Pharmacokinetics of long half-life antibacterials

Follath, F.

In: Journal of Antimicrobial Chemotherapy, 1979, vol. 5, no. Supplement_B, p. 97-102

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    Summary
    Trimethoprim (TMP), sulfamethoxazole (SMZ) and sulfadiazine (SDZ) are characterized by elimination half-lives of 9 to 15 h. Effective serum concentrations can therefore be maintained by twice daily administration, but without a loading dose steady state levels will be reached only after 3 days. Renal disease has little effect on the pharmacokinetics of unchanged SMZ, whereas TMP and SDZ elimination is prolonged in uremia. Dosage adaptation to creatinine clearance is difficult, since the ratio of the two components in serum and urine will be altered. Abnormal drug accumulation in liver disease during a treatment with TMP and SMZ has not been demonstrated