Tapentadol

Description

Tapentadol is an atypical opioid drug used for the treatment of moderate to severe acute and severe chronic pain which can be managed only with opioids. It belongs to the opioid group of drugs, which can be broadly described as ‘depressant’ drugs in that their various clinical effects are in contrast to those produced by stimulant drugs. Tramadol is also an NRI, similar to non-stimulant ADHD medication atomoxetine.

Pharmacology

Tapentadol is a full agonist at the mu (µ) opioid receptor (see Morphine for more details on opioid receptors) in the central and peripheral nervous systems.

Similar to tramadol, tapentadol also inhibits the recycling of neurotransmitter noradrenaline (NRI) which is thought to help alleviate neuropathic pain. However, tapentadol does not affect serotonin and is 2–3x more potent than tramadol at the µ-opioid receptor. Additionally, tapentadol doesn’t have any active metabolites making it more predictable.

Like tramadol, tapentadol can lower the threshold for seizures. Tramadol has also been shown to cause low blood pressure in some people.

Interactions

The combination of tapentadol with other depressants, such as alcohol and benzodiazepines, is associated with an increase in respiratory depression and overdose. Mixing tapentadol with antidepressants increases the risk of serotonin syndrome.

Harm Reduction

• Start low, go slow: Take a small amount and wait until you can feel the effects before taking more/anything else
• Try not to use alone: If something goes wrong, someone is there to get help
• Be careful mixing: Mixing tapentadol with other depressants or antidepressants increases overdose risk – avoid if you can, otherwise take less, as they can increase the effects and risks
• Carry naloxone: In case opioids are in the mix
• Test your stuff: Find out how to send a sample to WEDINOS for testing here: https://www.wedinos.wales or pick up some test strips at our Harm Reduction Hub
• If you’ve been prescribed tapentadol and you notice a tolerance starting to develop (you need to keep taking more to get the same effect) speak to your doctor – don’t just start increasing your dose yourself.
• Don’t suddenly stop taking them, or you may start to experience symptoms of withdrawal: these can range from a return of your original symptoms (possibly even worse than before) to totally new symptoms.
• If you have become physically dependent on tapentadol, the symptoms of abruptly stopping are likely to be even worse. It’s important to get proper medical advice on how to reduce your intake slowly.
• It’s also possible to become psychologically dependent on the drug (feeling like you need it all the time). If you think this is happening, see your doctor as soon as possible, but don’t suddenly stop taking it.

History

Tapentadol was first synthesised by chemist Helmut Buschmann and colleagues in the late 1980s at the German pharmaceutical company Grünenthal GmbH as a successor to tramadol with minimal serotonin activity. In 2010, the ACMD advised the UK government to control tapentadol as a Class A, Schedule II drug before it became available for clinical use. In May 2011, tapentadol was brought to the UK pharmaceutical market under the brand name Palexia for the treatment of severe chronic pain.

Between 2014 and 2022, as tramadol prescribing decreased, tapentadol prescriptions increased in England and Ireland by 179% and 389%, respectively. Additionally, some people seek tapentadol on the unregulated market either for recreational purposes or to self-medicate for unmet needs including pain. In recent years, tapentadol has been found as a contaminant in several samples from the UK’s unregulated drugs market including heroin, tramadol, modafinil, lorazepam, and morphine.

Law

• Class A
• Schedule 2

Possible offences

• Possession
  • Maximum sentence – 7 years imprisonment, a fine, or both
• Possession With Intent To Supply
  • Maximum sentence – life imprisonment, a fine, or both
• Supply (including being concerned in supply, conspiracy to supply, aggravated supply and offer to supply)
  • Maximum sentence – life imprisonment, a fine, or both
• Production
  • Maximum sentence – life imprisonment, a fine, or both

In practice maximum sentences are rarely used, for more detailed and accurate information go to our sentencing page.