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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 |