TB Flashcards
Bedaquiline (TMC-207)
MOA?
Treatment?

Properties of Rifampin?
DMPK
Metabolism
Excretion?

Ethambutol
Only used for?
Static or Cidal?
MOA?
Resistance?
DMPK?
Major Toxicity?

How resistant is Restistant TB?
TB
MDR TB
Definition and second line
XDR TB

First line treatment of TB needs to do what?
- Block the synthesis of Mycolic Acid and arabinogalactans
Standard TB Tx
TB exists in 3 portions:
Six month treatment (___)
7 points
Rationale for Therapeutic Combos
Multiple Targets?
Resistance
Toxicities
- At cell wall mycolic acid and arabanogalactan layer, transcription and translation
- High levels of resistance 3 to 4 durgs to overcome this
- Puts stress on the liver

Isoniazide (INH)
DMPK: Administration?
Distributes on an empty?
Toxicity?
MOA?
Resistance?


Pyrazinamide (PZN)
Static or cidal?
DMPK
MOA?
3 things
Toxicity?
Resistance?

TB drugs in development

Rifabutin and Rifaximin?
___ Macrolides?
Treatment of?
Rifaximin absorption admin, treats, alternative for?

Clinical properties of Rifampin
Usage
Prophylactic usage?
Toxicities?
Interactions?

Second line and alternative therapies for TB
- Unique second line
- Ethionamide, Cycloserine, PAS, Capremycin, Bedquiline
- Antibiotic classes already discussed
- FQs (levo, oflo, Moxi)
- AGs (kanamycin, amikacin, streptomycin)
- COmbo therapy needs (INH, Pyrazinamide, ethambutol)
INH is a ____ that gets converted by ____ then it can inhibit ___
Resistance is common with?
- Prodrug that eventually gets coverted by KatG then it can inhibit INHa
- Mutations in both of these sites pose problems
Schematic Diagram of Mycobacterial Cell wall
Or at least the parts that are targeted for TB
8 parts

Rifampin
Color?
Sensitive to?
MOA?
Static or Cidal?
Spectrum?
Resistance?

Second line agents cycloserine and p-aminosalicylic acid (PAS)
Cycloserine MOA, resistance, spectrum
Pamino- Inhibits?, Resistance?

Ethionamide
- Similar MOA to INH (mycolic acid synthesis inhibition)
- Only effective against mycobacterium
- Resistance is fast
Second line Capreomycin
MOA
static or cidal?
Admin?
Resistance?
Toxicity?

Mechanism of action of PZN

- Mechanism of action of pyrazinamide (PZA). PZA enters the bacilli by passive diffusion and is then converted by the nicotinamidase PncA into pyrazinoic acid (POA). POA exits the cell by passive diffusion, as well as by an efflux mechanism, which is not yet well characterized. In their revised mechanism, Zhang and co‐workers show that POA binds RpsA and blocks trans‐translation. Note: for simplicity, only the inner membrane of the mycobacterial cell envelope is depicted.