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.
Meprobamate acts on GABA receptors, producing sedative, anxiolytic, and muscle relaxant effects. It is used for short-term relief of anxiety and tension disorders. Chemical Formula: C₉H₁₈N₂O₄ Mechanism of Meprobamate: Enhances GABA-A receptor activity, similar to barbiturates. Also acts on spinal cord interneurons for muscle relaxant effect. Therapeutic Uses of Meprobamate: Anxiety (mild to moderate) Sedation … Read more
Paraldehyde is a central nervous system depressant, promoting sedation and muscle relaxation. It treats acute seizures and alcohol withdrawal symptoms. Chemical Formula: C₆H₁₂O₃ Mechanism of Action: CNS depressant: exact mechanism unclear. Possibly acts on GABA-A receptors and enhances inhibitory tone. Therapeutic Uses of Paraldehyde: Delirium tremens (alcohol withdrawal) Status epilepticus (historical use) Sedation (limited due … Read more
Ethchlorvynol acts on the CNS, enhancing inhibitory pathways to induce sleep and relaxation. It is used as a sedative-hypnotic for short-term relief of insomnia. Chemical Formula: C₇H₁₁ClO Mechanism of Action: CNS depressant with barbiturate-like action Potentiates GABA-mediated chloride currents Therapeutic Uses of Ethchlorvynol: Insomnia (short-term) Side Effects of Ethchlorvynol: Dizziness Euphoria Nausea Risk of dependence, … Read more
Glutethimide is used as a sedative-hypnotic for short-term insomnia management. It enhances GABAergic activity, inducing sleep with CNS depressant effects. Chemical Formula of: C₁₃H₁₅NO₂ Mechanism of Action: Depresses CNS via non-specific action on reticular formation. Weak GABA-A agonist effects (no specific receptor binding like BZDs). CYP450 inducer — may enhance metabolism of other drugs (notably … Read more
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
