Brimonidine | DrugBank Online

Step 1

Adkins JC, Balfour JA: Brimonidine. A review of its pharmacological properties and clinical potential in the management of open-angle glaucoma and ocular hypertension. Drugs Aging. 1998 Mar;12(3):225-41. doi: 10.2165/00002512-199812030-00005. [PubMed:9534022] Cantor LB, Burke J: Brimonidine. Expert Opin Investig Drugs. 1997 Aug;6(8):1063-83. doi: 10.1517/13543784.6.8.1063 . [PubMed:15989664] Cantor LB: The evolving pharmacotherapeutic profile of brimonidine, an alpha 2-adrenergic agonist, after four years of continuous use. Expert Opin Pharmacother. 2000 May;1(4):815-34. doi: 10.1517/14656566.1.4.815 . [PubMed:11249518] Stewart WC, Stewart JA, Jackson AL: Cardiovascular effects of timolol maleate, brimonidine or brimonidine/timolol maleate in concomitant therapy. Acta Ophthalmol Scand. 2002 Jun;80(3):277-81. [PubMed:12059866] Suwanwipat S, Buranakarl C, Chaiyabutr N: Effects of brimonidine ingestion on cardiovascular responses and renal function in conscious dogs. Vet Res Commun. 2007 Apr;31(3):323-34. doi: 10.1007/s11259-006-3414-1. Epub 2006 Dec 28. [PubMed:17195055] Greenfield DS, Liebmann JM, Ritch R: Brimonidine: a new alpha2-adrenoreceptor agonist for glaucoma treatment. J Glaucoma. 1997 Aug;6(4):250-8. [PubMed:9264305] Cantor LB: Brimonidine in the treatment of glaucoma and ocular hypertension. Ther Clin Risk Manag. 2006 Dec;2(4):337-46. [PubMed:18360646] Jackson JM, Knuckles M, Minni JP, Johnson SM, Belasco KT: The role of brimonidine tartrate gel in the treatment of rosacea. Clin Cosmet Investig Dermatol. 2015 Oct 23;8:529-38. doi: 10.2147/CCID.S58920. eCollection 2015. [PubMed:26566370] Toris CB, Gleason ML, Camras CB, Yablonski ME: Effects of brimonidine on aqueous humor dynamics in human eyes. Arch Ophthalmol. 1995 Dec;113(12):1514-7. [PubMed:7487618] Benkali K, Leoni M, Rony F, Bouer R, Fernando A, Graeber M, Wagner N: Comparative pharmacokinetics and bioavailability of brimonidine following ocular and dermal administration of brimonidine tartrate ophthalmic solution and gel in patients with moderate-to-severe facial erythema associated with rosacea. Br J Dermatol. 2014 Jul;171(1):162-9. doi: 10.1111/bjd.12881. Epub 2014 Jul 16. [PubMed:24506775] Galanopoulos A, Goldberg I: Clinical efficacy and neuroprotective effects of brimonidine in the management of glaucoma and ocular hypertension. Clin Ophthalmol. 2009;3:117-22. Epub 2009 Jun 2. [PubMed:19668554] Piwnica D, Pathak A, Schafer G, Docherty JR: In Vitro Safety Pharmacology Profiling of Topical alpha-Adrenergic Agonist Treatments for Erythema of Rosacea. Drugs R D. 2018 Mar;18(1):87-90. doi: 10.1007/s40268-018-0227-y. [PubMed:29374829] MIRVASO (brimonidine) topical gel - FDA Label [Link] Brimonidine (brimonidine tartrate) ophthalmic solution - Product Monograph [Link] Mirvaso (brimonidine) topical gel - EU Summary of Product Characteristics [Link] ALPHAGAN® (brimonidine tartrate ophthalmic solution) 0.2% - FDA Label [Link]

Step 2

Rauly I, Ailhaud M, Wurch T, Pauwels PJ: alpha(2A)-adrenoceptor: G(alphai1) protein-mediated pertussis toxin-resistant attenuation of G(s) coupling to the cyclic AMP pathway. Biochem Pharmacol. 2000 Jun 15;59(12):1531-8. [PubMed:10799649] Wikberg-Matsson A, Simonsen U: Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2049-55. [PubMed:11481271] Meana JJ, Barturen F, Garro MA, Garcia-Sevilla JA, Fontan A, Zarranz JJ: Decreased density of presynaptic alpha 2-adrenoceptors in postmortem brains of patients with Alzheimer's disease. J Neurochem. 1992 May;58(5):1896-904. [PubMed:1373179] Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Step 3

Trendelenburg AU, Philipp M, Meyer A, Klebroff W, Hein L, Starke K: All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons. Naunyn Schmiedebergs Arch Pharmacol. 2003 Dec;368(6):504-12. Epub 2003 Nov 11. [PubMed:14610637] Bohmann C, Schollmeyer P, Rump LC: Methoxamine inhibits noradrenaline release through activation of alpha 1- and alpha 2-adrenoceptors in rat isolated kidney: involvement of purines and prostaglandins. Naunyn Schmiedebergs Arch Pharmacol. 1993 Mar;347(3):273-9. [PubMed:8097565]

Step 4

Trendelenburg AU, Philipp M, Meyer A, Klebroff W, Hein L, Starke K: All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons. Naunyn Schmiedebergs Arch Pharmacol. 2003 Dec;368(6):504-12. Epub 2003 Nov 11. [PubMed:14610637] Orito K, Kishi M, Imaizumi T, Nakazawa T, Hashimoto A, Mori T, Kambe T: alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator. Br J Pharmacol. 2001 Oct;134(4):763-70. [PubMed:11606316] Zhang W, Ordway GA: The alpha2C-adrenoceptor modulates GABA release in mouse striatum. Brain Res Mol Brain Res. 2003 Apr 10;112(1-2):24-32. [PubMed:12670699] Prinster SC, Holmqvist TG, Hall RA: Alpha2C-adrenergic receptors exhibit enhanced surface expression and signaling upon association with beta2-adrenergic receptors. J Pharmacol Exp Ther. 2006 Sep;318(3):974-81. Epub 2006 Jun 6. [PubMed:16757535]

Step 5

Acheampong AA, Chien DS, Lam S, Vekich S, Breau A, Usansky J, Harcourt D, Munk SA, Nguyen H, Garst M, Tang-Liu D: Characterization of brimonidine metabolism with rat, rabbit, dog, monkey and human liver fractions and rabbit liver aldehyde oxidase. Xenobiotica. 1996 Oct;26(10):1035-55. [PubMed:8905918]