Burkin: Parasitic Pharmacology Flashcards
What are these drugs used for?
Quinine
Chloroquine
Primarquine
Antimetabolites
Malaria
What are other drugs used to treat protozoan parasites?
metronidazole
diloxanide
nifurtimox
suramin
Which antimalarial drug is active against malaria when it is NOT in RBCs? What about when it is in RBCs?
primaquine; chloroquine and quinine
Different antimalarial drugs act at different stages of the malarial parasite’s life cycle. Which drug works when the parasite is NOT within RBCs?
paraquine
What is the method of action of quinine? What is it used to treat?
blocks heme polymerization so that heme concentrations are at toxic levels to parasites; used to treat chloroquine resistant Plasmodium falciparum
What is an adverse reaction caused by quinine?
cinchonism (similar to salicylate toxicity), curare effect, myocardial depression
How does chloroquine work? What is it used to treat?
blocks polymerization of heme, leading to toxic heme concentrations (toxic to parasites); works against ERYTHROCYTIC forms - used for acute malarial attacks, prophylaxis (prevention)
What are the effects of chloroquine if used for prophylaxis? If used acutely? If used in large doses?
little toxicity; anorexia, vomiting, nausea, headache; photosensitivity, retinopathy, leukopenia
How does primaquine work?
binds to DNA –> damages mitochondria via oxidative stress –> inhibits protein synthesis
What is primaquine used for?
liver forms of P. vivax and P. ovale
**not very effective against P. falciparum or P. malariae
Adverse reactions for primaquine?
same as chloroquine + hemolytic anemia
What types of patients are particularly prone to hemolytic anemia while taking primaquine?
those with G6PDH deficiency
How does pyrimethamine-sulfadoxine work?
inhibits dihydrofolate reductase (in PABA/DHF/THF pathway) - no folic acid synthesis - can’t form DNA
What is the pathway that takes PABA to DNA and RNA?
PABA –> DHF acid via sulfadoxine
DHF –> THF via pyrimethamine
THF –> DNA and RNA
What is pyrimethamine-sulfadozine used to treat?
cholorquine-resistant P. falciparum