Antimalarials

Question 1

cases of malaria per year

Answer 1

300-500 million

Question 2

cause of plasmodium vivax

Answer 2

hypnozoites in the liver

Question 3

location for plasmodium falciparum

Answer 3

tropics

Question 4

location for plasmodium vivax

Answer 4

subtropics and temperate regions

Question 5

location for plasmodium ovale

Answer 5

West Africa

Question 6

most malarial deaths are due to what plasmodium?

Answer 6

falciparum

Question 7

form of malaria injected by mosquito

Answer 7

sporozoite

Question 8

form of malaria made in the liver

Answer 8

merozoite

Question 9

hypnozoite

Answer 9

latent stage of relapsing vivax and ovale cause this form

Question 10

sexual stages that are taken up by mosquitos

Answer 10

gametocytes

Question 11

Drugs that kill sporozoites

Answer 11

none, can’t prevent infection

Question 12

Chemoprophylaxis can do what?

Answer 12

prevent development of symptoms caused by asexual erythrocytic forms

Question 13

Complete elimination of infection (radical cure)

Answer 13

requires more than one drug

Question 14

Schizonticides tissue, blood act on

Answer 14

liver forms, RBC forms

Question 15

Gametocides

Answer 15

kill sexual stages and prevent transmission to mosquitos

Question 16

Liver exoerythrocytic schizonticides include

Answer 16

primaquine, atovaquine, and artemisinins

Question 17

chloroquine is an

Answer 17

aminoquinolone

Question 18

chloroquine is used for treatment of

Answer 18

non-falciparum erythrocytic stage and chemoprophylaxis

Question 19

chloroquine will NOT eliminate

Answer 19

hypnozoites

Question 20

MOA of chloroquine

Answer 20

concentrates in food vacuoles for parasite and limit hemozoin production so cause parasite death through heme toxicity

Question 21

resistance to chloroquine

Answer 21

pfMDR1 esp in vivax and falciparum

Question 22

some side effects of chloroquine

Answer 22

pruritis, nausea, dairrhea

Question 23

contraindication of chloroquine

Answer 23

psoriasis, porphyria, retinal field defects, myopathy

Question 24

what will influence absorption of chloroquine

Answer 24

calcium and magnesium containing antacids and antidiarrheals

Question 25

artemesinin MOA

Answer 25

endoperoxide active group that produces toxic free radicals through interacting with intracellular iron

Question 26

artemesinin

Answer 26

rapidly acting blood schizonticide for all species with no effect on liver stage

Question 27

limiting factor of artemesinin

Answer 27

short half life with recrudescence rate high after short course of treatment

Question 28

what would you NOT use artemesinin for?

Answer 28

chemoprophylaxis

Question 29

What is a problem you come across in combination therapy with artamesinin

Answer 29

short half life means resistance in partner drug becomes a concern

Question 30

what drugs would you pair with artemesinin

Answer 30

meflouquine and lumefantrine

Question 31

Coartem

Answer 31

artemether + lumefantrine

Question 32

artemesinin administration

Answer 32

insoluble, oral admin

Question 33

artamether administration

Answer 33

lipid soluble, oral, IM, rectal admin

Question 34

artesunate administration

Answer 34

water soluble, oral, IM, IV, rectal admin

Question 35

dihydroartemesinin admin

Answer 35

water soluble, oral admin

Question 36

adverse effect of artemesinin, consequence

Answer 36

embryotoxic, no use in first trimester of uncomplicated malaria

Question 37

quinine and quinidine

Answer 37

rapidly acting blood schizonticide against all Plasmodium and babesiosis

Question 38

quinidine and quinine treatment important for

Answer 38

first line alternate drug for falciparum

Question 39

downside of quinine and quinidine

Answer 39

very toxic

Question 40

sever falciparum malaria, give quinine/ quinidine

Answer 40

IV

Question 41

quinine and quinidine are metabolized by

Answer 41

CYP3A4

Question 42

consequences of quinine and quinidine admin because of liver

Answer 42

raise levels of warfarin, digoxin and interacts with antiretroviral drugs

Question 43

adverse effects of quinine

Answer 43

cinchonism, cardiotoxicity, mild uterine contractions, blackwater fever, severe hypotension

Question 44

cinchonism

Answer 44

tinnitis, headache, nausea, dizziness, flushing, visual disturbances

Question 45

how do you get severe hypotension with quinine treatment?

Answer 45

too rapid of infusion

Question 46

mefloquine

Answer 46

synthetic 4-quinolone derivative

Question 47

mefloquine treats

Answer 47

prophylactic and treatment of erythrocytic falciparum and vivax

Question 48

adverse reaction mefloquine

Answer 48

neurological problems, seizures, sleep disturbances

Question 49

mefloquine brand name

Answer 49

Lariam

Question 50

Primaquine

Answer 50

8 aminoquinolone

Question 51

MOA primaquine

Answer 51

ROS involved

Question 52

primaquine treats

Answer 52

liver stages of P. vivax and ovale(hypnozoite) and gametocidal to all four

Question 53

primaquine admin how?

