Antimycobacterials Flashcards
Isoniazid ADR
1st line
ADRs - peripheral neuritis caused by a relative pyridoxine deficiency (B6) so must give INH w/ B6 50mg, life threatening hepatits
-specific for TB
Rifampin ADR
1st line
ADRs-harmless red, reddish brown or orange color to urine, sweat, tears,saliva and onto contact lenses
- Cytochrome P450 enzyme inducer!!
- also used for leprosy when combined w/dapsone
Pyrazinamide
1st line
ADRs - hyperuricemia, hepatotoxicity
Ethambutol
1st line
dose related retrobulbar neuritis (loss of central vision and color discrimination
Rifapentine
1st line
CYP450 enzyme inducer.
similar to rifampin
Rifabutin
1st line
- not FDA approved for TB tx
- used as a sub for rifampin
combo first line agents
Rifamate: Contains INH/RIF
Rifater: Contains INH/PZA/RIF
streptomycin
2nd line tx
- used when TB is refractory to other therapies or if it is life threatening (HIV, meningitis)
- nephrotoxic, ototoxic (MONITOR peaks/troughs).
capreomycin
ethionamide
cycloserine
p-aminosalicylic acid (PAS)
2nd line tx
nephrotoxic, ototoxic
hepatic impairment,
CNS somnolence
Bedaquiline MOA
2nd line tx
diarylquinoline antimycobacterial drug that inhibits mycobacterial ATP synthase that is essential for the generation of energy
-only use with 3 other drugs
Common regimen for active TB
Initial phase: INH, RIF, PZA , EMB and B6 x 8 weeks
Continuation phase: INH, RIF and B6 for 18 weeks (Continuation phase may be extended in certain patients)
Children – same recommendations except avoid EMB
Principles of treatment for drug-resistant TB
Don’t add a single new drug, try at least 3 previously unused agents to which there is reported susceptibility
Use at least one drug via the parenteral route
Provide hospital-based or direct-observed therapy (DOT) to assure adherence
PPD positive
– all pts should be treated w/ INH 300 mg PO daily
Adults – 9 mos
isoniazid (INH) and rifapentine (RPT) administered weekly for 12 weeks as directly observed therapy (DOT) is equal alt
children – 9 mos
rifabutin
Indications: MAC prophylaxis in HIV pts, Tx of MAC infx in combo with azithromycin, clarithromycin or ethambutol for 16 weeks, TB
ADRs - rash, GI (take w/ meals to reduce effects), neutropenia, yellow-brown urine, sweat, tears, contact lenses.
clofazimine
Indications: MAC, leprosy, resistant TB
ADRs GI effects (N,V,D, anorexia), skin discoloration and discoloration of urine, sweat, tears (red-brown to black), increased LFTs, hepatitis