Route of penetration of topically instilled nipradilol into the ipsilateral posterior retina

Investigative Ophthalmology and Visual Science

Volumn 50, Issue 6, 2009, Pages 2839-2847

  Mizuno, Ken ^a   Koide, Takashi ^a   Shimada, Shunsuke ^a   Mori, Junko ^a   Sawanobori, Kimio ^a   Araie, Makoto ^b  

^a KOWA COMPANY LTD   (Japan)

^b UNIVERSITY OF TOKYO   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

NIPRADILOL; ANTIHYPERTENSIVE AGENT; PROPANOLAMINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; CHOROID; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG TISSUE LEVEL; ISOLATION PROCEDURE; LIQUID CHROMATOGRAPHY; MALE; MASS SPECTROMETRY; NONHUMAN; OPTIC NERVE; PRIORITY JOURNAL; RABBIT; RADIOACTIVITY; RETINA; ANIMAL; BIOAVAILABILITY; DRUG ADMINISTRATION ROUTE; METABOLISM; RAT; SPRAGUE DAWLEY RAT; TANDEM MASS SPECTROMETRY; TISSUE DISTRIBUTION; TOPICAL DRUG ADMINISTRATION;

ADMINISTRATION, TOPICAL; ANIMALS; ANTIHYPERTENSIVE AGENTS; AUTORADIOGRAPHY; BIOLOGICAL AVAILABILITY; CHOROID; CHROMATOGRAPHY, LIQUID; DRUG ADMINISTRATION ROUTES; MALE; PROPANOLAMINES; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; RETINA; TANDEM MASS SPECTROMETRY; TISSUE DISTRIBUTION;

EID: 66849127757     PISSN: 01460404     EISSN: 15525783     Source Type: Journal    
DOI: 10.1167/iovs.08-2922     Document Type: Article

References (39)

