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en>FunkinSheep: nothing was changed, trying to see how to add an experience since theres only 1 on the Tapentadol page, apologies.

2025-06-09T14:45:51Z

nothing was changed, trying to see how to add an experience since theres only 1 on the Tapentadol page, apologies.

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{{headerpanel|{{DepressantOD|opiates}} }}
{{SummarySheet}}
{{Template:SubstanceBox/Tapentadol}}

'''Tapentadol''' often sold under the brand name '''Nucynta''' is a synthetic [[opioid]] [[pain relief |analgesic]] similar in structure to [[tramadol]]. Tapentadol has a duel mechanism of action, working on both the μ-opioid [[receptor]] and also acting as a [[norepinephrine]] [[reuptake inhibitor]]. Tapentadol is used in the management of moderate to severe pain. The subjective effects of tapentadol are similar to those of [[tramadol]]. Many users report extreme pain when trying to insufflate tapentadol.

==Chemistry==
Tapentadol (3-((1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl) phenol hydrochloride) is a non-racemic molecule. The molecular formula of Tapentadol is C14H23NO.HCl. It was first synthesized in USA and marketed by Ortho-McNeil-Janssen Pharmaceuticals; its trade name was Nucynta.<ref>h{{cite journal | vauthors=((Singh, D. R.)), ((Nag, K.)), ((Shetti, A. N.)), ((Krishnaveni, N.)) | journal=Saudi Journal of Anaesthesia | title=Tapentadol hydrochloride: A novel analgesic | volume=7 | issue=3 | pages=322–326 | date= 2013 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3757808/ | issn=1658-354X | doi=10.4103/1658-354X.115319}}</ref>

Tapentadol is similar in structure to both [[tramadol]] and [[dextropropoxyphene]]. Tapentadol has one cyclic ring, unlike tramadol which has two. The empirical formula of tapentadol is C<sub>14</sub>H<sub>23</sub>NO and has a molar mass of 221.339 grams per mole.<ref>{{Citation | vauthors=PubChem | title=Tapentadol | url=https://pubchem.ncbi.nlm.nih.gov/compound/9838022#section=Chemical-and-Physical-Properties}}</ref> Tapentadol has thefull IUPAC name: 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol.

==Pharmacology==
[[Opioid]]s exert their effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]]. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their [[physical euphoria|euphoria]], [[pain relief]] and [[anxiolytic]] effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement. Tapentadol has an oral bioavailability of about 32%. Tapentadol is metabolized by the Cytochrome P450 system in the liver and is excreted by the kidneys in urine as well as in feces. Unlike most opioids, tapentadol is also a [[norepinephrine]] [[reuptake inhibitor]] and also has weak [[serotonin |serotonergic]] effects as well.<ref>{{cite journal | vauthors=((Fidman, B.)), ((Nogid, A.)) | journal=Pharmacy and Therapeutics | title=Role of Tapentadol Immediate Release (Nucynta) in the Management Of Moderate-to-Severe Pain | volume=35 | issue=6 | pages=330–357 | date= June 2010 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2888545/ | issn=1052-1372}}</ref>

Tapentadol is an orally available, synthetic benzenoid that acts as an agonist for the mu-opioid receptor (MOR) and inhibits the reuptake of noradrenaline, with potential anti-nociceptive activity. Upon oral administration, tapentadol binds to the MOR which enhances MOR-mediated signaling, interferes with the sensation of pain and results in an analgesic effect. Tapentadol also inhibits the reuptake of noradrenaline, which increases the levels of noradrenaline (NA), activates the inhibitory alpha-2 receptors and results in an analgesic effect.<ref>{{Citation | vauthors=PubChem | title=Tapentadol | url=https://pubchem.ncbi.nlm.nih.gov/compound/9838022}}</ref>

Tapentadol and its metabolites are excreted almost exclusively (99%) via the kidneys. Approximately 70% (55% O-glucuronide and 15% sulfate of tapentadol) is excreted in conjugated form. A total of 3% of drug was excreted in urine as unchanged drug.<ref>{{Citation | title=Tapentadol | url=https://go.drugbank.com/drugs/DB06204}}</ref>

==Subjective effects==
{{Preamble/SubjectiveEffects}}

{{effects/base
|{{effects/physical|
The general sensation of tapentadol can be described as one of euphoria, relaxation, anxiety suppression and pain relief.
*'''[[Effect::Pain relief]]'''
*'''[[Effect::Physical euphoria]]''' - This particular substance can be considered as less intense in its physical euphoria when compared with that of [[morphine]] or [[diacetylmorphine]] (heroin). The sensation itself can be described as extreme feelings of intense physical comfort, warmth, love and bliss.
*'''[[Effect::Itchiness]]'''
*'''[[Effect::Respiratory depression]]''' - At low to moderate doses, this effect results in the sensation that the breath is slowed down mildly to moderately, but does not cause noticeable impairment. At high doses and overdoses, opioid-induced respiratory depression can result in a shortness of breath, abnormal breathing patterns, semi-consciousness, or unconsciousness. Severe overdoses can result in a coma or death without immediate medical attention.
*'''[[Effect::Constipation]]'''
*'''[[Effect::Cough suppression]]'''
*'''[[Effect::Difficulty urinating]]'''
*'''[[Effect::Nausea]]'''
*'''[[Effect::Sedation]]'''
*'''[[Effect::Double vision]]'''
*'''[[Effect::Pupil constriction]]'''
*'''[[Effect::Decreased libido]]'''
*'''[[Effect::Appetite suppression]]'''
*'''[[Effect::Dizziness]]''' - Tapentadol causes dizziness at a higher rate than other opioids
*'''[[Effect::Orgasm suppression]]'''
*'''[[Effect::Dry mouth]]'''
}}

|{{effects/cognitive|

The cognitive effects of Tapentadol can be broken down into several components which progressively intensify proportional to dosage.

