Pharmacokinetics of furagin, a new nitrofurantoin congener, on human volunteers.

Abstract

The human pharmacokinetics of a nitrofurantoin congener furagin was studied after a single oral dose of 200 mg and during a 9-day continuous treatment with a dose of 100 mg t.i.d. The same dose of nitrofurantoin served as a reference medication. In the acute cross-over phase food greatly speeded up and atropine somewhat retarded the absorption of furagin, but the total absorption remained virtually unchanged as judged from the unchanged AUC values. The furagin concentrations in serum remain several hours above the MIC concentrations of many pathogenic bacteria. Despite the high concentrations in serum, the urine levels of furagin were generally lower than those of nitrofurantoin. The 24 hr recoveries in urine were 8--13% for furagin and about 36% for nitrofurantoin. In the prolonged trial furagin was absorbed and excreted in the same way as in the acute trial. On the 9th day the concentrations in serum and urine were higher than on the first day. The urinary concentrations of both furagin and nitrofurantoin always remained well above the MIC values of the most susceptible bacteria. Several volunteers complained of nightly cramps in their calves after taking furagin for some days, otherwise the side effects were minimal.