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Review

Adrenergic agonists and antagonists as antiglaucoma agents: a literature and patent review (2013–2019)

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Pages 805-815 | Received 30 Jul 2019, Accepted 04 Sep 2019, Published online: 09 Sep 2019

References

  • Quigley HA. Glaucoma. Lancet. 2011;377:1367–1377.
  • Zhang K, Zhang L, Weinreb RN. Ophthalmic drug discovery: novel targets and mechanisms for retinal disease and glaucoma. Nat Rev Drug Discov. 2012;11:541–559.
  • Quigley HA, Broman AT. The number of people with glaucoma worldwide in 2010 and 2020. Br J Ophthalmol. 2006;90:151–156.
  • Tham YC, Li X, Wong TY, et al. Global prevalence of glaucoma and projections of glaucoma burden through 2040: a systematic review and meta-analysis. Ophthalmology. 2014;121:2081–2090.
  • Martin MJ, Summer A, Gold EB. Race and primary open-angle glaucoma. Am J Ophthalmol. 1985;99:383–387.
  • Migdal C, Gregory W, Hitchings R. Long-term functional outcome after early surgery compared with laser and medicine in open-angle glaucoma. Ophthalmology. 1994;101:1651–1656.
  • Hoyng PFJ, van Beek LM. Pharmacological therapy for glaucoma. Drugs. 2000;59:411–434.
  • Yadav KS, Rajpurohit R, Sharma S. Glaucoma: current treatment and impact of advanced drug delivery systems. Life Sci. 2019;221:362–376.
  • Gazzard G, Konstantakopoulou E, Garway-Heath D, et al. Selective laser trabeculoplasty versus eye drops for first-line treatment of ocular hypertension and glaucoma (LiGHT): a multicentre randomised controlled trial. Lancet. 2019;393:1505–1516.
  • Whitson JT. Glaucoma: a review of adjunctive therapy and new management strategies. Expert Opin Pharmacother. 2007;8:3237–3249.
  • Mcauliffe-curtin D, Buckley C. Review of alpha adrenoceptor function in the eye. Eye. 1989;3:472–476.
  • Townsend DJ, Brubaker RF. Immediate effect of epinephrine on aqueous formation in the normal human eye as measured by fluorophotometry. Invest Ophthalmol Vis Sci. 1980;19:256–266.
  • Mandell AI, Stentz F, Kitabchi AE. Dipivalyl epinephrine: a new pro-drug in the treatment of glaucoma. Ophthalmology. 1978;85:268–275.
  • Kass MA, Mandell AI, Goldberg I, et al. Dipivefrin and epinephrine treatment of elevated intraocular pressure: a comparative study. Arch Ophthalmol. 1979;97:1865–1866.
  • Krieglstein GK, Gramer E. The response of ophthalmic arterial pressure to topically applied clonidine. Albrecht Von Graefes Arch Klin Exp Ophthalmol. 1978; 2071–2075.
  • Harrison R, Kaufmann CS. Clonidine: effects of a topically administered solution on intraocular pressure and blood pressure in open-angle glaucoma. Arch Ophthalmol. 1977;95:1368–1373.
  • Gharagozloo NZ, Relf SJ, Brubaker RF. Aqueous flow is reduced by the alpha-adrenergic agonist, apraclonidine hydrochloride (ALO 2145). Ophthalmology. 1988;95:1217–1220.
  • Toris CB, Tafoya ME, Camras CB, et al. Effects of apraclonidine on aqueous humor dynamics in human eyes. Ophthalmology. 1995;102:456–461.
  • Toris CB, Gleason ML, Camras CB, et al. Effects of brimonidine on aqueous humor dynamics in human eyes. Arch Ophthalmol. 1995;113:1514–1517.
  • Walters TR. Development and use of brimonidine in treating acute and chronic elevations of intraocular pressure: a review of safety, efficacy, dose response, and dosing studies. Surv Ophthalmol. 1996;41:S19–26.
  • Brooks AM, Gillies WE. Ocular beta-blockers in glaucoma management. Clinical pharmacological aspects. Drugs Aging. 1992;2:208–221.
  • Schehlein EM, Novack G, Robin AL. New pharmacotherapy for the treatment of glaucoma. Expert Opin Pharmacother. 2017;18:1939–1946.
  • Phillips CI, Howitt G, Rowlands DJ. Propranolol as ocular hypotensive agent. Br J Ophthalmol. 1967;51:222–226.
