Penetration into human urogenital tissues, muscle tissues, rib and cerebrospinal fluid of thiamphenicol.

The penetration of D(+)-threo-2-dichloroacetamido-1-(p-methylsulfonylphenyl)-1,3-propanediol (thiamphenicol, TAP, Urfamycine) into human renal, ureter, prostatic, testicular and muscle tissue, perirenal fat, rib as well as cerebrospinal fluid (CSF) after a single i.v. injection of 1.0 g of thiamphenicol glycinate ester was investigated. 2 h after TAP administration to 17 patients with severely diseased kidneys, the antibiotic concentration in renal tissue ranged from 9.8 to 138.7 microgram/g (mean value 40.4 +/- 29.9 microgram/g), in ureter tissue from 6.3 to 62.0 microgram/g (mean value 20.8 +/- 17.0 microgram/g), in muscle tissue from 1.7 to 13.7 microgram/g (mean value 8.2 +/- 3.6 microgram/g), in rib from 0.8 to 3.4 microgram/g (mean value 2.4 +/- 1.5 microgram/g) and in perirenal fat from 0.6 to 5.7 microgram/g (mean value 2.1 +/- 1.5 microgram/g). At the same time the TAP serum level varied from 4.6 to 15.2 microgram/ml (mean value 9.4 +/- 3.1 microgram/ml). Prostatic tissue concentration, measured in 16 patients with prostate adenomas, varied at 2 h after dosing, from 2.1 to 15.1 microgram/g (mean value 5.7 +/- 3.8 microgram/g). The simultaneous serum level was between 4.6 and 14.5 microgram/ml (mean value 8.9 +/- 3.4 microgram/ml). In 6 of these patients additionally CSF level was measured at 1.5 h post inj. and ranged from 0.11 to 0.65 microgram/ml (mean value 0.32 +/- 0.19 microgram/ml). Testicular tissue concentration assessed in 7 patients with prostate carcinomas varied at 2 h after i.v. injection from 3.4 to 8.4 microgram/g (mean value 6.1 +/- 1.9 microgram/g). The respective serum level in these patients was between 5.2 and 10.4 microgram/ml (mean value 8.5 +/- 1.7 microgram/ml). Several factors affecting the diffusion of TAP into the reported tissues and CSF are discussed. TAP should be regarded as an antibiotic with good penetration into urogenital tissues.