Oxycodone

Dihydrohydroxycodeinone

OxyContin, Roxicodone, Percocet, Percodan, Oxy

Psychoactive Class

Chemical Class

Oxycodone is a semisynthetic opioid of the morphinan class, synthesized from poppy-derived thebaine¹. Developed in Germany in 1916 as part of efforts to improve upon existing opioids such as morphine and codeine, it entered clinical use the following year¹. It is widely prescribed for moderate to severe pain in both immediate and extended release formulations. Compared to other opioids, it is reportedly more stimulating and mood-elevating, contributing to its significant potential for recreational misuse².

Dosage & Duration

Dosage

Threshold1-1 mg

Light2.5-10 mg

Moderate5-5 mg

Strong25-40 mg

Heavy40+ mg

Bioavailability

60-87%

Duration

Onset10-30 minutes

Come Up60-120 minutes

Peak1-2 hours

Offset0-2 hours

Total4-8 hours

Half-life

3.2-4.5 hours

Subjective Effects

Effects vary widely by individual, dose, and context.

Physical

The physical effects of oxycodeine can be broken down into several components which progressively intensify proportional to dosage. The general head space of codeine is described by many as one of intense euphoria, relaxation, anxiety suppression and pain relief.

Itchiness Constipation Cough suppression Difficulty urinating Nausea Stomach cramps Pupil constriction

Cognitive

The cognitive effects of codeine can be broken down into several components which progressively intensify proportional to dosage.

Anxiety suppression

Visual

Forked from Subjective Effect Documentation

by Josie KinsSeptember 2015.

Reagent Testing

Loading reagent data

Expected colorimetric results are being prepared.

Pharmacology

Pharmacodynamics

Oxycodone is a semisynthetic opioid that acts as a highly selective full agonist of the μ-opioid receptor.³ Binding at this receptor activates G protein-coupled signaling that inhibits neurotransmitter release through reduced cAMP production, closure of calcium channels, and opening of potassium channels.³ Oxycodone also acts as an agonist at the κ-opioid and δ-opioid receptors, though with low affinity at both sites.³

Pharmacokinetics

Oxycodone undergoes extensive hepatic metabolism (~95%) primarily through the cytochrome P450 system. CYP3A4 and CYP3A5 catalyze N-demethylation to the major metabolite noroxycodone (approximately 45-70% of the administered dose),⁴ while CYP2D6 catalyzes O-demethylation to oxymorphone (approximately 5-19%).⁴ Additional pathways include 6-keto-reduction and conjugation. Despite producing several metabolites with μ-opioid receptor activity, oxycodone itself accounts for approximately 83% of its analgesic effect after oral administration and approximately 95% after intravenous administration.⁵ Oral bioavailability averages 60-87% and is not affected by food.⁶ Oxycodone has a volume of distribution of 2.6 L/kg,³ with unbound brain concentrations approximately threefold higher than blood concentrations at equilibrium.⁷ The elimination half-life is approximately 3.2 hours for immediate-release formulations and 4.5 hours for extended-release formulations,³ with a clearance of 0.8 L/min.³ Oxycodone and its metabolites are primarily excreted in urine.³

Interactions

Dangerous

Highest risk

These combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.

AlcoholBenzodiazepinesCocaineDXMGHB/GBLKetamineMXEPregabalinTramadol

Unsafe

Avoid

There is considerable risk of physical harm when taking these combinations, they should be avoided where possible.

Diphenhydramine

Caution

Use caution

These combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.

AmphetaminesMAOIsMephedroneNitrous oxidePCP

TripSit

Tolerance

Full Tolerance

Oxycodone tolerance can develop for many effects after sustained repeated use, sometimes within days of daily administration. The pace differs by effect: constipation-related tolerance develops especially slowly compared with analgesic and euphoric tolerance. People taking oxycodone daily may need to raise their dose substantially to obtain similar effects, with some chronic users reporting daily doses of 200 mg or more compared with initial effective doses of 5-10 mg.

