- Oral Suspension: 100mg/ml
- Tablets: 200mg
MOA: Ketoconazole operates through at least two mechanisms of action.
- First, block both testicular and adrenal androgen biosynthesis, leading to a reduction in circulating testosterone levels.
- It produces this effect through inhibition of 17α-hydroxylase and 17,20-lyase, which are involved in the synthesis and degradation of steroids, including the precursors of testosterone.
- Due to its efficacy at reducing systemic androgen levels, ketoconazole has been used with some success as a treatment for androgen-dependent prostate cancer.
- Second, ketoconazole is an androgen receptor antagonist, competing with androgens such as testosterone and dihydrotestosterone (DHT) for binding to the androgen receptor.
Uses and Considerations:
- For infections by Candida spp.
- Blacstomycosis, and others Treatment could last 1-6 months for systemic infections.
- Take with food to avoid GI discomfort. Pregnancy category: C; PB: 95%; t 1/2 : 2-8h
- Systemic Candidiasis,
- Chronic mucocandidiasis,
- Oral candidiasis,
- Chromomycosis and
- Medical adrenalectomy
- Pityriasis versicolor
- Severe cutaneous dermatophyte infections resistant to therapy with topical or oral griseofulvin
- Contraindicated in patients hypersensitive to drug
- CNS: headache, nervousness, dizziness, somnolence, suicidal tendencies, severe depression
- ENT: photophobia
- GI: nausea, vomiting, abdominal pain, diarrhea
- GU: Impotence
- HEMATOLOGIC: thrombocytopenia, haemolytic anemia, leukopenia
- HEPATIC: fatal hepatoxicity
- METABOLIC: hyperlipidemia
- SKIN: pruritus
- Potent inhibitor of cytochrome P450 3A4
- Rifampin and phenytoin decrease ketoconazole levels
- Decreases efficacy of testosterone
- Ketoconazole increases cyclosporine, warfarin, astemizole, corticosteroid, and theophylline levels
- Many of these drug interactions are severe
- Drugs that increase gastric pH will decrease blood levels of ketoconazole Antacids, omeprazole, H2 blockers
- Antihistamines associated with an increased risk of cardiac arrhythmias in patients receiving erythromycin or ketoconazole include Terfenadine
- Ketoconazole would treat both dermatophytes and candidal infection
- Ketoconazole is Cyt. p450 inhibitor
- Ketoconazole are effective in the treatment of pityriasis versicolor
- Ketoconazole is used for medical adrenalectomy
- Ketoconazole decreases efficacy of testosterone
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