Skip to main content
SpringerLink
Log in

Ocular penetration of β-adrenergic blocking agents. An experimental study with atenolol, metoprolol, timolol and propranolol

  • Published:
Documenta Ophthalmologica Aims and scope Submit manuscript

Abstract

A comparison was made between the ocular penetration of topically applied 14C-atenolol, 14C-timolol, 14C-propranolol and 3H-metoprolol by means of liquid scintillation counting. Only one eye was treated, the fellow eye served as a control.

Blood plasma levels were measured as well. We could detect a relationship between the ocular penetration and the degree of lipophilicity of the drugs used, as was to be expected. Drugs with a higher degree of lipophilicity penetrated more readily into the eye, whereas they also achieved higher blood plasma levels. Relatively high concentrations of atenolol were found in the nictitating membrane, thus reflecting its poor ocular penetration.

The concentrations detected in the untreated eye were low and probably cannot explain the marked reduction in intraocular pressure observed after unilateral instillation of active β-adrenergic blocking drugs, as for instance timolol. Our findings suggest that the ocular penetration of β-adrenergic blocking agents on topical application only plays a minor part in their ocular hypotensive effect.

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

Access this article

Log in via an institution

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

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  • Barrett, A. M. The pharmacology of atenolol. Postgrad. Med. J. 53: 58–64 (1977).

    CAS  PubMed  Google Scholar 

  • Brenkman, R. F. Ocular hypotensive effect of atenolol 4% eye drops in glaucoma. In: Symposium on medical therapy in glaucoma. Docum. Ophthal. Proc. Ser., vol. 12, 85–94 ed. Dr. W. Junk 1977.

  • Brogden, R. N., Speight, T. M. & Avery, G. S. Timolol: a preliminary report of its pharmacological properties and therapeutic efficiency in angina and hypertension. Drugs 9: 164–177 (1915).

    Article  Google Scholar 

  • Brogden, R. N., Heel, R. C., Speight, T. M. & Avery, G. S. Metoprolol: a review of its pharmacological properties and therapeutic efficiency in hypertension and angina pectoris. Drugs 14: 321–348 (1977).

    Article  CAS  PubMed  Google Scholar 

  • Brown, H. C. Carruthers, S. G., Johnston, G. D., Kelly, J. G., McAinsh, J., McDevitt D. G. Shanks, R. G. Clinical pharmacologic observations on atenolol, a β-adrenoceptor blocker. Clin. Pharmacol. Ther. 20: 524–536 (1976).

    Article  CAS  PubMed  Google Scholar 

  • Phillips, C. I., Gore, S.M., MacDonald, M. J. & Cullen, P.M. Atenolol eye drops in glaucoma. A double masked, controlled study. Brit. J. Ophthal. 61: 349–353 (1977).

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Ruos, F. E., Dake, C. L., Offerhaus, L. & Greve, E. L. Atenolol 4% eye drops and glaucoma. Albrecht v. Graefes Arch. klin. exp. Ophthal. 205: 61–70 (1977).

    Article  Google Scholar 

  • Ros, F. E., Dake, C. L., Nagelkerke, N. D. & Greve, E. L. Metoprolol eye drops in the treatment of glaucoma. Albrecht v. Graefes Arch. klin. exp. Ophthal. 206: 247–254 (1978).

    Article  CAS  Google Scholar 

  • Ros, F. E., Innemee, H. C. & Van Zwieten, P. A. Penetration of atenolol in the rabbit eye. Albrecht v. Graefes Arch. klin. exp. Ophthal. 208: 235–240 (1978).

    Article  CAS  Google Scholar 

  • Shand, D. G. Pharmacokinetics of propranolol: a review. Postgrad. Med. J. 52, Suppl. 4: 22–25 (1976).

    Google Scholar 

  • Tieri, O., Polzella, A. Emploi clinique et mécanisme d'action du propranolol. Ophthalmologica 70: 36–42 (1975).

    Article  Google Scholar 

  • Timmermans, P. B. M. W. M., Brands, A. & van Zwieten, P. A. Lipophilicity and brain disposition of clonidine and structurally related imidazolidines. Naunyn Schmiedeberg's Arch. Pharmacol. 300: 217–226 (1977).

    Article  CAS  Google Scholar 

  • Vale, J., Gibbs, A. C. C. & Phillips, C. I. Topical propranolol and ocular tension in the human. Brit. J. Ophthal. 56: 770–775 (1972).

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Vareilles, P., Silverstone, D., Plazonnet, B., Le Douarec, J., Sears, M. L. & Stone, C. Comparison of the effects of timolol and other adrenergic agents on intraocular pressure in the rabbit. Invest. Ophthal. 16: 987–996 (1977).

    CAS  Google Scholar 

  • Zimmerman, T. J. & Kaufman, H. E. Timolol. A β-adrenergic blocking agent for the treatment of glaucoma. Arch. Ophthal. 95: 601–604 (1977).

    Article  CAS  PubMed  Google Scholar 

  • Zimmerman, T. J. & Kaufman, H. E. Timolol. Dose response and duration of action. Arch. Ophthal. 95: 605–607 (1911).

    Article  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Glaucoma Centre (Dr. C.L. Dake) of the Eye Clinic (Prof. Dr. R. A. Crone) Wilhelmina Gasthuis University of Amsterdam, Amsterdam, The Netherlands

    F. E. Ros

  2. Division of Pharmacotherapy, Muidergracht 24, Amsterdam, The Netherlands

    H. C. Innemee & P. A. Van Zwieten

Authors
  1. F. E. Ros
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. H. C. Innemee
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. P. A. Van Zwieten
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Ros, F.E., Innemee, H.C. & Van Zwieten, P.A. Ocular penetration of β-adrenergic blocking agents. An experimental study with atenolol, metoprolol, timolol and propranolol. Doc Ophthalmol 48, 291–301 (1980). https://doi.org/10.1007/BF00141456

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00141456

Keywords

Search

Navigation