Sharma R P, Smillie J, Palmer D G
Pharmacology. 1985;30(2):115-20. doi: 10.1159/000138059.
The concentrations of gold in whole blood, serum, urine and blood cells of patients with rheumatoid arthritis were measured during 6 months of oral treatment either with Auranofin or placebo. Any adverse effects attributable to the treatments were also recorded. Although the time course of gold during Auranofin therapy was similar to that of injected gold, the blood and serum gold concentrations were significantly lower than those measured in patients receiving injected gold. Between 45 and 58% of Auranofin gold in the blood was associated with blood cells. In comparison, following injections of gold thiomalate, only about 4% of the gold was present in the blood cells. During the 6-month period, 2 patients receiving Auranofin withdrew because of diarrhoea and another because of rash. 1 placebo patient withdrew because of headaches. No laboratory evidence of haematological, renal or hepatic abnormality was encountered. It is suggested that the markedly lower concentrations of gold in the body sustained during treatment with Auranofin may be the critical factor towards a greater tolerance of the drug in the treatment of rheumatoid arthritis.
在口服金诺芬或安慰剂进行6个月治疗期间,对类风湿性关节炎患者全血、血清、尿液和血细胞中的金浓度进行了测量。还记录了治疗引起的任何不良反应。虽然金诺芬治疗期间金的时间进程与注射金相似,但血液和血清中的金浓度明显低于接受注射金的患者所测得的浓度。血液中45%至58%的金诺芬金与血细胞相关。相比之下,注射硫代苹果酸金后,只有约4%的金存在于血细胞中。在6个月期间,2名接受金诺芬治疗的患者因腹泻退出,另一名因皮疹退出。1名安慰剂患者因头痛退出。未发现血液学、肾脏或肝脏异常的实验室证据。有人认为,金诺芬治疗期间体内维持的金浓度明显较低可能是该药物在类风湿性关节炎治疗中具有更高耐受性的关键因素。