Commonly Used Opioids for Pain Management
Morphine, oxycodone, hydromorphone, and fentanyl are the most commonly used opioids for pain management, with morphine being the standard first-choice opioid for moderate to severe pain. 1
Classification of Opioids by Pain Intensity
Mild to Moderate Pain (WHO Step II)
- Codeine (tablets 15-30-60 mg, duration 4-6 hours, max daily dose 360 mg) 1
- Tramadol (capsules 50 mg or drops 100 mg/ml, duration 2-4 hours, max daily dose 400 mg) 1
- Dihydrocodeine (modified-release tablets 60-90-120 mg, duration 12 hours, max daily dose 240 mg) 1
Moderate to Severe Pain (WHO Step III)
- Morphine (oral and parenteral forms, considered gold standard, no upper dose limit) 1
- Oxycodone (oral, 1.5-2 times more potent than oral morphine) 1
- Hydromorphone (oral, 7.5 times more potent than oral morphine) 1
- Fentanyl (transdermal, 4 times more potent than oral morphine) 1
- Methadone (oral, 4-12 times more potent than oral morphine depending on dose) 1
- Buprenorphine (oral and transdermal forms) 1
First-Line Opioid Selection
- Oral morphine is the opioid of first choice for moderate to severe cancer pain due to its effectiveness, tolerability, simple administration, and low cost 1
- For patients with severe pain requiring urgent relief, parenteral opioids (intravenous or subcutaneous) are recommended 1
- The relative potency ratio of oral to parenteral morphine is between 1:2 and 1:3 1
Special Considerations for Specific Opioids
Morphine
- Standard starting drug for opioid-naïve patients 1
- Initial oral dose of 5-15 mg or 2-5 mg IV for opioid-naïve patients 1
- Should be avoided in patients with renal disease and hepatic insufficiency due to accumulation of active metabolite morphine-6-glucuronide 1
Methadone
- More complicated to use due to marked inter-individual differences in plasma half-life and duration of action 1
- Should be initiated only by physicians with experience and expertise in its use 1
- Requires careful titration due to long half-life (8 to >120 hours) 1
Fentanyl
- Transdermal fentanyl is not indicated for rapid opioid titration 1
- Should only be used after pain is controlled by other opioids 1
- Conversion from IV to transdermal fentanyl can use a 1:1 conversion ratio 1
Not Recommended Opioids
- Mixed agonist-antagonists (butorphanol, pentazocine) 1
- Propoxyphene (contraindicated for chronic pain, especially with renal impairment) 1
- Meperidine (contraindicated for chronic pain due to neurotoxicity risk) 1
Clinical Pitfalls and Caveats
- Opioid selection should consider the patient's pain intensity, current analgesic therapy, and concomitant medical conditions 1
- Individual patients vary greatly in their response to different opioids, necessitating individualized approaches 1
- Opioids with short half-lives (morphine, hydromorphone, fentanyl, oxycodone) are preferred for titration compared to those with long half-lives (methadone, levorphanol) 1
- All opioids carry risks of tolerance, dependence, and potential for abuse 2, 3
- When switching between opioids, use caution with dose conversion as relative effectiveness varies considerably among patients 1
- For patients with refractory pain, opioid rotation may improve the therapeutic window and establish a more advantageous analgesia/toxicity relationship 1
By understanding the pharmacological properties, relative potencies, and specific considerations for each opioid, clinicians can make informed decisions to optimize pain management while minimizing adverse effects.