  • Coakes RL, Brubaker RF. The mechanism of timolol in lowering intraocular pressure in the normal eye. Arch Ophthalmol. 1978;96:2045–2048.
  • Obstbaum SA, Galin MA, Katz IM. Timolol: effect on intraocular pressure in chronic open-angle glaucoma. Ann Ophthalmol. 1978;10:1347–1351.
  • Katz IM, Berger ET. Effects of iris pigmentation on response of ocular pressure to timolol. Surv Ophthalmol. 1979;23:395–398.
  • McMahon CD, Shaffer RN, Hoskins HDJ, et al. Adverse effects experienced by patients taking timolol. Am J Ophthalmol. 1979;88:736–738.
  • Reiss GR, Brubaker RF. The mechanism of betaxolol, a new ocular hypotensive agent. Ophthalmology. 1983;90:1369–1372.
  • Caldwell DR, Salisbury CR, Guzek JP. Effects of topical betaxolol in ocular hypertensive patients. Arch Ophthalmol. 1984;102:539–540.
  • Nelson WL, Kuritsky JN. Early postmarketing surveillance of betaxolol hydrochloride, Sept 1985-Sept 1986. Am J Ophthalmol. 1987;103:592.
  • Cinotti A, Cinotti D, Grant W, et al. Levobunolol vs timolol for open-angle glaucoma and ocular hypertension. Am J Ophthalmol. 1985;99:11–17.
  • Berson FG, Cohen HB, Foerster RJ, et al. Levobunolol compared with timolol for the long-term control of elevated intraocular pressure. Arch Ophthalmol. 1985;103:379–382.
  • Mills KB, Raines M, Joyce P. A single blind, stratified, randomised, noncrossover trial comparing carteolol 1% with timolol 0.25% in the long-term management of glaucoma. Br J Clin Pract. 1987;51:10–12.
  • Van Brummelen P. The relevance of intrinsic sympathomimetic activity for beta-blocker-induced changes in plasma lipids. J Cardiovasc Pharmacol. 1983;5:S51–5.
  • Battershill PE, Sorkin EM. Ocular metipranolol: a preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in glaucoma and ocular hypertension. Drugs. 1988;36:601–615.
  • Bleckmann H, Pham Duy T, Grajewski O. Therapeutic efficacy of metipranolol eyedrops 0.3% versus timolol eyedrops 0.25%: a double blind cross over study. In: Merte HJ, editor. Metipranolol. Wien: Springer-Verlag; 1983. p. 106.
  • Hollo G, Topouzis F, Fechtner RD. Fixed combination intraocular pressure-lowering therapy for glaucoma and ocular hypertension: advantages in clinical practice. Expert Opin Pharmacother. 2014;15:1737–1747.
  • Rulo AH, Greve EL, Hoyng PF. Additive effect of latanoprost, a prostaglandin F2 alpha analogue, and timolol in patients with elevated intraocular pressure. Br J Ophthalmol. 1994;78:899–902.
  • Alm A, Widengard I, Kjellgren D, et al. Latanoprost administered once daily caused a maintained reduction of intraocular pressure in glaucoma patients treated concomitantly with timolol [see comments]. Br J Ophthalmol. 1995;79:12–16.
  • Stewart WC, Day DG, Sharpe ED, et al. Effi cacy and safety of timolol solution once daily vs timolol gel added to latanoprost. Am J Ophthalmol. 1999;128:692–696.
  • Guven Yilmaz S, Degirmenci C, Karakoyun YE, et al. The efficacy and safety of bimatoprost/timolol maleate, latanoprost/timolol maleate, and travoprost/timolol maleate fixed combinations on 24-h IOP. Ophthalmol. 2018;38:1425–1431.
  • Fuwa M, Shimazaki A, Mieda M, et al. Efficacy and safety of the fixed combinations of tafluprost/timolol and latanoprost/carteolol. Sci Rep. 2019;9:7491.
  • Hartleben C, Parra JC, Batoosingh A, et al. A masked, randomized, phase 3 comparison of triple fixed-combination bimatoprost/brimonidine/timolol versus fixed-combination brimonidine/timolol for lowering intraocular pressure. Ophthalmol. 2017;2017:4586763.
  • Lee DA, Gornbein JA. Effectiveness and safety of brimonidine as adjunctive therapy for patients with elevated intraocular pressure in a large, open-label community trial. J Glaucoma. 2001;10:220–226.
  • Erdogan H, Toker I, Arici MK, et al. A short-term study of the additive effect of latanoprost 0.005% and brimonidine 0.2%. Jpn. J Ophthalmol. 2003;47:473–478.
