Antimalaria Agents

Question 0

Used in acute attack of for prevention in sensitive areas
MOA : thought to prevent metabolism of hemoglobin by inhibiting the heme polymerase -> accumulation of heme causes oxidative stress

Side effects : pruritus and other skin issues, can be used to treat prophoryia ( side effects with large doses none when used for prophylaxis)

Answer 0

Chloroquine

Question 1

Chloroquine is administered ..

Answer 1

Orally . It is absorbed rapidly and completely from the GI tract. Antacids interferes with this.

Question 2

Major side effect of quinine

Answer 2

Arrhythmias because the cardiac muscle is sensitive to it and it is very similar to quinidine.

Hypoglycemia since it causes the release of insulin

Question 3

This drug has the longest half life of all the drugs -13-33 days

Answer 3

Mefloquine

So be careful if switching drugs and the pt was on quinidine or beta blockers

Question 6

May cause black water fever if used for a long time

Answer 6

Quinine

• characterized by hemolytic anemia with renal failure

Question 7

May cause the pt to have very vivid dreams and should not be used in pts with epilepsy of psychiatric disorders

Answer 7

Mefloquine

Question 9

If given in high IV dose may cause hypotension or arrhythmias

Answer 9

Chloroquine

Question 10

MOA of quinine and absorption

Answer 10

Similar to chloroquine . But thought to form a hydrogen bond with dsDNA that inhibits transcription and ultimately protein synthesis

Orally administered, 10 hr half life and antacids inhibit absorption

Question 11

MOA of pyrimethamine + Sulfadoxine

Answer 11

Inhibits dihydrofolate reductase (pyrimethamine ) and the Sulfadoxine inhibits dihydropteroate synthetase

Question 12

Side effects of this drug include blood dyscrasias, folic acid deficiency and Steven Johnson syndrome

Answer 12

Pyrimethamine + Sulfadoxine

Question 13

Don’t use this drug in pts with severe renal impairment or in pregnant people

Answer 13

Malarone ( a/p)

Other minor SE: abdominal pain, nausea/ vomiting, headache

Question 14

Who should you not use primaquine in

Answer 14

Pregnant women
People why polymorphism in G6PD. These people won’t be able tot produce NADPH which allows the generation of reduced glutathione and protects cells from oxidative stress. Without it the pt will get hemolytic anemia from the oxidative stress in the RBCs

Question 15

Use of mefloquine

Answer 15

Prophylaxis in chloroquine resistant falciparium but other options are preferred over this one. Pregnant Cat B

Question 17

Can cause cinchonism at high concentrations

Answer 17

Quinine - high concentrations used to treat falciparium

- cinchonism ( Nausea, dizziness so, tinnitus, headache and blurring of vision )

Question 18

Works via free radical type mechanism

Answer 18

Aretemether + lumefantrine ( lum works like chloroquine)

Question 19

Used of Aretemether + lumefantrine and side effects

Answer 19

Acute attack of chloroquine resistant plasmodium falciparium . Not used for prophylaxis

Side effects are well tolerated : GI symptoms, palpitations. Musculoskeletal and neuro symptoms

Question 21

Inhibits cytochrome bc1 complex of the ETC of the plasmodia and if administered with a prodrug that lowers the effective concentration at which the drug collapses the mitochondrial membrane potential

Answer 21

Atovaquone/ proquanil ( prodrug)

Malarone

Question 22

Only drug that works in the exoerythrocytic stage

Answer 22

Primaquine - so use with vivax or ovule since they are the only forms that can have a latent phase

Question 23

Use of malarone

Answer 23

Uncomplicated cases of chloroquine resistant or mdr malaria . Used for prophylaxis

Question 25

MOA of mefloquine

Answer 25

Thought to disrupt polymerization hemozoin

Question 27

At high doses may cause retinopathies because of high affinity for melanin

Answer 27

Chloroquine

Question 32

Primarily active against erythrocytic form but also has some activity against the primary plasmodium infection in the liver

Answer 32

Pyrimethamine +Sulfadoxine ( usually used with quinine)

Question 36

Used IV in severe cases of falciparium and orally with chloroquine resistant falciparium and vivax. It is used with doxy or clinda when used.

Answer 36

Quinine

Question 44

Drug of choice for pregnant women.

Answer 44

Chloroquine