Flashcards in Antiparasitics Deck (19):
Why is malaria difficult to target?
Undergoes gross changes in morphology, localisation and metabolic pathways.
Organic arsenical against trypanosomes. Inhibits lipoic-dependent and other dithiol containing Metallo-enzymes. Actively accumulated in trypanosoma.
Anti-trypanosomal without toxic metal atom. Cannot cross BBB so only effective in early stages.
Antimalarial. Inhibits the formation of hemozoin either by inhibiting polymerase or through complexation of heme.
Anti malarial anti metabolite. Inhibits folate synthesis pathway. Inhibits DHPS.
Anti malarial anti metabolite. Inhibits folate synthesis pathway. Inhibits DHFR.
Anti malarial anti metabolite. Inhibits folate synthesis pathway. Inhibits DHPS and DHFR. Combination drug.
What are helminths?
Multicellular eukaryotes such as nematodes (roundworms).
What are Protozoa?
What are the main targets of anti-helmintics?
Energy metabolism, neuromuscular coordination and micro tubule dynamics.
Antihelmentic that targets energy metabolism. Uncoupled oxidative phosphorylation.
Antihelmentic that targets energy metabolism. Inhibits glycolysis.
Block microtubule dynamics in helminths. Bind to beta-tubulin in tubular dimer and cause depolymerisation. 300-400 fold lower affinity for mammalian beta-tubulin.
Invermectin and piperazine
Anti helminths that target neuromuscular coordination. Enhance inhibitory neurotransmission.
Anti helminths that target neuromuscular coordination. Nicotinic ACh receptor agonist that causes muscle contraction and spastic paralysis.
Anti helminths that target neuromuscular coordination. Nicotinic antagonist - causes flaccid paralysis.
Broad spectrum anti helmintic that targets neuromuscular coordination. Binds to VGCa channels, causes Ca increase and sustained contraction - spastic paralysis. Also changes external surface structure facilitating antibody binding and sensitivity to immune response.