Pharmacokinetics of tetroxoprim/sulphadiazine in patients with impaired renal function

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Abstract
After the combined oral administration of tetroxoprim and sulphadiazine in 16 patients with normal or impaired renal function, a linear relationship was found between the elimination rate constant ( ke ) and the endogenous creatinine clearance (C1 cr ). The mean elimination half-life ( t1/2 ) for tetroxoprim in patients with healthy kidneys was 6·7 h and in anuric patients 13·8 h. In the case of sulphadiazine the values were h = 10 4 h (healthy kidneys) and Zi = 25·7 h (anuria). Both drugs were influenced in the same way and in parallel with the functional condition of the kidneys. For long term administration in anuric patients a dosage interval of τ=24h is required. The relative distribution volumes Vf for both substances are independent of the degree of renal insufficiency. The mean Ff values are calculated as 0–77 0·11 1/kg for tetroxoprim, and 0 36 0·07 1/kg for sulphadiazine.

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