DESCRIPTION & PHARMACOLOGY

Phenylbutazone chemically is 4-btuyl-1, 2-diphenyl-3, 5-pyrazolidinedione. It has the following structural formula:

Phenylbutazone was first synthesized in 1948 and introduced into human medicine in 1949, Kuzell1,2,3, Payne4, Fleming5, and Denko6, demonstrated the clinical effectiveness of phenylbutazone in gout, gouty arthritis, acute arthritis, acute rheumatism and various other rheumatoid disorders in humans. Fabre7, Domenjoz8, Wilhelmi9, and Yourish10, have established the anti-rheumatic and anti-inflammatory activity of phenylbutazone. It is entirely unrelated to the steroid hormones.

Toxicity of phenylbutazone has been investigated in rats and mice11, Ogilvie and Sutter12, have also made a study on the chronic toxicity of phenylbutazone in dogs. They have shown that dogs receiving 10 mg. and 100 mg. per Kg. body weight, per day for 90 days, maintain good appetites, excrete normal feces, gain weight and maintain a normal blood picture. They also report no abnormal macroscopic or microscopic changes in sacrificed animals which could have been attributed to the drug.

Phenylbutazone has been used by Camberos13 in thoroughbred horses. Favorable results were reported in cases of traumatism, muscle rupture, strains and inflammations of the third phalanx. Results were not as favorable in the periodic treatment of osteo-arthritis of medial and distal bones of the hock, arthritis of the stifle and hip, arthrosis of the trapezious muscles, and generalized arthritis. Sutter14 reported a favorable response in chronic equine arthritis of long duration, fair results in a severely bruised mare, and poor results in two cases where the condition was limited to the third phalanx.

REFERENCES

1. Kuzell, W.C., Schafferzick, R.W., Naughler, W.E., Gandia, G. and Mankle, E.A.: A.M.A. Arch. Inst. Med., 92;646 (1953).

2. Kuzell, W.C., Schafferzick, R.W., Brown, B. and Mankle, E.A.: J.A.M.A. 149;729 (1952).

3. Kuzell, W.C., and Schafferzick, R.W.: Calif. Med. 77;319 (1952).

4. Payne, R.W., Shelter, M.R., Farr, C.H., Hellbaum, A.A. and Ishmall, W.K.: J. Lab. Clin. Med., 45;331 (1955).

5. Fleming, J., and Will, G.: Ann. Rheumat. Dist., 12;95 (1953).

6. Denko, C.W., and Rumi, D.: American Pract. 6;1865 (1956).

7. Fabre, J., et al: Semain. Hop. (Paris) 31;87 (1955).

8. Domenjoz, R., et al: Arzneimittel-Forsch, 5;488 (1955).

9. Wilhelmi, G. and Pulver, R.: Arzneimittel-Forsch, 5;221 (1955).

10. Yourish, W., Paton, B., Brodie, B., Burns, J.:A.M.A. Arch. Ophth., 53;264 (1955).

11. Hazelton, L.W., Tusing, T.W. and Hollana, E.G.: J. Pharmacol. Exper. Ther., 109;387 (1953).

12. Ogilvie, F.B. and Sutter, M.D.: Vet. Med. 52;492-4 (1957).

13. Camberos, H.R.: Rev. Med. Vet. (Buenos Aires) 38;9 (1956).

14. Sutter, M.D.: Vet. Med., 53;83 (Feb. 1958).