Description
Tramadol is an atypical opioid drug with SNRI activity used for the treatment of moderate to severe acute and chronic pain. It is also sometimes prescribed for neuropathic pain.
Desirable Effects
- Pain relief
- Sedative
- Euphoria
- Reduced anxiety
Undesirable Effects
- Constipation
- Feeling/being sick
- Respiratory depression in combination with other depressants
- Seizures and serotonin syndrome
What does it look like?
Tablets: Tramadol is most commonly found as white tablets or capsules (50 mg), slow-release tablets (50–400 mg), or slow-release capsules (50–200 mg). Tramadol is sometimes prescribed as a combination tablet with paracetamol (usually 325 mg paracetamol / 37.5 mg tramadol).
Oral solutions: Sometimes it is provided as a liquid solution (100 mg/mL), or tablets that dissolve in water or in your mouth (50 mg).
Method of Use
Orally: swallowed as a tablet/capsule, mixed into water and drunk as a liquid solution or soluble tablet, placed on tongue and sucked as an orodispersible tablet
Pharmacology
Tramadol is a weak agonist at the mu (µ) opioid receptor (see Morphine for more details on opioid receptors) in the central and peripheral nervous systems. However, its active metabolite desmetramadol (DSMT) is considered to be responsible for tramadol’s opioid effects, which binds to the µ-opioid receptor ~200x more strongly. So, tramadol may be considered a prodrug similar to codeine.
It also inhibits the recycling of neurotransmitters serotonin and noradrenaline (SNRI), similar to some antidepressants like venlafaxine and duloxetine. This is thought to make tramadol particularly effective in the treatment of neuropathic pain (pain caused by damage to nerves) compared with other opioids. However, its serotonin activity can increase the risk of serotonin syndrome at high doses or in combination with other drugs.
Tramadol is known to lower the seizure threshold, which may be mediated by its activation of the delta-opioid receptor (DOR), or inhibition at the serotonin-2C (5-HT2C) or GABA-A receptor.
Interactions
The combination of tramadol with other depressants, such as alcohol and benzodiazepines, is associated with an increase in respiratory depression and overdose. Mixing tramadol with antidepressants or stimulants increases the risk of serotonin syndrome.
History
Tramadol was first synthesised in 1962 by scientists at the West German pharmaceutical company Grünenthal GmbH, and launched under the brand name Tramal in 1977. It was marketed as a “safer” painkiller than opioids like morphine. Tramadol was approved in the mid-1990s for use in the UK and the US.
During the early 2000s, tramadol’s popularity grew globally, and tramadol became one of the most widely prescribed opioids for moderate-to-severe pain in the UK. Following a rise in tramadol-related deaths, the Home Office classified tramadol as a Class C, Schedule 3 controlled drug in June 2014.
Non-prescribed sales of tramadol have increased to meet demands from people using the drug for a variety of reasons. These include use to induce the expected clinical effects, taking higher doses to achieve a ‘high’ or by those already with a dependency, combined use with other depressant drugs. Over the last few years in the UK, tapentadol, pregabalin, and oxycodone have been missold as tramadol on the unregulated market.
Law
Possible offences
- Possession
- Maximum sentence – 2 years/fine/both
- Possession With Intent To Supply
- Maximum sentence – 14 years/fine/both
- Supply (including being concerned in supply, conspiracy to supply, aggravated supply and offer to supply)
- Maximum sentence – 14 years/fine/both
- Production
- Maximum sentence – 14 years/fine/both
In practice maximum sentences are rarely used, for more detailed and accurate information go to our sentencing page.
