Skip to main content
Log in

Ocular hypotensive effect of topical ketanserin in timolol users

  • Clinical Investigation
  • Published:
Graefe's Archive for Clinical and Experimental Ophthalmology Aims and scope Submit manuscript

Abstract

• Background: Ketanserin is a specific antagonist of 5-HT2 and 5-HT1c receptors. These receptors are linked to the stimulation of phosphoinositide metabolism and are involved in IOP controls. Orally and topically administered ketanserin reduces IOP in normotensive and glaucomatous eyes. • Methods: Ketanserin 0.5% eye drops were administered to 20 patients with primary open-angle glaucoma in a randomised, crossover, double-masked fashion to evaluate the effect of ketanserin in glaucomatous patients already receiving timolol who did not have controlled IOP (>21 mmHg). Mean and range of IOP curve (8.00 a.m.–8.00 p.m.), pupil diameter, Schirmer 1, basal secretion test and BUT values were recorded at baseline and after 2 weeks of topical administration of ketanserin or placebo twice daily. The alternative treatment was given 2 weeks later and the same protocol was repeated. • Results: When patients received placebo no significant variations were found in the analysed parameters. Ketanserin significantly reduced mean IOP (19.5%) and was effective for up to 12 h without inducing variations of tear secretion or pupil diameter. No systemic side effects were observed, and no significant variations in ocular symptoms and signs were reported. • Conclusion: These results indicate that topical administration of ketanserin may be useful to reduce IOP in patients not controlled with beta-blockers.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Cazzola M, D'Amato G, Lobefalo G, Guillaro B, Sepe S, Assogna G (1987) Ketanserin, a new blocking agent of serotonin S2 receptors: respiratory functional effects in chronic obstruction of the airways. Chest 92: 863–867

    PubMed  Google Scholar 

  2. Chang Fw, Burke JA, Potter DE (1985) Mechanism of the ocular hypotensive action of ketanserin. J Ocul Pharmacol 1: 137–147

    PubMed  Google Scholar 

  3. Conway JL, Lewis RA (1980) Ocular hypotensive action of ketanserin. Invest Ophthalmol Vis Sci 30 [Suppl]: 24

    Google Scholar 

  4. Costagliola C, Scibelli G, Fasano ML, Ferrara LA and Mastropasqua L (1991) Effect on oral ketanserin administration on intraocular pressure in glaucomatous patients. Exp Eye Res 52: 507–510

    PubMed  Google Scholar 

  5. Costagliola C, Ferrara LA, Fasano L, Iuliano G, Menzione M, Scibelli G, Mastropasqua L (1993) Ketanserin as an ocular hypotensive agent. Glaucoma 15: 55–59

    Google Scholar 

  6. Costagliola C, Iuliano G, Rinaldi M, Russo V, Scibelli G, Mastropasqua L (1993) Effect of topical ketanserin administration on intraocular pressure. Br J Ophthalmol 77: 344–348

    PubMed  Google Scholar 

  7. Cyrlin MN, Thomas JV, Epstein DL (1982) Additive effect of epinephrine to timolol in primary open angle glaucoma. Arch Ophthalmol 100: 414–418

    PubMed  Google Scholar 

  8. Dermailly P, Lehner M, Etienne R, Trepsat C, Hout J, Raynaud G (1979) Rèsultant d'une ètude à mòyen terme en double aveugle comparant le malèate de timolol ou l'èpinèphrine sur 120 patients parteur d'un glaucome chronique à angle ouvert. J Fr Ophthalmol 12: 727–735

    Google Scholar 

  9. Frazer A, Maayani S, Wolfe BB (1990) Subtypes of receptors for serotonin. Annu Rev Pharmacol Toxicol 30:307–348

    PubMed  Google Scholar 

  10. Greenidge KC, Spaeth GL, Fiol-Silva Z (1983) Effect of argon laser trabeculoplasty on the glaucomatous diurnal curve. Ophthalmology 90: 800–809

    PubMed  Google Scholar 

  11. Hodapp E (1985) Computerized perimetry in glaucoma. In: Spaeth GL (ed) Computerized visual field. Slack, Thorofare, NJ, pp 197–238

    Google Scholar 

  12. Jones LJ (1966) The lacrimal system and its treatment. Am J Ophthalmol 62: 47–60

    PubMed  Google Scholar 

  13. Karnezis TA, Murphy MB, Weber RR, Nelson KS, Tripathi BJ, Tripathi RC (1988) Effects of selective dopamine 1-receptor activation on intraocular pressure in man. Exp Eye Res 47: 689–698

    PubMed  Google Scholar 

  14. Kass MA (1996) Standardizing the measurement of intraocular pressure for clinical research. Ophthalmology 103: 183–185

    PubMed  Google Scholar 

  15. Krootila K, Palkama A, Uusitalo H (1987) Effect of serotonin and its antagonist (ketanserin) on intraocular pressure in rabbits. J Ocular Pharmacol 3: 279–290

