Tapentadol is a relatively new, centrally acting pain relief medication. [1] It has a dual action, making it useful for treating various types of pain, including acute, chronic, and neuropathic pain. [1] However, tapentadol does have the potential to cause dependence and addiction, so it should be prescribed with caution by clinicians.Â
- Tapentadol is a painkiller with a dual action, helping it to be effective for different types of pain.
- Tapentadol has a high potential for abuse and addiction, and is subsequently a Schedule II controlled substance.
- Stopping tapentadol abruptly can lead to withdrawal symptoms similar to those from other opioids.
Tapentadol: Dual-action pain relief
Tapentadol is an opioid medication, but its dual action on both opioid and noradrenaline receptors gives it a unique quality. [1][2] Tapentadol has been FDA-approved since 2008, and its dual action makes it effective for acute, chronic, neuropathic, and cancer pain. [1][2] This, combined with its favourable side effect profile compared to other opioid medications, means tapentadol has become increasingly recognised as a preferred option for treating pain. [2]
How tapentadol works
Tapendatol affects two different receptors in the brain, working as both a μ-opioid receptor agonist and a noradrenaline reuptake inhibitor. [2] Regular opioids usually only bind to opioid receptors, which is where tapentadol differs from them. [3] Tapendatol’s effect on noradrenaline receptors helps to enhance its therapeutic benefit on both chronic and neuropathic pain (nerve pain). [1][4] This dual mechanism makes tapentadol versatile, but also allows for ‘opioid-sparing’. [2] This means it can provide similar pain relief to other opioids, but at a lower dose, leading to less severe side effects. [2]
What tapentadol is used for
Tapentadol is primarily used to treat pain. Research has demonstrated that tapentadol is effective for treating moderate-severe acute and chronic pain, but it is not recommended for mild pain. [2] It’s also effective in treating neuropathic pain, primarily due to its effect on noradrenaline receptors. [1][2]Â
Tapentadol can also be used for cancer pain, particularly in those experiencing side effects from higher doses of opioids. [2] Tapentadol has also been used extensively for people with musculoskeletal and osteoarthritic pain, including pain related to rheumatoid arthritis.Â
Tapentadol dosage and forms
Tapentadol is available in both immediate-release (IR) and extended-release (ER) forms. For IR tapentadol, the dose is typically 50-100mg every 4-6 hours, depending on pain intensity. [5] The maximum daily dose is 700mg on the first day, and 600mg on subsequent days. [5]
With ER tapentadol, the starting dose is usually 50mg every 12 hours, increasing to a maximum of 250mg every 12 hours, depending on response and pain intensity. [6] It’s noted that there is an increased risk of sedation and respiratory depression when switching from IR to ER formulations of tapentadol. [6]
Tapentadol side effects
Tapentadol is associated with several possible side effects. Tapentadol side effects are similar to other opioids, and include: [5]
- Nausea/vomiting
- Sedation & drowsiness
- Dizziness
- Respiratory depressionÂ
- ConstipationÂ
- Dry mouth
- Itching
- Headaches
The risk of side effects can be reduced by taking tapentadol at the lowest effective dose, and under the guidance of a medical professional.Â
Is tapentadol addictive?
Tapentadol does carry a high potential for addiction and dependence. [5] Addiction is defined by chronic drug-seeking despite negative consequences, whereas dependence is caused by the body becoming adapted to a drug, causing withdrawal symptoms if it’s stopped. [7] While there is some overlap between the two, it’s possible to be dependent on a drug without being addicted. When prescribing tapentadol, clinicians should do this in a way that reduces dependence and addiction risks, for example, short course lengths and lower doses.
As a result, tapentadol is a Schedule II controlled substance, reflecting its high potential for abuse. [5] Tapentadol shares its Schedule II classification with oxycodone, fentanyl, and cocaine, being viewed as having similar risks to these drugs. [8] This classification has resulted in stricter prescribing guidelines and monitoring compared to non-controlled medications.
