Strong H A, Angus R, Oates J, Sembi J, Howarth P, Renwick A G, George C F
Clin Pharmacokinet. 1986 Sep-Oct;11(5):402-10. doi: 10.2165/00003088-198611050-00005.
The renewed interest in sulphinpyrazone in recent years has arisen from its potential to inhibit platelet aggregation. In vivo much of the activity is probably due to the thioether or sulphide metabolite which has a greater potency and a longer half-life than the parent compound. The sulphide metabolite is formed exclusively by the gut microflora in man. The pharmacokinetics of sulphinpyrazone (200 mg orally) have been studied, with particular attention to the formation of the sulphide metabolite, in groups of patients who might be expected to show abnormal formation of this active metabolite due to altered delivery of the drug to the lower gut or altered gut flora. Five patients studied 1 month after a myocardial infarction did not differ markedly from young, normal volunteers with respect to either sulphinpyrazone or its metabolite. Crohn's disease in the quiescent phase did not significantly alter the pharmacokinetics or metabolism of the drug, but 1 patient who had undergone a hemicolectomy formed negligible concentrations of the active metabolite. Antimicrobial therapy produced highly variable results with almost complete suppression of sulphide formation in some subjects but no apparent effect in others.
近年来，人们对磺吡酮的兴趣再度兴起，源于其抑制血小板聚集的潜力。在体内，大部分活性可能归因于硫醚或硫化物代谢物，其效力比母体化合物更强，半衰期更长。硫化物代谢物仅由人体肠道微生物群形成。对口服200毫克磺吡酮的药代动力学进行了研究，特别关注硫化物代谢物的形成，研究对象为可能因药物向肠道下部输送改变或肠道菌群改变而导致该活性代谢物形成异常的患者群体。5名心肌梗死后1个月接受研究的患者，在磺吡酮及其代谢物方面与年轻的正常志愿者相比没有明显差异。静止期克罗恩病并未显著改变该药物的药代动力学或代谢，但1名接受过半结肠切除术的患者形成的活性代谢物浓度可忽略不计。抗菌治疗产生的结果差异很大，在一些受试者中几乎完全抑制了硫化物的形成，而在另一些受试者中则没有明显效果。
