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Multisystem Part 2 > Anti-malarials > Flashcards

Anti-malarials Flashcards

1
Q

which species causes the most mortality and morbidity?

A

falciparum

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2
Q

which species can cause relapse?

A

vivax and ovale

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3
Q

which species only infects OLD senescent RBCs (smoldering subclinical/late presentation infection)

A

malariae

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4
Q

4 classes of antimalarials

A

quinolones
antifolates/sulfa
antibiotics
artemisinins

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5
Q

quinoline and quinoline-like class of antimalarials

A

disrupts heme polymerization –> parasites due eat Hgb and die from their own waste products

quinine, quinidine, choroquine, hydroxychloroquine, mefloquine, lumefantrine, primaquine

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6
Q

which two quinolines are used as prophylais

A

chloroquine and mefloquine

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7
Q

which quinoline can be used as PART or radical cure?

A

primaquine

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8
Q

parenteral quinine/quinidine

A

used for severe falciparum infections

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9
Q

how to treat uncomplicated falciparum?

severe falciparum?

A

uncomplicated = oral quinine + doxy/clindamycin

severe = parenteral quinine/quinidine

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10
Q

side effects of quinine and quinidine

A

Cinchonism: tinnitus, headache, nausea, bitter taste

arrythmias/prolonged QTc interval/torsades

Induce insulin secretion –>hypoglycemia

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11
Q

chloroquine

A

therapy and chemoprophylaxis

used for a while so now lots of resistance –> can only be used in central america, haiti and dominican rep. for falciparum

usually vivax, ovale, and malariae are sensitive still

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12
Q

what drug is falciparum ussually resistant to?

A

chloroquine

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13
Q

mefloquine

A

long half life - good for bad adherence
use for chloroquine resistant falciparum
also chemoprophylaxis

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14
Q

what drug to use for chloroquine resistant falciparum

A

mefloquine

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15
Q

mefloquine side effects

A

cardiotoxic - dont use with conduction abnormalities

neuropsychiatric side effects/vivid dreams, tics, and motor disorders

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16
Q

what drug should be used as prophylaxis for long term travelers and pregnant women?

A

mefloquine

LONG HALF LIFE

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17
Q

PfMDR1

A

plasmodium falciparum multidrug resistance protein1

efflux pump for mefloquine, quinine, and quinidine

RESISTANCE!!

18
Q

primaquine

A

used for radical cure and PART (presumptive anti-relapse therapy)

FDA label at 15 mg –> use at 30 mg (higher dose!)

19
Q

PART

A

presumptive anti-relapse therapy
Prevention of relapses “only for persons who have had prolonged exposure in malaria-endemic areas (e.g., missionaries and Peace Corps volunteers).”

primaquine!

20
Q

primaquine side effect

A

can trigger hemolysis in G6PD deficiency individuals

test for G6PD before you prescribe primaquine!!

21
Q

test for ____ before you prescribe primaquine!!

A

G6PD deficiency

due to hemolysis

22
Q

pregnant patients with vivax and ovale infections should be _____

A

maintained on chloroquine prophylaxis for the duration of their pregnancy

23
Q

anti-folates/sulfa derivatives antimalarial class

A

Antifolates = Proguanil or Pyrimethamine

Sulfa = Sulfadoxine or Trimethoprim

prototypical drug = sulfadoxine-pyrimethamine

Mechanism: Inhibit Dihydropteroate synthase (DHPS) or dihydrofolate reductase (DHFR) –> nucleic acid synthesis

24
Q

IPT

A

intermittent preventative treatment
for pregnant women

empiric therapy Used in high malaria transmission regions

Single dose sulfadoxine-pyrimethamine in Africa
Still effective but becoming controversial due to widespread resistance

25
Q

atovaquone - proguanil

A

Inhibits parasite mitochondrial electron transport

USed for both therapy and prophylaxis

Causal prophylaxis (blood and liver stage)
Well tolerated, take with food/milk to enhance absorption

Single point mutation in the parasite cytochrome b gene confers resistance to atovaquone-proguanil
If used widespread in endemic setting resistance will rapidly emerge

a DAILY med

26
Q

ANTIBIOTIC ANTIMALARIALS

A

Doxycycline, tetracycline, clindamycin, azithromycin, fluoroquinolones

only kills in blood stage
Target ribsomal function within the apicoplast organelle

Doxy/tetra/clinda used in conjunction with quinine

27
Q

artemisinins

A

plant derived

artemether; arteether; artesunate; dihydroartemisinin

broad asexual effects –> blood stages (rings-schizonts), rapid effect

mechanism: endoperoxide –> free radicals

28
Q

Artemisinin Combined Therapy (ACT)

A

2 drugs with different mechanisms
for Efficacy and reduce resistance

Artemether-lumefantrine
1st line for uncomplicated Pf in most of the world

29
Q

Artemether-lumefantrine

A

an artemisinin + quinoline

1st line therapy ACT

30
Q

artesunate

A

for severe malaria, not FDA approved

31
Q

why are artemisinins more potent?

A

because of broader activity across the asexual life cycle of malaria

more rapid clearance across whole lifecycle

32
Q

presentation of uncomplicated vs severe malaria

A

Uncomplicated Malaria = Fever, Chills, Headache. Myalgias, Diarrhea, Mild-mod anemia, Mild-mod thrombocytopenia
Tolerates oral medications

Severe Malaria = Cerebral malaria, confusion, coma, seizure, Hypoglycemia (10%

33
Q

CDC criteria for severe malaria

A

> 5% parasitemia

HgB

34
Q

recommended for uncomplicated faciparum

A

artemether - lumefantrine

atovaquone - proguanil

quinine sulfate + doxy or clindamycin

35
Q

recommended for severe falciparum

A

IV artesunate (1st line)
or
IV quinine

36
Q

radical cure for relapsing malaria? (vivax or ovale)

A

choroquine (or any other effective regimen) + primaquine

37
Q

malaria therapy in preganancy

A

quinine + clindamycin (1st sem)
or
mefloquine
or ACT (2/3rd sem)

38
Q

always ____ patients with falciparum

A

ADMIT to ensure response to therapy

39
Q

travelers should treaT clothes with…

A

permethrin

40
Q

neuropsychiatric side effects associated with…

A

mefloquine

usually not recommended

Multisystem Part 2 (20 decks)

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