Amphotericin B
Amphotericin B is fungistatic or fungicidal depending on the concentration obtained in body fluids and the susceptibility of the fungus. The drug acts by binding to sterols (ergosterol) in the cell membrane of susceptible fungi. This creates a transmembrane channel, and the resultant change in membrane permeability allowing leakage of intracellular components. Ergosterol, the principal sterol in the fungal cytoplasmic membrane, is the target site of action of amphotericin B and the azoles. Amphotericin B, a polyene, binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.
Systemic Fungal Infections-Test dose: 1 mg IV infused over 20-30 minLoad: 0.25-0.5 mg/kg IV infused over 2-6 hourMaintenance: 0.25-1 mg/kg IV qDay OR up to 1.5 mg/kg IV every other day (may increase gradually by 0.25 mg-increments/day)
Increased toxicity with flucytosine. Drug induced renal toxicity enhanced in presence of other nephrotoxic medications. Antagonises effects of azole antifungals.
Amphotericin B is contraindicated in those patients who have demonstrated or have known hypersensitivity to amphotericin B deoxycholate or any other constituents of the product unless, in the opinion of the treating physician, the benefit of therapy outweighs the risk.
Common side effects are Fever, chills, convulsions, malaise; nausea, vomiting, diarrhoea, anorexia; tinnitus, vertigo, hearing loss; hypotension, hypertension, cardiac arrhythmias; peripheral neuropathy; phloebitis, pain at Inj site, disturbances in renal function and renal toxicity.
Pregnancy Category B. There have been no adequate and well-controlled studies of Amphotericin B in pregnant women. It is not known whether Amphotericin B is excreted in human milk.
As with any Tericin-containing product the drug should be administered by medically trained personnel. During the initial dosing period, patients should be under close clinical observation. Tericin has been shown to be significantly less toxic than Tericin deoxycholate; however, adverse events may still occur.
Other Antifungal preparations
Aseptically add 12 mL of Sterile Water for Injection, to each Tericin vial to yield a preparation containing 4 mg Tericin/mL. Immediately after the addition of water, shake the vial vigorously for 30 seconds to completely disperse the Tericin. This forms a yellow, translucent suspension. Visually inspect the vial for particulate matter and continue shaking until completely dispersed.
Unopened vials of lyophilized material are to be stored at temperatures up to 25°C. The reconstituted product concentrate may be stored for up to 24 hours at 2-8° C.
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