Antimalarials

Question 1

Tissue schizonticides for radical cure or terminal prophylaxis of Ovale & Vivax ?

Answer 1

Primaquine
Tafenoquine

14 days cours for primaquine ; single dose for Tafenoquine

Question 2

Clinical cure is achieved by killing all parasites responsible for clinical symptoms. Drugs used in clinical cures are called :

Answer 2

Blood schizonticides

Question 3

Chloroquine
Quinine
Mefloquine
Pyrimethamine
Examples of :

Answer 3

Blood schizonticides

Question 4

Chemoprophylaxis agent in sensitive falciparum endemic regions ?

Answer 4

Chloroquine

Question 5

Chloriquine resistant falciparum areae alternative prophylaxis ?

Answer 5

Mefloquine
Atovaquione-proguanil (malorone)
Artemisin
Quinine

Question 6

DOC for all sensitive plasmodium species :

Answer 6

Chloroquine

Question 7

MAO of chloroquine :

Answer 7

Inhibition of heme polymerase (cannot convert heme to hemozoin which is less toxic for the parasite)

Question 8

Mutation in what gene is responsible for rapidly developing resistance of falciparum to chloroquine ?

Answer 8

PfCRT

Question 9

Most common side effects of chloroquine ?

Answer 9

Cinchonism (tinnitus, vertigo)
Pruritus
Blurry vision and Retinal damage
Prolonged QT interval

Rapid IV use can cause hto, choc
Avoid if hepatic dysfunction, GI issues, psoriasis and prophyria acute attack

Question 10

Quinine uses :

Answer 10

Uncomplicated mild falciparum infection in combination with clindamycin in children or with doxycycline in adults ;

In chloroquine resistant & multidrug resistant malaria

As first line IV drug in severe p falciparum in **combination with Artesunate **

To delay the emergence of resistance - quinine should NOT be used routinely for prophylaxis.

Question 11

Main side effects of quinine :

Answer 11

GI
Cinchonism
Hypoglycemia
Hypotension
QT prolongation (cardiac monitoring required when IV infused)
Hemolysis in G6PD deficiency
Feototoxic (avoid in pregnancy)
HSR

Question 12

Rapidly acting blood schizonticide
Effective in uncomplicated chloroquine resistant & multidrug reisstant P. falciparum infections
Half-life 20 days, enter enterohepatic ciruclation
AVOID in psychiatric conditions, seizure disorders or cardiac conduction defects

Answer 12

Mefloquine

Question 13

Slow acting blood schizonticide combination of drug that inhibits sequential steps of folate synthesis & produce synergistic effects

Answer 13

Pyramethamine + sulfadoxine (FANSIDAR)

Question 14

Used in chemoprophylaxis in high risk patients such as HIV, children and in pregnant women in Africa OR for chloroquine-resistant P. falciparum malaria

Also toxoplasmosis & pneumocystitis

Answer 14

Pyramethamine + Sulfadoxine

Question 15

Main adverse events of Pyramethamine & sulfadoxine treatment ?

Answer 15

Megalobastic anemia (reversed by leucovorin)
SJS (if pt is allergic to sulfa drugs)

Question 16

Atovaquone + Proguanil (Malarone) use :

Answer 16

Alternative prophylaxis for resistant P. falciparum malaria

Question 17

Artemisinin mechanism of action :

Rapidly acting blood schizonticide to all malarial parasites

Answer 17

Creating of free radicals when interacts with iron which causes damage to parasite’s proteins.

Highly efficacious, safe and well tolerated but only short acting

Short acting prevents development of resistance but then must always be used in combination with long acting drugs. Specifically with Mefloquine in Southeast Asia and South America.
NOT used in chemoprophylaxis

Question 18

First line therapy in uncomplicated multi-drug resistant P. falciparum ?

Answer 18

Artemisinin

Question 19

Recommended therapy in 2nd and 3rd trimesters of pregnancy in uncomplicated falciparum ?

Answer 19

Artemisinin

First trimester quinine + mefloquine/clindamycin preferred.

Question 20

MAO via redox compounds that act as cellular oxidants which act at tissue level and also limits malaria transmission by acting as a gametocide ?

Answer 20

Primaquine

Question 21

Some metabolites are responsible for hemolysis and methemoglobinemia ; DO NOT USE IF G6PD deficiency or in pregnancy (fetus will have G6PD def) :

Answer 21

Primaquine

Prior to use, must estimate level of G6PD

Question 22

Treatment of malaria

Answer 22

Question 23

First line trx of Leishmaniasis (visceral, mucocutaenous and cutaneous)

Answer 23

Sodium stibogluconate

Question 24

Side effects of Sodium stibugluconate

Answer 24

Serious renal, hepatic and cardiac (long QT) toxicities + painful abscess at site of inhection, GI, fever & headaches.

NEED PERIODIC MONITORING.