Ant-Mycobacterial Drugs Flashcards
What are mycobacteria?
Slender, curved rods
Cell walls are complex
What are the 2 broad groups of mycobacteria?
Mycobacterium tuberculosis species
Nontuberculous species
What are 3 mycobacterial diseases?
T.B.
Leprosy
Lung infections in AIDS and CF patients
What is unique to mycobacteria structure?
Thick mycolate-rich outer covering -> efficient barrier
What is MDR-TB?
Multi drug resistant TB that is resistant to at least isoniazid and rifampicin
What is XDR-TB?
Extended drug resistance
What are the first line anti-TB drugs?
Isoniazid
Rifampicin
What are the 2nd line anti-TB drugs?
Aminoglycosides
Fluoroquinolone
How long is compound drug therapy for TB?
6 months
When is Isoniazid bactericidal?
For actively growing tubercle bacilli
What is Isoniazid’s MoA?
Inhibits synthesis of mycolic acids
Combines with an enzyme leading to disorganization of metabolism
How is resistance to Isoniazid developed?
Absence of catalase peroxidase
Reduced penetration
Over-expression of carrier proteins
How is isoniazid administered?
orally
How is isoniazid distributed?
Widely - reaches BBB
How is isoniazid metabolised?
Acetylation
How is isoniazid excreted?
Renal
What are s/e of Isoniazid?
Allergic skin reactions
Memory loss
hepatotoxicity
seizures
Is Rifampicin bactericidal for mycobacteria?
yes
What is the MoA of Rifampicin?
Binds to B subunit of DNA
Binds to RNA polymerase -> conformational change