Antifungal Drugs Flashcards
Mechanism of actions of drugs:
Cell membrane permeability Cell membrane synthesis Direct tissue target Nucleic acid analogue Cell wall synthesis
Primary antifungal drugs
For severe cases of mycoses
Derived: Streptomyces nodusos
Amphotericin B (AMB)
Admin.of AMB
Intravenous (IV)
Therapeutic use of AMB
Systemic mycoses Systemic candidiasis Cryprococcal meningitis Invasive aspergillosis Sporothricosis Mucormycosis
Adverse effect of AMB
Phlebitis *Nephrotoxic (dose dependent) Azotemia (increase bun and crea) Fever Anemia
First antibiotic against fungi
Nystatin
Admin.of nystatin
Oral
Topical
Suppository
Therapeutic used of Nystatin (Candidiasis)
Vaginal (suppository)
Oral
Esopangeal
Skin
Example of drugs under cell membrane permeability
AMB
Nystatin
Example of Azole drugs
Imidazole
Triazole
Inhibit the action of
CYTOCHROME P450 DEPENDENT-14-alpha-DEMETHYLASE
Azole dugs ( imidazole, triazole )
Prevent oxidation of squalene epoxidase
Allylamines drugs: Naftifine Terbinafine Amorilfine Butenafine
Under imidazole drug w/c is most toxic
Ketoconazole
Therapeutic use of ketoconazole
Chronic mucocutaneous candidiasis
Adverse effect of ketoconazole
Hepatotoxic
Male: dec. Testosterone component
Enlargement of breast (gynecomastia)
Therapeutic use of miconazole and clotrimazole
Tinea versicolor
Dermatophytosis
Cutaneous candidiasis
New version of drug that is less toxic and none more effective
Triazole
Admin.of fluconazole
Oral
Therapeutic use of fluconazole
Candidiasis (most commom opportunistic yeast infection)
Cryptococcal dx
Alternative of AMB
Itraconazole
Admin.of itraconazole
Oral
Therapeutoc use of itraconazole
Systemic fungal infection
- blastomycosis
- histoplasmosis
Subcutaneous
- Sporothricosis
- Chromomycosis
Invasive aspergillosis
Candidiasis
Admin.of Voriconazole (Vori) / Dosaconazole (Dosa)
Oral
Topical
Therapeutic use of voriconazole/ dosaconazole
Candidiasis
Aspergillosis
Admin.and therapeutic use of Naftifine
Oral
Dermatophytosis
Alternative drug for griseofulvin
Dermatophytosis (nail infection)
Terbinafine
Adverse effect of terbinafine
Gastrointestinal irritation
Griseofulvin derived from:
Penicillum griseofulvin
Therapuetic use and adverse effect of griseofulvin:
TU:
Dermatophytosis
AE:
Leukopenia
Neutripenia
Drug under direct tissue target
Griseofulvin
Drug under nucleic acid analogue
Flucytosine (5-FC)
Admin. of flucytosine
Oral / IV together with AMB
Therepeutic use of flucytosine
Cryptococcal meningitis
Candidiasis
Adverse effect of flucytosine
Leukopenia Thrombocytopenia Aplastic anemia Pancytopenia Increase liver enzyme
Drigs under cell wall synthesis
Caspofungin, Polyoxin D
Anidulafungin, Micafungin
Nikkomycin Z
Inhibit glucan synthesis
For candidiasis, aspergillosis
Anidulafungin, micafungin
Inhibit chitin synthesis
Nikkomycin Z
Factors to consider in the selection of drugs:
- Threat of morbidity/mortality pose by the infection
- Immune status of the px
- Toxicity of the drugs
- Probable activity of the antifungal agent agents the fungus