====== Oxycodone (Roxicodone®, OxyContin®) ======

<WRAP right 340px>
<WRAP infobox>
^ Oxycodone | {{ :neuro:opioids:oxycodone.svg?200 |}} |
| Brand Names | Roxicodone®, OxyContin®, Percocet®, Endocet® |
| Drug Class | [[neuro:opioids:start|Opioid]] (Full μ-agonist) |
| Primary Indication | Moderate–Severe Pain |
| Relative Potency | ~1.5× Morphine (oral) |
| Hypoglycemia Risk | N/A |
| Respiratory Depression | Yes (dose-dependent) |
| Weight Effect | Neutral |
| Elimination | Hepatic metabolism |
| Controlled Substance | Schedule II |
| FDA Approval | 1950 |
</WRAP>
</WRAP>

===== Overview =====

Oxycodone is a full μ-opioid receptor agonist used for the management of moderate to severe pain.

It has good oral bioavailability compared to morphine and is available in both immediate-release (IR) and extended-release (ER) formulations.

As a full agonist, oxycodone produces dose-dependent analgesia with no ceiling effect, but also carries dose-dependent risk of respiratory depression.

<WRAP clear></WRAP>

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===== Mechanism of Action =====

**Receptor Activity**
  * Full μ-opioid receptor agonist  
  * Gi-protein coupled receptor activation  

**Cellular Effects**
  * ↓ cAMP production  
  * ↑ Potassium efflux → neuronal hyperpolarization  
  * ↓ Calcium influx → ↓ substance P & glutamate release  

**Net Effect**
  * Decreased nociceptive transmission  
  * Altered perception of pain  

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===== Indications =====

  * Acute moderate to severe pain  
  * Chronic pain requiring opioid therapy  
  * Cancer-related pain  
  * Postoperative pain  

Extended-release formulations:
  * Reserved for chronic pain requiring around-the-clock therapy  

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<WRAP contra>
===== Contraindications =====

Absolute:
  * Significant respiratory depression  
  * Acute severe bronchial asthma  
  * Paralytic ileus  

Relative / Caution:
  * Hepatic impairment  
  * Renal impairment  
  * Elderly patients  
  * Obstructive sleep apnea  
  * Concurrent benzodiazepine use  
</WRAP>

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<WRAP details>
===== Dosing =====

Immediate-Release:
  * 5–15 mg every 4–6 hours as needed  

Extended-Release:
  * Dosed every 12 hours  

Dose adjustments required:
  * Hepatic impairment  
  * Renal impairment  

See:
  * [[neuro:opioids:equianalgesic_dosing|Equianalgesic Dosing Guide]]
</WRAP>

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<WRAP details>
===== Pharmacokinetics =====

Absorption:
  * Oral; high bioavailability (~60–87%)  

Metabolism:
  * CYP3A4 → noroxycodone (inactive)  
  * CYP2D6 → oxymorphone (active metabolite)  

Half-life:
  * IR: ~3–4 hours  
  * ER: ~12 hours  

Elimination:
  * Primarily hepatic metabolism with renal excretion of metabolites  
</WRAP>

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<WRAP details>
===== Adverse Effects =====

Common:
  * Sedation  
  * Constipation  
  * Nausea / vomiting  
  * Pruritus  
  * Dizziness  

Serious:
  * Respiratory depression  
  * Hypotension  
  * Physical dependence  
  * Opioid use disorder  

Constipation persists despite tolerance.

</WRAP>

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<WRAP details>
===== Drug Interactions =====

CYP3A4 inhibitors (↑ levels):
  * Azoles  
  * Macrolides  
  * Protease inhibitors  

CYP3A4 inducers (↓ levels):
  * Rifampin  
  * Carbamazepine  

CNS depressants:
  * Benzodiazepines  
  * Alcohol  
  * Other opioids  

Risk: additive respiratory depression  

</WRAP>

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<WRAP monitoring>
===== Monitoring =====

Clinical:
  * Pain control  
  * Sedation level  
  * Respiratory rate  

Risk monitoring:
  * Signs of misuse or dependence  
  * PDMP checks when appropriate  

</WRAP>

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<WRAP pearls>
===== Clinical Pearls =====

  * Full μ agonist → no ceiling effect.  
  * Higher oral bioavailability than morphine.  
  * CYP3A4 interactions significantly affect serum levels.  
  * Often combined with acetaminophen — monitor total daily APAP dose.  
  * Schedule II controlled substance.  
</WRAP>

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===== Toxicity =====

Classic opioid toxidrome:
  * CNS depression  
  * Respiratory depression  
  * Miosis  
  * Decreased bowel sounds  

Treatment:
  * [[neuro:opioids:naloxone|Naloxone]]

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===== Comparison Within Class =====

Compared to [[neuro:opioids:morphine|Morphine]]:
  * Better oral bioavailability  
  * Less histamine release  

Compared to [[neuro:opioids:hydromorphone|Hydromorphone]]:
  * Less potent  

Compared to [[neuro:opioids:hydrocodone|Hydrocodone]]:
  * Slightly more potent  

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===== Related =====

  * [[neuro:opioids:start|Opioids]]
  * [[neuro:opioids:morphine|Morphine]]
  * [[neuro:opioids:hydromorphone|Hydromorphone]]
  * [[neuro:opioids:oxymorphone|Oxymorphone]]
  * [[neuro:opioids:naloxone|Naloxone]]