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Oxycodone (brand names OxyContin, Percocet, Percodan, Roxicet, Roxicodone, Tylox, many others), known originally in Germany (where it was developed) as eukodal or dihydroxycodeinone, is a semisynthetic opioid synthesized from thebaine, an opioid alkaloid found in the Persian poppy, and one of the many alkaloids found in the opium poppy. It is a moderately potent opioid analgesic, generally indicated for relief of moderate to severe pain.^[7] Oxycodone was developed in 1917 in Germany^[8]^[9] as one of several semi-synthetic opioids in an attempt to improve on the existing opioids.^[1]

Oxycodone is available as single-ingredient medication in immediate release and controlled release. Parenteral formulations of 10 mg/mL and 50 mg/mL are available in the UK for IV/IM administration.^[10] Combination products are also available as immediate-release formulations, with non-narcotic analgesic ingredients such as paracetamol (acetaminophen) and nonsteroidal anti-inflammatory drugs (NSAIDs), including aspirin and ibuprofen. An abuse-deterrent combination with naloxone is available in managed-release tablets. If injected, the naloxone precipitates opioid withdrawal symptoms and blocks the effect of the medication.

1 Medical uses
- 1.1 Administration
- 1.2 Formulations
2 Adverse effects
- 2.1 Dependence, addiction and withdrawal
- 2.2 Hormone imbalance
3 Interactions
4 Pharmacology
- 4.1 Pharmacodynamics
  - 4.1.1 Controversy
- 4.2 Pharmacokinetics
  - 4.2.1 Absorption
  - 4.2.2 Distribution
  - 4.2.3 Metabolism
  - 4.2.4 Elimination
  - 4.2.5 Bioavailability
  - 4.2.6 Morphine equivalency
5 Physical and chemical properties
- 5.1 Biosynthesis
- 5.2 Detection in biological fluids
6 History
7 Society and culture
- 7.1 Legal status
  - 7.1.1 General
  - 7.1.2 Australia
  - 7.1.3 Canada
    - 7.1.3.1 Canadian legislative changes
    - 7.1.3.2 Canadian lawsuits
  - 7.1.4 Germany
  - 7.1.5 Hong Kong
  - 7.1.6 Japan
  - 7.1.7 Singapore
  - 7.1.8 United Kingdom
  - 7.1.9 United States
- 7.2 Recreational use
  - 7.2.1 Effects
  - 7.2.2 Preventive measures
  - 7.2.3 Australia
  - 7.2.4 Canada
  - 7.2.5 United Kingdom
  - 7.2.6 United States
- 7.3 Economics
8 Research
9 See also
10 References
11 Further reading

Medical uses

Oxycodone has been in clinical use since 1916,^[1] and it is used for managing moderate to moderately severe acute or chronic pain.^[11] It has been found to improve quality of life for those with many types of pain.^[12] Experts are divided regarding use for non cancer-related chronic pain, as most opioids have great potential for dependence and may also create paradoxical pain sensitivity.

Oxycodone is available as controlled-release tablet, intended to be taken every 12 hours.^[13] A 2006 review found that controlled-release oxycodone is comparable to instant-release oxycodone, morphine, and hydromorphone in management of moderate to severe cancer pain, with fewer side effects than morphine. The author concluded that the controlled release form is a valid alternative to morphine and a first-line treatment for cancer pain.^[14] In 2014, the European Association for Palliative Care recommended oral oxycodone as a second-line alternative to oral morphine for cancer pain.^[15]

In the US, extended-release oxycodone is approved for use in children as young as 11 years old. The approved indication is for relief of cancer pain, trauma pain, or pain due to major surgery, in children already treated with opioids, who can tolerate at least 20 mg per day of oxycodone; this provides an alternative to Duragesic (fentanyl) the only other extended-release opioid analgesic approved for children.^[16]

Administration

In the United States, oxycodone is only approved for oral use, available as tablets and oral solutions. In the United Kingdom, oxycodone is also approved for intravenous (IV) and intramuscular (IM) use. When first introduced in Germany during World War I, IV and IM oxycodone was commonly used for post-operative pain management of Central Powers soldiers.^[1]

Formulations

Oxycodone is available in a variety of formulations for oral or sublingual administration:^[17]^[18]^[19]^[3]

Immediate-release oxycodone (OxyFast, OxyIR, OxyNorm, Roxicodone)
Controlled-release oxycodone (OxyContin)
Immediate-release oxycodone with paracetamol (acetaminophen) (Oxycocet, Percocet, Roxicet, Tylox)
Immediate-release oxycodone with aspirin (Endodan, Oxycodan, Percodan, Roxiprin)
Immediate-release oxycodone with ibuprofen (Combunox)^[20]
Controlled-release oxycodone with naloxone (Targiniq)^[21]

Parenteral formulations of oxycodone (brand name OxyNorm) are also avaialable, and are widely used in Europe.^[22]^[23]^[24]

Adverse effects

Main side effects of oxycodone^[25]

Common side effects include euphoria, constipation, fatigue, somnolence, dizziness, nausea, vomiting, dry mouth, anxiety, itching, and sweating.^[26] Less common side effects (experienced by less than 5% of patients) include loss of appetite, nervousness, abdominal pain, diarrhea, urine retention, dyspnea, and hiccups.^[27]

In high doses, overdoses, or in some persons not tolerant to opioids, oxycodone can cause shallow breathing, bradycardia, cold-clammy skin, apnea, hypotension, miosis, circulatory collapse, respiratory arrest, and death.^[27]

Oxycodone in combination with naloxone in managed-release tablets, has been formulated to reduce side effects.^[28]

Dependence, addiction and withdrawal

The risk of experiencing severe withdrawal symptoms is high if a patient has become physically dependent and discontinues oxycodone abruptly. Medically, when the drug has been taken regularly over an extended period, it is withdrawn gradually rather than abruptly. People who regularly use oxycodone recreationally or at higher than prescribed doses are at even higher risk of severe withdrawal symptoms. The symptoms of oxycodone withdrawal, as with other opioids, may include "anxiety, panic attack, nausea, insomnia, muscle pain, muscle weakness, fevers, and other flu-like symptoms".^[29]

