U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C17H19NO4
Molecular Weight 301.3377
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of OXYMORPHONE

SMILES

CN1CC[C@@]23c4c5ccc(c4O[C@@]3([H])C(=O)CC[C@]2([C@@]1([H])C5)O)O

InChI

InChIKey=UQCNKQCJZOAFTQ-ISWURRPUSA-N
InChI=1S/C17H19NO4/c1-18-7-6-16-13-9-2-3-10(19)14(13)22-15(16)11(20)4-5-17(16,21)12(18)8-9/h2-3,12,15,19,21H,4-8H2,1H3/t12-,15+,16+,17-/m1/s1

HIDE SMILES / InChI

Molecular Formula C17H19NO4
Molecular Weight 301.3377
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 4 / 4
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021611lbl.pdf | https://www.drugs.com/pro/oxymorphone.html

Oxymorphone is an analgesic that is FDA approved for the treatment of moderate to severe pain. It is also indicated for relief of anxiety in patients with dyspnea associated with pulmonary edema secondary to acute left ventricular dysfunction. Oxymorphone (brand names Opana, Numorphan, Numorphone) is a full opioid agonist and is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. Adverse reactions (≥ 2% of patients): seen with the immediate release tablet formulation Nausea, pyrexia, somnolence, vomiting, pruritus, headache, dizziness, constipation, and confusion. Concomitant use with serotonergic drugs may result in serotonin syndrome. Avoid use of mixed agonist/antagonist and partial agonist opioid analgesics with Opana because they may reduce analgesic effect of Opana or precipitate withdrawal symptoms.

Originator

Sources: DOI:10.1021/ja01627a033

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
OPANA

Approved Use

Enter section text here - OPANA ER is an opioid agonist indicated for the relief of moderate to severe pain in patients requiring continuous around-the-clock opioid treatment for an extended period of time. (1) - Not intended for use as an as needed analgesic. Not indicated in the immediate post-operative period or if the pain is mild or not expected to persist for an extended period of time. (1), 1 INDICATIONS AND USAGE 1 INDICATIONS AND USAGE OPANA ER is indicated for the relief of moderate to severe pain in patients requiring continuous, around-the-clock opioid treatment for an extended period of time. Limitations of Usage OPANA ER is not intended for use as an as needed analgesic. OPANA ER is not indicated for pain in the immediate post-operative period if the pain is mild, or not expected to persist for an extended period of time. OPANA ER is only indicated for post-operative use if the patient is already receiving the drug prior to surgery or if the post-operative pain is expected to be moderate or 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

-339292800000
Palliative
OPANA

Approved Use

Enter section text here - OPANA ER is an opioid agonist indicated for the relief of moderate to severe pain in patients requiring continuous around-the-clock opioid treatment for an extended period of time. (1) - Not intended for use as an as needed analgesic. Not indicated in the immediate post-operative period or if the pain is mild or not expected to persist for an extended period of time. (1), 1 INDICATIONS AND USAGE 1 INDICATIONS AND USAGE OPANA ER is indicated for the relief of moderate to severe pain in patients requiring continuous, around-the-clock opioid treatment for an extended period of time. Limitations of Usage OPANA ER is not intended for use as an as needed analgesic. OPANA ER is not indicated for pain in the immediate post-operative period if the pain is mild, or not expected to persist for an extended period of time. OPANA ER is only indicated for post-operative use if the patient is already receiving the drug prior to surgery or if the post-operative pain is expected to be moderate or 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

-339292800000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.21 ng/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
2.54 ng/mL
20 mg 2 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4.47 ng/mL
40 mg 2 times / day multiple, oral
dose: 40 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2.59 ng/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
0.27 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.7 ng/mL
5 mg 2 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
17.81 ng × h/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
19.28 ng × h/mL
20 mg 2 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
36.98 ng × h/mL
40 mg 2 times / day multiple, oral
dose: 40 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
37.9 ng × h/mL
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
4.54 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.6 ng × h/mL
5 mg 2 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
9.89 h
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
9.35 h
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
11.3 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OXYMORPHONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
20 mg 4 times / day multiple, oral
Recommended
dose: 20 mg 4 times / day
route: oral
experiment_type: multiple
dose_type: Recommended
co-adm with
    data_source:
    https://pubmed.ncbi.nlm.nih.gov/15777102
    healthy, 27–44
    population: healthy
    age: 27–44
    sex: M+F
    food_status:
    n:
    data_source:
    https://pubmed.ncbi.nlm.nih.gov/15777102
    Disc. AE: Vomiting, Nausea...
    AEs leading to
    discontinuation/dose reduction:​
    Vomiting (mild, 4.3%)
    Nausea (4.3%)
    Dizziness (4.3%)

