate topical Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 17 March 2019.
^Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 550. ISBN9783527607495.
^"Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 29 June 2023. from the original on 29 June 2023. Retrieved 29 June 2023.
^British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1153. ISBN9780857113382.
^"The Top 300 of 2021". ClinCalc. from the original on 15 January 2024. Retrieved 14 January 2024.
^"Brimonidine - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
^Sena DF, Lindsley K (January 2017). "Neuroprotection for treatment of glaucoma in adults". The Cochrane Database of Systematic Reviews. 1 (1): CD006539. doi:10.1002/14651858.CD006539.pub4. PMC5370094. PMID 28122126.
^Toris CB, Camras CB, Yablonski ME (July 1999). "Acute versus chronic effects of brimonidine on aqueous humor dynamics in ocular hypertensive patients". American Journal of Ophthalmology. 128 (1): 8–14. doi:10.1016/s0002-9394(99)00076-8. PMID 10482088.
Further readingedit
Oh DJ, Chen JL, Vajaranant TS, Dikopf MS (January 2019). "Brimonidine tartrate for the treatment of glaucoma". Expert Opin Pharmacother. 20 (1): 115–122. doi:10.1080/14656566.2018.1544241. PMID 30407890. S2CID 53240954.
brimonidine, agonist, medication, used, treat, open, angle, glaucoma, ocular, hypertension, rosacea, rosacea, improves, redness, used, drops, applied, skin, clinical, datapronunciation, eentrade, namesalphagan, mirvaso, lumify, othersahfs, drugs, commonographm. Brimonidine is an a2 agonist medication used to treat open angle glaucoma ocular hypertension and rosacea 1 2 In rosacea it improves the redness 2 It is used as eye drops or applied to the skin 1 2 BrimonidineClinical dataPronunciation b r ɪ ˈ m oʊ n ɪ d iː n bri MOH nid eenTrade namesAlphagan Mirvaso Lumify othersAHFS Drugs comMonographMedlinePlusa601232License dataUS DailyMed BrimonidinePregnancycategoryAU B3Routes ofadministrationTopicalATC codeD11AX21 WHO S01EA05 WHO S01GA07 WHO Legal statusLegal statusUS only OTCPharmacokinetic dataMetabolismPrimarily liverElimination half life3 hours ocular 12 hours topical IdentifiersIUPAC name 5 Bromo N 4 5 dihydro 1H imidazol 2 yl quinoxalin 6 amineCAS Number59803 98 4 YPubChem CID2435IUPHAR BPS520DrugBankDB00484 YChemSpider2341 YUNIIE6GNX3HHTEKEGGD07540 YChEBICHEBI 3175 YChEMBLChEMBL844 YCompTox Dashboard EPA DTXSID3045221ECHA InfoCard100 149 042Chemical and physical dataFormulaC 11H 10Br N 5Molar mass292 140 g mol 13D model JSmol Interactive imageMelting point252 C 486 F SMILES Brc2c1nccnc1ccc2N C3 N CCN3InChI 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 YKey XYLJNLCSTIOKRM UHFFFAOYSA N Y verify Common side effects when used in the eyes include itchiness redness and a dry mouth 1 Common side effects when used on the skin include redness burning and headaches 2 More significant side effects may include allergic reactions and low blood pressure 2 1 Use in pregnancy appears to be safe 2 1 When applied to the eye it works by decreasing the amount of 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 3 It is available as a 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 Contents 1 Medical uses 2 Mechanism of action 3 Society and culture 3 1 Names 3 2 Over the counter 4 References 5 Further readingMedical uses editBrimonidine 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 editBrimonidine is an a2 adrenergic agonist 1 a2 agonists through the activation of a G protein coupled receptor inhibit the activity of adenylate cyclase This reduces cAMP and hence aqueous humour production by the ciliary body Peripheral a2 agonist activity results in vasoconstriction of blood vessels as opposed to central a2 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 a adrenergic stimulation This may lead to relaxed ciliary muscle and increased uveoscleral outflow 9 Society and culture editNames edit It is sold under the brand names Alphagan Alphagan P Mirvaso Lumify Brymont and others Over the counter edit In July 2018 Bausch and Lomb began to market 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 edit 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 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 Fischer J Ganellin CR 2006 Analogue based Drug Discovery John Wiley amp Sons p 550 ISBN 9783527607495 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 British national formulary BNF 76 76 ed Pharmaceutical Press 2018 p 1153 ISBN 9780857113382 The Top 300 of 2021 ClinCalc Archived from the original on 15 January 2024 Retrieved 14 January 2024 Brimonidine Drug Usage Statistics ClinCalc Retrieved 14 January 2024 Sena DF Lindsley K January 2017 Neuroprotection for treatment of glaucoma in adults The Cochrane Database of Systematic Reviews 1 1 CD006539 doi 10 1002 14651858 CD006539 pub4 PMC 5370094 PMID 28122126 Toris CB Camras CB Yablonski ME July 1999 Acute versus chronic effects of brimonidine on aqueous humor dynamics in ocular hypertensive patients American Journal of Ophthalmology 128 1 8 14 doi 10 1016 s0002 9394 99 00076 8 PMID 10482088 Further reading editOh DJ Chen JL Vajaranant TS Dikopf MS January 2019 Brimonidine tartrate for the treatment of glaucoma Expert Opin Pharmacother 20 1 115 122 doi 10 1080 14656566 2018 1544241 PMID 30407890 S2CID 53240954 Portal nbsp Medicine Retrieved from https en wikipedia org w index php title Brimonidine amp oldid 1209085674, wikipedia, wiki, book, books, library,