Withdrawal symptoms have also been reported in newborns whose mothers had been either injecting or orally taking oxycodone during pregnancy.^[30]

Hormone imbalance

As with other opioids, chronic use of oxycodone (particularly with higher doses) often causes concurrent hypogonadism or hormone imbalance.^[31]

Interactions

Oxycodone is metabolized by the enzymes CYP3A4 and CYP2D6, and its clearance therefore can be altered by inhibitors and inducers of these enzymes.^[23] Natural genetic variation in these enzymes can also influence the clearance of oxycodone, which may be related to the wide inter-individual variability in its half-life and potency.^[23]

Pharmacology

Pharmacodynamics

Oxycodone is a highly selective full agonist of the μ-opioid receptor (MOR), with very little affinity for the δ-opioid receptor (DOR) or κ-opioid receptor (KOR).^[23]^[22] After oxycodone binds to the MOR, a G protein-complex is released, which inhibits the release of neurotransmitters by the cell by reducing the amount of cAMP produced, closing calcium channels, and opening potassium channels.^[32]

Similarly to most other opioids, oxycodone increases prolactin secretion, but its influence on testosterone levels is unknown.^[22] Unlike morphine, oxycodone lacks immunosuppressive activity (measured by natural killer cell activity and interleukin 2 production in vitro); the clinical relevance of this has not been clarified.^[22]

Controversy

In 1997, a group of Australian researchers proposed (based on a study in rats) that oxycodone acts on KORs, unlike morphine, which acts upon MORs.^[33] Further research by this group indicated the drug appears to be a κ_2b-opioid agonist.^[34] However, this conclusion has been disputed, primarily on the basis that oxycodone produces effects that are typical of μ-opioid agonists, mainly because oxycodone is metabolized in the liver to oxymorphone as a metabolite, which is a more potent opioid agonist with stronger/higher (3- to 5-fold) binding affinity to μ-opioid receptors compared to oxycodone.^[35]^[4]

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 antinociceptive effects of oxycodone,^[36] while in nondiabetic mice, the μ₁-opioid receptor seems to be primarily responsible for these effects.^[37]

Pharmacokinetics

Absorption

After a dose of conventional (instant-release) oral oxycodone, the onset of action is 10–30 minutes,^[3]^[4] and peak plasma levels of the drug are attained within roughly 30–60 minutes;^[3]^[38]^[4] in contrast, after a dose of OxyContin (an oral controlled-release formulation), peak plasma levels of oxycodone occur in about three hours.^[27] The duration of instant-release oxycodone is 3 to 6 hours, although this can be variable depending on the individual.^[4]

Distribution

Oxycodone in the blood is distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, and brain.^[27] Conventional oral preparations start to reduce pain within 10–15 minutes on an empty stomach; in contrast, OxyContin starts to reduce pain within one hour.^[11]

Metabolism

Oxycodone is metabolized to α and β oxycodol; oxymorphone (a minor metabolite),^[22] then α and β oxymorphol and noroxymorphone; and noroxycodone, then α and β noroxycodol and noroxymorphone (N-desmethyloxycodone).^[38] (14-Methoxymetopon that in turn becomes 14-Hydroxydihydromorphine) These metabolites are true only for humans.^[39] As many as six metabolites for oxycodone (14-hydroxydihydromorphinone, 14-hydroxydihydrocodeine, 14-hydroxydihydrocodeinone N-oxide {oxycodone N-oxide}, 14-hydroxydihydroisocodeine, 14-hydroxydihydrocodeine N-oxide, and noroxycodone) have been found in rabbits,^[40] several of which are thought to be active metabolites to some extent, although a study using conventional oral oxycodone concluded oxycodone itself, and not its metabolites, is predominantly responsible for the drug's opioid effects on the brain.^[38]

Oxycodone is metabolized by the cytochrome P450 enzyme system in the liver, making it vulnerable to drug interactions.^[27] Some people are fast metabolizers, resulting in reduced analgesic effect, but increased adverse effects, while others are slow metabolisers, resulting in increased toxicity without improved analgesia.^[41]^[42] The dose of OxyContin must be reduced in patients with reduced hepatic function.^[11]

Elimination

Oxycodone and its metabolites are mainly excreted in the urine and sweat; therefore, it accumulates in patients with renal impairment.^[11]

Bioavailability

Oxycodone can be administered orally, intranasally, via intravenous, intramuscular, or subcutaneous injection, or rectally. The bioavailability of oral administration of oxycodone averages 60–87%, with rectal administration yielding the same results; intranasal varies between individuals with a mean of 46%.^[43]

Morphine equivalency

Taken orally, 20 mg of immediate release oxycodone is equivalent to 30 mg of morphine.^[44]^[45] Extended release oxycodone is considered to be twice as potent as oral morphine.^[46]

Physical and chemical properties

Oxycodone's chemical name is derived from codeine. The chemical structures are very similar, differing only in that

Oxycodone has a hydroxyl group at carbon-14 (codeine has just a hydrogen in its place)
Oxycodone has a 7,8-dihydro feature. Codeine has a double bond between those two carbons; and
Oxycodone has a carbonyl group (as in ketones) in place of the hydroxyl group of codeine.

