Medicinal Chemistry I is a core subject that explores the design, synthesis, and biological activity of drugs. It bridges organic chemistry and pharmacology to enhance understanding of therapeutic agents.
Butabarbital is used for short-term relief of insomnia and as a preoperative sedative. It is a barbiturate, enhances GABA activity to induce sedation and sleep Chemical Formula of Butabarbital: C₁₀H₁₆N₂O₃ Mechanism of Action: Intermediate-acting barbiturate acting via GABA-A receptor modulation. Therapeutic Uses: Short-term treatment of insomnia Preoperative sedation Side Effects: Sedation Hangover effect Cognitive impairment
Pentobarbital enhances GABA activity, acting as a short-acting barbiturate sedative-hypnotic. It is used for insomnia, preoperative sedation, and seizure control in emergencies. Chemical Formula: C₁₁H₁₈N₂O₃ Mechanism of Pentobarbital: Short-acting GABA-A receptor agonist. Therapeutic Uses of Pentobarbital: Sedation Anesthesia induction (older use) Euthanasia in veterinary and medical contexts Side Effects: Severe respiratory depression High abuse potential … Read more
Secobarbital is a barbiturate used for short-term insomnia treatment and preoperative sedation. It depresses CNS activity by enhancing GABA action, producing sedative and hypnotic effects. Chemical Formula: C₁₂H₁₈N₂O₃ Mechanism of Secobarbital: Short-acting barbiturate; increases GABA-mediated chloride influx. Therapeutic Uses of Secobarbital: Hypnotic Preoperative sedation Rarely used today due to dependence risk Side Effects: High abuse … Read more
Triclofos Sodium is used as a sedative-hypnotic for treating childhood insomnia and sleep disorders. It is a chloral hydrate derivative, induces sleep by depressing the CNS safely in children. Chemical Formula: C₈H₁₅Cl₃Na₂O₄P Mechanism of Triclofos Sodium: Prodrug; hydrolyzed to trichloroethanol (active), similar to chloral hydrate. Acts on GABA-A receptor to enhance inhibitory neurotransmission. Therapeutic Uses … Read more
Amobarbital helps manage insomnia, preoperative sedation, and certain seizure conditions. It is a barbiturate that enhances GABA action, producing sedative and hypnotic effects. Chemical Formula: C₁₁H₁₈N₂O₃ Mechanism of Amobarbital: Intermediate-acting GABA-A enhancer. Therapeutic Uses of Amobarbital: Short-term hypnotic Sedative Historically used as “truth serum” Side Effects of Amobarbital: Drowsiness Confusion CNS depression Dependency
Mephobarbital helps manage epilepsy and anxiety with sedative and anticonvulsant effects. This is a barbiturate, enhances GABA activity, producing CNS depression. Chemical Formula of Mephobarbital: C₁₁H₁₄N₂O₃ Mechanism of Action: Similar to phenobarbital but has a methyl group on N-1, leading to more sedation and slightly lower potency. Therapeutic Uses: Epilepsy (milder forms) Sedative (older use) … Read more
Phenobarbital is widely used as an anticonvulsant for epilepsy and as a sedative-hypnotic. Phenobarbital enhances GABA activity, prolonging chloride influx to produce CNS depression. Chemical Formula: C₁₂H₁₂N₂O₃ Mechanism of Phenobarbital: GABA-A receptor agonist; increases duration of Cl⁻ channel opening. Also reduces glutamate-mediated excitation. Therapeutic Uses of Phenobarbital: Generalized and partial seizures Sedation Febrile seizures in … Read more
Barbital (Veronal) was used as a sedative-hypnotic for insomnia and anxiety management. It is a barbiturate that depresses CNS activity, producing sedation and sleep. Chemical Formula: C₈H₁₂N₂O₃ Mechanism of Action: Enhances the action of GABA by prolonging the opening of Cl⁻ channels at the GABA-A receptor. Therapeutic Uses: Historically used as a sedative/hypnotic (no longer … Read more
Zolpidem (non-benzodiazepine hypnotic) treats insomnia by inducing fast sleep with minimal hangover. Zolpidem (non-benzodiazepine hypnotic) enhances GABA action, offering short-acting sedative effects. Chemical Formula: C₁₉H₂₁N₃O Mechanism of Zolpidem (non-benzodiazepine hypnotic): Selective binding to BZ1 (α1 subunit) of GABA-A receptor Induces sleep with minimal muscle relaxant or anticonvulsant activity Uses of Zolpidem (non-benzodiazepine hypnotic): Insomnia (short-term … Read more
Alprazolam treats anxiety and panic disorders by calming the nervous system. Alprazolam is a short-acting benzodiazepine enhancing GABA activity. Chemical Formula: C₁₇H₁₃ClN₄ Mechanism of Alprazolam: High affinity for α2/α3 GABA-A subunits → anxiolytic Moderate affinity for α1 → sedative effect Uses of Alprazolam: Panic disorder Generalized anxiety disorder (GAD) Short-term anxiety Side Effects: High abuse … Read more
