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Amphotericin B

Biological agents targetted Coccidiodes imitis, Histoplasma capsulatum
Generally effective against Active against a broad range of pathogenic yeasts and fungi.
Available forms Injection, oral suspension, topical cream.
Indications and usage

Intravenous amphotericin B is a drug of last resort for life-threatening systemic fungal infections. It is not to be used for less threatening non-invasive fungal infections such as vaginal candidiasis or oral thrush. In this form it is only to be used under clinical supervision and dosage rates must be very carefully monitored to avoid life-threatening complications including shock. The maximum dose is 1.5 mg/kg/day and should never be exceeded. Topical creams are widely used and effective against candidiasis of the skin.

Oral amphotericin B is also to be used under close medical supervision.

Topical amphoricin B is well tolerated and used for a range of fungal skin infections.

Contraindications Any known sensitivity to amphotericin B, kidney problems, loss of weight.
Drug interactions Generally speaking, use of other drugs with intravenous amphotericin B should be avoided if at all possible. If necessary, then close medical supervision is necessary. It is actually relatively toxic to humans and this can exacerbate the adverse effects of a number of other classes of drugs and antibiotics.
Adverse reactions and side effects

NOTE: all such reactions are rare.

Acute reactions are common in treatment with intravenous amphotericin B, including fever, chills accompanied by shivering, loss of blood pressure, loss of appetite, nausea, vomiting, headache and shallow breathing. The effects are at their worst during the first treatments and lessen with time. Some patients never develop a tolerance for the drug.

Tolerance may be improved by treatment with aspirin or acetaminophen, antihistamines or antiemetics. Chills are controlled with Meperidine in some patients.

Topical amphotericin B is generally well tolerated.

Mode of action Amphotericin B forms a complex with sterols of the cell membrane of the fungus leading to intracellular contents leaking out.
Structure
Chemical names

[1R-(1R*,3S*,5R*,6R*,9R*,11R*,15S*,16R*,17R*,18S*,19E,21E,23E
,25E,27E,29E,31E,33R*,35S*,36R*,37S*)]-33- [(3-amino-3,6-
dideoxy-.beta.-D-mannopyranosyl)oxy]-1,3,5,6,9,11,17,37-
octahydroxy-15,16,18-trimethyl-13-oxo-,14,39-dioxabicyclo
[33.3.1]nonatriaconta-19,21,23,25,27,29,31-heptaene-
3,6-carboxylic acid

CAS Registry number 1397-89-3
Synonyms and trade names
(known and reported, not all may be current.)
Trade Name Country
Abelcet United States
Ambisome United States
Amphocin United States
Ampho-Moronal  Germany
Amphotec United States
Fungilin Unknown - outside the United States
Fungizone IV United States
Fungizone Canada, France
Fungizone Topical  United States
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