Oxycodone

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Death may result 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.

Summary sheet: Oxycodone
Oxycodone
Oxycodone.svg
Chemical Nomenclature
Common names OxyContin, Oxy, Roxicodone, Oxecta, OxyIR, Endone, Oxynor, Codilek, Oxydor, Redocam, Oxygesic
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

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 1 - 2.5 mg
Light 2.5 - 10 mg
Common 10 - 25 mg
Strong 25 - 40 mg
Heavy 40 mg +
Duration
Total 4 - 6 hours
Onset 20 - 40 minutes



Insufflated
Dosage
Threshold 1 - 2.5 mg
Light 2.5 - 7.5 mg
Common 7.5 - 15 mg
Strong 15 - 25 mg
Heavy 25 mg +
Duration
Total 3 - 5 hours
Onset 2 - 5 minutes






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.

Interactions
Amphetamines
MAOIs
Nitrous
PCP
Alcohol
Benzodiazepines
Cocaine
DXM
GHB/GBL
Ketamine
MXE
Tramadol


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[2][3] as one of several new semi-synthetic opioids in an attempt to improve on the existing opioids.[4]

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,[5] while in nondiabetic mice, the μ1-opioid receptor seems to be primarily responsible for these effects.[6]

Subjective effects

Disclaimer: The effects listed below are cited from the subjective effect index, which is based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be treated with a healthy degree of skepticism. It is worth noting that these effects will rarely (if ever) occur all at once, although higher 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.

Physical effects
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Cognitive effects
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Visual 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

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.[7] 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.[8]

Dangerous interactions

Although many psychoactive substances are reasonably safe to use on their own, they can quickly become dangerous or even life-threatening when taken with other substances. The following lists some known dangerous combinations, but cannot be guaranteed to include all of them. 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.

  • Alcohol - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. Place affected patients in the recovery position to prevent vomit aspiration from excess. Memory blackouts are likely
  • Amphetamines - Stimulants increase respiration rate which allows for a higher dose of opiates than would otherwise be used. If the stimulant wears off first then the opiate may overcome the user and cause respiratory arrest.
  • Benzodiazepines - Central nervous system and/or respiratory-depressant effects may be additively or synergistically present. The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position blackouts/memory loss likely.
  • Cocaine - Stimulants increase respiration rate which allows for a higher dose of opiates than would otherwise be used. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
  • DXM - CNS depression, difficult breathing, heart issues, hepatoxic, just very unsafe combination all around. Additionally if one takes DXM, their tolerance of opiates goes down slightly, thus causing additional synergistic effects.
  • GHB/GBL - The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position
  • Ketamine - Both substances bring a risk of vomiting and unconsciousness. If the user falls unconscious while under the influence there is a severe risk of vomit aspiration if they are not placed in the recovery position.
  • MAOIs - Coadministration of monoamine oxidase inhibitors (MAOIs) with certain opioids has been associated with rare reports of severe and fatal adverse reactions. There appear to be two types of interaction, an excitatory and a depressive one. Symptoms of the excitatory reaction may include agitation, headache, diaphoresis, hyperpyrexia, flushing, shivering, myoclonus, rigidity, tremor, diarrhea, hypertension, tachycardia, seizures, and coma. Death has occurred in some cases.
  • MXE - This combination can potentiate the effects of the opioid
  • Nitrous - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. While unconscious, vomit aspiration is a risk if not placed in the recovery position. Memory blackouts are likely.
  • PCP - PCP can reduce opioid tolerance, increasing the risk of overdose.
  • Tramadol - Concomitant use of tramadol increases the seizure risk in patients taking other opioids. These agents are often individually epileptogenic and may have additive effects on seizure threshold during coadministration. Central nervous system- and/or respiratory-depressant effects may be additively or synergistically present

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.[9] The 1961 Single Convention on Narcotic Drugs of the United Nations, which replaced the 1931 convention, categorized oxycodone in Schedule I.[10]

  • Australia: Oxycodone is in Schedule I (derived from the Single Convention on Narcotic Drugs) of the Commonwealth's Narcotic Drugs Act 1967.[11] 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".[12]
  • 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).[citation needed]
  • Canada: Oxycodone is a controlled substance under Schedule I of the Controlled Drugs and Substances Act (CDSA).[13]
  • Germany: The drug is in Appendix III of the Narcotics Act (Betäubungsmittelgesetz or BtMG).[14] 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).[15]
  • Hong Kong: Oxycodone is regulated under Part I of Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance.[16]
  • 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.[17] 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.[18]
  • UK: Oxycodone is a Class A drug under the Misuse of Drugs Act.[19]
  • USA: Oxycodone is a Schedule II controlled substance.[20]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. German (DE) Patent 296916
  3. Sneader W (2005). Drug discovery: a history. Hoboken, NJ: Wiley. p. 119. ISBN 0-471-89980-1.
  4. Oxycodone (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/15907646
  5. Characterization of the antinociceptive effects of oxycodone in diabetic mice (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0014299906001282
  6. Involvement of μ1-opioid receptor on oxycodone-induced antinociception in diabetic mice (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0014299907000386
  7. Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2
  8. 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
  9. 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
  10. "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
  11. http://www.austlii.edu.au/au/legis/cth/consol_act/nda1967160/sch1.html
  12. http://www.comlaw.gov.au/ComLaw/Legislation/LegislativeInstrument1.nsf/0/3BBB39C4645284BCCA2574A6001C711F/$file/PoisonsStandard2008.pdf
  13. http://laws-lois.justice.gc.ca/eng/acts/c-38.8/fulltext.html
  14. http://www.gesetze-im-internet.de/btmg_1981/BJNR106810981.html
  15. http://www.gesetze-im-internet.de/btmg_1981/BJNR106810981.html
  16. http://www.hklii.hk/cgi-bin/sinodisp/eng/hk/legis/ord/134/sch1-19970630.html?stem=&synonyms=&query=oxycodone
  17. 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
  18. Misuse of Drugs Act (Singapore), section 5(1).
  19. https://www.gov.uk/government/uploads/system/uploads/attachment_data/file/277310/ControlledDrugsList4Feb2013.doc
  20. http://www.deadiversion.usdoj.gov/schedules/