Description
Dezocine is an injectable agonisthtagonist analgesic indicated when an opioid
analgesic is suitable for the management of pain. The drug differs from other opioid
agonisthtagonists by having a high affinity for both the mu and delta receptors and a
low effect on kappa receptors. Dezocine is reported to have a rapid onset of action,
short half-life and low abuse potential with insignificant side effects.
Originator
Wyeth-Ayerst (American Home Products) (U.S.A.)
Uses
Dezocine is an opioid analgesic that is related to Pentazocine (P274300). Dezocine is used to relieve post-operative pain with its potency comparable to Meperidine (M223900).
Definition
ChEBI: (7S,8S)-7-Amino-8-methyl-5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogen at position 8 and one of the hydrogens at position 6 are substituted by each end of a tetramethylene bridge. A synthetic opioid analgesic, it
has mixed opiod agonist and antagonist properties. Although it is used for pain management, it can produce opioid withdrawal syndrome in patients already dependent on other opioids, and its clinical application is limited by side effects such as dizziness.
Brand name
Dalgan (AstraZeneca).
Biological Functions
Dezocine (Dalgan) is a synthetic aminotetralin derivative
with potent agonist–antagonist effects.The onset of
activity and potency as an analgesic are comparable to
those of morphine. Although the drug requires glucuronidation
during metabolism, patients with hepatic
insufficiency clear it normally.The main route for clearance
is the kidney.Thus, patients with renal dysfunction
are prone to buildup of dezocine over time. As an antagonist,
dezocine is more potent than pentazocine. As
an agonist, dezocine produces analgesia and respiratory
depression (which is readily reversed by naloxone), but
unlike pentazocine, it has little if any effect on the cardiovascular
system.
Dezocine is indicated as an analgesic for moderate
to severe pain. In addition, it shows promise in chronic
pain states, such as with victims of severe burns.
Contraindications and adverse effects of the drug are
similar to those described for morphine. No tendency
toward abuse has been demonstrated thus far.
Mechanism of action
Dezocine is classified as a mixed agonist/antagonist. The SAR of dezocine is unique among the
opioids. It is a primary amine, whereas all other nonpeptide opioids are tertiary amines. Its exact
receptor selectivity profile has not been reported; however, its pharmacology is most similar to that
of buprenorphine. It seems to be a partial agonist at μ receptors, to have little effect at κ receptors,
and to exert some agonist effect at δ receptors.
Clinical Use
It is useful for the treatment of moderate to severe pain. It is available for intramuscular and intravenous dose. The drug is indicated for postoperative and cancerinduced pain.
