Naloxone Hydrochloride
Pharmacology of Naloxone Hydrochloride
Naloxone hydrochloride, known by the brand name Narcan, is an opiate antagonist medication used primarily to reverse or lessen the effects of an opiate overdose. It was first synthesized in 1982 by Jack Fishman of Rockefeller University. Later that year, Harold Blumberg of New York Medical College, found that the newly synthesized drug was a “potent, rapid-acting, and relatively pure narcotic antagonist. ”. When delivered into the blood stream it travels to the brain. Naloxone’s hydrophilic properties allows it to easily cross the blood brain barriers where it can make its way to the opiate receptors of the brain and, due to its high affinity for the opiate receptors it outcompetes opiates and binds to the receptors. The three opioid receptors are the mu, kappa and delta receptors. They all have analgesic (pain relieving) properties when activated however the mu receptor also causes respiratory depression. This is important for naloxone because it has the highest affinity for the mu receptor. In a person with any levels of opiates, whether naturally or artificially there, naloxone will prevent those opiates from binding and affecting the opiate receptors. This in turn stops any symptoms of an opiate overdose, and thus the reason for its use in overdoses. Naturally occurring opiates come in the form of endorphins in your body. They are vitally important to short term survival in critical situations. Endorphins will bind to the opioid receptors and create a temporary effect by blocking pain. They are released following injury and can give a person time to remove them selves from a dangerous situation. The effect of endorphins is short lived and they eventually detach from the receptor and pain ensues. This is why you often don’t feel pain immediately after getting injury. When there is no presence of opiates in the brain naloxone will continue to bind to the opiate receptors, however it won’t have any symptomatic effects either positively or negatively. This is due to the fact that it is a pure opioid receptor antagonist. This means that it has no agonist effect, which in this case would be an analgesic effect seen by opiates. Earlier opioid receptor antagonists, like nalorphine, had antagonistic effect on one of the receptors but had an agonist effect on another making it inefficient at treating overdoses. Again for this reason naloxone is an ideal medication for opiate overdoses, because even if it is not an opiate overdose there is no adverse effects of giving the medication. This unique pharmacological effect had lead to the universal adaptation of the use of naloxone in any person with suspected opiate overdose.
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Authored for BIOL 291.00 Health Service and Biomedical Analysis, taught by Joan Slonczewski, 2016, Kenyon College.
