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Tapentadol
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Revision as of 05:13, 11 February 2018 by >David Hedlund(sort)
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
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 opioidanalgesic similar in structure to tramadol. Tapentadol has a duel mechanism of action, working on both the μ-opioid receptor and also acting as a norepinephrinereuptake 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.
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-opioidreceptor. 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.
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWikicontributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects
The general sensation of tapentadol can be described as one of euphoria, relaxation, anxiety suppression and pain relief.
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.
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.
Cognitive euphoria - This particular substance can be considered as less intense in its cognitive euphoria when compared with that of morphine or diacetylmorphine (heroin). The sensation itself can be described as powerful and overwhelming feelings of emotional bliss, contentment, and happiness.
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
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 [[Toxicity::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.
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 [[Cross-tolerance::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.
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.
Combinations with the following substances can cause dangerously high serotonin levels. Serotonin syndrome requires immediate medical attention and can be fatal if left untreated.
. eISSN 1471-6771. ISSN 0007-0912. OCLC 01537271. PMID 16051647.