Ocular distribution of methyprylon after intravenous injection and transfer of the drug to recipient eye via corneal graft.

The purpose of the study was to determine chronologically the ocular distribution of methyprylon (Noludar) after a single intravenous injection (45 mg/kg) to rabbits, if the drug can be transferred from a donor treated with the drug to the recipient's eye via an allogeneic corneal graft, and the effect of methyprylon on corneal cell growth and protein synthesis. Gas chromatographic techniques showed that the drug was present in all the tissues and fluids of the eye from 0.5 to 18 hours after the injection. Postoperatively, the cornea and some of the other ocular tissues of the recipient contained methyprylon at least 24 hours after transplantation. Clinically, the graft remained clear, and there was no adverse reaction in the recipient eye for an observation period of 24 hours. Tissue culture studies showed that about 10 times more methyprylon than was found in the donor cornea was necessary to produce a cytotoxic reaction on the corneal cells in terms of cellular growth rate and protein synthesis. Our animal experiments and cytotoxicity tests suggest that corneas of donors treated with a high dose of methyprylon would be suitable for use as grafts.