Term
used for protozoal infections
MOA still unknown
proposed mechanism:
PRODRUG
in anaerobic organisms the nitro group is reduced to a hydroxylamine, during which the reactive derivative or reactive species are produced that cause destructive effects on cell components (DNA, proteins, membranes)
superoxide radical anion, hydrogen peroxide, and hydroxyl radicals are referred to as reactive oxygen species (ROS) and are reactive substances that are implicated in damage to critical cellular components of the parasite
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Definition
| MOA of metronidazole/tinidazole |
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Term
used for protozoal infections
oxidation and imidazole ring is broken
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Definition
| metabolism of metronidazole/tinidazole |
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Term
used for protozoal infections
PRODRUG
inhibits the enzyme pyruvate ferredoxin oxidoreductase: disruption of the bioenergetics of the microorganism (this enzyme is responsible for metabolism of nutrients and oxygen in the microorganism)
INTERMEDIATE IS THE MOST ACTIVE FORM
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Definition
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Term
protozoal infection
PRODRUG
MOA unknown |
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Definition
| what is diloxanide furoate used for? |
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Term
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Definition
| what is SMX/TMP used for? |
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Term
inhibits mitochondrial respiratory chain (ubiquinone reductase inhibitor)
used for protozoal infections |
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Definition
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Term
used for protozoal infections
PK: poorly absorbed, increased with meals
highly bound to plasma proteins
not significantly metabolized |
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Definition
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Term
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Definition
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Term
human liver stage: difficult to treat
human blood stage: sensitive to antimalarial drugs |
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Definition
| which stage of the malaria life cycle is difficult to treat and which is sensitive to antimalarial drugs? |
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Term
antimalarial drug
MOA: DNA intercalation (planar part of the drug molecule inserts itself into microorganism's DNA)
effective against asexual ERYTHROCYTIC forms, inactive against the hepatic form
resistance: spontaneous gene mutation |
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Definition
4-aminoquinolines (chloroquine):
MOA
effectiveness
resistance |
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Term
antimalarial drug
MOA: may become associated with the mitochondria of the EXOERYTHROCYTIC forms of the plasmodia growing causing the mitochondria to swell and become vacuoled
effective against the EXOERYTHROCYTIC stages
at higher doses some activity is obtained against the asexual blood form |
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Definition
8-aminoquinolines (primaquine):
MOA
effectiveness |
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Term
antimalarial drug
MOA: potent inhibitor of dihydrofolate reductase
effective against the ERYTHROCYTIC forms of P. falciparum
resistance: point mutation for the dihydrofolate reductase and dihydropteroate synthase enzymes |
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Definition
pyrimethamine:
MOA
effectiveness
resistance |
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Term
antimalarial drugs
synergistic combination
MOA: atovaquone inhibits the mitochondrial respiratory chain and proguanil is a dihydrofolate reductase inhibitor
resistance: slow uptake |
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Definition
atovaquone/proguanil:
MOA
resistance |
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Term
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Definition
| drugs for helminth infections |
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Term
used for helminth infections
inhibition of the enzyme fumarate reductase (disruption of the production of ATP) |
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Definition
| MOA of benzimidazoles (thibendazole, mebendazole, albendazole) |
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Term
used for helminth infections
poorly absorbed from the GI tract: this is okay b/c the drug needs to "topically" act in the GI tract where the worms are
metabolized by CYP450 and then glucuronidation |
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Definition
| ADME of benzimidazoles (thiabendazole, mebendazole, albendazole) |
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Term
used for helminth infections
decrease microfilarial concentrations: worm will no longer be able to attach to the host
AND
helps the host's GI tract to contract helping to eliminate the worm |
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Definition
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Term
more than one MOA:
Ca redistribution leads to helminth muscle contraction and parylsis leading to worm expulsion
AND
inhibits phosphoinositide metabolism leading to worm paraylsis
Also effect glycogen content and metabolism |
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Definition
MOA of praziquantel
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Term
used for helminth infections
rapidly absorbed and metabolized (hydroxylation)
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Definition
ADME of praziquantel
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Term
used for helminth infections
activated by esterification of the alcohol by sulfate or phosphate group to form active radicals that will interact/bind to DNA
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Definition
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