dopetalk does not endorse any advertised product nor does it accept any liability for it's use or misuse

This website has run out of funding so feel free to contribute if you can afford it (see footer)

Author Topic: the peripheral opiate receptors-i had no idea these even existed  (Read 3626 times)

Offline clinton (OP)

  • Jr. Member
  • **
  • Join Date: Nov 2015
  • Location: kansas city mo
  • Posts: 151
  • Reputation Power: 8
  • clinton is new on the scene.
  • Gender: Male
  • Last Login:May 13, 2016, 05:09:47 AM
  • Harm Reduction & Safe Using
http://www.practicalpainmanagement.com/treatments/pharmacological/opioids/taking-advantage-peripheral-opioid-receptor

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.



History may arguably show the discovery of the peripheral opioid receptor to be the most important clinical discovery in pain treatment in the past 20 years.1-6 This critical finding gives the practitioner and patient many therapeutic options other than oral opioids. About a year ago in these pages, I encouraged the use of topical morphine. Since that note, I have received much correspondence about the use of other topical opioids and I too have been experimenting with opioids other than morphine. In this effort, I have even encountered some patients who use topical morphine in enough quantity to produce a measurable blood level and some patients even report analgesic effects distant to the local, applied area. Of particular benefit has been the use of topical opioids for knee and spine pain.

The Inflammatory Pain Site
Shown here is an artist's rendition of the anatomical pain site (See Figure 1). It is fundamentally a wound in that it contains inflammatory compounds, sequestered electrical charges, and opioid receptors which are now known to propagate in inflamed tissue.7 The natural function of opioid receptors in inflammatory pain sites is to presumably attract the body's natural endorphin compounds for pain relief and immune enhancement. Re-tained or sequestered electrical charges in the pain site generate pain. The removal or displacement of sequestered electrical charges by various electromagnetic means including such simple measures as copper or magnets and various electromagnetic instruments—including electric currents, ultrasound, radiofrequency, infrared, and laser—are generally effective in reducing pain when electromagnetic measures are concomitantly used with topical opioids.





 

 
Home » Pain Treatments » Pharmacological » Opioids
 DOWNLOAD  EMAIL  PRINT  TWEET
 Subscribe or renew to PPM
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.
By Forest Tennant, MD, DrPH
Page 1 of 2
   141  
History may arguably show the discovery of the peripheral opioid receptor to be the most important clinical discovery in pain treatment in the past 20 years.1-6 This critical finding gives the practitioner and patient many therapeutic options other than oral opioids. About a year ago in these pages, I encouraged the use of topical morphine. Since that note, I have received much correspondence about the use of other topical opioids and I too have been experimenting with opioids other than morphine. In this effort, I have even encountered some patients who use topical morphine in enough quantity to produce a measurable blood level and some patients even report analgesic effects distant to the local, applied area. Of particular benefit has been the use of topical opioids for knee and spine pain.

The Inflammatory Pain Site
Shown here is an artist's rendition of the anatomical pain site (See Figure 1). It is fundamentally a wound in that it contains inflammatory compounds, sequestered electrical charges, and opioid receptors which are now known to propagate in inflamed tissue.7 The natural function of opioid receptors in inflammatory pain sites is to presumably attract the body's natural endorphin compounds for pain relief and immune enhancement. Re-tained or sequestered electrical charges in the pain site generate pain. The removal or displacement of sequestered electrical charges by various electromagnetic means including such simple measures as copper or magnets and various electromagnetic instruments—including electric currents, ultrasound, radiofrequency, infrared, and laser—are generally effective in reducing pain when electromagnetic measures are concomitantly used with topical opioids.


Figure 1. Illustration of the inflammatory pain site.

Which Opioids?
Not all opioids provide topical pain relief. The opioids most commonly prescribed by the author are: (1) morphine; (2) hydromorphone; and (3) oxycodone. Although not officially classified as an opioid, carisoprodol, the notorious and abusable Soma®, produces considerable analgesia when topically applied. Some patients use methadone topically and find it effective. There are some opioids that are inert on the skin surface. Hydrocodone, codeine, and tramadol are pro-drugs which require liver metabolism to convert them to active compounds. Fentanyl is extremely soluble and dissolves quickly through the skin making it a very effective systemic, but poor topical opioid. Morphine, hydromorphone, and oxycodone are relatively insoluble and act directly on opioid receptors without requiring further metabolism.

