B&l: Test 2: 5. Bridges : Antimalarials

Front 1

which form of malaria is most likely to kill you

Back 1

Plasmodium falciparum

most dangerous, potentially fatal
accounts for most serious complications & deaths
pts should be hospitalized for treatment

Front 2

clinical symptoms from malaria are due to what?

Back 2

are due to blood forms of the malaria

Front 3

Plasmodium vivax and ovale are likely to be what kind of malarias?

Back 3

relapsing

Front 4

Blood schizonticides are the antimalarial drug class that act where? use how?

Back 4

Act on erythrocytic parasites
Used for clinical and suppressive care

Front 5

Tissue schizonticides are the antimalarial drug class that act where? use how?

Back 5

Eliminate developing or dormant liver forms
Used for casual prophylaxis
Used to prevent relapse and provide a radical cure

Front 6

what is the target of treatment for P falciparum and P malariae

Back 6

Treatment eliminating erythrocytic parasites will cure infection

Front 7

in P vivax and P ovale what are we trying to attack?

Back 7

Hypnozoite (dormant hepatic state)

Front 8

drug used to stop relapses of P vivax and P ovale?

**

Back 8

Terminal prophylaxis with primaquine

Front 9

why don't you use primaquine all the time?

Back 9

you get drug resistance

so you don't want to give it prophylactically

remember: this is the drug used to stop relapses of P vivax and P ovale (the liver forms of malaria)

Front 10

What is the only drug that will hit the dormant liver form of malaria? what are the bugs causing that?

**

Back 10

Primaquine


P vivax and P ovale

Front 11

is primaquine effective against blood schizonts

Back 11

NO

only good for dormant liver forms of P vivax and P ovale

Front 12

what is the radical cure for malaria?

Back 12

Primaquine Used in combo w/ blood schizonticide (usually chloroquine) to do this

Front 13

Fetus/newborns should not use primaquine..why?

Back 13

Acute hemolytic anemia
Due to glucose-6-phosphate dehydrogenase deficiency
G6PD deficiency

Front 14

What is the most common enzymatic deficiency?

Back 14

GDPD deficiency

Front 15

largest adverse effect of primaquine?

Back 15

Acute hemolytic anemia
Due to glucose-6-phosphate dehydrogenase deficiency
G6PD deficiency

Front 16

Chloroquine is what kind of drug? effective against?

Back 16

A blood schizonticide

Effective against:
Erythrocytic forms
all Plasmodia except CQ-resistant falciparum
Gametocytes

Front 17

What type of schizonts is chloroquine not effective against?

Back 17

Not effective against tissue schizonts!!

Front 18

Why is Chloroquine not used as much anymore?

Back 18

resistance

Front 19

DOC for chemoprophylaxis & acute attacks

Back 19

Chloroquine

Front 20

can Chloroquine be used in preggos/kids

Back 20

YES

Front 21

MOA for Chloroquine

Back 21

Selective toxicity
Actively concentrated in parasitized erythrocytes

Chloroquine binds to heme
prevents heme polymerization to hemozoin (an insoluble pigment)

Causes accumulation of free heme which is cytotoxic, this then kills the parasite

Front 22

most P. falciparum are resistant to what drug?

Back 22

Chloroquine

Front 23

discuss the dosage of chloroquine

Back 23

only need to dose once a week (has large volume of distribution)

must start with a loading dose (volume of distribution x target therapeutic conc)

Front 24

Rare but important adverse effects for Chloroquine?

Back 24

Acute hemolysis (G6PD deficiency)

bad with Rheumatoid arthritis as well (irreversible ototoxicity
retinopathy
myopathy
peripheral neuropathy)

Front 25

Treatment of mild to moderate acute malaria(P falciparum or P vivax) you should use...

Back 25

Mefloquine

Front 26

Mefloquine is used for ?

Back 26

Treatment of mild to moderate acute malaria(P falciparum or P vivax)
Recommended for CQ-resistant or multidrug resistant P falciparum

Front 27

what drug is Recommended for CQ-resistant or multidrug resistant P falciparum

**

Back 27

Mefloquine

Front 28

MOA for Mefloquine

Back 28

unknown

Front 29

what anti-malarial has the worst neuropsychiatric effects?

***

Back 29

Mefloquine

Front 30

this drug is associated with Confusion, dysphoria, insomnia, anxiety, vivid dreams/nightmares, depression, hallucinations
Rarely psychosis, convulsions
and is Contraindicated in pts with neurologic & psychiatric disorders

Back 30

Mefloquine

Front 31

in addition to neuro problems, what is another major contraindication for Mefloquine?

**

Back 31

Cardiovascular
Conduction abnormalities in combo w/ other drugs
Don’t use in patients taking
Beta blockers
Calcium channel blockers

Front 32

what drug can you not use in pts taking B-Blockers, Ca channel blockers?

