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- Oxymorphone
Oxymorphone API Manufacturers & Suppliers
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Oxymorphone | CAS No: 76-41-5 | GMP-certified suppliers
A medication that provides potent analgesia for managing moderate-to-severe pain and serves as an adjunct to anesthesia in clinical settings.
Therapeutic categories
Primary indications
- For the treatment of moderate-to-severe pain
Product Snapshot
- Oxymorphone is available as injectable, oral, and suppository formulations including extended-release tablets and parenteral options
- It is primarily indicated for the management of moderate-to-severe pain
- The product holds approved status in the US and Canada markets
Clinical Overview
Pharmacodynamically, oxymorphone exerts potent analgesic effects primarily through central nervous system activity. It binds selectively to mu-opioid receptors, which are distributed across several brain regions including the posterior amygdala, hypothalamus, thalamus, basal ganglia structures such as the nucleus caudatus and putamen, as well as in spinal cord laminae I and II. The interaction with mu-receptors modulates pain by inhibiting GABAergic interneurons that normally suppress descending pain inhibitory pathways, thereby enhancing endogenous pain control mechanisms.
The therapeutic actions of oxymorphone include analgesia and sedation. Respiratory depression is a significant pharmacological effect caused by reduced responsiveness of brainstem respiratory centers to carbon dioxide and neural stimuli, representing a critical safety consideration. As with other opioids, oxymorphone carries risks of misuse, dependence, and abuse. Notably, the FDA requested removal of the injectable formulation from the U.S. market in 2017 due to concerns over abuse potential.
Key ADME characteristics involve hepatic metabolism primarily via cytochrome P450 isoforms CYP2D6 and CYP3A4, with resultant active and inactive metabolites. These metabolic pathways may affect pharmacokinetic profiles and drug interaction potential, necessitating consideration in clinical use and formulation.
Oxymorphone is categorized among high-risk opioids and requires strict regulatory controls. It is approved for human use in several jurisdictions, with veterinary approvals in select contexts.
For API procurement, sourcing should prioritize manufacturers adhering to stringent quality standards, including compliance with Good Manufacturing Practice (GMP) and regulatory certifications. Due to its controlled status and abuse potential, secure supply chains with robust documentation and traceability are essential for ensuring product integrity and regulatory compliance.
Identification & chemistry
| Generic name | Oxymorphone |
|---|---|
| Molecule type | Small molecule |
| CAS | 76-41-5 |
| UNII | 9VXA968E0C |
| DrugBank ID | DB01192 |
Pharmacology
| Summary | Oxymorphone is a semi-synthetic opioid analgesic that primarily targets mu-opioid receptors distributed in central and spinal nervous system regions involved in pain processing. It induces analgesia by inhibiting GABAergic interneurons, thereby facilitating descending pain inhibition pathways. Additionally, oxymorphone affects delta-opioid receptors and exerts central nervous system effects including sedation and respiratory depression through modulation of brainstem respiratory centers. |
|---|---|
| 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 (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. Also, it has been shown that oxymorphone binds to and inhibits GABA inhibitory interneurons via mu-receptors. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream. |
| Pharmacodynamics | 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 centers. The mechanism of respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Mu-type opioid receptor | Humans | agonist |
| Delta-type opioid receptor | Humans | antagonist |
ADME / PK
| Half-life | 1.3 (+/-0.7) hours |
|---|---|
| Metabolism | 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. |
Formulation & handling
- Oxymorphone is available in multiple dosage forms including oral tablets, extended-release formulations, suppositories, and parenteral injections suitable for intramuscular, intravenous, and subcutaneous administration. As a small molecule opioid agonist, it requires dosing on an empty stomach to avoid variability in absorption caused by food intake. Handling should consider its moderate water solubility and the contraindication to co-administer with alcohol due to potential CNS depression and altered pharmacokinetics.
Regulatory status
| Lifecycle | The API is in a late patent expiry phase in the United States, with key patents expiring between 2013 and 2027, reflecting a gradually increasing opportunity for generic competition in the US and Canadian markets. Market presence in these regions corresponds with a transition toward greater market maturity. |
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| Markets | US, Canada |
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Supply Chain
| Supply chain summary | The manufacturing and supply landscape for oxymorphone involves multiple originator companies producing and packaging branded products primarily in the US and Canadian markets. The presence of several patents extending through to 2027 indicates ongoing patent protection, suggesting limited generic competition currently but potential for increased generic entry upon patent expirations in the coming years. Branded formulations include various dosage forms such as injections and suppositories, supporting a broad product offering in North American markets. |
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Safety
| 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. Patients experiencing an overdose may develop apnea, circulatory collapse, and cardiac arrest. Intravenous mouse LD<sub>50</sub> is 172 mg/kg. |
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- Oxymorphone may cause severe respiratory depression and central nervous system depression upon overexposure
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Oxymorphone is a type of Opioid analgesics
Opioid analgesics are a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are commonly used for pain management. These potent substances interact with specific receptors in the central nervous system, producing analgesic effects and reducing the perception of pain. Opioid analgesics are derived from opium alkaloids or synthetic compounds that mimic their effects. They are classified based on their strength, with some being classified as strong opioids (e.g., morphine, fentanyl) and others as weak opioids (e.g., codeine, tramadol). These APIs work by binding to opioid receptors, primarily located in the brain, spinal cord, and gastrointestinal tract. By activating these receptors, opioid analgesics modulate pain signals, resulting in pain relief. Additionally, they can induce feelings of euphoria, sedation, and respiratory depression, which can be both beneficial and potentially harmful.
Due to their potency and potential for abuse, opioid analgesics are tightly regulated substances. They are primarily prescribed for acute and chronic pain management, such as post-surgical pain, cancer pain, and severe injuries. However, their misuse and addiction potential have led to a public health crisis in many countries.
In conclusion, opioid analgesics are a subcategory of pharmaceutical APIs that play a crucial role in pain management. While they provide effective pain relief, their use requires careful monitoring and adherence to prescribing guidelines to mitigate the risks associated with their potential for abuse and addiction.
Oxymorphone (Opioid analgesics), classified under Analgesics
Analgesics are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are commonly used to relieve pain. They are designed to alleviate discomfort by targeting the body's pain receptors or by reducing inflammation. Analgesics are widely utilized in the medical field to manage various types of pain, ranging from mild to severe.
One of the primary classes of analgesics is nonsteroidal anti-inflammatory drugs (NSAIDs). NSAIDs work by inhibiting the production of prostaglandins, substances that contribute to pain and inflammation. This class includes well-known drugs like ibuprofen and naproxen. Another class of analgesics is opioids, which are derived from opium or synthetic compounds that mimic the effects of opium. Opioids act on the central nervous system to reduce pain perception and provide potent pain relief. Examples of opioids include morphine, codeine, and oxycodone.
Analgesics are available in various forms, such as tablets, capsules, creams, and injections, allowing for different routes of administration based on the patient's needs. They are commonly used to manage pain associated with conditions like arthritis, headaches, dental procedures, and post-operative recovery.
It is important to note that analgesics should be used under medical supervision, as improper use or overuse can lead to adverse effects, including gastrointestinal complications, addiction, and respiratory depression in the case of opioids. Therefore, it is crucial for healthcare professionals to assess each patient's individual needs and prescribe the appropriate analgesic and dosage.
In summary, analgesics are a vital category of pharmaceutical APIs used to alleviate pain by targeting pain receptors or reducing inflammation. With various classes and forms available, they provide valuable options for pain management when used responsibly and under medical guidance.
