Exam 4 - Anti-Malarials Flashcards
DRUG LIST
Artemisinins
- Artemether (asexual/gametocyte
- Combo w/ Lumefantrine
DRUG LIST
Quinilones
- Quinine Sulfate (blood)
- Chloroquine Phosphate (blood)
- Primaquine (Hypnozoite Liver/Gametocyte blood)
DRUG LIST
Quinolone Adjuncts
- Doxycycline
- Tetracycline
- Clindamycin
Drug List
Other
Atovaquone-Proguanil
Artemisinins
Artemether
- P falciparum
- P vivax asexual blood stage
- toxic adducts, free radicals kill bug
- not useful for prophylaxis
- use combo therapy with Lumefantrine
Artemisinins
Adverse
- drug-drug interx’ns w/ antiretrovirals
- decrease RBCs and neutrophils
- not for children or 1st trimester preggos
Quninolones
Quinine
- P. falciparum asexual blood stage
- P vivax and ovale gametocyticidal
- interferes w/ heme digestion
- use for chloroquinine resistant P falciparum
- Resistance in SE Asia, South America
Quinolones
Quinine
Adverse
- fatal dose 2-8 g
- cinchonism: tinnitus, deafness, visual disturbance, headache, flushing
- increased hemolysis with G6PD deficiency
- contra’d with: hypersens, tinnitus, optic neuritis, dysrhythmias, warfarin, digoxin, renal insufficiency
Quinolones
Quinine
Adjuncts
Inhibition of protein translation for protozoa:
- Doxycycline
- Tetracycline
- Clindamycin
Quinolones
Chloroquine
Mechanism
- interferes with heme digestion
- mainly oral admin (IV can be lethal)
- resistance since the 60s!
Quinolones
Chloroquine
Adverse
- CV and CNS toxicities
- fatal for parenteral > 5g
- pruritius in black people
- hemolysis with G6PD deficiency
Quinolones
Primaquine
Mechanism
-primary and latent hepatic stages (P vivax, ovale)
-gametocyticidal against P falciparum
-elelctrophilic intermediates disrupt parasite mitochondrial ETC
(oxidative stress)
-oral administration
Quinolones
Primaquine
Adverse
-hemolytic anemia w/ G6PD deficiency
(African, Sephardic, Sardinian, Iranian descent)
-Contra’d in preggo, breast-feeding
Atovaquone
(Proguanil Combo)
Mechanism
- P falciparum asexual blood and liver stagez
- inhibits mitochondrial ETC
- combo with Proguanil
- Proguanil inhibits dihydrofolate reductase
Atovaquone-Proguanil
Adverse
Atovaquone: Rifamp/tetracycline plasma interactions