Abstract
While the endogenous opioid system has generally been associated with regulation of pain, it also modulates the experience of distress and may play a central role in many psychiatric and neurodevelopmental disorders. Decades of preclinical research on the analgesic effects of endogenous opioids, i.e., endorphins, suggests that opioid receptors have plastic bimodal (inhibitory/excitatory) properties that may explain conflicting findings in clinical research. An exploratory study with 60 healthy volunteer participants, using a cold pressor-induced pain paradigm, found evidence that a combination of a nutraceutical agent that enhances endorphin release (Endorphin Enhancer) with one that switches opioid receptors from an excitatory to inhibitory mode (Opioid Receptor Switcher) not only increases pain tolerance but also reduces emotional and physical distress. This discovery led to clinical application of a critically formulated endorphinergic treatment in 203 case studies over a two-year period. Findings revealed the remarkable clinical efficacy and safety of this treatment in the relief of chronic emotional and physical distress, including anxiety, anger, depression, cravings, and hyperalgesia, as well as enhancement of well-being, productivity, mental clarity, relationships, and an adaptive response to life’s stresses. These studies provide new insights into the role of endogenous opioid system imbalances in the development, treatment, and prevention of dysfunctional emotional and physical distress. We postulate that an Endorphinergic Distress Syndrome (EDS) consists of abnormal endorphin levels together with opioid receptors predominately in their excitatory mode. EDS may account for many core distress symptoms associated with chronic anxiety, addictions, pain, as well as affective personality, autism spectrum, attention-deficit, and distress-related medical problems. Our research has led to new endorphinergic formulations, combining Endorphin Enhancers, such as caffeine, with Opioid Receptor Switchers, such as n-acetylcysteine, for the relief of emotional and physical distress. Our studies also provide a novel method to reverse the anxiogenic effects of caffeine and related hyperexcitatory substances.
Highlights
There is significant evidence that the endogenous opioid system is involved in attenuation of the experience of pain [1]
These clinical “cold pressor” findings cast a new light on the earlier preclinical pain studies of Crain and Shen (Section 1), suggesting that reduced behavioral reactivity to pain-induction paradigms produced by our endorphinergic nutraceutical formulation is related more to emotional and physical distress relief than analgesia
That reliance on endogenous opioids for the relief of emotional and physical distress is much preferred over exogenous opioids, given the serious and at times fatal side effects of exogenous opioids, including marked cognitive impairments, gastrointestinal symptoms, as well as tolerance and dependence and, ironically, hyperalgesia or increased pain sensitivity
Summary
There is significant evidence that the endogenous opioid system is involved in attenuation of the experience of pain [1]. There is a critical need to understand these contradictory findings regarding the impact of endorphins on regulation of the stress response, and on modulation of the experience of distress This is important since chronic emotional and physical distress is at the core of most psychological disorders. The preclinical nerve tissue research of Crain and Shen [15,16] over the past three decades on the function of opioid receptors in the pain response may provide critical insights into these issues with important clinical implications [17] They discovered that whereas opioid receptors are normally in an inhibitory mode, thereby producing analgesia when triggered by the release of endorphins, opioid receptors could be switched to an excitatory mode, which literally stimulates the opposite effect, that is, hyperalgesia, or increased pain sensitivity. Crain and Crain [17] provide an extensive review of these preclinical pain studies on the bimodal nature of opioid receptor signaling in the endogenous opioid system and emphasize the significance of these studies in elucidating neuropharmacologic and neurochemical mechanisms that may mediate clinical distress disorders
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