Pharmacology of Antimalarials Flashcards
What is the MOA of Chloroquine?
Prevents the polymerization of heme to hemozoin. The accumulation of heme is toxic to the parasite
Describe the PK of Chloroquine.
PO administration, large Vd, longer half-life
What ADRs are associated with Chloroquine?
GI irritation, blurry vision, headache. High doses can cause irreversible eye and ear damage and myocardial depression
What ADRs are associated with Quinine?
Chinchonism, hemolysis, hypotension, QT prolongation, Blackwater fever
Describe the PK of Quinine.
PO administration, short half-life, Narrow TI
What is the first-line malarial prophylaxis in areas with resistant P. falciparum?
Mefloquine
Describe the PK or Mefloquine.
PO only, long half-life with weakly dosing
What anti-malarial drug accumulates to release toxic free radicals?
Artemisinin
Describe the PK of Artemisinin.
Very short half-life, rapid-acting
What is the only drug against quinine-resistant malaria strains?
Artemisinin
What is the most common adverse effect of Artemisinin?
GI discomfort
True/False. Artemisinin is used as a monotherapy for quinine-resistant malaria.
False. Artemisinin is never used as a monotherapy. Standard treatment combine Artemisinin with another anti-malarial drug
What anti-malarial is effective against all stages of the malaria parasite in the human body?
Primaquine & Tafenoquine
What drug should be used to prevent the relapse of a malaria infection?
Primaquine since it is effective against the gametocyte stage
Primaquine is generally well-tolerated, but is contraindicated/should be avoided in what patients?
GP6D deficiency, pregnancy
