One of the most common problems doctors see every day are patients in need of pain relief. They are usually in the kind of pain that an over-the-counter medication will not relieve and are in need of a doctor’s recommendation or prescribing pen to experience the relief they need to operate their lives as normal.
Unfortunately, the over-prescribing of opiates and opioids in America to treat pain has thrust our nation into an epidemic of silent addiction and it is time to understand what these medications are, what they do inside the body and why so many are addicted.
What are Opiates and Opioids?
Opiates are chemicals that are derived from the poppy plant and activate the bodies opioid receptors found in the brain giving a ‘feel good’ sensation. An opioid is a name originally used to describe the synthetic chemicals which either activate, partially activate, block or do a combination of these three actions on different subtypes of the opioid receptors. Today, the term opioid is often used to include both natural opiates, derived from the poppy plant like heroin and morphine, and synthetic chemicals like oxycodone and fentanyl. The term opioid may also refer to opioid receptor antagonists like naloxone and naltrexone and to partial agonists like buprenorphine.
How do Opiate and Opioids Work Inside the Body?
Opiates mimic the effect of beta-endorphin only with a much greater potency. Beta-endorphin is the bodies’ natural opioid receptor activator. When these opioid receptors are activated it results in the release of the pleasure-producing neurotransmitter, dopamine. Normally this process compels us to strive for things that are good for our survival like drinking water when we are thirsty or eating when we are hungry. Even the motivation to avoid painful situations before they occur is driven by this process. Beta-endorphin is nature’s pleasure hormone when things are going well for our survival, opiates and opioids are a chemical trick.
Synthetic opioids can be designed to have different effects on different opioid receptors in the body and have different potencies. Opioids can be engineered to activate some opioid receptors subtypes with different strengths or to block certain receptors and activate others. For example, Fentanyl works like morphine as it binds to the brain’s opioid mu receptor, but is 100 times more potent. Buprenorphine weakly activates the mu receptor and it also blocks the kappa receptor. (Both Mu and Kappa are opioid receptors that occur naturally in the body.) This is why Buprenorphine is known as a partial agonist. Buprenorphine has a ceiling effect on its activation of the opioid mu receptor. It is dose dependent only until it hits a certain level of plasma concentration and then it stops giving significant increases in reward with each dose. While the ceiling effect is not absolute, it does tend to reduce the abuse potential when buprenorphine is administered as directed in the opioid tolerate patient. Other synthetic opioids, like naloxone and naltrexone, can occupy the opioid receptors but do not activate it and create no reward. They will also block the effects of other opioids and opiates rendering them ineffective. This reversal effect of antagonist (blockers) on agonist (activators) is what creates the lifesaving effects of naloxone. In short, synthetic opioids allow scientists to create a much more sophisticated and specific approach to the manipulation of the bodies opioid receptor system.
How does Addiction to Opiates and Opioids Occur?
Pain (both physical and emotional) is the bodies most important defense mechanism. It drives us away from harm and destruction. Pain constantly tells us “don’t do that, it’s bad for you.” Pleasure (physical and emotional) is also important. Pleasure compels us to do certain things that are important to our survival. Under normal conditions, our balance of pain and pleasure is determined by our circumstances or the way we perceive that we are surviving in our environment.
There are about a hundred chemicals known to scientist that trick the bodies known pain and pleasure circuits creating a false sense of pleasure. When opioids create this sense of pleasure over time the brain will try to reset its baseline setting. This is the way of sensing pain even though the person is trying to trick their senses into a perception that their circumstances are better than they are. This effect is called tolerance and results in the need for higher and higher doses in order to achieve the same effect. The problem becomes further complicated by the fact that when the drug’s effect wears off, the pain and pleasure balance does not go back to a balanced state. When the opioid’s effect goes away the patient’s perception of their circumstances becomes a very painful state both physically and emotionally. Back pain seemingly does not heal, and patients become angry, depressed and apathetic. The need to use an opioid in order to feel normal is called dependence. Often the most common symptom of opioid withdrawal is physical pain.
In opioid addiction, physical withdrawal is only the tip of the iceberg. Craving becomes an all-consuming preoccupation of one’s attention. It is an unrelenting obsession to regain the balance of pain and pleasure. Craving can be divided into two categories. The first is tonic craving which is thought to be related to plasma concentrations and receptor activation of the drug addiction. Tonic craving is a continuum of mild withdrawals. The other type of craving is known as phasic craving is related to triggers. Triggers are environmental perceptions that remind the subconscious mind of the pleasure associated with the drug of addiction. Triggers could be people or places. They could even be smells, sounds or sites.
Brains that have been exposed to opioids over a long period of time often develop a condition of anhedonia or pleasure deafness. Once a person’s brain becomes dependent on the drug, they cannot experience pleasure or even contentment without it. Without the drug, their world becomes a very painful and dark place. This condition is known as chronic dysphoria or always present physical and emotional pain.
What to Remember and Know about Opiates and Opioids
Pain is important for survival. Pain compels us to avoid harm. Yet, human nature compels one to seek relief for pain and it is important to be aware of chemicals like opioids that highjack and short-circuit this process. They should be used with extreme caution and for the shortest amount of time possible so the body maintains a natural, healthy balance of pleasure and pain.
(Article was written by Dr. Brent Boyett, D.O., D.M.D., Chief Medical Officer for Pathway Healthcare, a national treatment center for substance abuse and dependency.)
