Oxycodone

Also known as

Roxicodone, oxycontin, oxecta, OxyIR, endone, oxynorm, OxyNEO, oxy, percocet, hillbilly heroin, OC, O, oxycotton, percs

Classification

Depressant, narcotic analgesic

Overview

Oxycodone is a semisynthetic derivative of codeine that acts as a narcotic analgesic more potent and addicting than codeine. An extended-release (ER) form of oxycodone (Xtampza ER) was approved for the management of daily, around-the-clock pain management in April, 2016 .

Medical usage

Oxycodone is available in combination with aspirin or acetaminophen to control pain and restless leg and Tourette syndromes. Used for the treatment of diarrhoea, pulmonary oedema and for the relief of moderate to moderately severe pain .

Street price

Between £9 and £10 .

Why take it?

Sought after effects

• euphoria,
• pain relief ,
• perceptions of less physical pain,
• euphoria,
• release of muscular tension,
• mental calm or relaxation .

Undesired effects

• nausea,
• constipation,
• CNS depression,
• drowsiness,
• sweating,
• dizziness,
• vomiting ,
• slowed or difficult breathing,
• confusion,
• alternating periods of sleep and consciousness .

Dosage

Abuse

Oral

• threshold 1 - 2.5 mgs,
• light 2.5 - 10 mgs,
• common 10 - 25 mgs,
• strong 25 - 40 mgs , .
• heavy 40 mg + .

Insufflated

• light 2.5 - 7.5 mg,
• common 7.5 - 15 mg,
• strong 15 - 25 mg .

How long do its effects last?

Onset of effects

• oral - 20 - 40 minutes .
• oral (immediate release) - 20 minutes,
• oral (extended release) - 40 minutes,
• insufflated - 2 - 5 minutes,
• intravenous - 0 - 1 minutes .

Duration of effects

• oral - 4 - 6 hours .
• oral (immediate release) - 4 - 6 hours,
• oral (extended release) - 6 - 8 hours,
• insufflated - 3 - 5 hours,
• intravenous - 3 - 5 hours .

After-effects

• oral (immediate release) - 1 - 24 hours,
• oral (extended release) - 1 - 24 hours,
• insufflated - 1 - 24 hours,
• intravenous - 1 - 24 hours .

Pharmacology

Pharmacodynamics

Oxycodone, a semisynthetic opiate agonist derived from the opioid alkaloid, thebaine, is similar to other phenanthrene derivatives such as hydrocodone and morphine .

Absorption

Well absorbed with an oral bioavailability of 60% to 87% .

Metabolism

Hepatic .

Half-life

Four and a half hours .

Elimination

Oxycodone and its metabolites are excreted primarily via the kidney .

Lethal dosage

LD50 3.0638 mol/kg in rats .

Mechanism of action

Oxycodone acts as a weak agonist at mu, kappa, and delta opioid receptors within the CNS. Oxycodone primarily affects mu-type opioid receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as oxycodone also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability .

Mode of use

Oxycodone is usually swallowed but is sometimes injected or used as a suppository .

Signs of usage

• constipation,
• nausea,
• sedation,
• dizziness,
• vomiting,
• headache,
• dry mouth,
• sweating,
• mood changes,
• flushing,
• loss of appetite,
• weakness .

Effects

Short-term effects

• euphoria,
• extreme relaxation,
• reduced anxiety,
• pain relief,
• sedation .

Long-term effects

• dental problems,
• swelling in the arms and legs,
• mood swings
• reduced sex drive and decreased level of testosterone (males) and menstrual problems (females),
• needing to use more to get the same effect,
• financial, work or social problems .

Physical effects

• physical euphoria,
• pupil constriction,
• skin flushing,
• appetite suppression,
• cough suppression,
• orgasm suppression,
• pain relief,
• respiratory depression,
• sedation,
• constipation,
• difficulty urinating,
• increased perspiration,
• itchiness,
• nausea,
• stomach cramps .

