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.
Isoflurane enhances GABA activity, causing CNS depression with rapid onset and smooth recovery. It is an inhalation anesthetic used for induction and maintenance of general anesthesia. Chemical Formula: C₃H₂ClF₅O Mechanism of Isoflurane: GABA-A receptor potentiation Inhibits NMDA receptors, 2-pore domain K+ channels Uses of Isoflurane: Maintenance of anesthesia Side Effects: Airway irritation (not ideal for … Read more
Enflurane enhances GABA activity, producing CNS depression with muscle relaxation and analgesia. It is an inhalation anesthetic used for induction and maintenance of general anesthesia. Chemical Formula: C₃H₂ClF₅O Mechanism of Enflurane : Enhances GABA-A activity Inhibits excitatory neurotransmission Uses of Enflurane: Maintenance of anesthesia (replaced by safer agents) Side Effects: CNS excitation → seizure-like EEG … Read more
Methoxyflurane provides potent inhalation anesthesia and analgesia in medical procedures. It is a volatile anesthetic acting on CNS to induce sedation and pain relief. Chemical Formula: C₃H₄Cl₂F₂O Mechanism of Methoxyflurane: Potentiates GABA-A, glycine receptors Inhibits neuronal calcium influx Uses of Methoxyflurane: Historical: inhalational anesthesia Current: analgesia in trauma (inhaler) — Australia, New Zealand Side Effects: … Read more
Halothane enhances GABA activity, causing CNS depression and smooth muscle relaxation. It is an inhalation anesthetic used for induction and maintenance of general anesthesia. Chemical Formula: C₂HBrClF₃ Mechanism of Action: Potentiates GABA-A and glycine receptor activity Inhibits NMDA receptors and neuronal excitability Alters membrane fluidity via interaction with lipid bilayer Uses: Induction and maintenance of … Read more
Classification of General Anesthetics is based on route (inhalation, intravenous) and chemical nature. General anesthetics are classified based on: Route of Administration Chemical Structure Inhalation Anesthetics These are gases or volatile liquids administered via inhalation. Common for their ease of control and pleasant induction. Examples: Halothane Methoxyflurane Enflurane Sevoflurane Isoflurane Desflurane Intravenous Anesthetics Administered through … Read more
Definition of General Anesthetics: General anesthetics are drugs that induce a reversible loss of consciousness. They are used during surgical procedures to render the patient unconscious, unresponsive, and incapable of feeling pain. Administration routes: Intravenous (IV) Inhalation Stages of General Anesthesia General anesthesia is typically divided into four stages, from the initial administration to the … Read more
Felbamate blocks NMDA receptors and modulates GABA, reducing abnormal neuronal excitability. It is an anticonvulsant effective in treating partial seizures and Lennox-Gastaut syndrome. Formula: C₁₁H₁₄N₂O₄ Mechanism of Action: Blocks NMDA receptors Potentiates GABA-A Uses of Felbamate: Refractory epilepsy Lennox-Gastaut syndrome Side Effects of Felbamate: Aplastic anemia Hepatotoxicity Insomnia, headache Notes: Reserved for severe, resistant epilepsy
Gabapentin modulates calcium channels, reducing excitatory neurotransmitter release in the CNS. It is prescribed for neuropathic pain, partial seizures, and restless leg syndrome. Formula: C₉H₁₇NO₂ Mechanism of Gabapentin: Binds α2δ subunit of voltage-gated calcium channels Reduces excitatory neurotransmitter release Uses of Gabapentin: Partial seizures Neuropathic pain Postherpetic neuralgia Side Effects: Drowsiness Weight gain Ataxia Notes: … Read more
Primidone metabolizes to phenobarbital and PEMA, enhancing GABA to reduce neuronal excitability. It is prescribed for epilepsy, controlling partial and generalized tonic-clonic seizures. Formula: C₁₂H₁₄N₂O₂ Mechanism of Primidone: GABA-A enhancement via phenobarbital metabolite Direct Na⁺ channel effects Uses of Primidone: Generalized tonic-clonic seizures Essential tremor Side Effects: Sedation Nausea Ataxia Notes: Used in patients who … Read more
Valproic Acid treats epilepsy, bipolar disorder, and prevents migraine attacks. It increases GABA levels, stabilizing neuronal firing and reducing seizures. Formula: C₈H₁₆O₂ Mechanism of Action: Na⁺ channel blocker T-type Ca²⁺ channel inhibitor ↑ GABA levels by inhibiting GABA transaminase Uses of Valproic Acid: Broad-spectrum AED (absence, myoclonic, tonic-clonic, partial) Bipolar disorder Migraine prophylaxis Side Effects … Read more
