Tramadol
Also called Tramal, Tadol, Tramacur, Tramundin
Dosage
Oral bands as drawn from PsychonautWiki's ranges below. The table is the source of truth.
When sources disagree, both rows are shown as published. Nothing is averaged or merged.
Oral
| Source | Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|---|
| PsychonautWiki | 25 mg PW | 25–100 mg PW | 100–250 mg PW | 250–300 mg PW | 300 mg+ PW |
| TripSit | – | 50–100 mg TS | 100–250 mg TS | – | 250–400 mg TS |
Bioavailability: 70–90%[15] PW
NOTE: Tramadol has a ceiling dose, where recreational effects are not increased. Risk of seizure at doses over 300mg. Tramadol decreases the seizure threshold, use extreme caution. Dosing insufflated is ineffective. TS
TripSit dose text
TripSit's factsheet also states its doses as text.
Oral Light: 50-100mg Common: 100-250mg Heavy: 250-400mg | NOTE: Tramadol has a ceiling dose, where recreational effects are not increased. Risk of seizure at doses over 300mg. Tramadol decreases the seizure threshold, use extreme caution. Dosing insufflated is ineffective. TS
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Duration
Oral, drawn at the midpoint of each PsychonautWiki range.
| Route · source | Onset | Come-up | Peak | Offset | Total | After-effects |
|---|---|---|---|---|---|---|
| Oral · PsychonautWiki | 15–60 minutes PW | 30–60 minutes PW | 2–6 hours PW | 2–4 hours PW | 6–10 hours PW | – |
TripSit factsheet
Mixing
Acute combinations: what happens when these are taken close together. Entries backed by a medical journal or agency are listed first.
Backed by medical journals
PsychonautWiki also lists dangerous combinations shared across a whole group (phenylpropylamine opioids) in a table this page does not copy. Read that list on PsychonautWiki.
TripSit combination chart
TripSit rates each pairing. Only pairings with a number carry a citation from TripSit. See the whole chart, with TripSit's note for every pairing.
Dangerous
Risks and toxicity
Tramadol has a low toxicity relative to dose. As with all opioids, long-term effects can vary but can include diminished libido, apathy and memory loss. It is also potentially lethal when mixed with depressants like alcohol or benzodiazepines and generally has a wider range of substances which it is dangerous to combine with in comparison to other opioids. It should not be taken during benzodiazepine withdrawals as this can potentially cause seizures. PW
It is strongly recommended that one use harm reduction practices when using this drug. PW
Dependence and abuse potential
As with other opioids, the chronic use of tramadol can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal symptoms may occur if a person suddenly stops their usage. PW
Tolerance to many of the effects of tramadol develops with prolonged and repeated use. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Tramadol presents cross-tolerance with all other opioids, meaning that after the consumption of tramadol all opioids will have a reduced effect. PW
Serotonin syndrome risk
Combinations with the following substances can lead to dangerously high serotonin levels. Serotonin syndrome requires immediate medical attention and can be fatal if left untreated. PW
- MAOIs such as syrian rue, banisteriopsis caapi, phenelzine, selegiline, and moclobemide[23] PW
- Serotonin releasers such as MDMA, 4-FA, methamphetamine, methylone and aMT PW
- 2C-T-x PW
- DXM PW
TripSit factsheet
Testing
Effects
euphoriaelevated moodoverall feeling of contentednessitchingdrowsinessvomitingurinary retentionnauseaconstipationrisk of seizure above 300mg TS
Overview
Tramadol (also known as Ultram, Ralivia or Tramal) is a synthetic opioid substance of the phenylpropylamine class that is structurally related to codeine and morphine. It acts as a weak μ-opioid receptor agonist and a reuptake inhibitor of norepinephrine and serotonin.[1]
A synthetic opioid analgesic, tramadol is used to treat moderate pain and can be considered a medium-strength opioid. Tramadol also has the unusual effect of being a serotonin releasing agent and a serotonin reuptake inhibitor, and as a consequence should not be taken in excess due to the risk of serotonin syndrome. Risk of seizures above 300mg doses.[3]
Tramadol, sold under the brand name Tramal among others, is an opioid pain medication and a serotonin–norepinephrine reuptake inhibitor (SNRI) used to treat moderate to severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an hour. It is also available by injection. It is available in combination with paracetamol (acetaminophen).[6–9] WP
As is typical of opioids, common side effects include constipation, itchiness, and nausea. Serious side effects may include hallucinations, seizures, increased risk of serotonin syndrome, decreased alertness, and drug addiction. A change in dosage may be recommended in those with kidney or liver problems. It is not recommended in those who are at risk of suicide or in those who are pregnant. While not recommended in women who are breastfeeding, those who take a single dose should not generally have to stop breastfeeding. Tramadol is converted in the liver to O-desmethyltramadol (desmetramadol), an opioid with a stronger affinity for the μ-opioid receptor.[8–11] WP
Tramadol was patented in 1972 and launched under the brand name Tramal in 1977 by the West German pharmaceutical company Grünenthal GmbH. In the mid-1990s, it was approved in the United Kingdom and the United States. It is available as a generic medication and marketed under many brand names worldwide. In 2023, it was the 36th most commonly prescribed medication in the United States, with more than 16 million prescriptions.[6]
History
Patent history
The U.S. Food and Drug Administration (FDA) approved tramadol in March 1995, and an extended-release (ER) formulation in September 2005. ER Tramadol was protected by US patents nos. 6,254,887 and 7,074,430. The FDA listed the patents' expiration as 10 May 2014. However, in August 2009, the US District Court for the District of Delaware ruled the patents invalid, a decision upheld the following year by the Court of Appeals for the Federal Circuit. Manufacture and distribution of generic equivalents of Ultram ER in the United States was therefore permitted before the expiration of the patents.[24–28] WP
Legal status
- Austria: Tramadol is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich). PW⚠ PsychonautWiki itself has flagged this text: citation needed.
