Ketamine Hydrochloride

  • Ketamine Hydrochloride blocks NMDA receptors, producing dissociative anesthesia with analgesia.
  • It is used for anesthesia, pain relief, and emergency sedation.

Chemical Formula:

  • C₁₃H₁₆ClNO·HCl
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Ketamine Hydrochloride

Mechanism of Action:

  • NMDA receptor antagonist
  • Also interacts with opioid, monoaminergic, and muscarinic receptors
  • Increases sympathetic output → ↑ BP, HR, CO
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Uses of Ketamine Hydrochloride:

  • Induction of anesthesia
  • Short surgical procedures
  • Pediatric and battlefield anesthesia
  • Treatment-resistant depression (IV or nasal)

Side Effects of Ketamine Hydrochloride:

  • Emergence delirium, hallucinations
  • Increased ICP, BP, HR
  • Nystagmus, muscle rigidity
  • Hypersalivation
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SAR of Ketamine:

  1. Arylcyclohexylamine structure:

    • Essential for NMDA antagonism.
    • Phenyl ring increases lipophilicity and CNS activity.
  2. Chiral center:

    • (S)-ketamine is more potent than (R)-ketamine.
  3. Cyclohexanone ring:

    • Maintains proper orientation for NMDA receptor binding.
  4. Amino group on side chain:

    • Allows for water solubility as hydrochloride salt.
  5. Lipophilic aryl ring:

    • Crucial for CNS penetration and rapid onset.

Synthesis of Ketamine:

 

Synthesis of Ketamine

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