Rimexolone

被引:2
作者
Balfour, JA
Benfield, P
机构
[1] Adis International Limited,
关键词
D O I
10.2165/00063030-199707020-00007
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
Rimexolone is a locally active nonfluorinated glucocorticoid which has minimal systemic effects and is virtually devoid of any atrophogenic effects on the skin. It has high corticosteroid receptor affinity and remains localised at the injection site for a prolonged period after intra-articular injection. Thus, serum rimexolone concentrations remain low. Rimexolone had the longest mean intra-articular residence time of several intra-articular steroid preparations (25 days, vs 6 days for triamcinolone hexacetonide and 1 to 4 days for the other drugs, which included methylprednisolone acetate), Single intra-articular injections of rimexolone provided long-lasting improvement of clinical efficacy parameters in patients with rheumatoid arthritis or osteoarthritis. in patients with rheumatoid arthritis, rimexolone was superior to placebo for treating knee joints and superior to placebo and similar to methylprednisolone acetate for treating small joints of the hand. Inpatients with osteoarthritis of the knee joint, rimexolone was superior to placebo, tended to be slightly more effective than methylprednisolone acetate and was similar to triamcinolone acetonide or a depot preparation of betamethasone dipropionate.
引用
收藏
页码:158 / 163
页数:6
相关论文
共 13 条
[1]   SERUM METHYLPREDNISOLONE LEVELS FOLLOWING INTRA-ARTICULAR INJECTION OF METHYLPREDNISOLONE ACETATE [J].
ARMSTRONG, RD ;
ENGLISH, J ;
GIBSON, T ;
CHAKRABORTY, J ;
MARKS, V .
ANNALS OF THE RHEUMATIC DISEASES, 1981, 40 (06) :571-574
[2]  
DASKALOPOULOU EV, 1987, BR J RHEUMATOL, V26, P450
[3]   COMPARATIVE PHARMACOKINETIC EVALUATION OF GLUCOCORTICOIDS AFTER INTRAARTERIAL ADMINISTRATION [J].
DERENDORF, H ;
MOLLMANN, HW ;
BARTH, J .
AKTUELLE RHEUMATOLOGIE, 1990, 15 (04) :145-153
[4]   PHARMACOKINETICS OF RIMEXOLONE AFTER INTRAARTICULAR ADMINISTRATION [J].
DERENDORF, H ;
MOLLMANN, H ;
VOORTMAN, G ;
VANDENOUWELAND, FA ;
VANDEPUTTE, LBA ;
GEVERS, G ;
DEQUEKER, J ;
VANVLIETDASKALOPOULOU, E .
JOURNAL OF CLINICAL PHARMACOLOGY, 1990, 30 (05) :476-479
[5]  
FOX PK, 1980, ARZNEIMITTEL-FORSCH, V30-1, P55
[6]   A HIGH-DOSE (UP TO 200 MG) TOLERANCE AND EFFICACY STUDY OF INTRAARTICULAR RIMEXOLONE (ORG-6216) IN RHEUMATOID SYNOVITIS OF THE KNEE [J].
GEVERS, G ;
DEQUEKER, J ;
VANHOLSBEECK, M ;
VANVLIETDASKALOPOULOU, E .
CLINICAL RHEUMATOLOGY, 1994, 13 (01) :103-109
[7]   BINDING AFFINITIES OF RIMEXOLONE (ORG-6216), FLUNISOLIDE AND THEIR PUTATIVE METABOLITES FOR THE GLUCOCORTICOID RECEPTOR OF HUMAN SYNOVIAL TISSUE [J].
HOCHHAUS, G ;
MOELLMANN, HW .
AGENTS AND ACTIONS, 1990, 30 (3-4) :377-380
[8]   PROTECTIVE EFFECT OF RIMEXOLONE ON CARTILAGE DAMAGE IN ARTHRITIC MICE - A COMPARATIVE-STUDY WITH TRIAMCINOLONE HEXACETONIDE [J].
JOOSTEN, LAB ;
HELSEN, MMA ;
VANDENBERG, WB .
AGENTS AND ACTIONS, 1990, 31 (1-2) :135-142
[9]  
KOEHLER BE, 1974, J RHEUMATOL, V1, P117
[10]   REDUCTION OF CORTISOL-LEVELS AFTER SINGLE INTRAARTICULAR AND INTRAMUSCULAR STEROID INJECTION [J].
LAZAREVIC, MB ;
SKOSEY, JL ;
DJORDJEVICDENIC, G ;
SWEDLER, WI ;
ZGRADIC, I ;
MYONES, BL .
AMERICAN JOURNAL OF MEDICINE, 1995, 99 (04) :370-373