Pharm 47: Antimycobacterial Drugs – Q&A
What are some characteristics of mycobacteria (4) that make them resistant
to most antibiotics? ✔️Ans - slow-growing (can also be dormant)
Lipid-rich cell wall
Intracellular (in macrophages)
develop resistance quickly
What is a way to remember the 5 drugs used in treatment of TB?
Which is/are used in prophylaxis (*)? ✔️Ans - RIPE(S)
Rifampin
*Isoniazid (INH)
Pyrazinamide
Ethambutol
Streptomycin- not used anymore
What is an easy way to remember the toxicities of Isoniazid? ✔️Ans -
Abbreviated as INH
I=isoniazid N= neurotoxicity H= hepatotoxicity
what is responsible for activating the Isoniazid prodrug? ✔️Ans - KatG, the
mycobacterial catalase-peroxidase
How does Isoniazid kill mycobacteria? ✔️Ans - inhibiting synthesis of
mycolic acids, an essential part of their cell walls
deletion of what gene is responsible for high-level resistance to isoniazid?
✔️Ans - katG
Deletion of what gene is responsible for low-level resistance of isoniazid?
✔️Ans - inhA
What do you have to be careful of when dosing Isoniazid? ✔️Ans - Fast
acetylators (Asian+native americans)
vs. Slow (european +african descent)
Which drug is the "most important" in TB therapy? ✔️Ans - INH
, How does rifampin kill mycobacteria? ✔️Ans - inhibits DNA-dependent
RNA polymerase (encoded by rpo gene)
What are the toxicities of rifampin? ✔️Ans - Light-chain proteinuria
(impaired antibody responses)
Skin rashes
thrombocytopenia
nephritis
liver dysfunction
what do you have to be careful of when dosing Rifampin? ✔️Ans - induces
metabolizing enzymes so it enhances elimination of other a lot of other drugs
How does treatment of TB in an AIDS pt differ from TB w/o AIDS? ✔️Ans -
rifabutin is preferred over rifampin
How does Rifaximin treat traveler's diarrhea? ✔️Ans - Rifaximin is not
absorbed from the GI tract and can stay and wage war on those intruding
upon our land of poop.
How does Ethambutol kill mycobacteria? ✔️Ans - inhibits
arabinosyltransferases (arabinoglycan is a component of mycobacterial cell
walls)
What is the most common adverse effect associated with Ethambutol?
✔️Ans - visual disturbances that usually regress when drug is stopped
(Ethambutol is drunk in the eyes)
Besides nongouty polyarthralgia, what other toxic effects occur from
pyrazinamide? ✔️Ans - Myalgia
GI irritation
Maculopapular rash
Hepatic Dysfunction
Porphyria
Photosensitivity reactions
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