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What is Ketamine?
Ketamine (brand name: Ketalar) is a dissociative injected anesthetic (blocks sensory perception) that has been available by prescription in the U.S. since the 1970s for human and veterinary uses. Esketamine (Spravato), the S-enantiomer of racemic ketamine, was approved in 2019 for treatment-resistant depression and is approved for use in depressed patients with acute suicidal ideation or behavior. Ketaset is the brand name of a surgical anesthesia used by veterinarians
Dissociative drugs can lead to distortion of sights, colors, sounds, self, and one’s environment. Ketamine is available in a clear liquid or off-white powder form for intravenous injection or as a nasal spray. Examples of other dissociative drugs include phencyclidine (PCP) and dextromethorphan (DXM).
Why is Ketamine Used Medically?
- Ketamine can provide pain relief and short-term memory loss (for example, amnesia of a medical procedure).
- In surgery, it is used an induction and maintenance agent for sedation and to provide general anesthesia.
- It has also been used for pain control in burn therapy, battlefield injuries, and in children who cannot use other anesthetics due to side effects or allergies.
- Ketamine, through blocking at the N-methyl-D-aspartate (NMDA) site, has rapid action in controlling symptoms of depression and acute suicidal ideation.
- At normal doses, it is often preferred as an anesthetic in patients at risk of bronchospasm and respiratory depression.
Pharmacology of Ketamine
Ketamine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist, and it blocks HCN1 receptors. However, at higher doses it may also bind to the opioid mu and sigma receptors. It disrupts the neurotransmitter (brain chemical) glutamate. Glutamate is involved with learning, memory, emotion, and pain recognition. It can exhibit sympathomimetic activity which can lead to rapid heart rate and elevated blood pressure.
It is related to phencyclidine (PCP), but has less than 10% of the potency of pure PCP.
This agent is a lipid soluble compound, has an initial rapid distribution and large volume of distribution, with a half-life of 10 to 15 minutes. Secondarily, the drug distributes into peripheral tissues with a slower elimination half-life of up to 3 hours, undergoes hepatic metabolism and is excreted in the urine.
How is Ketamine Abused?
In addition to its legal, medical uses, ketamine and and synthesized analogs have become drugs of abuse with hallucinogenic properties. It has also been used as a “date rape” drug.