  • Zabriski N, Netland PA. Brimonidine with latanoprost study groups I and II: comparison of brimonidine/latanoprost and timolol/dorzolamide: two randomized, double-masked, parallel clinical trials. Adv Ther. 2003;20:92–100.
  • Netland PA, Michael M, ROsner SA, et al. Brimonidine purite and bimatoprost compared with timolol and latanoprost in patients with glaucoma and ocular hypertension. Adv Ther. 2003;20:20–30.
  • Kass MA. Efficacy of combining timolol with other antiglaucoma medications. Surv Ophthalmol. 1983;28:274–279.
  • Tsoy EA, Meekins BB, Shields MB. Comparison of two treatment schedules for combined timolol and dipivefrin therapy. Am J Ophthalmol. 1986;102:320–324.
  • Alexander DW, Berson FG, Epstein DL. A clinical trial of timolol and epinephrine in the treatment of primary open-angle glaucoma. Ophthalmology. 1988;95:247–251.
  • Berson FG, Epstein DL. Separate and combined effects of timolol maleate and acetazolamide in open-angle glaucoma. Am J Ophthalmol. 1981;92:788–791.
  • Kass MA, Korey M, Gordon M, et al. Timolol and acetazolamide. A study of concurrent administration. Arch Ophthalmol. 1982;100:941–942.
  • Strohmaier K, Snyder E, Dubiner H, et al. The efficacy and safety of the dorzolamide-timolol combination versus the concomitant administration of its components. Ophthalmology. 1998;105:1936–1944.
  • Boyle JE, Ghosh K, Gieser DK, et al. A randomized trial comparing the dorzolamide-timolol combination given twice daily to monotherapy with timolol and dorzolamide. Ophthalmology. 1998;105:1945–1951.
  • Mundorf TK, Rauchman SH, Williams RD, et al. A patient preference comparison of Azarga (brinzolamide/timolol fixed combination) vs Cosopt (dorzolamide/timolol fixed combination) in patients with open-angle glaucoma or ocular hypertension. Brinzolamide/Timolol preference study group. Clin Ophthalmol. 2008;2:623–628.
  • Balsak S, Kaydu A, Erdem S, et al. Brimonidine-timolol versus brinzolamide-timolol for treatment of elevated intraocular pressure after phacoemulsification surgery. Int Ophthalmol. 2018;38:1583–1589.
  • Cheng JW, Cheng SW, Gao LD, et al. Intraocular pressure-lowering effects of commonly used fixed-combination drugs with timolol: a systematic review and meta-analysis. PLoS One. 2012;7:e45079.
  • Tanihara H, Inoue T, Yamamoto T, et al. K-115 clinical study group. Additive intraocular pressure-lowering effects of the rho kinase inhibitor ripasudil (K-115) Combined with timolol or latanoprost: A report of 2 randomized clinical trials. JAMA Ophthalmol. 2015;133:755–761.
  • Greig SL, Deeks ED. Brinzolamide/brimonidine: a review of its use in patients with open-angle glaucoma or ocular hypertension. Drugs Aging. 2015;32:251–260.
  • Seibold LK, DeWitt PE, Kroehl ME, et al. The 24-hour effects of brinzolamide/brimonidine fixed combination and timolol on intraocular pressure and ocular perfusion pressure. J Ocul Pharmacol Ther. 2017;33:161–169.
  • Gupta S, Vyas SP. Carbopol/chitosan based pH triggered in-situ gelling system for ocular delivery of timolol maleate. Sci Pharm. 2010;78:959–976.
  • Pang X, Li J, Pi J, et al. Increasing efficacy and reducing systemic absorption of brimonidine tartrate ophthalmic gels in rabbits. Pharm Dev Technol. 2018;23:231–239.
  • Achouri D, Alhanout K, Piccerelle P, et al. Recent advances in ocular drug delivery. Drug Dev Ind Pharm. 2013;39:1599–1617.
  • Gupta H, Jain S, Mathur R, et al. Sustained ocular drug delivery from a temperature and pH triggered novel in-situ gel system. Drug Deliv. 2007;14:507–515.
  • Azmin MN, Florence AT, Handjani-Vila RM, et al. The effect of non-ionic surfactant vesicle (niosome) entrapment on the absorption and distribution of methotrexate in mice. J Pharm Pharmacol. 1985;37:237–242.