    data_source:
    https://pubmed.ncbi.nlm.nih.gov/15777102
    79.4 mg 1 times / day multiple, oral
    Highest studied dose
    dose: 79.4 mg 1 times / day
    route: oral
    experiment_type: multiple
    dose_type: Highest studied dose
    co-adm with
      data_source:
      https://pubmed.ncbi.nlm.nih.gov/15629415
      unhealthy, 45.5-47.5
      population: unhealthy
      age: 45.5-47.5
      sex: M+F
      food_status:
      n:
      data_source:
      https://pubmed.ncbi.nlm.nih.gov/15629415
      Disc. AE: Abdominal pain, Chest pain...
      AEs leading to
      discontinuation/dose reduction:​
      Abdominal pain (1.4%)
      Chest pain (1.4%)
      Serum creatine phosphokinase increased (1.4%)
      Serum creatine phosphokinase MB increased (1.4%)
      Back pain (1.4%)

      data_source:
      https://pubmed.ncbi.nlm.nih.gov/15629415
      0.5 mg 5 times / day multiple, intravenous
      Recommended
      dose: 0.5 mg 5 times / day
      route: intravenous
      experiment_type: multiple
      dose_type: Recommended
      co-adm with
        data_source:
        https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
        unhealthy
        population: unhealthy
        age:
        sex:
        food_status:
        n:
        data_source:
        https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
        Disc. AE: Opioid abuse, Respiratory depression...
        AEs leading to
        discontinuation/dose reduction:​
        Opioid abuse
        Respiratory depression
        Addiction
        Hypotension (severe)

        data_source:
        https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
        1.5 mg 5 times / day multiple, intramuscular|subcutaneous
        Recommended
        dose: 1.5 mg 5 times / day
        route: intramuscular|subcutaneous
        experiment_type: multiple
        dose_type: Recommended
        co-adm with
          data_source:
          https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
          unhealthy
          population: unhealthy
          age:
          sex:
          food_status:
          n:
          data_source:
          https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
          Disc. AE: Opioid abuse, Respiratory depression...
          AEs leading to
          discontinuation/dose reduction:​
          Opioid abuse
          Respiratory depression
          Addiction
          Hypotension (severe)

          data_source:
          https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
          20 mg 5 times / day multiple, oral
          Recommended
          dose: 20 mg 5 times / day
          route: oral
          experiment_type: multiple
          dose_type: Recommended
          co-adm with
            data_source:
            https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
            unhealthy
            population: unhealthy
            age:
            sex:
            food_status:
            n:
            data_source:
            https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
            Disc. AE: Opioid abuse, Addiction...
            AEs leading to
            discontinuation/dose reduction:​
            Opioid abuse
            Addiction
            Respiratory depression (grade 3-5)
            Withdrawal syndrome neonatal
            Anaphylaxis
            Hypotension (severe)
            Angioedema
            Hypersensitivity reaction
            Adrenal insufficiency

            data_source:
            https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
            AEs