Cognitive effects

• cognitive euphoria,
• compulsive redosing,
• dream potentiation,
• anxiety suppression,
• decreased libido .

Visual effects

• internal hallucinations .

Insufflated abuse

• burning feeling inside of the nose,
• dry mouth,
• constriction of the pupils,
• tightness of the chest,
• closing of the nostrils, causing one to be unable to breathe through his or her nose,
• severe headache,
• shaking / tremors,
• slurred speech,
• restlessness,
• irritability and agitation,
• drowsiness .

Positive

• euphoria,
• pain relief .

Neutral

• itching .

Negative

• nausea,
• constipation,
• CNS depression,
• drowsiness,
• sweating,
• dizziness,
• vomiting .

Side-effects

• nausea,
• vomiting,
• loss of appetite,
• dry mouth,
• constipation,
• dizziness,
• stomach pain,
• drowsiness,
• flushing,
• sweating,
• weakness,
• headache,
• mood changes .

Overdose

• chest pain or discomfort,
• decreased awareness or responsiveness,
• extreme drowsiness and loss of consciousness,
• no muscle tone or movement,
• slow or irregular heartbeat ,
• constricted pupils non-reactive to light,
• periods of extreme sedation difficult to wake,
• lack of responsiveness (even to painful stimuli),
• respiratory arrest,
• cyanosis ,
• difficulty breathing,
• slowed or stopped breathing,
• dizziness,
• fainting,
• cold, clammy skin,
• loss of consciousness or coma .

Risks

Injection

• harms from injecting tablet particles that can lodge in blood vessels and small capillaries in the lungs
• risks of blood-borne viral infections if injection equipment is shared,
• harms related to injection of non-sterile preparations not intended for injection,
• risks of polydrug use,
• harm related to pre-existing conditions for which opioids may be contra-indicated .

Snorting oxycodone increases the risk of overdose

Because snorting this substance causes an individual's bloodstream to absorb greater amounts of the drug than it would when taken orally, it puts the user at a much higher risk of overdosing.

This is especially true when users snort crushed extended release tablets of Oxycodone because, as the nature of the drug is to provide long-lasting relief and therefore has a higher potency, people are forcing the drug to cross the blood-brain barrier all at one time instead of allowing it to work as it is designed to in providing extended relief. This sudden rush of Oxycodone entering the bloodstream can cause a person's body to exceed its limit of tolerance and result in overdose.

However, even when snorting a small dose of Oxycodone, there are a host of possible physical side-effects that one can experience, please see Insufflated abuse above .

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, GBL / GHB, 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 .

Dangerous

• 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.
• MXE - This combination can potentiate the effects of the opioid.
• 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.
• Cocaine - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
• 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.
• GBL / GHB - 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.
• 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
• 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 .

Caution

• PCP - PCP can reduce opioid tolerance, increasing the risk of overdose.
• Nitrous oxide - 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.
• Amphetamines - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
• 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, diarrhoea, hypertension, tachycardia, seizures, and coma. Death has occurred in some cases .

Withdrawal

Symptoms usually last for approximately one week and can include -

• watering eyes,
• runny nose,
• uncontrollable yawning,
• difficulty sleeping and severe restlessness,
• hot and cold flushes,
• pains in muscles and joints,
• muscle spasms and tremors,
• loss of appetite,
• nausea,
• vomiting,
• increased heart rate and blood pressure,
• uncontrolled kicking movements , ,
• rebound pain,
• increased pain sensitivity,
• appetite changes,
• diarrhoea,
• diaphoresis,
• feeling cold and shivering .

Drug testing

How long does oxycodone stay in the urine?

Oxycodone is detectable in a urine test for 3 - 4 days .

How long can oxycodone be detected in blood?

A blood test will detect Oxycodone for up to 24 hours .

How long can a saliva test detect oxycodone?

A saliva test will detect Oxycodone from 1 - 4 days .

How long can a hair test detect oxycodone?

Oxycodone, like many other drugs, can be detected with a hair follicle drug test for up to 90 days .

