Faculty of Pharmacy Pharmaceutical Chemistry Department CNS Depressants Drugs in Market Under supervision of: Dr. Ayman Bastawy By: Shaimaa AbdElrahim 1121201 Class CNS Depressant Drugs Example in Market Barbiturates: Phenobarbital Pentobarbital Secobarbital Thiopental Phenobarbital: Etaphylline Phenobarbital® Benzodiazepines: Diazepam Lorazepam Clonazepam: Clonazepam Amotril® Temazepam Alprazolam Midazolam NonDrugs Acting Benzodiazepines: on GABA Zopiclone Receptors Zolpidem Zaleplon Eszopiclone: Night Calm® Uses Anticonvulsant Targeted Receptors As α/β subunits of the synaptic Agonist GABA-A receptor Action ↑ Cl channel opening lifetime → inhibitory GABA actions Treat panic α/γ subunits of disorders, severe ↑ Cl channel opening frequency → enhance synaptic GABA- Agonist anxiety, and GABA binding to its receptor A receptor seizures α1 subunit of GABA-A synaptic receptor Agonist → enhance the inhibitory GABA actions α4 subunit of extrasynaptic General anesthetic GABA-A receptors Agonist → enhance the inhibitory actions of GABA sedative-hypnotic that treat insomnia Propofol Propofol: Recofol® Etomidate Etomidate: Amidate® Short-acting IV anesthetic β2 subunit of synaptic GABA- Agonist A receptor ↑ Cl channel opening lifetime → postsynaptic inhibitory GABA actions Baclofen Baclofen: Mylobac® Muscle relaxant GABA-B receptor y in Agonist the spinal cord ↓ substance P release → muscle relaxantation and sedation CNS Depressant Drugs Example in Market Drugs Acting Dexmedetomidine on Tizanidine Adrenergic Receptors Tizanidine: Sirdalud® Class Uses Targeted Receptors As Action Presynaptic Muscle relaxant α2 adrenergic receptor Agonist ↓ inhibits NA release treat anorexia & Drugs Acting Tetrahydrocann weight loss in HIV on abinol Dronabinol: patients CB1 receptor Cannabinoid Cannabidiol Marinol® treat nausea & Receptors Dronabinol vomiting in cancer chemotherapy Agonist ↓ pain, sedation, and changes in emotions and cognition Drugs Acting on Serotonin Receptors Aripiprazole Clozapine Olanzapine Risperidone Clozapine: Clozapex® Controls schizophrenia 5-HT2A receptor Antagonist ↓ the neuronal excitation Drugs Acting on Opioids Receptors Morphine Fentanyl Fentanyl: Durogesic® Treat severe pain Mu opioid receptor Agonist → CNS depressant actions Drugs Acting Haloperidol on Haloperidol: Controls psychotic ↓ neurons excitation in the brain Sulpiride D2 receptors Antagonist Dopamine Halonace® disorders and cause CNS depressant effect Chlorpromazine Receptors References: https://www.preprints.org/manuscript/202101.0503/v1 https://go.drugbank.com/drugs
