Antimalarials

Question 1

MOA of artesunate

Answer 1

metabolize din food vacuole forming toxic free radicals

Question 2

ADE of artesunate

Answer 2

N/V, diarrhea, mild

Question 3

USE of artesunate

Answer 3

blood shizonticide. NO good for prophylax because super short half-life.
ONLY drug reliable against quinine-resistant strains.

Question 4

MOA of artemether/lumefantrine

Answer 4

artemether - metabolized in food vacuole forming toxic free radicals

Lumefantrine - ??

Question 5

ADE of artemether/lumefantrine

Answer 5

artemether - N/V, dairrh, mild

lumefantrine -??

Question 6

MOA of chloroquine

Answer 6

accumulates in food vacuole of plasmodia and prevents polymerization of heme into hemozoin. Intracellular heme accumulation is toxic to parasite.
Only a blood schizonticide.

Question 7

ADE of chloroquine

Answer 7

GI irritaiton, rash, headaches, lesions, peripheral neuropathy, myocardial depression, retinal damage, auditory impair, toxic psychosis. Porphyria attacks.

Question 8

USE of chloroquine

Answer 8

DOC for acute nonfalciparum attacks or sensitive falciparum. Exclusively a blood schizonticide. Also good for RA

Question 9

MOA of doxycycline

Answer 9

tetracycline. inhibits 30s ribosomal subunit.

Question 10

ADE of doxycylcline

Answer 10

tooth discoloration in kids.
Photosensitivity
hepato and nephrotoxicity
elevated BUN.

Question 11

MOA of mefloquine

Answer 11

synthetic quinoline. Oral only. Blood schizonticide

Quinine MOA = binds dsDNA to prevent separation and block replication and RNA transcription.

Question 12

ADE of mefloquine

Answer 12

local irritaiton so oral only. GI distress, rash, headache, dizziness.
Cardiac conduction defects, psych disorders, neuro symptoms/seizures.

Question 13

USE of mefloquine

Answer 13

1st line prophylaxis in all geographics with chlorquine resitance. Alternative to quinine.

Question 14

MOA of primaquine

Answer 14

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.

Question 15

ADE of primaquine

Answer 15

GI, pruritis, HA, methemoglobinemia
Hemolysis in G6PD deficient.
No preggers.

Question 16

USE of primaquine

Answer 16

eradicates liver stages of P vivax and P ovale. Should be given with a blood chizonticide.

Question 17

MOA of quinine

Answer 17

complexes with dsDNA to prevent separation and block replication and transcription to RNA.
only a BLOOD schizonticide

Question 18

ADE of quinine

Answer 18

Cinchonism - GI, headache, vertigo, blurred vision, tinnitus.
OVerdose = cardiac conduction, hematotoxic,
Beware G6PD deficients
-Blackwater fever = intravascular hemolysis rare and fatal.
No preggers.

Question 19

USE of quinine

Answer 19

P falciparum that is chloroquine resistant. Often given with doxy.

Question 20

MOA of pyrimethamine

Answer 20

inhibits DHFR. often given with sulfadizine to achieve sequential blockade

Question 21

ADE of pyrimehtamien

Answer 21

GI irritation, glossitic, neuro symptoms, hematotoxicty

Question 22

USE of pyrimethamine

Answer 22

combo with sulfadoxine to achieve sequential blockade of 2 steps in folic acid synthesis.
Regimen of choice for prophylaxis against and treatment of toxoplasmosis

Question 23

MOA of sulfadoxine

Answer 23

long lasting sulfonamide. blocks dihydropteroate synthase by acting as antimetabolites of PABA, inteferring with folate synthesis.

Question 24

ADE of sulfadoxine

Answer 24

GI irrtation, glossitis, neuro symptoms, hematotoxicity

Question 25

USE of sulfadoxine

Answer 25

combo with pyrimethamine to achieve sequential blockade of 2 steps in folic acid synthesis.
Regimen of choice for prophylaxis against and treatment of toxoplasmosis

Question 26

What is blackwater fever and what drug can cause it?

Answer 26

caused by quinine and its derivatives.
intravascular hemolysis in quinine-sesnsitized persons. Rare and sometimes fatal. Beware giving quinine products to G6PD deficient patients

Question 27

What is cinchonism?

Answer 27

quinine product overdose.
fever, tinnitus, blurred vision, impaired hearing, confusion, HA, ab pain, rashes, vertigo, N/V.
Usually reversible