Anti-Fungal Agents

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Anonymous
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292599
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Anti-Fungal Agents
Updated:
2015-01-07 14:37:49
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Anti fungal Pharmacology
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Description:
Vet Med - Module 7
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  1. List some of the reasons why fungal infections may be on the increase
    • Use of agents that disrupt normal host microflora
    • Failure to develop a strong immune system
    • Patient management that suppresses the immune system
    • Chemotherapy, HIV/AIDs, transplants, steroid treatments
    • Diabetes
    • Antibiotic use - disrupts communities of microbes and allows fungal populations to increase
    • AgeĀ 
    • Invasive surgical procedures that introduce fungi
  2. What are fungal infections called?
    Mycoses
  3. Give examples of systemic and superficial fungal infections
    • Systemic - aspergillus, candida, cyrptococcus
    • Superficial - dermatophytes, candida, malessezia
  4. Fungi are prokaryotes/eukaryotes?
    Eukaryotes
  5. What are some of the sites of action of common anti-fungal drugs?
    • Cell wall
    • Cell membrane
    • Fungal DNA
    • Microtubules
  6. What steoid are fungal cell membranes rich in?
    Ergosterol
  7. Which three classes of anti fungal drugs target ergosterol?
    • Allyamines
    • Azoles
    • Amphotericin B (polyenes)
  8. What is the mechanism of action of Allyamines?
    Inhibits ergosterol biosynthesis via inhibition of squalene epoxidase
  9. What is the spectrum of activity of Allyamines?
    Dermatophytes
  10. What are routes of administration for Allyamines?
    Oral and topical
  11. Describe the pharmacokinetics of allyamines
    Highly lipophilic, hepatic metabolism, faecal and renal elimination
  12. Are allyamines fungicidal or fungistatic?
    Fungicidal
  13. What is the mechanism of action of azoles?
    Inhibition of cytP450-dependent 14-sterol de-methylase
  14. What are the side effects of azoles?
    GIT, anorexia, hepatotoxicity, suppression of steroid production, teratogenic
  15. What are the routes of administration for azoles?
    Oral and topical
  16. Describe the pharmacokinetics of azoles
    • Depends on the agent:
    • Ketoconazole and Itraconazole - weak bases, lipophilic, highly plasma protein bound, hepatic metabolism and excretion in faeces
    • Fluconazole - not affected by gastric pH, water soluble and can be given IV, minimally plasma protein bound, minimally metabolised, 80% excreted by kidney unchanged
  17. What is the mechanism of action of polyenes?
    Binds to ergosterol and disrupts osmotic integrity of the membrane
  18. What are the side effects of polyenes?
    Nephrotoxicity, hypokalaemia, thrombophlebitis
  19. What are the routes of administration of polyenes?
    Some are now encapsulated in liposomes/lipid complexes to increase uptake in certain areas of the body
  20. Describe the pharmacokinetics of polyenes
    Poorly water soluble, little absorption from GIT
  21. What is the cell wall of fungal cells composed of?
    Chitin is on the inside and mannoproteins & b-glucans on the outside
  22. What is the mechanism of action of drugs that target the cell wall?
    Block the synthesis of b(1,3)glucan
  23. What is the spectrum of activity of cell wall antifungals?
    Candida and aspergillus species
  24. What is the route of administration of cell wall antifungals?
    IV
  25. Describe the pharmacokinetics of cell wall antifungals
    Water soluble, highly plasma protein bound, eliminated in urine and faeces as metabolites
  26. What type of anti fungal drug targets protein synthesis?
    Antimetabolites
  27. What is the mechanism of action of antimetabolites?
    Disrupts protein synthesis
  28. What is the spectrum of activity of antimetabolites?
    Cryptococcus and Candida species
  29. What is the route of administration of antimetabolites?
    Oral
  30. Describe the pharmacokinetics of antimetabolites
    Excreted unchanged by the kidney
  31. What other anti fungal drug are antimetabolites combined with to give better anti fungal action?
    Amphotericin B
  32. What type of anti fungal drug targets microtubules?
    Griseofulvin
  33. What is the mechanism of action of griseofulvin?
    Selectively deposited in newly formed keratin, inhibits mitosis, disorganises the spindle microtubules
  34. What are the side effects of griseofulvin?
    Idiosyncratic reaction in cats, teratogenic
  35. What is the route of administration of griseofulvin?
    Oral (with high fat diet)
  36. Describe the pharmacokinetics of grisefulvin
    Poorly water soluble, hepatic metabolism and faecal elimination
  37. What is griseofulvin licenced for in the UK?
    Treating ringworm in horses

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