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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.