It is also similar to hydrocodone, differing only in that it has a hydroxyl group at carbon-14.^[11]

Expanded expression for the compound oxycodone in the academic literature include "dihydrohydroxycodeinone",^[6]^[47]^[48] "Eucodal",^[47]^[48] "Eukodal",^[1]^[49] "14-hydroxydihydrocodeinone",^[6]^[47] and "Nucodan".^[47]^[48] In a UNESCO convention, the translations of "oxycodone" are oxycodon (Dutch), oxycodone (French), oxicodona (Spanish), الأوكسيكودون (Arabic), 羟考酮 (Chinese), and оксикодон (Russian).^[50] The word "oxycodone" should not be confused with "oxandrolone", "oxazepam", "oxybutynin", "oxytocin", or "Roxanol".^[51]

Oxycodone is marketed as various salts, most commonly as the hydrochloride salt. The free base conversion ratios of different salts are: hydrochloride (0.896), bitartrate (0.667), tartrate (0.750), camphosulphonate (0.576), pectinate (0.588), phenylpriopionate (0.678), sulphate (0.887), phosphate (0.763), and terephthalate (0.792). The hydrochloride salt is the basis of most American oxycodone products whilst bitartrate, tartrate, pectinate, terephthalate and phosphate salts are also available in European products. Methyiodide and hydroiodide are mentioned in older European publications.

Biosynthesis

In terms of biosynthesis, oxycodone has been found naturally in nectar extracts from the orchid family Epipactis helleborine; together along with another opioid: 3-{2-{3-{3-benzyloxypropyl}-3-indol, 7,8-didehydro- 4,5-epoxy-3,6-d-morphinan.^[52]

Detection in biological fluids

Oxycodone and/or its major metabolites may be measured in blood or urine to monitor for clearance, abuse, confirm a diagnosis of poisoning, or assist in a medicolegal death investigation. Many commercial opiate screening tests cross-react appreciably with oxycodone and its metabolites, but chromatographic techniques can easily distinguish oxycodone from other opiates.^[53]

History

Freund and Speyer of the University of Frankfurt in Germany first synthesized oxycodone from thebaine in 1916,^[9] a few years after the German pharmaceutical company Bayer had stopped the mass production of heroin due to hazardous use, harmful use, and dependence. It was hoped that a thebaine-derived drug would retain the analgesic effects of morphine and heroin with less dependence. Unfortunately, this was ultimately not found to be the case.

The first clinical use of the drug was documented in 1917, the year after it was first developed.^[9]^[49] It was first introduced to the US market in May 1939. In early 1928, Merck introduced a combination product containing scopolamine, oxycodone, and ephedrine under the German initials for the ingredients SEE, which was later renamed Scophedal (SCOpolamine ePHEDrine and eukodAL). This combination is essentially an oxycodone analogue of the morphine-based Twilight Sleep, with ephedrine added to reduce circulatory and respiratory effects.^{[citation needed]}

The personal notes of Adolf Hitler's physician, Dr. Theodor Morell, indicate Hitler received repeated injections of "eukodal" (oxycodone).^[54]

In the early 1960s, the United States government classified oxycodone as a schedule II drug.

In 1996, Purdue Pharma introduced OxyContin, a controlled release formulation of oxycodone.^[55]^[56] The product has been a commercial success,^[55] and since its introduction, Purdue has earned more than $31 billion from OxyContin.^[57]

Society and culture

Legal status

General

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.^[58] The 1961 Single Convention on Narcotic Drugs of the United Nations, which replaced the 1931 convention, categorized oxycodone in Schedule I.^[59] Global restrictions on Schedule I drugs include "limit[ing] exclusively to medical and scientific purposes the production, manufacture, export, import, distribution of, trade in, use and possession of" these drugs; "requir[ing] medical prescriptions for the supply or dispensation of [these] drugs to individuals"; and "prevent[ing] the accumulation" of quantities of these drugs "in excess of those required for the normal conduct of business".^[59]

Australia

Oxycodone is in Schedule I (derived from the Single Convention on Narcotic Drugs) of the Commonwealth's Narcotic Drugs Act 1967.^[60] 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".^[61]

Canada

Oxycodone is a controlled substance under Schedule I of the Controlled Drugs and Substances Act (CDSA).^[62]

Canadian legislative changes

In February 2012, Ontario passed legislation to allow the expansion of an already existing drug-tracking system for publicly funded drugs to include those that are privately insured. This database will function to identify and monitor patient’s attempts to seek prescriptions from multiple doctors or retrieve from multiple pharmacies. Other provinces have proposed similar legislation, while some, such as Nova Scotia, have legislation already in effect for monitoring prescription drug use. These changes have coincided with other changes in Ontario’s legislation to target the misuse of painkillers and high addiction rates to drugs such as oxycodone. As of February 29, 2012, Ontario passed legislation delisting oxycodone from the province’s public drug benefit program. This was a first for any province to delist a drug based on addictive properties. The new law prohibits prescriptions for OxyNeo except to certain patients under the Exceptional Access Program including palliative care and in other extenuating circumstances. Patients already prescribed oxycodone will receive coverage for an additional year for OxyNeo, and after that, it will be disallowed unless designated under the exceptional access program.^[63]

Much of the legislative activity has stemmed from Purdue Pharma’s decision in 2011 to begin a modification of Oxycontin’s composition to make it more difficult to crush for snorting or injecting. The new formulation, OxyNeo, is intended to be preventative in this regard and retain its effectiveness as a painkiller. Since introducing its Narcotics Safety and Awareness Act, Ontario has committed to focusing on drug addiction, particularly in the monitoring and identification of problem opioid prescriptions, as well as the education of patients, doctors, and pharmacists.^[64] This Act, introduced in 2010, commits to the establishment of a unified database to fulfil this intention.^[65] Both the public and medical community have received the legislation positively, though concerns about the ramifications of legal changes have been expressed. Because laws are largely provincially regulated, many speculate a national strategy is needed to prevent smuggling across provincial borders from jurisdictions with looser restrictions.^[66]

In 2015, Purdue Pharma's abuse-resistant OxyNEO and six generic versions of OxyContin had been on the Canada-wide approved list for prescriptions since 2012. In June 2015, then federal Minister of Health Rona Ambrose announced that within three years all oxycodone products sold in Canada would need to be tamper-resistant. Some experts warned that the generic product manufacturers may not have the technology to achieve that goal, possibly giving Purdue Pharma a monopoly on this opiate.^[67]