            AEs

            AESignificanceDosePopulation
            Abdominal pain 1.4%
            Disc. AE
            79.4 mg 1 times / day multiple, oral
            Highest studied dose
            dose: 79.4 mg 1 times / day
            route: oral
            experiment_type: multiple
            dose_type: Highest studied dose
            co-adm with
              data_source:
              https://pubmed.ncbi.nlm.nih.gov/15629415
              unhealthy, 45.5-47.5
              population:
              age:
              sex:
              food_status:
              n:
              data_source:
              https://pubmed.ncbi.nlm.nih.gov/15629415
              Back pain 1.4%
              Disc. AE
              79.4 mg 1 times / day multiple, oral
              Highest studied dose
              dose: 79.4 mg 1 times / day
              route: oral
              experiment_type: multiple
              dose_type: Highest studied dose
              co-adm with
                data_source:
                https://pubmed.ncbi.nlm.nih.gov/15629415
                unhealthy, 45.5-47.5
                population:
                age:
                sex:
                food_status:
                n:
                data_source:
                https://pubmed.ncbi.nlm.nih.gov/15629415
                Chest pain 1.4%
                Disc. AE
                79.4 mg 1 times / day multiple, oral
                Highest studied dose
                dose: 79.4 mg 1 times / day
                route: oral
                experiment_type: multiple
                dose_type: Highest studied dose
                co-adm with
                  data_source:
                  https://pubmed.ncbi.nlm.nih.gov/15629415
                  unhealthy, 45.5-47.5
                  population:
                  age:
                  sex:
                  food_status:
                  n:
                  data_source:
                  https://pubmed.ncbi.nlm.nih.gov/15629415
                  Serum creatine phosphokinase MB increased 1.4%
                  Disc. AE
                  79.4 mg 1 times / day multiple, oral
                  Highest studied dose
                  dose: 79.4 mg 1 times / day
                  route: oral
                  experiment_type: multiple
                  dose_type: Highest studied dose
                  co-adm with
                    data_source:
                    https://pubmed.ncbi.nlm.nih.gov/15629415
                    unhealthy, 45.5-47.5
                    population:
                    age:
                    sex:
                    food_status:
                    n:
                    data_source:
                    https://pubmed.ncbi.nlm.nih.gov/15629415
                    Serum creatine phosphokinase increased 1.4%
                    Disc. AE
                    79.4 mg 1 times / day multiple, oral
                    Highest studied dose
                    dose: 79.4 mg 1 times / day
                    route: oral
                    experiment_type: multiple
                    dose_type: Highest studied dose
                    co-adm with
                      data_source:
                      https://pubmed.ncbi.nlm.nih.gov/15629415
                      unhealthy, 45.5-47.5
                      population:
                      age:
                      sex:
                      food_status:
                      n:
                      data_source:
                      https://pubmed.ncbi.nlm.nih.gov/15629415
                      Dizziness 4.3%
                      Disc. AE
                      20 mg 4 times / day multiple, oral
                      Recommended
                      dose: 20 mg 4 times / day
                      route: oral
                      experiment_type: multiple
                      dose_type: Recommended
                      co-adm with
                        data_source:
                        https://pubmed.ncbi.nlm.nih.gov/15777102
                        healthy, 27–44
                        population:
                        age:
                        sex:
                        food_status:
                        n:
                        data_source:
                        https://pubmed.ncbi.nlm.nih.gov/15777102
                        Nausea 4.3%
                        Disc. AE
                        20 mg 4 times / day multiple, oral
                        Recommended
                        dose: 20 mg 4 times / day
                        route: oral
                        experiment_type: multiple
                        dose_type: Recommended
                        co-adm with
                          data_source:
                          https://pubmed.ncbi.nlm.nih.gov/15777102
                          healthy, 27–44
                          population:
                          age:
                          sex:
                          food_status:
                          n:
                          data_source:
                          https://pubmed.ncbi.nlm.nih.gov/15777102
                          Vomiting mild,4.3%
                          Disc. AE
                          20 mg 4 times / day multiple, oral
                          Recommended
                          dose: 20 mg 4 times / day
                          route: oral
                          experiment_type: multiple
                          dose_type: Recommended
                          co-adm with
                            data_source:
                            https://pubmed.ncbi.nlm.nih.gov/15777102
                            healthy, 27–44
                            population:
                            age:
                            sex:
                            food_status:
                            n:
                            data_source:
                            https://pubmed.ncbi.nlm.nih.gov/15777102
                            Addiction
                            Disc. AE
                            0.5 mg 5 times / day multiple, intravenous
                            Recommended
                            dose: 0.5 mg 5 times / day
                            route: intravenous
                            experiment_type: multiple
                            dose_type: Recommended
                            co-adm with
                              data_source:
                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                              unhealthy
                              population:
                              age:
                              sex:
                              food_status:
                              n:
                              data_source:
                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                              Opioid abuse
                              Disc. AE
                              0.5 mg 5 times / day multiple, intravenous
                              Recommended
                              dose: 0.5 mg 5 times / day
                              route: intravenous
                              experiment_type: multiple
                              dose_type: Recommended
                              co-adm with
                                data_source:
                                https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                unhealthy
                                population:
                                age:
                                sex:
                                food_status:
                                n:
                                data_source:
                                https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                Respiratory depression
                                Disc. AE
                                0.5 mg 5 times / day multiple, intravenous
                                Recommended
                                dose: 0.5 mg 5 times / day
                                route: intravenous
                                experiment_type: multiple
                                dose_type: Recommended
                                co-adm with
                                  data_source:
                                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                  unhealthy
                                  population:
                                  age:
                                  sex:
