Tapentadol

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Death may occur when opiates are combined with other depressants such as benzodiazepines, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

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Summary sheet: Tapentadol
Tapentadol
Tapentadol.svg
Chemical Nomenclature
Common names Tapentadol, Nucynta, Palexia, Yantil, Yantil SR
Systematic name 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol
Class Membership
Psychoactive class Opioid
Chemical class Phenol
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold Common Heavy
12.5 - 25 - 50 - 75 - 150 mg
Light Strong
Threshold 12.5 - 25 mg
Light 25 - 50 mg
Common 50 - 75 mg
Strong 75 - 150 mg
Heavy 150 mg +
Duration
Onset 15 - 45 minutes
Peak 4 - 6 hours
After effects 1 - 6 hours









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Tapentadol often sold under the brand name Nucynta is a synthetic opioid 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

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You can help by adding to it.

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 C14H23NO and has a molar mass of 221.339 grams per mole.[2]

Pharmacology

Opioids exert their effects by binding to and activating the 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 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 serotonergic effects as well.[3]

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
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Cognitive effects
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Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Toxicity and harm potential

Tapentadol 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. Tapentadol is known to lower the seizure threshold. It should not be taken during benzodiazepine withdrawals as this can potentially cause seizures.

It is strongly recommended that one use harm reduction practices when using this drug.

Tolerance and addiction potential

As with other opioids, the chronic use of tapentadol 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.

Tolerance to many of the effects of tapentadol 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). Tapentadol presents cross-tolerance with all other opioids, meaning that after the consumption of tapentadol all opioids will have a reduced effect.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

  • Depressants (1,4-Butanediol, 2m2b, alcohol, barbiturates, benzodiazepines, GHB/GBL, methaqualone) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
  • Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
  • Stimulants - It is dangerous to combine tapentadol, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of tapentadol, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of tapentadol will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only taking a certain amount of tapentadol.
  • Psychedelics - Tapentadol is well known to lower seizure threshold and psychedelics also cause occasional seizures.

Serotonin syndrome risk

Combinations in the list below may increase the amount of neurotransmitters such as serotonin and dopamine to dangerous or even fatal levels.

Legal issues

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This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

  • United States - Tapentadol is a Schedule II Controlled Substance.[5]
  • United Kingdom - Tapentadol is a Class A, Schedule 2 drug in the United Kingdom.[6]

See also

External links

References