Effects of multiple treatments of isoxicam on organ weights and serum SGPT, AP, and BUN in adjuvant-induced polyarthritic rats.

Isoxicam at 25 mg/kg/day x 28 days significantly inhibited the multiple alterations with the developing polyarthritis. In rats, this drug did not induce any changes in the relative liver weights or serum SGPT, AP, or BUN in polyarthritic rats. Isoxicam absorption was similar in normal and arthritic rats.

Anti-inflammatory activity of isoxicam in combination with aspirin or D-propoxyphene.

Unlike several arylacetic acid derivatives (indomethacin, fenoprofen, ibuprofen, flurbiprofen and naproxen), the anti-arthritic activity of isoxicam is not reduced in the adjuvant-induced polyarthritis assay by the concomitant administration of aspirin or D-propoxyphene.

The anti=inflammatory properties of isoxicam (4-hydroxy-2methyl-N-(5-methyl-3isoxolyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide).

Isoxicam is a potent, orally active, nonsteroidal anti-inflammarory drug with prolonged activtiy in experimentally induced inflammation in rats. Isoxicam is less ulcerogenic, acutely less toxic and, therefore, appears to have a therapeutic ratio superior to other standard agents to which it was compared.

The evaluation of cotton twine as a new anti-inflammatory assay.

A new anti-inflammatory assay is described, utilizing a subcutaneously implanted elongated section of cotton twine to induce granuloma in rats. The cotton twine irritant is easily introduced under the abdominal skin and after seven days a well formed granuloma is established. The procedure works effectively for both steroidal and non-steroidal anti-inflammatory drug evaluation. Consistency of the cotton twine eliminates individual weighing of each section and uniformity in compactness affords reproducible results.

Effect of single and multiple treatments with phenylbutazone in normal and adjuvant-induced polyarthritic rats.

Liver function alterations, in the adjuvant induced polyarthritis procedure in rats, has been demonstrated by many investigators. We observed a significant inhibition of the polyarthritis with phenylbutazone but we were unable to find any changes in the relative liver weights of SGPT, AP or BUN in polyarthritic or phenylbutazone treated rats. However, we did observe that polyarthritic rats maintained a significantly higher plasma phenylbutazone concentration than the corresponding non-arthritic controls. This appears to futher substantiate the influence of 'pathopharmacodynamics' on the disposition and activity of drugs.

Estrogenic profile on a water-soluble estrogen, estrazinol hydrobromide.

PIP: The estrogenic properties of estrazinol hydrobromide (EZ), a water-soluble estrogen, were compared with those of Premarin (PR), another water-soluble estrogen preparation consisting of conjugated equine estrogens. Estradiol-17beta, estra-1,3,5(10)-triene-3,17beta-diol (E), and ethinyl estradiol, 17alpha-ethinyl-1,3,5 (10)-estratriene-3,17beta-diol (EE) were used as reference standards. Subcutaneous progesterone (400 mcg) given to rabbits primed with comparable subcutaneous doses of either E or EE produced full secretory changes of the endometrium, while such a transformation could not be elicited in orally primed animals regardless of the estrogen used. The biological profile or orally administered EZ was very similar to that of oral EE and different from oral PR. Howerver, the oral EZ-induced morphological changes of the rabbit endometrium appeared somewhat different from those produced by oral EE. The findings indicated that following oral administration, EZ-induced endometrial transformation is more "normal" and/or adequate than the changes produced by either EE or PR.^ieng

Biological profile of quingestanol acetate.

PIP: An orally active progestagen, 17 alpha-ethynyl-19-nor-testosterone-17 beta-acetate-3-cyclopeotyl enol-ether (ENTACP) was found to be a potent antiestrual and contraceptive agent in rats. It was evaluated with respect to: 1) progestational activity, 2) pregnancy maintenance, 3) androgenic activity, 4) masculinization of female fetuses, 5) uterotropic activity, 6) effect on adrenal and adrenocortical function, 7) effect on organs and body weight, 8) effect on pregnancy, 9) storage in body fat. ENTACP was twice as effective in producing secretory changes of the endometrium as its parent compound. Pregnancy was not maintained; however, after 22 days, resorption sites were still visable. ENTACP was about 1.5 times as effective as its parent compound in stimulating accessory organs during daily administration. A daily dose of .9 mg orally produced masculinization of the female fetuses, but did not interfere with parturition. Resorption of fetuses occurred more frequently in rats treated with ENTACP than with other compounds tested. ENTACP behaved like an estrogen in stimulating uterine growth. Adrenal weight was significantly increased with ENTACP administration and it reduced the capacity of the adrenal cortical tissue to respond to ACTH. Body weight gain suffered in direct proportion to dose administration. Adrenals, hypophysis, and thyroid increased when expressed in mg/100 gm body weight, and thymus decreased. The oral daily dose of .5 mg/animal from day 1-11 after mating did not prevent pregnancy. At the 5 mg/animal dose nidation was interfered with. Oral administration was not followed by storage of steroid material in body fat.^ieng