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Details

Stereochemistry ABSOLUTE
Molecular Formula C18H21NO4.H3O4P
Molecular Weight 413.3588
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of OXYCODONE PHOSPHATE

SMILES

OP(O)(O)=O.COC1=C2O[C@H]3C(=O)CC[C@@]4(O)[C@H]5CC(C=C1)=C2[C@@]34CCN5C

InChI

InChIKey=TZKVACZYAHJHRA-RKXJKUSZSA-N
InChI=1S/C18H21NO4.H3O4P/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;1-5(2,3)4/h3-4,13,16,21H,5-9H2,1-2H3;(H3,1,2,3,4)/t13-,16+,17+,18-;/m1./s1

HIDE SMILES / InChI

Molecular Formula C18H21NO4
Molecular Weight 315.3636
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 4 / 4
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula H3O4P
Molecular Weight 97.9952
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including http://reference.medscape.com/drug/oxycontin-xtampza-er-oxycodone-343321 | https://www.ncbi.nlm.nih.gov/pubmed/23880538 | https://www.drugs.com/oxycodone.html

Oxycodone is a semisynthetic opioid used for the management of acute and chronic pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Oxycodone is a highly selective full agonist of the μ-opioid receptor (MOR), with low affinity for the δ-opioid receptor (DOR) and κ-opioid receptor (KOR). 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. After a dose of conventional (instant-release) oral oxycodone, the onset of action is 10–30 minutes, and peak plasma levels of the drug are attained within roughly 30–60 minutes in contrast, after a dose of OxyContin (an oral controlled-release formulation), peak plasma levels of oxycodone occur in about three hours. The duration of instant-release oxycodone is 3 to 6 hours, although this can be variable depending on the individual. Oxycodone in the blood is distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, and brain. Serious side effects of oxycodone include reduced sensitivity to pain (beyond the pain the drug is taken to reduce), euphoria, anxiolysis, feelings of relaxation, and respiratory depression. Common side effects of oxycodone include constipation (23%), nausea (23%), vomiting (12%), somnolence (23%), dizziness (13%), itching (13%), dry mouth (6%), and sweating (5%).

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
500.0 nM [EC50]
16000.0 nM [EC50]
4000.0 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
PERCODAN-DEMI

Approved Use

OxyContin Tablets are a controlled-release oral formulation of oxycodone hydrochloride indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. OxyContin is NOT intended for use as a prn analgesic. Physicians should individualize treatment in every case, initiating therapy at the appropriate point along a progression from non-opioid analgesics, such as non-steroidal anti-inflammatory drugs and acetaminophen to opioids in a plan of pain management such as outlined by the World Health Organization, the Agency for Healthcare Research and Quality (formerly known as the Agency for HealthCare Policy and Research), the Federation of State Medical Boards Model Guidelines, or the American Pain Society. OxyContin is not indicated for pain in the immediate postoperative period (the first 12-24 hours following surgery), or if the pain is mild, or not expected to persist for an extended period of time. OxyContin is only indicated for postoperative use if the patient is already receiving the drug prior to surgery or if the postoperative pain is expected to be moderate to severe and persist for an extended period of time. Physicians should individualize treatment, moving from parenteral to oral analgesics as appropriate. (See American Pain Society guidelines.)

Launch Date

1950
Primary
PERCODAN-DEMI

Approved Use

OxyContin Tablets are a controlled-release oral formulation of oxycodone hydrochloride indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. OxyContin is NOT intended for use as a prn analgesic. Physicians should individualize treatment in every case, initiating therapy at the appropriate point along a progression from non-opioid analgesics, such as non-steroidal anti-inflammatory drugs and acetaminophen to opioids in a plan of pain management such as outlined by the World Health Organization, the Agency for Healthcare Research and Quality (formerly known as the Agency for HealthCare Policy and Research), the Federation of State Medical Boards Model Guidelines, or the American Pain Society. OxyContin is not indicated for pain in the immediate postoperative period (the first 12-24 hours following surgery), or if the pain is mild, or not expected to persist for an extended period of time. OxyContin is only indicated for postoperative use if the patient is already receiving the drug prior to surgery or if the postoperative pain is expected to be moderate to severe and persist for an extended period of time. Physicians should individualize treatment, moving from parenteral to oral analgesics as appropriate. (See American Pain Society guidelines.)

