Antimalarials Flashcards

1
Q

What are the antimalarials

A
Chloroquine
Quinidine
Quinine
Mefloquine
Primaquine
Atovaquone
Proguanil
Pyrimethamine
Sulfadoxine
Doxycycline
Artemisinins
Halofantrine
Lumefantrine
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2
Q

DOC Tx and prophylaxis Vivax and Ovale, uncomplicated Falciparum

A

Chloroquine

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3
Q

DOC severe Falciparum

A

Quinidine
Quinine
Artemisinins (IV)

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4
Q

Pregnant prophylaxis against Chloroquine-resistant

A

Mefloquine

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5
Q

DOC dormant liver form eradication

A

Primaquine

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6
Q

Tx and Prophylaxis uncomplicated Falciparum

A

Atovaquone

Proguanil

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7
Q

Can cause Cinchonism

A

Quinidine

Quinine

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8
Q

Great for blood schizonts, but not liver

A

Chloroquine
Quinidine
Quinine

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9
Q

Safe in pregnancy

A
Chloroquine
Quinidine
Quinine
Mefloquine
Atovaquone
Pyrimethamine
Proguanil
Sulfadoxine
Artemisinins
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10
Q

Contraindicated in pregnancy

A

Primaquine

Doxycycline\Halofantrine

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11
Q

How does Chloroquine work

A

Raises internal pH of parasite
Interfere with Hb metabolism to hemozoin
Lysis of parasite and RBC

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12
Q

Who do you not give Chloroquine to

A

G6PD deficiency
Psoriasis
Porphyria
Retinal/Visual field abnormalities

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13
Q

How does Chloroquine resistance arise

A

Mutation in Falciparum putative transporter (PfCRT)

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14
Q

When can you give Chloroquine for Falciparum

A

Uncomplicated disease

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15
Q

Chloroquine AE

A

Pruritis
N/V
Abdomenal pain
HA, anorexia, malaise, urticaria

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16
Q

What is the most important Chloroquine AE

A

Retinopathy

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17
Q

What should you combine with Doxycycline for severe Falciparum

A

Quinidine

Quinine

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18
Q

How do the Quinidines work

A

Decreased O2 and CHO metabolism

Intercalates DNA

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19
Q

What do you not combine Quinidines with

A

Mefloquine

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20
Q

Quinidine drug interactions

A

Increase serum Warfarin and Digoxin

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21
Q

Where is Quinidine resistance rising

A

SE Asia

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22
Q

What are the Quinidine AE

A
QT prolongation
Blackwater fever
HS
Heme disturbance
Hypoglycemia (increases insulin)
Uterine contraction
Hypotension
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23
Q

What is Blackwater Fever

A

RBC hemolysis releasing Hb into blood and urine

Leads to kidney failure

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24
Q

Useful for mild/moderate Chloroquine resistant strains

A

Mefloquine

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25
Q

How does Mefloquine work

A

Destroys asexual blood forms

26
Q

Why don’t you combine Mefloquine and Quinidines

A

Chemically related, so similar resistances

27
Q

When should you discontinue Quinidines in pregnancy

A

If there’s hemolysis

28
Q

Who should avoid Quinidines

A

Visual/Auditory/Cardiac problems

29
Q

When is Mefloquine contraindicated

A

Epilepsy, psych problems

Arrhythmia, drug sensitivities

30
Q

What is the main Mefloquine AE

A

Neuropsychiatric toxicity

31
Q

What are the high dose Mefloquine AE

A
Leukocytosis
Thrombocytopenia
Aminotransferase elevation
Arrhythmias
Bradycardia
32
Q

What else do you not give Mefloquine with

A

Halofantrine

33
Q

What is Malarone

A

Atovaquone + Proquanil

34
Q

How does Malarone work

A

Disrupts Mito ETC

35
Q

What are the Malarone AE

A

Gi upset
HA
Rash

36
Q

Which schizonts is Malarone effective against

A

Tissue, RBC

37
Q

What are the inhibitors of Folate Synthesis

A

Pyramethamine
Proguanil
Sulfadoxine

38
Q

What are the Folate Synthesis inhibitors good for

A

Chemoprophylaxis

Intermittent prevention in high risk pts

39
Q

What can you give for mild/moderate Chloroquine-resistant falciparum

A

Pyrimethamine

Sulfadoxine

40
Q

Which Folate Synthesis inhibitor is slow against RBC form

A

Pyrimethamine + Proguanil

41
Q

Which Folate Synthesis inhibitor is good for some hepatic forms

A

Proguanil

42
Q

Which Folate Synthesis inhibitor is good for RBC forms

A

Sulfadoxine

43
Q

What does Sulfadoxine inhibit

A

Dihydropteroate reductase

44
Q

What does Pyrimethamine + Proguanil inhibit

A

DHF reductase

45
Q

Folate Synthesis inhibitor AE

A

GI problems
Rash
Itching

46
Q

Proguanil AE

A

Mouth ulcers

Alopecia

47
Q

Pyrimethamine + Sulfadoxine AE

A

Erythema multiforme

Stevens-Johnson syndrome

48
Q

Sulfadoxine toxicities

A
Hematological
GI
CNS
Derm
Renal
49
Q

What is an alternative to Doxycycline

A

Clindamycin

50
Q

What are the Doxycycline AE

A
Photosensitivity
Discoloration and Hypoplasia of teeth
Growth stunting
GI upset
Vaginal candidiasis
Hepatotoxicity in pregnancy
51
Q

Works on RBC stage of all parasites

A

Halofantrine

Lumefantrine

52
Q

What are the Artemisinins

A

Artesunate
Artemether
Dihydroartemisinin

53
Q

What is Coartem

A

Artemether + Lumefantrine

54
Q

How do the Artemisinins work

A

Bind Fe
Break down peroxide bridges
Create free radicals

55
Q

Should not be used as monotherapy

A

Artemisinins

56
Q

What are the Artemisinin AE

A

Neurotoxicity

QT prolongation

57
Q

Do Artemisinins work on liver stage

A

No

58
Q

What is the Halofantrine AE

A

Cardiac toxicity

59
Q

How is Lumefantrine given

A

Only as Coartem

60
Q

What is the Lumefantrine AE

A

QT prolongation (Clinically insignificant)

61
Q

Why don’t you give Artemisinins for prophylaxis

A

Short t1/2