                                  food_status:
                                  n:
                                  data_source:
                                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                  Hypotension severe
                                  Disc. AE
                                  0.5 mg 5 times / day multiple, intravenous
                                  Recommended
                                  dose: 0.5 mg 5 times / day
                                  route: intravenous
                                  experiment_type: multiple
                                  dose_type: Recommended
                                  co-adm with
                                    data_source:
                                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                    unhealthy
                                    population:
                                    age:
                                    sex:
                                    food_status:
                                    n:
                                    data_source:
                                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                    Addiction
                                    Disc. AE
                                    1.5 mg 5 times / day multiple, intramuscular|subcutaneous
                                    Recommended
                                    dose: 1.5 mg 5 times / day
                                    route: intramuscular|subcutaneous
                                    experiment_type: multiple
                                    dose_type: Recommended
                                    co-adm with
                                      data_source:
                                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                      unhealthy
                                      population:
                                      age:
                                      sex:
                                      food_status:
                                      n:
                                      data_source:
                                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                      Opioid abuse
                                      Disc. AE
                                      1.5 mg 5 times / day multiple, intramuscular|subcutaneous
                                      Recommended
                                      dose: 1.5 mg 5 times / day
                                      route: intramuscular|subcutaneous
                                      experiment_type: multiple
                                      dose_type: Recommended
                                      co-adm with
                                        data_source:
                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                        unhealthy
                                        population:
                                        age:
                                        sex:
                                        food_status:
                                        n:
                                        data_source:
                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                        Respiratory depression
                                        Disc. AE
                                        1.5 mg 5 times / day multiple, intramuscular|subcutaneous
                                        Recommended
                                        dose: 1.5 mg 5 times / day
                                        route: intramuscular|subcutaneous
                                        experiment_type: multiple
                                        dose_type: Recommended
                                        co-adm with
                                          data_source:
                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                          unhealthy
                                          population:
                                          age:
                                          sex:
                                          food_status:
                                          n:
                                          data_source:
                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                          Hypotension severe
                                          Disc. AE
                                          1.5 mg 5 times / day multiple, intramuscular|subcutaneous
                                          Recommended
                                          dose: 1.5 mg 5 times / day
                                          route: intramuscular|subcutaneous
                                          experiment_type: multiple
                                          dose_type: Recommended
                                          co-adm with
                                            data_source:
                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                            unhealthy
                                            population:
                                            age:
                                            sex:
                                            food_status:
                                            n:
                                            data_source:
                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
                                            Addiction
                                            Disc. AE
                                            20 mg 5 times / day multiple, oral
                                            Recommended
                                            dose: 20 mg 5 times / day
                                            route: oral
                                            experiment_type: multiple
                                            dose_type: Recommended
                                            co-adm with
                                              data_source:
                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                              unhealthy
                                              population:
                                              age:
                                              sex:
                                              food_status:
                                              n:
                                              data_source:
                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                              Adrenal insufficiency
                                              Disc. AE
                                              20 mg 5 times / day multiple, oral
                                              Recommended
                                              dose: 20 mg 5 times / day
                                              route: oral
                                              experiment_type: multiple
                                              dose_type: Recommended
                                              co-adm with
                                                data_source:
                                                https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                unhealthy
                                                population:
                                                age:
                                                sex:
                                                food_status:
                                                n:
                                                data_source:
                                                https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                Anaphylaxis
                                                Disc. AE
                                                20 mg 5 times / day multiple, oral
                                                Recommended
                                                dose: 20 mg 5 times / day
                                                route: oral
                                                experiment_type: multiple
                                                dose_type: Recommended
                                                co-adm with
                                                  data_source:
