C.2. Antimycobacterial drugs Flashcards
list the 1st line antimycobacterial agents
'RIPE' Rifampin Isoniazid (INH) Pyrazinamide Ethambutol
list the 2nd line antimycobacterial agents
streptomycin Amikacin Kanamycin Cycloserine Ciprofloxacin Ofloxacin linezolid
what is the MoA of Isoniazid?
inhibits synthesis of mycolic acid
bactericidal effect
what is the mechanism of resistance of Isoniazid?
deletions in katG gene
what is the most important drug used in TB treatment?
Isoniazid
what are the indications for TB prophylaxis (3)?
- TB exposure in young children, TST negative
- TST conversion in the past 2 years
- TST reactors with high risk (diabetes, HIV positive, immunosuppressive treatment, leukemia)
what is the MoA of Rifampin?
inhibits DNA-dependent RNA polymerase (transcription inhibitor)
bactericidal effect
what is the mechanism of resistance of Rifampin?
alteration of the polymerase enzyme
which agents are given prophylaxis TB?
Isoniazid (INH) or Rifampin
how are TB and leprosy drugs given?
Orally
what are the other indications for Rifampin other than TB?
- leprosy
- in combination with vancomycin–>active against MRSA and PRSP
- Prophylaxis: N.meningitidis, H. influenza, staphylococci
what is the MoA of Ethambutol?
inhibits synthesis of arabinogalactan
what is the mechanism of resistance of Ethambutol
alteration of drug target
which TB drug is an inhibitor of CYP450 enzymes?
Isoniazid
which TB drug is an inducer of CYP450 enzymes?
Rifampin
mechanism of action of Pyrazinamide
unknown
bacteriostatic
mechanism of resistance of Pyrazinamide
mutations in gene encoding enzymes involved in drug activation