Antimalarials Flashcards
MOA of artesunate
metabolize din food vacuole forming toxic free radicals
ADE of artesunate
N/V, diarrhea, mild
USE of artesunate
blood shizonticide. NO good for prophylax because super short half-life.
ONLY drug reliable against quinine-resistant strains.
MOA of artemether/lumefantrine
artemether - metabolized in food vacuole forming toxic free radicals
Lumefantrine - ??
ADE of artemether/lumefantrine
artemether - N/V, dairrh, mild
lumefantrine -??
MOA of chloroquine
accumulates in food vacuole of plasmodia and prevents polymerization of heme into hemozoin. Intracellular heme accumulation is toxic to parasite.
Only a blood schizonticide.
ADE of chloroquine
GI irritaiton, rash, headaches, lesions, peripheral neuropathy, myocardial depression, retinal damage, auditory impair, toxic psychosis. Porphyria attacks.
USE of chloroquine
DOC for acute nonfalciparum attacks or sensitive falciparum. Exclusively a blood schizonticide. Also good for RA
MOA of doxycycline
tetracycline. inhibits 30s ribosomal subunit.
ADE of doxycylcline
tooth discoloration in kids.
Photosensitivity
hepato and nephrotoxicity
elevated BUN.
MOA of mefloquine
synthetic quinoline. Oral only. Blood schizonticide
Quinine MOA = binds dsDNA to prevent separation and block replication and RNA transcription.
ADE of mefloquine
local irritaiton so oral only. GI distress, rash, headache, dizziness.
Cardiac conduction defects, psych disorders, neuro symptoms/seizures.
USE of mefloquine
1st line prophylaxis in all geographics with chlorquine resitance. Alternative to quinine.
MOA of primaquine
forms quinoline-quinone metabolites that are electron-transferring redox compounds that act as cellular oxidants.
Tissue schizonticide!!!!! Hits the PRIMary source or reinfections.
Gametocide also.
ADE of primaquine
GI, pruritis, HA, methemoglobinemia
Hemolysis in G6PD deficient.
No preggers.
USE of primaquine
eradicates liver stages of P vivax and P ovale. Should be given with a blood chizonticide.
MOA of quinine
complexes with dsDNA to prevent separation and block replication and transcription to RNA.
only a BLOOD schizonticide
ADE of quinine
Cinchonism - GI, headache, vertigo, blurred vision, tinnitus.
OVerdose = cardiac conduction, hematotoxic,
Beware G6PD deficients
-Blackwater fever = intravascular hemolysis rare and fatal.
No preggers.
USE of quinine
P falciparum that is chloroquine resistant. Often given with doxy.
MOA of pyrimethamine
inhibits DHFR. often given with sulfadizine to achieve sequential blockade
ADE of pyrimehtamien
GI irritation, glossitic, neuro symptoms, hematotoxicty
USE of pyrimethamine
combo with sulfadoxine to achieve sequential blockade of 2 steps in folic acid synthesis.
Regimen of choice for prophylaxis against and treatment of toxoplasmosis
MOA of sulfadoxine
long lasting sulfonamide. blocks dihydropteroate synthase by acting as antimetabolites of PABA, inteferring with folate synthesis.
ADE of sulfadoxine
GI irrtation, glossitis, neuro symptoms, hematotoxicity
USE of sulfadoxine
combo with pyrimethamine to achieve sequential blockade of 2 steps in folic acid synthesis.
Regimen of choice for prophylaxis against and treatment of toxoplasmosis
What is blackwater fever and what drug can cause it?
caused by quinine and its derivatives.
intravascular hemolysis in quinine-sesnsitized persons. Rare and sometimes fatal. Beware giving quinine products to G6PD deficient patients
What is cinchonism?
quinine product overdose.
fever, tinnitus, blurred vision, impaired hearing, confusion, HA, ab pain, rashes, vertigo, N/V.
Usually reversible
