Trimethoprim and Sulfadiazine Penetration into Bile and Gallbladder in Acute Cholecystitis

Abstract

The concentrations of trimethoprim (TMP) and sulfadiazine (SDZ) in serum, bile and gallbladder wall of 9 patients with acute cholecystitis were measured after b.i.d. treatment with 160 mg of TMP + 500 mg of SDZ. The samples were collected 2–4 h after the last dose. Mean TMP concentrations were 1.71 ± (SE) 0.51 μg/ml, 4.53 ± 5.26 μg/ml and 2.31 ± μg/g in serum, bile and gallbladder, respectively. Mean SDZ concentrations were 22.2 ± 14.9 μg/ml in serum, 9.37 ± 8.99 μg/ml in bile and 16.1. ± 10.1 μg/g in gallbladder. The average ratios of bile-serum and gallbladder-serum concentrations were 2.64 and 1.35 for TMP and 0.42 and 0.73 for SDZ. There was a significant correlation between serum and gallbladder concentrations of both TMP and SDZ. No correlation existed between serum and bile levels.

Biological uptake and depuration of sulfadiazine and sulfamethoxazole in common carp (Cyprinus carpio)

“…Additionally, greater BCF values for SDZ were observed than SMZ for the following reasons: (1) SDZ was likely metabolized more slowly than SMZ (Bergan et al, 1986;Mattila et al, 1987). (2) Protein binding could result in fewer free sulfonamides available to get into fish tissues, and SMZ might be easier to be bound to plasma protein which existed extensively in fish blood (Bergan et al, 1986;Mandell et al, 1995).…”