Anti-Malarials

Question 1

Drugs for the prevention of malaria in travelers in areas without resistant P. falciparum

Answer 1

Chloroquine

Question 2

Drugs for the prevention of malaria in travelers in areas with chloroquine resistant P. falciparum

Answer 2

Atovaquone + Proguanil (Malarone) Mefloquine

Question 3

Drugs for the prevention of malaria in travelers in areas with multidrug resistant P. falciparum

Answer 3

Doxycycline

Question 4

Terminal prophylaxis of P. vivid and P. ovale infections; alternative for primary prevention

Answer 4

Primaquine

Question 5

4 species of plasmodium which cause malaria

Answer 5

– Plasmodium falciparum – Plasmodium vivax – Plasmodium malariae – Plasmodium ovale

Question 6

Most virulent species of plasmodium; responsible for most of serious complications & deaths

Answer 6

Plasmodium falciparum

Question 7

Drug resistance (important therapeutic problem is most notable with this virulent species)

Answer 7

Plasmodium falciparum

Question 8

primarily pathogenic to monkeys; now known to cause illness to humans in Asia

Answer 8

P. knowlesi

Question 9

Stage 1 of lifecycle: Transmission of (1) by Plasmodium-infected Anopheles into the bloodstream

Answer 9

1. sporozoites

Question 10

Stages 2&3 of lifecycle: (1) invade (2); divide forming (3)

Answer 10

1. Sporozoites 2. Liver 3. multinucleated schizonts (pre-erythrocytic stage)

Question 11

Active against hepatic-stage schizonts (stages 2 and 3)

Answer 11

Atovaquone-proguanil and primaquine

Question 12

Stage 4: (1) rupture & release (2) to blood; invade RBC, forming (3) & later (4)

Answer 12

1. Schizonts 2. merozoites 3. trophozoites 4. multinucleated schizonts (erythrocytic stage)

Question 13

Blood-stage schizonticides (stage 4)

Answer 13

Quinoline derivatives (Chloroquine, amodiaquine, quinine, quinidine, mefloquine, primaquine, lumefantrine & halofantrine) Antifolates (sulfadoxine-pyrimethamine, atovaquone-proguanil) Antimicrobials (tetracycline, doxycycline and clindamycin) Artemisinin derivatives interrupt schizogony within red cells

Question 14

Quinoline derivatives (Chloroquine, amodiaquine, quinine, quinidine, mefloquine, primaquine, lumefantrine & halofantrine)

Answer 14

stages 2, 3, 4, 5 Active against hepatic-stage schizonts Active against blood-stage schizonticides gametocidal drug (primaquine)

Question 15

Antifolates (sulfadoxine-pyrimethamine, atovaquone-proguanil)

Answer 15

stages 2, 3, 4 Active against hepatic-stage schizonts Active against blood-stage schizonticides

Question 16

Antimicrobials (doxycycline)

Answer 16

Active against Blood-stage schizonticides (stage 4)

Question 17

Artemisinin derivatives interrupt schizogony within red cells

Answer 17

Active against Blood-stage schizonticides (stage 4) gametocidal drugs (Stage 5)

Question 18

Stage 5. Some merozoites differentiate into ♂ or ♀ (1); ingested by the Anopheles mosquito & mature in the mid-gut to (2) (migrate to the salivary glands of the mosquito)

Answer 18

1. gametocytes 2. sporozoites

Question 19

gametocidal drugs

Answer 19

Artemisinin derivatives and Primaquine

Question 20

Tissue schizonticides

Answer 20

drugs that eliminate developing or dormant liver forms

Question 21

Blood schizonticides

Answer 21

drugs that act on erythrocytic forms of the parasites

Question 22

Gametocidal drugs

Answer 22

drugs that kill sexual stages & prevent transmission to mosquitoes

Question 23

Causal prophylactic drugs

Answer 23

prevent erythrocytic infection

Question 24

Treatment & chemoprophylaxis of infection with sensitive parasites

Answer 24

Chloroquine

Question 25

Treatment of severe P. falciparum infections, especially cerebral malaria

Answer 25

Quinine

Question 26

Chemoprophylaxis and Treatment of infections with P. falciparum

Answer 26

Mefloquine

Question 27

Treatment of infections with some chloroquine‐resistant P. falciparum; could be combined with artesunate; preventive therapy in endemic areas

