Amphotericin B Mechanism of Action

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Questions and Answers

What is the mechanism of action of Amphotericin B?

  • Inhibiting the synthesis of fungal proteins
  • Activating the host's immune response against fungal infections
  • Forming pores in fungal cell membranes that disrupt membrane function (correct)
  • Inhibiting the synthesis of fungal cell walls

What is the primary route of excretion of Amphotericin B?

  • Sweat
  • Bile
  • Faeces
  • Urine (correct)

What is the purpose of premedication with a corticosteroid or antipyretic before administering Amphotericin B?

  • To mitigate the risk of nephrotoxicity
  • To prevent allergic reactions
  • To enhance the antifungal activity
  • To reduce the risk of infusion-related reactions (correct)

What is the significance of the low therapeutic index of Amphotericin B?

<p>It has a high risk of adverse effects (A)</p> Signup and view all the answers

What is the primary mechanism of action of Amphotericin B against fungal cells?

<p>Disrupting membrane function (D)</p> Signup and view all the answers

What is the significance of adequate hydration in patients receiving Amphotericin B?

<p>It decreases the risk of nephrotoxicity (A)</p> Signup and view all the answers

What is the effect of Amphotericin B on fungal cells?

<p>It has both fungicidal and fungistatic properties (B)</p> Signup and view all the answers

What is the purpose of co-formulating Amphotericin B with sodium deoxycholate or artificial lipids?

<p>To increase its solubility in water (C)</p> Signup and view all the answers

What is the effect of other nephrotoxic drugs on the risk of nephrotoxicity associated with Amphotericin B?

<p>They increase the risk of nephrotoxicity (A)</p> Signup and view all the answers

What is the type of antifungal agent that Amphotericin B is classified as?

<p>Polyene (A)</p> Signup and view all the answers

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Study Notes

Amphotericin B

  • Derived from Streptomyces nodosus, a naturally occurring polyene antifungal
  • Used to treat life-threatening mycoses

Mechanism of Action

  • Binds to ergosterol in fungal cell membranes
  • Forms pores that disrupt membrane function, causing leakage of electrolytes and small molecules
  • Ultimately leads to cell death
  • Exhibits both fungicidal and fungistatic properties

Spectrum of Activity

  • Effective against a broad range of fungi, including:
    • Candida albicans
    • Histoplasma capsulatum
    • Cryptococcus neoformans
    • Coccidioides immitis
    • Blastomyces dermatitidis
    • Various strains of Aspergillus
  • Also used to treat leishmaniasis

Pharmacokinetics

  • Administered through slow IV infusion
  • Insoluble in water, requires co-formulation with sodium deoxycholate or artificial lipids
  • Extensively bound to plasma proteins
  • Distributed throughout the body
  • Excreted primarily in the urine over an extended period
  • Limited penetration into certain body fluids

Adverse Effects

  • Low therapeutic index
  • Fever and chills:
    • Occur 1-3 hours after IV administration
    • Premedication with corticosteroid or antipyretic recommended
  • Renal impairment:
    • Azotemia exacerbated by other nephrotoxic drugs (aminoglycosides, cyclosporine, vancomycin)
    • Adequate hydration can decrease severity

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