Availability in Hospital Keningau
- Cap Fluconazole 50mg & 200mg
- Tab Griseofulvin 125mg
- Cap Itraconazole 100mg
- Tab Ketoconazole 200mg
- Suspension Nystatin 100 000 units/ml
Comparison of Oral Antifungals
| Antifungal | Indication (FUKKM) | Pharmacokinetics |
| Ketoconazole 200mg (B) | - Systemic Mycoses (other skin mycosis)
| - Absorption can be increased by administration with a cola beverage (requires acidic condition)
- Half life elimination is biphasic (initial 2 hours and terminal 8 hours)
|
| Fluconazole 50mg
Fluconazole 100mg (A) | - Oropharyngeal candidiasis, atrophic oral candidiasis
- Tinea Pedis, corporis, cruris, versicolor and dermal candidiasis
- Invasive candida & cryptocococcal infections (includes meningitis)
- Prevention of relapse cryptococcal meningitis in AIDS after completion of primary therapy
- Prevention of fungal infections in immunocompromised patients
| - Oral bioavailability > 90%
- The long serum half-life (approximately 24 hours) allows once-daily dosing
- Good penetration into CSF
- Absorption is not affected by the presence of food or gastric pH.
|
| Itraconazole 100mg (A/KK) | - Dermatomycosis including pityriasis versicolor
- Palmar tinea manus and plantar tinea pedis
| - Capsule bioavailability of approximately 55%
- Relatively long half-life, approaching 25 to 50 hours thus allows OD dosing
- Absorption increased by concurrent ingestion of cola or cranberry juice
|
| Voriconazole 200mg
Voriconazole 50mg (A*) | - Treatment of immunocompromised patients with progressive, possibly life-threatening infections such as invasive aspergillosis, fluconazole-resistant serious invasive candidiasis, candidiasis of the oesophagus, serious fungal infections caused by Scedosporium species and Fusarium species
- Prevention of breakthrough fungal infections in febrile high risk neutropenic patients
| - Oral biovailability >90% in adult and may vary with <12 year old
|
| Syr. Nystatin 500 000 (B) | - Prevention and treatment of candidiasis of the skin and mucous membranes
- Protection against candidas overgrowth during antimicrobial /corticosteroid therapy and as selective decontamination regimens
| - Excreted unchanged at feces
- Should be swished about the mouth and retained in the mouth for as long as possible (several minutes) before swallowing.
|
| Griseofulvin (B) | - Dermatophyte infection of the skin, scalp, hair and nails, where topical therapy has failed or inappropriate
| - Absorption is almost complete (ultramicrosize)
- Half life elimination is 9-24 hours
|
| Flucytosine 500mg (A*) | - Only for the treatment of fungal meningitis
| - Bioavailability 78%-89% (decreased in neonates
|
Spectrum of activity
Imidazole (Ketoconazole)
- Ketoconazole causes more gastrointestinal disturbances compared to other azoles.
- Has been largely replaced by other triazoles due to favourable pharmacokinetic and safety profile
- Should not be used as first-line treatment for any fungal infection.
- It should be used for the treatment of endemic mycoses (eg, histoplasmosis, blastomycosis) only when alternative antifungal therapies are not available or tolerated.
- Contraindicated in acute or chronic liver disease.
Triazole (Itraconazole, Fluconazole, Voriconazole)
- The drugs in this class offer activity against many fungal pathogens without the serious nephrotoxic effects observed with amphotericin B
- Due to its inotropic effects, itraconazole’s labeling includes a black box warning in patients with heart failure, particularly in patients receiving a total daily oral dose of 400 mg
Pyrimidine (Flucytosine)
- Flucytosine has limited clinical indication and is used primarily in combination with Amphotericin B as combination therapy for cryptococcal meningitis and selected life threatening Candida syndromes
References
- Uptodate
- https://mycology.adelaide.edu.au/docs/antifungals.pdf
- https://www.uspharmacist.com/article/the-fungus-among-us-an-antifungal-review
- Lexicomp
- FUKKM
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