Oxymorphone: Medication Information and Guidelines

Recommended Dose and Dosage Regimen

The recommended dose of oxymorphone varies depending on the patient’s age, weight, medical condition, and response to treatment. For the management of moderate to severe pain, the typical starting dose of oxymorphone extended-release tablets is 10 mg orally every 12 hours, titrated to individual patient needs and tolerability. The dose may be adjusted based on pain intensity and response, with careful consideration of the risk of opioid-related adverse effects and respiratory depression. Oxymorphone immediate-release tablets may be used for breakthrough pain as needed, with initial doses ranging from 5 mg to 10 mg orally every 4 to 6 hours as tolerated. Consult with a healthcare provider for personalized dosing recommendations.

Frequency of Administration

Oxymorphone extended-release tablets are typically administered orally every 12 hours, while immediate-release tablets may be used as needed for breakthrough pain, with dosing intervals ranging from every 4 to 6 hours. The dosing frequency may be adjusted based on individual patient response, pain intensity, and duration of analgesic effect. Patients should be instructed to take oxymorphone exactly as prescribed by their healthcare provider and to avoid exceeding the maximum recommended daily dose to minimize the risk of opioid-related adverse effects and overdose. Regular reassessment of pain intensity and treatment response is essential for optimizing pain management outcomes.

Route of Administration

Oxymorphone is administered orally in the form of extended-release tablets or immediate-release tablets, which should be swallowed whole with a full glass of water to facilitate drug absorption and ensure proper dosing. Oxymorphone extended-release tablets should not be crushed, chewed, or dissolved, as this may lead to rapid release of the drug and increase the risk of overdose. Immediate-release tablets may be administered with or without food, depending on individual patient preference and tolerability. Consult with a healthcare provider or pharmacist for guidance on proper administration techniques and dosing instructions.

Mechanism of Action (MOA)

Oxymorphone is a potent opioid analgesic that acts primarily as a mu-opioid receptor agonist to produce analgesia and euphoria. Oxymorphone exerts its pharmacological effects by binding to mu-opioid receptors in the central nervous system, thereby activating inhibitory G-protein-coupled signaling pathways and inhibiting the transmission of pain signals along ascending pain pathways. This results in modulation of pain perception and nociceptive processing, leading to pain relief and subjective feelings of well-being. Oxymorphone also has affinity for kappa-opioid receptors and delta-opioid receptors, which may contribute to its analgesic efficacy and side effect profile.

Pharmacokinetics (PK)

The pharmacokinetics of oxymorphone are characterized by rapid absorption, extensive distribution, and hepatic metabolism. Oxymorphone is well absorbed after oral administration, with peak plasma concentrations achieved within 1 to 2 hours. The bioavailability of oxymorphone is approximately 10% to 15% due to extensive first-pass metabolism in the liver. Oxymorphone is metabolized primarily by glucuronidation via the uridine diphosphate glucuronosyltransferase (UGT) enzyme system, with inactive metabolites excreted renally. The elimination half-life of oxymorphone is approximately 3 to 6 hours in healthy adults, but may be prolonged in patients with hepatic impairment or renal insufficiency.

Pharmacodynamics (PD)

Oxymorphone exerts its pharmacological effects by binding to mu-opioid receptors in the central nervous system, thereby activating inhibitory G-protein-coupled signaling pathways and inhibiting the transmission of pain signals along ascending pain pathways. This results in modulation of pain perception and nociceptive processing, leading to pain relief and subjective feelings of well-being. Oxymorphone also has affinity for kappa-opioid receptors and delta-opioid receptors, which may contribute to its analgesic efficacy and side effect profile. The analgesic potency of oxymorphone is estimated to be 5 to 10 times greater than that of morphine.

Pathophysiology

Pain is a complex sensory and emotional experience that results from activation of nociceptive pathways in response to tissue injury or inflammation. Moderate to severe pain may arise from various etiologies, including trauma, surgery, cancer, neuropathy, or musculoskeletal disorders. Oxymorphone is indicated for the management of moderate to severe pain in patients who require continuous opioid analgesia for an extended period. Oxymorphone provides effective pain relief by activating mu-opioid receptors in the central nervous system, thereby modulating pain perception and inhibiting nociceptive transmission.

Primary Indications

Oxymorphone is indicated for the management of moderate to severe pain in patients who require continuous opioid analgesia for an extended period. Oxymorphone extended-release tablets are indicated for the treatment of chronic pain that is not adequately controlled with non-opioid analgesics or immediate-release opioids. Oxymorphone immediate-release tablets may be used for breakthrough pain as needed, in addition to around-the-clock opioid therapy. Oxymorphone should be reserved for use in patients who have not responded to non-pharmacological interventions or other analgesic agents, as it carries a high risk of dependence, addiction, and overdose.

