By Suleiman Tajudeen
CITIZENS COMPASS—Pentazocine is a generic opioid drug used to treat moderate to severe pain. In the United States of America (USA), It is available in combination with naloxone to reduce misuse potential. Pentazocine is more effective by activating certain opioid receptors while blocking others, providing pain relief. Here’s a historical perspective of pentazocine in Nigeria and globally;
Consumption, effects on the brain:
Background
Pentazocine was first synthesized in the 1950s and approved for medical use in 1964. It was initially used as a safer alternative to morphine due to its perceived lower risk of addiction. However, its potential for abuse and dependence soon became apparent. In the 1970s, recreational users discovered that combining pentazocine with tripelennamine produced a euphoric sensation, leading to widespread misuse.
Usage in Nigeria
In Nigeria, pentazocine has been widely used as a pre-anesthetic medication and post-operative analgesic, particularly in low- and middle-income settings. However, its off-label use has raised concerns about adverse events, especially in pediatric patients. A study in Northern Nigeria found that pentazocine was associated with multiple adverse events, including rapid breathing, fast pulse, and sleepiness. Clinical experience in Nigeria demonstrates that most SCD patients are prescribed pentazocine for acute severe pain episodes. Sometimes the result is addiction requiring in-patient hospitalisation. Other pain-relieving medications may also be abused.
A sizable number of patients admitted at the Lagos University Teaching Hospital, Psychiatry Department for substance abuse are people living with sickle cell disorder who have abused pentazocine.
Consumption patterns
Pentazocine can be administered orally or via injection. Unfortunately, its injectable form has been linked to tissue damage and severe injection site necrosis. In some cases, users have developed dependence on pentazocine, particularly when used for extended periods or in high doses.
When it become addictive
Pentazocine can become addictive when taken without a prescription, in excess, or for non-medical purposes. Repeated use can lead to physical dependence and tolerance, increasing the risk of addiction. Healthcare professionals and patients must be aware of the signs of misuse and addiction of pentazocine as follows:
Taken without a prescription: Using pentazocine without a valid prescription increases the risk of addiction.
Excessive use: Taking pentazocine in excess or for prolonged periods can lead to physical dependence and addiction.
Non-medical purposes: Using pentazocine for non-medical reasons, such as to feel euphoric or to self-medicate, can increase the risk of addiction.
Repeated use: Repeated use of pentazocine can lead to tolerance, making it more difficult to control use and increasing the risk of addiction.
Lack of medical supervision: Using pentazocine without regular medical check-ups or supervision can contribute to addiction.
Dose escalation: Gradually increasing the dose of pentazocine without medical guidance can lead to addiction.
Withdrawal symptoms: Experiencing withdrawal symptoms when attempting to stop or reduce pentazocine use can indicate addiction.
Neglecting responsibilities: Neglecting responsibilities, such as work or family obligations, to use pentazocine can be a sign of addiction.
Continued use despite harm: Continuing to use pentazocine despite physical, psychological, or social harm can indicate addiction.
Loss of control: Feeling unable to control pentazocine use or experiencing cravings can be a sign of addiction.
Functions in the body
Binding to opioid receptors: Pentazocine works by binding to opioid receptors in the brain and spinal cord, specifically kappa and mu receptors.
Pain relief: By activating kappa receptors and partially activating mu receptors, pentazocine helps to reduce pain perception.
Mixed agonist-antagonist: Pentazocine’s unique mechanism of action as a mixed agonist-antagonist contributes to its potential for abuse and addiction.
Effects on the brain of the abuser
Dopamine release: Pentazocine use can lead to the release of dopamine, a neurotransmitter associated with pleasure and reward.
Reward pathway activation: Activation of the brain’s reward pathway can contribute to the development of addiction.
Tolerance and dependence: Repeated use of pentazocine can lead to tolerance and physical dependence.
Changes in brain chemistry: Long-term pentazocine use can alter brain chemistry, leading to changes in mood, motivation, and behavior.
Cognitive impairment: Pentazocine abuse can impair cognitive function, including memory and decision-making.
Mood changes: Pentazocine abuse can lead to mood changes, including irritability, anxiety, and depression.
Increased risk of addiction: The brain’s response to pentazocine can increase the risk of addiction, particularly in individuals with a history of substance abuse.
Withdrawal symptoms: Stopping pentazocine use can lead to withdrawal symptoms, including anxiety, agitation, and physical discomfort.
Brain adaptation: The brain adapts to the presence of pentazocine, leading to changes in normal functioning and potentially contributing to addiction.
Long-term consequences: Long-term pentazocine abuse can have lasting consequences for brain health and overall well-being.
