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Biomedical subjects

P Conquet

Publications and source records attributed to P Conquet.

8 recordsLinked to original sources
PubMed1985

On the pharmacology of L-645,151: a topically effective ocular hypotensive carbonic anhydrase inhibitor.

L-645,151 [(2-sulfamoyl-6-benzothiazolyl)-2,2-dimethylpropionate] is the O-pivaloyl ester of L-643,799 (6-hydroxybenzothiazole-2-sulfonamide), topically administered L-645,151 being a substrate for ocular esterases with the resultant liberation of the active moiety, L-643,799, during penetration of the ocular surface. The minimum concentrations of topically administered suspensions (1 drop of 50 microliters into both eyes) of L-645,151, L-643,799, dichlorphenamide and methazolamide significantly lowering the elevated intraocular pressure (IOP) of the alpha-chymotrypsinized rabbit eye were 0.25, 2, 10 and 5%, respectively. IOP was not significantly decreased by 10% suspensions of acetazolamide or ethoxzolamide. The IOP lowering action of L-645,151 was local as the unilateral instillation of L-645,151 (0.25%) into the contralateral eye was devoid of effect in alpha-chymotrypsinized rabbits. L-645,151 (2%) decreased aqueous humor inflow in both the conscious rabbit and the anesthetized dog. Outflow facility in the conscious rabbit was unaltered by a 10% suspension of L-645,151. Low peak levels (0.52 microgram/g) of L-643,799 were present in rabbit renal cortex after the instillation of L-645,151 (2%) into both eyes; this treatment did not induce diuresis in the conscious rabbit. The corresponding maximum concentration in the iris + ciliary body was 4.01 micrograms/g. These preclinical studies reveal that L-645,151 is the most potent, topically effective ocular hypotensive carbonic anhydrase inhibitor described to date.

Administration, Topical↗
PubMed1975

Arachidonic acid-induced elevation of intraocular pressure and anti-inflammatory agents.

Arachidonic acid, a precursor of prostaglandin E2 subconjunctivally injected into rabbit eyes in concentrations of 0.8 to 5 per cent, produced a dose-related rise of intraocular pressure (IOP) similar to the one observed after topical administration of PGE2 in concentrations of 0.001 to 0.1 per cent. Indomethacin, a nonsteroidal anti-inflammatory agent, had an inhibitory effect when administered systemically or topically prior to arachidonic acid. Dose-response relationships were demonstrated by topical and oral administration of Indomethacin which, as expected, had no effect on PGE2. Dexamethasone did not exert any inhibitory effect on the increased IOP following arachidonic acid administration. Indomethacin applied topically readily penetrated into the aqueous humor in concentrations considerably above those appearing in the plasma, which justifies the use of this route of administration. Since prostaglandin (PG) appeared to be implicated in ocular inflammation, these findings underline the specificity of action of Indomethacin and suggest its use in the topical treatment of ocular inflammation.

Administration, Oral↗