Antimalarials Flashcards
Quinoline derivatives?
Quinine, Chloroquine, Hydroxychloroquine, Mefloquine, Primaquine
Quinine is also called?
Quinidine (used in anti-arrhythmias)
Quinoline derivative mxn?
Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yeilding oxidative damage to membranes and digestive proteases. Primaquine is unique in that it inhibits exoerythrocytic schyzogony by forming quinoline-quinone intermediats that oxidize schizont membranes
Quinoline derivatives for?
Prophylaxiws, treatment of acute malarial attacks
Quinine side effects?
Cinchonism, hypotension, hypoglycemia, abortion, arrythmias
Chloroquine side effects?
Itching (Africans), retinitis (rare)
Primaquine side effects?
Hemolysis (G6PD), methemoglobinemia, fever, N/V
Hydroxychloroquine is?
Quinoline derivative
Mefloquine is?
Quinoline derivative
Chloroguanide class and mxn?
Antifolate, Dihydrofolate reductase inhibitor
AKA Proguanil?
Chloroguanide
Chloroguanide used exclusively with?
As combination therapy: Chloroguanide (Proguanil with Atovaquone)
Atovaquone class and mxn?
Napthalene, Depolarizes parasitic mitochondria and inhibits their electron transport
Atovaquone + Chloroguanide (Proguanil) used for?
Prophylaxis and treatment of malaria due to P. falciparum, including chloroquine-resistant strains
Major resistance amongst P. falciparum to this quinoline derivative?
Chloroquine
Artesunate class and mxn?
Artemisinin compound, specifically and selectively inhibits SERCA of P. falciparum
Artesunate side effects?
Neurotoxicity, QT prolongation
Artemether class and mxn?
Artemisinin compound, specifically and selectively inhibits SERCA of P. falciparum
Artemisinin compounds?
Artesunate, Artemether
AKA benflumetol?
Lumefantrine
AKA Lumefantrine?
Benflumetol
Lumefantrine class?
Aminoalcohol
Lumefantrine used in combo with?
Artemether (“coartemether”)
Prophylaxis in chloroquine-sensitive zone?
Chloroquine
Prophylaxis in chloroquine-resistant zone?
Mefloquine, Doxycycline, Atovaquone/Proguanil
Mefloquine-resistant zone?
Doxycycline, Atovaquone/Proguanil
Terminal prophylaxis?
Primaquine
Antibiotics used to treat malaria?
Tetracycline, Clindamycin, Doxycycline
Antibiotics treat what?
Severe malaria and chloroquine-resistant uncomplicated malaria
Doxycycline side effect?
Photosensitivity
Amantadine mxn?
Positive charge helps chloroquine overcome chloroquine-resistant malaria vacuoles; pt mutations against amantadine return bacteria to chloroquine-sensitivity
Tx of severe malaria?
IV quinidien gluconate + antibiotic; IV artesunate followed by atovaquone-proguanil, doxycycline (clindamycin in pregnant woman), or mefloquine; blood transfusion
Use for “radical cure” of acute attack of P. vivax or P. ovale?
Primaquine phosphate
Has P. malaria developed resistance to chloroquine?
No
Has P knowlesi developed resistance to chloroquine?
No
Tx of uncomplicated malaria in P. falciparum, P. malariae, or P. knowlesi?
Chloroquine phosphate (or hydroxychloroquine)
Tx of uncomplicated malaria in chloroquine-sensitive P. vivax or P. ovale?
Chloroquine phosphate + Primaquine phosphate (or Hydroxychloroquine + Primaquine phosphate)
Tx of uncomplicated malaria in P. falciparum?
Atovaquone-Proguanil (or Artemether-Lumefantrine, Quinine sulfate + Antibiotic, Mefloquine)
Has P. falciparum developed resistance to chloroquine?
Yes
Has P. vivax developed resistance to chloroquine?
Some strains have
Tx of uncomplicated malaria in chloroquine-resistane P. vivax?
Quinine sulfate + Doxycycline or Tetracycline + Primaquine phosphate (or Atovaquone-proguanil + Primaquine phosphate, Mefloquine + Primaquine phosphate)
