Abelcet

Lipid-associated formulations of amphotericin B, liposomal amphotericin B (AmBisome) and amphotericin B lipid complex (Abelcet) have been approved for use in proven cases of candidiasis however, patients with invasive candidiasis have also been treated successfully with amphotericin B colloid dispersion (Amphotec or Amphocil). The lipid-associated formulations are less toxic but as effective as amphotericin B deoxycholate. 

For the purposes of comparison, commercial AmB-lipid formulations were obtained as follows. Amphotec was obtained from Intermune (U.S.A.). AmBisome and Abelcet were kind gifts from Gilead Sciences (Foster City, California, U.S.A.) and Zedeus Pharma (Versailles, France), respectively. Ampholiposomes (cationic oligolameller liposomes containing AmB) were supplied by the Pharmacie Centrale des Hopitaux (Paris, France). 

The low acute toxicity of LC-AmB would be expected to allow higher cumulative doses of the antibiotic to be administered. This hypothesis was tested in CDl mice, which were given various doses of LC-AmB daily for three weeks. Groups were also treated with Fungizone (0.5mg/kg) and Abelcet (10 mg/kg) according to the same regimen. At the end of the treatment period, mice were sacrificed and various biochemical parameters were measured (28). 

The results of the chronic administration study indicate that LC-AmB does not induce any new toxicity and that its side effects are the same as those produced by the conventional formulation (Fungizone) and a commercial lipid formulation (Abelcet) but that they appear at higher doses. This difference is probably due to both the stability of the formulation, preventing rapid release of AmB as aggregates or transfer to lipoproteins, and its size difference with Abelcet, which could lead to less rapid uptake by phagocytic cells. These encouraging results with respect to toxicity prompted us to test the efficacy of the formulation. For this, we chose to look at in vitro and in vivo models of Leishmaniasis, as well as the immuno-modulating properties of AmB. 

In one experiment, LC-AmB was compared with AmBisome (small unilamellar liposomes). LC-AmB was found to have an ED50 of 0.19 mg/kg and an ED90 of 0.51 mg/kg, whereas for AmBisome both these parameters were below 0.20 mg/kg, the lowest dose tested. In another experiment, LC-AmB was compared with Abelcet and showed a better reduction of parasite burden after three injections of 1 mg/kg, but there were not sufficient data to allow ED50 values to be calculated (22). Therefore, we can conclude that this new AmB formulation retains antileishmanial activity in vivo, but it is difficult to position it with respect to other formulations. 

Abelcet) at 5 mg/kg/day and 5 children with hepatosplenic candidiasis were effectively treated with 2.5 mg/kg/day. Safety and efficacy in patients younger than 1 month of age have not been established. 

Amphotericin B (Amphocin) Amphotericin B Cholesteryl (Amphotec) Amphotericin B Lipid Complex (Abelcet) Amphotericin B Liposomal (AmBisome) Anidulafungin (Eraxis)... 

Brand Name(s) Abelcet (ABLC) AmBisome, Amphotec, Fungizone (IV and topical) Chemical Class Amphoteric polyene lipid complex (ABLC)... 

Pharmacokinetics Protein binding 90%. Widely distributed. Metabolic fate unknown. Cleared bynonrenal pathways. Minimal removal by hemodialysis. Amphotec and Abelcet are not dialyzable. Amphotec Half-life 26-28 hr. Abelcet Half-life 7.2 days. AmBisome Half-life 100-153 hr. 

Suspension for Injection-. 5 mg/ml (Amphotericin B lipid complex, Abelcet). 

Invasive fungal infections unresponsive orintoleranttoFungizone (Abelcet) IV Infusion... 

Abelcet-. Chills, fever, increased serum creatinine, multiple organ failure AmBisome-. Hypokalemia, hypomagnesemia, hyperglycemia, hypocalcemia, edema, abdominal pain, back pain, chills, chest pain, hypotension, diarrhea, nausea, vomiting, headache, fever, rigors, insomnia, dyspnea, epistaxis, increased liver/renal function test results... 

Adedoyin, A., C.E. Swenson, L.E. Bolcsak, A. Hellmann, D. Radowska, G. Horwith, A.S. Janoff, and R.A. Branch, A pharmacokinetic study of amphotericin B lipid complex injection (Abelcet) in patients with definite or probable systemic fungal infections. Antimicrob Agents Chemother, 2000.44(10) 2900-2. 

Abelcet) 100 mg/20 mL suspension for injection (AmBisome) 50 mg powder for injection (Amphotec) 50, 100 mg powder for injection Topical 3% cream, lotion, ointment Butoconazole (Gynazole-1, Mycelex-3)... 

Abelcet , amphotericin lipid complex injection. Liposome Co., Princeton, NJ. 

Several newer forms of amphotericin B (Abelcet, AmBisome, Amphotec) have also been developed. These drugs are encapsulated in small lipid spheres (liposomes) and then injected slowly by intravenous infusion.26,57 The lipid-based preparations appear to deliver higher doses of amphotericin B to the site of... 

Abelcet consists of ribbon-like structures having a diameter in the 2-5 pm range. 

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