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Malaria & Schistosomiasis
Pharmacology - Unit 4
18
Pharmacology
12/14/2011

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Term
Quinine/Quinidine
Definition
Only parenteral drug available in US since 1991.
Mechanism-Inhibit the polymerization of heme molecues w/in parasite vacuoles. Heme is very toxic, causing oxidative damage to membranes and digestive proteases.
Resistance-transporter mutation pumps chloroquine out of vacuole.
Term
Chloroquine
Definition
Mechanism-Inhibit the polymerization of heme molecues w/in parasite vacuoles. Heme is very toxic, causing oxidative damage to membranes and digestive proteases.
Resistance-transporter mutation pumps chloroquine out of vacuole.
Term
Mefloquine
Definition
Mechanism-Inhibit the polymerization of heme molecues w/in parasite vacuoles. Heme is very toxic, causing oxidative damage to membranes and digestive proteases.
Resistance-transporter mutation pumps chloroquine out of vacuole.
Neurotoxicity & psychoses
Term
Primaquine
Definition
Only drug available to tx relapses/latent infxns.
CAUTION: primaquine depletes glutathione reserves; individuals w/ glucose-6-phosphate dehydrogenase deficiency are at great risk for hemolysis/anemia!!!
Term
Pyrimethamine
Definition
Dihydrofolate Reductase Inhibitor
Term
Chloroguanide
Definition
Dihydrofolate Reductase Inhibitor
Term
Sulfonamides & Sulfones
Definition
Dihydrofolate Reductase Inhibitor (actually interferes w/ tetrahydrofolate synthesis earlier in pathway).
Term
Atovaquone
Definition
Depolarizes parasitic mitochondria & inhibits their electron transport (low incidence of resistance).
Used in combo w/ Proguanil
Term
Artemether
Definition
Mech: inhibits parasite SERCA of P. falciparum
Term
Artesunate
Definition
Mech: inhibits parasite SERCA of P. falciparum
Term
Hydroxychloroquine
Definition
Similar to chloroquine; available as an alternative to chloroquine.
Term
Tetracycline
Definition
inhibits protein translation.
Term
Doxycycline
Definition
inhibits protein translation.
Term
Clindamycin
Definition
inhibits protein translation.
Term
Proguanil
Definition
Dihydrofolate Reductase Inhibitor
used in combination w/ atovaquone
Term
Praziquantal
Definition
Use-Schistosomiasis
Mechanism-increases permeability of worm to Ca2+, causing contractions and paralysis of worm musculature -> outer membran breaks down -> host immune response.
Side Effects-some abdominal discomfort & head ache, but quite safe.
Term
Lumefantrine
Definition
aka benflumetol; synthesized in China.
used in combination w/ artemether called coartemether.
other than that, was not discussed much.
Term
Proguanil with Atovaquone
Definition
Used prophylactivally and to tx active infx with Plasmodium falciparum, including chloroquine resistant strains.