Anti-Mycobacterial Agents Flashcards
Treatment for rapidly growing tuberculosis with high bacillary load (cavitary)
Isoniazid
Treatment for spurters within the caseous material (caseous)
Rifampicin
Slow growing tuberculosis located intracellularly in macrophages and inflamed site
Pyrazinamide
Treatment for dormant tuberculous bacilli
Not susceptible
Symptoms of TB
chronic cough, fever, and weight loss
Drug with the strongest/most potent sterilizing activity that covers all subpopulations
Rifampicin
First line anti-TB drug that prevents relapse
Pyrazinamide
First line anti-TB drug that prevents resistance
Ethambutol
MOA of Rifampicin
RNA synthesis inhibitor
MOA of Isoniazid
Mycolic acid (Cell wall) synthesis inhibitor)
MOA of Pyrazinamide
Disruption of membrane energy metabolism
MOA of Ethambutol
Cell wall synthesis inhibition (Arabinoglycan)
DME inducer of the first line anti-TB drugs
Rifampicin
DME inhibitor of the first line anti-TB drugs
Isoniazid
Rifampicin’s adverse effect
Red orange secretions and urine
Isoniazid’s adverse effect
Peripheral neuritis
Pyrazinamide’s adverse effect
Hyperuricemia
Ethambutol’s adverse effect
Optic neuritis and impaired red-green color discrimination
Mechanism of resistance against Isoniazid
Mutation in Kat G and Inh A
First line drug used for latent TB infection; bactericidal after 24 hours
Isoniazid
Adverse effects of Isoniazid
Peripheral neuropathy (Vit B6 deficiency), Hepatitis, elevated ALT
Co-administration of this drug inactivates isoniazid
Vitamin C
Isoniazid increases toxicity of these drugs:
Phenytoin and Theophylline
Isoniazid increases its hepatotoxicity with:
Rifampicin and alcohol
Mechanism of resistance to Rifampicin
Mutation in rpo gene
Alternative to Isoniazid for latent TB infection, to Isoniazid resistant organisms, or to MOTT
Rifampicin
Drug given as an alternative to Rifampicin in HIV and TB patients
Rifabutin
This first line anti-TB drug is inactive at neutral pH
Pyrazinamide
Mechanism of resistance to Pyrazinamide
Mutation in pncA gene
Dosage effects of Ethambutol
Bacteriostatic at usual dose (15mg/kg/day)
Bactericidal at high dose (>25mg/kg/day)
Mechanism of resistance to Ethambutol
Mutation in emb B gene
Clinical use of Ethambutol
Intermittent therapy for drug resistant TB, prevent emergence of resistance, treatment of NMTB
First of the 2 phases of DOTS
Intensive or bactericidal phase: First 2 months, at least 4 drugs
Second of the 2 phases of DOTS
Continuation or sterilizing phase: 3rd to 6th months, uses Isoniazid and Rifampicin
Advantages of Fixed Dose Combination
Simplicity, monotherapy is avoided (less drug resistance), and improve patient compliance
Resistance to a drug without prior treatment
Primary drug resistance
Resistance to a drug developed during the treatment
Secondary drug resistance
MDR plus resistance to fluoroquinolones and 1 injectable drug
Extensive drug resistance
Presence of at least 1% of mycobacterium strains resistant to both isoniazid and rifampicin
Multi-drug resistance
Indicated for TB meningitis and pericarditis
Steroids
Mechanism of resistance to Streptomycin
Mutation in S12 protein encoded by rpsl and 16s rRNA encoded by rss gene
Clinical indication for Streptomycin
Serious forms of TB (Disseminated TB and TB meningitis), and MDR-TB susceptible to streptomycin
Drugs used for streptomycin resistant strains
Amikacin and Kanamycin
Drugs used for streptomycin and kanamycin resistant strains
Capreomycin
This hepatotoxic drug has an obnoxious taste and blocks mycolic acid synthesis similar to isoniazid
Ethionamide
Mechanism of resistance to Ethionamide
Mutation in inhA
Folic acid synthesis inhibitor used in patients with extended spectrum of drug resistance (XDR)
PAS (Para-amino salicylic acid)
Drugs with flu-like syndrome
PAS and Rifampicin
This drug is used in combination regimen for MDR-TB and is the last resort drug for MDR-TB resistant to first and second line drugs
Linezolid
Adverse effect of Linezolid
Bone marrow suppression
Respiratory fluoroquinolones having better activity than ciprofloxacin against TB Bacilli
Gatifloxacin and Moxifloxacin
Potent analog of Rifamycins with a longer half life
Rifapenine
Newly repurposed anti-tuberculosis drugs
Bedaquiline and Delamanid
MOA of Fluoroquinolones
DNA gyrase inhibition
Booster for BCG Vaccine
MYA85A
MOA of Dapsone
Dihydropteroate synthase inhibitor (inhibiting folic acid synthesis)
Used for all forms of leprosy, dermatitis herpetiformis and prophylaxis and treatment of Pneumocystis jirovecii
Dapsone
Adverse effects of Dapsone
Steven-Johnson syndrome and Sulfone Syndrome
Fastest bactericidal for Mycobacterium leprae
Rifamycin
Greatest limiting factor for Rifamycin usage
Cost
This drug accumulates in tissues for prolonged periods making possible discontinuous treatment separated by 4 weeks
Clofazimine
Drug used for Erythema Nodosum Leprosum and M. avium intracellulare infection
Clofazimine
Long acting tetracycline that has ototoxic effects
Minocycline
Drug of choice for treatment of Erythema Nodosum Leprosum
Thalidomide
Alternative treatment for Erythema Nodosum Leprosum
Corticosteroid