Ketoconazole
Mechanism :
Ketoconazole impairs the synthesis of ergosterol, which is a vital component of fungal cell membranes.
Indication :
- Patients of systemic fungal infections who have failed other therapy or are intolerant.
- Histoplasmosis
- Blastomycosis
- Paracoccidioidomycosis
- Coccidioidomycosis
- Chromomycosis
Contraindications :
Ketoconazole is contraindicated in patients who have shown hypersensitivity to the drug or excipients of the formulation. Keep out of eyes. It is contraindicated in children below 2 years of age.
Dosing :
Under years: Safety and efficacy not established.
Above 2 years:
3.3-6.6 mg/kg/day given orally.
Adverse Effect :
Nausea and vomiting, abdominal pain, pruritus, alopecia, headache, hyperlipidemia, dizziness, diarrhea, impotence, thrombocytopenia erythema multiforme, gynecomastia, hepatotoxicity, xeroderma, fever and chills, somnolence, depression, bulging fontanelles, jaundice, dysgeusia, decreased platelet count, dyspepsia, photophobia, hemolytic anemia, leukopenia, orthostatic hypotension.
Interaction :
Terfenadine: Has led to elevated plasma concentrations of terfenadine, resulting in rare instances of life-threatening cardiac dysrhythmias.
Astemizole: Inhibits the metabolism of astemizole, resulting in elevated plasma concentrations of astemizole which may prolong QT intervals.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Not dialysed. Dose as in normal renal function |
| HD | Not dialysed. Dose as in normal renal function |
| HDF/High flux | Unknown dialysability. Dose as in normal renal function |
| CAV/VVHD | Unknown dialysability. Dose as in normal renal function |
Hepatic Dose :
Oral use is contraindicated in patients with acute or chronic hepatic disease. Monitor liver function weekly for one month after initiation of the treatment, then monthly for 6 months and then weekly for one month whenever the dose is increased.
ALT or AST >3 times the ULN: Discontinue the drug and do not restart.
ALT or AST < 3 times the ULN: more frequent monitoring of liver function tests and the daily dose should be decreased.
Use of shampoo or cream in patients with liver disease is not contraindicated.
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