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QuickView for Oxymorphone (compound)
PubChem
| Name: | Oxymorphone |
|---|---|
| PubChem Compound ID: | 4639 |
| Description: | An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) |
| Molecular formula: | C17H19NO4 |
| Molecular weight: | 301.337 g/mol |
| Synonyms: |
Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-methyl-, (5.alpha.)-; 7,8-Dihydro-14-hydroxymorphinone
|
DrugBank
Identification
| Name: | Oxymorphone |
|---|---|
| Name (isomeric): | DB01192 |
| Drug Type: | small molecule |
| Description: | An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) |
| Synonyms: |
Oximorphonum; Dihydroxymorphinone; 14-Hydroxydihydromorphinone; Dihydrohydroxymorphinone; Oxymorphine; EN3202
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| Brand: | OPANA ER, Opana, Numorphan |
| Category: | Adjuvants, Anesthesia, Narcotics, Adjuvants, Analgesics, Opiate Agonists, Analgesics, Opioid |
| CAS number: | 76-41-5 |
Pharmacology
| Indication: | For the treatment of moderate-to-severe pain. |
|---|---|
| Pharmacology: |
Oxymorphone is a semi-synthetic opioid substitute for morphine. It is a potent analgesic. Opioid analgesics exert their principal pharmacologic effects on the CNS and the gastrointestinal tract. The principal actions of therapeutic value are analgesia and sedation. Opioids produce respiratory depression by direct action on brain stem respiratory ce...
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| Mechanism of Action: |
Oxymorphone interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (s...
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| Biotransformation: | Oxymorphone undergoes extensive hepatic metabolism in humans. After a 10 mg oral dose, 49% was excreted over a five-day period in the urine. Of this, 82% was excreted in the first 24 hours after administration. The recovered drug-related products contained the oxymorphone (1.9%), the conjugate of oxymorphone (44.1%), the 6(beta)-carbinol produced by 6-keto reduction of oxymorphone (0.3%), and the conjugates of 6(beta)-carbinol (2.6%) and 6(alpha)-carbinol (0.1%). |
| Route of elimination: | Oxymorphone is highly metabolized, principally in the liver, and undergoes reduction or conjugation with glucuronic acid to form both active and inactive products. Because oxymorphone is extensively metabolized, <1% of the administered dose is excreted unchanged in the urine. |
| Half Life: | 1.3 (+/-0.7) hours |
| Toxicity: | Oxymorphone overdosage is characterized by respiratory depression, extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. In a severe case of overdose, apnea, circulatory collapse, cardiac arrest, and death may occur. Intravenous mouse LD50 is 172 mg/kg. |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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Targets
Enzymes
