|Summary sheet: Oxycodone|
|Common names||OxyContin, Oxy, Roxicodone, Oxecta, OxyIR, Endone, Oxynor, Codilek, Oxydor, Redocam, Oxygesic|
|Routes of Administration|
Oxycodone (trade names Roxicodone, OxyContin, Oxecta, OxyIR, Endone, Oxynorm, and OxyNEO) is a semi-synthetic opioid synthesized from poppy-derived thebaine. It is a narcotic analgesic within the morphinan chemical class and is generally indicated for relief of moderate to severe pain. It was developed in 1916 in Germany as one of several new semi-synthetic opioids in an attempt to improve on the existing opioids.
Oxycodone is available as single-ingredient medication in immediate release and controlled release. Combination products formulated with non-narcotic ingredients such as NSAIDs and Tylenol (acetaminophen) are also available.
Oxycodone, or dihydro hydroxy codeinone, is an opioid of the morphinan class. Oxycodone and other molecules of this class contain a polycyclic core of three benzene rings fused in a zig-zag pattern called a phenanthrene. A fourth nitrogen containing ring is fused to the phenanthrene at R9 and R13, with the nitrogen member looking at R17 of the combined structure. This structure is called morphinan.
Oxycodone, along with other morphinans, contains an ether bridge between two of its rings, connecting R4 and R5 through an oxygen group. It contains a carbonyl group bound at R6 and a methyl group located on the nitrogen atom at R17. The carbon-oxygen double bond of the carbonyl saturates the benzene ring it is bonded with. Thus oxycodone lacks the double bond on that ring found in codeine. Oxycodone also shares the 3-methoxy substitution found in codeine; however, it contains an additional hydroxy group at R14. Oxycodone is analogous to the other morphinans including dihydrocodeine, heroin, ethylmorphine, and codeine.
Oxycodone produces effects that are typical of μ-opioid agonists, suggesting a pharmacological similarity to more traditional opioids, such as codeine and morphine. These compounds 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.
In 2006, research by a Japanese group suggested the effect of oxycodone is mediated by different receptors in different situations. Specifically in diabetic mice, the κ-opioid receptor appears to be involved in the direct pain relief caused by oxycodone, while in nondiabetic mice, the μ1-opioid receptor seems to be primarily responsible for these effects.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These 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 of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- Pain relief
- Euphoria - In comparison to other opioids, this particular substance can be considered similar in its physical euphoria when compared with that of morphine or diacetylmorphine (heroin) and more intense when compared to kratom and hydrocodone. 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.
- Sedation - Oxycodone is considerably less sedating than codeine but more sedating than kratom.
- Cough suppression
- Decreased libido
- Difficulty urinating
- Pupil constriction
- Stomach cramps
- Appetite suppression
- Orgasm suppression
- Increased perspiration
- Skin flushing
- Euphoria - This seems to be caused by both µ-opioid receptor agonism and downstream dopamine reinforcement. In comparison to other opioids, this particular substance can be considered similar in its cognitive euphoria when compared with that of morphine or diacetylmorphine (heroin) and more intense when compared to kratom and hydrocodone. The sensation itself can be described as powerful and overwhelming feelings of emotional bliss, contentment, and happiness.
- Ego inflation
- Anxiety suppression
- Compulsive redosing
- Dream potentiation
Toxicity and harm potential
Oxycodone 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.
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 oxycodone 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 oxycodone 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). Oxycodone presents cross-tolerance with all other opioids, meaning that after the consumption of oxycodone all opioids will have a reduced effect.
The risk of fatal opioid overdoses rise sharply after a period of cessation and relapse, largely because of reduced tolerance. To account for this lack of tolerance, it is safer to only dose a fraction of one's usual dosage if relapsing. It has also been found that the environment one is in can play a role in opioid tolerance. In one scientific study, rats with the same history of heroin administration were significantly more likely to die after receiving their dose in an environment not associated with the drug in contrast to a familiar environment.
Although many psychoactive substances are safe to use on their own, they can quickly become dangerous or even life-threatening when combined with other substances. The following lists some known dangerous combinations, but may not include all of them. A combination that appears to be safe in low doses can still increase the risk of injury or death. Independent research should always be conducted to ensure that a combination of two or more substances is safe to consume. Some interactions listed have been sourced from Tripsit.