Answer 53

short term orally

Question 54

contraindication of primaquine

Answer 54

G6PDH deficiency, granulocytopenia, methemoglobinemia, patients on myelosuppressive drugs

Question 55

Why should you not use primaquine in pregnant patients?

Answer 55

fetus is G6PDH deficient

Question 56

if an individual has G6PDH and you give primaquine, what happens

Answer 56

hemolytic anemia

Question 57

Fansidar consists of

Answer 57

pyremethamine + sulfodoxine

Question 58

what does sulfodoxine do?

Answer 58

inhibits dihydropteroate synthase (PABA > dihydrofolic acid)

Question 59

what does pyrmethamine do?

Answer 59

inhibits dihydrofolate reductase (dihydrofolate > tetrahydrofolate)

Question 60

Fansidar treats

Answer 60

erythrocytic schizonticides and toxoplasmosis

Question 61

sulfadiazine can be replaced by what drug in Fansidar?

Answer 61

clindamycin

Question 62

What would you treat pneumocystis with?

Answer 62

trimethoprim + sulfamethoxazole

Question 63

why should you not use single antifolates?

Answer 63

Resistance develops easily

Question 64

when synergistically used, what happens to the dose of each component

Answer 64

20 fold reduction

Question 65

half life of pyrmethamine

Answer 65

90 hours

Question 66

half life of sufadoxine

Answer 66

170 hours

Question 67

proguanil?

Answer 67

antifolate drug

Question 68

Atavaquone?

Answer 68

disrupts mitochondrial electron transport

Question 69

Malarone

Answer 69

proguanil + atavaquone

Question 70

why dont you use atavaquone on its own?

Answer 70

develops resistance really quickly

Question 71

Atavaquone treatment for what else?

Answer 71

P. jiroveci

Question 72

What do you use malarone for primarily?

Answer 72

chemoprophylaxis and falciparum treatment

Question 73

what antibiotics are used as antimalarials?

Answer 73

tetracycline, doxycycline, clindamycin

Question 74

what do antibiotics in malaria target?

Answer 74

components of the apicoplast as blood schizonticide

Question 75

what is an apicoplast?

Answer 75

plant like organelle that carries out many biochemical processes

Question 76

What do you tend to pair doxycycline with in malaria tx?

Answer 76

quinine/ quinidine for falciparum malaria, chemoprophylaxis

Question 77

metronidazole is the drug of choice for what

Answer 77

extraintestine E. histolytica, giardiasis, and trichomoniasis

Question 78

what does metronidazole kill?

Answer 78

trophozoites, not cysts

Question 79

what do you follow metronidazle with?

Answer 79

luminal drug to eliminate asymptomatic infection

Question 80

what is the brand name of metronidazole?

Answer 80

Flagyl

Question 81

what is the antabuse effect related to?

Answer 81

metronidazole and alcohol ingestion

Question 82

what is metronidazole going to inhibit that causes the antabuse effect?

Answer 82

acetaldehyde dehydrogenase

Question 83

Iodoquinol

Answer 83

luminal amecide used in conjunction with metronidazole to kill trophozoites

Question 84

problem with iodoquinol?

Answer 84

low bioavailability

Question 85

where does iodoquinol act?

Answer 85

GI lumen

Question 86

pentamidine

Answer 86

aromatic diamidine

Question 87

how to admin pentamidine

Answer 87

parenteral

Question 88

what to use pentamidine for

Answer 88

trypanosomiasis in West Africa

Question 89

problem with pentamidine

Answer 89

highly toxic!

Question 90

Nifurtimox

Answer 90

commonly used in T. cruzi

Question 91

MOA nifurtimox

Answer 91

reduction, oxidation, ROS production

Question 92

what does nifurtimox do to illnesses?

Answer 92

reduces severity of acute phase

Question 93

Limitation of nifurtimox

Answer 93

no complete elimination of parasite, no prevention of disease progression

Question 94

toxicity issues with nifurtimox

Answer 94

hypersensitivity, GI

Question 95

how long does nifurtimox tend to be used?

Answer 95

3-4 months

Question 96

miltefosine used for

Answer 96

anti cancer, anti leshmaniasis (visceral)

Question 97

miltefosine

Answer 97

phospholipid analog

Question 98

miltefosine cure rate in visceral leshmaniasis

Answer 98

100% after 28 daily doses

Question 99

main side effect of miltefosine

Answer 99

teratogenic

Question 100

nitazoxanide treats

Answer 100

giardia, cryptosporidium

Question 101

Early stage of West African Sleeping Sickness treated iwth

Answer 101

Pentamidine

Question 102

Late stages of West African Sleeping Sickness treated with

Answer 102

Eflornithine

Question 103

East African Sleeping Sickness Early stages

Answer 103

Suramin

Question 104

Late stage East African Sleeping Sickness

Answer 104

melarsoprol