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Oxymorphone is a lesser-known but potent opioid analgesic prescribed for the management of moderate to severe pain. It was introduced in the U.S. in 1959 and approved by the U.S. Food and Drug Administration (FDA). Although it is recognized for its effectiveness in relieving patients with acute or chronic pain conditions, its powerful analgesic properties carry substantial risks. Over the years, regulatory agencies have implemented stricter guidelines on its prescription and distribution to prevent misuse and related health complications, which include addiction.
In this article, we will explore the medical uses of oxymorphone, its recommended dosage and administration, contraindications, and the potential for misuse. We will also discuss why the extended-release formulation, Opana ER, was discontinued and review options for managing withdrawal or seeking safer pain management alternatives.
- Oxymorphone is a potent opioid prescribed for severe pain, but it carries a high risk of dependence and misuse.
- The FDA requested the withdrawal of Opana ER (the extended-release form of oxymorphone) due to public health risks linked to injection misuse.
- Safer alternatives to oxymorphone, including non-opioid medications and other opioids with lower misuse potential, are available for managing pain.
Understanding oxymorphone
Oxymorphone is a powerful opioid medication derived from thebaine, a natural substance found in opium poppies (Papaver somniferum). [1] It's closely related to some other opioids (like morphine or oxycodone) but has a slightly altered chemical structure, making it especially effective at handling severe or persistent pain.
Providers prescribe oxymorphone in two main forms. There's an immediate-release version, which acts quickly and is indicated for intense or sudden pain. The extended-release form, previously sold under the brand Opana ER (now discontinued), was designed to deliver medication into the bloodstream over several hours, maintaining steady pain relief throughout the day. [2]
How it works
Oxymorphone works by binding to mu-opioid receptors located in the brain and spinal cord. When oxymorphone binds to these receptors, it alters the perception of pain by altering how the brain perceives and responds to pain signals, providing relief. Alongside pain relief, oxymorphone often induces relaxation or drowsiness, which some people find calming. [3]
However, these calming effects can also contribute to misuse or dependence in some people. Because oxymorphone is primarily processed by the liver, individuals with impaired liver or kidney function may require dosage adjustments to avoid side effects or potential drug accumulation. [1]
After taking an immediate-release oxymorphone tablet, relief typically begins within 30 minutes to an hour. Extended-release tablets were specifically developed to maintain steady relief over about 12 hours. They're often used for ongoing, severe pain conditions, like chronic discomfort after physical trauma or cancer-related pain. Given the variability in how individuals respond to opioids, careful supervision by healthcare providers is essential for safe and effective pain management. [4]
Oxymorphone vs. Oxycodone
Oxymorphone and oxycodone are both semisynthetic opioids, but they aren’t the same. Oxymorphone is stronger, so smaller doses provide the same effect. [3] Oxycodone is prescribed more often because it has been in use longer and comes in more forms.
Both can cause drowsiness, nausea, constipation, and slowed breathing. Because oxymorphone is stronger, the risk of serious side effects is more pronounced if it’s not dosed carefully. [1] The choice between them then depends on potency, side effects, effectiveness, and patient-specific factors.
Recommended dosage and administration
Safe dosing of oxymorphone depends on the formulation and the patient’s opioid tolerance. Oxymorphone is available as immediate-release tablets (for as-needed pain relief), extended-release tablets (for continuous pain management), and an injectable formulation (for inpatient use in the hospital). [1]
General guidelines include:
- Immediate-release (IR): This form is typically used for acute pain. For opioid-naïve adults (those not already taking opioids), the starting dose is usually low, often 5 to 10 mg by mouth every 4 to 6 hours as needed. Dosing can be carefully adjusted, based on pain relief and side effects. Some sources note that opioid-naïve patients might start at 5 mg every 4–6 hours, with the option to take another 5 mg if the initial dose is ineffective. [7]
- Extended-release (ER): This form is used for chronic severe pain requiring longer-lasting pain relief. Opioid-naïve patients should start at 5 mg every 12 hours (the lowest ER dose). [1][7] The dose may then be cautiously uptitrated (or increased) by 5–10 mg increments every few days as needed for adequate pain control. [7]
Patients who are already opioid-tolerant (e.g., those who are taking moderate or high doses of another opioid currently or previously) can be started on a calculated equivalent dose of ER oxymorphone. An equianalgesic chart is often used to calculate an equivalent dose, though individual variation requires careful monitoring and dosage adjustments. [6]
Safety considerations
Because of its risks, oxymorphone should be used exactly as prescribed. Patients are warned not to increase their dose or dosing frequency on their own. They should consult their doctor if pain is uncontrolled, rather than taking extra doses. Furthermore, mixing oxymorphone with other opioids, alcohol, benzodiazepines, or other sedatives is dangerous; alcohol intensifies oxymorphone’s sedating effect and can precipitate respiratory failure. [7]
In practice, doctors follow opioid prescribing guidelines and often use the lowest effective dose for the shortest duration to reduce risks.
