Pharmacology - Malaria Flashcards
Which kind of malaria is involved in relapses?
P. ovale
Class: Quinine aka quinidine
Quinoline derivative
Class: Chloroquine
Quinoline derivative
Class: Mefloquine
Quinoline derivative
Class: Primaquine
Quinoline derivative
MOA: Quinoline derivatives except Primaquine
Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
Therapeutic Uses: Quinoline derivatives
Prophylaxis, treatment of acute malarial attacks
MOA: Primaquine
Forms quinolone-quinone intermediates that oxidize schizont membranes
Only drug that inhibits exoerythrocytic schyzogony
What drug should you not give people with G6PD deficiency to treat malaria?
Primaquine
Hemolysis (G6PD), methemoglobinemia
Side Effects: Quinoline
Cinchonism, hypotension, hypoglycemia, abortion, arrhythmias
What is Cinchonism?
toxicity due to overdosage of cinchona alkaloids ie Quinoline; symptoms are tinnitus and slight deafness, photophobia and other visual disturbances, mental dullness, depression, confusion, headache, and nausea. Called also quininism.
Quinoloine derivatives Artemisinin compounds Antifolates Antibiotics Other Make up what kinds of drugs:
Anti-Malarial Drugs
What drug can temporarily make resistant P. falciparum sensitive to chloroquine?
Amantadine
MOA: Chloroguanide
Inhibitor of folate metabolism (dihydrofolate reductase inhibitors)
Chloroguanide (Proguanil) used in combination with Atovaquone = Malarone
MOA: Atovaquone
depolarizes parasitic mitochondria and inhibits their electron transport
Atovaquone selectively interferes with mitochondrial electron transport and related processes such as ATP and pyrimidine biosynthesis in susceptible malaria parasites. It acts selectively at the cytochrome bc1 complex of the parasite’s mitochondria to inhibit electron transport and collapse the mitochondrial membrane potential.
Chloroguanide (Proguanil) used in combination with Atovaquone = Malarone