Dezocine
Encyclopedia
Dezocine was developed by American Home Products and is an opioid
analgesic
related to pentazocine
, with a similar profile of effects that include analgesic action and euphoria at low doses, but produces dysphoria
and hallucinations at high doses, most likely due to action at κ-opioid receptors
.
Dezocine has been found to be an effective painkiller comparable to meperidine (pethidine), and so is a more effective analgesic than pentazocine, but causes relatively more respiratory depression than pentazocine. It is a useful drug for the treatment of pain, but side effects such as dizziness limit its clinical application, and it can produce opioid withdrawal syndrome in patients already dependent on other opioids.
Dezocine is unusual among opioids as it is one of the only primary amines known to be an active opioid (along with bisnortilidine, an active metabolite of tilidine
). It is a mixed agonist-antagonist as with other drugs in this class, and despite having a stronger respiratory depressant effect than morphine, dezocine shows a ceiling effect on its respiratory depressive action so above a certain dose this effect does not get any more severe.
Opioid
An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
related to pentazocine
Pentazocine
Pentazocine is a synthetically prepared prototypical mixed agonist-antagonist narcotic drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain...
, with a similar profile of effects that include analgesic action and euphoria at low doses, but produces dysphoria
Dysphoria
Dysphoria is medically recognized as a mental and emotional condition in which a person experiences intense feelings of depression, discontent and indifference to the world around them.Mood disorders can induce dysphoria, often with a heightened risk of suicide, especially in...
and hallucinations at high doses, most likely due to action at κ-opioid receptors
Kappa Opioid receptor
The κ-opioid receptor is a protein that in humans is encoded by the OPRK1 gene. The κ-opioid receptor is one of five related receptors that bind opium-like compounds in the brain and are responsible for mediating the effects of these compounds...
.
Dezocine has been found to be an effective painkiller comparable to meperidine (pethidine), and so is a more effective analgesic than pentazocine, but causes relatively more respiratory depression than pentazocine. It is a useful drug for the treatment of pain, but side effects such as dizziness limit its clinical application, and it can produce opioid withdrawal syndrome in patients already dependent on other opioids.
Dezocine is unusual among opioids as it is one of the only primary amines known to be an active opioid (along with bisnortilidine, an active metabolite of tilidine
Tilidine
Tilidine , or tilidate is a synthetic opioid analgesic, used mainly in Germany, Switzerland and Belgium for treatment of moderate to severe pain, both acute and chronic.-Pharmacology:...
). It is a mixed agonist-antagonist as with other drugs in this class, and despite having a stronger respiratory depressant effect than morphine, dezocine shows a ceiling effect on its respiratory depressive action so above a certain dose this effect does not get any more severe.