    Google Scholar 

  16. Kurowski M (1985) Bioavailability and pharmacokinetics of ketanserin in elderly subjects. Eur J Clin Pharmacol 28: 411–417

    PubMed  Google Scholar 

  17. Leier CV, Baker ND, Weber PA (1986) Cardiovascolar effects of ophthalmic timolol. Ann Intern Med 104: 197–199

    PubMed  Google Scholar 

  18. Marwood JF, Stokes GS (1984) Serotonin (5-HT) and its antagonists: involvement in the cardiovascular system. Clin Exp Pharmacol Physiol 11: 439–456

    PubMed  Google Scholar 

  19. MacMahon CD, Shaffer RM, Hoskins HD, Hetherington J (1979) Adverse effects experienced by patients taking timolol. Am J Ophthalmol 88: 736–741

    PubMed  Google Scholar 

  20. Osborne NN (1980) In vitro experiments on the metabolism uptake and release of 5-hydroxytryptamine in bovine retina. Brain Res 184: 283–291

    PubMed  Google Scholar 

  21. Osborne NN, Tobin AB (1987) Serotonin accumulating cells in the irisciliary body and cornea of various species. Exp Eye Res 44: 731–746

    PubMed  Google Scholar 

  22. Osborne NN, Meyer-Bothling U, Barnett NL (1994) Serotonin receptors in the eye. In: Anderson DR, Drance SM (eds) Encounters in glaucoma research. 1. receptor biology and glaucoma. Fogliazza, Abbiategrasso, Italy, pp 331–360

    Google Scholar 

  23. Palkama A, Lehtosalo J, Uusitalo H (1984) 5-Hydroxytryptamine receptors in the cornea and ciliary processes of the rabbit and human eyes. Ophthalmic Res 16: 207–208

    Google Scholar 

  24. Peroutka SJ (1990) 5-Hydroytryptamine receptor subtypes. Pharmacol Toxicol 67: 373–383

    PubMed  Google Scholar 

  25. Rolando M (1984) Semeiotica della patologia del film lacrimale. In: Calabria G, Rolando M (eds) Fisiopatologia del film lacrimale. Soc Ophthalmol Ital, Rome, pp 97–132

    Google Scholar 

  26. Riemann IW, Frolich JC (1983) Mechanism of antihypertensive action of ketanserin in man. Br Med J 287: 381–383

    Google Scholar 

  27. Schirmer O (1903) Studien zur Physiologie und Pathologie der Tränenabsonderung und Tränenabfuhr. Graefes Arch F Ophthalmol 56: 197–291

    Google Scholar 

  28. Setten GV van, Stephen R, Tervo T, Salonen EM, Tarkkanen A, Vaheri A (1990) Effects of the Schirmer test on the fibrinolytic system in the tear fluid. Exp Eye Res 50: 135–141

    PubMed  Google Scholar 

  29. Suda K, Furushima M, Kihara K (1961) Influence of antiglaucomatous surgery on the diurnal variation of the ocular tension in simple glaucoma. Acta Soc Ophthalmol Jpn 65: 1711–1719

    Google Scholar 

  30. Symoens J, Janssens M (1986) Ketanserin: a novel cardiovascular drug. Drug Dev Res 8: 159–172

    Google Scholar 

  31. Tobin AB, Unger W, Osborne NN (1988) Evidence for the presence of serotonergic neurones and receptors in the iris-ciliary body complex of the rabbit. J Neurosci 8: 3713–3721

    PubMed  Google Scholar 

  32. Uusitalo H, Lehtosalo J, Laakso J, Harkonen M, Palkama A (1982) Immunocytochemical and biochemical evidence for 5-hydroxytryptamine containing nerves in the anterior part of the eye. Exp Eye Res 35: 671–675

    PubMed  Google Scholar 

  33. Weinreb RN, Caldwell DR, Goode SM, Horwitz BL, Laibovitz R, Shrader E, Stewart RH, Williams T (1990) A double-masked three-month comparison between 0.25% betaxolol suspension and 0.5% betaxolol ophthalmic solution. Am J Ophthalmol 110:189–192

    PubMed  Google Scholar 

  34. Worthen DM (1976) Effect of pilocarpine drops on the diurnal intraocular pressure variation in patients with glaucoma. Invest Ophthalmol 15: 784–790

    PubMed  Google Scholar 

  35. Yablonski ME, Zimmermam T, Walman S, Becker B (1987) A fluorophotometric study of the effect of topical timolol on aqueous humor dynamics. Exp Eye Res 44: 135–142

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Mastropasqua, L., Ciancaglini, M., Carpineto, P. et al. Ocular hypotensive effect of topical ketanserin in timolol users. Graefe's Arch Clin Exp Ophthalmol 235, 130–135 (1997). https://doi.org/10.1007/BF00941719

Download citation

  • Received:

  • Revised:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00941719

Keywords

Navigation