The mechanism of the antimicrobial action of nitrofurantoin is unusual among antibacterials. Nitrofurantoin is a nitrofuran antimicrobial agent with activity against certain Gram-positive and Gram-negative bacteria. When nitrofurantoin is administered with food, the bioavailability of nitrofurantoin is increased by approximately 40%. Nitrofurantoin is highly soluble in urine, to which it may impart a brown color. Plasma nitrofurantoin concentrations after a single oral dose of the 100 mg nitrofurantoin capsule (monohydrate/macrocrystals) are low, with peak levels usually less than 1 mcg/mL. Approximately 20% to 25% of a single dose of nitrofurantoin is recovered from the urine unchanged over 24 hours. Based on urinary pharmacokinetic data, the extent and rate of urinary excretion of nitrofurantoin from the 100 mg nitrofurantoin capsule (monohydrate/macrocrystals) are similar to those of the 50 mg or 100 mg nitrofurantoin macrocrystals capsule. The remaining 75% is nitrofurantoin monohydrate contained in a powder blend which, upon exposure to gastric and intestinal fluids, forms a gel matrix that releases nitrofurantoin over time. Twenty-five percent is macrocrystalline nitrofurantoin, which has slower dissolution and absorption than nitrofurantoin monohydrate. Each nitrofurantoin capsule (monohydrate/macrocrystals) contains two forms of nitrofurantoin.
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