Oxymorphone side effects and risks
Like all opioids, oxymorphone can cause a spectrum of side effects. Some may be mild and resolve on their own, while others can be severe and warrant immediate medical attention. Below is a table that highlights the potential risks and side effects.
| Details | Management | |
|---|---|---|
| Common side effects |
| These are typically mild and may resolve on their own.Supportive treatments:
|
| Serious adverse effects |
| These require immediate medical attention, as they are potentially life-threatening. |
| Risk factors for complications |
| Patients must disclose all medications and supplements.Careful monitoring is needed to avoid interactions. |
Oxymorphone controlled substance status
Oxymorphone is a Schedule II controlled substance under the U.S. Controlled Substances Act. [1] This classification indicates that while oxymorphone has recognized medical uses, it also has a high potential for abuse and dependence. Doctors must write a new prescription for each fill (no refills allowed on the same prescription), and in many places, these prescriptions must be electronic or on tamper-proof paper.
Clinics, hospitals, and pharmacies must maintain detailed logs of Schedule II medications to ensure they are prescribed and dispensed responsibly. [1]
Illicit uses and risks of addiction
Unfortunately, oxymorphone’s potency and the fact that it is an opioid make it a target for misuse. Taking any amount of a potent opioid may cause adverse effects, dependence, or addiction. When taken without a prescription or in higher doses than prescribed, the risks are even higher for the drug to induce euphoria and lead to physical and psychological dependence. [1] Street names for oxymorphone include “Blue Heaven,” “Blues,” “Mrs. O,” “Pink O,” “Pink Lady,” “Stop Signs,” and “The O Bomb,” in part reflecting the distinct color and branding of specific formulations.
People who non-medically use oxymorphone sometimes crush, snort, or inject different formulations of the drug, with dramatic increases in the risk of overdose and blood-borne infections, like HIV and hepatitis. [4] Prolonged misuse can result in further morbidity and mortality with severe withdrawal symptoms, organ damage, and fatal overdoses.
Why was Opana ER discontinued?
The FDA requested the removal of Opana ER from the market in 2017 due to the “significant risks” associated with its misuse and abuse. [2] There was evidence indicating that people using oxymorphone were crushing the extended-release tablets to use for intravenous injections. The FDA established that the injection of Opana ER led to the spread of HIV and hepatitis C, linked to people sharing needles. [2]
Although the manufacturer voluntarily removed Opana ER from circulation, other formulations of oxymorphone remain available by prescription. Patients currently receiving oxymorphone therapy are advised to discuss alternative pain management strategies or consider different formulations under medical supervision.
Disclaimer:
In 2017, the FDA requested that Endo Pharmaceuticals voluntarily withdraw Opana ER from the market due to concerns about its risks of injection drug use. [7] This decision was influenced by public health risks, including an HIV outbreak in Scott County, Indiana, where Opana ER was identified as a possible factor. However, the available data came from observational studies with small sample sizes, and many of the affected people had used multiple drugs. These factors made isolating Opana ER as the sole cause challenging.
The withdrawal was not due to a direct finding that Opana ER alone caused harm but rather a combination of epidemiological data, regulatory scrutiny, and broader concerns about opioid misuse. Endo Pharmaceuticals ultimately pulled the drug under significant regulatory and public pressure.
Withdrawal symptoms and management
When a person becomes physically dependent on oxymorphone, abruptly stopping or significantly reducing their dose can trigger withdrawal symptoms.
Common withdrawal symptoms include: [1]
- Restlessness
- Muscle and bone pain
- Insomnia
- Diarrhea
- Vomiting,
- Involuntary leg movements
- Severe distress
These symptoms can be severe, and this may drive people to continue using the drug to stave off discomfort.
Managing withdrawal usually involves tapering the drug under medical supervision. Healthcare providers should gradually decrease the dose of oxymorphone or use medication-assisted treatment with a longer-acting opioid or opioid agonist, such as methadone or buprenorphine, along with supportive therapies, like therapy and counseling, plus psychosocial support. [6]
In severe cases, it is recommended that a person receive medically supervised detoxification.
Alternative options
Given the high risk of dependence, many healthcare providers explore safer alternatives before prescribing oxymorphone.
Non-opioid pain relievers, such as acetaminophen or nonsteroidal anti-inflammatory drugs (NSAIDs), can be effective for mild to moderate pain. [3] Neuropathic pain, for example, can be managed with adjuvant medications, like antidepressants or anticonvulsants. [4]
Other interventional and integrative methods, like physical therapy, acupuncture, and nerve blocks, can help reduce reliance on chronic opioid use for pain. This multimodal analgesic approach reduces reliance on opioids while maintaining effective pain management. If an opioid is necessary, substances like tramadol or tapentadol—while still carrying risks—may offer a somewhat lower potential for misuse and dependence. [6]
Pain management should be tailored, balancing therapeutic benefits with potential risks.
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