Contraindications

Contraindications to oxymorphone use include hypersensitivity to oxymorphone or any component of the formulation, significant respiratory depression, acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment, paralytic ileus, and concurrent use of monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuation of an MAOI. Use caution when prescribing oxymorphone to patients with a history of substance abuse or addiction, respiratory dysfunction, hepatic impairment, renal insufficiency, or head injury, as they may be at increased risk of adverse effects or overdose. Oxymorphone therapy should be initiated at the lowest effective dose and shortest duration necessary to achieve pain relief, with regular monitoring of treatment response and adverse effects.

Purpose of Taking Medication

The purpose of oxymorphone therapy is to provide effective pain relief for patients with moderate to severe pain who require continuous opioid analgesia for an extended period. Oxymorphone acts by binding to mu-opioid receptors in the central nervous system, thereby modulating pain perception and inhibiting nociceptive transmission. Oxymorphone should be used as part of a comprehensive pain management plan that includes non-pharmacological interventions, such as physical therapy, cognitive-behavioral therapy, and interventional procedures, to optimize pain control and functional outcomes.

Usage Instructions

Oxymorphone should be taken exactly as prescribed by your healthcare provider, typically orally every 12 hours for extended-release tablets or as needed for breakthrough pain with immediate-release tablets. Swallow the tablets whole with a full glass of water to facilitate drug absorption and ensure proper dosing. Do not crush, chew, or dissolve oxymorphone extended-release tablets, as this may lead to rapid release of the drug and increase the risk of overdose. Do not exceed the maximum recommended daily dose of oxymorphone to minimize the risk of opioid-related adverse effects and overdose. Follow-up with your healthcare provider regularly to monitor pain intensity, treatment response, and adverse effects.

Precautions and Care

Patients taking oxymorphone should be monitored regularly for signs of opioid-related adverse effects, including respiratory depression, sedation, dizziness, confusion, constipation, and urinary retention. Use caution when prescribing oxymorphone to elderly or debilitated patients, as they may be more sensitive to the effects of opioids and at increased risk of adverse events. Avoid concurrent use of oxymorphone with other central nervous system depressants, including benzodiazepines, sedatives, hypnotics, or alcohol, as this may potentiate respiratory depression and increase the risk of overdose. Oxymorphone therapy should be initiated at the lowest effective dose and shortest duration necessary to achieve pain relief, with regular monitoring of treatment response and adverse effects.

Dietary Considerations

There are no specific dietary restrictions associated with oxymorphone therapy for the management of pain. Patients should maintain adequate hydration and nutritional intake during oxymorphone therapy to support overall health and well-being. Avoid consuming alcohol or grapefruit juice while taking oxymorphone, as they may potentiate the sedative effects of the medication and increase the risk of adverse events. Consult your healthcare provider or pharmacist if you have any questions or concerns about dietary considerations during oxymorphone therapy.

Missed Dose

If a dose of oxymorphone is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. Patients should not double the dose to make up for a missed one. Do not exceed the maximum recommended daily dose of oxymorphone to minimize the risk of opioid-related adverse effects and overdose. Follow the specific dosing regimen prescribed by your healthcare provider for optimal pain management. Regular reassessment of pain intensity and treatment response is essential for optimizing pain control and functional outcomes.

Possible Side Effects

Common side effects of oxymorphone may include constipation, nausea, vomiting, dizziness, drowsiness, headache, dry mouth, and sweating. Less common side effects may include pruritus, urinary retention, orthostatic hypotension, confusion, euphoria, and respiratory depression. Long-term use of oxymorphone may be associated with tolerance, physical dependence, addiction, and opioid use disorder. Contact your healthcare provider if you experience severe or persistent side effects while taking oxymorphone, as they may require medical evaluation or adjustment of therapy.

Storage and Disposal

Oxymorphone tablets should be stored at room temperature away from moisture, heat, and light, in their original packaging. Keep oxymorphone out of reach of children and pets to prevent accidental ingestion or misuse. Unused or expired medication should be disposed of properly according to local guidelines, such as through a medication take-back program or by mixing with an undesirable substance (such as coffee grounds or cat litter) and disposing of in the household trash. Do not flush oxymorphone tablets down the toilet or pour them down the drain, as this may contaminate water sources and harm the environment.

Overdose or Emergency

In case of overdose or emergency, contact your local poison control center or emergency medical services immediately. Symptoms of oxymorphone overdose may include respiratory depression, extreme drowsiness, pinpoint pupils, hypotension, bradycardia, and coma. Emergency medical treatment may be necessary to manage symptoms of overdose, such as airway management, administration of naloxone, and supportive care. Do not attempt to induce vomiting or administer other medications without medical supervision. Always consult with a healthcare professional for personalized medical advice and guidance regarding the use of oxymorphone, especially regarding dosing, administration, and potential side effects.

Important Note: Always consult with a healthcare professional for personalized medical advice and guidance regarding the use of given drug, especially regarding dosing, administration, and potential side effects. Your healthcare provider can provide tailored recommendations based on your individual medical history, current medications, and specific treatment needs. Never self-adjust your given drug regimen or discontinue treatment without first consulting your healthcare provider. If you have any questions or concerns about given drug or its use, talk to your doctor or pharmacist for further information and assistance.