Opioid tapering under the umbrella of palmitoylethanolamide

The interpretation of opioid prescribing trends over the past decade is the subject of current international debate. In the United States and Australia the increased prescribing of opioids has been paralleled by problems of misuse and opioid related harms. Their use however is limited by adverse effects, such as constipation tolerance, and
withdrawal syndrome. Not only increasing the death and hospital admissions due to opioid side effects, but the problem of hyperalgesia induced by chronic opioid use is an increasing recognized issue. At the EFIC in FLorence it was also pointed out:

Although similar trends in prescribing are seen in Europe, the extent to which these drugs are misused is unknown but the prescription data suggest that many patients may be taking opioids without clinical benefit. (From: OPIOID USE FOR PERSISTENT PAIN: A 21ST CENTURY PERSPECTIVE by C. Stannard)

Reasons for opioid tapering

• Inadequate analgesia. Patients with severe pain and disability
despite a high dose (above 200 mg morphine equivalent per day)
often experience improved pain, function and mood with tapering.
• Side effects or medical complications. Adverse effects primarily
include sedation, constipation, falls in the elderly, sleep apnea,
and overdose. Most of these side effects are dose-related.
• Opioid misuse and addiction. Patients who are addicted but
primarily acquire their opioids from their physician may receive
‘structured opioid therapy,’ with tapering, frequent dispensing (as
often as daily), and urine drug screening. If this fails or if the
patient acquires opioids from multiple physicians or the street,
methadone or buprenorphine treatment may be needed.

Slow tapering is recommended: “Taper slowly; ate may vary from 10% of the total daily dose EVERY DAY to 10% of
total daily dose EVERY 1-2 WEEKS, the latter is prefered for outpatient tapering.”


Opioid tapering under the umbrella of palmitoylethanolamide

structure of palmitoylethanolamide

structure of palmitoylethanolamide

Currently various pain physicians in the world are started to explore the value of palmitoylethanolamide in tapering off from opioids. Treatment with opioids can induce hyperalgesia in humans and animals, and activation of Toll-like receptor 4 (TLR4) has been proposed to induce such hyperalgesia. Furthermore other routes exist to hyperactivate glia and non-neuronal cells.

Palmitoylethanolamide is a known inhibitor of these non-neuronal pathways and of the Toll-4 pathway, and thus it can be used for directly counteract hyperalgesia induced by opioids, and due to its analgesic and anti-inflammatory effect, it can be substituted for opioids if a rational taper off- taper in schedule is chosen.

We suggest the following: start palmitoylethanolamide 3 times 400 mg and after 2 weeks start tapering off opioids in a very gradual step by step fashion. If pain does not decrease sufficiently, try increasing the PEA umbrella to the double dose (2400 mg/day). PEA is known to enhance the analgesic effects of low dose opioids, and so there are different reasons for using the combination opioids-PEA and use the PEA umbrella to tapering off opioids.

Esposito G, Capoccia E, Turco F, Palumbo I, Lu J, Steardo A, Cuomo R, Sarnelli G, Steardo L. Palmitoylethanolamide improves colon inflammation through an enteric glia/toll like receptor 4-dependent PPAR-α activation. Gut. 2013 Sep 30. doi: 10.1136/gutjnl-2013-305005.

Hanke ML, Kielian T Toll-like receptors in health and disease in the brain: mechanisms and therapeutic potential. Clin Sci (Lond). 2011 Nov 1 121(9)367-87

RAT MODEL OF POSTOPERATIVE PAIN by M.Á. Martínez-García et al.

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