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.
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
Lorazepam is a drug which treats anxiety, insomnia, and seizures with calming effects. Lorazepam, a benzodiazepine, enhances GABA activity for sedation. Chemical Formula: C₁₅H₁₀Cl₂N₂O₂ Mechanism of Lorazepam: Enhances GABAergic inhibition Intermediate-acting BZD with no active metabolites Uses of Lorazepam: Status epilepticus (IV) Anxiety Pre-op sedation Side Effects: CNS depression Amnesia Less hepatic metabolism → safe … Read more
Clorazepate Dipotassium treats anxiety, seizures, and alcohol withdrawal symptoms. Clorazepate Dipotassium treats anxiety, seizures, and alcohol withdrawal symptoms. Chemical Formula: C₁₆H₁₁ClN₂O₄ Mechanism of Clorazepate Dipotassium: Converted to active diazepam-like compound in the stomach Modulates GABA-A receptors Uses of Clorazepate Dipotassium: Anxiety Partial seizures Alcohol withdrawal Side Effects: Sedation Dizziness Long duration of action due to … Read more
Oxazepam treats anxiety, alcohol withdrawal, and insomnia with safer short-acting control. Oxazepam, a benzodiazepine, is an active metabolite of Diazepam with slower onset. Chemical Formula: C₁₅H₁₁ClN₂O₂ Mechanism of Oxazepam: Short-acting GABA-A modulator Does not undergo hepatic oxidation (safe in liver disease) Uses of Oxazepam: Anxiety Alcohol withdrawal Short-term insomnia Side Effects: Sedation Confusion (elderly) Less … Read more
Diazepam treats anxiety, seizures, muscle spasms, and alcohol withdrawal effectively. Diazepam enhances GABA action, producing sedative, anxiolytic, and anticonvulsant effects. Chemical Formula: C₁₆H₁₃ClN₂O Mechanism: Enhances GABAergic transmission at GABA-A receptors by increasing frequency of Cl⁻ channel opening Uses: Anxiety Muscle spasms Seizures (status epilepticus) Alcohol withdrawal Premedication for procedures Side Effects: Drowsiness, sedation Amnesia Muscle … Read more
Chlordiazepoxide treats anxiety, alcohol withdrawal, and muscle spasms effectively. Chlordiazepoxide is a benzodiazepine enhancing GABA action for calming effects. Chemical Formula: C₁₆H₁₄ClN₃O Mechanism of Chlordiazepoxide: Binds to GABA-A receptor (α, γ subunits) to enhance GABA effect (↑ Cl⁻ influx) Uses of Chlordiazepoxide: Generalized anxiety disorder Alcohol withdrawal Preoperative sedation Side Effects: Drowsiness Impaired coordination Tolerance, … Read more
