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10 Cards in this Set

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Amphotericin B

Binds ERGOSTEROL and Forms PORES -> allows leakage of electrolytes.




Use: Serious, SYSTEMIC mycoses.


Cryptococcal meningitis (w,w/o Flucytosine).


Blastomyces, Coccidioides, Histoplasma, Candida, Mucor.




Supplement K/Mg -> altered renal tubule permeability.




Toxicity: Fever/Chills, Hypotension, NEPHROTOXICITY (hydrate), IV Phlebitis, arrhythmias.

Nystatin

Same mechanism as Amphotericin B -> binds ERGOSTEROL to form PORES and cause leakage of electrolytes.




Use: Swish and swallow for oral candidiasis.


Topical for diaper rash or vaginal candidiasis.

Fluconazole, Ketoconazole, Clotrimazole, Miconazole, Itraconazole, Voriconazole

Inhibit fungal ERGOSTEROL SYNTHESIS (by inhibiting CYP450 enzyme that converts lanosterol to ergosterol).




Use: Localized, less serious mycoses.




Fluconazole -> chronic suppression of cryptococcal meningitis in AIDS pts and ALL candidal infections.




Itraconazole for Blastomyces, Coccidioides, Histoplasma.




Clomitrazole/Miconazole for topical fungal infections.




Toxicity: INHIBITS TESTOSTERONE SYNTHESIS (Ketoconazole causes Gynecomastia), Hepatic dysfunction (CYP450 inhibition).

Flucytosine

Inhibits DNA/RNA biosynthesis by conversion to 5-FU by CYTOSINE DEAMINASE.




Use: SYSTEMIC Fungal infections (esp cryptococcal meningitis) in COMBINATION with Amphotericin B.




Toxicity: BM Suppression

Capsofungin, Micafungin, Anidulafungin

Echinocandins that inhibit B-glucan Synthesis -> inhibit cell wall synthesis.




Use: INVASIVE Aspergillosis, Candida




Toxicity: GI upset, FLUSHING (HISTAMINE release)

Terbinafine

Inhibits squalene Epoxidase (required to convert Squalene into Ergosterol).




Use: DERMATOPHYTES (esp ONYCHOMYCOSIS -> fungal infection of finger/toe nails).




Toxicity: GI upset, headaches, hepatotoxicity, Taste disturbance

Griseofulvin

Interferes with microtubule function -> disrupts mitosis.


Deposits in keratin-containing tissues (NAILS).




Use: oral treatment of superficial infections, inhibits growth of DERMATOPHYTES (tinea, ringworm).




Toxicity: teratogen, carcinogenic, confusion, headaches.




Induces CYP450 -> increased warfarin meatbolism.

Antiprotozoan Therapy

Pyrimethamine (inhibit DHFR) + Sulfadiazine
-> toxoplasmosis.




Suramin or Melarsoprol -> Trypanosoma Brucei.




Nitrofurtimox -> T Cruzi (Chagas)




Sodium Stibogluconate -> Leishmaniasis.

Chloroquine


blocks detoxification of Heme into Hemozoin.

Heme accumulates -> toxic to plasmodia.




Use: treatment of plasmodial species EXCEPT P Falciparum.


Treat P Falciparum with artemether/lumefantrine or atovaquone/proguanil.


For life-threatening Malaria, use QUINIDINE or Artesunate.




Toxicity: Retinopathy, PRURITIS (esp in dark-skinned pts).




Resistance: membrane pump that decreases intracellular concentration of drug.

Antihelminthic Therapy

Mebendazole, Pyrantel Pamoate, Ivermectin, Diethylcarbamazine, Praziquantel -> all immobilize helminths.




Use PRAZIQUANTEL against flukes (trematodes) -> SCHISTOSOMA.