Term
|
Definition
| Atovaquone interferes with mitochondrial electron transport and ATP and pyrimidine biosynthesis. Proguanil (prodrug) inhibits dihydrofolate reductase-thymidylate synthetase (folic acid synthesis). |
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Term
|
Definition
| Releases free radicals which attack the cell membrane and inhibits parasite heme detoxification |
|
|
Term
| quinine/tetracycline or doxycycline |
|
Definition
| Unknown, may increase vesicle pH and interfere with macromolecular transport. Not effective against exoerythrocytic forms of the parasite |
|
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Term
|
Definition
Unknown
Does not eliminate the exoerythrocytic (intrahepatic) stages. |
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Term
|
Definition
| May prevent organism from converting heme to nontoxic metabolites where the build up of heme is then toxic. Not effective against exoerythrocytic forms of the parasite (major organism resistance for P. falciparum) |
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Term
|
Definition
| Unknown, may interfere with plasmodium DNA. Only effective against P. vivax liver forms preventing relapse |
|
|
Term
| metronidazole (tinidazole) |
|
Definition
| Activated in anaerobic cells causing DNA breakage and loss of structure. Tinidazole has a longer half life with more convenient dosing |
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Term
|
Definition
| Unknown –may inhibit protein synthesis (luminal only) |
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Term
|
Definition
| Aminoglycoside inhibiting protein synthesis |
|
|
Term
|
Definition
| Unknown mechanism but may involve zinc chelation and metabolism |
|
|
Term
| amphotericin B (liposomal) |
|
Definition
| Binds to sterols and disrupts membranes |
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Term
|
Definition
| Unknown—Metal ion Sb+5 to Sb+3 in cell and compromises cellular function |
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|
Term
| miltefosine (not available in US) |
|
Definition
| Unknown-- synthetic ether phospholipid analog which may stimulate T-cell activation |
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Term
|
Definition
| interference with anaerobic energy metabolism. |
|
|
Term
| furazolidone (not available in US) |
|
Definition
| Inhibits Kreb cycle enzymes |
|
|
Term
|
Definition
|
|
Term
| benznidazole (not available in US) |
|
Definition
| Unknown, may interfere with the synthesis of macromolecules |
|
|
Term
| pentamidine (early stage T.b.g) |
|
Definition
| Interferes with DNA and RNA |
|
|
Term
| suramin (early stage T.b.g & T.b.r*) |
|
Definition
|
|
Term
| melarsoprol (late stage T.b.g & T.b.r*) |
|
Definition
| Combination drug -- melarsen oxide (arsenic compound) and dimercaprol (reduces toxicity), easily penetrates parasite membranes and inactivates enzymes sulfhydryl groups |
|
|
Term
| eflornithine (late stage T.b.g) |
|
Definition
| Inhibits ornithine decarboxylase and cell division |
|
|
Term
| pyrimethamine plus sulfadiazine |
|
Definition
| dihydropteroate synthase blocking folic acid synth. |
|
|
Term
|
Definition
| Readily absorbed by worms and increases permeability of membrane to calcium resulting in paralysis and detachment |
|
|
Term
niclosamide
(not available in US) |
|
Definition
| Kills only adult worms (not eggs) possibly by inhibiting oxidative phosphorylation or stimulation of ATPase activity |
|
|
Term
mebendazole
(benzimidazole) |
|
Definition
| Selectively damages cytoplasmic microtubules preventing glucose uptake and disrupts secretory substances causing cell autolysis (luminal only) |
|
|
Term
albendazole
(benzimidazole) |
|
Definition
| Inhibits polymerization of tubulin and the microtubule-dependent uptake of glucose by binding free β-tubulin by susceptible intestinal worms |
|
|
Term
|
Definition
| A depolarizing neuromuscular blocking agent causing paralysis of worms |
|
|
Term
|
Definition
| Selectively opens glutamate gated chloride channels in parasites and disrupts nerves and muscles resulting in hyperpolarization, paralysis |
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Term
|
Definition
| displaces microfilariae from tissues increasing their susceptibility to the host immune system |
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