  • Fernández-Colino A, Quinteros DA, Allemandi DA, et al. Self-assembling elastin-like hydrogels for timolol delivery: development of an ophthalmic formulation against glaucoma. Mol Pharm. 2017;14:4498–4508.
  • Li J, Tian S, Tao Q, et al. Montmorillonite/chitosan nanoparticles as a novel controlled-release topical ophthalmic delivery system for the treatment of glaucoma. Int J Nanomedicine. 2018;13:3975–3987.
  • Zhao R, Li J, Wang J, et al. Development of timolol-loaded galactosylated chitosan nanoparticles and evaluation of their potential for ocular drug delivery. AAPS PharmSciTech. 2017;18:997–1008.
  • Lancina MGIII, Singh S, Kompella UB, et al. Fast dissolving dendrimernanofiber mats as alternative to eye drops for more efficient antiglaucoma drug delivery. ACS Biomater Sci Eng. 2017;3:1861–1868.
  • Shokry M, Hathout RM, Mansour S. Exploring gelatin nanoparticles as novel nanocarriers for timolol maleate: augmented in-vivo efficacy and safe histological profile. Int J Pharm. 2018;545:229–239.
  • De Souza F, Júlio NM, Kamila PSDO, et al. Ocular inserts based on chitosan and brimonidine tartrate: development, characterization and biocompatibility. J Drug Delivery Sci Technol. 2016;32:21–30.
  • Ken C, Wenkui FK, Corpuz EG; et al. Therapeutic compounds. JP2014139175. 2014
  • Huang GT, Jackson B, Burke JA, et al. Sustained release intraocular implants and methods for treating ocular vasculopathies. US2019167858. 2019.
  • Spada LT, Ghebremeskel AN, Robinson MR Biodegradable alpha-2 agonist polymeric implants and therapeutic uses thereof. US2018353426. 2018.
  • Aleksandrovich MI, Fedorovich MJ, Jurevich MD Pharmaceutical composition in form of gel-like ophthalmic drops for treating glaucoma. RU2576778. 2016.
  • Leland JL, Yang M, Bauman J, et al. Drugs and compositions for ocular delivery. WO2019118924. 2019.
  • Enkatraman S, Boey YCF, Natarajan J Sustained timolol maleate delivery from liposomes for glaucoma therapy and occular hypertension. US2017246175. 2017.
  • Gambino TJ, Khoo CCL Microparticle formulations for delivery of active agents. WO2019016686. 2019.
  • Horn G Compositions and methods for treatment of glaucoma. US2017143676. 2017.
  • Sampietro A, Goldberg D, Frost A, et al. Compositions and methods for treating eyes and methods of preparation. US2018318319. 2018.
  • Onishchenko AL, Kolbasko AV, Tarash OS Method for preparation of patient for glaucoma surgery. RU2530647. 2014.
  • Savinainen A, Shawer M. Compounds and compositions for the treatment of ophthalmic disorders. US2018215788. 2018.
  • Karavas E Preservative free pharmaceutical composition for ophthalmic administration containing bimatoprost and timolol. US2019076442. 2019.
  • Qi P, Liu C, Chen Q Brimonidine and betaxolol composition for local ophthalmology application. CN103006662. 2013.
  • Kaushal S Composition for treating ocular disorders such as macular degeneration, retinopathy and glaucoma. WO2019090010. 2019.
  • Koutris EC, Karavas EA A preservative-free ophthalmic formulation comprising dorzolamide and timolol. GR1008505. 2015.
  • Jiao J, Chang CM, Gore AV, et al. Fixed dose combination of brimonidine and timolol. US2018078500. 2018.
  • Reunamaeki T, Oksala O, Alajuuma P, et al. Ophthalmic composition and a method for treating ocular hypertension and glaucoma. WO2018033854. 2018.
  • Csermely P, Agoston V, Pongor S. The efficiency of multi-target drugs: the network approach might help drug design. Trends Pharmacol Sci. 2005;26:178–182.
  • Nocentini A, Ceruso M, Bua S, et al. Discovery of β-adrenergic receptors blocker-carbonic anhydrase inhibitor hybrids for multitargeted antiglaucoma therapy. J Med Chem. 2018;61:5380–5394.
  • Masini E, Carta F, Scozzafava A, et al. Antiglaucoma carbonic anhydrase inhibitors: a patent review. Expert Opin Ther Pat. 2013;23:705–716.
  • Supuran CT. Carbonic anhydrase inhibitors and their potential in a range of therapeutic areas. Expert Opin Ther Pat. 2018;28:709–712.

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