Oxycodone

 

• 1Introduction to oxycodone
• 2Using oxycodone
  • 2.1Ways of administration
  • 2.2Effects of oxycodone
  • 2.3Combinations with oxycodone
• 3Pharmacology of oxycodone
• 4The dangers of oxycodone
• 5Producing oxycodone
• 6Forms of oxycodone
• 7Legal status of oxycodone
  • 7.1Canada
  • 7.2USA
  • 7.3EU
• 8History of oxycodone
• 9More oxycodone Sections
• 10The latest oxycodone threads
• 11References

[top]Introduction to oxycodone

Oxycodone is an opioid derived from thebaine, an alkaloid in opium. It is about twice as effective in treating analgesia as morphine. Like other opioids, it has analgesic, sedative, and anxyiolitic properties. Recreational users usually consume oxycodone for its euphoric effects characteristic of other opiates/opioids. It is used commonly for the treatment of moderate to severe pain. Oxycodone was first synthesized in 1916, approved by the FDA in 1995.

[top]Using oxycodone

Oxycodone is commonly prescribed for analgesia, ie post-operation, chronic back pain, etc. It is also used recreationally for its relaxing and euphoric properties.

[top]Ways of administration

Oxycodone is most commonly taken orally. Unlike many other drugs (specifically opioids), it has a relatively high oral bioavailability (60-80%) due to low first pass metabolism. It is also less commonly administered intravenously, sublingually, rectally, or insufflated.
Here are some threads on injecting oxycodone:
Injecting Basics
HOWTO: Inject plain oxycodone, fast acting type (not oxycontin & not percocet)
Extracting oxycodone from generic oxycontin for injectable use

[top]Effects of oxycodone

Effects of oxycodone include: analgesia, anxiolysis, sedation, euphoria, miosis (pupil constriction), nausea, dizziness, itching, dry mouth, sexual dynsfunction, and respiratory depression. Adverse effects usually increase as dose increases.

[top]Combinations with oxycodone

Oxycodone is potentiated/potentiates other opiates/opioids, benzodiazepines, alcohol, and other central nervous system depressants. It is not a good idea to combine CNS depressants. The risk of respiratory depression increases and can be fatal if care is not taken to keep oneself safe. Oxycodone may potentiate effects of tricyclic antidepressants. Combining with MAOI's may increase risk of severe hypotension. There is an increased risk of serotonin syndrome when combined with serotonergic drugs. Always have experience with two or more drugs before attempting their combinations, as usually a smaller dose is required and effects can be a bit different.

Oxycodone and cocaine: oxycodone promotes dopamine release, while cocaine blocks its reuptake, therefore the combination is synergistic. Euphoria is increased (euphoria associated with oxycodone is a result of increased concentrations of dopamine). Sedative properties of oxycodone might be attenuated/completely cancelled out. A lower dose of each might be needed. Some relevant experiences and information are available in the thread Oxycodone and Cocaine.

Oxycodone and other stimulants: Other stimulants such as amphetamine work differently than cocaine but the end result is increased concentrations of dopamine. Coupled with oxycodone's heightened release of dopamine, this combination will also produce greater euphoria and stimulation. A lower dose of each might be needed. Stimulation from stimulants can overpower the sedation caused by oxycodone, but this is dose-dependent.

Oxycodone and alcohol: This is a dangerous combination. Risk of severe respiratory depression is increased, however the combination has been anecdotally championed as enjoyable. Sedation, relaxation, will be increased. Higher doses might induce nausea. Smaller doses of each are mandatory.

Oxycodone and benzodiazepines: Like with alcohol, risk of respiratory depression is increased. Sedation, relaxation will be increased. Smaller doses of each are mandatory.

[top]Pharmacology of oxycodone

Oxycodone, like many other opioids, is a mu, k, and d-opioid receptor agonist. Binding of oxycodone to its receptors, which are G-coupled, causes hyperpolarization of its cells. Adenylyl cyclase system is inhibited, and cyclic AMP is decreased. GABA release is increased. Oxycodone's affinity and subsequent binding to kappa and mu-opioid receptors is responsible for its antinociceptive effects. Oxycodones affinity for these receptors is 1/10 to 1/40th that of morphine.

Pharmacokinetics: Oxycodone's structure allows it to avoid serious first-pass metabolism. In the liver, oxycodone is metabolized to its more potent metabolite, oxymorphone (about 11% of dose), by O-demethylation mediated by CYP3A, and to noroxycodone and noroxymorphone (about 45% of dose) by N-demethylation mediated by CYP2D6. Poor CYP2D6 metabolizers (4-10% of Caucasians) might experience less effects from oxycodone.

Relevant data-
Half life: 3-6 hours
Bioavailability: 60-87% orally, 61.6% +/- 30.2% rectally, 46% intranasally, 45.4% +/- 20.1% sublingual
Time to maximum serum concentrations: 1 hour

[top]The dangers of oxycodone

Oxycodone is a relatively safe drug. Immediate dangers associated with oxycodone, especially when combined with other drugs, are the risk of nausea, oversedation, respiratory depression, other breathing problems. Generally at recreational/common analgesic doses, these dangers are minimal. Continued use can lead to addiction, which is dose- and frequency-dependent.