Tapendatol misuse involves using it for its sedating and euphoric effects. Whilst this can involve taking higher doses orally, there have been increasing reports of tablets being crushed and injected, being used as an alternative to heroin. [9] This carries with it increased risks from infection and overdose. Using higher doses can also cause individuals to develop tolerance, meaning they require higher doses of tapentadol to cause the same effects.Â
Tapentadol withdrawal
Withdrawal symptoms occur when a person has become dependent on a drug or medication and suddenly cuts back or stops taking it. Tapentadol withdrawal, as with other opioids, can cause many symptoms. However, research has shown that withdrawal symptoms are experienced less frequently with tapentadol compared with other opioids. [10] The possible withdrawal symptoms include: [11]
- Nausea/vomiting
- Diarrhea
- Muscle aches
- Insomnia
- Sweating
- Runny nose
- Watery eyes
- High heart rateÂ
- High blood pressure
Withdrawal timeline
Most of the time, opioid withdrawal begins within 24 hours of the last dose, peaks after a few days, and subsides within about a week. Withdrawal timelines may differ slightly for instant versus extended release formulations. The typical timeline for tapentadol withdrawal is as follows:
- Day 1: Withdrawal symptoms typically start to occur within 24 hours after taking the last dose. This timeframe can be slightly longer if taking ER preparations.Â
- Day 2-4: Withdrawal symptoms are likely to be most intense during this period.
- Day 5: From around day 5, withdrawal symptoms should start to reduce.
Stopping tapentadol abruptly increases the chance of withdrawal symptoms. If an individual is planning to stop tapentadol after a period of regular use, a medical professional should provide guidance on how to safely taper down the dose. Tapering is important to help reduce withdrawal symptoms.
Tapentadol vs. Other similar opioids
Tapentadol has similar effects to other opioids, but differs slightly because it also works on norepinephrine. This provides a dual-action mechanism of targeting pain and can be effective for nerve pain and arthritic pain, which traditional opioids are less effective in treating.
Below is a table comparing tapentadol to tramadol and oxycodone, two commonly used opioids.Â
| Tapentadol [1] | Tramadol [12] | Oxycodone [13] | |
|---|---|---|---|
| Schedule | Schedule II | Schedule IV | Schedule II |
| Mechanism | μ-opioid receptor agonist, noradrenaline reuptake inhibitor. | μ-opioid receptor agonist, serotonin, and noradrenaline reuptake inhibitor. | Agonist to multiple opioid receptors. |
| Abuse potential | High | Moderate | High |
Overdose risk and safety
Tapentadol overdose is serious and potentially life-threatening. More people overdose on opioids each year than on any other type of drug, and the risk of fatal overdose is highest when combining opioids with alcohol or other CNS depressants. [14] Opioid-naive individuals, those who take high doses, or those who inject tapentadol, are at an increased risk of overdose.
Signs of tapentadol overdose include:
- Extreme sedation
- Slow breathing
- Pinpoint pupils
- Loss of consciousness [14]
To maintain safety when using tapentadol, it should only be taken as prescribed by a medical professional and should not be combined with other substances that also cause central nervous system depression, such as benzodiazepines and alcohol. If you suspect someone has had a tapentadol overdose, you should call 911 for immediate medical assistance. Naloxone (Narcan) can be used to reverse the effects of tapentadol overdose.Â
Who should avoid tapentadol
Tapentadol should be avoided in the following groups of people: [5]
- Anyone under the age of 18.
- During pregnancy or when breastfeeding.
- Individuals with impaired liver or kidney function.
- Individuals with impaired lung function.Â
- Individuals with gastrointestinal problems, particularly paralytic ileus.
- Individuals with a history of addiction, particularly opioid use disorder.
Before prescribing tapentadol, your medical professional will ensure there are no interactions with any other medications you take.
When to seek help
If you, or someone you know, is struggling with tapentadol misuse or addiction, it’s important to get professional help. Signs of addiction or misuse include taking tapentadol in larger amounts than prescribed, being unable to cut down despite wanting to, continuing to use tapentadol despite negative consequences, or experiencing withdrawal symptoms when stopping. If these features resonate with you, please reach out to a professional as soon as possible.Â
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