                                                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                  unhealthy
                                                  population:
                                                  age:
                                                  sex:
                                                  food_status:
                                                  n:
                                                  data_source:
                                                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                  Angioedema
                                                  Disc. AE
                                                  20 mg 5 times / day multiple, oral
                                                  Recommended
                                                  dose: 20 mg 5 times / day
                                                  route: oral
                                                  experiment_type: multiple
                                                  dose_type: Recommended
                                                  co-adm with
                                                    data_source:
                                                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                    unhealthy
                                                    population:
                                                    age:
                                                    sex:
                                                    food_status:
                                                    n:
                                                    data_source:
                                                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                    Hypersensitivity reaction
                                                    Disc. AE
                                                    20 mg 5 times / day multiple, oral
                                                    Recommended
                                                    dose: 20 mg 5 times / day
                                                    route: oral
                                                    experiment_type: multiple
                                                    dose_type: Recommended
                                                    co-adm with
                                                      data_source:
                                                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                      unhealthy
                                                      population:
                                                      age:
                                                      sex:
                                                      food_status:
                                                      n:
                                                      data_source:
                                                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                      Opioid abuse
                                                      Disc. AE
                                                      20 mg 5 times / day multiple, oral
                                                      Recommended
                                                      dose: 20 mg 5 times / day
                                                      route: oral
                                                      experiment_type: multiple
                                                      dose_type: Recommended
                                                      co-adm with
                                                        data_source:
                                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                        unhealthy
                                                        population:
                                                        age:
                                                        sex:
                                                        food_status:
                                                        n:
                                                        data_source:
                                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                        Withdrawal syndrome neonatal
                                                        Disc. AE
                                                        20 mg 5 times / day multiple, oral
                                                        Recommended
                                                        dose: 20 mg 5 times / day
                                                        route: oral
                                                        experiment_type: multiple
                                                        dose_type: Recommended
                                                        co-adm with
                                                          data_source:
                                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                          unhealthy
                                                          population:
                                                          age:
                                                          sex:
                                                          food_status:
                                                          n:
                                                          data_source:
                                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                          Respiratory depression grade 3-5
                                                          Disc. AE
                                                          20 mg 5 times / day multiple, oral
                                                          Recommended
                                                          dose: 20 mg 5 times / day
                                                          route: oral
                                                          experiment_type: multiple
                                                          dose_type: Recommended
                                                          co-adm with
                                                            data_source:
                                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                            unhealthy
                                                            population:
                                                            age:
                                                            sex:
                                                            food_status:
                                                            n:
                                                            data_source:
                                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                            Hypotension severe
                                                            Disc. AE
                                                            20 mg 5 times / day multiple, oral
                                                            Recommended
                                                            dose: 20 mg 5 times / day
                                                            route: oral
                                                            experiment_type: multiple
                                                            dose_type: Recommended
                                                            co-adm with
                                                              data_source:
                                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                              unhealthy
                                                              population:
                                                              age:
                                                              sex:
                                                              food_status:
                                                              n:
                                                              data_source:
                                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
                                                              Overview

