Furazolidone

Chemical formula: C₈H₇N₃O₅  Molecular mass: 225.16 g/mol  PubChem compound: 3435

Pharmacodynamic properties

Furazolidone is a microbicidal. It is a broad-spectrum anti-infective that is effective against most gastrointestinal tract pathogens.

Furazolidone interferes with several bacterial enzyme systems. It neither significantly alters normal bowel flora nor results in fungal overgrowth.

Furazolidone also acts as a monoamine oxidase inhibitor (MAOI). MAOIs prevent the inactivation of tyramine by hepatic and gastrointestinal monoamine oxidase. Tyramine in the bloodstream releases norepinephrine from the sympathetic nerve terminals and produces a sudden increase in blood pressure.

Pharmacokinetic properties

Absorption

Radiolabeled drug studies indicate that furazolidone is well absorbed following oral administration.

Distribution

Limited pharmacokinetic information is available in humans; however, recent data have reported that variable plasma concentrations were measured in subjects given therapeutic doses. One study of 8 meningitis patients showed that cerebral spinal fluid (CSF) concentrations reached levels comparable to serum concentrations. Also, significant concentrations have been measured in the bile of rats.

Biotransformation

Furazolidone is rapidly and extensively metabolized; the primary metabolic pathway identified begins with nitro-reduction to the aminofuran derivative.

Elimination

Radiolabeled drug studies showed that more than 65% of an oral dose was recovered in the urine of humans and animals. Also found in feces.

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