Launch Date

1950
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
22.2 ng/mL
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
39.3 ng/mL
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
19 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: FASTED
17.7 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: FED
15.7 ng/mL
5 mg 4 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
12.9 ng/mL
3.33 mg 6 times / day steady-state, oral
dose: 3.33 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
128.2 ng × h/mL
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
268.2 ng × h/mL
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
105 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: FASTED
133 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: FED
113.3 ng × h/mL
5 mg 4 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
99 ng × h/mL
3.33 mg 6 times / day steady-state, oral
dose: 3.33 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.55 h
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3.85 h
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2.9 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: FASTED
3.3 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
55%
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
55%
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
55%
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: FASTED
55%
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: FED
55%
5 mg 4 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
55%
3.33 mg 6 times / day steady-state, oral
dose: 3.33 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OXYCODONE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
30 mg 1 times / day single, oral
Studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: single
Dose: 30 mg, 1 times / day
Sources:
healthy, 30 years
Health Status: healthy
Age Group: 30 years
Sex: M
Sources:
Other AEs: Pulmonary edema...
Other AEs:
Pulmonary edema
Sources:
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Disc. AE: Nausea, Dizziness...
AEs leading to
discontinuation/dose reduction:
Nausea (grade 1-2, 1.7%)
Dizziness (grade 1-2, 1.7%)
Abdominal pain (grade 1-2, 0.8%)
Sources:
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Disc. AE: Headache, Vomiting...
AEs leading to
discontinuation/dose reduction:
Headache (grade 1-2, 0.8%)
Vomiting (grade 1-2, 0.8%)
Nausea (grade 1-2, 0.8%)
Somnolence (grade 1-2, 0.8%)
Sources:
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Disc. AE: Nausea, Dizziness...
AEs leading to
discontinuation/dose reduction:
Nausea (grade 1-2, 6.3%)
Dizziness (grade 1-2, 4.8%)
Confusion (grade 1-2, 3.2%)
Sources:
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Disc. AE: Vomiting, Flu syndrome...
AEs leading to
discontinuation/dose reduction:
Vomiting (grade 1-2, 0.8%)
Flu syndrome (grade 1-2, 0.8%)
Confusion (grade 1-2, 0.8%)
Fatigue (grade 1-2, 0.8%)
Sources:
6 mg 2 times / day single, oral
Studied dose
Dose: 6 mg, 2 times / day
Route: oral
Route: single
Dose: 6 mg, 2 times / day
Sources:
healthy, mean age 33 years
Disc. AE: Vomiting...
15 mg 1 times / day single, oral
Studied dose
Dose: 15 mg, 1 times / day
Route: oral
Route: single
Dose: 15 mg, 1 times / day
Sources:
healthy, mean age 36 years
Health Status: healthy
Age Group: mean age 36 years
Sex: M+F
Sources:
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (2.5%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Pulmonary edema
30 mg 1 times / day single, oral
Studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: single
Dose: 30 mg, 1 times / day
Sources:
healthy, 30 years
Health Status: healthy
Age Group: 30 years
Sex: M
Sources:
Abdominal pain grade 1-2, 0.8%
Disc. AE
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Dizziness grade 1-2, 1.7%
Disc. AE
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 1-2, 1.7%
Disc. AE
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Headache grade 1-2, 0.8%
Disc. AE
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 1-2, 0.8%
Disc. AE
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Somnolence grade 1-2, 0.8%
Disc. AE
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 1-2, 0.8%
Disc. AE
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Confusion grade 1-2, 3.2%
Disc. AE
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Dizziness grade 1-2, 4.8%
Disc. AE
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 1-2, 6.3%
Disc. AE
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Confusion grade 1-2, 0.8%
Disc. AE
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Fatigue grade 1-2, 0.8%
Disc. AE
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Flu syndrome grade 1-2, 0.8%
Disc. AE
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 1-2, 0.8%
Disc. AE
5 mg 4 times / day multiple, oral
Recommended
Dose: 5 mg, 4 times / day
Route: oral
Route: multiple
Dose: 5 mg, 4 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting 11.4%
Disc. AE
6 mg 2 times / day single, oral
Studied dose
Dose: 6 mg, 2 times / day
Route: oral
Route: single
Dose: 6 mg, 2 times / day
Sources:
healthy, mean age 33 years
Vomiting 2.5%
Disc. AE
15 mg 1 times / day single, oral
Studied dose
Dose: 15 mg, 1 times / day
Route: oral
Route: single
Dose: 15 mg, 1 times / day
Sources:
healthy, mean age 36 years
Health Status: healthy
Age Group: mean age 36 years
Sex: M+F
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



