Antitubercular Drugs Flashcards
PULMONARY TUBERCULOSIS is known as?
“Koch’s Disease”
In Gram staining: appears as “ghost”
Mycobacterium tuberculosis
Acid-Fast staining of TB
“Ziehl-Neelsen stain”
Isolated from Streptomyces mediterranei
RIFAMPICIN
MOA OF Rifampicin?
Binds strongly to the bacterial DNA-dependent RNA polymerase and
thereby inhibits RNA synthesis (transcription),
TRUE OR FALSE Rifampicin is a CYP450 Enzyme inducer?
TRUE
Adverse effect of Rifampicin?
Red orange secretion
Semi-synthetic derivative of Rifamycin
Rifampicin
Other terms for Isoniazid?
- Isonicotinic acid hydrazide
- Isonicotinyl hydrazide (INH)
Vitamin to manage peripheral neuritis caused by Isoniazid?
Pyridoxine/Vitamin B6
MOA of Isoniazid?
Targets the enzymes acyl carrier protein reductase (InhA)
and β-ketoacyl-ACP synthase (KasA), which are essential for the
synthesis of mycolic acid
A/E of Isoniazid?
- Peripheral neuritis 2. GI disturbances
(constipation, loss of appetite) - Hepatotoxicity.
Synthetic analogue of nicotinamide
Pyrazinamide
What is the active form of Pyrazinamide?
Pyrazinoic acid
MOA of Pyrazinamide?
inhibit incorporation of mycolic acid in cell wall.
Most hepatotoxic of all TB drugs; ↑ uric acid level → acute gouty arthritis.
Pyrazinamide
MOA of Ethambutol?
Inhibits arabinosyl transferase—an enzyme important for
the synthesis of the mycobacterial cell wall (arabinogalactan).
A/E of Ethambutol?
- Retrobulbar neuritis (optic neuritis) impairing visual acuity
and red-green color discrimination/blindness - hyperuricemia.
Isolated from Streptomyces griseus
Streptomycin
MOA of Streptomycin?
Irreversible inhibition of mycobacterial protein synthesis by binding to
30s ribosomal subunit.
First antibiotic effective in the treatment of TB
Streptomycin
A/E of Streptomycin?
- Ototoxicity
- vestibulotoxicity
Structural analogue of p-aminobenzoic
acid (PABA) just like sulfonamides
Para-aminosalicylic acid
MOA of PAS?
Folate synthesis antagonist that
interferes with the incorporation of
PABA into folic acid (inhibits folate
synthesis / antimetabolite).
Derivative of INH?
Ethionamide
MOA of Ethionamide?
MOA: inhibition of O2 dependent mycolic acid synthesis.
A/E of Ethionamide?
- GI disturbances (N/V , intense gastric irritation)
- neurological
disturbances (confusion, peripheral neuropathy
Isolated from the 3 different streptomyces species:
- Streptomyces orchidaceous
- Streptomyces garyphalus
- Streptomyces lavendulus
Cycloserine
MOA of Cycloserine?
Acts through a competitive inhibition of the D-alanine that
is involved in bacterial cell wall synthesis.
A/E of Cycloserine?
Toxicity: Dizziness, confusion, irritability, psychotic behavioural
changes & suicidal tendency.
Isolated from S. capreolus?
Capreomycin
Reserved for the treatment of MDR-TB
Capreomycin
Considered in the treatment of MDR tuberculosis after streptomycin &
capreomycin.
Aminoglycosides
Last line for TB used as an agent for Last-Resort for Multi-Drug Resistant TB.
Clafazimine
A/E of Clofazimine?
Red-brown discoloration of the skin.