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Bioinorg Chem Appl. 2003;113-22. doi: 10.1155/S1565363303000098.

Effect of metal ions on melanin--local anaesthetic drug complexes.

Bioinorganic chemistry and applications

Ewa Buszman, Bozena Betlej, Dorota Wrześniok, Bozena Radwańska-Wala

Affiliations

  1. Medical University of Silesia, School of Pharmacy, Department of Pharmaceutical Chemistry, Jagiello?ska str. 4, Sosnowiec 41-200, Poland.

PMID: 18365047 PMCID: PMC2267052 DOI: 10.1155/S1565363303000098

Abstract

The affinity of melanin biopolymers for metal ions, drugs and other organic compounds is an important factor in the etiology of toxic retinopathy, hiperpigmentation, otic lesions and irreversible extrapyramidal disorders. The aim of the presented work was to examine the interaction of local anaesthetic drugs used in ophthalmology with model DOPA-melanin in the presence of metal ions. It has been demonstrated that the analyzed drugs form complexes with melanin biopolymer. Based on the .values of association constants,, the following order of drugs affinity to melanin was found: tetracaine > procaine >> bupivacaine > lidocaine. It has also been shown that Cu(2+) and Zn(2+) ions administered to DOPA-melanin before complexing with drugs decrease the total amount of local anaesthetics bound to melanin. The blocking of some active centers in melanin molecules by metal ions, which potentially exist in living systems, may change the clinical therapeutic efficiency of the analyzed local anaesthetic drugs.

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