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8 Cards in this Set
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quinoline derivatives
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quinine
quinidine chloroquine mefloquine amodiaquine primaquine |
MOA-concentrated in caguoles of parasites, inhibits heme polymerase in parasites.
Quinine used for severe malaria that is chloroquine resistant falciparum. Also used with clindamycin for babesiosis Toxicity-GI, cinchonism(tinnitus, headache, nausea, blurred vision), hypotension, hyperinsulinemia, myocardial depression, black water fever Chloroquine used for treatment and prophylaxis for malaria, there is widespread resistance to this drug toxicity-well tolerated, headache, dizziness, blurred vision, GI, confusion fatigue, rarely retinal damage and psoriases. Contraindicated with psoriasis, retinal disease or porphyria mefloquine used for treatment of falciparum, vivax, ovale and malariae, can be used prophylactically toxicity-dose related GI and neurophychiatric contraindicated-quinine, beta blockets, history of seizures of psychiatric disorders primaquine used for elimination of hepatic forms, radical cure for vivax and ovale, also for toxo toxicity-hemolysis in G6PD deficiency, methemoglobinemia |
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artemisinin derivatives
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used in chinese medicine as an herbal tea.
used with other active agents and not prophylaxis. only fixed dose combinations given orally, intramuscularly, IV or rectal toxicicty-GI, nausea, vomiting, increased lever enzymes, decreased reticulocytes |
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proguarnil
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MOA-inhibits plasmodial dihydrofolate reductase
kills erythrocytic forms of parasite and some activity against hepatic form well tolerated-rarely hematologic toxicity used in combination with atovaquone |
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pyrimethamine
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structurally similar to proguanil
1000 times more active against parasitic enzyme toxicicty-bone marrow suppression with daily use used with fulfonamide for chloroquine resisitant falciparum, also for PCP and toxo |
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Atovaquone
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MOA-interferes with mitochondrial electron transport
toxicicty-GI, fever, rash, headache, insomnia used-malarial with rpoquanil, babesiosis with azithromycin, pneumocystis jirovecii and toxo second line |
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Toxoplasmosis
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pyrimethamine with sulfadiazine is first line therapy, clindamycin can replace sulfadiazine
trimethoprim-sulfamethoxazole for prophylaxis dapsone + pyrimethamine/atovaquone alternatives for prophylaxis |
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Nitroimidazoles
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Metronidazole
tinidazole |
MOA-produces free radicals in cells causing cell death
absorbed orally, metabolized in liver and excreted in urine Toxicity-headache, nausea, dry mouth, metallic tase, disulfiram effect, peripheral neuropathy, neutropenia metronidale used for anaerobic and microarophilic bacterial, entamoeba histolytica, gardia, trichomonas Tinidazole better tolerated uses-metronidazole resistant trichomonas, gardia, entamoeba histolytica |
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Benzimidazoles
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albendazole
mebendazole |
MOA-binds to beta tubulin, inhibits glucose uptake causing celld eath
albendazole uses-echinococcus, neurocysticercosis, enterobius toxcicity-minimal for short term-long term-reversible hepatotoxicity Mebendazole not as well absorbed uses-enterbius toxicity-abdominal pain/diarrhea |
