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Antifungal Drugs

  1. Amphoptericin B
    1. Amp B is ampipathic (soluble in lipid and water)
    2. Inhibits ergosterol *biosynthesis (*Fungal cholesterol equivalent) 
    3. Given along with normal saline
    4. *Fungal cholesterol equivalent
    5. Saline loading protects kidneys
    6. Given along with deoxycholic acid
    7. P/k: Long acting; not absorbed orally
    8. Half life =2 weeks
    9. Inactivated by liver
    10. Dosage does not need modification in renal failure
    11. Use:
      1. DOC for:                        
      2. Systemic fungal infections    
      3. Safe in pregnancy        
      4. Cryptococcal meningitis

Side effects

  1. MC-chills with rigors
  2. Anemia
  3. Nephrotoxicty
  • Renal tubular acidosis
  • Proteinuria
  • Glomerulonephritis does not occur
  1. Hypokalemia                
  2. Hyperkalemia              
  3. Hypomagnesemia  

2. Ketoconazole

  1. Maintenance drug;
  2. Given by oral route
  3. Inhibits lanosterol-danosterol synthesis
  4. pH dependent absorption; avoided with antacids
  5. Inhibits CYP enzymes
  6. T1/2= 24 hours
  7. Rx-recurrent moniliasis
  8. Topically, used for dandruff
  9. Hepatitis-serious side effect
  10. Antiandrogenic  

3. Fluconazole

  1. Fungistatic                    
  2. Long acting                  
  3. Half life 24 hours
  4. Eliminated unchanged          
  5. Avoided in renal failure

Use:

  1. Cryptococcal meningitis        
  2. Coccidia                
  3. Candida (single dose) 

4. Itraconazole

  1. Fungistatic
  2. Long acting
  3. Food increases absorption
  4. pH dependent absorption
  5. Very weak inhibitor of CYP enzymes*
  6. DOC
    1. Histoplasmosis              
    2. Blastomycosis              
    3. Sporothrix

Side effect- Hypokalemia

*Saquinavir is even weaker than itraconazole as an enzyme inhibitor

 

5. Griseofulvin

  1. Obtained from penicillium
  2. Inhibits mitotic spindles but does not cause metaphasic arrest
  3. Keratinophillic drug
  4. Food increases absorption
  5. Half life=24 hours
  6. Eliminated by bile
  7. Absorption reduced by phenobarbitone
  8. Griseofulfin reduces absorption of warfarn (?bleeding/clotting)
  9. DOC:
    1. Dermatophytosis
    2. Past DOC onychomysosis

Side effects

  1. Headache
  2. Dilsulfiram like reaction

C/I

Avoided in acute intermittent porphyria

 

6. Terbinafine

  1. Fungicidal drug
  2. Long acting
  3. Blocks synthesis of squalene epoxide
  4. This causes squalene accumulation---kills fungi
  5. DOC
     
    i. Onycomycosis

Weak antifungal drugs

  1. Tolnaftate            
  2. Cyclopirax            
  3. Olamine oleate      
  4. Clotriamazole 1%
  5. Saliylic acid          
  6. Benzoic acid          
  7. Natamycin            
  8. Netilmycin





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