- Depressants (1,4-Butanediol, 2M2B, alcohol, benzodiazepines, barbiturates, GHB/GBL, methaqualone, opioids) - This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration. There is also an increased risk of suffocating on one's vomit while unconscious. If nausea or vomiting occurs before a loss of consciousness, users should attempt to fall asleep in the recovery position or have a friend move them into it.
- Stimulants - It can be dangerous to combine depressants with stimulants due to the risk of accidental excessive intoxication. Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states. This combination can also potentially result in severe dehydration if one's fluid intake is not closely monitored. If choosing to combine these substances, one should strictly limit themselves to a pre-set schedule of dosing only a certain amount per hour until a maximum threshold has been reached.
- Dissociatives - This combination can unpredictably potentiate the amnesia, sedation, motor control loss and delusions that can be caused by each other. It may also result in a sudden loss of consciousness accompanied by a dangerous degree of respiratory depression. If nausea or vomiting occurs before consciousness is lost, users should attempt to fall asleep in the recovery position or have a friend move them into it.
Oxycodone is subject to international conventions on narcotic drugs. In addition, oxycodone is subject to national laws that differ by country. The 1931 Convention for Limiting the Manufacture and Regulating the Distribution of Narcotic Drugs of the League of Nations included oxycodone. The 1961 Single Convention on Narcotic Drugs of the United Nations, which replaced the 1931 convention, categorized oxycodone in Schedule I.
- Australia: Oxycodone is in Schedule I (derived from the Single Convention on Narcotic Drugs) of the Commonwealth's Narcotic Drugs Act 1967. In addition, it is in Schedule 8 of the Australian Standard for the Uniform Scheduling of Drugs and Poisons ("Poisons Standard"), meaning it is a "controlled drug... which should be available for use but require[s] restriction of manufacture, supply, distribution, possession and use to reduce abuse, misuse and physical or psychological dependence".
- Austria: Oxycodone is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).
- Canada: Oxycodone is a controlled substance under Schedule I of the Controlled Drugs and Substances Act (CDSA).
- Germany: The drug is in Appendix III of the Narcotics Act (Betäubungsmittelgesetz or BtMG). The law allows only physicians, dentists, and veterinarians (Ärzte, Zahnärzte und Tierärzte) to prescribe oxycodone and the federal government to regulate the prescriptions (e.g., by requiring reporting).
- Hong Kong: Oxycodone is regulated under Part I of Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance.
- Singapore: Oxycodone is listed as a Class A drug in the Misuse of Drugs Act of Singapore, which means offences in relation to the drug attract the most severe level of punishment. A conviction for unauthorized manufacture of the drug attracts a minimum sentence of 10 years of imprisonment and corporal punishment of five strokes of the cane, and a maximum sentence of life imprisonment or 30 years of imprisonment and 15 strokes of the cane. The minimum and maximum penalties for unauthorized trafficking in the drug are respectively five years of imprisonment and five strokes of the cane, and 20 years of imprisonment and 15 strokes of the cane.
- UK: Oxycodone is a Class A drug under the Misuse of Drugs Act.
- USA: Oxycodone is a Schedule II controlled substance.
- Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
- German (DE) Patent 296916
- Sneader W (2005). Drug discovery: a history. Hoboken, NJ: Wiley. p. 119. ISBN 0-471-89980-1.
- Oxycodone (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/15907646
- Characterization of the antinociceptive effects of oxycodone in diabetic mice (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0014299906001282
- Involvement of μ1-opioid receptor on oxycodone-induced antinociception in diabetic mice (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0014299907000386
- Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2
- Siegel, S., Hinson, R., Krank, M., & McCully, J. (1982). Heroin “overdose” death: contribution of drug-associated environmental cues. Science, 216(4544), 436–437. https://doi.org/10.1126/science.7200260
- VI.8a Convention for limiting the Manufacture and regulating the Distribution of Narcotic Drugs. Geneva, 13 July 1931 | https://treaties.un.org/doc/Treaties/1931/07/19310713%2006-44%20AM/Ch_VI_8_ap.pdf
- "United Nations conference for the adoption of a single convention on narcotic drugs. Final act | https://treaties.un.org/doc/Treaties/1964/12/19641213%2002-14%20AM/Ch_VI_15p.pdf
- Misuse of Drugs Act (Singapore), section 5(1).