Antimycobacterial Drugs Flashcards
First line of drugs for TB
RIPE R Rifampin I Isoniazid P Pyrazinamide E Ethambutol
What is LTBI?
Latent Tuberculosis Infection. Infected with tuberculosis without sign and symptoms of active TB.
Treatment for LTBI?
- Isoniazid (monotherapy for 9 months)
2. Isoniazid + Rifapentine (12 once weekly higher doses)
Duration of susceptible TB therapy?
6 months
Treatment last for 2 years of?
Multidrug resistant TB (MDR-TB)
Drugs for extensively drug resistant TB (XDR-TB)?
Clofazimine and linezolid
What is DOT?
Directly Observed Therapy. Patients take drugs under supervision of health care team. Decreases drug resistance and improves cure rates.
Isoniazid is activated by?
KatG, catalase-peroxidase
MOA of Isoniazid?
Targets InhA and KasA, inhibits mycolic acid synthesis, disrupting bacterial cell wall
Isoniazid also called?
INH
Resistance of Isoniazid develops as?
- Mutations/deletion of KatG
- Mutation of InhA (acyl carrier protein)
- Overexpression of InhA
Pharmacokinetics of Isoniazid
Oral administration. Food impairs absorption
Undergoes n-acetylation
90 minutes half life
Excreted through kidney
Adverse effects of Isoniazid?
Hepatitis
Paresthesia of hand n feet (pins and needles sensation)
Convulsions, rashes, fever, nystagmus, ataxia
Why Isoniazid causes paresthesia?
Due to pyridoxine deficiency. Should take daily pryidoxine (VITAMIN B6)
Drugs of Rifamycins?
Rifampin
Rifabutin
Rifapentine
MOA of Rifampin?
Blocks RNA transcription.
By beta subunit of mycobacterium DNA dependent RNA polymerase