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ANTIFUNGAL DRUGS
Dr. Dilip kumar singh
JR 1
Pharmacology and Therapeutics
KGMU Lucknow
FUNGAL INFECTION
classification:
• Superficial infections
Skin and mucous membrane
Incidence rate is high
e.g. Ringworm (tinea)
Systemic infections:
opportunistic infections
Fatality rate is high
e.g. Candida albicans, Histoplasma
Antifungal agents classification
• Based on structure:
1) Antibiotics:
Polyenes: Amphotericin B, Nystatin
Heterocyclic Benzofuran: Griseofulvin
Echinocandins: Caspofungin
2) Azole Topical- Clotrimazole, Miconazole
a) Imidazoles
Systemic- Ketoconazole
Antifungal agents classification……
B. Triazoles: Fluconazole, Itraconazole, Voriconazole
3) Allylamine: Terbinafine
4) Antimetabolite: Flucytosine
5) Other Topical: Benzoic acid, Quiniodochlor,
Sod.thiosulfate
Antifungal spectrum
• Broadest spectrum antifungal
• Fungicidal at high and fungistatic at low concentration
• Active against most of Fungi-
e.g. Candida albicans, Histoplasma capsulatum
Aspergillus, Cryptococcus neoformans…
• AMB also active against various species of Leishmania
Adverse effect
• Toxicity of Amphotericin-B is high
Acute reaction:
Occurs with each infusion these are-
 Chills , fever , body aches, ,nausea, vomiting
Dyspnoea (lasting for 2 to 5 hrs)
Inj. Hydrocortisone 0.6 mg/kg with infusion may reduce the
intensity of reaction
Adverse effect…..
Long term toxicity:
• Nephrotoxicity- most important, dose related
-Azotemia, ↓ GFR, acidosis, hypokalaemia
Anaemia, inability to conc. urine
• CNS Toxicity- Occurs only on intrathecal injection
Headache, vomiting, nerve palsies etc.
• Hepatotoxicity some time
Pharmacokinetics
• Irregular oral absorption due to very low water solubility
• ↑ by taking with fat and microfine particle
• Get concentrated in keratinized tissue
• Metabolised in liver
• Excreted in urine
• Plasma half life 24 hr
AZOLES
• Synthetic antifungal ,Broad spectrum
• Most commonly used
• Both fungistatic and Fungicidal depending on conc.
• Classified in two groups
• IMIDAZOLE TRIAZOLE
2 Nitrogen in structure 3 Nitrogen in structure
• Both have same mechanisms of action
THANK YOU

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Antifungal drugs

  • 1. ANTIFUNGAL DRUGS Dr. Dilip kumar singh JR 1 Pharmacology and Therapeutics KGMU Lucknow
  • 2.
  • 3. FUNGAL INFECTION classification: • Superficial infections Skin and mucous membrane Incidence rate is high e.g. Ringworm (tinea) Systemic infections: opportunistic infections Fatality rate is high e.g. Candida albicans, Histoplasma
  • 4. Antifungal agents classification • Based on structure: 1) Antibiotics: Polyenes: Amphotericin B, Nystatin Heterocyclic Benzofuran: Griseofulvin Echinocandins: Caspofungin 2) Azole Topical- Clotrimazole, Miconazole a) Imidazoles Systemic- Ketoconazole
  • 5. Antifungal agents classification…… B. Triazoles: Fluconazole, Itraconazole, Voriconazole 3) Allylamine: Terbinafine 4) Antimetabolite: Flucytosine 5) Other Topical: Benzoic acid, Quiniodochlor, Sod.thiosulfate
  • 6.
  • 7.
  • 8.
  • 9.
  • 10.
  • 11.
  • 12.
  • 13.
  • 14. Antifungal spectrum • Broadest spectrum antifungal • Fungicidal at high and fungistatic at low concentration • Active against most of Fungi- e.g. Candida albicans, Histoplasma capsulatum Aspergillus, Cryptococcus neoformans… • AMB also active against various species of Leishmania
  • 15.
  • 16. Adverse effect • Toxicity of Amphotericin-B is high Acute reaction: Occurs with each infusion these are-  Chills , fever , body aches, ,nausea, vomiting Dyspnoea (lasting for 2 to 5 hrs) Inj. Hydrocortisone 0.6 mg/kg with infusion may reduce the intensity of reaction
  • 17. Adverse effect….. Long term toxicity: • Nephrotoxicity- most important, dose related -Azotemia, ↓ GFR, acidosis, hypokalaemia Anaemia, inability to conc. urine • CNS Toxicity- Occurs only on intrathecal injection Headache, vomiting, nerve palsies etc. • Hepatotoxicity some time
  • 18.
  • 19.
  • 20. Pharmacokinetics • Irregular oral absorption due to very low water solubility • ↑ by taking with fat and microfine particle • Get concentrated in keratinized tissue • Metabolised in liver • Excreted in urine • Plasma half life 24 hr
  • 21.
  • 22.
  • 23.
  • 24.
  • 25. AZOLES • Synthetic antifungal ,Broad spectrum • Most commonly used • Both fungistatic and Fungicidal depending on conc. • Classified in two groups • IMIDAZOLE TRIAZOLE 2 Nitrogen in structure 3 Nitrogen in structure • Both have same mechanisms of action
  • 26.
  • 27.
  • 28.
  • 29.
  • 30.
  • 31.
  • 32.
  • 33.
  • 34.
  • 35.
  • 36.
  • 37.
  • 38.
  • 39.
  • 40.
  • 41.