Canadian lawsuits

Several class action suits across Canada have been launched against the Purdue group of companies and affiliates. Claimants argue the pharmaceutical manufacturers did not meet a standard of care and were negligent in doing so. These lawsuits reference earlier judgments in the United States, which held that Purdue was liable for wrongful marketing practices and misbranding. Since 2007, the Purdue companies have paid over $650 million in settling litigation or facing criminal fines.^[68]

Germany

The drug is in Appendix III of the Narcotics Act (Betäubungsmittelgesetz or BtMG).^[69] 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).^[69]

Hong Kong

Oxycodone is regulated under Part I of Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance.^[70]

Japan

Oxycodone is a restricted drug in Japan. Its import and export is strictly restricted to specially designated organizations having prior permit to import it. In a high-profile case a top Toyota executive, who claimed to be unaware of the law, was arrested for importing oxycodone into Japan.^[71]^[72]

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 5 strokes of the cane, and a maximum sentence of life imprisonment or 30 years of imprisonment and 15 strokes of the cane.^[73] The minimum and maximum penalties for unauthorized trafficking in the drug are respectively 5 years of imprisonment and 5 strokes of the cane, and 20 years of imprisonment and 15 strokes of the cane.^[74]

United Kingdom

Oxycodone is a Class A drug under the Misuse of Drugs Act.^[75] For Class A drugs, which are "considered to be the most likely to cause harm", possession without a prescription is punishable by up to seven years in prison, an unlimited fine, or both.^[76] Dealing of the drug illegally is punishable by up to life imprisonment, an unlimited fine, or both.^[76] In addition, oxycodone is a Schedule 2 drug per the Misuse of Drugs Regulations 2001 which "provide certain exemptions from the provisions of the Misuse of Drugs Act 1971".^[77]

United States

Under the Controlled Substances Act, enacted in 1971 by President Richard Nixon,^[78] oxycodone is a Schedule II controlled substance whether by itself or part of a multi-ingredient medication. The DEA lists oxycodone both for sale and for use in manufacturing other opioids as ACSCN 9143 and in 2013 approved the following annual aggregate manufacturing quotas: 131.5 metric tons for sale, down from 153.75 in 2012, and 10.25 metric tons for conversion, unchanged from the previous year.^[79]

Recreational use

Effects

Oxycodone, like other opioid analgesics, tends to induce feelings of euphoria, relaxation and reduced anxiety in those who are occasional users.^[80] These effects make it one of the most commonly abused pharmaceutical drugs in the United States.^[81]

Preventive measures

In August 2010, Purdue Pharma reformulated their long-acting oxycodone line, marketed as OxyContin, using a polymer, Intac,^[82] to make the pills extremely difficult to crush or dissolve^[83] in water to reduce OxyContin abuse.^[84] The FDA approved relabeling the reformulated version as abuse-resistant in April 2013.^[85]

Pfizer manufactures a preparation of short-acting oxycodone, marketed as OXECTA, which contains inactive ingredients, referred to as tamper-resistant AVERSION® Technology.^[86] It does not deter oral abuse. Approved by the FDA in the US in June 2011, the new formulation makes crushing, chewing, snorting, or injecting the opioid impractical because of a change in its chemical properties.^[87]

Australia

The non-medical use of oxycodone existed from the early 1970s, but by 2015, 91% of a national sample of injecting drug users in Australia had reported using oxycodone, and 27% had injected it in the last six months.^[88]

Canada

Opioid-related deaths in Ontario had increased by 242% from 1969 to 2014.^[89] By 2009 in Ontario there were more deaths from oxycodone overdose than from cocaine overdose.^[90] Deaths from opioid pain relievers had increased from 13.7 deaths per million residents in 1991 to 27.2 deaths per million residents in 2004.^[91] The abuse of oxycodone in Canada became a problem. Areas where oxycodone is most problematic are Atlantic Canada and Ontario, where its abuse is prevalent in rural towns, and in many smaller to medium-sized cities.^[92] Oxycodone is also widely available across Western Canada, but methamphetamine and heroin are more serious problems in the larger cities, while oxycodone is more common in rural towns. Oxycodone is diverted through doctor shopping, prescription forgery, pharmacy theft, and overprescribing.^[92]^[93]

The recent formulations of oxycodone, particularly Purdue Pharma's crush-, chew-, injection- and dissolve-resistant OxyNEO^[94] which replaced the banned OxyContin product in Canada in early 2012, have led to a decline in the abuse of this opiate but have increased the abuse of the more potent drug fentanyl.^[95] According to a Canadian Centre on Substance Abuse study quoted in Maclean's magazine, there were at least 655 fentanyl-related deaths in Canada in a five-year period.^[96]

In Alberta, the Blood Tribe police claimed that from the fall of 2014 through January 2015, oxycodone pills or a lethal fake variation referred to as Oxy 80s^[97] containing fentanyl made in illegal labs by members of organized crime were responsible for ten deaths on the Blood Reserve, which is located southwest of Lethbridge, Alberta.^[98] Province-wide, approximately 120 Albertans died from fentanyl-related overdoses in 2014.^[97]

United Kingdom

Abuse and diversion of oxycodone in the UK commenced in the early- to mid-2000s.^[99] The first known death due to overdose in the UK occurred in 2002.^[100] However, recreational use remains relatively rare.

