Summary
The absorption of timolol after topical administration to the eye was studied in 11 healthy volunteers and in 5 patients with bilateral open angle glaucoma. The volunteers received 2 drops of 0.5% timolol ophthalmic solution in each eye, equivalent to 0.8mg of timolol maleate. Overflow was absorbed by paper tissue. The patients received the same dose twice daily for 2 weeks and were then investigated. In the paper tissue, 12 to 88% of the dose administered was recovered. Plasma concentrations were never above 5ng/ml and not always detectable (detection limit 1 to 2ng/ml). However, timolol was absorbed as the drug was found in the urine samples from all volunteers and glaucomatous patients.
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References
Akers, M.J.; Schoenwald, R.D. and McGinity, J.W.: Practical aspects of ophthalmic drug development. Drug Development and Industrial Pharmacy 3: 185–217 (1977).
Bobik, A.; Jennings, G.L.; Ashley, P. and Komer, P.I.: Timolol pharmacokinetics and effects on heart rate and blood pressure after acute and chronic administration. European Journal of Clinical Pharmacology 16: 243–249 (1979).
Boger, W.P. III; Puliafito, C.A.; Steinert, R.F. and Langston, D.P.: Long-term experience with timolol ophthalmic solution in patients with open-angle glaucoma. Ophthalmology 85: 259–267 (1978a).
Boger, W.P. III; Steinert, R.F.; Puliafito, C.A. et al: Clinical trial comparing timolol ophthalmic solution to pilocarpine in open-angle glaucoma. American Journal of Ophthalmology 86: 8–18 (1978b).
Bonomi, L. and Steindler, P.: Effect of pindolol on intraocular pressure. British Journal of Ophthalmology 59: 301–303 (1975).
Chrai, S.; Patton, T.F.; Mehta, A. and Robinson, J.R.: Lacrimal and instilled fluid dynamics in rabbit eyes. Journal of Pharmaceutical Sciences 62: 1112–1121 (1973).
Cote, G. and Drance, S.M.: The effect of propranolol on human intraocular pressure. Canadian Journal of Ophthalmology 3: 207–212 (1968).
Else, O.F.; Sorenson, H. and Edwards, I.R.: Plasma timolol levels after oral and intravenous administration. European Journal of Clinical Pharmacology 14: 431–434 (1978).
Heel, R.C.; Brogden, R.N.; Speight, T.M. and Avery, G.S.; Timolol: A review of its therapeutic efficacy in the topical treatment of glaucoma. Drugs 17: 38–55 (1979).
Jones, F.L. and Ekberg, N.L.: Exacerbation of asthma by timolol. New England Journal of Medicine 301: 270 (1979).
Patton, T.F. and Francoeur, M.: Ocular bioavailability and systemic loss of topically applied ophthalmic drugs. American Journal of Ophthalmology 85: 225–229 (1978).
Phillips, C.I.; Howitt, G. and Rowlands, D.J.: Propranolol as ocular hypotensive agent. British Journal of Ophthalmology 51; 222–226 (1967).
Sears, M.L. and Barany, E.H.: Outflow resistance and adrenergic mechanisms. Archives of Ophthalmology 64: 839–848, (1960).
Tocco, J.; deLuna, F.A. and Duncan, A.E.W.: Electron-capture GLC determination of timolol in human plasma and urine. Journal of Pharmaceutical Sciences 64: 1879–1881 (1975).
Vale, G.; Gibbs, A.C. and Phillips, C.I.: Topical propranolol and ocular tension in the human. British Journal of Ophthalmology 56: 770–775 (1972).
Wetrell, K.: Beta-adrenoceptor antagonism and intraocular pressure. Acta Ophthalmologica Suppl. 134 (1977).
Zimmerman, T.J. and Kaufman, H.E.: A beta-adrenergic blocking agent for the treatment of glaucoma. Archives of Ophthalmology 95: 601–604 (1977).
Zimmerman, T.J.; Harbin, R.; Pett, M. and Kaufman, H.E.: Timolol and facility of outflow. Investigational Ophthalmology Visual bsciences 16: 623–624 (1977).
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Supported by the Swedish Medical Research Council (04X-3902).
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Alvan, G., Calissendorff, B., Seideman, P. et al. Absorption of Ocular Timolol. Clin Pharmacokinet 5, 95–100 (1980). https://doi.org/10.2165/00003088-198005010-00004
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DOI: https://doi.org/10.2165/00003088-198005010-00004