Author: Mrs. Neelam Singh
Volume: 01
First Online: 31 August 2024
Pages: 177-192
DOI:

Barbiturates, a class of sedatives and hypnotics, act by enhancing the action of GABA at the GABA-A receptor, leading to increased neuronal inhibition. The structure-activity relationship (SAR) of barbiturates reveals that modifications to the barbituric acid core influence their onset and duration of action. For instance, adding alkyl or aryl groups can enhance lipid solubility, allowing for faster onset and shorter duration of action. Barbital and phenobarbital are longacting barbiturates used for their sedative and anticonvulsant properties. Mephobarbital and amobarbital have intermediate durations, useful for anxiety and insomnia, while butabarbital, pentobarbital, and secobarbital are shortacting, providing quick sedation for procedures or severe insomnia. Miscellaneous sedatives include amides, imides, alcohols, and their derivatives. Glutethimide, an imide, acts similarly to barbiturates and is used for short-term insomnia treatment. Alcohol and their carbamate derivatives, such as meprobamate and ethchlorvynol, also act on the CNS to provide sedative effects. Meprobamate is utilized for its anxiolytic and muscle relaxant properties, while ethchlorvynol is used for insomnia. Aldehyde derivatives like triclofos sodium and paraldehyde serve as hypnotics, with triclofos sodium often used in pediatric sedation and paraldehyde in managing acute convulsions. These diverse agents provide a range of options for treating anxiety, insomnia, and seizure disorders, each with distinct pharmacokinetic profiles and clinical uses.