Baseline Reset

1-2 weeks of abstinence in the absence of further consumption. Fatal overdose risk can rise steeply when someone resumes use after a break because tolerance has fallen. Environmental context may also affect tolerance; research has shown that familiar drug-associated settings can provide some tolerance protection compared with novel settings.

Half Tolerance

3-7 days

Cross Tolerance

All other opioids

Harm Potential

Addiction & Dependence

Psychological

High

Oxycodone is highly addictive with significant potential for abuse and psychological dependence.⁸ Compulsive redosing is commonly reported, and many users find themselves consuming more than intended. The drug induces feelings of euphoria and relaxation that strongly reinforce continued use.

Physical

High

Physical dependence develops rapidly with regular use, reportedly faster than with morphine. Withdrawal symptoms include anxiety, panic attacks, nausea, insomnia, muscle pain and weakness, restlessness, irritability, depression, sweating, cold shivers, vomiting, diarrhea, and painful cramps.⁹ Severe withdrawal is expected after abrupt cessation in dependent individuals.

Toxicity

Respiratory

Dose-dependent respiratory depression occurs at all doses, becoming clinically significant at higher doses or in opioid-naive individuals; overdose can result in respiratory arrest and death.⁹

Gastrointestinal

Constipation is extremely common (affecting approximately 23% of users)⁹ and persists with continued use as tolerance to this effect develops slowly; chronic use has been implicated in life-threatening bowel perforations.¹⁰

Cardiovascular

Acute cardiovascular effects including bradycardia, hypotension, and histamine-mediated flushing can occur; serious cardiovascular depression is primarily associated with overdose situations.

Endocrine

Chronic use, particularly at higher doses, commonly causes hormonal disruption including hypogonadism and decreased libido.¹¹

Psychosis Risk

Hallucinations, confusion, and delirium are documented but uncommon side effects.⁹ These psychiatric manifestations are less frequent with oxycodone compared to some other opioids.

Seizure Risk

Seizures and convulsions are uncommon but have been reported.⁹

History & Culture

Discovery and Early Development

Oxycodone was first synthesized from the opium poppy alkaloid thebaine by Martin Freund and Edmund Speyer at the University of Frankfurt in Germany, with their synthesis published in 1916.¹ Clinical application of the drug followed the next year, when it was initially employed…

Legality

International

1961 Convention: Schedule I.

1971 Convention: not internationally scheduled.

1988 Convention: not internationally scheduled.

By Country

United StatesPrescription onlySchedule II

Schedule II⁴³

Controlled under the Controlled Substances Act since 1970.⁴⁴ Illegal to sell without a DEA license and illegal to purchase or possess without a valid prescription.⁹ The FDA revoked approval of the original sustained-release OxyContin formulation in 2010 due to widespread misuse, with reformulated abuse-deterrent versions subsequently approved.

By state

Most state and territorial schedules reviewed classify oxycodone consistently with federal Schedule II treatment.

Alaska

Prescription onlySchedule IA controlled substance

AustriaPrescription onlyAnhang I

Prescription only (AMG/SMG)²²

Legal for medical use under the Arzneimittelgesetz (Medicines Act). Possession or sale without a valid prescription is prohibited under the Suchtmittelgesetz (Addiction Substances Act).

GermanyPrescription onlyAnlage III

Anlage III BtMG²⁵²⁶

Listed in Appendix III of the Betäubungsmittelgesetz (Narcotics Act), meaning it is a controlled narcotic available for medical prescription.²⁷ Only licensed physicians, dentists, and veterinarians may prescribe oxycodone, and the federal government regulates prescriptions through reporting requirements.

NetherlandsPrescription onlyLijst I

List I (Opiumwet)²⁸

Classified as a List I substance under the Opium Act, designating it as a 'hard drug' associated with significant health risks. Despite this classification, physicians retain the ability to prescribe oxycodone for legitimate medical purposes under the Medicines Act.