                                                              Overview

                                                              CYP3A4CYP2C9CYP2D6hERG


                                                              OverviewOther

                                                              Other InhibitorOther SubstrateOther Inducer


                                                              Drug as perpetrator​Drug as victim

                                                              Drug as victim

                                                              TargetModalityActivityMetaboliteClinical evidence
                                                              no
                                                              PubMed

                                                              PubMed

                                                              TitleDatePubMed
                                                              The use of liquid chromatography/mass spectrometry for quantitative analysis of oxycodone, oxymorphone and noroxycodone in Ringer solution, rat plasma and rat brain tissue.
                                                              2004
                                                              Cardiopulmonary effects of medetomidine, oxymorphone, or butorphanol in selegiline-treated dogs.
                                                              2004 Apr
                                                              In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone.
                                                              2004 Jan 12
                                                              Efficacy of oxymorphone extended release in postsurgical pain: a randomized clinical trial in knee arthroplasty.
                                                              2004 Jul
                                                              Establishing the dosage equivalency of oxymorphone extended release and oxycodone controlled release in patients with cancer pain: a randomized controlled study.
                                                              2004 Jun
                                                              Relationship between 4,5-epoxymorphinan structure and in vitro modulation of cell proliferation.
                                                              2004 Jun 28
                                                              Screening postmortem whole blood for oxycodone by ELISA response ratios.
                                                              2004 May
                                                              The efficacy and safety of oral immediate-release oxymorphone for postsurgical pain.
                                                              2004 Nov
                                                              Sedative effects and serum drug concentrations of oxymorphone and metabolites after subcutaneous administration of a liposome-encapsulated formulation in dogs.
                                                              2004 Oct
                                                              Pain management in cats--past, present and future. Part 2. Treatment of pain--clinical pharmacology.
                                                              2004 Oct
                                                              Identification of new oxycodone metabolites in human urine by capillary electrophoresis-multiple-stage ion-trap mass spectrometry.
                                                              2004 Oct 8
                                                              Prevalence of opioid adverse events in chronic non-malignant pain: systematic review of randomised trials of oral opioids.
                                                              2005
                                                              Single- and multiple-dose pharmacokinetic and dose-proportionality study of oxymorphone immediate-release tablets.
                                                              2005
                                                              Efficacy and safety of oxymorphone immediate release for the treatment of mild to moderate pain after ambulatory orthopedic surgery: results of a randomized, double-blind, placebo-controlled trial.
                                                              2005 Dec
                                                              Effectiveness and safety of oral extended-release oxymorphone for the treatment of cancer pain: a pilot study.
                                                              2005 Jan
                                                              Oxymorphone extended release does not affect CYP2C9 or CYP3A4 metabolic pathways.
                                                              2005 Mar
                                                              Safety, tolerability, and effectiveness of oxymorphone extended release for moderate to severe osteoarthritis pain: a one-year study.
                                                              2005 Mar-Apr
                                                              Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.
                                                              2005 May 5
                                                              Direct analysis of opiates in urine by liquid chromatography-tandem mass spectrometry.
                                                              2005 Oct
                                                              Comparison of oxycodone pharmacokinetics after buccal and sublingual administration in children.
                                                              2006
                                                              Dissociative anaesthesia during field and hospital conditions for castration of colts.
                                                              2006
                                                              Predictors of opioid misuse in patients with chronic pain: a prospective cohort study.
                                                              2006 Apr 4
                                                              Comparison of the in vitro efficacy of mu, delta, kappa and ORL1 receptor agonists and non-selective opioid agonists in dog brain membranes.
                                                              2006 Feb 16