United States

In the United States, more than 12 million people use opioid drugs recreationally.^[101] In 2010, 16,652 deaths were related to opioid overdose in combination with other drugs such as benzodiazepines and alcohol.^[102] In September 2013, the FDA released new labeling guidelines for long acting and extended release opioids requiring manufacturers to remove moderate pain as indication for use, instead stating the drug is for "pain severe enough to require daily, around-the-clock, long term opioid treatment."^[103] The updated labeling will not restrict physicians from prescribing opioids for moderate, as needed use.^[101]

Oxycodone is the most widely recreationally used opioid in America. The US Department of Health and Human Services estimates that about 11 million people in the US consume oxycodone in a non-medical way annually.^[104] In 2007, about 42,800 emergency room visits occurred due to "episodes" involving oxycodone.^[105] Diverted oxycodone may be taken orally or ingested through insufflation; used intravenously, or the heated vapors inhaled. In 2008, recreational use of oxycodone and hydrocodone were involved in 14,800 deaths. Some of the cases were due to overdoses of the acetaminophen component, resulting in fatal liver damage.^[106]

Reformulated OxyContin is causing some recreational users to change to heroin, which is cheaper and easier to obtain.^[107]

Economics

The International Narcotics Control Board estimated 11.5 short tons (10.4 t) of oxycodone were manufactured worldwide in 1998;^[108] by 2007 this figure had grown to 75.2 short tons (68.2 t).^[108] United States accounted for 82% of consumption in 2007 at 51.6 short tons (46.8 t). Canada, Germany, Australia and France combined accounted for 13% of consumption in 2007.^[108]^[109] In 2010, 1.3 short tons (1.2 t) of oxycodone were illegally manufactured using a fake pill imprint. This accounted for 0.8% of consumption. These illicit tablets were later seized by the US Drug Enforcement Administration, according to the International Narcotics Control Board.^[110] The board also reported 122.5 short tons (111.1 t) manufactured in 2010. This number had decreased from a record high of 135.9 short tons (123.3 t) in 2009.^[111]

Research

There are a few case reports that oxycodone may have antidepressant effects in some individuals with severe, treatment-resistant major depressive disorder.^[112]

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UpToDate Contents

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1. Management of chronic pain in chronic kidney disease
2. 米国外の緩和ケアとホスピス palliative care and hospice outside of the united states
3. Urogynecologic surgery: Perioperative patient care issues
4. Conservative management of end-stage renal disease
5. オピオイド系薬剤を用いた癌疼痛のマネージメント：至適鎮痛作用 cancer pain management with opioids optimizing analgesia

English Journal

The Analgesic Concentration of Oxycodone with Co-administration of Paracetamol - A Dose-Finding Study in Adult Patients Undergoing Laparoscopic Cholecystectomy.

Kokki M, Broms S, Eskelinen M, Neuvonen PJ, Halonen T, Kokki H.SourceDepartment of Anaesthesia and Operative Services, Kuopio University Hospital, Kuopio, Finland; School of Medicine, University of Eastern Finland, Kuopio, Finland.
Basic & clinical pharmacology & toxicology.Basic Clin Pharmacol Toxicol.2012 Dec;111(6):391-5. doi: 10.1111/j.1742-7843.2012.00916.x. Epub 2012 Jul 21.
We have previously shown that paracetamol has an opioid-sparing effect in tonsillectomy, and now, we evaluated the analgesic efficacy of paracetamol i.v. in early post-operative pain after laparoscopic cholecystectomy (LCC). Twenty-four patients with LCC were randomized to receive paracetamol i.v. 1
PMID 22734581

Occupational allergic contact dermatitis caused by oxycodone.

Wootton CI, English JS.SourceDepartment of Dermatology, Queens Medical Centre, NG7 2UH Nottingham, UK.
Contact dermatitis.Contact Dermatitis.2012 Dec;67(6):383-4. doi: 10.1111/j.1600-0536.2012.02137.x.
PMID 23151197

Japanese Journal

神経障害性癌疼痛の急性増悪に対し,オキシコドン速放性製剤とプレガバリンの同時投与が著効を示した1症例

馬場美華,後明郁男
麻酔 61(10), 1148-1152, 2012-10
NAID 40019448955

がん性疼痛におけるオピオイド (特集疼痛緩和医療におけるDDS)

服部政治,五十嵐妙,寶田潤子 [他]
Drug delivery system 26(5), 461-467, 2011-09
NAID 40019043229

Related Pictures

★リンクテーブル★

リンク元	「麻薬性鎮痛薬」「オキシコドン」
拡張検索	「oxycodone hydrochloride hydrate」「oxycodone hydrochloride」「combination of compound oxycodone and atropine」

「麻薬性鎮痛薬」

Oxycodone (INN, USAN, BAN, JAN)
Systematic (IUPAC) name
	(5R,9R,13S,14S)-4,5α-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one
Clinical data
Trade names	Combunox, Endodan, Oxycocet, Oxycodan, OxyContin, OxyFast, OxyIR, OxyNorm, Percocet, Percodan, Roxicet, Roxicodone, Roxiprin, Targiniq, Tylox, many others
AHFS/Drugs.com	Monograph
MedlinePlus	a682132
Pregnancy; category	AU: C; US: B (No risk in non-human studies); ;
Dependence; liability	High
Routes of; administration	Oral, sublingual, intramuscular, intravenous, intranasal, subcutaneous, transdermal, rectal, epidural
Legal status
Legal status	AU: S8 (Controlled); CA: Schedule I; DE: Anlage III (Prescription only); UK: Class A; US: Schedule II;
Pharmacokinetic data
Bioavailability	60–87%
Protein binding	45%
Metabolism	Hepatic: mainly CYP3A, and, to a much lesser extent, CYP2D6 to oxymorphone (~5%); 95% metabolized (i.e., 5% excreted unchanged)
Onset of action	10–30 minutes (IR); 1 hour (CR)
Biological half-life	2–3 hours (variable) (same t1/2 for all ROAs)
Duration of action	3–6 hours (IR) (variable); 12 hours (CR)
Excretion	Urine (83%)
Identifiers
CAS Number	76-42-6
ATC code	N02AA05 (WHO); N02AA55 (WHO) (in combinations)
PubChem	CID 5284603
IUPHAR/BPS	7093
DrugBank	DB00497
ChemSpider	4447649
UNII	CD35PMG570
KEGG	D05312
ChEBI	CHEBI:7852
ChEMBL	CHEMBL656
Synonyms	Eukodal, eucodal; dihydrohydroxycodeinone, 7,8-dihydro-14-hydroxycodeinone, 6-deoxy-7,8-dihydro-14-hydroxy-3-O-methyl-6-oxomorphine
Chemical data
Formula	C18H21NO4
Molar mass	315.364 g/mol
	SMILES O=C4[C@@H]5Oc1c2c(ccc1OC)C[C@H]3N(CC[C@]25[C@@]3(O)CC4)C ;
	InChI InChI=1S/C18H21NO4/c1-19-8-7-17-14-10-3-4-12(22-2)15(14)23-16(17)11(20)5-6-18(17,21)13(19)9-10/h3-4,13,16,21H,5-9H2,1-2H3/t13-,16+,17+,18-/m1/s1 ; Key:BRUQQQPBMZOVGD-XFKAJCMBSA-N ;
Physical data
Solubility in water	HCl: 166 mg/mL (20 °C)
(verify)

