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Mafenide (Mafenide Acetate) - Description and Clinical Pharmacology

 
 



DESCRIPTION


Mafenide Acetate, USP is a synthetic antimicrobial agent designated chemically as α-amino-p-toluenesulfonamide monoacetate. It has the following structural formula:


Mafenide Acetate, USP is a white, crystalline powder which is freely soluble in water.
 
Mafenide Acetate,USP For 5% Topical Solution is provided in packets containing 50 g of sterile Mafenide Acetate to be reconstituted in 1000 mL of Sterile Water for Irrigation, USP or 0.9% Sodium Chloride Irrigation, USP. After mixing, the solution contains 5% w/v of mafenide acetate. The solution is an antimicrobial preparation suitable for topical administration. The solution is not for injection. The reconstituted solution may be held up to 28 days after preparation if stored in unopened containers. ONCE A CONTAINER IS OPENED, ANY UNUSED PORTION SHOULD BE DISCARDED AFTER 48 HOURS. Store the reconstituted solution at 20° to 25°C (68° to 77°F). Limited storage periods at 15° to 30°C (59° to 86°F) are acceptable.

CLINICAL PHARMACOLOGY


Mechanism of Action:
The mechanism of action of Mafenide is not known, but is different from that of the sulfonamides. Mafenide is not antagonized by pABA, serum, pus or tissue exudates, and there is no correlation between bacterial sensitivities to mafenide and to the sulfonamides. Its activity is not altered by changes in the acidity of the environment. The osmolality of the 5% topical solution is approximately 340 mOsm/kg.

 Absorption and Metabolism:
Applied topically, Mafenide Acetate diffuses through devascularized areas. Approximately 80% of a Mafenide Acetate dose is delivered to burned tissue over four hours following topical application of the 5% solution. Following application of Mafenide Acetate cream and solution, peak Mafenide concentrations in human burned skin tissue occur at two and four hours, respectively. Peak tissue concentrations are similar following administration of the solution or cream. Once absorbed, Mafenide is rapidly converted to an inactive metabolite (p-carboxybenzenesulfonamide) which is cleared through the kidneys. Clinical studies have shown that when applied topically to burns as an 11.2% Mafenide Acetate cream, blood levels of the parent drug peaked at 2 hours following application, ranging from 26 to 197 µg/mL for single doses of 14 to 77 g of Mafenide Acetate. Metabolite levels peaked at 3 hours, ranging from 10 to 340 µg/mL. Twenty-four hours after application, combined parent and metabolite blood levels had fallen to pretreatment levels.
 
Antimicrobial Activity:
Mafenide Acetate exerts broad bacteriostatic action against many gram-negative and gram-positive organisms, including Pseudomonas aeruginosa and certain strains of anaerobes.

In Vitro
Cytotoxicity:
Data from in vitro studies on cell culture suggests that Mafenide Acetate may have a deleterious effect on human keratinocytes. The clinical significance of this information is unknown.

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