ANTIMYCOBACTERIALS Flashcards
Antibacterial activity
• Gram-positive bacteria, gram-negative bacteria
(E. coli, Pseudomonas, Proteus, Klebsiella)
• BACTERICIDAL for Mycobacteria with good penetration into most tissues and phagocytic cells
• effective for both ACTIVE and LATENT forms of TB
RIFAMYCINS
Rifampin or Rifampicin (most commonly used), Rifapentine, Rifabutin
Binds to the β subunit of bacterial DNA dependent RNA polymerase inhibiting RNA synthesis
RIFAMYCINS
Rifampin or Rifampicin (most commonly used), Rifapentine, Rifabutin
• Rifampin (Rifampicin) best taken on an empty
stomach because absorption will be better.
• Rifapentine best taken WITH food (not commonly
used)
Undergoes enterohepatic recirculation
RIFAMYCINS
• Mainly excreted in the feces as deacylated metabolites; a small amount is also excreted in the urine.
• No dose adjustments required for patients with renal disease or undergoing dialysis
RIFAMYCINS
Harmless orange discoloration
o Liver enzymes are elevating more than 3 times or higher than the normal range → close monitoring of symptoms for cases of drug induced hepatotoxicity
Flu-like syndrome
CYP 450 inducer
RIFAMYCINS
Used before as a prophylaxis for meningococcemia exposure, but now replaced by Ciprofloxacin
RIFAMYCINS
- Antibacterial activity
• Against Mycobacteria residing within the acidic environment of the lysosomes - Activated under acidic conditions
- Converted to pyrazinoic acid (active form) by mycobacterial
PYRAZINAMIDE (PZA)