Antimalarials Flashcards

1
Q

P. Falciparum

A

Malignant tertian malaria. Most lethal. Fever occurs every third day. No secondary tissue forms. Cerebral malaria. Has many drug resistant forms.

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2
Q

P. Vivax

A

Benign tertian malaria. Fever occurs every third day. Has dormant forms in the liver (hypnozoites). Relapses for months/years. Duffy antigen was thought to be protective but isn’t.

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3
Q

P. ovale

A

Rare. Has secondary tissue forms in the liver (hypnozoites). Relapses.

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4
Q

P. Malariae

A

Quartan malaria. Fever occurs every four days. No tissue forms but can cause chronic infection.

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5
Q

Blood Schizonticides

A

Act on RBC forms. Provide a clinical cure for vivax and ovale and a radical cure for malariae and faliparum.

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6
Q

Tissue schizonticides

A

Act on the hepatic stages. Doesn’t effect the symptoms. Kill vivax and ovale to prevent relapse.

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7
Q

Gametocidal agents

A

Eliminate proliferation. Doesn’t cure the disease just sloes the spread.

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8
Q

Malaria DOC

A

Chloroquine

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9
Q

Chloroquine (aralen) resistance

A

especially falciparum due to efflux pumps.

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10
Q

Chloroquine MOA

A

Actively concentrate in plasmodia food vacule where they interfere with the degradation of hemoglobin producing a toxic by product.

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11
Q

Chloroquine kinetics

A

Oral. accumulates in melanin-rich tissue. metabolized by CYP3A4.

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12
Q

Cholorquine toxicity

A

retinal/corneal toxicity, ototoxicity, hemolysis (G6PD deficiency), QT prolongation.

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13
Q

Cholorquine contraindications

A

psoriasis and porphyria.

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14
Q

Mefloquine (Lariam) uses

A

Second-line drug for cholorquine-resistant strains.

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15
Q

Mefloquine toxicity

A
  1. ) depression of the myocardium, potential cardiac toxicity. (don’t combine with quinine).
  2. ) seizures and aggravation of latent psychoses.
  3. ) sleep and behavioral disturbances, vivid dreams
  4. ) teratogenic
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16
Q

Mefloquine contraindications

A

history of mental illness or epilepsy and pregnancy

17
Q

Quinine/Quinidine Gluconate uses

A

DOC for complicated chloroquine-resistant plasmodia and for unconscious patients.

18
Q

Quinine/Quinidine Gluconate kinetics

A

quinine=oral quinidine gluconate=IV. Combined with doxycycline or clindamycin to decrease the length of treatment.

19
Q

Quinine/Quinidine Gluconate toxicity

A

Cinchonism (tinnitus, HA, dizziness, flushing, visual distrubances), antiarrhythmis agent, QT prolongation, Hemolysis (G6PD deficiency)

20
Q

Doxycycline uses

A

combined with Quinine/Quinidine Gluconate to treat complicated choloroquine-resistant strains.

21
Q

Fansidar

A

pyrimethamine+sulfadoxine. Not available in the US

22
Q

Fansidar uses

A

presumptive treatment and acute attacks. especially used in affected areas for pregnant women and children.

23
Q

Malarone

A

atovaquone+proguanil. Synergistic combo effective in regions with high resistance

24
Q

Atovaquone MOA

A

Interferes with mitochondrial processes like the ETC/ATP and pyrimidine biosynthesis.

25
Q

Malarone uses

A

Active against blood and tissue forms.

26
Q

Artemisinin (Qinghaosu)

A

Most rapid action against falciparum. Not on US market.

27
Q

Artemeter/lumefantrine (Coartem)

A

Available in the US for cholorquine resistant falciparum and vivax

28
Q

Coartem toxicity

A

Prolonged QT (don’t use in patients with cardiac disease).

29
Q

Primaquine

A

Only tissue schizonticide. Active against vivax and ovale for a radical cure.

30
Q

Primaquine contraindications

A

G6PD deficiency, SLE, RA, pregnancy (due to unknown fetal G6PD status)

31
Q

DOC for sensitive plasmodia

A

chloroquine or hydroxycholorquine

32
Q

DOC for cholorquine resistant falciparum

A
  1. ) quinine with doxycycline or clindamycin
  2. ) Mefloquine
  3. ) Malarone
  4. ) Coartem
33
Q

DOC for severe malaria

A
  1. ) Quinidine with doxycycline or clindamycin

2. ) Artemisinin combo therapy

34
Q

DOC for vivax or ovale

A

Always given primaquine to prevent relapse plus:

  1. ) choroquine
  2. ) quinine with doxycycline or clindamycin
  3. ) Mefloquine
  4. ) Malarone