Making The Topical Preparation
I teach patients to obtain a low cost cold cream and crush oral opioid tablets to mix in the cold cream. Inexpensive standard dosage oral tablets are recommended. Table 1 presents a summary of the opioid, tablet dosage, and strength of topical preparations

Table 1. Summary of the Opioid, Tablet Dosage, and Strength of Topical Preparations
Opioid   Dosage of Tablets(mg)   Tablets Mixed in Cold Cream
Morphine                          30            1 or 2 per ounce
Hydromorphone             4 or 8            Same
Oxycodone                          30            Same


Some patients get creative. They find creams, oils, lotions, and gel preparations they feel get them better relief than ordinary cold cream. Some compounding pharmacists utilize very soluble, effective carrier creams. Cost and insurance coverage is usually the barrier to this approach. With a little instruction to patients, however, inexpensive cold cream will get the job done.

Use of Electromagnetic Devices
Essentially all of the electromagnetic devices on the market will drive topical opioids through the skin and deep into the tissue. These include electric currents, ultrasound, radiofrequency, infrared, and laser. Plain heat, massage, and vibration also enhance the penetration of topical opioids. Table 2 presents a summary of electromagnetic measures for use with topical opioids. These devices and techniques have the added advantage of removing or displacing sequestered electric charges in the pain site. Electromagnetic treatments may also promote blood flow and activate tissue to heal. When topical opioids that attach to peri-pheral receptors are combined with electromagnetic measures, a powerful healing and therapeutic approach is initiated. Ultrasound, infrared, electric current, and vibrator/massage devices are now quite available, inexpensive, and can be used at-home by patients (See Figures 2-4). Rather than take additional opioids for pain flares or breakthrough pain, some patients will use a topical opioid and an electromagnetic device for enhanced relief.

Systemic Effects
In my early studies, I found no morphine in blood or urine following topical use.8 I've now observed a few patients who show low levels of morphine in blood and/or urine. Patients who use topical morphine regularly may show morphine in body fluids following topical application. In fact, they usually report that topical morphine is their mainstay for pain control or their major measure to control pain flares. Reported here are two such cases.

Case 1
A 54 year old male has severe, intractable pain in his right hand, arm, shoulder and chest wall. This neuropathic state was caused by a motor vehicle accident. Each day he applies an average of about 240mg of topical morphine. He covers his entire right arm, shoulder and chest wall with it. His blood concentration of morphine is 58.7ng/ml, and, at the time this blood specimen was taken, he submitted a urine sample which showed over 10,000ng/ml. He has reduced his intake of oral opioids by using topical morphine and he now considers topical morphine to be his primary pain treatment. Without topical morphine his right arm and hand are non-functional.

Case 2
A 62-year-old female has severe spine degeneration with multiple disc replacements. She also has severe bilateral knee degeneration. Genetic testing revealed Cytochrome P450-2C9 deficiency. Consequently, she poorly metabolizes oral opioids and requires a very high oral dosage to obtain even modest pain relief. Topical morphine applied to the skin over her spine and knees provide great relief. In her words, “I can hardly walk without putting morphine on my knees.” She applies about 60mg a day. Her blood concentration of morphine shows a trace at less than 5ng/ml and she shows 60ng/ml in her urine. She claims that without topical morphine she is house-bound.


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.

Summary
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.


In the vein...

Offline thetalkingasshole

  • Self-Transforming Machine Elf
  • Sr. Member
  • ****
  • SA_Chat+
  • **
  • Join Date: Jan 1970
  • Location: Somewhere between the sacred silence and sleep
  • Posts: 712
  • Reputation Power: 0
  • thetalkingasshole has hidden their reputation power
  • Last Login:July 06, 2019, 06:22:48 AM
  • Always with an arm out and a leg up
Re: the peripheral opiate receptors-i had no idea these even existed
« Reply #1 on: November 15, 2015, 12:43:14 PM »
So I can make morphine cream
and rub it into my jugular vein
And that will be effective?