The most prominent of these cognitive effects generally include:

*'''[[Effect::Anxiety suppression]]'''
*'''[[Effect::Cognitive euphoria]]''' - In comparison to other [[opioids]], Tapentadol can be considered as less intense in its cognitive euphoria when compared with that of [[morphine]] or [[diacetylmorphine|heroin]].
*'''[[Effect::Dream potentiation]]'''
*'''[[Effect::Increased music appreciation]]'''
*'''[[Effect::Focus enhancement]]''' - Focus enhancement occurs at lower doses and disappears as the dose is increased and the sedative and euphoric effects take over.
*'''[[Effect::Motivation enhancement]]'''
*'''[[Effect::Sleepiness]]''' - In high dosages this can get to the point where the user may be drifting in and out of consciousness or even experience what is called "nodding".
*'''[[Effect::Thought acceleration]]'''
*'''[[Effect::Irritability]]'''

}}
{{effects/visual|

The visual effects of Tapentadol are much more pronounced compared to other [[opioids]] of its class. They can be broken down into several components which progressively intensify proportional to dosage.

====Suppressions====
*'''[[Effect::Double vision]]'''
*'''[[Effect::Visual acuity suppression]]'''
====Hallucinatory states====
*'''[[Effect::Internal hallucination]]''' - The internal hallucinations of Tapentadol can be described as much more solid than psychedelics and do not seem to be composed of visual geometry. They typically manifest themselves through hypnagogic scenarios. They are noticeable at most doses and can cause difficulty sleeping. They can be described [[Visual_effects:_Internal_hallucinations#Variations|variations]] as lucid in believability, fixed in style, autonomous in controllability, and equal in new experiences and memory replays in content.

}}
}}
===Experience reports===
Anecdotal reports which describe the effects of this compound within our [[experience index]] include:
{{#ask: [[Category:Tapentadol]][[Category:Experience]]|format=ul|Columns=1}}
Additional experience reports can be found here:

*[https://www.erowid.org/experiences/subs/exp_Tapentadol.shtml Erowid Experience Vaults: Tapentadol]

==Toxicity and harm potential==
Tapentadol has a [[Toxicity::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 [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[benzodiazepines]]]] and generally has a wider range of substances which it is [[tapentadol#Dangerous interactions|dangerous to combine with]] in comparison to other opioids. Tapentadol is known to lower the seizure threshold. It should not be taken during [[Benzodiazepine#Discontinuation|benzodiazepine withdrawals]] as this can potentially cause [[seizure]]s.

It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug.
===Tolerance and addiction potential===
As with other [[opioids]], the chronic use of tapentadol can be considered [[Addiction potential::moderately addictive with a high potential for abuse]] and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and [[Opioids#Discontinuation|withdrawal symptoms]] may occur if a person suddenly stops their usage.

Tolerance to many of the effects of tapentadol [[Time to full tolerance::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 [[Time to half tolerance::3 - 7 days]] for the tolerance to be reduced to half and [[Time to zero tolerance::1 - 2 weeks]] to be back at baseline (in the absence of further consumption). Tapentadol presents cross-tolerance with [[Cross-tolerance::all other [[opioids]]]], meaning that after the consumption of tapentadol all [[opioid]]s will have a reduced effect.

===Dangerous interactions===
{{DangerousInteractions/Intro}}
{{DangerousInteractions/Opioids}}

====[[Serotonin syndrome]] risk====
{{DangerousInteractions/SerotoninSyndrome}}

==Legal status==
{{LegalStub}}

*'''Australia''': Tapentadol is a Schedule 8 substance, the highest schedule behind illegal substances. It can only be accessed through a request & prescription.

*'''Germany:''' Tapentadol is a controlled substance under Anlage III of the BtMG. It can only be prescribed on a narcotic prescription form.<ref>{{Citation | title=Anlage III BtMG - Einzelnorm | url=https://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html}}</ref>
*'''Switzerland''': Tapentadol is a controlled substance specifically named under Verzeichnis A. Medicinal use is permitted.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref>
*'''United Kingdom:''' Tapentadol is a Class A, Schedule 2 drug in the United Kingdom.<ref>{{Citation | title=List of most commonly encountered drugs currently controlled under the misuse of drugs legislation | url=https://www.gov.uk/government/publications/controlled-drugs-list--2/list-of-most-commonly-encountered-drugs-currently-controlled-under-the-misuse-of-drugs-legislation}}</ref>
*'''United States:''' Tapentadol is a Schedule II Controlled Substance.<ref>DEA Controlled Substances | https://www.deadiversion.usdoj.gov/schedules/orangebook/e_cs_sched.pdf</ref>

==See also==

*[[Responsible use]]
*[[Opioid]]
*[[Tramadol]]
*[[Fentanyl]]
*[[O-Desmethyltramadol]]

==External links==

*[https://en.wikipedia.org/wiki/Tapentadol Tapentadol (Wikipedia)]
*[https://isomerdesign.com/PiHKAL/explore.php?id=10530 Tapentadol (Isomer Design)]
*[https://go.drugbank.com/drugs/DB06204 Tapentadol (DrugBank)]
*[https://www.drugs.com/tapentadol.html Tapentadol (Drugs.com)]
*[https://drugs-forum.com/wiki/Tapentadol Tapentadol (Drugs-Forum)]

==References==
<references />

[[Category:Phenylpropylamine]]
[[Category:Opioid]]

{{#set:Featured=true}}

Tapentadol - Revision history

Sysop: 1 revision imported

en>FunkinSheep: nothing was changed, trying to see how to add an experience since theres only 1 on the Tapentadol page, apologies.