Biological half-life and volume of distribution of the drug are the key parameters in understanding the pharmacokinetics of the drugs within the body as they affect all the pharmacokinetic processes including absorption, distribution, metabolism and elimination of drugs and also associated with each other, ultimately effecting the Pharmacological action of the drug on its target site. Given study elaborates the various aspects of half-life, i.e., Alpha & beta half-lives, the contribution of Zero-order and first-order kinetics in ADME and interrelation among the volume of distribution & half-life along with the distribution & redistribution of the drug within the body. Moreover, the importance of half-life & Vd and the idea of Steady-state concentration is also discussed. Various types of physiological barriers, including the blood-brain barrier, placental barrier, blood-CSF barrier, affect the distribution of drugs.