Back 32

Mefloquine

Front 33

what do you use for hospitalized pts with severe/complicated falciparum infections...remember location

Back 33

Quinidine IV in US,

quinine outside the US

Front 34

DOC for uncomplicated CQ-resistant strains of falciparum malaria

Back 34

oral Quinine

Front 35

when you have a pt who is on Quinine for treatment of uncomplicated CQ resistant falciparum malaria.. what drug combo will you use with it? Why?


****TEST

Back 35

doxycycline or clindamycin (kids)

to shorten duration of use and limit toxicity

Front 36

QT prolongation is a side effect of what anti-malarial drug

Back 36

Quinine

Front 37

Curare-like effects is a side effect of what anti-malarial drug

Back 37

Quinine

Front 38

what drug cant you use in pts with myasthenia gravis

Back 38

Quinine

Front 39

Oxytocic (promotes rapid labor by stimulating contractions of the myometrium) is a side effect of what drug?

Back 39

Quinine

Front 40

Cinchonism (tinnitus, headache, nausea, dizziness, flushing, visual disturbances; vomiting, diarrhea, abdominal pain) is a side effect of what drug?

Back 40

Quinine

Front 41

Hypoglycemia is a side effect of what?

Back 41

Quinine

Front 42

Blackwater fever (Massive hemolysis, hemoglobinemia, hemoglobinuria, renal failure) is a side effect of what?

Back 42

Quinine

Front 43

hemolysis (G6PD deficiency) and hypoglycemia can be side effects of what?

Back 43

Quinine

Front 44

what type of drug is Pyrimethamine? what is it used in combo with

*

Back 44

A blood schizonticide:

Slow acting
Folate synthesis inhibitor
Used in combination with sulfadoxine

Front 45

what is Pyrimethamine effective against?

Back 45

P falciparum including CQ-resistant falciparum
Less active against other species

Front 46

why is Pyrimethamine given with a sufa drug? what was this drug?

Back 46

Combination is synergistic
Combination retards the emergence of drug resistance

combination with sulfadoxine

Front 47

what is presumptive treatment of febrile illness with suspected malaria?

Back 47

Pyrimethamine

Front 48

MOA for Pyrimethamine

Back 48

Inhibits plasmodial dihydrofolate reductase (DHFR)
Synergistic with sulfonamides and sulfones in sequential inhibition of folate synthesis

Front 49

why can't Pyrimethamine be used for prophylaxis

Back 49

Too toxic for prophylaxis
Hemolytic anemia and agranulocytosis (high doses)
Sulfa’s usually account for toxicities in combo preps
Hematologic, GI, CNS & renal
Dermatologic; Potentially fatal reactions including Stevens-Johnson syndrome & toxic epidermal necrolysis

Front 50

what is meant by the fact that Proguanil is a prodrug?

Back 50

requires metabolic activation

Front 51

which anti-malarial is a prodrug

Back 51

Proguanil

Front 52

MOA for Proguanil

Back 52

Inhibits dihydrofolate reductase (DHFR)
a folate synthesis inhibitor
Has both tissue and blood schizonticidal activity
No activity against hypnozoites

Front 53

atovaquone + proguanil treats what? should be avoided in who?

Back 53

Prevention and treatment of P. falciparum incl CQ-resistant and MDR strains

Avoid in pregnant females

Front 54

MOA of Atovaquone

Back 54

selectively deprives the parasite of energy by inhibiting mitochondrial electron transport

Front 55

together atovaquone + proguanil do what?

Back 55

they inhibit nucleic acid synthesis and replication

Front 56

what is a good prophylaxis for drug resistant falciparum

Back 56

Doxycycline

Front 57

what can't you use Doxycycline in?

Back 57

No kids, pregnant or lactating females, and avoid sun

Front 58

For travel to areas of risk where CQ-resistant P falciparum has NOT been reported what should you use to protect from malaria?

Back 58

chloroquine

Front 59

Travelers unable to take chloroquine can take what other 3 options?

Back 59

atovaquone + proguanil (Malarone)
doxycycline
mefloquine

Front 60

For travel in areas with risk of CQ-resistant P falciparum exist…take what 3 options?

Back 60

mefloquine
doxycycline
atovaquone + proguanil (Malarone)

Front 61

In mefloquine-resistant areas (P falciparum) take what? 2 options

Back 61

Either doxycycline or 

atovaquone + proguanil can be used

Front 62

What drug do you use:

areas with CQ-sensitive P falciparum

Back 62

cloroquine (CQ)

Front 63

What drug do you use:

areas with CQ-resistant P falciparum

Back 63

mefloquine (MQ)

Front 64

What drug do you use:

areas with MDR – P falciparum

Back 64

doxycycline

Front 65

What drug do you use:

alternative regimen to replace MQ

Back 65

atovaquone – proguanil

Front 66

What drug do you use:

terminal prophylaxis of P vivax and P ovale (when leaving area)

Back 66

primaquine

Front 67

What drug do you use:

P vivax and P ovale infections

Back 67

chloroquine then primaquine (if G6PD normal)

Front 68

What drug do you use:

CQ-sensitive P falciparum and P malariae infections

Back 68

chloroquine