From the Guidelines
Nalbuphine should be avoided in patients receiving opioid addiction treatment due to its potential to precipitate acute opioid withdrawal 1. When considering the use of nalbuphine, it is essential to weigh the potential benefits against the risks, particularly in patients with a history of opioid dependence.
- Nalbuphine is a synthetic opioid analgesic that acts as a partial agonist at mu-opioid receptors and an agonist at kappa-opioid receptors.
- It is primarily used for the management of moderate to severe pain, particularly in perioperative settings.
- The typical adult dosage is 10-20 mg administered intramuscularly, subcutaneously, or intravenously every 3-6 hours as needed for pain, with a maximum daily dose of 160 mg.
- Nalbuphine has a ceiling effect for respiratory depression, making it potentially safer than pure mu-opioid agonists like morphine in terms of this side effect.
- However, its use in patients receiving opioid addiction treatment is contraindicated due to the risk of precipitating acute opioid withdrawal 1.
- In patients who are not receiving opioid addiction treatment, nalbuphine can be used to treat opioid-induced pruritus, as it is a mixed agonist/antagonist opioid analgesic 1.
- Common side effects of nalbuphine include sedation, dizziness, nausea, vomiting, and sweating.
- Nalbuphine is classified as a Schedule II controlled substance in many countries due to its potential for abuse, though this risk is considered lower than with pure mu-opioid agonists.
- It should be used cautiously in patients with respiratory conditions, head injuries, or liver/kidney impairment, and is contraindicated in patients with hypersensitivity to the drug.
From the FDA Drug Label
Nalbuphine Hydrochloride Injection is indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. The primary use of Nalbuphine is for the management of severe pain.
- Key points:
- Nalbuphine can be used as a supplement to balanced anesthesia.
- It can be used for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery.
- The use of Nalbuphine should be reserved for patients for whom alternative treatment options are inadequate 2. Important considerations:
- Nalbuphine should not be used for an extended period unless the pain remains severe enough to require an opioid analgesic and alternative treatment options continue to be inadequate.
- Dosage should be adjusted according to the severity of the pain, physical status of the patient, and other medications which the patient may be receiving 3 2.
From the Research
Nalbuphine Overview
- Nalbuphine is an agonist/antagonist analgesic that has been commercially available for 40 years for the treatment of acute pain 4.
- It has a unique pharmacology, acting as a µ antagonist and partial κ agonist, which provides benefits such as less nausea, pruritus, and respiratory depression compared to morphine 4.
Pharmacological Properties
- Nalbuphine is approximately equipotent to morphine in analgesic activity after parenteral administration 5.
- It produces a "ceiling" effect on respiratory depression, beyond which further depression does not readily occur 5, 6.
- Nalbuphine has a relatively low abuse potential compared to other opioids, but its potential for abuse cannot be ruled out 5, 4.
Clinical Use
- Nalbuphine can be used to reverse opioid-induced respiratory depression, but it may cause side effects such as hypertension, increased heart rate, and agitation 6.
- It is not recommended for use in patients on sustained-release opioids, as it can cause withdrawal symptoms 4.
- Nalbuphine may be a useful alternative to morphine in patients with moderate to severe pain, particularly in those who are at risk of respiratory depression 5.
Comparison to Other Analgesics
- Nonsteroidal anti-inflammatory drugs (NSAIDs) and acetaminophen may be effective alternatives to opioids, including nalbuphine, for acute pain management 7.
- Combination therapy using a small amount of opioid with a nonopioid pain reliever may be effective and reduce opioid consumption 7.
- Nalbuphine has been compared to naloxone as an antagonist of opioid-induced respiratory depression, with similar efficacy and safety profiles 8.