Trimethoprim and sulfadiazine penetration into bile and gallbladder in acute cholecystitis.
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 micrograms/ml, 4.53 +/- 5.26 micrograms/ml and 2.31 +/- micrograms/g in serum, bile and gallbladder, respectively. Mean SDZ concentrations were 22.2 +/- 14.9 micrograms/ml in serum, 9.37 +/- 8.99 micrograms/ml in bile and 16.1 +/- 10.1 micrograms/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.
D000208:Acute Disease; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D001646:Bile / Q000378:metabolism*; D002764:Cholecystitis / Q000188:drug therapy*; D004338:Drug Combinations / Q000097:blood / Q000378:metabolism / Q000627:therapeutic use; D005260:Female; D005704:Gallbladder / Q000378:metabolism*; D006801:Humans; D008297:Male; D008875:Middle Aged; D013411:Sulfadiazine / Q000097:blood / Q000378:metabolism* / Q000627:therapeutic use; D014295:Trimethoprim / Q000097:blood / Q000378:metabolism* / Q000627:therapeutic use; D000096926:Benzenesulfonamides
D004338:Drug Combinations; D013411:Sulfadiazine; D014295:Trimethoprim; C024873:sulfadiazine, trimethoprim drug combination; D000096926:Benzenesulfonamides