Amphotericin B liposomal: Difference between revisions
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{{Amphotericin B liposomal}} | {{Amphotericin B liposomal}} | ||
{{CMG}}; {{AE}} {{AZ}} | {{CMG}}; {{AE}} {{AZ}} | ||
{{SK}} Liposomal AmB; L-AmB | |||
==Overview== | ==Overview== | ||
Amphotericin B (AmBisome) is a [[polyene antimycotic|polyene]] [[Antifungal medication|antifungal drug]], often used [[intravenous]]ly for systemic [[fungi|fungal]] [[infection]]s. It was originally extracted from ''[[Streptomyces]] , a | Amphotericin B (AmBisome) is a [[polyene antimycotic|polyene]] [[Antifungal medication|antifungal drug]], often used [[intravenous]]ly for systemic [[fungi|fungal]] [[infection]]s. | ||
It was originally extracted from ''[[Streptomyces]]'', a filamentous [[bacterium]], in 1955 at the Squibb Institute for Medical Research from cultures of an undescribed streptomycete isolated from the soil collected in the Orinoco River region of Venezuela. Its name originates from the chemical's amphoteric properties. Two amphotericins, amphotericin A and amphotericin B are known, but only B is used clinically, because it is significantly more active in vivo. Amphotericin A is almost identical to amphotericin B (having a double C=C bond between the 27th and 28th carbons), but has little antifungal activity. | |||
Currently, the drug is available as plain amphotericin B, as a cholesteryl sulfate complex (ABCD), as a lipid complex (ABLC), and as a liposomal formulation (LAmB). The latter formulations have been developed to improve tolerability for the patient, but may show considerably different pharmacokinetic characteristics compared to plain amphotericin B. | Currently, the drug is available as plain amphotericin B, as a cholesteryl sulfate complex (ABCD), as a lipid complex (ABLC), and as a liposomal formulation (LAmB). The latter formulations have been developed to improve tolerability for the patient, but may show considerably different pharmacokinetic characteristics compared to plain amphotericin B. | ||
==Category== | ==Category== | ||
Antifungal | Antifungal | ||
==US Brand Names== | ==US Brand Names== | ||
AMBISOME<sup>®</sup> | AMBISOME<sup>®</sup> | ||
==FDA Package Insert== | ==FDA Package Insert== | ||
''' [[Amphotericin B liposomal description|Description]]''' | |||
| [[Amphotericin B liposomal clinical pharmacology|Clinical Pharmacology]] | '''| [[Amphotericin B liposomal clinical pharmacology|Clinical Pharmacology]]''' | ||
| [[Amphotericin B liposomal microbiology|Microbiology]] | '''| [[Amphotericin B liposomal microbiology|Microbiology]]''' | ||
| [[Amphotericin B liposomal indications and usage|Indications and Usage]] | '''| [[Amphotericin B liposomal indications and usage|Indications and Usage]]''' | ||
| [[Amphotericin B liposomal contraindications|Contraindications]] | '''| [[Amphotericin B liposomal contraindications|Contraindications]]''' | ||
| [[Amphotericin B liposomal warnings and precautions|Warnings and Precautions]] | '''| [[Amphotericin B liposomal warnings and precautions|Warnings and Precautions]]''' | ||
| [[Amphotericin B liposomal adverse reactions|Adverse Reactions]] | '''| [[Amphotericin B liposomal adverse reactions|Adverse Reactions]]''' | ||
| [[Amphotericin B liposomal drug interactions|Drug Interactions]] | '''| [[Amphotericin B liposomal drug interactions|Drug Interactions]]''' | ||
| [[Amphotericin B liposomal overdosage|Overdosage]] | '''| [[Amphotericin B liposomal overdosage|Overdosage]]''' | ||
| [[Amphotericin B liposomal clinical studies|Clinical Studies]] | '''| [[Amphotericin B liposomal clinical studies|Clinical Studies]]''' | ||
| [[Amphotericin B liposomal dosage and administration|Dosage and Administration]] | '''| [[Amphotericin B liposomal dosage and administration|Dosage and Administration]]''' | ||
| [[Amphotericin B liposomal how supplied|How Supplied]] | '''| [[Amphotericin B liposomal how supplied|How Supplied]]''' | ||
| [[Amphotericin B liposomal labels and packages|Labels and Packages]] | '''| [[Amphotericin B liposomal labels and packages|Labels and Packages]]''' | ||
==Mechanism of Action== | ==Mechanism of Action== | ||
As with other polyene [[antifungals]], amphotericin B binds with [[ergosterol]], a component of fungal cell membranes, forming a transmembrane channel that leads to monovalent ion ([[potassium|K<sup>+</sup>]], [[sodium|Na<sup>+</sup>]], [[hydrogen|H<sup>+</sup>]] and [[chloride|Cl<sup>−</sup>]]) leakage, which is the primary effect leading to fungal cell death. Recently, however, researchers found evidence that pore formation is not necessarily linked to cell death.<ref name=Baginski2009>{{cite journal |last1= Baginski |first1= M. |last2= Czub |first2= J. |title= Amphotericin B and Its New Derivatives–Mode of Action |journal= Current Drug Metabolism |volume= 10 |issue= 5 |year= 2009 |pages= 459–69 |pmid= 19689243 }}</ref> The actual mechanism of action may be more complex and multifaceted. | |||
==References== | ==References== | ||
Latest revision as of 01:11, 28 January 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2]
Synonyms and keywords: Liposomal AmB; L-AmB
Overview
Amphotericin B (AmBisome) is a polyene antifungal drug, often used intravenously for systemic fungal infections.
It was originally extracted from Streptomyces, a filamentous bacterium, in 1955 at the Squibb Institute for Medical Research from cultures of an undescribed streptomycete isolated from the soil collected in the Orinoco River region of Venezuela. Its name originates from the chemical's amphoteric properties. Two amphotericins, amphotericin A and amphotericin B are known, but only B is used clinically, because it is significantly more active in vivo. Amphotericin A is almost identical to amphotericin B (having a double C=C bond between the 27th and 28th carbons), but has little antifungal activity.
Currently, the drug is available as plain amphotericin B, as a cholesteryl sulfate complex (ABCD), as a lipid complex (ABLC), and as a liposomal formulation (LAmB). The latter formulations have been developed to improve tolerability for the patient, but may show considerably different pharmacokinetic characteristics compared to plain amphotericin B.
Category
Antifungal
US Brand Names
AMBISOME®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages
Mechanism of Action
As with other polyene antifungals, amphotericin B binds with ergosterol, a component of fungal cell membranes, forming a transmembrane channel that leads to monovalent ion (K+, Na+, H+ and Cl−) leakage, which is the primary effect leading to fungal cell death. Recently, however, researchers found evidence that pore formation is not necessarily linked to cell death.[1] The actual mechanism of action may be more complex and multifaceted.