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Flashcards in Antimalaria Agents Deck (24):
0

Chloroquine is administered ..

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

1

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)

Chloroquine

2

Major side effect of quinine

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

Hypoglycemia since it causes the release of insulin

3

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

Mefloquine

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

6

May cause black water fever if used for a long time

Quinine

- characterized by hemolytic anemia with renal failure

7

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

Mefloquine

9

If given in high IV dose may cause hypotension or arrhythmias

Chloroquine

10

MOA of quinine and absorption

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

11

MOA of pyrimethamine + Sulfadoxine

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

12

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

Pyrimethamine + Sulfadoxine

13

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

Malarone ( a/p)

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

14

Who should you not use primaquine in

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

15

Use of mefloquine

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

17

Can cause cinchonism at high concentrations

Quinine - high concentrations used to treat falciparium
- cinchonism ( Nausea, dizziness so, tinnitus, headache and blurring of vision )

18

Works via free radical type mechanism

Aretemether + lumefantrine ( lum works like chloroquine)

19

Used of Aretemether + lumefantrine and side effects

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

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

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

Atovaquone/ proquanil ( prodrug)
Malarone

22

Only drug that works in the exoerythrocytic stage

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

23

Use of malarone

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

25

MOA of mefloquine

Thought to disrupt polymerization hemozoin

27

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

Chloroquine

32

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

Pyrimethamine +Sulfadoxine ( usually used with quinine)

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.

Quinine

44

Drug of choice for pregnant women.

Chloroquine