Indications
Furazolidone is specifically indicated for the treatment of bacterial or protozoal diarrhea and enteritis caused by organisms susceptible to its effects. It addresses both specific and symptomatic relief in affected patients.
Pharmacodynamics
Furazolidone exhibits a broad antibacterial spectrum, effectively targeting a wide range of pathogenic microorganisms commonly found in the gastrointestinal tract. These include Escherichia coli, staphylococci, Salmonella, Shigella, Proteus species, Aerobacter aerogenes, Vibrio cholerae, and Giardia lamblia. Its bactericidal activity arises from interference with DNA replication and protein synthesis, thereby minimizing the emergence of resistant strains.
Absorption
Studies utilizing radiolabeled compounds have demonstrated that furazolidone is efficiently absorbed following oral administration. This characteristic ensures adequate bioavailability for therapeutic efficacy.
Metabolism
Once absorbed, furazolidone undergoes rapid and extensive metabolism. The primary metabolic pathway starts with the nitro-reduction to the aminofuran derivative. This process yields two major metabolites: 3-amino-2-oxazolidone (AOZ) and beta-hydroxyethylhydrazine (HEH), with AOZ notably contributing to the inhibition of monoamine oxidase. The detoxification and elimination of furazolidone are primarily facilitated through conjugation with glutathione.
Mechanism of Action
Furazolidone operates by a distinctive mechanism whereby it and its associated free radical derivatives interact with DNA, promoting the formation of cross-links. This interaction significantly impacts bacterial DNA, rendering it particularly vulnerable to the drug's effects. As a result, there is a notable increase in both transitions and transversions within the bacterial chromosome, leading to elevated mutation rates.
