Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 45, 2015 - Issue 5
368
Views
10
CrossRef citations to date
0
Altmetric
Research Article

An in vitro approach to investigate ocular metabolism of a topical, selective β1-adrenergic blocking agent, betaxolol

, &
Pages 396-405 | Received 26 Sep 2014, Accepted 10 Nov 2014, Published online: 05 Dec 2014

References

  • Al-Ghananeem AM, Crooks PA. (2007). Phase I and phase II ocular metabolic activities and the role of metabolism in ophthalmic prodrug and codrug design and delivery. Molecules 12:373–88
  • Barar J, Javadzadeh AR, Omidi Y. (2008). Ocular novel drug delivery: impacts of membranes and barriers. Expet Opin Drug Deliv 5:567–81
  • Campbell DA, Schoenwald RD, Duffel MW, Barfknecht CF. (1991). Characterization of arylamine acetyltransferase in the rabbit eye. Invest Ophth Vis Sci 32:2190–200
  • Dunne CE, Bushee JL, Argikar UA. (2013). Metabolism of bromopride in mouse, rat, rabbit, dog, monkey, and human hepatocytes. Drug Metab Pharmacokinet 28:453–61
  • Farag HH, Wu WM, Barros MD, et al. (1997). Ocular-specific chemical delivery systems of betaxolol for safe local treatment of glaucoma. Drug Des Discov 15:117–30
  • Frishman WH, Kowalski M, Nagnur S, et al. (2001). Cardiovascular considerations in using topical, oral, and intravenous drugs for the treatment of glaucoma and ocular hypertension: focus on beta-adrenergic blockade. Heart Dis 3:386–97
  • Frishman WH, Tepper D, Lazar EJ, Behrman D. (1990). Betaxolol: a new long-acting beta 1-selective adrenergic blocker. J Clin Pharmacol 30:686–92
  • Fukano Y, Kawazu K. (2009). Disposition and metabolism of a novel prostanoid antiglaucoma medication, tafluprost, following ocular administration to rats. Drug Metab Dispos 37:1622–34
  • Gammons MV, Fedorov O, Ivison D, et al. (2013). Topical antiangiogenic SRPK1 inhibitors reduce choroidal neovascularization in rodent models of exudative AMD. Invest Ophthalmol Vis Sci 54:6052–62
  • Gevariya HB, Patel JK. (2013). Long acting betaxolol ocular inserts based on polymer composite. Curr Drug Deliv 10:384–93
  • Girol AP, Mimura KK, Drewes CC, et al. (2013). Anti-inflammatory mechanisms of the annexin A1 protein and its mimetic peptide Ac2-26 in models of ocular inflammation in vivo and in vitro. J Immunol 190:5689–701
  • Gunduz M, Argikar UA, Baeschlin D, et al. (2010). Identification of a novel N-carbamoyl glucuronide: in vitro, in vivo, and mechanistic studies. Drug Metab Dispos 38:361–7
  • Hermann P, Fraisse J, Allen J, et al. (1984). Determination of betaxolol, a new beta-blocker, by gas chromatography mass spectrometry: application to pharmacokinetic studies. Biomed Mass Spectrom 11:29–34
  • Holló G, Whitson JT, Faulkner R, et al. (2006). Concentrations of betaxolol in ocular tissues of patients with glaucoma and normal monkeys after 1 month of topical ocular administration. Invest Ophth Vis Sci 47:235–40
  • Jain K, Kumar RS, Sood S, Dhyanandhan G. (2013). Betaxolol hydrochloride loaded chitosan nanoparticles for ocular delivery and their anti-glaucoma efficacy. Curr Drug Deliv 10:493–9
  • Lee VH, Chien DS, Sasaki H. (1988). Ocular ketone reductase distribution and its role in the metabolism of ocularly applied levobunolol in the pigmented rabbit. J Pharmacol Exp Ther 246:871–8
  • Lee VH. (1983). Esterase activities in adult rabbit eyes. J Pharm Sci 72:239–44
  • Lesar TS. (1987). Comparison of ophthalmic beta-blocking agents. Clin Pharm 6:451–63
  • Levin LA, Nilsson SFV, Hoeve JV, Qu SM. (2011). Adler’s Physiology of the eye. New York, NY: Saunders Elsevier Inc
  • Ludden TM, Boyle DA, Gieseker D, et al. (1988). Absolute bioavailability and dose proportionality of betaxolol in normal healthy subjects. J Pharm Sci 77:779–83
  • Mohutsky MA, Wrighton SA, Ring BJ. (2008). In vitro metabolism: subcellular Fractions. In: Pearson PG, LC W, eds. Handbook of drug metabolism. New York: Informa Healthcare, 445–64
  • Nakamura K, Fujiki T, Tamura HO. (2005). Age, gender and region-specific differences in drug metabolising enzymes in rat ocular tissues. Exp Eye Res 81:710–15
  • Phan TM, Nguyen KP, Giacomini JC, Lee DA. (1991). Ophthalmic beta-blockers: determination of plasma and aqueous humor levels by a radioreceptor assay following multiple doses. J Ocul Pharmacol 7:243–52
  • Quistad GB, Staiger LE, Schooley DA. (1986). The role of carnitine in the conjugation of acidic xenobiotics. Drug Metab Dispos 14:521–5
  • Schmetterer L, Strenn K, Findl O, et al. (1997). Effects of antiglaucoma drugs on ocular hemodynamics in healthy volunteers. Clin Pharmacol Ther 61:583–95
  • Schwartzman ML, Masferrer J, Dunn MW, et al. (1987). Cytochrome P450, drug metabolizing enzymes and arachidonic acid metabolism in bovine ocular tissues. Curr Eye Res 6:623–30
  • Sparks DL, Thomas TN, Buckholtz NS. (1981). Monamine oxidase activity in bovine retina: subcellular distribution and drug sensitivities. Neurosci Lett 21:201–16
  • Stagni G, Davis PJ, Ludden TM. (1991). Human pharmacokinetics of betaxolol enantiomers. J Pharm Sci 80:321–4
  • Ulrich RG, Bacon JA, Cramer CT, et al. (1998). Disruption of mitochondrial activities in rabbit and human hepatocytes by a quinoxalinone anxiolytic and its carboxylic acid metabolite. Toxicology 131:33–47
  • Volotinen M, Maenpaa J, Kankuri E, et al. (2009). Expression of cytochrome P450 (CYP) enzymes in human nonpigmented ciliary epithelial cells: induction of CYP1B1 expression by TCDD. Invest Ophthalmol Vis Sci 50:3099–105
  • Watkins 3rd JB, Wirthwein DP, Sanders RA. (1991). Comparative study of phase II biotransformation in rabbit ocular tissues. Drug Metab Dispos 19:708–13
  • Wong YW, Ludden TM. (1990). Determination of betaxolol and its metabolites in blood and urine by high-performance liquid chromatography with fluorimetric detection. J Chromatogr 534:161–72
  • Zateyshchikov DA, Minushkina LO, Brovkin AN, et al. (2007). Association of CYP2D6 and ADRB1 genes with hypotensive and antichronotropic action of betaxolol in patients with arterial hypertension. Fundam Clin Pharm 21:437–43
  • Zhang T, Xiang CD, Gale D, et al. (2008). Drug transporter and cytochrome P450 mRNA expression in human ocular barriers: implications for ocular drug disposition. Drug Metab Dispos 36:1300–7
  • Zimmerman TJ. (1993). Topical ophthalmic beta blockers: a comparative review. J Ocul Pharmacol 9:373–84

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.