- Malaysia: Tramadol is not listed as a First Schedule drug in the Dangerous Drugs Act 1952 of Malaysia.[29] PW
- Germany: Tramadol is a prescription medicine, according to Anlage 1 AMVV.[30] PW
- South Africa: Tramadol is legal for prescribed medical use only and is considered a Schedule 5 controlled substance. Sale and possession is decriminalized and considered misdemeanor.[31] PW
- Sweden: As of May 2008, Sweden has chosen to classify tramadol as a controlled substance in the same way as codeine and dextropropoxyphene. This means that the substance is a scheduled drug. But unlike codeine and dextropropoxyphene, a normal prescription can be used at this time.[32] PW
- Switzerland: Tramadol is listed as a "Abgabekategorie A" pharmaceutical, which requires a prescription. PW⚠ PsychonautWiki itself has flagged this text: citation needed.
- Turkey: Tramadol is a 'green prescription' only substance and illegal when sold or possessed without a prescription.[33] PW⚠ PsychonautWiki itself has flagged this text: citation needed.
- United Kingdom: On June 10th, 2014, tramadol was made a Class C drug under the Misuse of Drugs Act.[34] PW
- United States: Tramadol is a Schedule IV controlled substance in the United States.[35] PW
Formulations
Available dosage forms include liquids, syrups, drops, elixirs, effervescent tablets, and powders for mixing with water, capsules, tablets including extended-release formulations, suppositories, compounding powder, and injections.[36] WP
Brand names
- Tilodol - UK WP
Legal status
Effective August 2014, tramadol has been placed into Schedule IV of the federal Controlled Substances Act in the United States. Before that, some US states had already classified tramadol as a Schedule IV controlled substance under their respective state laws.[37–41] WP
Tramadol is classified in Schedule 4 (prescription only) in Australia, rather than as a Schedule 8 Controlled Drug (possession without authority illegal) like most other opioids.[36] WP
Effective May 2008, Sweden classified tramadol as a controlled substance in the same category as codeine and dextropropoxyphene, but allows a normal prescription to be used. In June 2014, the United Kingdom's Home Office classified tramadol as a Class C, Schedule 3 controlled drug, but exempted it from the safe custody requirement. In October 2023, New Zealand's Medsafe reclassified tramadol as a Class C2 Controlled Drug (in addition to its existing status as a prescription only medication). Effective 22 August 2025, the government of Liberia increased regulations on tramadol. Its use was "strictly limited to licensed hospital settings under the direct supervision of professional medical staff" according to the Liberian Observer. Liberian health authorities claimed that tramadol was the "most widely abused drug" in the country.[42–45] WP
In sport
The WADA has prohibited the use of tramadol in competition since 1 January 2024.[46] WP
Misuse of painkillers is up to four times more common among athletes compared to the general population.
From March 2019, the Union Cycliste Internationale (UCI) banned the drug, after riders were using the painkiller to improve their performance.
