Dezocine

Absorption

Rapid and complete following intramuscular administration.

Toxicity

Symptoms of overdose include cold and clammy skin, confusion, nervousness, or severe restlessness, convulsions (seizures), severe dizziness, severe drowsiness, low blood pressure, pinpoint pupils of eyes, slow heartbeat, slow or troubled breathing and severe weakness.

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.)

The Uses of Dezocine

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).

Indications

Indicated in the treatment of moderate to severe pain.

Background

Dezocine is a partial opiate drug and is used for pain management. Dezocine is a very effective alternative to fentanyl when administered during outpatient laparoscopy, although is associated with an increased incidence of postoperative nausea.

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.

Pharmacokinetics

Dezocine is a parenteral narcotic analgesic possessing both agonist and antagonist activity. It is similar to morphine with respect to analgesic potency and onset and duration of action. The narcotic antagonist activity is greater than that of pentazocine.

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.

Metabolism

Hepatic, via conjugation (glucuronidation).