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Repositioning Candidate Details

Candidate ID: R0141
Source ID: DB00497
Source Type: approved; illicit; investigational
Compound Type: small molecule
Compound Name: Oxycodone
Synonyms:
Molecular Formula: C18H21NO4
SMILES: [H][C@@]12OC3=C(OC)C=CC4=C3[C@@]11CCN(C)[C@]([H])(C4)[C@]1(O)CCC2=O
Structure:
DrugBank Description: Oxycodone is a semisynthetic opioid analgesic derived from thebaine in Germany in 1917.[A178696] It is currently indicated as an immediate release product for moderate to severe pain and as an extended release product for chronic moderate to severe pain requiring continuous opioid analgesics for an extended period.[Label] The first oxycodone containing product, Percodan, was approved by the FDA on April 12, 1950.[L6460]
CAS Number: 76-42-6
Molecular Weight: 315.3636
DrugBank Indication: Oxycodone is indicated for the treatment of moderate to severe pain.[Label] There is also an extended release formulation indicated for chronic moderate to severe pain requiring continuous opioid analgesics for an extended period.[Label]
DrugBank Pharmacology: Oxycodone acts directly on a number of tissues not related to its analgesic effect. These tissues include the respiratory centre in the brain stem, the cough centre in the medulla, muscles of the pupils, gastrointestinal tract, cardiovascular system, endocrine system, and immune system.[Label] Oxycodone's effect on the respiratory centre is dose dependant respiratory depression.[Label] The action on the cough centre is suppression of the cough reflex.[Label] Pupils become miopic or decrease in size, peristalsis of the gastrointestinal tract slows, and muscle tone in the colon may increase causing constipation.[Label] In the cardiovascular system histamine may be released leading to pruritis, red eyes, flushing, sweating, and decreased blood pressure.[Label] Endocrine effects may include increased prolactin, decreased cortisol, and decreased testosterone.[Label] It is not yet known if the effects of opioids on the immune system are clinically significant.[Label]
DrugBank MoA: The full mechanism of oxycodone is not known.[Label] Under conditions of inflammation or hyperalgesia, opioid receptors in the heart, lungs, liver, gastrointestinal tract, and reproductive system are upregulated and transported to nerve terminals.[A178696] Oxycodone and its active metabolites, noroxycodone, oxymorphone, and noroxymorphone are opioid agonists.[A178639] These compounds passively diffuse across the blood brain barrier or may be actively transported across by an unknown mechanism.[A178696] Oxycodone and its active metabolites can selectively bind to the mu opioid receptor, but also the kappa and delta opioid receptors in the central nervous system and periphery, and induce a G protein coupled receptor signalling pathway.[A178696] Activation of mu opioid receptors inhibits N-type voltage operated calcium channels, inhibiting responses to pain.[A178735]
Targets: Mu-type opioid receptor; Kappa-type opioid receptor; Delta-type opioid receptor
Inclusion Criteria: