KETOCONAZOLE

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KETOCONAZOLE

Ketoconazole 3

1.       TYPE OF DRUG – KETOCONAZOLE
Ketoconazole is a synthetic imidazole antifungal drug used primarily to treat fungal infections.

 

2.       INDICATIONS (USE) – KETOCONAZOLE
For the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.

 

3.       MECHANISM OF ACTION (MOA) – KETOCONAZOLE
Inhibition of 14-a-demethlyase blocks formation of ergosterol and leads to the buildup of toxic methylated 14-a-sterols and depletes ergosterol in the cell membrane.

 

4.       ROUTES OF ADMINISTRATION- KETOCONAZOLE
Cream, topical:  2% (15g, 30g, 60g)

Shampoo, topical: 1% (6mL, 120 mL, 210mL)

Tablet: 200 mg

 

5.       ONSET OF EFFECT OR ACTION- KETOCONAZOLE
The drug begins to work within a few hours; full beneficial effect may take several days.

 

6.      DOSAGE (DOSING INFORMATION) – KETOCONAZOLE
Mucosal infections/cutaneous infection:  200 mg/day for 2 weeks

Extensive mucosal infection/recalcitrant dermatophyte infections:  400 mg/day for 4 weeks

Systemic mycoses:  400 mg/day for 6-12 months

Shampoo:  Apply twice weekly for 4 weeks with at least 3 days between each shampoo.

Topical:  Rub gently into the affected area once daily to twice daily.

 

7.       HALF LIFE (DURATION OF ACTION) – KETOCONAZOLE
2 hours

 

8.       ADVERSE EFFECTS OR SIDE EFFECTS – KETOCONAZOLE
  • Gastrointestinal: nausea, vomiting, abdominal pain, anorexia
  • Skin and appendages  pruritus, rash, potentially exfoliative
  • Liver and biliary system:  Elevation of hepatic transaminases (<10%), hepatitis
  • Immunologic:  anaphylaxis
  • Endocrine: adrenal insufficiency, decreased testosterone synthesis, menstrual irregularities
  • Special senses:  photophobia
  • Nervous System: headache

 

9.       CONTRAINDICATIONS – KETOCONAZOLE
Contraindications: hypersensitivity to ketoconazole; CNS fungal infections (due to poor CNS penetration); coadministration with ergot derivatives, astemizole, or cisapride is contraindicated due to risk of potentially fatal cardiac arrhythmias

 

10.   DRUG INTERACTIONS – KETOCONAZOLE
Ketoconazole is a potent inhibitor of the cytochrome P450 3A4 isoenzyme system.  Caution should be exercised and monitoring is suggested when concomitantly administering ketoconazole with drugs that have narrow therapeutic windows and are substrates of the CYP3A4 substrates.

 

11.    EXCRETION- KETOCONAZOLE
More than 50% of a dose is excreted in feces within 4 days; drug and metabolites are secreted in bile. About 13% is excreted unchanged in urine. It probably appears in breast milk. Half-life is biphasic, initially 2 hours, with a terminal half-life of 8 hours.

 

Ketoconazole 4

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