No significant improvements in performance were found when compared to placebo.[47]
In 2026 the International Go Federation (IGF) revoked Korean player Sa Woo Kim’s third place in the 2025 World Amateur Go Championship in Vancouver, Canada because he had tested positive for tramadol. The IGF adopted the World Anti-Doping Code in October 2020.[50–53] WP
In war
Illicit use of the drug is thought to be a major factor in the success of the Boko Haram terrorist organization. When used at higher doses, the drug "can produce similar effects to heroin." One former member said, "whenever we took tramadol, nothing mattered to us anymore except what we were sent to do because it made us very high and very bold, it was impossible to go on a mission without taking it." Tramadol is also used as a coping mechanism in the Gaza Strip. In the 2020's Anti-balaka militias in the Central African Republic were reported to be in control of the Tramadol trade, providing it to fighters, workers in illegal goldmines and organising the sale on local markets. Researchers report the drug is brought by Dubai based company Shalina from India and China to the Democratic Republic of the Congo, from where it is smuggled into the Central African Republic.[54–58] WP
Pharmacology
Mechanism of action
Tramadol induces analgesic effects through a variety of different targets on the noradrenergic system, serotonergic system, and opioid receptors system. Tramadol affects serotonin and norepinephrine reuptake inhibition similarly to certain antidepressants known as serotonin–norepinephrine reuptake inhibitors (SNRIs), such as venlafaxine and duloxetine. Tramadol exists as a racemic mixture, the positive enantiomer inhibits serotonin reuptake while the negative enantiomer inhibits noradrenaline re-uptake, by binding to and blocking the transporters. Both enantiomers of tramadol are agonists of the μ-opioid receptor and its M1 metabolite, O-desmetramadol, is also a μ-opioid receptor agonist but is 6 times more potent than tramadol itself. All of these actions may work synergistically to induce analgesia.[83–87] WP⚠ A table follows this text in the source and is not copied here. Open the source to see it.
Tramadol has been found to possess these actions:[66]
- Agonist of the μ-opioid receptor (MOR) and to a far lesser extent of the δ-opioid receptor (DOR) and κ-opioid receptor (KOR)[66]
[67] [85] WP - Serotonin reuptake inhibitor (SRI) and norepinephrine reuptake inhibitor; hence, an SNRI[66]
[67] [85] WP - Serotonin 5-HT2C receptor antagonist[66]
[67] [85] WP - M₁ and M₃ muscarinic acetylcholine receptor antagonist[66]
[67] [85] WP - α7 nicotinic acetylcholine receptor antagonist[66]
[67] [85] WP - NMDA receptor antagonist (very weak)[66]
[67] [85] WP - TRPA1 inhibitor[66]
[67] [85] WP
Tramadol acts on the opioid receptors through its major active metabolite desmetramadol, which has as much as 700-fold higher affinity for the MOR relative to tramadol. Moreover, tramadol itself has been found to possess no efficacy in activating the MOR in functional activity assays, whereas desmetramadol activates the receptor with high intrinsic activity (Eₘₐₓ equal to that of morphine). As such, desmetramadol is exclusively responsible for the opioid effects of tramadol. Both tramadol and desmetramadol have pronounced selectivity for the MOR over the DOR and KOR in terms of binding affinity.[11]
Tramadol is well-established as an SRI. In addition, a few studies have found that it also acts as a serotonin releasing agent (1–10 μM), similar in effect to fenfluramine. The serotonin releasing effects of tramadol could be blocked by sufficiently high concentrations of the serotonin reuptake inhibitor 6-nitroquipazine, which is in accordance with other serotonin releasing agents such as fenfluramine and MDMA. However, two more recent studies failed to find a releasing effect of tramadol at respective concentrations up to 10 and 30 μM. In addition to serotonergic activity, tramadol is also a norepinephrine reuptake inhibitor. It is not a norepinephrine releasing agent. Tramadol does not inhibit the reuptake or induce the release of dopamine.[1]
A positron emission tomography imaging study found that single oral 50-mg and 100-mg doses of tramadol to human volunteers resulted in 34.7% and 50.2% respective mean occupation of the serotonin transporter (SERT) in the thalamus. The estimated median effective dose (ED₅₀) for SERT occupancy hence was 98.1 mg, which was associated with a plasma tramadol level of about 330 ng/mL (1,300 nM). The estimated maximum daily dosage of tramadol of 400 mg (100 mg q.i.d. (four times per day)) would result in as much as 78.7% occupancy of the SERT (in association with a plasma concentration of 1,220 ng/mL or 4,632 nM). This is close to that of SSRIs, which occupy the SERT by 80% or more.[97] WP
