Abstract Title:

Metabolism of ophthalmic timolol: new aspects of an old drug.

Abstract Source:

Basic Clin Pharmacol Toxicol. 2011 Mar 8. Epub 2011 Mar 8. PMID: 21385322

Abstract Author(s):

Marjo Volotinen, Jukka Hakkola, Olavi Pelkonen, Heikki Vapaatalo, Jukka Mäenpää

Article Affiliation:

Institute of Biomedicine, Pharmacology, University of Helsinki, Helsinki, Finland Santen Oy, Tampere, Finland Institute of Biomedicine, Department of Pharmacology and Toxicology, University of Oulu, Oulu, Finland.


  Glaucoma is a common eye disease which can cause irreversible blindness if not diagnosed and treated in the early stages of progression. This disease is often, albeit not always, associated with increased intraocular pressure, which is also the most important risk factor for glaucoma. Currently,the only treatment option of glaucoma is reduction of intraocular pressure. A β-adrenergic antagonist, timolol, has been used for the treatment of glaucoma and increased intraocular pressure for more than thirty years and still remains the drug of choice. Locally, timolol is well tolerated. However, it has been reported that approximately 80% of a topically administered eye drop is systemically absorbed. Thus, ophthalmic timolol may cause severe adverse cardiovascular and respiratory effects. On the basis of the above situation, it is somewhat surprising to notice that the metabolism of timolol has only recently been studied in detail even though the drug has been used for decades. Earlier clinical studies have suggested that timolol is metabolized by CYP2D6, an important member of the cytochrome P450 family. Our recent in vitro studies demonstrated convincingly that CYP2D6 is the mainenzyme contributing to timolol metabolism, although also CYP2C19 may have a minor role. Liver is the principal site of timolol metabolism, because - according to our recent findings - only negligible amounts of CYP2D6 are expressed in human ocular tissues. After topical administration, systemic timolol concentrations may be high enough to cause cardiovascular and respiratory adverse effects especially in patients who are CYP2D6 poor metabolizers or use concomitant CYP2D6 inhibitors.

Study Type : Review

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