ANTIINFLAMMATORY, ANALGESIC, ANTIPYRETIC AND RELATED PROPERTIES OF MELOXICAM, A NEW NONSTEROIDAL ANTIINFLAMMATORY AGENT WITH FAVORABLE GASTROINTESTINAL TOLERANCE

被引:279
作者
ENGELHARDT, G
HOMMA, D
SCHLEGEL, K
UTZMANN, R
SCHNITZLER, C
机构
[1] Department of Pharmacologic Research, Dr. Karl Thomae GmbH, Biberach/Riss
关键词
MELOXICAM; NONSTEROID ANTIINFLAMMATORY DRUGS; ANTIINFLAMMATORY ACTIVITY; ANALGESIC ACTIVITY; GASTROINTESTINAL TOLERANCE;
D O I
10.1007/BF01757699
中图分类号
Q2 [细胞生物学];
学科分类号
071009 ; 090102 ;
摘要
The anti-inflammatory, analgesic and antipyretic properties of the new non-steroidal anti-inflammatory agent, meloxicam, were investigated in a variety of animal models and compared with the properties of piroxicam, diclofenac, indomethacin and several other NSAIDs. With respect to the total effect of a single oral dose, the anti-exudative effect of meloxicam on carrageenan-induced oedema in the rat exceeded that of all the NSAIDs included in the comparison. Additionally, meloxicam showed the greatest potency of all the compounds examined with respect to adjuvant-induced arthritis in the rat, the granuloma pouch model and the cotton pellet test in the rat. Unlike indomethacin, in the carrageenan pleurisy model in the rat, meloxicam caused both a dose-dependent reduction in exudate volume and also inhibition of leucocyte migration. Meloxicam showed a strong and lasting effect on inflammatory pain in the rat. Like other NSAIDs, but unlike dipyrone, meloxicam had no effect in the hot plate and tail clamp tests, which are used to identify weak central analgesic effects. Unlike dipyrone and like indomethacin, meloxicam had no effect in a model of visceral distention pain. In common with other NSAIDs, meloxicam had no influence on the body temperature of normothermic rats in the anti-inflammatory dose range, but did reduce yeast-induced fever in the rat in a dose-dependent manner. Like piroxicam, meloxicam had a uricosuric effect on rats treated with oxonic acid. Low-dose meloxicam inhibited both bradykinin-induced and PAF-induced bronchospasm in the guinea-pig, but had no effect on acetylcholine-induced bronchospasm. Piroxicam had greater ulcerogenic effects in the rat stomach than meloxicam. The therapeutic range of meloxicam in the rat, with regard to inhibition of adjuvant arthritis, was several times greater than that of piroxicam, indomethacin, diclofenac and naproxen.
引用
收藏
页码:423 / 433
页数:11
相关论文
共 54 条
[1]  
[Anonymous], 1971, PROBIT ANAL
[2]   EFFECTS OF AGE ON THE PHARMACOKINETICS OF PIROXICAM IN RATS [J].
BOUDINOT, SG ;
FUNDERBURG, ED ;
BOUDINOT, FD .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1993, 82 (03) :254-257
[3]  
BUSCH U, 1990, DRUG EXP CLIN RES, V16, P49
[4]  
BUSCH U, 1994, SCAND J RHEUMATOL S, V98, pA119
[5]   A SATISFACTORY APPARATUS FOR STUDY OF ANALGESIA IN MICE [J].
CHEN, JYP ;
BECKMAN, H .
SCIENCE, 1951, 113 (2944) :631-631
[6]   ANALGESIC ANTIPYRETIC DRUGS AS ANTAGONISTS OF BRADYKININ [J].
COLLIER, HOJ ;
SHORLEY, PG .
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1960, 15 (04) :601-610
[7]  
COLLIER HOJ, 1959, J PHYSIOL-LONDON, V149, pP54
[8]   CORRELATION BETWEEN GASTRIC IRRITANCY AND ANTI-INFLAMMATORY ACTIVITY OF NON-STEROIDAL ANTI-INFLAMMATORY DRUGS [J].
DEARDEN, JC ;
NICHOLSON, RM .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1984, 36 (10) :713-715
[9]  
DIROSA M, 1979, HDB EXPT PHARM, V50, P223
[10]  
DJAHANGUIRI B, 1969, SCAND J GASTROENTERO, V4, P265