Peak plasma concentrations during treatment with clinical dosages of tramadol have generally been found to be in the range of 70 to 592 ng/mL (266–2,250 nM) for tramadol and 55 to 143 ng/mL (221–573 nM) for desmetramadol. The highest levels of tramadol were observed with the maximum oral daily dosage of 400 mg per day divided into one 100-mg dose every 6 hours (i.e., four 100-mg doses evenly spaced out per day). Some accumulation of tramadol occurs with chronic administration; peak plasma levels with the maximum oral daily dosage (100 mg q.i.d. (four times per day)) are about 16% higher and the area-under-the-curve levels 36% higher than following a single oral 100-mg dose. Positron emission tomography imaging studies have reportedly found that tramadol levels are at least four-fold higher in the brain than in plasma. Conversely, brain levels of desmetramadol "only slowly approach those in plasma". The plasma protein binding of tramadol is only 4–20%; hence, almost all tramadol in circulation is free, thus bioactive.[94]
Pharmacokinetics
Tramadol is metabolised in the liver via the cytochrome P450 isozyme CYP2B6, CYP2D6, and CYP3A4, being O- and N-demethylated to five different metabolites. Of these, desmetramadol (O-desmethyltramadol) is the most significant, since it has 200 times the μ-affinity of (+)-tramadol, and furthermore has an elimination half-life of 9 hours, compared with 6 hours for tramadol itself. As with codeine, in the 6% of the population who have reduced CYP2D6 activity (hence reducing metabolism), a reduced analgesic effect is seen. Those with decreased CYP2D6 activity require a dose increase of 30% to achieve the same degree of pain relief as those with a normal level of CYP2D6 activity.[104]
Phase II hepatic metabolism renders the metabolites water-soluble, which are excreted by the kidneys. Thus, reduced doses may be used in renal and hepatic impairment.[98] WP
Its volume of distribution is around 306 L after oral administration and 203 L after parenteral administration.[98] WP
Detection in biological fluids
Tramadol and desmetramadol may be quantified in blood, plasma, serum, or saliva to monitor for abuse, confirm a diagnosis of poisoning or assist in the forensic investigation of a sudden death. Most commercial opiate immunoassay screening tests do not cross-react significantly with tramadol or its major metabolites, so chromatographic techniques must be used to detect and quantify these substances. The concentration of desmetramadol in the blood or plasma of a person who has taken tramadol is generally 10–20% that of the parent drug.[106]
Receptor binding · Wikipedia
Tramadol (and metabolite)
| Site | Tramadol | DSMT (Desmetramadol) | Species |
|---|---|---|---|
| MOR (μ-Opioid receptor) | 1,600–12,486; 2,120–8,300; ≥1,000 (EC₅₀) | 5.4–18.6; 17 ((+) ((+)-desmetramadol)); ≥240 (EC₅₀) | Human; Rat; Human[11] |
| DOR (δ-Opioid receptor) | >10,000; 57,600–100,000 | ≥2,900; 690 (+) ((+)-desmetramadol)) | Human; Rat[59] |
| KOR (κ-Opioid receptor) | >10,000; 42,700–81,000 | ≥450; 1,800 (+) ((+)-desmetramadol)) | Human; Rat[59] |
| SERT (Serotonin transporter) | ~900 (IC₅₀); 992–1,190 | >20,000 (IC₅₀); 2,980 ((−) ((−)-desmetramadol)) (IC₅₀) | Human; Rat[11] |
| NET (Norepinephrine transporter) | 14,600; 785 | 1,080 (−) ((−)-tramadol) (IC₅₀); 860 (IC₅₀) | Human; Rat[11] |
| DAT (Dopamine transporter) | >100,000 | >20,000 | Rat[65–68] |
| 5-HT1A | >20,000 | >20,000 | Rat[65–68] WP |
| 5-HT2A | >20,000 | >20,000 | Rat[65–68] WP |
| 5-HT2C | 1,000 (IC₅₀) | 1,300 (IC₅₀) | Rat[65] |
| 5-HT₃ | >20,000 | >20,000 | Rat[65–68] WP |
| NK₁ | IA (Inactive) | ? | Rat[65] |
| M₁ | >20,000; 3,400 (IC₅₀) | >20,000; 2,000 (IC₅₀) | Rat; Multiple[65–68] |
| M₂ | ND (No data) | ND (No data) | ND (No data)[65] |
| M₃ | 1,000 (IC₅₀) | IA (Inactive) | Human[65] |
| M₄ | ND (No data) | ND (No data) | ND (No data)[65] |
| M₅ | ND (No data) | ND (No data) | ND (No data)[65] |
| α7 | 7,400 | ND (No data) | Chicken[65] |
| σ₁ | >10,000 | ND (No data) | Rat[65] |
| σ₂ | >10,000 | ND (No data) | Rat[65] |
| NMDAR (N-Methyl-D-aspartate receptor) | 16,400 (IC₅₀) | 16,500 (IC₅₀) | Human[65] |
| NMDAR (N-Methyl-D-aspartate receptor) (MK-801) | >20,000 | >20,000 | Rat[65–68] WP |
| GABAA (GABAA receptor) | >100,000 (IC₅₀) | >100,000 (IC₅₀) | Human[65] |
| GlyR (Glycine receptor) | >100,000 (IC₅₀) | >100,000 (IC₅₀) | Human[65] |
| TRPA1 (Transient receptor potential channel ankyrin 1) | 100–10,000 (SI (significant inhibition)) | 1,000–10,000 (SI (significant inhibition)) | Human[65] |
| TRPV1 (Transient receptor potential channel vanilloid 1) | >10,000 (IC₅₀) | >10,000 (IC₅₀) | Human[65] |
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References
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