　　[★]

英: narcotic analgesic, narcotic analgesics
同: オピオイド鎮痛薬、モルフィン鎮痛薬？？？
関: オピオイド

モルフィン鎮痛薬

内因性オピオイド

外因性オピオイド

合成

phenylheptylamines

メタドン methadone

phenylpiperadines

オピオイド受容体拮抗薬

ナロキソン naloxone

麻酔薬として

心臓手術やハイリスク患者の麻酔に用いる。
使用される薬にはクエン酸ファンタネルやモルヒネがある。
脳神経に存在する麻酔特有の受容体(オピオイド受容体)をしげきする
鎮痛作用は協力
麻酔薬なので常習性がある。
副作用：呼吸抑制、精神神経作用、消化器症状がある。
注意：患者さんの状態に合わせて、睡眠作用のある薬を使用。すなわち、これ単独では眠らない(記憶を失わない)
○強力な鎮痛・鎮静。血圧安定
×術中覚醒。呼吸抑制。筋硬直。徐脈。術中高血圧

パンクロニウム(長時間使用で頻脈になる)を併せて使うことがある。

依存性

麻薬(オピオイド)には精神依存性・身体依存性がある。
慢性的に疼痛が持続しているような癌患者では、κ受容体が賦活され、μ受容体(身体・精神依存性に関与)が抑制されている。このため、依存は起こらない。(SAN.411改変)

副作用

(高頻度)悪心・嘔吐、(高頻度)便秘、眠気、譫妄

「オキシコドン」

　　[★]

英: oxycodone
同: ジヒドロヒドロキシコデイノン dihydrohydroxycodeinone
化: 塩酸オキシコドン oxycodone hydrochloride、オキシコドン塩酸塩
商: オキシコンチン、オキノーム、オキファスト、パビナール・アトロピン、パビナール
関: アヘンアルカロイド系麻薬

添付文書

オキノーム散2.5mg／**オキノーム散5mg／**オキノーム散10mg

http://www.info.pmda.go.jp/go/pack/8119002B2023_1_01/8119002B2023_1_01?view=body

「oxycodone hydrochloride hydrate」

　　[★]

塩酸オキシコドン水和物

関: oxycodone、oxycodone hydrochloride

「oxycodone hydrochloride」

　　[★] オキシコドン、塩酸オキシコドン

「combination of compound oxycodone and atropine」

　　[★] 複方オキシコドン・アトロピン合剤

[Kalso-1] Kalso E (2005). "Oxycodone". Journal of Pain and Symptom Management. 29 (5S): S47–S56. doi:10.1016/j.jpainsymman.2005.01.010. PMID 15907646.

[MSR-2] "Roxicodone, OxyContin (oxycodone) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 8 April 2014.

[ElliottSmith2016-3] ^ ^a ^b ^c ^d ^e ^f Jennifer A. Elliott; Howard S. Smith (19 April 2016). Handbook of Acute Pain Management. CRC Press. pp. 82–. ISBN 978-1-4665-9635-1.

[SmithPassik2008-4] ^ ^a ^b ^c ^d ^e ^f ^g ^h Howard Smith; Steven Passik (25 April 2008). Pain and Chemical Dependency. Oxford University Press, USA. pp. 195–. ISBN 978-0-19-530055-0.

[YarbroWujcik2010-5] Connie Henke Yarbro; Debra Wujcik; Barbara Holmes Gobel (15 November 2010). Cancer Nursing: Principles and Practice. Jones & Bartlett Publishers. pp. 695–. ISBN 978-1-4496-1829-2.

[MerckIndex-6] O'Neil, Maryadele J., ed. (2006). The Merck index (14 ed.). Whitehouse Station, NJ: Merck & Co. ISBN 978-0-911910-00-1.

[7] Drewes, Asbjørn M; Jensen, Rasmus D; Nielsen, Lecia M; Droney, Joanne; Christrup, Lona L; Arendt-Nielsen, Lars; Riley, Julia; Dahan, Albert (2013). "Differences between opioids: pharmacological, experimental, clinical and economical perspectives" (PDF). British Journal of Clinical Pharmacology. 75 (1): 60–78. doi:10.1111/j.1365-2125.2012.04317.x. ISSN 0306-5251. PMC 3555047. PMID 22554450.

[8] German (DE) Patent 296916

[Oxysynthesis-9] Sneader W (2005). Drug discovery: a history. Hoboken, NJ: Wiley. p. 119. ISBN 0-471-89980-1.

[10] "eMC". eMC. Retrieved 1 July 2014.

[AHFS-11] "Oxycodone". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.

[Riley2008-12] Riley J, Eisenberg E, Müller-Schwefe G, Drewes AM, Arendt-Nielsen L (2008). "Oxycodone: a review of its use in the management of pain". Curr Med Res Opin. 24 (1): 175–192. doi:10.1185/030079908X253708. PMID 18039433.

[13] Biancofiore G (September 2006). "Oxycodone controlled release in cancer pain management". Ther Clin Risk Manag. 2 (3): 229–34. doi:10.2147/tcrm.2006.2.3.229. PMC 1936259. PMID 18360598.

