Anti mycobacterial Flashcards
bactericidal
works at the bacterial cell wall inhibiting mycobacterial cell wall by inhibiting mycelia acid production
activated by catalase peroxidase katc
INH
resistance due to deletion or down regulation of katc
INH
metabolized by liver enzyme N acetyl transferase - slowacetylators have higher risk of SE
INH
neuropathy caused by vit b6 excretion promoted by
INH
SE: sideroblastic anemia, hepatotoxicity, drug induced lupus, inhibits CYP450, G6PD def hemolysis
INH
bactericidal
activated by CYP450
binds to bacterial DNA dependent RNA polymerase
rifampin
point mutation in rpoB
resistance of rifampin
used in tx of prophylactic mono therapy in close contacts of h flu and n meningitis
rifampin
SE: hepatotoxicity and orange urine and body fluids
rifampin
Other note: contraceptive failure with oral combined contraceptives; admin with INH to prevent rapid resistance
rifampin
blocks arabinosyl transferase
inhibiting carbohydrate formation at the cell wall
bacteriostatic
ethambutol
SE: optic neuritis (loss of visual acuity, red and green color blindness)
ethambutol
pyrazinamide converted to pyrazinoic acid by
mycobacterial pyrazinamidase
distrupts mycobacterial cell membrane metabolism
pyrazinoic acid
active at ph 5.5
bactericidal
inhibits bacteria in lysosome of macrophage (intracellular back.)
pyrazinamide
bactericidal
crosses BBB
active against extracellular mycobacterium
SE: ototoxicity and nephrotoxicity
streptomycin
inhibits bacterial cell wall syndrome (alanine racemes which links 2-D ala residues)
cycloserine
SE: peripheral neuropathy, anemia, CNS dysfxn: depression and psychotic rxn; pyridoxine ameliorates neurotoxicity
cycloserine
inhibits dihydropteroate synthase and mycobactin synthesis
high [ ] in urine can cause crystalluria
aminosalicyclic acid
active against TB, MAC, M fortuitous
less potent inducer of P450
preferred in px with HIV co inf
rifabutin
longer half life
should not be used in px with HIV
potent P450 inducer
used after 2 mon of TB tx
rifapentin
mycobacterial adenosine
triphosphate synthase inhibitor
bedaquiline - new drug
nitroimidazole derivative
mycelia acid synthesis inhibitor
delaminid - new drug
temporary exacerbation of sx’s and signs on starting tx
paradoxical rxn in HIV px with active TB
Tx with Prednisone
IRIS - immune reconstitution inflammatory syn