Antifungal Drugs antimycotic drugs

These drugs are used to treat two types of fungal infections

1. Superficial fungal infections of skin or mucous membrane.

2. Systemic fungal infections of the lung or central nervous system.

The conditions may be mild such as tinea pedis (ahtlete's foot), or severe as in pulmonary conditions or meningitis.

Fungi, such as Candida spp. (yeast), are normal flora of mouth, skin, intestine, and vagina. Candidiasis might be an opportunistic infection when the defense mechanisms are impaired. Antibiotics, oral contraceptives, and immunosuppressives may alter the body's defense mechanisms. Infections can be mild (vaginal yeast infection) or severe (systemic fungal infection). There are four groups of anti-fungal medications. They are:

1. Polyenes, including amphotericin B and nystatin.

2. Imidazoles which include ketoconazole, miconazole, and clotrimazole.

3. Antimetabolic antifungal flucytosine.

4. Antiprotozoal agents.

Polyenes such as amphotericin B are the drug of choice for treating severe systemic infections. It is effective against numerous diseases including histo-plasmosis, cryptococcosis, coccidioidomycosis, aspergillosis, blastomycosis, and candidiasis (system infection), however, it is very toxic. It is not absorbed from the GI tract so it cannot be given by mouth.

It is usually prescribed as Amphotericin B (Fungizone). A test dose is given IV: 0.25-1.0 mg in 20 mL of D5W infused over 20-30 min; IV: 0.25-1.0 mg/kg/d in D5W or 1.5 mg/kg qod; max; 1.5 mg/kg/d. The drug is pregnancy category: B; PB: 95%; 24 h.

Side effects and adverse reactions include flushing, fever, chills, nausea, vomiting, hypotension, paresthesias, and thrombophlebitis. It is highly toxic, causes nephrotoxicity and electrolyte imbalance, especially hypokalemia (low potassium) and hypomagnesemia (low serum magnesium). Urinary output, BUN, and serum creatinine levels should be closely monitored.

Nystatin (Mycostatin) can be given orally or topically to treat candidal infection. It is available in suspensions, cream, ointment, and vaginal tablets. It is poorly absorbed via the GI tract but the oral tablet form is used for intestinal candidiasis. It is more commonly used as an oral suspension for candidal infection in the mouth as a swish and swallow.

Side effects include anorexia, nausea, vomiting, diarrhea (large doses), stomach cramps, rash; vaginal: rash, burning sensation. There are no reported adverse reactions.

It is used topically and PO at doses of 500,000-1,000,000 U tid or q8h. This drug has a Pregnancy category: C; PB: UK; t/2: UK.

The Imidazole group is effective against candidiasis (superficial and systemic), coccidioidomycosis, cryptococcosis, histoplasmosis, and paracoccidioidomycosis.

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