Tuberculosis is a bacterial infection caused by Mycobacterium tuberculosis, which spreads from infected person through salivary or cough droplets. In the present review it has been clearly described about the pharmacokinetic and pharmacodynamic study of first line anti-tubercular drugs like Isoniazid, Rifampicin, Pyrazinamide, Ethambutol and streptomycin. The biochemistry of the drugs were discussed along with their mechanism of action and its correlation with the structure of the active molecule of the drug. All the adverse drug reactions and various approaches for management of ADR’S have also been discussed with various comments of safety and efficacy.