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Vol. 26, Issue 8, 745-754, August 1998
Glaucoma Research Laboratories, Pharmacia & Upjohn
Latanoprost (13,14-dihydro-17-phenyl-18,19,20-trinor-prostaglandin
F2
-1-isopropyl ester) is a unique
prostaglandin analogue developed for the treatment of glaucoma. To
investigate the pharmacokinetics, tritium-labeled latanoprost was
administered topically on the eyes of rabbits and intravenously. About
7.7% of the applied dose was found in the cornea at 15 min after the
drug administration. The following Cmax
and elimination half-life (interval 1-6 hr) values of the total
radioactivity in the eye tissues were found: aqueous humor, 0.09 ng
eq/ml and 3.0 hr; anterior sclera, 1.49 ng eq/mg and 1.8 hr; cornea,
1.59 ng eq/mg and 1.8 hr; ciliary body, 0.39 ng eq/mg and 2.8 hr;
conjunctiva, 1.41 ng eq/mg and 1.4 hr; and iris, 0.39 ng eq/mg and 2.1 hr. Latanoprost was rapidly hydrolyzed, and most of the radioactivity
found in the aqueous humor, anterior eye tissues, and plasma
corresponded to the pharmacologically active acid of latanoprost. The
initial plasma elimination half-life of the acid of latanoprost was
9.2 ± 3.2 min after iv and 2.3 ± 1.9 min after topical
administration on the eyes. The plasma clearance of the acid of
latanoprost was 1.8 ± 0.3 liters/hr·kg, and the volume of
distribution was 0.4 ± 0.1 liter/kg after iv administration.
Based on the retention times on HPLC and GC-MS, the main metabolite in
urine and feces was identified as the 1,2,3,4-tetranor metabolite of
acid of latanoprost. This acid existed in equilibration with the
corresponding 
-lactone. The AUC of radioactivity in the eye tissues
was approximately 1000 times higher than in plasma AUC. The recovery of
radioactivity was complete.
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