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Details

Stereochemistry ABSOLUTE
Molecular Formula 2C18H21NO4.C8H6O4
Molecular Weight 796.8581
Optical Activity UNSPECIFIED
Defined Stereocenters 8 / 8
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of OXYCODONE TEREPHTHALATE

SMILES

OC(=O)C1=CC=C(C=C1)C(O)=O.COC2=C3O[C@H]4C(=O)CC[C@@]5(O)[C@H]6CC(C=C2)=C3[C@@]45CCN6C.COC7=C8O[C@H]9C(=O)CC[C@@]%10(O)[C@H]%11CC(C=C7)=C8[C@@]9%10CCN%11C

InChI

InChIKey=BTEYIHUKHHAVAN-KDKWOIFOSA-N
InChI=1S/2C18H21NO4.C8H6O4/c2*1-19-8-7-17-14-10-3-4-12(22-2)15(14)23-16(17)11(20)5-6-18(17,21)13(19)9-10;9-7(10)5-1-2-6(4-3-5)8(11)12/h2*3-4,13,16,21H,5-9H2,1-2H3;1-4H,(H,9,10)(H,11,12)/t2*13-,16+,17+,18-;/m11./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 C8H6O4
Molecular Weight 166.1308
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
Opioid formulations: tailoring to the needs in chronic pain.
2001
Strategies for the treatment of cancer pain in the new millennium.
2001
The preemptive analgesic effect of intraarticular bupivacaine and morphine after ambulatory arthroscopic knee surgery.
2001 Apr
Time-release analgesic drug causes fatal overdoses in United States.
2001 Aug
"No, Duke. No divorce".
2001 Aug 20
The potent perils of a miracle drug.
2001 Jan 8
Federal reports say oxycodone abuse is on the rise.
2001 Jul 1
'Not an appropriate use'. Did the makers of OxyContin push too hard?
2001 Jul 2
Relative variability in bioavailability of oral controlled-release formulations of oxycodone and morphine.
2001 Jul-Aug
Controlled-release oxycodone hydrochloride (OxyContin).
2001 Sep
Managing postoperative pain.
2001 Sep
Hydromorphone for acute and chronic pain.
2002
Oxy's offspring.
2002 Apr 22
Minimal interaction between gatifloxacin and oxycodone.
2002 Aug
Treatment of postherpetic neuralgia: a systematic review of the literature.
2002 Feb
Comparison of pre- and postoperative administration of ketoprofen for analgesia after tonsillectomy in children.
2002 Feb
Treatment of painful sickle cell leg ulcers with topical opioids.
2002 Feb 1
Combination hydrocodone and ibuprofen versus combination oxycodone and acetaminophen in the treatment of moderate or severe acute low back pain.
2002 Jan
A comparison of oral transmucosal fentanyl citrate and oral oxycodone for pediatric outpatient wound care.
2002 Jan-Feb
Safety and efficacy of controlled-release oxycodone: a systematic literature review.
2002 Jul
Gateways to clinical trials.
2002 Jul-Aug
An evaluation of the efficacy and tolerability of oral tramadol hydrochloride tablets for the treatment of postsurgical pain in children.
2002 Jun
Preoperative administration of controlled-release oxycodone for the management of pain after ambulatory laparoscopic tubal ligation surgery.
2002 May
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
Oxycontin: the concept of a "ghost pill" and the postmortem tissue distribution of oxycodone in 36 cases.
2002 Oct
Oxycontin--misuse and abuse.
2002 Summer
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 Mon Mar 31 17:54:14 GMT 2025
Edited
by admin
on Mon Mar 31 17:54:14 GMT 2025
Record UNII
M04XWV43UF
Record Status Validated (UNII)
Record Version
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Name Type Language
CODOXY COMPONENT OXYCODONE TEREPHTHALATE
Preferred Name English
OXYCODONE TEREPHTHALATE
MART.   ORANGE BOOK   USP   VANDF   WHO-DD  
Common Name English
PERCODAN-DEMI COMPONENT OXYCODONE TEREPHTHALATE
Common Name English
14-HYDROXYDIHYDROCODEINONE TEREPHTHALATE (2:1)
Common Name English
MORPHINAN-6-ONE, 4,5-EPOXY-14-HYDROXY-3-METHOXY-17-METHYL-, 1,4-BENZENEDICARBOXYLATE (2:1 SALT), (5.ALPHA.)
Common Name English
ROXIPRIN COMPONENT OXYCODONE TEREPHTHALATE
Common Name English
OXYCODONE TEREPHTHALATE [USP IMPURITY]
Common Name English
OXYCODONE TEREPHTHALATE [MART.]
Common Name English
OXYCODONE TEREPHTHALATE [USP MONOGRAPH]
Common Name English
4,5?-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one 1,4-benzenedicarboxylate (2:1 salt)
Common Name English
OXYCODONE TEREPHTHALATE [ORANGE BOOK]
Common Name English
OXYCODONE TEREPHTHALATE [VANDF]
Common Name English
Oxycodone terephthalate [WHO-DD]
Common Name English
Classification Tree Code System Code
DEA NO. 9143
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
NCI_THESAURUS C67413
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
NCI_THESAURUS C1506
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
Code System Code Type Description
EVMPD
SUB03585MIG
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
ChEMBL
CHEMBL656
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
SMS_ID
100000085510
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
NCI_THESAURUS
C48009
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
PUBCHEM
23724882
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
WIKIPEDIA
Oxycodone terephthalate
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
FDA UNII
M04XWV43UF
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
DRUG BANK
DBSALT001326
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
RXCUI
159821
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY RxNorm
MESH
C016026
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
DAILYMED
M04XWV43UF
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
CAS
124133-68-2
Created by admin on Mon Mar 31 17:54:14 GMT 2025 , Edited by admin on Mon Mar 31 17:54:14 GMT 2025
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY