Antituberculosis Flashcards
Name the activity, route and line of p-salicylic acid
STATIC, oral, second-line
What is the MoA of PSA?
alters intermediates in biosynthesis as it is a structural analog of PABA - it is a substrate for DHPS, but doesn’t inhibit the enzyme. exact MoA not known
Name the activity, route and line of isoniazid
CIDAL, oral and IM, first-line
What is the MoA of Isoniazid
after KatG converts it to active form, Isoniazid binds with NAD and NADP to create adducts - one of these adducts inhibits mycobacterial DHFR and inhibits nucleic acid synthesis, the other inhibits mycolic acid
What is the active form of Isoniazid?
isonicotinoyl radical - converted by KatG, a multifunctional catalase-peroxidase
Name the activity, route and line of Ethambutol
STATIC, oral, first line
What is the MoA of Ethambutol?
inhibits the enzyme arabinosyl transferase, therefore inhibiting the polymerization of arabinoglycan, an essential component of a mycobacterial cell wall
Name the activity, route and line of pyrazinamide.
Cidal, oral and first line
What is the active form of pyrazinamide?
pyrazinoic acid - converted by nicotinamidase
What is the MoA of pyrazinamide?
binds to and inhibits the ribosomal protein S1, therefore inhibiting trans-translation (essential for replication under stressful conditions), inhibits fatty acid synthase type I (mycolic acid synthesis), reduces intracellular pH, disrupts cell membrane metabolism
Name the activity, route and line of ethionamide
static, oral, second line
What is the MoA of ethionamide?
Inhibits enoyl-ACP reductase of fatty acid synthase II