Anti-Malarials Flashcards
Quinine (Qualaquin)
Class: Quinolone Derivative
Mechanism: Accumulate in parasite’s food vacuole disrupt heme polymerization to hemozoin yielding oxidative damage to membranes and digestive proteases.
Thera: Prophylaxis and treatment of acute malarial attacks.
Tox:Cinchonism, hypotension, hypoglycemia, abortion, arrhythmias
Misc: Also called quinidine (used in anti-arrhythmias)
Chloroquine
Class: Quinolone Derivative
Mechanism: Accumulate in parasite’s food vacuole disrupt heme polymerization to hemozoin yielding oxidative damage to membranes and digestive proteases.
Thera: Prophylaxis and treatment of acute malarial attacks.
Tox: Itching (Africans)
Retinitis (rare)
Hydroxychloroquine
Class: Quinolone Derivative
Mechanism: Accumulate in parasite’s food vacuole disrupt heme polymerization to hemozoin yielding oxidative damage to membranes and digestive proteases.
Thera: Prophylaxis and treatment of acute malarial attacks.
Mefloquine
Class: Quinolone Derivative
Mechanism: Accumulate in parasite’s food vacuole disrupt heme polymerization to hemozoin yielding oxidative damage to membranes and digestive proteases.
Thera: Prophylaxis and treatment of acute malarial attacks.
Primaquine
Class: Quinolone derivative
Mech: Forms quinolone-quinolone intermediates that oxidize schizont membranes
Thera: Prophylaxis, treatment of acute malarial attacks
Tox: Hemolysis (G6PD), methemoglobinemia
Fever, nausea vomiting
Misc: Only drug that inhibits exoerythrocytic schyzogony
Amantadine
Class: N/A
Mech: Positive charge helps chloroquine overcome chloroquine-resistant malaria vacuoles; point mutations against amantadine return bacteria to chloroquine-sensitivity
Thera: N/A
Tox: N/A
Artesunate
Class: Artemisinin compound
Mech: Specifically and selectively inhibit SERCA of P. falciparum
Thera: N/A
Tox: Neurotoxicity, prolongation of QT interval
Artemether
Class: Artemisinin compound
Mech: Specifically and selectively inhibit SERCA of P. falciparum
Thera: N/A
Tox: N/A
Lumefantrine
Class: Aminoalcohol
Mech: N/A
Thera: Used in combination w/artemether (called Coartem)
Tox: N/A
Misc: AKA benflumentol
Atovaquone
Class: Napthalene
Mech: Depolarizes parasitic mitochondria and inhibits their electron transport.
Thera: Used in combo with proguanil
Tox: N/A
Chloroguanide
Class: Antifolates
Mech: Dihydrofolate reductase inhibitors (human and parasite pathway)
Thera: N/A
Tox: Rare
Misc. Also called proguanil
Tetracycline
Class: Antibiotic
Mech: N/A
Thera: Severe malaria and chloroquine resistant uncomplicated malaria
Clindamycin
Class: Antibiotic
Mech: N/A
Thera: Severe malaria and chloroquine resistant
Doxycycline
Class: Antibiotic
Mech: N/A
Thera: Severe malaria and chloroquine resistant
Tox: Photosensitivity