From the Guidelines
Nucynta (tapentadol) should be used with caution and as a last resort for managing chronic neuropathic pain due to its high risk of addiction and modest pain reduction benefits, as evidenced by recent studies 1.
Introduction to Nucynta
Nucynta (tapentadol) is a prescription pain medication that works as both an opioid agonist and norepinephrine reuptake inhibitor, making it effective for moderate to severe acute and chronic pain. It's available in immediate-release tablets (50-100mg every 4-6 hours as needed) and extended-release formulations (50-250mg twice daily).
Efficacy and Safety
The efficacy and safety of tapentadol have been evaluated in several studies, including a systematic review and meta-analysis that found the evidence supporting its effectiveness in reducing neuropathic pain to be inconclusive 2, 1. Additionally, the use of extended-release tapentadol is not generally recommended as a first- or second-line therapy due to its high risk of addiction and safety concerns compared with the relatively modest pain reduction benefits.
Side Effects and Precautions
Common side effects of Nucynta include nausea, dizziness, constipation, and drowsiness. As with all opioids, Nucynta carries risks of dependence, addiction, and respiratory depression, especially at higher doses or when combined with other central nervous system depressants. Patients should avoid alcohol while taking Nucynta and should inform their healthcare provider about all other medications they're taking to prevent dangerous interactions.
Key Considerations
- Nucynta should be used at the lowest effective dose for the shortest duration necessary, with careful monitoring for side effects.
- Patients with a history of substance abuse or addiction should be closely monitored while taking Nucynta.
- Alternative pain management options, such as duloxetine, should be considered before initiating Nucynta therapy, especially for chronic neuropathic pain conditions like diabetic peripheral neuropathy 2, 1.
From the FDA Drug Label
NUCYNTA (tapentadol) tablets are a mu-opioid receptor agonist, available in immediate-release film-coated tablets for oral administration, containing 58.24, 87.36 and 116. 48 mg of tapentadol hydrochloride in each tablet strength, equivalent to 50, 75, and 100 mg of tapentadol free-base, respectively. The chemical name is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol monohydrochloride, and it has the following chemical structure: NUCYNTA tablets expose users to risks of addiction, abuse, and misuse, which can lead to overdose and death. NUCYNTA tablets are an opioid analgesic indicated for the management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate
Key Information about Nucynta (Tapentadol)
- Drug Class: Mu-opioid receptor agonist
- Indication: Management of acute pain severe enough to require an opioid analgesic
- Dosage Forms: Immediate-release film-coated tablets for oral administration
- Available Strengths: 50 mg, 75 mg, and 100 mg of tapentadol free-base
- Risks: Addiction, abuse, misuse, overdose, and death; respiratory depression; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines or other CNS depressants 3, 4, 5
From the Research
Mechanism of Action
- Tapentadol (Nucynta) is a centrally acting synthetic analgesic that exerts its effects via two mechanisms: mu-opioid receptor agonism and norepinephrine reuptake inhibition 6, 7, 8
- This dual mechanism of action allows for a synergistic effect on pain relief 8
Clinical Use
- Tapentadol is approved for the relief of moderate to severe acute pain in patients aged 18 years and older 6, 7, 9
- It is also approved for the treatment of chronic moderate to severe pain, including painful diabetic neuropathy 7, 8
- Tapentadol is available in immediate-release (IR) and extended-release (ER) formulations 7, 8
Efficacy and Safety
- Clinical trials have shown that tapentadol IR is effective in relieving moderate to severe acute pain, with a similar analgesic effect to oxycodone IR but with fewer gastrointestinal adverse effects 6, 7
- Tapentadol ER has also been shown to be effective in relieving chronic moderate to severe pain, with fewer gastrointestinal adverse effects compared to oxycodone controlled release 7, 8
- Common side effects of tapentadol include nausea, vomiting, dizziness, and somnolence 7
- Tapentadol has a lower risk of opioid-related gastrointestinal adverse events compared to traditional opioid agonists 6, 7
Toxicity and Abuse
- There have been reports of fatal intoxication due to tapentadol overdose, with possible mechanisms of death including respiratory depression, central nervous system depression, and serotonin syndrome 10
- Tapentadol is classified as a Schedule II controlled substance, indicating a high potential for abuse and dependence 9