Of amphotericin

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. 

The insolubility of amphotericin B (1) in common organic solvents necessitated the preparation of tractable intermediates that were more... 

A demonstration of the usefulness of this deglycosidation reaction in the preparation of amphotericin B aglycon derivatives is shown in Scheme 3. Exposure of amphotericin B derivatives 5ab to NBS and CaC03 in CCI4 results in the formation of heptaenones 6ab in 18-30% yield (two isomers) together with bicyclic system 7 (10%) and mycosamine derivative 8 (9%). 

In the selection of suitable chiral starting materials for the total synthesis of amphotericin B (1) and amphoteronolide B (2), the recognition of subtle symmetry in the targets played a crucial role. 

A patient weighs 140 pounds. If amphotericin B 1.5 mg/kg per day is prescribed, what is the total daily dosage of amphotericin B for this patient ... 

Altered tissue distribution of amphotericin B by liposomal encapsulation Comparison of normal mice and mice infected with Candida albicans. Cancer Drug Deliv., 1, 199-205. 

Newman, M. S., Guo, L., McCalden, T. A., Levy, M., Porter, J., Wong, A., and Fielding, R. M. (1989). A colloidal dispersion of amphotericin B with reduced lethality and non lethal toxicity, Proc. AAPS Western Regional Meet., February 26-March 1, 1989. 

Pilot study of amphotericin B entrapped in sonicated liposomes in cancer patients with fungal infections, Eur. J. Cancer cun. Oncol., 24, 527-538. 

This procedure has been recently applied to the synthesis of L-lyxitol and the polyhydroxylated chain of amphotericin Interesting results have also been obtained in the reduction of ) -oxo derivatives of dithioacetal monoxides. In the reaction sequence of equation 322 two successive asymmetric inductions are involved. After the first reaction, involving acylation of the carbanion, a diastereoisomeric mixture in a 65 35 ratio is produced. When this mixture is reduced with NaBH4 in MeOH-conc. aqueous solution of ammonia, among four possible diastereoisomeric alcohols, the stereoisomer 523 is obtained with a stereoselectivity of 98% . Guanti and coworkers have found that the LiAlH4 reduction of the same substrates at — 78° in THF/ether leads to 523 with a stereoselectivity 99 i6i3.6i4... 

Amphotericin B-induced ARF occurs in as many as 40% to 65% of patients treated with the conventional desoxycholate formulation.30 Nephrotoxicity is due to renal arterial vasoconstriction and distal renal tubule cell damage. Risk factors include high doses, treatment for at least 7 days, preexisting kidney dysfunction, and concomitant use of other nephrotoxic drugs.31 Three lipid-based formulations of amphotericin B have been developed in an attempt to decrease the incidence of ARF amphotericin B lipid complex, amphotericin colloidal dispersion, and liposomal amphotericin B. The range of... 

Two to three weeks of fluconazole or itraconazole solution are highly effective and demonstrate similar clinical response rates.32 Doses of 100 to 200 mg are effective in immunocompetent patients but doses up to 400 mg are recommended for immunocompromised patients. Due to variable absorption, ketoconazole and itraconazole capsules should be considered second-line therapy. In severe cases, oral azoles may prove ineffective, warranting the use of amphotericin B for 10 days. Although echinocandins and voriconazole are effective in treatment of esophageal candidiasis, experience remains limited. 

Preclinical studies suggest mold-active azoles plus echinocandins have enhanced activity against Aspergillus A. terreus should be considered resistant to amphotericin B Activity of amphotericin B and voriconazole is decreased versus Aspergillus species higher doses or combination therapy may be indicated in more refractory cases... 

Fusariosis Lipid formulations of amphotericin B OR Voriconazole 6 mg/kg q12hour for 1 day, then 4 mg/kg q12hour OR Posaconazole 200 mg PO qid for 14 days, then 200 mg PO q12hour OR Combination therapy ... 

Kullberg BJ, Sobel JD, Ruhnke M, et al. Voriconazole versus a regimen of amphotericin B followed by fluconazole for candidaemia in non-neutropenic patients a randomised non-inferiority trial. Lancet 2005 366 1435-1442. 

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