I call bullshit
As I grew up, I opened my eyes and saw the real world, and I began to laugh, and I haven't stopped since

Offline corlene

  • Full Member
  • ***
  • Join Date: Jul 2015
  • Location: Ft. Lauderdale
  • Posts: 446
  • Reputation Power: 12
  • corlene is new on the scene.
  • Gender: Male
  • Last Login:September 30, 2016, 08:32:51 AM
  • I alternate morphine and dilaudid in my PCA
Re: the peripheral opiate receptors-i had no idea these even existed
« Reply #2 on: November 15, 2015, 01:01:00 PM »
Years ago when I went to the CRPS/RSD clinic up in Tampa the doctor prescribed a compounded cream with morphine, ketamine, lidocaine and about 9 other things,

I don't know what helped the most though, probably the ketamine.

Offline clinton (OP)

  • Jr. Member
  • **
  • Join Date: Nov 2015
  • Location: kansas city mo
  • Posts: 151
  • Reputation Power: 8
  • clinton is new on the scene.
  • Gender: Male
  • Last Login:May 13, 2016, 05:09:47 AM
  • Harm Reduction & Safe Using
Re: the peripheral opiate receptors-i had no idea these even existed
« Reply #3 on: November 15, 2015, 01:03:31 PM »
According to the article when the body has inflammation it creates receptors in the damaged area ..I found it hard to believe too but the body is a pretty amazing thing
In the vein...

Offline Chip

  • Server Admin
  • Hero Member
  • *****
  • Administrator
  • *****
  • Join Date: Dec 2014
  • Location: Australia
  • Posts: 6464
  • Reputation Power: 0
  • Chip has hidden their reputation power
  • Gender: Male
  • Last Login:Yesterday at 05:57:05 AM
  • Deeply Confused Learner
  • Profession: IT Engineer
Re: the peripheral opiate receptors-i had no idea these even existed
« Reply #4 on: November 17, 2015, 08:25:38 PM »
wow ! amazing. next time i can't get that shot in, i'm going to RUB the bugger in.

jokes aside, excellent article.
I do not condone or support any illegal activities. All information is for theoretical discussion and wonder.
All activities discussed are considered fictional and hypothetical. Information of all discussion has been derived from online research and in the spirit of personal Freedom.

Tags:
 

Related Topics

  Subject / Started by Replies Last post
8 Replies
6853 Views
Last post March 09, 2019, 02:19:24 AM
by bignasty
28 Replies
9907 Views
Last post September 23, 2016, 12:27:54 PM
by StM34081
12 Replies
5098 Views
Last post April 21, 2017, 01:27:39 AM
by 6-mam
2 Replies
1975 Views
Last post July 25, 2018, 09:08:01 AM
by Chip
1 Replies
2123 Views
Last post September 05, 2018, 12:48:49 PM
by Chip
0 Replies
1082 Views
Last post May 27, 2019, 08:48:40 PM
by Chip
0 Replies
1397 Views
Last post June 01, 2019, 02:46:14 PM
by Chip
0 Replies
1417 Views
Last post July 12, 2019, 07:49:50 AM
by Chip
0 Replies
163 Views
Last post April 14, 2021, 10:42:48 PM
by Chip
0 Replies
82 Views
Last post June 11, 2021, 06:51:11 PM
by Chip


dopetalk does not endorse any advertised product nor does it accept any liability for it's use or misuse





TERMS AND CONDITIONS

In no event will d&u or any person involved in creating, producing, or distributing site information be liable for any direct, indirect, incidental, punitive, special or consequential damages arising out of the use of or inability to use d&u. You agree to indemnify and hold harmless d&u, its domain founders, sponsors, maintainers, server administrators, volunteers and contributors from and against all liability, claims, damages, costs and expenses, including legal fees, that arise directly or indirectly from the use of any part of the d&u site.


TO USE THIS WEBSITE YOU MUST AGREE TO THE TERMS AND CONDITIONS ABOVE


Founded December 2014
SimplePortal 2.3.6 © 2008-2014, SimplePortal