Antimalarial

Question 1

what are the 4 Plasmodium that infect humans

Answer 1

• P. falciparum
• P. Vivaz
• P. Ovale
• P. Malariae

Question 2

Malaria has what two stages

Answer 2

• human liver stage: dormant
  
  • hypnozoite
• human blood stage
  
  • merozoite

Question 3

which plasmodium species have secondary tissue forms?

Answer 3

P. Ovale and P. vivax

Question 4

what is a “clinical cure”

Answer 4

• therapy that is used to suppress symptoms

Question 5

function of blood schizonticides

Answer 5

act on erythrocytic forms of the parasite

• ***Do NOT affect the secondary tissue forms of P. vivax and P. Ovale

Question 6

function of tissue schizonticides

Answer 6

• act on hepatic stages
• prevent relapses
• do not suppress symtpoms once erythrocytic stages have been established
• can prevent initial development of malaria (Prophylaxis), but generally too toxic

Question 7

function of gametocidal agents

Answer 7

• act on gametocytes
• may slow spread of the disease

Question 8

DOC: sensitive plasmodium organisms

Answer 8

Chloroquine

Question 9

function of Chloroquine

Answer 9

active against asexual erythrocytic forms

Question 10

problem with treating with Chloroquine

Answer 10

resistant forms (particularly P. Falciparum) are a serious problem

• transport pump removes drug from parasite

Question 11

MOA: Chloroquine

Answer 11

• exact MOA not fully elucidated
• may interfere with lysosomal degradation of hemoglobin

Question 12

route of administration: Chloroquine

Answer 12

oral or parenteral

Question 13

accumulation of Chloroquine

Answer 13

melanin-rich tissues: skin, retina

Question 14

toxicity of Chloroquine

Answer 14

• retinal and corneal toxicity
• ototoxicity
• hemolysis - G6PD deficiency
• QT prolongation

Question 15

DOC: plasmodium infections that are chloroquine-resistant

Answer 15

Mefloquine

Question 16

DOC: prophylaxis against all chloroquine-resistant plasmodia

Answer 16

Mefloquine

Question 17

route of administration of Mefloquine

Answer 17

oral

Question 18

toxicity of Mefloquine

Answer 18

• depression of myocardium
• seizures
• may aggravate latent psychoses
• vivid dreams

Question 19

contraindications for Mefloquine

Answer 19

• patients with a history of mental illness or epilepsy
• pregnant women: teratogenicity

Question 20

function of Quinine and Quinidine Gluconate

Answer 20

• acts on erythrocytic forms

Question 21

Quinine and Quinidine Gluconate is Gametocidal against which plasmodium organisms

Answer 21

• P. vivax
• P. ovale

Question 22

which therapys are found in cinchona bark

Answer 22

Quinine and Quinidine Gluconate

Question 23

DOC: treatment of complicated, chloroquine-resistant plasmodia

Answer 23

Quinine and Quinidine Gluconate

Question 24

DOC: unconscious patient

Answer 24

Quinine and Quinidine Gluconate combined with doxycycline or clindamycin

Question 25

route of administration of quinine

Answer 25

oral

Question 26

route of administration of Quinidine Gluconate

Answer 26

IV

Question 27

toxicity of Quinine and Quinidine Gluconate

Answer 27

* **Cinchonism**: overdose: tinnitus, HA, dizziness, flushing, visual disturbances * antiarrhythmic agent: class 1A * QT elongation * hemolysis in G6PD

Question 28

Use of doxycycline with quinidine gluconate (or quinine sulfate)

Answer 28

another option for treatment of complicated chloroquine-resistant malaria

Question 29

Use of clindamycin with quinidine gluconate (or quinine sulfate)

Answer 29

another option for treatment of complicated chloroquine-resistant malaria in children/pregnant women

Question 30

Name the 4 folate metabolism inhibitors

Answer 30

* Pyrimethamine * Proguanil * Trimethoprim * pyrimethamine + sulfadoxine (not available in US)

Question 31

folate metabolism inhibitors target what malaria forms

Answer 31

main effect on erythrocytic forms

Question 32

how does malaria become resistant to folate metabolism inhibitors?

Answer 32

create mutations in dihydrofolic acid

Question 33

specific MOA of sulfadoxine

Answer 33

* \*\*sulfonamide * inhibits incorporation of PABA into folic acid

Question 34

specific MOA of pyrimethamine and proguanil

Answer 34

inhibit dihydrofolate reductase, blocking conversion of dihydrofolic acid to tetrahydrofolic acid

Question 35

Function of atovaquone + proguanil

Answer 35

* synergistic combination * active against tissue and erythrocytic forms

Question 36

Is Artemisinin used as monotherapy

Answer 36

No! * artemisinin combination treatment (ACT)

Question 37

use of Artemether/Lumefantrine

Answer 37

* chloroquine resistant P. falciparum and P. vivax

Question 38

contraindications Artemether/Lumefantrine

Answer 38

patients with a h/o cardiac disease or prolonged QT interval

Question 39

what is the therapy for tissue schizonticide

Answer 39

Primaquine

Question 40

List the Blood Schizonticides

Answer 40

* Choloquine * Mefloquine * Quinine sulfate and Quinidine gluconate * doxycycline * pyrimethamine + sulfadoxine * trimethoprim * proguanil * atovaquone + proguanil * artemisinin

Question 41

"radical cure"

Answer 41

* of P. vivax and P.ovale * used for terminal prophylaxis

Question 42

route of administration of Primaquine

Answer 42

oral

Question 43

toxicity of Primaquine

Answer 43

* hemolytic anemia: G6PD deficiency

Question 44

contraindications of Primaquine

Answer 44

1. G6PD deficiency: treat relapse 2. SLE or RA 3. pregnant females

Question 45

treatment options for chloroquine-resistant P. falciparum

Answer 45

* quinine sulfate + doxycycline/clindamycin/tetracycline * mefloquine * atovaquone with proguanil * artemether-lumefantrine

Question 46

treatment for severe malaria

Answer 46

* Quinidine + doxycycline/clindamycin/tetracycline

Question 47

treatment for prevention of relapse from P. vivax and P. ovale

Answer 47

Primaquine

Question 48

treatment of P. vivax or P. ovale

Answer 48

* chloroquine * quinine sulfate + doxycycline * mefloquine * atovaquone with proguanil