
Oxycodone: Difference between revisions
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Revision as of 18:30, 28 March 2017
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.
Oxycodone | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Chemical Nomenclature | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Common names | OxyContin, Oxy, Roxicodone, Oxecta, OxyIR, Endone, Oxynor, Codilek, Oxydor, Redocam, Oxygesic, Percodan, Percocet | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Substitutive name | Oxycodone | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Systematic name | (5R,9R,13S,14S)-4,5α-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Class Membership | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Psychoactive class | Opioid | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Chemical class | Morphinan | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Routes of Administration | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Grapefruit |
Summary sheet: Oxycodone |
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[4][5] as one of several new semi-synthetic opioids in an attempt to improve on the existing opioids.[6]
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.
Chemistry
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.
Pharmacology
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,[7] while in nondiabetic mice, the μ1-opioid receptor seems to be primarily responsible for these effects.[8]
Subjective effects
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 PsychonautWiki contributors. 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
- 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.
- Constipation
- Cough suppression
- Decreased libido
- Difficulty urinating
- Itchiness
- Nausea
- Pupil constriction
- Stomach cramps
- Appetite suppression
- Orgasm suppression
- Increased perspiration
- Skin flushing
Cognitive effects
- 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.
- Anxiety suppression
- Compulsive redosing
- Dream potentiation
Visual effects
- Internal hallucinations - One may experience a state of semi-consciousness and hypnagogia during heavy dosage nodding which results in dream-like states and up to level 3 imagery and mild geometry.
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
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 [[Toxicity::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 [[Cross-tolerance::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.[9] 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.[10]
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 oxycodone, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of oxycodone, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of oxycodone 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 oxycodone.
Legal issues
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.[11] The 1961 Single Convention on Narcotic Drugs of the United Nations, which replaced the 1931 convention, categorized oxycodone in Schedule I.[12]
- Australia: Oxycodone is in Schedule I (derived from the Single Convention on Narcotic Drugs) of the Commonwealth's Narcotic Drugs Act 1967.[13] 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".[14]
- Canada: Oxycodone is a controlled substance under Schedule I of the Controlled Drugs and Substances Act (CDSA).[15]
- Germany: The drug is in Appendix III of the Narcotics Act (Betäubungsmittelgesetz or BtMG).[16] 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).[17]
- Hong Kong: Oxycodone is regulated under Part I of Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance.[18]
- 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.[19] 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.[20]
- UK: Oxycodone is a Class A drug under the Misuse of Drugs Act.[21]
- USA: Oxycodone is a Schedule II controlled substance.[22]
See also
External links
References
- ↑ Risks of Combining Depressants - TripSit
- ↑ https://pmc.ncbi.nlm.nih.gov/articles/PMC6602093/
- ↑ https://pmc.ncbi.nlm.nih.gov/articles/PMC4006196/#S9
- ↑ 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
- ↑ http://www.austlii.edu.au/au/legis/cth/consol_act/nda1967160/sch1.html
- ↑ http://www.comlaw.gov.au/ComLaw/Legislation/LegislativeInstrument1.nsf/0/3BBB39C4645284BCCA2574A6001C711F/$file/PoisonsStandard2008.pdf
- ↑ http://laws-lois.justice.gc.ca/eng/acts/c-38.8/fulltext.html
- ↑ http://www.gesetze-im-internet.de/btmg_1981/BJNR106810981.html
- ↑ http://www.gesetze-im-internet.de/btmg_1981/BJNR106810981.html
- ↑ http://www.hklii.hk/cgi-bin/sinodisp/eng/hk/legis/ord/134/sch1-19970630.html?stem=&synonyms=&query=oxycodone
- ↑ http://statutes.agc.gov.sg/aol/search/display/view.w3p;page=0;query=DocId%3Ac13adadb-7d1b-45f8-a3bb-92175f83f4f5%20Depth%3A0%20Status%3Ainforce;rec=0
- ↑ Misuse of Drugs Act (Singapore), section 5(1).
- ↑ https://www.gov.uk/government/uploads/system/uploads/attachment_data/file/277310/ControlledDrugsList4Feb2013.doc
- ↑ http://www.deadiversion.usdoj.gov/schedules/