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
MOA: Artemisinin compounds
Specifically and selectively inhibit SERCA of P. falciparum
sarco-endoplasmic reticulum ca2+ atpase
Class: Artesunate
Artemisinin compounds
Class: Artemether
Artemisinin compounds
Class: Lumefantrine
Aminoalcohol
What is the only drug that inhibits exoerythrocytic schyzogony?
Primaquine
used for prophylaxis and to prevent relapses
Drug of choice for persistent exoerythrocyticparasites after clinical cure of acute attack by P. vivax or P. ovale.
Primaquine
Side Effects: doxycycline
photosensitivity
Side Effects: Artesunate
Neurotoxocity, prolongation of QT interval
_________ is a drug of choice for suppressing acute symptoms of P. malariae.
Chloroquine
_______ is the only drug that destroys the late hepatic stages and latent tissue forms of P. vivax and P. ovale.
Primaquine
use to prevent relapses
MOA Proguanil
inhibits dihydrofolate reductase
antimalarial
part of Malarone