Mixing with other drugs

• Oxycodone + alcohol - increased confusion and clumsiness, and breathing difficulties.
• Oxycodone + some antidepressants (monoamine oxidase inhibitors - MAOIs) - delirium, convulsions, respiratory failure, coma and death .

Harm reduction

To prevent OxyContin tablets being injected by people who misuse them, they were reformulated in April, 2014. The tablets are now resistant to crushing and become a thick gel when added to water. They also have controlled release properties, even as a gel .

Statistics

• nearly 60 million prescriptions for oxycodone-containing drugs were written in 2013,
• in 2012, 16 million people reported abusing oxycodone in their lifetime, which is an increase of more than a million individuals compared with the previous year,
• in 2011, oxycodone was responsible for more than 150,000 emergency room visits,
• in 2009, law enforcement documented more oxycodone-related infractions than any other prescription drug .

History

The potential dangers of oxycodone can be traced as far back as the 1960's when the United Nations Office on Drugs and Crime classified it as a dangerous drug as part of The Dangerous Drugs (Amendment) Ordinance, 1960. Abuse in the United States has been a continuing problem since the early 1960's, prompting the United States Government to classify it as a Schedule II drug. Until 1995, when the FDA approved OxyContin there was little concern over the abuse of oxycodone producers. But, in 1996 when the manufacturer of OxyContin began to market and distribute the drug, concerns and reports of illicit use and abuse began to increase . At first, drug abuse treatment centers, law enforcement personnel, and pharmacists in Maine, Virginia, West Virginia, Ohio, Kentucky, and Maryland reported increases in the abuse of OxyContin. Now, abuse of the drug has expanded throughout the United States , .

Patented in Germany in 1916, Oxycodone has been in use for just shy of a century. It is likely that it was discovered around the same time Germany was researching opioid analgesics, with the goal of finding a cost effective, synthetically assisted/tweaked to address the imperfections of the contemporary opioid analgesics, which were limited essentially to the naturally occurring alkaloids of papaver somniferum, so until the 1900's, you were lucky to get either codeine, morphine (most likely), or heroin (heroin was at that time marketed as a less-addicting version of morphine, very similar marketing techniques / omissions of truth that can be seen today and throughout history in the Pharmaceutical Industry).

In 1995, Purdue Pharmaceuticals introduced OxyContin, marketing it as a miracle drug, a less addictive pain killer that was often better tolerated in terms of side-effects compared to common alternatives such as morphine sulphate (a drug so old that even Big Pharma has trouble patenting it, so they look to the trees ..... i.e. Evergreening) add in their time-released version of oxycodone, and boom, the results are a nearly 100 year old drug, but with their controlled release CR technology, they've been granted patent after patent, making it expensive and allowing for record-breaking revenue/profit for Purdue and the consequent pharmaceutical companies that jumped on the bandwagon, releasing generic versions, some in violation of Purdue's patent, which inevitably lead to the re-structuring of the oxycodone industry as Purdue's death grip on their #1 money maker Oxycodone choked out the competition and re-introduced OxyContin in the 2010's, reformulated with the OP imprint and an abuse-deterrent system .

Timeline

• 1916 - Oxycodone is created.
• 1939 - Oxycodone is first introduced to America.
• 1950 - Percodan - a combination of oxycodone and aspirin - is released to American doctors for prescription.
• 1963 - The attorney general of California cites Percodan abuse as the source of one-third of all drug addiction in the state.
• 1970 - Oxycodone is listed as a Schedule II drug in the new Controlled Substances Act. According to the DEA - Schedule II drugs, substances, or chemicals are defined as drugs with a high potential for abuse, less abuse potential than Schedule I drugs, with use potentially leading to severe psychological or physical dependence. These drugs are also considered dangerous.
• 1974 - Percocet is approved by the FDA.
• 1989 - The Texas Medical Board adopts language to support wider use of painkillers by doctors. Fourteen states follow in its footsteps.
• 1996 - Perdue Pharma releases OxyContin .

---