                                                              Effects of oxymorphone and hydromorphone on the minimum alveolar concentration of isoflurane in dogs.
                                                              2006 Jan
                                                              A synthetic fraction of feline facial pheromones calms but does not reduce struggling in cats before venous catheterization.
                                                              2006 Jul
                                                              Controlled clinical trials in cancer pain. How controlled should they be? A qualitative systematic review.
                                                              2006 Jun 5
                                                              A 2-week, multicenter, randomized, double-blind, placebo-controlled, dose-ranging, phase III trial comparing the efficacy of oxymorphone extended release and placebo in adults with pain associated with osteoarthritis of the hip or knee.
                                                              2006 Mar
                                                              Comparison of an automated and point-of-care immunoassay to GC-MS for urine oxycodone testing in the clinical laboratory.
                                                              2006 Mar
                                                              Comparison of the antinociceptive response to morphine and morphine-like compounds in male and female Sprague-Dawley rats.
                                                              2006 Mar
                                                              Opioid receptor-mediated hyperalgesia and antinociceptive tolerance induced by sustained opiate delivery.
                                                              2006 Mar 20
                                                              Opioid analgesics in primary care: challenges and new advances in the management of noncancer pain.
                                                              2006 Mar-Apr
                                                              Pharmacokinetics and pharmacodynamics of oral oxycodone in healthy human subjects: role of circulating active metabolites.
                                                              2006 May
                                                              An automated and fully validated LC-MS/MS procedure for the simultaneous determination of 11 opioids used in palliative care, with 5 of their metabolites.
                                                              2006 May
                                                              Incomplete recovery of prescription opioids in urine using enzymatic hydrolysis of glucuronide metabolites.
                                                              2006 Oct
                                                              Antinociception by spinal and systemic oxycodone: why does the route make a difference? In vitro and in vivo studies in rats.
                                                              2006 Oct
                                                              Low-level quantitation of oxycodone and its oxidative metabolites, noroxycodone, and oxymorphone, in rat plasma by high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry.
                                                              2007 Apr 1
                                                              Comment: Oral oxymorphone for pain management.
                                                              2007 Dec
                                                              Extended-duration agents for perioperative pain management.
                                                              2007 Feb
                                                              Effect of naloxone-3-glucuronide and N-methylnaloxone on the motility of the isolated rat colon after morphine.
                                                              2007 Feb
                                                              Efficacy and safety of OPANA ER (oxymorphone extended release) for relief of moderate to severe chronic low back pain in opioid-experienced patients: a 12-week, randomized, double-blind, placebo-controlled study.
                                                              2007 Feb
                                                              Evidence that oxymorphone-induced increases in micronuclei occur secondary to hyperthermia.
                                                              2007 Feb
                                                              New pain management options: drugs.
                                                              2007 Jan
                                                              Oral oxymorphone (Opana).
                                                              2007 Jan 1
                                                              The effect of opiates on the activity of human placental aromatase/CYP19.
                                                              2007 Jan 15
                                                              Oral extended-release oxymorphone: a new choice for chronic pain relief.
                                                              2007 Jul
                                                              Oral oxymorphone for pain management.
                                                              2007 Jul
                                                              Oxymorphone hydrochloride, a potent opioid analgesic, is not carcinogenic in rats or mice.
                                                              2007 Mar
                                                              Use of oral oxymorphone in the elderly.
                                                              2007 May
                                                              Requirements and ontology for a G protein-coupled receptor oligomerization knowledge base.
                                                              2007 May 30
                                                              Rapid analysis of metabolites and drugs of abuse from urine samples by desorption electrospray ionization-mass spectrometry.
                                                              2007 Sep
                                                              Patents