Major causes of addiction to pentazocine
Self-medication for chronic pain: Individuals with chronic pain may become dependent on pentazocine due to inadequate pain management or lack of access to alternative treatments.
Working in healthcare-related fields: Hospital workers or health personnel with sickle cell disease are more likely to abuse pentazocine, possibly due to easier access and familiarity with the medication.
Lack of regulation and oversight: Inadequate regulation of prescription drugs and pharmacies can contribute to pentazocine misuse.
Personal history of substance abuse: Individuals with a history of substance abuse are more susceptible to pentazocine addiction.
Mental health issues: Underlying mental health issues, such as depression or anxiety, can increase the risk of pentazocine addiction.
Social and environmental factors: Peer pressure, social norms, and environmental factors can contribute to pentazocine misuse.
Lack of education and awareness: Limited knowledge about the risks and consequences of pentazocine addiction can contribute to misuse.
Easy access: Easy access to pentazocine, particularly in healthcare settings, can increase the risk of addiction.
Genetic predisposition: Genetic factors can play a role in the development of pentazocine addiction.
Trauma or stress: Experiencing trauma or stress can increase the risk of pentazocine addiction as individuals may turn to the medication as a coping mechanism.
Prevalence of Pentazocine Addiction in Nigeria and Globally
The exact prevalence rates are not well-documented, studies suggest that pentazocine misuse is a significant issue, particularly among individuals with sickle cell disease in Nigeria. A study found that 64% of affected persons had previously failed to discontinue pentazocine abuse or medical rehabilitation.
Some studies have reported the following statistics:
A study in Benin City, Nigeria, found that 90.4% of SCD patients obtained pentazocine without a doctor’s prescription.
Another study in Nigeria observed that 63.6% of SCD patients who abused pentazocine did not need prescription papers to purchase the drug.
The mean duration of pentazocine abuse was 7.4 years, with a mean daily dose of 279mg.
Globally, pentazocine abuse is more prevalent in developing countries like Nigeria and India, whereas developed countries have seen a decrease in its abuse. The complications associated with pentazocine abuse include:
Physical complications: Chronic ulcers, abscesses, lymphedema, fibrous myopathies, and contractures.
Socioeconomic burden: Loss of job, reduced economic productivity, and increased healthcare costs.
Significant issues in Nigeria: Pentazocine misuse is a significant issue in Nigeria, particularly among individuals with sickle cell disease.
Limited data: Exact prevalence rates of pentazocine addiction are not well-documented, highlighting the need for further research.
Increasing trend: The misuse of pentazocine may be increasing, particularly among young people and individuals with chronic pain.
Regional variations: Prevalence rates may vary across different regions and populations.
Healthcare worker abuse: Healthcare workers, particularly those with access to pentazocine, are at risk of addiction.
Sickle cell disease: Individuals with sickle cell disease are disproportionately affected by pentazocine addiction.
Comorbidities: Individuals with comorbidities, such as chronic pain and mental health issues, are more susceptible to pentazocine addiction.
Socioeconomic factors: Socioeconomic factors, such as poverty and lack of access to healthcare, can contribute to pentazocine misuse.
Need for awareness: Raising awareness about pentazocine addiction and its risks can help prevent misuse.
General effects of pentazocine addiction
Physical complications: Chronic ulcers, abscesses, deep wounds, lymphedema, ankylosis, vascular injury, and venous thrombosis.
Psychological and social problems: Changes in mood or personality, increased risk-taking behavior, lying or stealing to obtain pentazocine, financial problems, and relationship issues.
Regular use of pentazocine may worsen the health condition of sickle cell patients (i.e. regular use of meperidine could lead to seizure disorder).
Increased risk of cardiovascular problems: Heart failure, myocardial infarction, and other cardiovascular issues.
Chronic ulcers: Pentazocine addiction can lead to chronic ulcers and other skin problems.
Abscesses and deep wounds: Injection site abscesses and deep wounds are common among individuals addicted to pentazocine.
Lymphedema: Pentazocine addiction can cause lymphedema, a condition characterized by swelling in the affected limb.
Ankylosis: Long-term pentazocine use can lead to ankylosis, a condition characterized by joint stiffness and limited mobility.
Vascular injury: Pentazocine addiction can cause vascular injury, including damage to blood vessels and increased risk of cardiovascular problems.
Increased risk of infections: Pentazocine addiction can…
To be continued…
Dr Suleiman Tajudeen is Director, Clinical Psychology, LUTH (Retired) & CEO/Director of Clinical Psychology, Clear Mind Psychological Consult, Km 15, Badagry Expressway, Ojo, Lagos State. +234 803 402 4457
