Yü T F, Perel J, Berger L, Roboz J, Israili Z H, Dayton P G
Am J Med. 1977 Nov;63(5):723-8. doi: 10.1016/0002-9343(77)90158-9.
Complex interactions occur between pyrazinamide (PZA) and probenecid in man involving both the metabolism and distribution of the drugs, and their effects on renal tubules. Pretreatment with PZA prolonged the half-life (T 1/2) of probenecid without changing its plasma-binding. As the rate of probenecid metabolism is decreased, its uricosuric action tends to be prolonged and the effect of PZA lessened. The PZA-suppressible urate level is increased to values well above control after the administration of probenecid; it is less after alkalinization of urine, although still larger than the value for PZA-suppressible urate after the administration of PZA alone. Urinary probenecid excretion is much greater when urine is alkalinized. These observed drug interactions, plus the known effect of probenecid to block secretion of PZA, have to be considered in evaluating the effect of the two drugs given together, compared to the effect of each drug given separately.
吡嗪酰胺（PZA）与丙磺舒在人体内会发生复杂的相互作用，涉及药物的代谢、分布及其对肾小管的影响。PZA预处理可延长丙磺舒的半衰期（T1/2），而不改变其血浆结合率。由于丙磺舒的代谢速率降低，其促尿酸排泄作用往往会延长，而PZA的作用则会减弱。服用丙磺舒后，PZA可抑制的尿酸水平会升高至远高于对照值；尿液碱化后该值会降低，尽管仍高于单独服用PZA后PZA可抑制的尿酸值。尿液碱化时，丙磺舒的尿排泄量会大大增加。在评估两种药物联合使用的效果时，与单独使用每种药物的效果相比，必须考虑这些观察到的药物相互作用，以及丙磺舒阻断PZA分泌的已知作用。
