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Pharmacology Exam 3 (Lauren) > Antimalarial Agents > Flashcards

Antimalarial Agents Flashcards

1
Q

What are the 4 plasmodia species that are known to infect humans?

A

Falciparum

Vivax

Ovale

Malariae

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2
Q

Which two plasmodium species go dormant in the liver?

A

Vivax

Ovale

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3
Q

What are hypnozoites?

A

Dormant liver stage of vivax and ovale

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4
Q

Are falciparum and malariae ever dormant?

A

No

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5
Q

What is meant by secondary tissue forms of malaria?

A

It means the dormant liver phase

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6
Q

What does a clinical cure do?

A

Eradicates erythrocytic forms of the parasite

Secondary tissue forms in the liver not affected

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7
Q

What is a radical cure?

A

Eradicates all forms of the parasite, including secondary tissue forms

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8
Q

What do blood schizonticides do?

A

Give a “clinical cure” by acting on the erythrocytic form of the parasite

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9
Q

What do tissue schizonticides do?

A

Eliminate the hepatic stages of the parasite, and prevent relapses from vivax and ovale

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10
Q

Will tissue schizonticides suppress symptoms once erythrocytic stages have been established?

A

No

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11
Q

What is the most effective way to control malaria?

A

Don’t get bit by mosquitos

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12
Q

What 3 things do you need to take into consideration when choosing a treatment for your pt’s malaria?

A
  1. What species do they have?
  2. Do they have complicated or uncomplicated malaria: oral v parenteral
  3. Drug susceptibility of the infecting parasite (what area did they get it in, were they on chemoprophylaxis)
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13
Q

What are the blood schizonticides?

A

Chloroquine and hydroxychloroquine

Quinine sulfate and quinidune gluconate

Doxycycline and clindamycin

Artemisinin- artesunate OR artemether can be COMBINED with:
Atovaquone-proguanil
Lumefantrine
Pyrimethamine-sulfadoxine
Mefloquine
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14
Q

If there is no resistance, what is the DOC for a blood schizonticide?

A

Chloroquine

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15
Q

What is the main way malaria becomes resistant to chloroquine?

A

Transport pump

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16
Q

Can chloroquine be used prophylactically?

A

Yes, for organisms that are sensitive

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17
Q

What is the MOA of chloroquine?

A

It gets concentrated inside the parasite that is inside a RBC. Then it keeps the bug from degrading hemoglobin

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18
Q

How is chloroquine administered

A

Orally

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19
Q

In what tissues does chloroquine accumulate, and what are the side effects this causes?

A

Melanin-rich tissues: skin and retina

Causes skin discoloration and eye damage

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20
Q

How often do you need to administer chloroquine for prophylaxis?

A

Once a week (long duration of action)

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21
Q

What are the main toxicities of chloroquine?

A

QT prolongation

Eye and ear toxicity

Hemolysis-caution in G6PD patients

Exacerbates psoriasis and porphyria

22
Q

Who is chloroquine contraindicated for?

A

Psoriasis

Porphyria

23
Q

Which malaria drugs have the most rapid action?

A

The Artemisinins: artesunate and artemether

24
Q

Why do you always combine the Art drugs with other antimalarials?

A

They have a very quick clearance, so any leftover malaria needs to be knocked out with another drug

25
Q

What is the difference between artemisinin, artesunate, and artemether?

A

Artesunate and artemether and derivatives of artemisinin that have higher potency and bioavailability

26
Q

When do we use ACT (artemisinin combination therapy)?

A

For chloroquine-resistant falciparum and vivax

27
Q

Which ACT combos do we use first and are equally recommended?

A

Artesunate+ atovoqione-proguanil

Artemether+ lumefantrine

28
Q

Which ACT combo is a drug of last resort?

A

Artesunate+ mefloquine

29
Q

Which ART combo is reserved for pregnant women or IPT?

A

Artesunate+ sulfadoxine-pyrimethamine

30
Q

Which drugs inhibit folate metabolism?

A

Proguanil

Pyrimethamine+sulfadoxine

31
Q

How does malaria develop resistance to proguanil and pyrimethamine+sulfadoxine?

A

Mutations in DHFR (dihydrofolate reductase)

Remember, they inhibit folic acid metabolism

32
Q

Why do we combine atovaquone and proguanil?

A

They have a synergistic effect!
Proguanil-targets folate via DHFR

Atovaquine- interferes with ATP

PLUS we then combine it with artesunate for rapid clearance and decrease in resistance

33
Q

What do we have to give with proguanil when we give it to pregnant women?

A

Leucovorin, so that we can rescue the folate

34
Q

What are the main side effects of lumefantrine+ artemether?

One of the main treatments for chloroquine resistant malaria

A

Headache in 56%

QT prolongation***

35
Q

When would we use quinine and quinidine?

A

Complicated, chloroquine resistant malaria

VERY TOXIC

36
Q

What do we have to combine quinine or quinidine gluconate with?

A

Doxycycline, tetracycline, or clindamycin
(Clindamycin is the only one safe for kids and pregant women)

By combining it with one of these, we reduce the length or treatment, and therefore, adverse side effects

37
Q

What is the difference between quinine and quinidine?

A

Quinine-oral

Quinidine- oral AND IV- comatose pt gets IV quinidine

38
Q

Quinine and quinidine are VERY TOXIC! What are the main toxicities?

A

Cinchonism (tinnitus, headache, dizziness, flushing, visual disturbances)

Antiarrythmic agent class 1A (quinidine only)

QT elongation (careful combining w mefloquine)

39
Q

If a pregnant woman has chloroquine-resistant malaria, what do we have to avoid?

A

Quinine+ doxycycline/tetracycline

Mefloquine

Primaquine (tissue schizonticide)

(If giving proguanil, you must also give leucovorin to rescue folate)

40
Q

What forms of malaria does mefloquine act on?

A

Erythrocytic

41
Q

Is mefloquine a drug of absolute last resort?

A

Yes, it is toxic to another level

42
Q

What are the main toxicities of mefloquine?

A

Depression of heart muscle (DON’T COMBINE with quinine)

Seizures

PSYCHOSIS**

Vivid dreams

43
Q

Who should you never ever ever ever give mefloquine to?

A

history of mental illness

History of epilepsy

Pregnant

44
Q

What drug is used for empiriacla treatment and preventative intermittent therapy in pregnant women?

A

Pyrimethamine+sulfadoxine

(Combined with artesunate)

Prevents spread from mom to baby

45
Q

What forms of malaria is primaquine active against?

A

Tissue forms (it is a tissue schizonticide)

46
Q

Can we use primaquine + a blood schizonticide as as radical cure/terminal prophylaxis?

A

Yes

47
Q

What are the main toxicities of primaquine?

A

Hemolytic anemiaespecially if G6PD deficient**

48
Q

Who should we NOT give primaquine to?

A

Pregnant women

Infants under 6 months

Breastfeeding women

G6PD deficient with extreme caution

49
Q

Do pregnant moms get radical cures for malaria?

A

No, they can get clinical cure until the baby is delivered. We can’t give them primaquine due to the huge risk of fetal hemolytic anemia. (We don’t know if the baby is G6PD deficient)

50
Q

What is the MOA of chloroquine?

A

It accumulates in the plasmodia and causes hemoglobin to accumulate, which is toxic

50
Q

Are there a lot of side effects for atovaquone + proguanil?

A

No because it is a new drug

Pharmacology Exam 3 (Lauren) (8 decks)

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