Overview
| Generic Names: | Dihydrohydroxycodeinone; Dihydrohydroxycondeinone; Dihydrone; Oxicodona [INN-Spanish]; Oxycodone Hcl; Oxycodone Hydrochloride; Oxycodonum [INN-Latin]; PTI-821; oxycodone |
|---|---|
| Trade Names: | Combunox; Dihydroxycodeinone; Dinarkon; Diphydrone; Endocet; Endodan; Endone; Eubine; Eucodal; Eucodalum; Eukodal; Eutagen; Oxanest; Oxicon; Oxicone; Oxikon; OxyFAST; OxyIR; OxyNorm; Oxycodeinone; Oxycodon; Oxycon; Oxycontin; Pancodine; Percobarb; Percodan; Percolone; Remoxy; Roxicodone; Supendol; Supeudol; Tecodin; Tekodin; Thecodine; Thekodin |
| Brand Mixtures: | Combunox (Ibuprofen + Oxycodone Hydrochloride); Endocet (Acetaminophen + Oxycodone Hydrochloride); Endodan (Aspirin + Oxycodone Hydrochloride); Percocet (Acetaminophen + Oxycodone Hydrochloride); Percodan (Aspirin + Oxycodone Hydrochloride); Rivacocet (Acetaminophen + Oxycodone Hydrochloride); Roxicet (Acetaminophen + Oxycodone Hydrochloride); Roxiprin (Aspirin + Oxycodone Hydrochloride); Tylox (Acetaminophen + Oxycodone Hydrochloride) |
| PharmGKB Accession Id: | PA450741 |
Description
Semisynthetic derivative of codeine that acts as a narcotic analgesic more potent and addicting than codeine. PubChem (source: Drug Bank)
Indication
For the treatment of diarrhoea, pulmonary oedema and for the relief of moderate to moderately severe pain. (source: Drug Bank)
ATC Therapeutic Category
- N02AA:Natural opium alkaloids
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Oxycodone acts as a weak agonist at mu, kappa, and delta opioid receptors within the central nervous system (CNS). Oxycodone primarily affects mu-type opioid receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as oxycodone also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability. (source: Drug Bank)
Pharmacology
Oxycodone, a semisynthetic opiate agonist derived from the opioid alkaloid, thebaine, is similar to other phenanthrene derivatives such as hydrocodone and morphine. Oxycodone is available in combination with aspirin or acetaminophen to control pain and restless leg and Tourette syndromes. (source: Drug Bank)
Food Interactions
Take without regard to meals. Avoid alcohol. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
45% (source: Drug Bank)
Absorption
Well absorbed with an oral bioavailability of 60% to 87% (source: Drug Bank)
Toxicity
Symptoms of overdose include respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, bradycardia, hypotension, and death. (source: Drug Bank)
Isomeric SMILES Code:
CN1CC[C@]23c4c5ccc(c4O[C@H]2C(=O)CC[C@]3([C@H]1C5)O)OC (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
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ABCB1 |
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CYP2D6 |
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CYP3A |
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CYP3A4 |
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CYP3A5 |
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OPRM1 |
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Publications |
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UGT2B7 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| OPRD1 |
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(source: Drug Bank) |
| OPRK1 |
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(source: Drug Bank) |
| OPRM1 |
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(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| cimetidine |
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Cimetidine increases the effect of the narcotic (source: Drug Bank) |
| citalopram |
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Increased risk of serotonin syndrome (source: Drug Bank) |
| escitalopram |
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Increased risk of serotonin syndrome (source: Drug Bank) |
| fluoxetine |
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Increased risk of serotonin syndrome (source: Drug Bank) |
| fluvoxamine |
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Increased risk of serotonin syndrome (source: Drug Bank) |
| naltrexone |
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Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals (source: Drug Bank) |
| paroxetine |
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Increased risk of serotonin syndrome (source: Drug Bank) |
| sertraline |
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Increased risk of serotonin syndrome (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Drug interaction with drug |
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Publications |
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Pain |
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Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.
