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1/20/20

Peptides for Pain

These days, everybody looks for alternatives to opioids in the treatment of pain.  Sadly, there just aren’t that many treatments that are both affordable and available to replace opioids for chronic pain therapy.

Readers of this blog are familiar with our ongoing efforts to replace opioids with less harmful alternatives:  we use IV therapies for chronic pain, we evaluate our patients from a Functional Medicine perspective, and we endeavor to use interventional Regenerative Medicine treatments.

As part of our philosophy of using as little opioid and steroid as possible, we have found peptides as some of the most promising and helpful molecules.  We routinely use them as part of our Regenerative Programs and our cognitive optimization - more about those peptides in later blogs.  However, we would like to present some information about several most interesting peptides used for pain syndromes.

So what are peptides? They are strings of amino acids, shorter than proteins, with therapeutic properties.  Almost all peptides in use have proven effects in animal studies, with some also proven in human studies.  Most of them have effects similar to hormones.  In fact, insulin was probably the first isolated peptide used therapeutically.  We use peptides made in the United States in just one pharmacy regulated by the FDA.

The following are highlights of the peptide pain therapies we employ.  I know this blog is more technical than most.  This is unavoidable with such a subject.  The information below is to form a general idea of what we have been working on.  Please feel free to call and come talk to us if you believe something like this may help you.  

ARA290 

ARA290, also known as pyroglutamate helix B surface peptide has been evaluated extensively in neuropathic pain.  It is derived from erythropoietin (EPO), a hormone secreted by the kidneys.

The innate repair receptor (IRR) is typically not expressed in normal tissues, but it is unregulated in response to tissue injury, low oxygen, or metabolic stress.

ARA290 selectively activates the IRR, which turns on anti-inflammatory and tissue repair pathways.

ARA290 may activate IRRs within the central nervous system (brain and spine), as well as peripheral sites.

Some of the effects of ARA290 include:

• improved sensory nerve function and reduction of epidermal nerve loss in diabetic neuropathy

• reduced allodynia (sympathetic mediated pain) and improved motor function in rodents after L5 spinal nerve transection, dorsal root ganglion crush injury.

• reduced signs of spinal and brain inflammation

• promotes repair of small autonomic nerve fibers in sympathetic ganglia in a mouse model of diabetic neuropathy.

ARA290 administered IV to patients with moderate to severe neuropathic pain from sarcoidosis and type 2 diabetes mellitus showed no relevant side effects and 25% reduction in pain after 3 administrations. 

ARA290 also protects mice from systemic lupus erythematosus and helps heal skin burns. 

ARA290 also shows beneficial metabolic effects such as decreased in hemoglobin A1c, triglycerides, and decreased ratio of total serum cholesterol to high-density lipoprotein cholesterol.

Semax

Semax is a synthetic peptide, analog of a fragment of the adrenocorticotropic hormone (ACTH).  ACTH is a hormone produced by the pituitary gland in the brain in response to stress and regulates cortisol secretion.

Semax has nerve protective effects and also protects against cognitive decline (nootropic).

Some of the effects of the Semax include:

• reduces the number of cells damaged by oxidative stress

• increases survival of brain cerebellar neurons during glutamate toxicity and in a variety of other conditions

• helps to adapt to hypoxia (low oxygen conditions

Amongst other clinical effects, Semax is an analgesic (pain medication) and helps weaning off opioids.

Selank

Selank is a peptide synthetic analog of tuftsin.  Tuftsin is a regulator of the peripheral nervous system that also impacts the central nervous system (CNS).

Tuftsin (and Selank) offer resistance to pain and increased memory.  It also has antidepressant and anti-anxiety effects and abolishes the reaction of aggression and fear in primates with neurosis.

Delta Sleep Inducing Peptide (DSIP)

This peptide can act as a stress limiting factor, and may have anti-oxidant effects.  More importantly, treatment with DSIP is beneficial for withdrawal symptoms of both alcohol and opioid use.  

It increases sleep efficiency and shortens sleep latency.

DSIP is a potent analgesic in mice, and reduced the pain of migraine headaches, vasomotor headaches, and foot pain of psychogenic origin.

DSIP also stimulates luteinizing hormone secretion for greater testosterone levels, which indirectly helps painful symptoms.

Pentosan Polysulfate (PPS)

PPS is an FDA-approved oral medication with anti-inflammatory properties and cartilage repair action.  It is therefore used successfully in pain from osteoarthritis.

Cerebrolysin

This is peptide used in treatment of painful diabetic neuropathy

Thymosin Beta 4.

TB4 is a restorative/regenerative peptide for neurological injury and neurodegenerative diseases.

Insulin-like Growth Factor 1 (IGF-1)

Used in diabetic neuropathy and amyotrophic lateral sclerosis (ALS).

As a nerve growth factor, IGF-1 promotes nerve lengthening and branching.

As a muscle growth factor, IGF-1 promotes muscle cell differentiation, proliferation, and growth.  It may also activate muscle stem cells during the regenerative process

As a blood vessel growth factor, IGF-1 promotes blood vessel formation in muscle regeneration.

Well, you made it to the end!  Thank you for sticking with us on this more complicated write-up.  In the weeks following, we will send more information about other pain treatments that are alternatives to opioids and steroids, and also about other peptides used in Regenerative Medicine.

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