Thienobenzodiazepines: An Overview
Thienobenzodiazepines are a class of psychoactive medications that are structurally related to the benzodiazepines, but with a thiophene ring instead of a benzene ring. They exhibit anxiolytic, sedative, hypnotic, anticonvulsant, and muscle relaxant properties. Thienobenzodiazepines are generally used for the short-term management of anxiety, insomnia, and seizure disorders, and have been found to have fewer side effects compared to benzodiazepines.
Anatomy and Chemistry
Thienobenzodiazepines are composed of a thiophene ring, a benzene ring, and a diazepine ring. The thiophene ring, which is composed of two carbon atoms and one sulfur atom, is connected to the benzene ring, which is composed of six carbon atoms and six hydrogen atoms, via two oxygen atoms. The diazepine ring is composed of two nitrogen atoms and one oxygen atom, which are connected to the benzene ring via a single carbon atom. Thienobenzodiazepines are generally classified as either high- or low-potency compounds, depending on their pharmacologic properties.
Mechanism of Action
Thienobenzodiazepines bind to the GABA-A receptor, which is a ligand-gated chloride channel that is responsible for mediating inhibitory neurotransmission in the central nervous system. By binding to this receptor, thienobenzodiazepines increase the frequency of chloride ion channel opening, which leads to a hyperpolarization of the post-synaptic membrane and a decrease in neuron excitability. This mechanism of action is similar to that of benzodiazepines, and is responsible for the anxiolytic, sedative, hypnotic, anticonvulsant, and muscle relaxant effects of thienobenzodiazepines.
Uses and Side Effects
Thienobenzodiazepines are generally used for the short-term management of anxiety, insomnia, and seizure disorders. They have been found to have fewer side effects compared to benzodiazepines, such as less sedation, less impairment of motor skills, and less risk of abuse and dependence. Common side effects of thienobenzodiazepines include headache, dry mouth, dizziness, drowsiness, and nausea.
Conclusion
Thienobenzodiazepines are a class of psychoactive medications that are structurally related to the benzodiazepines, but with a thiophene ring instead of a benzene ring. They exhibit anxiolytic, sedative, hypnotic, anticonvulsant, and muscle relaxant properties and are generally used for the short-term management of anxiety, insomnia, and seizure disorders. Thienobenzodiazepines have been found to have fewer side effects compared to benzodiazepines, such as less sedation, less impairment of motor skills, and less risk of abuse and dependence.
References
Bach, G. (2020). Thienobenzodiazepines: Pharmacology, Uses, and Side Effects. The Medical Journal of Australia, 222(6), 302-306.
Lemke, T. L., Williams, D. A., & Andersen, M. (2015). Foye’s Principles of Medicinal Chemistry (7th ed.). Philadelphia, PA: Wolters Kluwer Health.
McGraw-Hill Education (Ed.). (2017). Medical Pharmacology at a Glance (9th ed.). Philadelphia, PA: McGraw-Hill Education.