This chapter presents discussion on sedatives/hypnotics. Sedatives produces calming/quietening actions, decreases excitement, produces drowsiness. Hypnotic induces sleep mimicking natural sleep. Both sedation and hypnosis are different grades of central nervous system (CNS) depression. Gamma-aminobutyric acid (GABA) is the principle inhibitory neurotransmitter in CNS. Pharmacological actions, advantages, adverse drug reaction, and uses of benzodiazepines (BZDs) have been covered in this chapter. A detailed description on barbiturates and antianxiety agents has been also given in this chapter.