pharm malaria drugs

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USUHS14
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152404
Filename:
pharm malaria drugs
Updated:
2012-05-05 21:00:51
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pharm malaria drugs
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pharm malaria drugs
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  1. Quinine
    • Group: Arylaminoalcohol
    • Use: oral for uncomplicated, iv for complicated
    • Mechanism of action: inhibits heme polymerization and toxic heme concentrations kill the parasite
    • Adverse effects: Prolonged QT; hypoglycemia; thrombocytopenia; cinchonism; 'blackwater fever'
    • Pharmacokinetics: metabolized by CYP450
    • Resistance in SE Asia
  2. Quinidine
    • Group: Arylaminoalcohol
    • Use: oral for uncomplicated, iv for complicated
    • Mechanism of action: inhibits heme polymerization and toxic heme concentrations kill the parasite
    • Adverse effects:
    • Prolonged QT; hypoglycemia; thrombocytopenia; cinchonism; 'blackwater fever'
    • Pharmacokinetics: metabolized by CYP450; inhibits CYP2D6
    • Resistance in SE Asia
  3. Mefloquine
    • Group: Arylaminoalcohol
    • Use: oral only; prophylaxis or treatment of uncomplicated malaria
    • Mechanism of action: inhibits heme polymerization and toxic heme concentrations kill the parasite
    • Adverse effects: cardiotoxicity; sleep disturbances; neuro-psych concerns (not given to pilots)
  4. Chloroquine
    • Group: 4-aminoquinolines
    • Uses: prophylaxis; kills blood stage parasites
    • Mechanism: inhibits heme polymerization and toxic heme concentrations kill the parasite
    • Adverse effects: mild GI disturbance; retinal damage at high/prolonged doses; seizures; nerve type deafness
    • Pharmacokinetics: prodrug; rapidly & completely absorbed; long elimination half life; better tolerated than quinine
    • P. falciparum is resistant
  5. Primaquine
    • Group: 8-aminoquinolines
    • Use: hypnozoites in liver; terminal prophylaxis
    • Mechanism: unknown
    • Adverse effects: contraindicated in G6PD deficiency, pregnancy, and young children
  6. Doxycycline
    • Group: Antibiotics
    • Uses: blood stage Tx; prophylaxis of MDR malaria; always used in combination
    • Mechanism: inhibits protein synthesis
    • Adverse effects: interfere with bone an tooth development - contraindicated in pregnancy and young children; esophageal ulcers
  7. Atovaquone
    • Uses: (in combination with Proguanil) uncomplicated MDR P. falciparum; prophylaxis
    • Mechanism: inhibits mitochondrial electron transport at cytochrome bc1 complex
    • Adverse effects: nausea, vomiting, abdominal pain
    • Pharmacokinetics: oral absorption inc. by food; not metabolized
  8. Proguanil
    • Uses: (in combination with atovaquone) uncomplicated MDR P. falciparum; prophylaxis
    • Mechanism: DHFR inhibitor
    • Adverse effects: granulocytopenia and aplastic anemia
    • Pharmacokinetics: Oral absorption inc. by food; metabolized by CYP2D19 (10% of caucasians and 25-30% of Africans are poor metabolizers)

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