PolandPrescription onlyNarcotic drug

Regulation of the Minister of Health on the list of psychotropic substances, narcotic drugs and new psychoactive substances³⁰

Oksykodon is included in Poland's official list of narcotic drugs. Its handling is controlled under the counteracting drug addiction framework.

SingaporePrescription onlyClass A

Class A (Misuse of Drugs Act)³¹³²

Listed as a Class A drug, attracting the most severe penalties under Singapore law. Unauthorized manufacture carries a minimum sentence of 10 years imprisonment plus 5 strokes of the cane, with maximum penalties of life imprisonment or 30 years plus 15 strokes. Trafficking offenses carry minimum penalties of 5 years imprisonment plus 5 strokes, and maximum penalties of 20 years plus 15 strokes.

SwitzerlandPrescription onlyVerzeichnis a

Verzeichnis A³⁵³⁶

Specifically named as a controlled substance under Verzeichnis A of Swiss narcotics legislation. Medicinal use is permitted with appropriate prescription.

United KingdomPrescription onlyClass A / Schedule 2

Class A / Schedule 2³⁹⁴⁰

Controlled under the Misuse of Drugs Act as a Class A substance, considered among those most likely to cause harm.⁴¹ Possession without prescription is punishable by up to seven years imprisonment, an unlimited fine, or both. Dealing carries penalties up to life imprisonment. Also listed as Schedule 2 under the Misuse of Drugs Regulations 2001, permitting medical prescription.⁴²

AustraliaPrescription onlySchedule 8

Schedule 8 (Poisons Standard) / Schedule I (Narcotic Drugs Act)¹⁸¹⁹

Listed in Schedule I of the Commonwealth's Narcotic Drugs Act 1967 pursuant to international treaty obligations.²⁰ Additionally classified as Schedule 8 under the Poisons Standard, designating it as a controlled drug available for medical use but requiring restriction of manufacture, supply, distribution, possession, and use to reduce potential for abuse and dependence.²¹

CanadaPrescription onlySchedule I

Schedule I (CDSA)²³

Controlled substance under Schedule I of the Controlled Drugs and Substances Act.²⁴ Note that Canadian scheduling differs significantly from the United States system. Possession and distribution without authorization carry criminal penalties.

Hong KongSchedule 1, Part I (Dangerous Drugs Ordinance)Citation needed

Regulated under Part I of Schedule 1 of Chapter 134, the Dangerous Drugs Ordinance. Unauthorized possession, manufacture, and trafficking are criminal offenses.

NorwayPrescription onlyN I

Forskrift om narkotika (narkotikaforskriften)²⁹

Oksykodon is on Norway's narcotics list as N I. It is regulated as a narcotic drug.

RussiaSchedule II

Classified as a Schedule II controlled substance under Russian narcotics legislation. Medical use is permitted under strict regulation.

SpainPrescription onlyEstupefaciente

Ley 17/1967 sobre estupefacientes³³³⁴

Oxicodona is an estupefaciente in Spain's official narcotics list. Narcotic medicines are prescribed and dispensed under the applicable special-control rules.

TurkeyPrescription onlyMadde 1

Uyuşturucu Maddelerin Murakabesi Hakkında Kanun (Law No. 2313)³⁷³⁸

Oxycodone is controlled in Turkey as Ökodal (Eugodal) under Law No. 2313, which has applied since its publication on 24 June 1933. Retail supply of controlled narcotic substances is confined to pharmacies and requires a prescription; unauthorized sale by a pharmacy is punishable under the Turkish Penal Code. Unauthorized manufacture, import, export, sale, supply, transport, storage, purchase, acceptance, or possession of a narcotic or stimulant substance is also punishable under Article 188 of the Penal Code.

References

Source Pages

Citations

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Oxycodone

Dihydrohydroxycodeinone

OxyContin, Roxicodone, Percocet, Percodan, Oxy

Psychoactive Class

Opioid Depressant Sedative

Chemical Class

Morphinan (substituted)