Title:Recent Update on Pharmacokinetics and Drug Metabolism in CNS-based Drug
Discovery
Volume: 29
Issue: 20
Author(s): Sachin Nashik Sanap, Amol Chhatrapati Bisen, Ashwini Kedar, Sristi Agrawal and Rabi Sankar Bhatta*
Affiliation:
- Pharmaceutics and Pharmacokinetics Division, CSIR-Central Drug Research Institute, Lucknow 226031, India
- Academy of
Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India
Keywords:
Brain barriers, CNS targeting, drug delivery, ADME, pharmacokinetics, pharmacodynamics.
Abstract: Despite significant advancements in CNS research, CNS illnesses are the most important and serious
cause of mental disability worldwide. These facts show a tremendous unmet demand for effective CNS medications
and pharmacotherapy since it accounts for more hospitalizations and extended care than practically all
other disorders combined. The site-targeted kinetics of the brain and, pharmacodynamics of CNS effects are
determined/regulated by various mechanisms after the dose, including blood-brain barrier (BBB) transport and
many other processes. These processes are condition-dependent in terms of their rate and extent because they
are dynamically controlled. For effective therapy, drugs should access the CNS “at the right place, time, and
concentration”. Details on inter-species and inter-condition variances are required to translate target site pharmacokinetics
and associated CNS effects between species and illness states, improving CNS therapeutics and
drug development. The present review encircles a short discussion about the barriers that affect effective CNS
treatment and precisely focuses on the pharmacokinetics aspects of efficient CNS therapeutics.