Malaria Drugs

Question 1

Chloroquine
MOA
Selectivity
Adverse

Answer 1

• inhibitis ferroprotoporphyrin IX, prevents hematin –> hemazoin transformation. hematin is toxic to protozoa
• 25x concentrated in infected cells
• usually mild, blindness in high doses

Question 2

Quinine

MOA
Selectivity
Adverse

Answer 2

• same as chloroquine
• same as chloroquine
• blindness at high doses

Question 3

Quinidine

MOA
Selectivity
Adverse

Answer 3

• inhibits Na+ and K+ (cardiac anti-arrythmic)
• same as chloroquine
• cardiac arrythmias: need pre-therpay EKG

Question 4

Metfloquine

MOA
Selectivity
Adverse

Answer 4

• same as chloroquine
• same as chloroquine
• neuropsychiatric Sx**

Question 5

Atovaguane-Proguanil

MOA
Selectivity
Adverse

Answer 5

Atovaguane

MOA: depolarizes mitochondria, inhibits e- transport chain

Adverse: drug interactions

Proguanil

MOA: inhibits DHFR, selective for plasmodial

*slow acting

Question 6

Artemisinins

MOA
Selectivity
Adverse

Answer 6

-heme iron in malarial pigment makes free radicals –> parasite damage

*rapid acting

*given in combination

Question 7

Lumefantine

MOA
Selectivity
Adverse

Answer 7

• unknown
• long t_1/2

Question 8

Primaquine

MOA
Selectivity
Adverse

Answer 8

• unknown
• selective
• hemolytic anemia in G6PD deficiency (need to balance therapy with adverse)

**rescue therapy**