CLINICAL PHARMACOLOGY Each Macrobid capsule contains two forms of nitrofurantoin. Twenty-five percent is macrocrystalline nitrofurantoin, which has slower dissolution and absorption than nitrofurantoin monohydrate. 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. Based on urinary pharmacokinetic data, the extent and rate of urinary excretion of nitrofurantoin from the 100 mg Macrobid capsule are similar to those of the 50 mg or 100 mg Macrodantin ® (nitrofurantoin macrocrystals) capsule. Approximately 20-25% of a single dose of nitrofurantoin is recovered from the urine unchanged over 24 hours. Plasma nitrofurantoin concentrations after a single oral dose of the 100 mg Macrobid capsule are low, with peak levels usually less than 1 mcg/ mL. Nitrofurantoin is highly soluble in urine, to which it may impart a brown color. When Macrobid is administered with food, the bioavailability of nitrofurantoin is increased by approximately 40%. Microbiology: Nitrofurantoin is bactericidal in urine at therapeutic doses. The mechanism of the antimicrobial action of nitrofurantoin is unusual among antibacterials. Nitrofurantoin is reduced by bacterial flavoproteins to reactive intermediates which inactivate or alter bacterial ribosomal proteins and other macromolecules. As a result of such inactivations, the vital biochemical processes of protein synthesis, aerobic energy metabolism, DNA synthesis, RNA synthesis, and cell wall synthesis are inhibited. | ||||
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