AntiMalarials

Question 1

1 Stage Antimalarials

Answer 1

Blood Stages only, mostly P. falciparum

Artemisinins - 
*Artemether
*Artemether-Lumefantrine
Quinolones
*Quinine sulfate
*Quinidine Cluconate
*Chloroquine Phosphate

Question 2

2 Stage Antimalarials

Answer 2

Blood and Liver stages of P. falciparum, some vivax

• Atovaquone
• Proguanil

Question 3

3 Stage Antimalarials

Answer 3

Primaquine

Liver stages P. vivax and ovale

Question 4

Artemether

Answer 4

• Stage 1 Antimalarial
• Endoperoxide moiety activated in Digestive Vacuole, causing buildup of radicalized heme molecules and death of parasite
• Mostly oral, but also parenteral
• Short t1/2
• Liver clearance
• METABOLIZED BY p450
• Pregnancy CatC and Teratogenic

Question 5

Lumefantrine

Answer 5

• 1 Stage Antimalarial
• Combination with Artemether
• Pregnancy Cat C

Question 6

Quinolones

Answer 6

• Quinine Sulfate
• Quinidine Gluconate
• Mostly for severe P. falciparum
• Oral (and others, w side effects) - Aluminum antiacids interfere with absorption
• Cleared by Kidneys
• Metabolized by p450
• Lots of side effects, worse than Chloroquines: Fatal oral dose, CNS stuff associated with Cinchoism, Hemolysis (esp. w G6PD deficiency), neuromuscular interactions leading to dsyrhythmias in heart (also the people who should not receive)

Question 7

Chloroquine Phosphate

Answer 7

*Weak base accumulates in digestive vacuole to interfere with heme metabolism. Similar to Quinolones.
*Oral
*Metabolized by some p450s, INHIBITS OTHERS
*

Question 8

Three Orders of AntiMalarials

Answer 8

1 - Just blood stages
2 - Blood AND LIVER stages of P. falciparum, some action on other spp.
3 - LIVER STAGES of P. vivax and ovale and GAMETOCYTES