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Antifungals amphotericin B

Polyketides are an extraordinarily valuable class of natural products, numbering over 10,000 compounds. Commercially important polyketides include antibiotics (erythromycin A, tetracycline) and immunosuppressants (rapamycin), as well as anticancer (doxorubicin), antifungal (amphotericin B), and cholesterol-lowering (lovastatin) agents (Figure 25.15). It has been estimated that the sales of these and other polyketide pharmaceuticals total more than 15 billion per year. [Pg.1031]

Clotrimazole and other azole derivatives have a different mode of action than the polyenes, eg, amphotericin B. The latter biad to the ergosterol present ia the membranes of yeasts and fungi, but azole derivatives inhibit the cytochrome P-450 dependent biosynthesis of ergosterol (8—11). This inhibition not only results in a reduction of ergosterol, but also in an accumulation of C-14 methyl sterols. They disturb membrane permeabiUty, inhibit cell rephcation, and are basically responsible, in combination with the reduction of ergosterol levels, for the antifungal action. [Pg.253]

Amoxicillin — see Penicillin, D-n-amino-p-hydroxybenzyl-Amozonolysis cycloalkenes, 6, 876 Amphotericin B antifungal agent veterinary use, 1, 211... [Pg.515]

Antifungal drugs are used to treat superficial and deep fungal infections. The antifungal drugs specifically discussed in this chapter are amphotericin B (Fungizone), flucona-... [Pg.130]

Amphotericin B is particularly effective against systemic infections caused by C. albicans and Cryptococcus neoformans. It is poorly absorbed from the gastrointestinal tract and is thus usually administered by intravenous injection under strict medical supervision. Amphotericin B methyl ester (Fig. 5.15C) is water-soluble, unlike amphotericin B itself, and can be administered intravenously as a solution. The two forms have equal antifungal activity but higher peak serum levels are obtained with the ester. Although the ester is claimed to be less toxic, neurological effects have been observed. An ascorbate salt has recently been described which is water-soluble, of similar activity and less toxic. [Pg.114]

Treatment of fungal IE is exceptionally difficult. There is a significant lack of studies to identify and recommend the most appropriate therapy. Currently, amphotericin B is the most common treatment. However, valve replacement surgery is often considered an adjunct therapy. Intravenous antifungal therapy requires high doses for a minimum of 8 weeks of treatment. Oral azoles (e.g., fluconazole) are used as long-term suppressive therapy to prevent relapse. The exact role of some... [Pg.1100]

Clinical trials performed by the National Institute of Allergy and Infectious Diseases (NIAID) Mycoses Study Group showed that 2 weeks of induction antifungal therapy with combination amphotericin B (0.7 mg/kg per day) plus... [Pg.1211]

Response to antifungal therapy in invasive candidiasis is often more rapid than for endemic fungal infections. Resolution of fever and sterilization of blood cultures are indications of response to antifungal therapy. Toxicity associated with antifungal therapy is similar in these patients as described earlier with the caveat that some toxicities maybe more pronounced in crit-ically-ill patients with invasive candidiasis. Nephrotoxicity and electrolyte disturbances, with amphotericin B in particular, are problematic and may not be avoidable even with lipid amphotericin B formulations. Fluconazole and echinocandins are generally safer options, and are generally well tolerated. Decisions to use one class of agents over the other is principally driven by concerns of non-albicans species, patient tolerability, or history of prior fluconazole exposure (risk factor for non-albicans species.). [Pg.1223]

Certain compounds are known to achieve higher absorption rates from the GI tract if they are taken with food, and this observation has been linked to their solubilization by bile salts [74], Bile salts, especially those of cholic and deoxycholic acids, have been used to solubilize steroid hormones [75], antibiotics [76], and nonsteroidal antiinflammatory drugs [77]. For example, amphotericin B (an antifungal agent) has been solubilized for parenteral use in micelles composed of sodium desoxycholate [78], As illustrated in Fig. 11, the degree of solubilization of carbamazepine by sodium desoxycholate is minimal below the critical micelle concentration but increases rapidly above this value [79]. At sufficiently high concentrations, when the micelles become saturated in carb-amezepine, the apparent solubility reaches a limiting value approximately seven times the true aqueous solubility in the absence of desoxycholate. [Pg.349]

HIV-infected patients should receive induction therapy with amphotericin B and chronic suppressive therapy with an oral azole antifungal. Itraconazole is the drug of choice for non-life-threatening histoplasmosis. [Pg.429]

Specific antifungals (and their usual dosages) for the treatment of coccidioidomycosis include amphotericin B IV (0.5 to 1.5 mg/kg/day), ketocona-zole (400 mg orally daily), IV or oral fluconazole (usually 400 to 800 mg daily, although dosages as high as 1,200 mg/day have been utilized without complications), and itraconazole (200 to 300 mg orally twice daily as either capsules or solution). If itraconazole is used, measurement of serum concentrations may be helpful to ascertain whether oral bioavailability is adequate. [Pg.431]


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See also in sourсe #XX -- [ Pg.243 ]




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