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v t e Opioid receptor modulators

MOR	Agonists (abridged; see here for a full list): 7-Acetoxymitragynine 7-Hydroxymitragynine ψ-Akuammigine α-Chlornaltrexamine α-Narcotine Acetyldihydrocodeine Acetylfentanyl Acrylfentanyl Adrenorphin (metorphamide) AH-7921 Akuammicine Akuammidine Alfentanil Anileridine Apparicine β-Endorphin BAM-12P BAM-18P BAM-22P Benzhydrocodone Benzylmorphine Bezitramide Biphalin BU08070 Buprenorphine Butorphan Butorphanol Butyrfentanyl BW-373U86 Carfentanil Casokefamide Cebranopadol Chloroxymorphamine Codeine DADLE DAMGO (DAGO) Dermorphin Desomorphine Dextromoramide Dextropropoxyphene (propoxyphene) Dezocine Dimethylaminopivalophenone Eluxadoline Diamorphine (heroin) Dihydrocodeine Dihydroetorphine Dihydromorphine Diphenoxylate Dipipanone Dynorphin A Embutramide Endomorphin-1 Endomorphin-2 Eseroline Ethylmorphine Etorphine Fentanyl Fluorophen Frakefamide Hemorphin-4 Herkinorin Hodgkinsine Hydrocodone Hydromorphinol Hydromorphone IBNtxA Ketamine Ketobemidone Kratom Laudanosine Lefetamine Leu-enkephalin Levacetylmethadol Levomethorphan Levorphanol Lexanopadol Loperamide Matrine Meptazinol Met-enkephalin (metenkefalin) Methadone Metkefamide Metopon Mitragynine Mitragynine pseudoindoxyl Morphiceptin Morphine Nalbuphine Nalbuphine sebacate NalBzOH Nalmexone Naltalimide Neopine Nicocodeine Nicodicodeine Nicomorphine NKTR-181 Norketamine O-Desmethyltramadol Octreotide Oliceridine OM-3-MNZ Oripavine Oxycodone Oxymorphazone Oxymorphonazine Oxymorphone Oxymorphone phenylhydrazone OxyPNPH Papaver somniferum (opium) Pentazocine Pericine Pethidine (meperidine) Phenazocine Phencyclidine Piminodine Piritramide PL-017 Prodine Propiram Racemethorphan Racemorphan Remifentanil Salsolinol Sinomenine Sufentanil Tapentadol Tetrahydropapaveroline TH-030418 Thebaine Thienorphine Tianeptine Tilidine Tramadol Trimebutine TRIMU 5 TRV734 Tubotaiwine U-47700 Valorphin Viminol Xorphanol PAMs: BMS-986121 BMS-986122 Antagonists: (3S,4S)-Picenadol 2-(S)-N,N-(R)-Viminol 4-Caffeoyl-1,5-quinide 4′-Hydroxyflavanone 4',7-Dihydroxyflavone 6β-Naltrexol 6β-Naltrexol-d4 18-MC α-Gliadin β-Chlornaltrexamine β-Funaltrexamine Akuammine Alvimopan AM-251 Apigenin AT-076 Axelopran Bevenopran Catechin Catechin gallate Clocinnamox CTAP CTOP Cyclofoxy Cyprodime Diacetylnalorphine Diprenorphine ECG EGC Epicatechin Eptazocine Gemazocine Ginsenoside R Hyperoside Ibogaine Levallorphan Lobeline LY-255582 LY-2196044 Methocinnamox Methylnaltrexone Methylsamidorphan chloride Naldemedine Nalmefene Nalodeine (N-allylnorcodeine) Nalorphine Nalorphine dinicotinate Naloxazone Naloxegol Naloxol Naloxonazine Naloxone Naltrexazone Naltrexonazine Naltrexone Naltrindole Naringenin Noribogaine Oxilorphan Pawhuskin A Rimonabant Quadazocine Samidorphan Taxifolin Unknown/unsorted: Cannabidiol Coronaridine Cyproterone acetate Dihydroakuuamine Tabernanthine Tetrahydrocannabinol

DOR	Agonists: 6'-GNTI 7-SIOM ADL-5747 (PF-04856881) ADL-5859 Amoxapine AR-M100390 (ARM390) AZD2327 β-Endorphin BAM-18P Biphalin BU-48 Butorphan Butorphanol BW-373U86 Casokefamide Cebranopadol Codeine Cyclazocine DADLE Deltorphin A Deltorphin I Deltorphin II Desmethylclozapine Dezocine Diamorphine (heroin) Dihydroetorphine Dihydromorphine DPDPE DPI-221 DPI-3290 DSLET Ethylketazocine Etorphine Fentanyl FIT Fluorophen Hemorphin-4 Hydrocodone Hydromorphone Ibogaine Isomethadone JNJ-20788560 KNT-127 Kratom Laudanosine Leu-enkephalin Levomethorphan Levorphanol Lexanopadol Lofentanil Met-enkephalin (metenkefalin) Metazocine Metkefamide Mitragynine Mitragynine pseudoindoxyl Morphine N-Phenethyl-14-ethoxymetopon Norbuprenorphine NalBzOH O-Desmethyltramadol Oripavine Oxycodone Oxymorphone Pethidine (meperidine) Proglumide Racemethorphan Racemorphan RWJ-394674 Samidorphan SB-235863 SKF-10047 SNC-80 SNC-162 TAN-67 (SB-205,607) TH-030418 Thebaine Thiobromadol (C-8813) Tianeptine Tonazocine Tramadol TRV250 Xorphanol Zenazocine Antagonists: 4',7-Dihydroxyflavone 5'-NTII 6β-Naltrexol 6β-Naltrexol-d4 α-Santolol β-Chlornaltrexamine Apigenin AT-076 Axelopran Bevenopran BNTX Catechin Catechin gallate Clocinnamox Diacetylnalorphine Diprenorphine ECG EGC Eluxadoline Epicatechin ICI-154129 ICI-174864 LY-255582 LY-2196044 Methylnaltrexone Methylnaltrindole N-Benzylnaltrindole Nalmefene Nalorphine Naltrexone Naltriben Naltrindole Naloxone Naringenin Noribogaine Pawhuskin A Quadazocine SDM25N SoRI-9409 Taxifolin Thienorphine Unknown/unsorted: 18-MC Cannabidiol Coronaridine Cyproterone acetate Tabernanthine Tetrahydrocannabinol