Answer 27

Sulfadoxine-pyrimethamine

Question 28

Treatment and chemoprophylaxis of P. falciparum infections

Answer 28

Atovaquone + Proguanil (Malarone)

Question 29

Radical cure and terminal prophylaxis of infections with P. vivax and P. ovale; alternative chemoprophylaxis for all species

Answer 29

Primaquine

Question 30

Drug of choice for treatment of P. falciparum-sensitive malaria & chemoprophylaxis of malaria

Answer 30

Chloroquine

Question 31

Mutations in a (1) correlates with P. falciparum resistance

Answer 31

1. putative transporter (PfCRT)

Question 32

Terminate fever in 24-48 hours; Clears parasitemia in 48-72 hours

Answer 32

Chloroquine

Question 33

Almost complete GIT absorption

Answer 33

Chloroquine

Question 34

mechanism of action: concentrates in parasite food vacuoles; increases (1) and toxicity to parasite

Answer 34

1. free heme Chloroquine; Amodiaquine

Question 35

Amodiaquine a/e

Answer 35

Agranulocytosis, aplastic anemia and hepatotoxicity are common adverse effects

Question 36

Chloroquine a/e

Answer 36

Pruritus Nausea, abdominal pain, blurring of vision Hemolysis in persons deficient in G6PD Hypotension ECG changes: QRS widening; T wave abnormalities

Question 37

First line therapies for P. falciparum malaria, especially cerebral malaria

Answer 37

Quinine

Question 38

Alkaloid from bark of cinchona tree

Answer 38

Quinine

Question 39

Rapid-acting, highly effective schizonticide against all four human malaria parasites

Answer 39

Quinine

Question 40

Quinine: gametocidal against (1) but not (2)

Answer 40

1. P. vivax and P. ovale 2. P. falciparum

Question 41

Quinine versus quinidine - which has shorter half life

Answer 41

Quinidine

Question 42

Quinine a/e

Answer 42

Cinchonism: Tinnitus; Headache; Visual disturbances; Nausea; Dizziness; Flushing Hypersensitivity reactions Hemolytic abnormalities Hypoglycemia ECG abnormalities

Question 43

Contraindicated with quinine

Answer 43

Mefloquine Al3+ containing antacids warfarin and digoxin

Question 44

Strong blood schizonticidal activity against P. falciparum and P. vivax

Answer 44

Mefloquine

Question 45

Disrupts plasmodia mitochondria electron transport

Answer 45

Atovaquone + Proguanil (Malarone)

Question 46

Acts against Tissue/Erythrocytic schizonts

Answer 46

Atovaquone + Proguanil (Malarone)

Question 47

Atovaquone + Proguanil (Malarone) a/e

Answer 47

Abdominal pain, nausea, vomiting, diarrhea, rash

Question 48

Contraindication Atovaquone + Proguanil (Malarone)

Answer 48

Co-administration with tetracycline or rifampin

Question 49

Answer 49

Question 50

Active drug = Cycloguanil, a triazine metabolite

Answer 50

Proguanil

Question 51

Folate synthesis blockade ‐ selec􀆟􀆟ve ↓ of plasmodial dihydrofolate reductase activity)

Answer 51

Proguanil

Question 52

Erythrocytic forms of all four human malarial species

Answer 52

Pyrimethamine Proguanil

Question 53

↓Bacterial protein synthesis (also ↓Protein synthesis in plasmodial species)

Answer 53

Doxycyclin and Tetracyclin

Question 54

a/e of doxycyclin and tetracyclin

Answer 54

GI symptoms; photosensitivity

Question 55

standard prophylactic drug in SE Asia

Answer 55

Doxycyclin (in combination with Mefloquine)

Question 56

Available as a fixed dose combination with Artemether – 1st line therapy for uncomplicated malaria in most of Africa

Answer 56

Lumefantrine

Question 57

a/e of Halofantrine

Answer 57

Dose-related QT and PR intervals prolongation Embryo-toxic, thus contraindicated in pregnancy

Question 58

production of free radicals following iron catalyzed cleavage of artemisinin endoperoxide bridge in the parasite’s food vacuole

Answer 58

Artemisinin

Question 59

inhibition of parasite’s calcium ATPase

Answer 59

Artemisinin

Question 60

Artemisinin a/e

Answer 60

N/V diarrhea, dizziness Rare: neutropenia, anemia, hemolysis, allergic reactions