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ANTIFUNGAL
ANTIFUNGAL, ANTIPROTOZOAN, ANTIHERLMINTHIC
Question | Answer |
---|---|
Lanesterol synthesis inhibitor | Terbinafine |
Ergosterol synthesis inhibitiors | Azoles |
Cell wall synthesis inhibitors | Echinocandins (-fungin) |
Inhibit formation of Membrane Pores | Polyenes 1. Amphotericin B 2. Nystatin |
Nucleid acid inhibitors | 5-Flucytosine |
Amphotericin B; MOA | Binds ergosterol; forms membrane pores that allow leakage of electrolytes. |
Amphotericin B; CLINICAL USE | 1. Systemic mycoses. 2. Cryptococcal meningitis (with/without flucytosine) 3. Blastomyces, Coccidioides, Histoplasma, Candida, Mucor. 4. lntrathecally for fungal meningitis. Supplement K and Mg because of altered renal tubule permeability. |
Amphotericin B; TOXICITY ("amphoterrible") | Fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis. |
IV phlebitis | Amphotericin B |
What reduces Amphotericin´s nephrotoxicity | Hydration |
What reduces Amphotericin´s toxicity | Liposomal amphotericin |
Nystatin; CLINICAL USE | 1. Oral: oral candidiasis (thrush) 2. Topical: diaper rash or vaginal candidiasis |
Azoles; MOA | Inhibit fungal sterol (ergosterol) synthesis, by inhibiting the P-450 enzyme that converts lanosterol to ergosterol. |
Azoles; CLINICAL USE | Local and less serious systemic mycoses. Clotrimazole and miconazole for topical fungal infections. |
Cryptococcal meningitis in AIDS patients and candidal infections of all types | Fluconazole |
Itraconazole | Blastomyces, Coccidioides, Histoplasma. |
Topical fungal infections | Clotrimazole and miconazole |
Azoles; TOXICITY | 1. Testosterone synthesis inhibition (gynecomastia, esp. with ketoconazole) 2. Liver dysfunction (inhibits cytochrome P-450). |
Inhibits DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminase. | Flucytosine |
Flucytosine; CLINICAL USE | Meningitis caused by Cryptococcus in combination with Amphotericin B |
Inhibits cell wall synthesis by inhibiting synthesis of beta-glucan. | Echinocandins (-fungin) |
Echinocandins (-fungin); CLINICAL USE | Invasive Aspergillosis, Candida |
Echinocandins (-fungin); TOXICITY | FLUSHING |
Inhibits Squalene Epoxide | Terbinafine |
Terbinafine; CLINICAL USE | Dermatophytoses (especially onychomycosis-fungal infection of finger or toe nails). |
Terbinafine; TOXICITY | GI upset, headaches, hepatotoxicity, taste disturbance. |
Taste disturbance | Terbinafine |
Monitor LFT´s | Terbinafine |
Griseofulvin; MOA | Interferes with microtubule function; disrupts mitosis. Deposits in keratin-containing tissues (e.g., nails). |
Deposits in keratin-containing tissues (e.g., nails). | Griseofulvin |
Interferes with microtubule function | Griseofulvin |
Griseofulvin; CLINICAL USE | Oral treatment of superficial infections; inhibits growth of dermatophytes (tinea, ringworm). |
Griseofulvin; TOXICITY | Teratogenic, carcinogenic, confusion, headaches, Induces P-450 and warfarin metabolism. |
Antiprotozoan therapy | 1. Pyrimethamine (toxoplasmosis), 2. Suramin and Melarsoprol (Trypanosoma brucei), 3. Nifurtimox (T cruzi), 4. Sodium Stibogluconate (leishmaniasis) |
Chloroquine; MOA | Blocks detoxification of heme into hemozoin. Heme accumulates and is toxic to plasmodia |
Chloroquine; CLINICAL USE | Plasmodial species other than P. falciparum |
P. falciparum | artemether/lumifantrine or atovaquone/proguanil. |
Life-threatening malaria | Quinidine |
Chloroquine; TOXICITY | 1. Retinopathy 2. Pruritus (especially in dark-skinned individuals) |
Pruritus (especially in dark-skinned individuals) | Chloroquine |
Antihelminthic therapy; immobilize helminths. | Mebendazole, pyrantel pamoate, ivermectin, diethylcarbamazine, praziquantel |
Against flukes (trematodes) such as Schistosoma. | Praziquantel |