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Pharmacology I Exam 3 > Antimalarials > Flashcards

Antimalarials Flashcards

1
Q

How is Chloroquine administered?

A

Oral

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2
Q

What is the MOA of Chloroquine?

A

Blood Schizonticide

Actively concentrated within plasmodia that reside within erythrocytes; May interfere with lysosomal degradation of Hb (reduces symptoms – “clinical cure”)

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3
Q

What are the uses of Chloroquine?

A

DOC:
P. falciparum
P. malariae (if no resistance)

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4
Q

What are the toxicities of Chloroquine?

A
  • Accumulates in melanin-rich tissues: skin, retina (ototox)
  • CNS (dizziness, HA, tinnitus)
  • Hemolysis – use caution in G6PD deficient
  • QT prolongation
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5
Q

What are contraindications of Chloroquine?

A
  • Ocular disease
  • Psoriasis
  • Porphyria
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6
Q

How is resistance developed to Chloroquine?

A

Transport pumps

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7
Q

How is Artesunate & Artemether administered?

A

Oral

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8
Q

What are the uses of Artesunate & Artemether?

A

DOC:
Chloroquine resistant
P. falciparum
P. vivax

(must be used in combination with other antimalarials - “ACT”)

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9
Q

What is the DOC for P. falciparum and P. malariae?

A

Chloroquine

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10
Q

What is the DOC for uncomplicated Chloroquine resistant malaria?

A

ACT + Atovoquone-Proquanil

OR

ACT + Lumefantrine

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11
Q

What is the 2nd DOC for uncomplicated Chloroquine resistant malaria?

A

Quinine + Doxy/Tetra/Clinda

Tetra is the preferred combo, but Clinda is used in children under 8 and pregnancy

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12
Q

What is the MOA of Sulfadoxine-Pyrimethamine + ACT

A

Sulfa inhibits PABA into folic acid

Pyrimethamine inhibits DHFR, blocking conversion of DHF to tetrahydrofolic

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13
Q

What is the use of Sulfadoxine-Pyrimethamine + ACT?

A

Prophylaxis treatment of malaria in pregnant women who reside in areas where malaria is epidemic.

DO NOT give in a pregnant woman who has active disease

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14
Q

How is resistance acquired against Sulfadoxine-Pyrimethamine?

A

Mutation in DHFR

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15
Q

What is the MOA for Atovaquone-Proquanil + ACT?

A

Atovaquone – interferes with mitochondrial electron transport and ATP pyrimidine biosynthesis

Proquanil – prodrug; converted to cycloguanil – DHFR inhibitor

Synergistic combo – effective in regions where Chloroquine resistance is high

Combined with Artesunate for rapid clearance and decrease in resistance

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16
Q

What are the uses of Atovaquone-Proquanil + ACT?

A

Uncomplicated chloroquine-resistant malaria

Prophylaxis against chloroquine-resistant P. falciparum

17
Q

What are the toxicities of Atovaquone-Proquanil + ACT?

A
  • Rash, fever

- Vomiting and diarrhea reduce absorption and efficacy, so must be discontinued

18
Q

What are the toxicities of Artemether + Lumefantrine?

A
  • Headache

- QT prolongation

19
Q

What is the DOC for complicated Chloroquine-resistance malaria?

A

Quinidine + Tetra/Doxy/Clinda

Tetra is the preferred combo, but Clinda is used in children under 8 and pregnancy

20
Q

How is Quinine and Quinidine Gluconate administered?

A

Quinine (oral); Quinidine (IV)

Given in combination with Doxy, Tetra, or Clinda

Tetra is the preferred combo, but Clinda is used in children under 8 and pregnancy

21
Q

What are toxicities of Quinine and Quinidine Gluconate?

A
  • Cinchonsim – tinnitus, HA, dizziness, flushing, visual disturbances
  • Antiarrhythmic agent – Class 1A
  • QT elongation
  • Diarrhea
  • Hemolysis in G6PD deficiency
  • Stimulates insulin release (caution in those with hypoglycemia)
22
Q

What are the uses of Mefloquine + ACT?

A

Uncomplicated Chloroquine-resistant plasmodia, but only as a LAST RESORT

23
Q

What are toxicities of Mefloquine + ACT?

A
  • Depression of myocardium
  • Seizures
  • May aggravate latent psychoses
  • Vivid dreams
  • Teratogenic
24
Q

What are contraindications to using Mefloquine + ACT?

A
  • Pregnancy
  • History of mental illness
  • Epilepsy
25
Q

What drug should not be given with Mefloquine and why?

A

Do not give with Quinine due to both having cardiac toxicity

26
Q

What is the MOA for Primaquine?

A

Tissue Schizonticide

Eliminate plasmodia from tissue and acts on hepatic stages (exoerythrocytic) – Eliminates dormant phase to prevent relapse – “radical cure”

27
Q

What are the uses of Primaquine?

A

Radical cure of P. vivax and P. ovale

28
Q

What are toxicities of Primaquine?

A
  • Hemolysis in G6PD deficiency (use low dose once daily x 8 wks)
  • Fetal hemolytic anemia
  • Teratogenic
29
Q

What are contraindications of Primaquine?

A
  • Pregnancy, breastfeeding
  • Infants < 6 months
  • SLE, RA
30
Q

What is the MOA of Tafenoquine?

A

Tissue Schizonticide

Eliminate plasmodia from tissue and acts on hepatic stages (exoerythrocytic) – Eliminates dormant phase to prevent relapse – “radical cure”

31
Q

What are the uses of Tafenoquine?

A

Prophylaxis ( > 18 years old)

Radical cure of P. vivax and P. ovale ( > 16 years old)

32
Q

What are toxicities of Tafenoquine?

A
  • Back pain, HA
  • Keratopathy
  • Teratogenic
33
Q

What are contraindications of Tafenoquine?

A
  • G6PD deficiency or unknown G6PD status

- Pregnancy

34
Q

What are the uses of Quinine?

A

Uncomplicated Chloroquine-resistant plasmodia

Pharmacology I Exam 3 (8 decks)

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