1. Jarvinen K, Jarvinen T, Urtti A. Ocular absorption following topical delivery. Adv Drug Deliv Rev. 1995;16(1):3-19.
2. Conroy CW. Sulfonamides do not reach the retina in therapeutic amounts after topical application to the cornea. J Ocul Pharmacol Ther. 1997;13(5):465-472.
3. Maurice DM. Drug delivery to the posterior segment from drops. Surv Ophthalmol. 2002;47(suppl 1):S41-S52.
4. Acheampong AA, Shackleton M, Tang-Liu DD, Ding S, Stern ME, Decker R. Distribution of cyclosporin A in ocular tissues after topical administration to albino rabbits and beagle dogs. Curr Eye Res. 1999;18(2):91-103.
5. Acheampong AA, Shackleton M, John B, Burke J, Wheeler L, Tang-Liu D. Distribution of brimonidine into anterior and posterior tissues of monkey, rabbit, and rat eyes. Drug Metab Dispos. 2002; 30(4):421-429.
6. Hughes PM, Olejnik O, Chang-Lin JE, Wilson CG. Topical and systemic drug delivery to the posterior segments. Adv Drug Deliv Rev. 2005;57(14):2010-2032.
7. Kent AR, Nussdorf JD, David R, Tyson F, Small D, Fellow D. Vitreous concentration of topically applied brimonidine tartrate 0. 2%. Ophthalmology. 2001;108(4):784-787.
8. Osborne NN, DeSantis L, Bae JH, et al. Topically applied betaxolol attenuates NMDA-induced toxicity to ganglion cells and the effects of ischaemia to the retina. Exp Eye Res. 1999;69(3):331-342.
9. Kent AR, King L, Bartholomew LR. Vitreous concentration of topically applied brimonidine-purite 0. 15%. J Ocul Pharmacol Ther. 2006;22(4):242-246.
10. Koevary SB, Nussey J, Lake S. Accumulation of topically applied porcine insulin in the retina and optic nerve in normal and diabetic rats. Invest Ophthalmol Vis Sci. 2002;43(3):797-804.
11. Okamura T, Kitamura Y, Uchiyama M, Toda M, Ayajiki K, Toda N. Canine retinal arterial and arteriolar dilatation induced by nipradilol, a possible glaucoma therapeutic. Pharmacology. 1996; 53(5):302-310.
12. Mizuno K, Koide T, Yoshimura M, Araie M. Neuroprotective effect and intraocular penetration of nipradilol, a beta-blocker with nitric oxide donative action. Invest Ophthalmol Vis Sci. 2001;42(3): 688-694.
13. 2+ antagonist: ocular and periocular penetration after instillation. Invest Ophthalmol Vis Sci. 2003;44(3):1169-1177.
14. Mizuno K, Koide T, Saito N, et al. Topical nipradilol: effects on optic nerve head circulation in humans and periocular distribution in monkeys. Invest Ophthalmol Vis Sci. 2002;43(10):3243-3250.
15. Sponsel WE, Terry S, Khuu HD, Lam KW, Frenzel H. Periocular accumulation of timolol and betaxolol in glaucoma patients under long-term therapy. Surv Ophthalmol. 1999;43(suppl 1):S210-S213.
16. Nilsson SF, Sperber GO, Bill A. The effect of prostaglandin F2 alpha-1-isopropylester (PGF2 alpha-IE) on uveoscleral outflow. Prog Clin Biol Res. 1989;312:429-436.
17. Huang HS, Schoenwald RD, Lach JL. Corneal penetration behavior of beta-blocking agents II: assessment of barrier contributions. J Pharm Sci. 1983;72(11):1272-1279.
18. Huang HS, Schoenwald RD, Lach JL. Corneal penetration behavior of beta-blocking agents III: In vitro-in vivo correlations. J Pharm Sci. 1983;72(11):1279-1281.
19. Prausnitz MR, Noonan JS. Permeability of cornea, sclera, and conjunctiva: a literature analysis for drug delivery to the eye. J Pharm Sci. 1998;87(12):1479-1488.
20. Schoenwald RD, Huang HS. Corneal penetration behavior of betablocking agents I: physiochemical factors. J Pharm Sci. 1983; 72(11):1266-1272.
21. Ohira A, Wada Y, Fujii M, Nakamura M, Kasuya Y, Hamada Y, Shigenobu K. Effects of nipradilol (K-351) on alpha-adrenoceptor mediated responses in various isolated tissues. Arch Int Pharmacodyn Ther. 1985;278(1):61-71.
22. Uchida Y, Nakamura M, Shimizu S, Shirasawa Y, Fujii M. Vasoactive and beta-adrenoceptor blocking properties of 3,4-dihydro-8-(2-hydroxy-3-isopropylamino) propoxy-3-nitroxy-2H-1-benzopyran (K-351), a new antihypertensive agent. Arch Int Pharmacodyn Ther. 1983;262(1):132-149.
23. Kanno M, Araie M, Tomita K, Sawanobori K. Effects of topical nipradilol, a beta-blocking agent with alpha-blocking and nitroglycerin-like activities, on aqueous humor dynamics and fundus circulation. Invest Ophthalmol Vis Sci. 1998;39(5):736-743.
24. Kanno M, Araie M, Koibuchi H, Masuda K. Effects of topical nipradilol, a beta blocking agent with alpha blocking and nitroglycerin-like activities, on intraocular pressure and aqueous dynamics in humans. Br J Ophthalmol. 2000;84(3):293-299.
25. Kanno M, Araie M, Masuda K, et al. Phase III long-term study and comparative clinical study of nipradilol ophthalmic solution in patients with primary open-angle glaucoma and ocular hypertension. Arzneimittelforschung. 2006;56(12):729-734.
26. Kanno M, Araie M, Masuda K, et al. Phase III long-term study and comparative clinical study of nipradilol ophthalmic solution in patients with primary open-angle glaucoma and ocular hypertension. Part 2. Arzneimittelforschung. 2006;56(12):820-825.
27. Shih RL, Lee VH. Rate limiting barrier to the penetration of ocular hypotensive beta blockers across the corneal epithelium in the pigmented rabbit. J Ocul Pharmacol. 1990;6(4):329-336.
28. Ullberg S. Studies on the distribution and fate of S35-labelled benzylpenicillin in the body. Acta Radiol. 1954;118:1-110.
29. Barza M, Kane A, Baum J. Marked differences between pigmented and albino rabbits in the concentration of clindamycin in iris and choroid-retina. J Infect Dis. 1979;139(2):203-208.
30. Kabuto S, Kimata H, Yonemitsu M, Suzuki J. Metabolism of nipradilol by liver homogenates from different species. I. Comparative studies on the denitration of nipradilol and other organic nitrates. Xenobiotica. 1986;16(4):307-315.
31. Koide T, Fujino H, Yoshimura M, Kimata H. Metabolic fate of [14C]KT-210 (nipradilol ophthalmic solution) in rabbits (3): metabolism in plasma, eye and aqueous humor after single instillation to rabbits. Jpn Pharmacol Ther. 1996;24:71-76.
32. Acheampong AA, Shackleton M, Tang-Lu DDS. Comparative ocular pharmacokinetics of brimonidine after a single dose application to the eyes of albino and pigment rabbits. Drug Metab Dispos. 1995; 23(7):708-712.
33. Araie M, Takase M, Sakai Y, Ishii Y, Yokoyama Y, Kitagawa M. Beta-adrenergic blockers: ocular penetration and binding to the uveal pigment. Jpn J Ophthalmol. 1982;26(3):248-263.
34. Fukuda M, Sasaki K. Intraocular dynamic mode differences of new quinolone antibacterial agents between pigmented and albino rabbit eyes. Lens Eye Toxic Res. 1989;6:339-351.
35. Poynter D, Martin LE, Harrison C, Cook J. Affinity of labetalol for ocular melanin. Br J Clin Pharmacol. 1976;3(suppl 3):711-720.
36. Ichikawa M, Okada Y, Asai Y, Hara H, Ishii K, Araie M. Effect of topically instilled bunazosin, an _1-adrenoceptor antagonist, on constrictions induced by phenylephrine and ET-1 in rabbit retinal arteries. Invest Ophthalmol Vis Sci. 2004;45:4041-4048.
37. Yamada Y, Takayanagi R, Ozeki T, Yokoyama H, Iga T, Araie M. Predicting systemic adverse effects associated with nipradilol ophthalmic solution based on beta-receptor occupancy. J Eye. 2006; 23(1):87-94.
38. Grover S, Apushkin MA, Fishman GA. Topical dorzolamide for the treatment of cystoid macular edema in patients with retinitis pigmentosa. Am J Ophthalmol. 2006;141(5):850-858.
39. Maren TH, Conroy CW, Wynns GC, Levy NS. Ocular absorption, blood levels, and excretion of dorzolamide, a topically active carbonic anhydrase inhibitor. J Ocul Pharmacol Ther. 1997;13(1): 23-59.