Nalbuphine is an opioid agonist-antagonist analgesic, approved to treat severe pain. Nalbuphine is not a controlled substance, but it should be administered only by a professional, as it can cause adverse effects. The misuse of nalbuphine can occur and may lead to the development of dependence and addiction.
- Nalbuphine (Nubain) is an opioid analgesic medication, available only as an injection, which must be administered professionally.
- Nalbuphine is a mixed opioid agonist-antagonist, which means that it also exerts some opioid blocking effects alongside its analgesic effects.
- Although nalbuphine abuse and addiction are not as common as with other opioids, they can still occur.
What is nalbuphine?
Nalbuphine (Nubain) is a synthetic opioid analgesic, or pain relief medication. It is chemically similar to both naloxone, an opioid antagonist, and oxymorphone, a potent opioid analgesic. Nalbuphine works by acting as an agonist at kappa opioid receptors and as an antagonist at mu opioid receptors. [1]
Because of its dual action, nalbuphine can be used both as an analgesic, with an effect as potent as morphine, and as an antagonist, or opioid reversal agent, at doses equal to or lower than its analgesic dose. This means it can block dangerous effects caused by opioids, such as respiratory depression, and can also cause withdrawal in those with opioid dependency. [1][2]
Nalbuphine is approved by the Food and Drug Administration (FDA) for use in the treatment of severe pain that cannot be managed by alternative treatments. It can also be used as pre- or post-operative analgesia and obstetric anesthesia. [1][2]
Nalbuphine can also be used off-label, for non-FDA-approved purposes. This includes opioid-related issues, such as respiratory depression, urinary retention, or pruritus. [2]
Clinical considerations: Dosing, side effects, and monitoring
As nalbuphine can be used for a range of purposes, the appropriate dosage will vary and may depend on individual factors. As with all opioids, nalbuphine should be used with caution and requires careful monitoring throughout treatment.
Formulations and dosing
Nalbuphine is available as an injection that can be administered intravenously, intramuscularly, or subcutaneously. Injectable solutions are available in 10 mg/ml and 20 mg/ml strengths. Nalbuphine is not available as an oral formulation as it has poor oral bioavailability. [2]
- A standard dose for an adult weighing 70 kg is 10 mg, which can be administered every three to six hours. People who are not opioid-tolerant can be given a maximum single dose of 20 mg, and up to a maximum daily dose of 160 mg. [2]
- People with opioid dependence should be administered a reduced dose of 75% of the recommended amount. As such, a standard dose will be 7.5 mg, and the maximum daily dose will be 120 mg. A reduced dose can help to reduce the risk of withdrawal symptoms precipitated by nalbuphine, and careful monitoring will be required. [2]
- Older adults can be at increased risk of respiratory depression, and nalbuphine should be used with extreme caution if necessary. [1]
- People with kidney or liver impairment should be administered the medication in a reduced dose and with caution. [1]
- Nalbuphine is sometimes administered during labor, although this can cause risks to the fetus. If required, nalbuphine can be used within the first three days of breastfeeding, after which alternative analgesics should be used. The infant will require monitoring during this time to manage any adverse effects. [1][2]
Side effects and monitoringÂ
Side effects are common with the administration of nalbuphine. Often, side effects can be managed without professional intervention and will subside. Common side effects of nalbuphine include: [1][2]
- Sedation
- Sweating
- Nausea and vomiting
- Dizziness
- Dry mouth
- Headache
- Nervousness
- Changes in mood
- Unusual dreams or nightmares
- Numbness
- Derealization
- Depersonalization
- Changes in heart rate
- Bitter taste
- ShakingÂ
- WeaknessÂ
Side effects of nalbuphine that may be more serious and therefore may require professional advice and treatment include: [1][2]
- DepressionÂ
- Agitation and hostility
- Anxiety
- Severe confusion
- Hallucinations
- Delusions
- SeizuresÂ
- Extreme changes in heart rate and blood pressure
- Trouble breathing
- Itching, rash, or hives
- Difficulty with speech
- Urinary urgency
- Vision impairment
Nalbuphine must always be administered by a licensed medical professional, who can also provide close monitoring after administration. Should serious side effects emerge, treatments may be required to manage the individual’s safety.
Interactions
Nalbuphine can interact with other substances, causing an increased risk of adverse effects. This includes: [1][2]
- CNS depressants: Central nervous system (CNS) depressants, including alcohol, other opioids, and benzodiazepines, can cause an increased risk of oversedation, respiratory depression, and coma when used alongside nalbuphine and may be life-threatening.Â
- MAOIs: Monoamine oxidase inhibitors (MAOIs), a type of antidepressant, should not be used within 14 days of nalbuphine, as this can cause serotonin syndrome or opioid toxicity.
