Sandoz Fluorometholone Product Monograph

DETAILED PHARMACOLOGY

When tested in monkeys, fluorometholone was found to be two to three times more potent than hydrocortisone acetate in tests of catabolic effects(l). In the inhibition of rat granuloma, the anti-inflammatory effect of fluorometholone was found to be as much as 100-135 times greater than that of hydrocortisone(2). In healthy adult rabbits, fluorometholone was found to penetrate into the cornea and aqueous humor (3).

TOXICOLOGY

When studied in rats, topically applied fluorometholone in doses five times greater than proposed in humans, was not absorbed in sufficient quantities to affect the concentration of corticosteroids in the bloodstream (4) . Twenty-one day studies of topical ocular application in healthy rabbits of up to ten times the proposed dosage in humans demonstrated the tolerance for the drug. No differences were noted between the ocular structures of the controls and the experimental group (5).

REFERENCES

1. 1.

   Duncan, G.W. and Stucki, J.C.: Catabolic Activity of Steroidal Anti-Inflammatory

   Compound. Metabolism 11:940-945, 1962.

2. 2. Glenn, E.M., Miller, W.L., and Schagel, C.A.: Metabolic Effects of Adrenocortical Steroids in Vivo and in Vitro; Relationship to Anti-inflammatory Effects. Rec. Progr. Horm. Res., 107, G. Pincus ed., Academic Press, New York, 1963.
3. 3.

   Kupferman, A. and Leibowitz, H.: Penetration of Fluorometholone into the Cornea and

   Aqueous Humor, Arch. of Ophthal., 2i:425-427, June 1975.

4. 4.

   Alcon Laboratories Inc.: Relazione Tossicologica, e Farmacologica del prodotto Flumetol -

   S. 1975.

5. 5. Ibid.