                                                              Sample Use Guides

                                                              In Vivo Use Guide
                                                              Curator's Comment:: http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021611lbl.pdf
                                                              Subcutaneous or Intramuscular administration: Initiate treatment with 1mg to 1.5 mg, every 4 to 6 hours.
                                                              Route of Administration: Other
                                                              In Vitro Use Guide
                                                              Oxymorphone hydrochloride was not mutagenic when tested in the in vitro bacterial reverse mutation assay (Ames test) at concentrations of ≤5270 ug/plate, or in an in vitro mammalian cell chromosome aberration assay performed with human peripheral blood lymphocytes at concentrations ≤5000 ug/mL with or without metabolic activation.
                                                              Substance Class Chemical
                                                              Created
                                                              by admin
                                                              on Sat Jun 26 02:14:48 UTC 2021
                                                              Edited
                                                              by admin
                                                              on Sat Jun 26 02:14:48 UTC 2021
                                                              Record UNII
                                                              9VXA968E0C
                                                              Record Status Validated (UNII)
                                                              Record Version
                                                              • Download
                                                              Name Type Language
                                                              OXYMORPHONE
                                                              INN   MI   VANDF   WHO-DD  
                                                              INN  
                                                              Official Name English
                                                              OXYMORPHONE [WHO-DD]
                                                              Common Name English
                                                              OXYMORPHONE CII [USP-RS]
                                                              Common Name English
                                                              4,5.ALPHA.-EPOXY-3,14-DIHYDROXY-17-METHYLMORPHINAN-6-ONE
                                                              Systematic Name English
                                                              NIH 10323
                                                              Code English
                                                              OXYMORPHONE [VANDF]
                                                              Common Name English
                                                              DIHYDROXYMORPHINONE
                                                              Common Name English
                                                              IDS-NO-003
                                                              Code English
                                                              MORPHINAN-6-ONE, 4,5-EPOXY-3,14-DIHYDROXY-17-METHYL-
                                                              Systematic Name English
                                                              14-HYDROXYDIHYDROMORPHINONE
                                                              Common Name English
                                                              OXYCODONE HYDROCHLORIDE IMPURITY, OXYMORPHONE- [USP]
                                                              Common Name English
                                                              OXYCODONE HYDROCHLORIDE SPECIFIED IMPURITY A [EP]
                                                              Common Name English
                                                              OXYMORPHONE [INN]
                                                              Common Name English
                                                              OXYMORPHONE CII
                                                              USP-RS  
                                                              Common Name English
                                                              7,8-DIHYDRO-14-HYDROXYMORPHINONE
                                                              Common Name English
                                                              OXYMORPHONE [MI]
                                                              Common Name English
                                                              NSC-19045
                                                              Code English
                                                              Classification Tree Code System Code
                                                              NDF-RT N0000175690
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              NCI_THESAURUS C67413
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              LIVERTOX 728
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              NDF-RT N0000175684
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              NCI_THESAURUS C1506
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              FDA ORPHAN DRUG 6185
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              DEA NO. 9652
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              Code System Code Type Description
                                                              HSDB
                                                              8060
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              RXCUI
                                                              7814
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY RxNorm
                                                              NCI_THESAURUS
                                                              C29314
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              PUBCHEM
                                                              5284604
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              EVMPD
                                                              SUB09569MIG
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              USP_CATALOG
                                                              1488000
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY USP-RS
                                                              MERCK INDEX
                                                              M8338
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY Merck Index
                                                              WIKIPEDIA
                                                              OXYMORPHONE
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              DRUG BANK
                                                              DB01192
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              ECHA (EC/EINECS)
                                                              200-959-7
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              ChEMBL
                                                              CHEMBL963
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              EPA CompTox
                                                              76-41-5
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              FDA UNII
                                                              9VXA968E0C
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              DRUG CENTRAL
                                                              2034
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              LACTMED
                                                              Oxymorphone
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              INN
                                                              937
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              MESH
                                                              D010111
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              IUPHAR
                                                              7094
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              CAS
                                                              76-41-5
                                                              Created by admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
                                                              PRIMARY
                                                              Related Record Type Details
                                                              SALT/SOLVATE -> PARENT
                                                              APPROXIMATE PURE ANHYDROUS DRUG CONTENT (IN PERCENT)
                                                              BINDER->LIGAND
                                                              BINDING
                                                              SALT/SOLVATE -> PARENT
                                                              APPROXIMATE PURE ANHYDROUS DRUG CONTENT (IN PERCENT)
                                                              Related Record Type Details
                                                              METABOLITE -> PARENT
                                                              6-OH-oxymorphone has been shown in animal studies to have analgesic bioactivity
                                                              MAJOR
                                                              PLASMA; URINE
                                                              PARENT -> METABOLITE ACTIVE
                                                              Highly variable 40 fold higher potency than Oxycodone
                                                              MINOR
                                                              PLASMA; URINE
                                                              METABOLITE -> PARENT
                                                              MAJOR
                                                              PLASMA
                                                              METABOLITE -> PARENT
                                                              6-OH-oxymorphone has been shown in animal studies to have analgesic bioactivity.
                                                              MAJOR
                                                              URINE
                                                              Related Record Type Details
                                                              PARENT -> IMPURITY
                                                              CHROMATOGRAPHIC PURITY (HPLC/UV)
                                                              USP
                                                              Related Record Type Details
                                                              ACTIVE MOIETY
                                                              Name Property Type Amount Referenced Substance Defining Parameters References
                                                              Biological Half-life PHARMACOKINETIC Elimination
                                                              PHARMACOKINETIC
                                                              Elimination
                                                              PHARMACOKINETIC
                                                              Volume of Distribution PHARMACOKINETIC