Ketoconazole

Indications
 Oral
Fungal infections
Adult: 200 mg once daily. Increase to 400 mg once daily if clinical response is insufficient. Treatment duration: 14 days and for at least 1 wk after symptoms have cleared and cultures have become negative.
Child: ≥2 yr: 3.3-6.6 mg/kg daily as a single dose. Treatment duration: 1-2 wk for candidiasis; at least 4 wk in recalcitrnt dermatophyte infections and up to 6 mth for other systemic mycoses.
Oral
Chronic vaginal candidiasis
Adult: 400 mg once daily for 5 days.
Topical/Cutaneous
Seborrhoeic dermatitis
Adult: As 2% cream: Apply to the affected area bid for 4 wk or until clinical clearing. As 2% foam: Apply to the affected area bid for 4 wk. As 1 or 2% shampoo: Apply on the scalp twice wkly for 2-4 wk; continue for a few days until symptoms disappear. For prophylaxis: 2% shampoo is used once every 1-2 wk.
Topical/Cutaneous
Skin fungal infections
Adult: As 2% cream: Apply 1-2 times daily to cover affected and surrounding area until at least a few days after disappearance of symptoms. For treatment of pityriasis versicolor: As 2% shampoo: Apply on the skin once daily for up to 5 days. For prophylaxis: 2% shampoo is used once daily for a max of 3 days before exposure to sunshine.
Topical/Cutaneous
Pityriasis versicolor
Adult: As 2% cream: Apply 1-2 times daily to cover affected and surrounding area until at least a few days after disappearance of symptoms. For treatment of pityriasis versicolor: As 2% shampoo: Apply on the skin once daily for up to 5 days. For prophylaxis: 2% shampoo is used once daily for a max of 3 days before exposure to sunshine.
Contraindications
 Hypersensitivity; preexisting liver disease, porphyria. Concurrent use with cisapride, terfenadine or astemizole.
Warnings / Precautions
 Hepatic impairment; monitor liver function regularly. Pregnancy, lactation. Predisposition to adrenocortical insufficiency. Discontinue treatment if there is persistent or worsening of liver enzyme elevation.
Adverse Reactions
 GI disturbances e.g. nausea and vomiting; rash, dermatitis, burning sensation, pruritus; headache, dizziness, somnolence, fever and chills; thrombocytopenia; gynaecomastia, impotence; raised intracranial pressure; photophobia; transient elevations in LFTs.
Potentially Fatal: Hepatotoxicity.
Drug Interactions
 Reduced absorption with antimuscarinics, antacids, H2-blockers, PPIs, sucralfate. Reduced plasma concentrations with rifampicin, isoniazid, efavirenz, nevirapine or phenytoin. May reduce concentrations of isoniazid and rifampicin. May increase plasma concentrations of CYP3A4 substrates such as benzodiazepines, mirtazapine, nefazodone, tacrolimus, oral anticoagulants, rosiglitazone, sertindole, sildenafil. Disulfiram-like reaction with alcohol. May reduce efficacy of oral contraceptives. Avoid concurrent use with clopidogrel.
Potentially Fatal: Increased risk of cardiac arrhythmias with astemizole, cisapride, pimozide, quinidine or nilotinib. May reduce metabolism of conviptan; avoid concurrent usage. Increased risk of dofetilide toxicity when used together.
See Below for More ketoconazole Drug Interactions
Mechanism of Actions
 Ketoconazole interferes with biosynthesis of triglycerides and phopholipids by blocking fungal cytochrome P450, thus altering cell membrane permeability in susceptible fungi. It also inhibits other fungal enzymes resulting in the accumulation of toxic concentrations of hydrogen peroxide.
Absorption: Variably absorbed from the GIT (oral), may be increased with decreasing gastric pH. Minimally absorbed systemically (topical or vaginal). Peak plasma concentrations after 2 hr (oral).
Distribution: Widely distributed, CSF (poor penetration); enters breast milk. Protein-binding: >90%, mainly to albumin.
Metabolism: Hepatic; converted to inactive metabolites.
Excretion: Via faeces (as metabolites and unchanged drug), via urine; 2 hr (initial half-life), 8 hr (terminal half-life).
Administration
 Should be taken with food.
Storage Conditions
 Oral: Store at 15-25°C (59-77°F). Topical/Cutaneous: Store below 25°C (77°F).
ATC Classification
 D01AC08 - ketoconazole ; Belongs to the class of imidazole and triazole derivatives. Used in the topical treatment of fungal infection.
G01AF11 - ketoconazole ; Belongs to the class of imidazole derivative antiinfectives. Used in the treatment of gynecological infections.
J02AB02 - ketoconazole ; Belongs to the class of imidazole derivatives. Used in the systemic treatment of mycotic infections.
Storage
 Oral: Store at 15-25°C (59-77°F). Topical/Cutaneous: Store below 25°C (77°F).
Available As
  • Ketoconazole 1% w/v
  • Ketoconazole 12% w/v
  • Ketoconazole 150 mg
  • Ketoconazole 2 mg
  • Ketoconazole 2%
  • Ketoconazole 2% w/v
  • Ketoconazole 2% w/w
  • Ketoconazole 20 mg
  • Ketoconazole 200 mg

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