Oxymorphone Hydrochloride

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Cat Number

API357073

CAS Number

357-07-3

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Product Detail Description Scientific Support Customer Q&A

CAS Number

357-07-3

Synonyms

Oxymorphone HCl

Molecular Formula

C17H20ClNO4

Molecular Weight

337.8

Smiles

CN1CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)O)O4)O.Cl

Appearance

Crystalline solid

General Description

Oxymorphone Hydrochloride is a semi-synthetic opioid analgesic derived from thebaine. It is structurally related to morphine but possesses significantly greater analgesic potency.

Mechanism of Action

Oxymorphone agonizes mu-opioid receptors in the central nervous system, activating G-protein-coupled signaling that inhibits adenylate cyclase, closes voltage-gated calcium channels, and opens potassium channels, reducing neuronal excitability and pain transmission.

Application

Used in the management of moderate to severe pain. Oxymorphone Hydrochloride is indicated for acute postoperative pain, cancer pain, and chronic severe pain requiring opioid management.

Oxymorphone is a typical mu-opioid agonist that is effective in both immediate-release and extended-release oral formulations. The mechanism of action involves binding to mu-opioid receptors in the central nervous system, where it alters the perception of and response to painful stimuli while producing generalized central nervous system depression. Oxymorphone is more lipid soluble than morphine, resulting in a rapid onset of action when given in tablet formulation, with a duration of action of approximately 4-6 hours in immediate-release and 12 hours in extended-release preparations. Oral oxymorphone provides excellent pain relief for significant pain including acute postoperative pain, chronic arthritis pain, chronic low back pain, and chronic cancer pain. Multiple double-blind, prospective, placebo-controlled clinical trials have demonstrated the clinical efficacy and safety of this oral opioid formulation.

Fig. 1 Mean single-dose and steady-state plasma concentrations of oxymorphone IR. (Sloan P. 2008)

References

Sloan P. Review of oral oxymorphone in the management of pain. Therapeutics and Clinical Risk Management, 2008, 4(4): 777-787.

What distinguishes Oxymorphone from morphine in pain management?

Oxymorphone provides approximately ten times the analgesic potency of morphine, allowing effective pain control at lower doses with a different metabolic profile.