Action and Spectrum

Actions and Spectrum: 

dezocine is an opioid analgesic that is used for pain management. It has both agonist and antagonist properties at opioid receptors. Its mechanism of action involves binding to and modulating various opioid receptors in the central nervous system. 

• Mu Receptors (μ-opioid receptors): dezocine is a partial agonist at mu receptors. Mu receptors are associated with pain relief, sedation, and euphoria. As a partial agonist, dezocine can activate these receptors to a certain extent, producing analgesic effects, but its activity is limited compared to full agonists like morphine or fentanyl. This partial agonism helps reduce the risk of respiratory depression and other side effects associated with potent mu receptor agonists. 
• Kappa Receptors (κ-opioid receptors): dezocine is also a Kappa receptor antagonist. Kappa receptors are involved in analgesia, dysphoria, and sedation. By acting as an antagonist, dezocine can counteract the activation of kappa receptors, potentially reducing the adverse emotional effects and sedation associated with kappa receptor activation. 
• Delta Receptors (δ-opioid receptors): dezocine may also interact with delta receptors, which are involved in pain modulation and other neurobehavioral effects. Its effects on delta receptors contribute to its overall analgesic properties. 

The spectrum of activity for dezocine primarily focuses on managing moderate to moderately severe pain. Its combination of partial mu receptor agonism and kappa receptor antagonism provides effective pain relief while minimizing the risk of severe respiratory depression and other side effects commonly associated with more potent opioid agonists. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Mild gastrointestinal discomfort  

Dizziness 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: Patients with known hypersensitivity or allergy to dezocine or its components should not use this medication. 
• Respiratory depression: dezocine is an opioid analgesic that can potentially cause respiratory depression, especially at higher doses. It should be avoided in patients with severe respiratory conditions or compromised respiratory function. 
• Acute or Severe Bronchial Asthma: dezocine can suppress respiratory function, which may worsen acute or severe bronchial asthma or other chronic obstructive pulmonary diseases. 
• Head Injury and Increased Intracranial Pressure: Opioids like dezocine can increase intracranial pressure, making them unsuitable for patients with head injuries, intracranial lesions, or conditions that may lead to increased pressure within the skull. 
• Central Nervous System (CNS) Depression: dezocine can cause sedation and central nervous system depression. It should be used cautiously or avoided in patients with impaired consciousness, altered mental status, or conditions that can lead to CNS depression. 
• Paralytic Ileus: Opioids can exacerbate or prolong paralytic ileus (a condition where the intestines stop moving). Therefore, dezocine should be avoided in patients with this condition. 
• Substance Abuse or Addiction: Patients with a history of substance abuse or addiction, including opioid addiction, should be cautious when using dezocine due to potential misuse and dependency. 

Caution: 

• Elderly Patients: Elderly patients may be more sensitive to the effects of dezocine, including sedation, respiratory depression, and other side effects. Dosage adjustments might be necessary to avoid excessive sedation or respiratory depression. 
• Renal and Hepatic Impairment: Patients with impaired kidney or liver function might experience altered drug metabolism and clearance, leading to the potential accumulation of dezocine or its metabolites. Dose adjustments may be necessary in these patients to prevent adverse effects. 
• Patients with CNS Conditions: Patients with conditions affecting the central nervous system, such as increased intracranial pressure, head injuries, or seizures, should use dezocine with caution due to the potential for exacerbating these conditions. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

dezocine is an opioid analgesic with a complex pharmacological profile, combining the properties of both agonists and antagonists at various opioid receptors. It is used for pain management, particularly for moderate to severe pain.  

• Mu (μ) Receptors: dezocine is a partial agonist at mu receptors. These receptors are involved in pain relief, sedation, and respiratory depression. As a partial agonist, dezocine can activate mu receptors to a certain extent, producing analgesia and other opioid-mediated effects, but with a ceiling effect that limits its activity. This feature reduces the risk of severe respiratory depression compared to full mu agonists like morphine. 
• Kappa (κ) Receptors: dezocine is an antagonist at kappa receptors. These receptors are involved in analgesia, diuresis, and dysphoria. dezocine may reduce the adverse emotional effects and sedation associated with kappa receptor activation by antagonizing kappa receptors. 
• Delta (δ) Receptors: dezocine’s effects on delta receptors contribute to its analgesic properties. Delta receptors are involved in pain modulation and other neurobehavioral effects. 

Pharmacokinetics: 

Absorption 

• dezocine is available in various formulations, including intravenous (IV), intramuscular (IM), and subcutaneous (SC) injections. 
• dezocine’s onset of action is rapid when administered intravenously due to direct introduction into the bloodstream. 
• Other routes of administration might result in varying rates of absorption.

Distribution 

• dezocine’s distribution in the body involves central and peripheral compartments, including the central nervous system. 
• It can cross the blood-brain barrier, allowing it to affect the central nervous system.

Metabolism 

• dezocine undergoes metabolism in the liver primarily through cytochrome P450 enzymes, with CYP3A4 and CYP2D6 playing significant roles in its metabolism. 
• The exact metabolites of dezocine might vary, and their pharmacological activities can contribute to the drug’s overall effects. 

Elimination and Excretion 

• Both dezocine and its metabolites are eliminated primarily through the kidneys via urine.  
• The elimination half-life of dezocine is around 2 to 3 hours, meaning it takes half of the administered dose to be cleared from the body. 

Adminstartion

Administration: 

Intravenous (IV) Administration: 

• Intravenous administration is typically used in acute settings, such as hospitals or clinics, where immediate pain relief is required. 
• dezocine is delivered directly into the bloodstream through a vein. 
• This route provides rapid onset of action, as the drug doesn’t need to be absorbed through tissues.

Intramuscular (IM) Administration: 

• Intramuscular administration involves injecting dezocine into a muscle, usually the thigh or upper arm. 
• This route allows slower absorption than IV administration but provides rapid pain relief. 

Subcutaneous (SC) Administration: 

• Subcutaneous administration involves injecting dezocine into the layer of tissue just beneath the skin. 
• This route can provide sustained pain relief over a longer duration than IV or IM administration. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: dezocine 

Why do we use dezocine? 

dezocine is primarily used to manage moderate to moderately severe pain. It is an opioid analgesic with a unique pharmacological profile, combining partial agonist and antagonist properties at different opioid receptors.  

• Pain Management: dezocine is prescribed to relieve various types of pain, including postoperative pain, pain related to medical procedures, and acute or chronic pain conditions. Its combination of partial mu agonism and kappa receptor antagonism allows analgesia while potentially reducing the risk of severe respiratory depression. 
• Surgical pain: dezocine may be used to manage pain following surgical procedures, including primary and minor surgeries. 
• Labor Pain: In some cases, dezocine may be used to manage pain during labor and childbirth, particularly if a more controlled analgesic effect is desired than full mu agonists. 
• Trauma and Injury Pain: dezocine might be used for managing pain resulting from traumatic injuries or accidents. 
• Medical Procedures: It can manage pain associated with medical procedures, such as diagnostic tests, biopsies, or other interventions. 
• Chronic Pain: While dezocine’s use is more commonly associated with acute pain, it might also be considered for some instances of chronic pain when other treatment options have been explored.