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31 Cards in this Set

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  • 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.
What drug can block further sequential blockade of folic acid production?
Trimethoprim (inhibits dihydrofolate reductase)
Who uses pyruvate-ferredoxin oxidoreductase, and what is it used for?
Certain anaerobic protozoans that lack mitochondria, posses this enzyme to generate acetyl-CoA via an electron transport.
What is metronidazole's affect on pyruvate ferredoxin oxidoreductase?
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.
What does trypanothione do? And what drug acts on trypanothione reductase?
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)
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?
Allopurinol (although, only mini pharm indicates this), which degrades purines.
Ornithine decaroxylase is required for growth for, and what drug acts on this enzyme?
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.
What is the MOA of suramin?
Binds to glycolytic enzymes and may prevent the incorporation of the enzymes into the glycosome.
Dihydrofolate reductase is a target for? And what drugs work on it?
Antimicrobial and cancer chemotherapy. Pyrimethamine and Trimethoprim
How does atovaquone work?
It is a quinone, an antimalarial drug (also Pneumocystis carinii infections) that works on the cytochrome complex and inhibits MT electron transport.
What drug inhibits microtubule synthesis and function and affects what parasite?
Mebendazole (and albenazole), and acts on helminths.
What drug activates parasitic nicotinic receptors, and what parasite does this work on?
Pyrantel pamoate, and works on hookworms, roundworms, and pinworms.
What drug increases Ca++ uptake, causing parasite contraction and paralysis? And works on?
Praziquantel. The drug is antischistosomal and antitapeworm agent.
What drug acts on ergosterol, the principal sterol in plasma membranes and found in?
Azole family (e.g., ketoconazole). Ergosterol are found in fungus, and T. cruzi and Leishmania.

Amphotericin B also works on ergosterol.
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?
Pyruvate-ferredoxin oxidoreductase. Metronidazole inhibits this enzyme.
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?
Allopurinol (gout drug, used as an inhibitor of xanthine oxidase)
One chemotherapeutic strategy used to eradicate the bloodstream form of African trypanosomes is based on the absolute dependence of the organism on?
Cytochrome-dependent electron transfer, a clycolytic enzyme inhibitor (salicylhydroxamic acid)
What drug enhances GABA actions on the neuromuscular junctions of nematodes and arthropods)?
Ivermectin and is the DOC for Onchocerca volvulus.
Which drug is an antimetabolite that inhibits a trypanosomal enzyme involved
Eflornithine, a suicide inhibitor of ornithine decarboxylase. (not that important of a drug!?!?!)
Anticoccidial 4-hydroxyquinolines inhibit?
MT respiration in Eimeria species. And only this species
Mebendazole binds to?
Tubulins to alter the transport functions of microtubules
Metronidazole is activated in the parasite to?
A cytotoxic product
Salicylhydroxamic acid inhibits?
Glycerol-3-phosphate oxidase, which brings the parasite into an anaerobic state. (not that important of a drug?!?!?)
Sulfonamides inhibit?
7,8 dihydropteroate
What are some enzymes unique to parasites?
Dihydropteroate synthesase, pyruvate-ferridoxin oxidoreductase, purine nucleoside phosphotransferase, trypanothione reductase.
Amprolium inhibits?
Thiamin transport in Eimeria species (parasite of poultry, who cares!?!)
Sulfadoxine is an inhibitor of?
Dihydropteroate synthase in malaria
Suramin binds to?
Glycolytic enzymes and prevents their incorporation into glycosomes.
MOA of thiopurinol riboside?
Phosphorylates thiopurinol riboside to form the corresponding nucleotide, interfering with purine and nucleic acid metabolism.
"Baghdad boil" is a form of cutaneous leishmaniasis that occurs commonly in Iraq, and can be treated with?
Fluconazole (although it is not the DOC). They inhibit ergosterol
Which drug increases membrane permeability to calcium in trematode and cestode muscles?
Pyrantel pamoate and praziquantel, which are antihelmintics.