[top]Producing oxycodone

[top]Forms of oxycodone

There is some confusion about oxycodone and the brand name drugs such as Roxicodone and OxyContin.

OxyContin vs Roxicodone vs Oxycodone

There is a lot of confusion about OxyContin particularly, one can assume this is because the name is so similar to oxycodone. OxyContin is not a drug, it is a brand name for a preparation of oxycodone. Oxycodone is the active chemical in OxyContin, the rest is fillers (otherwise some pills would be tiny), binders, or substances which create the time-release mechanism. The same goes for Roxicodone, and other common preparations. Some preparations, such as Percocet, also contain acetaminophen to prevent abuse or supposedly to contribute to pain relief, although if one is on prescription painkillers it is likely that acetaminophen is not strong enough to treat the pain one is experiencing.

IR vs CR

OxyIR is oxycodone hydrochloride and fillers/binders. It is designed for acute treatment of pain, and is an immediate release formulation, meaning as soon as it is ingested it goes to work. OxyContin is designed for longer lasting analgesia, releasing the drug over a period of about 12 hours. It contains an outer colored coating, which, contrary to popular belief, is not the time release mechanism. The colored coating is just a system so that ingredients can be easily recognized. The time release mechanism is a wax matrix inside which "suspends" the oxycodone. Even after removing the coating, the pill must be crushed to defeat the mechanism to make it suitable for insufflation or injecting.

Oxycodone comes in a variety of forms:
OxyIR (oxycodone hydrochloride): 5 mg, 10 mg, 20 mg (Canada)
OxyContin (oxycodone hydrochloride and time release mechanism): 5 mg (blue, only available in Canada and the UK), 10 mg (white, Canada, US, UK), 15 mg (grey, US), 20 mg (pink, Canada, US, UK), 30 mg (brown, US), 40 mg (tan, Canada, US, UK), 60 mg (red, US), and 80 mg (green, Canada, US, UK), 160 mg used to be available but was taken off shelves due to a few accidental deaths and because of "diversion" problems.
Roxicodone (generic oxycodone hydrochloride): 5 mg (white, recently ceased), 15 mg (green), 30 mg (blue); 5mg/5ml oral solution; 20mg/ml concentrate
Percocet (oxycodone hydrochloride/acetaminophen, Canada and US): 2.5 mg/325 mg (pink oval), 5 mg/325 mg (blue round), 7.5 mg/325 mg (peach oval), 7.5mg/500 mg (peach capsule-shaped), 10 mg/325 mg (yellow capsule-shaped), 10 mg/650 mg (yellow oval), 10 mg/1000 mg (blue oval)
Percodan (oxycodone hydrochloride/aspirin, US only): 5 mg/325 mg
OxyNorm (oxycodone hydrochloride solution): 5, 10, or 20 mg capsules; 5 mg/5 ml, 250 ml bottles (Australia, NZ, UK), 10mg/ml and 50mg/ml injection solution (NZ, UK)
Depalgos (oxycodone hydrochloride/acetaminophen, Italy): 5 (yellow), 10 (pink), and 20 (red) mg/325 mg

[top]Legal status of oxycodone

[top]Canada

Oxycodone is Schedule I in Canada. Schedules in Canada are much different than those in the USA.

[top]USA

Oxycodone is Schedule II in the United States. This means it is illegal to sell without a DEA license and illegal to buy or possess without a license or prescription.

[top]EU

Oxycodone is Schedule II/Class A in the U.K., making it illegal to buy or possess without a prescription.

[top]History of oxycodone

[top]More oxycodone Sections

Oxycodone Experiences Post & read experiences with oxycodone.

[top]The latest oxycodone threads

 

 

Oxycodone File Archive Upload and read research & articles on oxycodone.

Opioids/Opiates Forum Post and read about oxycodone.

Oxycodone Image Gallery Post and view pictures of oxycodone.

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Category: Opioids
Opiates
Opium

[top]References

http://www.drugs.com/oxycodone.html
http://www.erowid.org/pharms/oxycodone/oxycodone_effects.shtml
http://www.mims.com/Page.aspx?menuid=mng&name=oxycodone#Indications
http://therapistunlimited.com/index/Articles/Substance+Abuse/Oxycodone/the+history+of+oxycodone
http://www.purduepharma.com/PI/Prescription/Oxycontin.pdf
http://www.drugs-forum.com/forum/local_links.php?action=ratelink&catid=24&linkid=46 15
http://www.drugs-forum.com/forum/local_links.php?action=ratelink&catid=24&linkid=73 07
http://www.drugs-forum.com/forum/local_links.php?action=ratelink&catid=138&linkid=8 357
http://www.drugs-forum.com/forum/local_links.php?action=ratelink&catid=138&linkid=8 356