- Serotonergic drugs: Using serotonergic drugs, including antidepressants, tramadol, triptans, and certain muscle relaxants, alongside nalbuphine can increase the risk of serotonin syndrome. If these drugs are medically necessary, doses should be adjusted, and careful monitoring is advised.Â
- Anticholinergic drugs: Effects of anticholinergic drugs, including some antihistamines, asthma medications, Parkinson’s disease medications, and anti-nausea medications, can be exacerbated by nalbuphine and may cause dangerous urinary retention or constipation.
- Muscle relaxants: Using muscle relaxants alongside nalbuphine can increase the risk of respiratory depression and should be administered with caution.
- Diuretics: Nalbuphine can reduce the effect of diuretics. It may be necessary to use an increased dose of diuretics when used concurrently.
Nalbuphine vs. Other opioid analgesics
Opioid analgesics produce a pain-relieving effect through opioid receptor agonist mechanisms. Some opioid analgesics, such as oxycodone and morphine, are opioid agonists, while others are mixed agonists-antagonists, such as nalbuphine and pentazocine. [3]
Opioid antagonist drugs block or reverse the effects of opioids and are commonly used in opioid management, such as naloxone.Â
Mixed agonist-antagonist drugs produce analgesic effects only up to a certain dose, with no greater effect beyond this point, known as a ‘ceiling effect’. They can also cause the onset of withdrawal symptoms in a person with opioid dependence. [1]
Nalbuphine is as potent as morphine in terms of its analgesic qualities. However, compared to morphine and other opioid agonists, nalbuphine does not cause the same level of euphoria and rewarding effects, thus reducing its addiction potential. [1][3]
Abuse potential, dependence, and misuse risks
Compared to most other opioids, nalbuphine has a lower potential for abuse and addiction. This is because of its antagonist effect on mu opioid receptors, which prevents the euphoric effects that are commonly associated with drug abuse and addiction. [3] However, some people misuse and abuse nalbuphine because of its sedating and analgesic effects, which can contribute to the development of physical dependence and addiction.Â
For example, some reports suggest that nalbuphine misuse is most common among bodybuilders, who use the drug for its analgesic effects, so that they can train without pain. These reports show that nalbuphine may be used alone, with performance-enhancing drugs such as anabolic steroids, or with psychoactive drugs such as cocaine. Among these individuals, all met the criteria for opioid dependence. [4]
Because of its opioid agonist effects, nalbuphine can lead to withdrawal symptoms, particularly when it is stopped abruptly. This can include restlessness, irritability, aches and pains, insomnia, nausea and vomiting, increased heart rate and blood pressure, sweating, and chills. [1]
Overdose and emergency management
Nalbuphine use can cause overdose, whether used alone or alongside other substances, and may cause fatal effects. The risk of overdose can be particularly high when nalbuphine is used with other opioids or CNS depressants. [1]
Overdose symptoms can include: [1][2]
- Extreme weakness
- Extreme sedation
- Difficulty breathing
- Stopped breathing
- Cold and clammy skin
- Constricted pupils
- Severe change in heart rate and blood pressure
- ArrhythmiaÂ
- Cardiac arrest
- Loss of consciousness
In the event of an overdose, emergency care will be required. This can include airway management and ventilation, oxygen administration, and other symptom management. Naloxone should be administered to reverse opioid effects. [1]
Is nalbuphine a controlled substance?
Nalbuphine is not a controlled substance due to its lower potential for abuse and use as an opioid blocking agent. However, it is only available on prescription and can only be administered by a professional. Misusing nalbuphine can increase the risk of dangerous or fatal effects.
Nalbuphine in the context of pain and substance use treatment
Nalbuphine can be dangerous when used by individuals with an opioid use disorder (OUD) or opioid dependence, as it can cause the onset of withdrawal symptoms. As such, people in active opioid addiction or those using methadone maintenance treatment should not be administered nalbuphine. [5]Â
People in substance use recovery should be prescribed non-opioid pain relief where possible, to help prevent relapse. However, if opioid pain relief is required, nalbuphine may be appropriate for those who have not recently taken opioids, as it is less likely to cause euphoric or reinforcing effects than other opioid analgesics. [5]
People with a history of or current substance use disorder, who are experiencing severe pain, should seek advice from a medical professional who can provide appropriate and supportive care.Â
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