Oxycodone

Death may occur when opiates are combined with depressants such as benzodiazepines, alcohol or other GABAergic substances. Taking large amounts of these substances together is strongly discouraged.

Oxycodone
The skeletal formula of oxycodone
Chemical Nomenclature
Common names	Oxycodone
Substitutive name	OxyContin, Oxy, Roxicodone, Oxecta, OxyIR, Endone, Oxynorm
Systematic name	(5R,9R,13S,14S)-4,5α-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one
Class Membership
Psychoactive class	Depressant
Chemical class	Opioid
Routes of Administration
Oral Dosage WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. DISCLAIMER: PW's dosage information is a summary of data gathered from users and resources. It is not a recommendation and should be verified with other sources for accuracy. The below dosage assumes no tolerance. Threshold 2.5 - 5 mg Light 5 - 10 mg Common 10 - 30 mg Strong 30 - 40 mg Heavy 40+ "+" can not be assigned to a declared number type with value 40. mg (Heavy doses may make the user feel sick and nauseous) Duration Total 4 - 6 hours Onset 20 - 40 minutes

Summary sheet: Oxycodone

Oxycodone (Oxycontin) is a semi-synthetic opioid synthesized from poppy-derived thebaine. It is a narcotic analgesic 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.

Chemistry

Oxycodone, or dihydrohydroxycodeinone, 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 which suggests that it is pharmacologically similar to more traditional opioids such as codiene and morphine. These all appear to mimic endogenous endorphins. Endorphins are responsible for analgesia (reducing pain), causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or excitement. This mimicking of natural endorphins results in the drug's euphoric, analgesic (pain relief), and anxiolytic (anti-anxiety) effects.

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.

Metabolism

In humans, Oxycodone is metabolized to oxycodol; oxymorphone, then oxymorphol and noroxymorphone; and noroxycodone, then noroxycodol and noroxymorphone.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

The general head space of codeine is described by many as one of intense euphoria, relaxation, anxiety suppression and pain relief.

• 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 blissful euphoria.
• 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.
• Itchiness
• Constipation
• Cough suppression
• Difficulty urinating
• Nausea
• Stomach cramps
• Pupil constriction

Cognitive effects

• Euphoria - This seems to be caused by both u 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 feeling of emotional bliss, contentment, and happiness.
• Anxiety suppression

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.

Toxicity and harm potential

Like most opioids, unadulterated oxycodone does not seem to cause many long-term complications other than dependence and constipation. In fact outside of the extremely powerful addiction and physical dependence the harmful or toxic aspects of opioid usage are exclusively associated with not taking appropriate precautions in regards to its administration, overdosing and using impure products.

It should also be noted that since opioids can cause nausea and vomiting, a significant number of deaths attributed to overdose are caused by aspiration of vomit by an unconscious victim. This is when an unconscious or semiconscious user who is lying on their back vomits into their mouth and unknowingly suffocates as a result. It can be prevented by ensuring that one is laying on their side with their head tilted downwards so that one's airways cannot be blocked in the event of vomiting whilst unconscious.

Lethal dosage

The lethal dosage at which oxycodone is likely to cause overdose due to respiratory depression is unknown. It seems to differ between individuals based on tolerance and personal metabolism and it's because of this that one is recommended to start off with a lighter dosage and work their way up in order to ensure personal safety.

It is strongly recommended that one use harm reduction practices when using this drug.

Tolerance and addiction potential

As with other opiate-based painkillers, chronic use of oxycodone can be considered as extremely addictive and is capable of causing both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage.

Tolerance to many of the effects of oxycodone develops with prolonged use, including therapeutic effects. This results in users having to administer increasingly large doses to achieve the same effects. 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.

Interactions

Opioids are dangerous to use in combination other depressants as many fatalities reported as overdoses are in fact caused by interactions with other depressant drugs such as alcohol or benzodiazepines resulting in dangerously high levels of respiratory depression.

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. 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".
• 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.

See also

• Responsible use
• Oxycodone (Wikipedia)
• Oxycodone (Erowid)
• Extraction of opioids from painkiller products
• Depressants
• Codeine
• Kratom