Droxicam showed high antiinflammatory activity in
carrageenin-induced
edema in rat. At doses of 0.25 and 0.5 mg/kg,
droxicam was as active as
piroxicam and more active than
phenylbutazone given at 2.5 and 5 mg/kg. Against
nystatin-induced
edema,
droxicam (ED50, p.o., 5, 6, 7, 8 h: 7.5, 12.9, 4.8, 8.4 mg/kg) was 4-11 times more active than
phenylbutazone and more than 12 times more active than
isoxicam. In cotton pellet-induced
granuloma in rats, title compound was as active as
suprofen. In U.V. light-induced
erythema in guinea pigs,
droxicam (ED50, p.o., 1, 2, 3, 4 h: 0.51, 0.94, 1.56, 4.88 mg/kg) was 5-9 times more active than
phenylbutazone. At doses of 0.1, 0.33 and 1.0 mg/kg/day,
droxicam, similar to
piroxicam, showed good antiarthritic activity in rats injected with Mycobacterium butyricum against primary and secondary lesions.
Droxicam demonstrated strong
analgesic activity in protecting against writhings: induced by
phenylbenzoquinone in mice: ED50:
droxicam = 5.3,
phenylbutazone = 61.5,
acetylsalicylic acid = 90.7,
dipyrone = 83.6,
isoxicam = 88.3 mg/kg, p.o.; induced by
acetylcholine bromide in mice: ED50:
droxicam = 1.1,
phenylbutazone = 32.1,
acetylsalicylic acid = 32.2,
isoxicam = 32.7 mg/kg, p.o.; induced by
acetic acid in rat: ED50:
droxicam = 0.94,
acetylsalicylic acid = 8.72,
isoxicam = 4.70 mg/kg, p.o.
Antipyretic activity of title compound was demonstrated in rats with pyresis induced by brewer's yeast, being 4-13 times more active than
dipyrone. In pyresis induced by Salmonella typhi,
droxicam was more active than
acetylsalicylic acid and
4-aminoantipyrine at all times and doses. In a study of protection against
diarrhea induced by
castor oil in rats,
droxicam and
piroxicam showed equal activity (ED50 = 0.081 and 0.079 mg/kg, p.o., respectively) and were 3.9 and 15.6 times more active than
isoxicam and
phenylbutazone, respectively.
Droxicam significantly inhibited peritoneal capillary permeability in mice at a dose of 5 mg/kg, p.o., while
isoxicam and
phenylbutazone required 100 and 200 mg/kg, p.o., respectively.
Droxicam did not exhibit uricosuric activity in rats. It did not show cardiovascular or respiratory effects in anesthetized cats, nor modify their response to administration of
acetylcholine,
norepinephrine and
histamine. In the Irwin's test,
droxicam did not alter rat behavior (80 mg/kg, i.p.) nor that of mice (160 mg/kg, p.o.). Induction of gastrointestinal
injuries in rats by
droxicam was 10 times less than by
piroxicam (UD50:
droxicam, 57 mg/kg, p.o.;
piroxicam, 5.6 mg/kg, p.o.). The potentiation of gastric
injuries induced by stress through cold in rats was also studied.(ABSTRACT TRUNCATED AT 400 WORDS)