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31 Cards in this Set
- Front
- Back
Dihydropteroate synthase is used by, and what is important about this? |
Sporozoans (e.g., Plasmodium, Toxoplasma, Eimeria species) and other bacteria. Bacteria and sporozoans lack the ability to obtain exogenous folate. Sulfonamides are antimetabolities of para-aminobenzoic acid (PABA, which is a dihydrofolic acid precursor) and competitively inhibits dihydropteroate synthase.
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What drug can block further sequential blockade of folic acid production?
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Trimethoprim (inhibits dihydrofolate reductase)
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Who uses pyruvate-ferredoxin oxidoreductase, and what is it used for?
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Certain anaerobic protozoans that lack mitochondria, posses this enzyme to generate acetyl-CoA via an electron transport.
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What is metronidazole's affect on pyruvate ferredoxin oxidoreductase?
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Pyruvate-ferredoxin oxidoreductase transfers electorns form pyruvate to a nitro group to nitroimidazoles (e.g., metronidazole) forming cytotoxic products that inhibit growth by binding to the parasite's proteins and DNA.
This enzyme has no counterpart in humans. |
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What does trypanothione do? And what drug acts on trypanothione reductase?
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A form of glutathione in protozoans known as kinetoplastidans. It helps maintain a reduced state of intracellular thiols, and is essential for survival.
Nifurtimox is used in Chagas' disease (T. cruzi) |
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Since protozoan parasites require purine salvage because they are unable to synthesize them, what gout agent can you use to treat Lesihmania, Schistomoma, and Trpanosoma species?
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Allopurinol (although, only mini pharm indicates this), which degrades purines.
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Ornithine decaroxylase is required for growth for, and what drug acts on this enzyme?
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Certain parasites (Trypanosoma, Plasmodium, and Giardia) (insignificant drug!?! can't really cross reference), where the enzyme forms polyamine, and putrescine. Eflornithine acts as a suicide substrate.
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What is the MOA of suramin?
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Binds to glycolytic enzymes and may prevent the incorporation of the enzymes into the glycosome.
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Dihydrofolate reductase is a target for? And what drugs work on it?
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Antimicrobial and cancer chemotherapy. Pyrimethamine and Trimethoprim
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How does atovaquone work?
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It is a quinone, an antimalarial drug (also Pneumocystis carinii infections) that works on the cytochrome complex and inhibits MT electron transport.
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What drug inhibits microtubule synthesis and function and affects what parasite?
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Mebendazole (and albenazole), and acts on helminths.
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What drug activates parasitic nicotinic receptors, and what parasite does this work on?
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Pyrantel pamoate, and works on hookworms, roundworms, and pinworms.
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What drug increases Ca++ uptake, causing parasite contraction and paralysis? And works on?
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Praziquantel. The drug is antischistosomal and antitapeworm agent.
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What drug acts on ergosterol, the principal sterol in plasma membranes and found in?
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Azole family (e.g., ketoconazole). Ergosterol are found in fungus, and T. cruzi and Leishmania.
Amphotericin B also works on ergosterol. |
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Certain anaerobic protozoan parasites lack MT and generate energy-rich compounds such as acetyl-CoA by means of enzymes present in organelles called hydrogenosomes. A key enzyme involved is?
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Pyruvate-ferredoxin oxidoreductase. Metronidazole inhibits this enzyme.
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WHich compound is a good substrate for hypoxanthine-guanine phosphoribosyltransferase in trypanosomes (but not mammals) and is eventually converted into metabolites that are incorporated into RNA?
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Allopurinol (gout drug, used as an inhibitor of xanthine oxidase)
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One chemotherapeutic strategy used to eradicate the bloodstream form of African trypanosomes is based on the absolute dependence of the organism on?
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Cytochrome-dependent electron transfer, a clycolytic enzyme inhibitor (salicylhydroxamic acid)
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What drug enhances GABA actions on the neuromuscular junctions of nematodes and arthropods)?
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Ivermectin and is the DOC for Onchocerca volvulus.
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Which drug is an antimetabolite that inhibits a trypanosomal enzyme involved
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Eflornithine, a suicide inhibitor of ornithine decarboxylase. (not that important of a drug!?!?!)
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Anticoccidial 4-hydroxyquinolines inhibit?
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MT respiration in Eimeria species. And only this species
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Mebendazole binds to?
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Tubulins to alter the transport functions of microtubules
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Metronidazole is activated in the parasite to?
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A cytotoxic product
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Salicylhydroxamic acid inhibits?
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Glycerol-3-phosphate oxidase, which brings the parasite into an anaerobic state. (not that important of a drug?!?!?)
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Sulfonamides inhibit?
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7,8 dihydropteroate
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What are some enzymes unique to parasites?
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Dihydropteroate synthesase, pyruvate-ferridoxin oxidoreductase, purine nucleoside phosphotransferase, trypanothione reductase.
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Amprolium inhibits?
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Thiamin transport in Eimeria species (parasite of poultry, who cares!?!)
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Sulfadoxine is an inhibitor of?
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Dihydropteroate synthase in malaria
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Suramin binds to?
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Glycolytic enzymes and prevents their incorporation into glycosomes.
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MOA of thiopurinol riboside?
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Phosphorylates thiopurinol riboside to form the corresponding nucleotide, interfering with purine and nucleic acid metabolism.
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"Baghdad boil" is a form of cutaneous leishmaniasis that occurs commonly in Iraq, and can be treated with?
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Fluconazole (although it is not the DOC). They inhibit ergosterol
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Which drug increases membrane permeability to calcium in trematode and cestode muscles?
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Pyrantel pamoate and praziquantel, which are antihelmintics.
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