Exam 4- 3 Antifungal Drugs Flashcards
Antifungal Drugs
Drugs used to treat infections caused by fungi
- systemic
- topical
Fungi
Very large and diverse group of microorganisms
- broken down into yeasts and molds
- fungal infections also known as mycoses
- some fungi are part of the normal flora of the skin, mouth, intestines, vagina
Yeasts
Single cell fungi -reproduced by budding -can be used for baking alcoholic beverages
Molds
- multicellular
* characterized by long, branching filaments called hyphae
Mycotic Infections
Four General Types: -Cutaneous -Subcutaneous -Superficial -Systemic can be life threatening usually occur in immunocompromised host
Mycotic Infections:
Candida albicans
Vaginal candidiasis
Candida albicans
- Due to antibiotic therapy, antineoplastics or immuniosuppressants (corticosteroids)
- May result in overgrowth and systemic infections
- Growth in the mouth is called thrush or oral candidiasis
- Common is newborn infants and immunocompromised patients
Vaginal candidiasis
- Yeast infection
* Pregnancy, women with diabetes mellitus, women taking antibiotics
Antifungal Drugs
Systemic
Topical
Antifungal Drugs: Systemic
-amphotericin B, caspofungin, fluconazole, ketoconazole
Antifungal Drugs: Topical
*clotrimazole, miconazole, nystatin
Antifungal Drugs: Characteristics
*Broken down into major groups based on their chemical structure:
-Polyenes: amphotericin B and nystatin
-Imidazoles:ketoconazole
-Triazoles: fluconazole, itraconazole, voriconazole
-Echinocandins: caspofungin, micafungin
-Miscellaneous
griseofulvin, flucytosine
Mechanism of Action: flucytosine
- Also known as 5-fluorocytosine (antimetabolite)
- Taken up by fungal cells and interferes with DNA synthesis
- Result: fungal cell death
Mechanism of Action: griseofulvin
- disrupts cell division
* results: inhibit fungal mitosis (reproduction)
Mechanism of Action: Polyenes: amphotericin B and nystatin
- Bind to sterols in cell membrane
- Result: fungal cell death
- Do not bind to human cell membranes or kill human cells
Mechanism of Action: Imidazoles and triazoles: ketoconazole, fluconazole, itraconazole, voriconazole
- Inhibit fungal cell cytochrome P-450 enzymes, resulting in cell membrane leaking
- Lead to altered cell membrane
- Results: altered cellular metabolism and fungal cell death
Mechanism of Action: Echinocandins: caspofungin, micafungin
- Prevents the synthesis of glucans, which are essential components of fungal cell walls
- Causes fungal cell death
Indications:
- Systemic and topical fungal infections
* Drug of choice for the treatment of many severe systemic fungal infections is amphotericin B
Adverse Effects: Amphotericin B
fever chills cardiac dysrhythmias Nausea and GI upset Renal toxicity Headache Malaise Hypotension Tingling, numbness in hands and feet lowered potassium and magnesium levels
Main concerns for Amphotericin B
- Renal toxicity
* Neurotoxicity: seizures and paresthesias
Antifungal Drugs: Adverse Effects/fluconazole
- Nausea, vomiting, diarrhea, stomach pain,
- Increased liver enzymes
- Use with caution in patients with renal and liver dysfunction
Antifungal Drugs: Adverse Effects/nystatin
*Nausea, vomiting, anorexia, diarrhea, local irritation, rash
Antifungal Drugs: Contraindications
- Liver failure
- Renal failure
- Porphyria (griseofulvin)
- Drug allergy