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25 Cards in this Set
- Front
- Back
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major pathogen for malaria
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Plasmodium falciparum
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Stages of Malaria
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1st => liver (exoerythrocytic)- no symptoms
2nd => 1-2 weeks - forms appear in blood - infected RBCs Parasites consume heme and destroy RBCs |
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Drugs that for the treatment/ prophylaxis of Malaria
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Chloroquine, Quinine, Mefloquine, Artemisinin
Primaquine, Atovaquone Doxycline, Tetracycline, Clindamycin, Sulfadoxine-pyrimethamine, proguanil |
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Inhibitors of heme metabolism in malaria
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Chloroquine
quinine mefloquine Artemisinin |
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Chloroquine
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Concentrated 100-fold in PARASITIZED RBCs
binds to ferriprotoporphyrin IX => prevents detoxification Therapy/Prophylactic - malaria Problem: Resistance |
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Quinine
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plant alkaloid
probably intercalates into DNA Treatment ONLY - malaria |
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Mefloquine
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quinoline compound
ADR: psychiatric manifestations Treatment ONLY - malaria |
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Artemisinin
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forms free radical compounds, can alkylate many compounds including heme
ADR: potential neurotoxicity and cardiotoxicity Therapy ONLY- malaria To protect its effectiveness: do NOT use alone (use in FIXED combinations) |
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Inhibitors of electron transport - malaria
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Primaquine
Atovaquone |
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Primaquine
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attacks at liver stage - only use of this drug
Problem: innate resistance and individuals with G6PD deficiency (massive, fatal hemolysis) malaria |
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Atovaquone
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Electron transport shuttle inhibitor
therapy & prophylaxis resistance arises quickly |
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Inhibitors of translation and folate metabolisms
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doxycycline, tetracycline, clindomycin
sulfadoxine-pyrimethamine proguanil |
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Doxycycline
tetracycline clindamycin |
tetracyclines
clindamycin => inhibitor of protein synthesis |
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Sulfadoxine- pyrimethamine
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inhibitor of DIHYROPTEROATE pathway & FOLATE REDUCTASE pathway
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Proguanil
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pyrimidine derivative
acts on liver stage |
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metronidazole (Flagyl)
related drugs: nitazoxanide & tinidazole |
inactive until reduced
most effective against tissue trophozoites AE: GI discomfort, metallic taste, do NOT drink EtOH w/ this med => causes flushing and increased BP Anti-protozoal (E. Histolytica) |
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African Sleeping Sickness treatments
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Pentamidine
Suramin Melarsoprol |
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Pentamidine
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Used in early stages of African Sleeping sickness (before CNS symptoms)
Inhibits DNA, RNA, protein, phospholipid synthesis |
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Suramin
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Used in early stage of African Sleeping sickness (before CNS)
inhibits many enzymes (MOA unknown) |
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Melarsoprol
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Used in LATE stages of African Sleeping sickness (CNS involvement)
OLD drug (1916) aresenical => arsenic inhibits trypanosome pyruvate kinase Problem: corrosive to plastic- bad for IV admin. |
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Anti- Helminth drugs
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Ivermectin
"Bendazoles"- Albendazole, Mebendazole, Thiabendazole Praziquantel Deithylacarbamazine (DEC) |
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Ivermectin
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Anti-helminth
semi-synthetic lactone treat: onchocerciasis, riverblindness, and suppress microfilariae Does not cross BBB Disadvantage: does not kill adult worms, must take 1-2 x year |
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Albendazole
Mebendazole Thiabendazole |
Anti-Helminth
treats: tapeworm in humans and in pets MOA: binds to beta-tubulin & inhibits polymerization. Disrupt motility & DNA replication |
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Praziquantel
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Anti-Helminth
Treat: tapeworm and trematodes (liver flukes & schistosomes) MOA: open Ca+ channels => paralysis. Also inhibits adenine uptake (worms can't make their own) ADR: HA, GI |
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Diethylacarbamazine (DEC)
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Anti- Helminth
used for: lymphatic filariasis caused by Wuchereria bancrofti & Brugia Malayi MOA: inhibit acrachidonic acid metabolism in filarial microfilaria Advantage: Kills ADULT worms Disadvantage: kills adult warms=> inflam reaction to rease of warm antigen (Fatal) |
