Descrição
Oxymorphone – Potent Opioid Analgesic (Rx, Controlled Substance)
Oxymorphone is a semi-synthetic opioid analgesic indicated for the management of moderate to severe pain requiring continuous, around-the-clock treatment when alternative therapies are inadequate. It acts primarily as a µ-opioid receptor agonist, producing analgesia through inhibition of ascending pain pathways, alteration of the perception of and response to pain, and generalized CNS depression.
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Oxymorphone is available in immediate-release (IR) formulations for acute pain and extended-release (ER) formulations for chronic pain requiring long-term opioid therapy. Due to its high potency and risk profile, it is classified as a controlled substance and must be prescribed and monitored carefully.
Key Details
- Active Ingredient: Oxymorphone hydrochloride
- Drug Class: Opioid analgesic (µ-opioid receptor agonist)
- Indication: Moderate to severe pain
- Formulations: Immediate-release (IR) and extended-release (ER) tablets
- Prescription Status: Controlled prescription-only medication
- Therapeutic Use: Acute and chronic pain management
Specifications
- Dosage Forms: Oral tablets (IR and ER)
- Common Strengths:
- IR: 5 mg, 10 mg
- ER: 5 mg, 10 mg, 20 mg, 40 mg
- Onset of Action (IR): ~30 minutes
- Peak Effect (IR): ~1 hour
- Duration:
- IR: ~4–6 hours
- ER: ~12 hours
- Half-Life:
- IR: ~7–9 hours
- ER: prolonged due to formulation
- Metabolism: Hepatic (primarily via glucuronidation; minimal CYP involvement)
- Excretion: Renal
- Administration: Oral, typically on an empty stomach for consistent absorption
Dosage & Administration
- Dose must be individualized based on pain severity, prior opioid exposure, and patient response
- ER formulations are typically administered every 12 hours
- Should be initiated at the lowest effective dose and titrated carefully
- Must not be crushed or chewed (ER formulations)
Compatibility / Suitable Use
- Adults requiring opioid-level analgesia
- Patients with moderate to severe pain unresponsive to non-opioid treatments
- Suitable for opioid-tolerant patients (especially ER formulations)
- Requires strict medical supervision and monitoring
Contraindications
- Significant respiratory depression
- Acute or severe bronchial asthma (unmonitored settings)
- Known or suspected gastrointestinal obstruction
- Hypersensitivity to oxymorphone
Warnings & Precautions
- High risk of respiratory depression, especially during initiation or dose escalation
- Potential for addiction, abuse, and misuse
- Risk of overdose and death, particularly if misused
- May cause sedation, hypotension, and CNS depression
- Use caution in elderly patients, hepatic or renal impairment
- Avoid concurrent use with alcohol or other CNS depressants
Adverse Effects
- Common: Nausea, vomiting, constipation, dizziness, sedation
- Serious: Respiratory depression, hypotension, dependence
- Long-term use: Tolerance, physical dependence
Drug Interactions
- CNS depressants (benzodiazepines, alcohol): Increased sedation and respiratory depression
- Other opioids: Additive effects
- Limited CYP interactions (primarily glucuronidation pathway)
Why Use Oxymorphone?
Oxymorphone provides potent analgesia for patients with severe pain when other treatments are insufficient. Its availability in both immediate and extended-release formulations allows for flexible pain management strategies, though its use requires careful clinical oversight due to its safety profile.