OverviewOther

Other InhibitorOther SubstrateOther Inducer







Drug as perpetrator​

Drug as perpetrator​

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
minor
yes
yes
yes
yes (co-administration study)
Comment: When both oxidative pathways of the metabolism of oxycodone were inhibited with paroxetine and itraconazole (CYP3A4 AND CYP2D6 inhibitors), the mean AUC(0,∞) of oxycodone increased by 2.9-fold (P < 0.001), and its Cmax by 1.8-fold (P < 0.001).
Page: 7.0
yes
yes (co-administration study)
Comment: When both oxidative pathways of the metabolism of oxycodone were inhibited with paroxetine and itraconazole (CYP3A4 AND CYP2D6 inhibitors), the mean AUC(0,∞) of oxycodone increased by 2.9-fold (P < 0.001), and its Cmax by 1.8-fold (P < 0.001).
Tox targets
PubMed

PubMed

TitleDatePubMed
Equianalgesic dose ratios for opioids. a critical review and proposals for long-term dosing.
2001 Aug
Time-release analgesic drug causes fatal overdoses in United States.
2001 Aug
A curse and a cure. Is the crackdown on an abused drug causing needless suffering?
2001 Aug 6
Opioid analgesic prescribing and use - an audit of analgesic prescribing by general practitioners and The Multidisciplinary Pain Centre at Royal Brisbane Hospital.
2001 Dec
On the frontlines of old battles.
2001 Jul
Addressing OxyContin abuse.
2001 Jul-Aug
Prescription for addiction?
2001 Mar
Narcotic analgesics for dental pain: available products, strengths, and formulations.
2001 Mar-Apr
The use of oxycodone in cancer-related pain: a literature review.
2001 Nov
Clinical case study.
2001 Nov-Dec
Acetaminophen, aspirin, or Ibuprofen in combination analgesic products.
2001 Nov-Dec
Opioid therapy for chronic painful conditions.
2001 Oct
States respond to growing abuse of painkiller.
2001 Oct-Nov
Controlled-release oxycodone hydrochloride (OxyContin).
2001 Sep
Managing postoperative pain.
2001 Sep
Interscalene brachial plexus block with continuous intraarticular infusion of ropivacaine.
2001 Sep
Valdecoxib.
2002
Hydromorphone for acute and chronic pain.
2002
The simultaneous determination of codeine, morphine, hydrocodone, hydromorphone, 6-acetylmorphine, and oxycodone in hair and oral fluid.
2002 Apr
Capillary electrophoresis and capillary electrophoresis-ion trap multiple-stage mass spectrometry for the differentiation and identification of oxycodone and its major metabolites in human urine.
2002 Apr 25
More blame and praise for a pain drug.
2002 Apr 29
Minimal interaction between gatifloxacin and oxycodone.
2002 Aug
The influence of anaesthesia and surgery on the circadian rhythm of melatonin.
2002 Jan
Combination hydrocodone and ibuprofen versus combination oxycodone and acetaminophen in the treatment of moderate or severe acute low back pain.
2002 Jan
Recovery after tonsillectomy in adults: a three-week follow-up study.
2002 Jan
Perioperative management in children with sickle cell disease undergoing laparoscopic surgery.
2002 Jan-Mar
Gateways to clinical trials.
2002 Jul-Aug
OxyContin and neonatal abstinence syndrome.
2002 Jun
An evaluation of the efficacy and tolerability of oral tramadol hydrochloride tablets for the treatment of postsurgical pain in children.
2002 Jun
Comparison of the opioid-sparing efficacy of diclofenac and ketoprofen for 3 days after knee arthroplasty.
2002 Mar
There is no accounting for accountability.
2002 Mar
Validity and reliability of three commercially available breath-by-breath respiratory systems.
2002 Mar
Pain management after major orthopaedic surgery: current strategies and new concepts.
2002 Mar-Apr
OxyContin Use and Abuse.
2002 Mar-Apr
The analgesic efficacy of valdecoxib vs. oxycodone/acetaminophen after oral surgery.
2002 May
Preoperative administration of controlled-release oxycodone for the management of pain after ambulatory laparoscopic tubal ligation surgery.
2002 May
Oral ondansetron, tropisetron or metoclopramide to prevent postoperative nausea and vomiting: a comparison in high-risk patients undergoing thyroid or parathyroid surgery.
2002 May
Sevoflurane versus halothane: effect of oxycodone premedication on emergence behaviour in children.
2002 May
Venous malformations associated with central pain: report of a case.
2002 Nov
Synergy between mu opioid ligands: evidence for functional interactions among mu opioid receptor subtypes.
2002 Nov
Simultaneous quantitation of opioids in blood by GC-EI-MS analysis following deproteination, detautomerization of keto analytes, solid-phase extraction, and trimethylsilyl derivatization.
2002 Oct
Detection of cocaine analytes and opiates in nails from postmortem cases.
2002 Oct
Oxycontin: the concept of a "ghost pill" and the postmortem tissue distribution of oxycodone in 36 cases.
2002 Oct
Pharmacogenomics as molecular autopsy for postmortem forensic toxicology: genotyping cytochrome P450 2D6 for oxycodone cases.
2002 Oct
Determination of 6-oxo-morphinans, as the oximes, by difference circular dichroism spectroscopy.
2002 Oct
Propacetamol as adjunctive treatment for postoperative pain after cardiac surgery.
2002 Oct
Induced hypothermia for drug overdose.
2002 Sep
[Pain therapy in rheumatic diseases. Oxycodon is not a weak opioid].
2002 Sep 12
Paravertebral somatic nerve block compared with peripheral nerve blocks for outpatient inguinal herniorrhaphy.
2002 Sep-Oct
Review: tricyclic antidepressants, capsaicin, gabapentin, and oxycodone are effective for postherpetic neuralgia.
2002 Sep-Oct
Patents

