Miconazole Amphotericin

Ketoconazole. For treatment of systemic mycoses with amphotericin B or miconazole, the patient must be admitted to a hospital. This is not always possible, particularly in areas where systemic mycoses occur frequently, nor is it always desirable, because of the expense. For these reasons, it was desirable to find an antimycotic that combined safety and broad-spectmm activity with oral adraiinistration. Ketoconazole (10), which is orally active, met most of these requirements. This inhibitor of the ergosterol biosynthesis is an A/-substituted imidazole, that differs from its precursors by the presence of a dioxolane ring (6,7). Ketoconazole is rapidly absorbed in the digestive system after oral adrninistration. Sufficient gastric acid is required to dissolve the compound and for absorption. Therefore, medication that affects gastric acidity (for example, cimetidine and antacids) should not be combined with ketoconazole. 

A combination of amphotericin B, miconazole (16), and rifampin (17) was used to successfully cure one patient. In addition, tetracycline (7) and minocycline (18) have been recommended although their clinical efficacy have not been estabUshed. No proven therapeutic agents exist for treating A.catbamoeba infections, however, the phenothiazines, trifluoperazine [117-89-5] and chlorpromazine [50-53-3], show promise in vitro. 

Hoeprich and Huston [117] assessed the stability of miconazole and three other antifungal agents under conditions encountered in bioassay and susceptibility testing in vitro. Although the amphotericins were labile as compared with other drugs, tests should be reliable with all four drugs in view of the rapid action of the polyenes and the relatively slow action of miconazole and 5-fluorocytosines. 

The answer is d. (Hardman, pp 1183-1184.) Mucocutaneous infections, most commonly Candida albicans, involve the moist skin and mucous membranes. Agents used topically include amphotericin B, nystatin, miconazole, and clotrimazole. Ketoconazole and fluconazole are administered orally in pill form for treatment of chronic infections... 

Mucocutaneous infections caused primarily by the fungus Candida albicans occm in regions of moist skin and mucous membranes (i.e. gastrointestinal tract, perianal, and vulvovaginal areas). Amphotericin B, miconazole, clotrimazole, and nystatin are used topically to treat such infections. For chronic infections, ketoconazole is taken orally. 

Drugs that may interact with miconazole include amphotericin B, astemizole, cisapride, oral anticoagulants, phenytoin, and terfenadine. 

Miconazole, oxiconazole, ketoconazole, sulconazole, clotrimazole (along with betamethasone dipropionate), terbinafine (SEBIFIN), naftifine, butenafine, tolnaftate, nystatin, amphotericin B, cyclopirox... 

Amifostine Amifostine is incompatible with many drugs such as acyclovir sodium, amphotericin, cefoperazone sodium, hydroxyzine hydrochloride, miconazole, minocycline hydrochloride, and prochlorpherazine edisylate.239 Care should be exercised when handling amyl nitrate, since it is highly flammable. Volatile nitrites, such as poppers, are abused and fatal adverse effects are reported.240,241... 

A rabbit model for Candida albicans compared the efficacy of topical amphotericin B with four other antifungal agents. Amphotericin B and 5% natamycin were the most effective, 1% miconazole and 1% flucytosine were effective but inferior to the polyenes, and 1% ketoconazole was not effective (O Day et al.). 

The cytoplasmic membrane inside the cell wall is the site of most of the microbial cell s biochemical activity. Drugs that interfere with its function include polyenes (nystatin, amphotericin), azoles (fluconazole, itraconazole, miconazole), polym5odns (colistin, polymyxin B). 

Cutaneous infection is generally treated with topical amphotericin, clotrimazole, econazole, miconazole or nystatin. Local hygiene is also important An imder-lying explanation should be sought if a patient fails to respond to these measures, e.g. diabetes, the use of a broad-spectrum antibiotic or of immimosuppressive drugs. 

Candidiasis of the alimentary tract mucosa responds to amphotericin, fluconazole, ketoconazole, miconazole or nystatin as lozenges (to suck, for oral infection), gel (held in the mouth before swallowing), suspension or tablets. 

Nystatin and miconazole have a spectrum of activity similar to that of amphotericin B against the common yeast and fungi responsible for otomycosis. Nystatin is occasionally used in solution as an ototopic drop. Miconazole is rarely used because it is readily available only as a cream. Application into the ear canal is difficult without impairing the hearing. 

Fig. 4.3 Structures of polyene (amphotericin B) and azole (itraconazole, fluconazole, miconazole and ketoconazole) antifungal agents.

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