KOR	Agonists: 6'-GNTI 8-CAC 18-MC 14-Methoxymetopon β-Chlornaltrexamine β-Funaltrexamine Adrenorphin (metorphamide) Akuuamicine Alazocine Allomatrine Asimadoline BAM-12P BAM-18P BAM-22P Big dynorphin Bremazocine BRL-52537 Butorphan Butorphanol BW-373U86 Cebranopadol Ciprefadol CR665 Cyclazocine Cyclorphan Cyprenorphine Diamorphine (heroin) Diacetylnalorphine Difelikefalin Dihydroetorphine Dihydromorphine Diprenorphine Dynorphin A Dynorphin B (rimorphin) Eluxadoline Enadoline Eptazocine Erinacine E Ethylketazocine Etorphine Fedotozine Fentanyl Gemazocine GR-89696 GR-103545 Hemorphin-4 Herkinorin HS665 Hydromorphone HZ-2 Ibogaine ICI-199,441 ICI-204,448 Ketamine Ketazocine Laudanosine Leumorphin (dynorphin B-29) Levallorphan Levomethorphan Levorphanol Lexanopadol Lofentanil LPK-26 Lufuradom Matrine MB-1C-OH Menthol Metazocine Metkefamide Mianserin Mirtazapine Morphine Moxazocine MR-2034 N-MPPP Nalbuphine Nalbuphine sebacate NalBzOH Nalfurafine Nalmefene Nalodeine (N-allylnorcodeine) Nalorphine Naltriben Niravoline Norbuprenorphine Norbuprenorphine-3-glucuronide Noribogaine Norketamine O-Desmethyltramadol Oripavine Oxilorphan Oxycodone Pentazocine Pethidine (meperidine) Phenazocine Proxorphan Racemethorphan Racemorphan RB-64 Salvinorin A (salvia) Salvinorin B ethoxymethyl ether Salvinorin B methoxymethyl ether Samidorphan SKF-10047 Spiradoline (U-62,066) TH-030418 Thienorphine Tifluadom Tricyclic antidepressants (e.g., amitriptyline, desipramine, imipramine, nortriptyline) U-50,488 U-54,494A U-69,593 Xorphanol Antagonists: 4′-Hydroxyflavanone 4',7-Dihydroxyflavone 5'-GNTI 6'-GNTI 6β-Naltrexol 6β-Naltrexol-d4 β-Chlornaltrexamine Buprenorphine/samidorphan Amentoflavone ANTI Apigenin Arodyne AT-076 Axelopran AZ-MTAB Binaltorphimine BU09059 Buprenorphine Catechin Catechin gallate CERC-501 (LY-2456302) Clocinnamox Cyclofoxy Dezocine DIPPA EGC ECG Epicatechin Hyperoside JDTic LY-255582 LY-2196044 LY-2444296 LY-2459989 LY-2795050 MeJDTic Methylnaltrexone ML190 ML350 MR-2266 N-Fluoropropyl-JDTic Naloxone Naltrexone Naltrindole Naringenin Norbinaltorphimine Noribogaine Pawhuskin A PF-4455242 RB-64 Quadazocine Taxifolin UPHIT Zyklophin Unknown/unsorted: Akuammicine Akuammine Coronaridine Cyproterone acetate Dihydroakuuamine Ibogamine Tabernanthine

NOP	Agonists: (Arg14,Lys15)Nociceptin ((pF)Phe⁴)Nociceptin(1-13)NH₂ (Phe¹Ψ(CH₂-NH)Gly²)Nociceptin(1-13)NH₂ Ac-RYYRWK-NH₂ Ac-RYYRIK-NH₂ BU08070 Buprenorphine Cebranopadol Dihydroetorphine Etorphine JNJ-19385899 Levomethorphan Levorphanol Levorphanol Lexanopadol MCOPPB MT-7716 NNC 63-0532 Nociceptin (orphanin FQ) Nociceptin (1-11) Nociceptin (1-13)NH₂ Norbuprenorphine Racemethorphan Racemorphan Ro64-6198 Ro65-6570 SCH-221510 SCH-486757 SR-8993 SR-16435 TH-030418 Antagonists: (Nphe¹)Nociceptin(1-13)NH₂ AT-076 BAN-ORL-24 J-113397 JTC-801 LY-2940094 NalBzOH Nociceptin (1-7) Nocistatin SB-612111 SR-16430 Thienorphine Trap-101 UFP-101

Unsorted	β-Casomorphins Amidorphin BAM-20P Cytochrophin-4 Deprolorphin Gliadorphin (gluteomorphin) Gluten exorphins Hemorphins Kava constituents MEAGL MEAP NEM Neoendorphins Nepetalactone (catnip) Peptide B Peptide E Peptide F Peptide I Rubiscolins Soymorphins

Others	Enkephalinase inhibitors: Amastatin BL-2401 Candoxatril D -Phenylalanine Dexecadotril (retorphan) Ecadotril (sinorphan) Kelatorphan Racecadotril (acetorphan) RB-101 RB-120 RB-3007 Opiorphan Selank Semax Spinorphin Thiorphan Tynorphin Ubenimex (bestatin) Propeptides: β-Lipotropin (proendorphin) Prodynorphin Proenkephalin Pronociceptin Proopiomelanocortin (POMC) Others: Kyotorphin (met-enkephalin releaser/degradation stabilizer)

See also: Peptide receptor modulators

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「oxycodone hydrochloride hydrate」

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