Sample Use Guides

For opioid naïve patients, initiate treatment with 5 mg to 15 mg every 4 to 6 hours as needed for pain.
Route of Administration: Oral
Human embryonic kidney (HEK)-293 were used for activity evaluation. Receptor G protein-mediated responses were determined by measuring changes in cAMP using the cAMP–homogenous timeresolved fluorescence kit (Cisbio, Codolet, France). MOR, KOR, DOR all couple to Gai so G protein coupling was measured as inhibition of forskolin-stimulated cAMP accumulation in the presence of 1.5 mkM NKH-477 (water-soluble forskolin, Tocris catalog #1603) and 500 mkM 3-isobutyl-1-methylxanthine (IBMX). cAMP accumulation assays were run in parallel with b-arrestin-2 recruitment, using the same cells, drug dilutions, and assay buffers [1% dimethylsulfoxide (DMSO), F12 Ham’s buffer] to ensure accurate assay-to-assay comparisons of data. Plates were read using a time-resolved fluorescence ratio (665 nm/620 nm) on a PheraStar plate reader
Substance Class Chemical
Created
by admin
on Wed Apr 02 10:49:36 GMT 2025
Edited
by admin
on Wed Apr 02 10:49:36 GMT 2025
Record UNII
GRM3MU4DWP
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
OXYCODONE PHOSPHATE
Common Name English
OXYCODONE PHOSPHATE SALT
Preferred Name English
MORPHINAN-6-ONE, 4,5-EPOXY-14-HYDROXY-3-METHOXY-17-METHYL-, (5.ALPHA.)-, PHOSPHATE (1:1)
Systematic Name English
(4R,4AS,7AR,12BS)-4A-HYDROXY-9-METHOXY-3-METHYL-2,4,5,6,7A,13-HEXAHYDRO-1H-4,12-METHANOBENZOFURO(3,2-E)ISOQUINOLIN-7-ONE;PHOSPHORIC ACID
Systematic Name English
Code System Code Type Description
CAS
1211844-14-2
Created by admin on Wed Apr 02 10:49:36 GMT 2025 , Edited by admin on Wed Apr 02 10:49:36 GMT 2025
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SMS_ID
300000041678
Created by admin on Wed Apr 02 10:49:36 GMT 2025 , Edited by admin on Wed Apr 02 10:49:36 GMT 2025
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PUBCHEM
68824785
Created by admin on Wed Apr 02 10:49:36 GMT 2025 , Edited by admin on Wed Apr 02 10:49:36 GMT 2025
PRIMARY
FDA UNII
GRM3MU4DWP
Created by admin on Wed Apr 02 10:49:36 GMT 2025 , Edited by admin on Wed Apr 02 10:49:36 GMT 2025
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE