Sufentanil: Difference between revisions
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Revision as of 07:19, 14 November 2016
Fatal overdose 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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| Chemical Nomenclature | |||||||||||||||||||||||||||
| Common names | Sufentanil, Sufentanyl, Sufenta, Chronogesic, | ||||||||||||||||||||||||||
| Systematic name | N-[4-(Methoxymethyl)-1-(2-thiofuran-2-ylethyl)-4-piperidyl]-N-phenylpropanamide | ||||||||||||||||||||||||||
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| Psychoactive class | Opioid | ||||||||||||||||||||||||||
| Chemical class | Anilidopiperidine | ||||||||||||||||||||||||||
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| Summary sheet: Sufentanil |
Sufentanil, also known as sufentanyl and by the brand name Sufenta, is an extremely potent synthetic piperidine opioid analgesic. Sufentanil has a rapid onset and short mechanism and is used medically as an analgesic in surgical procedures or for the management of post-operative pain. Sufentanil is roughly 500 to 1,000 times more potent than pharmaceutical grade morphine and is approximately 10 times more potent than pharmaceutical grade fentanyl. The subjective effects of sufentanil are similar to those of heroin, with the exception that many users report a significantly less euphoric "high" associated with the drug and stronger respiratory depression, sedation and pain relief. Sufentanil is the most potent opioid analgesic currently used in human medicine.
Chemistry
Sufentanil is synthetic piperidine that is similar in structure to both fentanyl and acetylfentanyl. One of the key differences is that one of the phenyl groups in sufentanil has been replaced with a thiophene or thiofuran group. Thiophene groups can typically replace phenyl groups without a significant drop in potency. The empirical formula of sufentanil is C22H30N2O2S and has a molar mass of 386.552 grams per mole.
Pharmacology
The recreational effects of sufentanil occur 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. Like endorphins, sufentanil is an extremely potent μ-opioid agonist.
Sufentanil has an extremely short biological half life of only 162 minutes.
Subjective effects
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.
Physical effects
- Pain relief - In comparison to other opiates, sufentanil can be described as a strong analgesic, providing relief even at non-recreational doses.
- Physical euphoria - This particular substance can be considered as less intense in its physical euphoria when compared with that of morphine or fentanyl. The sensation itself can be described as strong feelings of physical comfort, warmth and bliss which spread throughout the body.
- Itchiness - This compound presents very little itch response due to little to no amounts of histamine being release, unlike other opioids.
- Respiratory depression - In comparison to other opiates, sufentanil displays this effect at lower doses relative to euphoria then other opiates, and even at low doses 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. In the hospital setting, patients that are administered sufentanil are constantly monitored to ensure their breathing is not significantly depressed.
- Sedation - Sufentanil can be described as much more sedating then other opioids. Even at moderate dosages, this compound can result in overwhelming feelings of sedation and tiredness that is considerably more sedating than that of heroin and oxycodone.
- Constipation
- Cough suppression
- Decreased libido
- Difficulty urinating
- Pupil constriction
- Increased perspiration
- Low blood pressure
- Appetite suppression
- Orgasm suppression
Cognitive effects
- Cognitive euphoria - This particular substance can be considered as significantly less intense in its cognitive euphoria when compared with that of morphine or fentanyl. It is still, however, capable of extreme intensity and overwhelming bliss at heavier dosages with a low tolerance. The sensation itself can be described as powerful and overwhelming feeling of emotional bliss, contentment, and happiness.
- Anxiety suppression
- Compulsive redosing
Toxicity and harm potential
Recreational use of sufentanil by individuals without opioid tolerance is extremely dangerous due to its potency. It is potentially fatal at heavy dosages and even those with opiate tolerances are at high risk for overdoses. Once the sufentanil is in the user's system, it is extremely difficult to stop its course because of the nature of absorption. Because of the extremely high strength of pure sufentanil powder, it is very difficult to dilute appropriately, and often the resulting mixture may be far too strong and, therefore, very dangerous. It is also [[Toxicity::potentially lethal when mixed with depressants like alcohol or benzodiazepines]].
Like most opioids, unadulterated sufentanil at appropriate dosages does not cause many long-term complications other than dependence and constipation. Outside of the extremely powerful addiction and physical dependence, the harmful or toxic aspects of opioid usage are exclusively associated with not taking the necessary precautions in regards to its administration, overdosing and using impure products.
It is important to consider that particular care must be taken with sufentanil due to its extreme potency and ability to be absorbed through the skin. This means that simply unintentionally spilling a very small amount of sufentanil on one's skin could result in a fatal overdose.
Heavy dosages of sufentanil can result in respiratory depression, leading onto fatal or dangerous levels of anoxia (oxygen deprivation). This occurs because the breathing reflex is suppressed by agonism of µ-opioid receptors proportional to the dosage consumed.
Sufentanil can also cause nausea and vomiting; a significant number of deaths attributed to opioid overdose are caused by aspiration of vomit by an unconscious victim. This is when an unconscious or semi-conscious user who is lying on their back vomits into their mouth and unknowingly suffocates. It can be prevented by ensuring that one is lying on their side with their head tilted downwards so that the airways cannot be blocked in the event of vomiting while unconscious (also known as the recovery position). In case of overdose, it is advised to administer a dose of naloxone intravenously or intramuscularly to reverse the effects of opioid agonism. It has been noted that naloxone is not very effective for the management of opioid overdoses in cases where extremely potent opioids like sufentanil have been used. In the case of sufentanil, naltrexone should be used in case of an overdose.
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 sufentanil can be considered extremely 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 sufentanil 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. It is unknown how long it takes for sufentanil tolerance to decrease to baseline (no distinguishable tolerance). Sufentanil presents cross-tolerance with [[Cross-tolerance::all other opioids]], meaning that after the consumption of sufentanil 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 fentanyl, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of fentanyl, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of fentanyl will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to taking a certain amount of fentanyl.
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 - Sufentanil is classified as a Schedule II Controlled Substance under the Controlled Substances Act.[2]