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Taking Advantage of the Peripheral Opioid Receptor

Opioids applied in a topical cream that directly target the peripheral opioid receptors (which grow in inflammatory pain sites to attract natural endorphin compounds for pain relief and immune enhancement) may have advantages relative to oral opioids.
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Advantages of Topical Opioids

There are many advantages of topical opioids compared to oral opioids. They are inexpensive, safe, non-abusable, and give the patient great control over their condition. Topical opioids allow the chronic pain patient to control flares and breakthrough episodes. Fewer oral opioids are required and may not even be required in some cases. A summary of the benefits of topical opioids is presented in Table 3.

Table 3. Advantages of Topical Opioids
  • Inexpensive
  • Safe—no known side effects
  • Pain control in localized areas
  • Use less of oral opioids
  • Non-abusable
  • Patient self control
  • No liver metabolism required

Unanswered Question

To date, reports of topical opioids have been in chronic pain patients who also take systemic opioids.6,8 The question is “Should topical opioids be used as a clinical trial before systemic opioids are initiated?” An alternate formulation of the question is “Should topical opioids be used in acute pain and in the early stages of chronic pan rather than oral opioids?” For example, should topical opioids be used for post-operative or post-injury pain before resorting to oral opioids? Any readers of this article who have used topical opioids in acute pain or in lieu of oral opioids should report their results and help us answer this question.


The discovery of the peripheral opioid receptor and conceptualization of the inflammatory pain site are helping to advance practical pain care. Peripheral opioid receptors grow in inflammatory pain sites to attract natural endorphin compounds for pain relief and immune enhancement. Patients report outstanding relief with topical opioids and their delivery to the pain site is enhanced by electro-magnetic devices which drive the opioid through the skin into deep tissue compartments. Topical opioids are inexpensive, safe, and effective enough to be given trials to substitute for oral opioids.

Last updated on: December 28, 2011