Opioid Receptors: A look at Their Function and Effects

Opioid receptors are responsible for positive and negative side effects associated with opioid use

Opioid drugs produce a pain-numbing effect throughout the body by binding to special protein sites called opioid receptors.  These binding sites are located throughout the brain, spinal cord, and gastrointestinal tract, and control various bodily functions including movement, appetite, digestion, and sensations of pain.

When opioid medications like oxycodone, Vicodin, or Percocet enter the blood stream they bind to opioid receptor sites and interfere with the brain’s ability to recognize pain. At the same time, they also stimulate areas of the brain that are responsible for feelings of pleasure and euphoria, creating a drug-induced “high.”

Opioid receptors were first discovered in the early 1970’s, and there are now four major subtypes of receptors that have been identified, including delta, kappa, mu and Nociception receptors. All receptor types are located in the brain, while mu receptors are found in the brain, spinal cord, and intestinal tract. This specific type of opioid receptor is sometimes considered the most important as it are responsible for producing several different effects, including analgesia (pain relief), respiratory depression, reduced gastrointestinal function, physical dependence, and the sensation of euphoria.

With continued opioid use, many patients begin to build up tolerance to the medications, thus needing to take increasingly higher doses to achieve the same pain relieving effect. This phenomenon occurs because of a process called endocytosis, where the opioid receptors are actually internalized by the cell itself. Endocytosis results in fewer opioid binding sites on the cell surface that are openly available to provide pain relief. With fewer opioid receptors on the cell surface, more opioids are needed to achieve the same reduction in pain relief.

The Waismann Method of rapid opiate detox is a safe and proven treatment for opiate dependency that utilizes the most advanced medical techniques available.  Performed under the close supervision of board-certified doctors, patients sleep comfortably under a light anesthetic while special medications are carefully administered to cleanse the opioid receptors. Patients experience minimal conscious withdrawal or suffering, as they unconsciously experience an accelerated withdrawal in a matter of hours rather than days with traditional methods.

If you or anyone you know is experiencing issues with opiate dependency, we urge you to consult your health professional or contact us directly for information about safe and effective treatment options.

Or send us a