Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C18H21NO4.C14H28O2 |
Molecular Weight | 543.7346 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCCCCCCCCCCC(O)=O.COC1=CC=C2C[C@H]3N(C)CC[C@@]45[C@@H](OC1=C24)C(=O)CC[C@@]35O
InChI
InChIKey=OIORLIPHCJBIJB-RKXJKUSZSA-N
InChI=1S/C18H21NO4.C14H28O2/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;1-2-3-4-5-6-7-8-9-10-11-12-13-14(15)16/h3-4,13,16,21H,5-9H2,1-2H3;2-13H2,1H3,(H,15,16)/t13-,16+,17+,18-;/m1./s1
Molecular Formula | C14H28O2 |
Molecular Weight | 228.3709 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
DescriptionCurator'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
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%).
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL233 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23880538 |
500.0 nM [EC50] | ||
Target ID: CHEMBL237 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23880538 |
16000.0 nM [EC50] | ||
Target ID: CHEMBL236 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23880538 |
4000.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | PERCODAN-DEMI Approved UseOxyContin 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 Date1950 |
|||
Primary | PERCODAN-DEMI Approved UseOxyContin 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 Date1950 |
|||
Primary | PERCODAN-DEMI Approved UseOxyContin 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 Date1950 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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 |
Other AEs: Pulmonary edema... |
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%) Sources: Dizziness (grade 1-2, 1.7%) Abdominal pain (grade 1-2, 0.8%) |
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%) Sources: Vomiting (grade 1-2, 0.8%) Nausea (grade 1-2, 0.8%) Somnolence (grade 1-2, 0.8%) |
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%) Sources: Dizziness (grade 1-2, 4.8%) Confusion (grade 1-2, 3.2%) |
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%) Sources: Flu syndrome (grade 1-2, 0.8%) Confusion (grade 1-2, 0.8%) Fatigue (grade 1-2, 0.8%) |
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 Health Status: healthy Age Group: mean age 33 years Sex: M+F Sources: |
Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (11.4%) Sources: |
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
AE | Significance | Dose | Population |
---|---|---|---|
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 |
|
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 Health Status: healthy Age Group: mean age 33 years Sex: M+F Sources: |
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
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical 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
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Advancement of opioid analgesia with controlled-release oxycodone. | 2001 |
|
Responding rationally to recent report of abuse/diversion of Oxycontin. | 2001 May |
|
[Treatment of pain in cancer with systemically administered opioids]. | 2001 May 19 |
|
Conversion ratio and cost of oxycodone. | 2001 May-Jun |
|
OxyContin, the media, and law enforcement. | 2001 May-Jun |
|
Clinical case study. | 2001 Nov-Dec |
|
Acetaminophen, aspirin, or Ibuprofen in combination analgesic products. | 2001 Nov-Dec |
|
The simultaneous determination of codeine, morphine, hydrocodone, hydromorphone, 6-acetylmorphine, and oxycodone in hair and oral fluid. | 2002 Apr |
|
More blame and praise for a pain drug. | 2002 Apr 29 |
|
Comparison of the pharmacokinetics of oxycodone administered in three Percocet formulations. | 2002 Feb |
|
An evaluation of the efficacy and tolerability of oral tramadol hydrochloride tablets for the treatment of postsurgical pain in children. | 2002 Jun |
|
There is no accounting for accountability. | 2002 Mar |
|
Validity and reliability of three commercially available breath-by-breath respiratory systems. | 2002 Mar |
|
Venous malformations associated with central pain: report of a case. | 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 |
|
Massive OxyContin ingestion refractory to naloxone therapy. | 2002 Oct |
|
Induced hypothermia for drug overdose. | 2002 Sep |
|
Review: tricyclic antidepressants, capsaicin, gabapentin, and oxycodone are effective for postherpetic neuralgia. | 2002 Sep-Oct |
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23880538
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
Edited
Wed Apr 02 10:22:40 GMT 2025
by
admin
on
Wed Apr 02 10:22:40 GMT 2025
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Record UNII |
96P3HS657Y
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Record Status |
Validated (UNII)
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Record Version |
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96P3HS657Y
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100000182573
Created by
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118947059
Created by
admin on Wed Apr 02 10:22:40 GMT 2025 , Edited by admin on Wed Apr 02 10:22:40 GMT 2025
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |
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