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Anti-Malarial Drugs
N/A
22
Pharmacology
Graduate
03/09/2010

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Cards

Term
Which anti-malarial agents work in the RBC?
Definition
Chloroquine, Mefloquine, Quinine
Term
What is the mechanism of Chloroquine?
Definition
Weak base that becomes concentrated in the acidic digestive vacuoles of plasmodia; inhibits heme polymerization, causing a buildup of toxic heme
Term
How is Chloroquine administered?
Definition
Orally
Term
How does plasmodia develop resistance to Chloroquine?
Definition
Decreases the concentration of drug in the vacuoles, actively extrudes the drug
Term
What are the side effects of Chloroquine?
Definition
  1. Dizziness
  2. Headache
  3. Nerve deafeness
  4. Psychosis
  5. Retinal damage
  6. Rash (Steven's Johnson syndrome)
Term
Which drugs are used prophylactically?
Definition
  1. Mefloquine
  2. Doxycycline
  3. Atovaquone (+ Proguanil)
Term
What is the mechanism of Mefloquine?
Definition
Same as Chloroquine but is used prophylactically
Term
Which drug is used for Chloroquine resistant strains of plasmodia?
Definition
Quinine
Term
What is the mechanism of Quinine?
Definition
Concentrates in the vacuoles of plasmodia and alters digestion of hemoglobin, binds to DNA
Term
What are the side effects of Quinine?
Definition
  1. Fetal damage
  2. Cinchonism:
  • Blurred vision
  • Tinnitus
  • Hearing loss
  • Arrhythmias
  • GI effects
  • Increase in insulin release
  • Hemolysis in G6PD deficient patients
Term
Which agents are used to treat latent malarial infections?
Definition
Primaquine
Term
What is the mechanism of Primaquine?
Definition
Causes oxidative damage to plasmodium
Term
What are the side effects of Primaquine?
Definition
Hemolysis in G6PD deficient patients
Term
Which agents inhibit plasmodial replication?
Definition
  1. Proguanil
  2. Trimethoprim
  3. Pyrimethamine
  4. Doxycycline
Term
Sulfa drugs are often used in combination with which drugs to inhibit plasmodium replication?
Definition
Proguanil, Trimethoprim, Pyrimethamine
Term
What is Fansidar and what is it used for?
Definition

Sulfadoxine (sulfa drug) + Pyrimethamine

Inhibits plasmodium replication

Term
What is the mechanism of Atovaquone?
Definition
Inhibits electron transport in plasmodium mitochondria
Term
What are the side effects of Atovaquone?
Definition
  1. Diarrhea
  2. Fever
  3. Nausea
Term
What are the Artemisin drugs?
Definition
Artesunate, Artemether
Term
What is the mechanism of the Artemisinin drugs?
Definition
Prodrugs that are converted to active form by iron in RBCs, inhibit plasmodium Ca ATPase and form free radicals
Term
What are the side effects of the Artemisinins?
Definition
Neurotoxicity and cardiotoxicity
Term
How do Proguanil, Trimethoprim, and Pyrimethamine inhibit plasmodium replication?
Definition
Inhibit dihydrofolate reductase to prevent purine synthesis in plasmodia
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