Anticholinesterase agents have been used for the control of intraocular pressure for many years. The first was physostigmine (eserine), an alkaloid obtained from the Calabar bean. In 1863 Fraser noted that physostigmine caused pupillary constriction, and Laqueur in 1875 employed it for the treatment of glaucoma.8 At that time it was noted that undesirable side-effects occurred with the drug. Ever since, an intermittent search for a more potent, less irritating anticholinesterase agent has been under way. A variety of cholinesterase agents have been tried. These include those which form a reversible union with cholinesterase as does physostigmine, namely, neostigmine and o-neostigmine and p-neostigmine. Other anticholinesterase agents inhibit cholinesterase irreversibly and include tetraethylpyrophosphate (TEPP), tetraisopropylpyrophosphate (TIPP) hexaethylpyrophosphate (HEPP), p-nitrophenyldiethylphosphate, (Mintacol), parathion (o,o-diethyl-o-p-nitrophenyl thiophosphate), isoflurophate (DFP, Floropryl), and tabun (dimethylamidoethoxy-phosphoryl cyanide).1 Of these, physostigmine, neostigmine (Prostigmin), and isoflurophate have stood the test of time
LEOPOLD IH, GOLD P, GOLD D. Use of a Thiophosphinyl Quaternary Compound (217-MI) in Treatment of Glaucoma. AMA Arch Ophthalmol. 1957;58(3):363–366. doi:10.1001/archopht.1957.00940010375007
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