Opioids, especially high dose Schedule II (the more potent opioids), can cause a situation where patients become trapped.  They cannot travel during part of the month because they are dependent on having their prescription refilled at their pharmacy, cannot take extended vacations, have to continually safeguard their medications (sometimes with large safes and security alarms), constantly worry about the medications being stolen, and are at the mercy of the drugs with doses being absolutely necessary to prevent escalation of pain just before the next dosage and withdrawal symptoms.  In addition, they frequently fight the urge to take more or take additional amounts during the worst pain causing them to run short and go into withdrawal before the next prescription is filled.  This is chemical dependency.  Some engage in drug seeking behaviors such as going to their physician a few days early each month (pharmacies will frequently fill these medications 2 days early).  It is miserable being so dependent on these medications, with the random drug testing (or even worse, monthly drug testing by physicians who own their own testing machine), scrutiny by the pharmacy staff, being made to feel like a street drug addict, and having to adhere to changing by rigid clinic rules that if violated will instantly cut off your prescription opioids.  In the current environment, finding another physician to prescribe opioids may be impossible if you are discontinued as a patient from another clinic.  

 

Many people do not recognize their dependence on the medications, but believe the escalation of pain that occurs just before the next dosage demonstrates the need for opioids due to the pain.  In fact, what is happening is they have opioid induced hyperalgesia and withdrawal induced pain amplification.  Opioids have two effects on the body's receptors- reduction of pain through action on the opioid receptors and worsening of pain through action on the NMDA receptors.  At low doses of opioids or when first used for acute pain, the opioid receptor effect predominates.  However at higher doses or with protracted usage, the NMDA receptor effect of creating worsening pain becomes more important.  At the end of the dosage, the pain experienced (with high dose opioids or protracted usage) does not simply return to the baseline pain- it overshoots, causing much worse pain than the original pain.  The patient believes this is a sign their pain is getting worse or needs more opioid to control it.  But their pain is not getting worse: this effect is due to the opioid itself as it affects the NMDA receptor, which is activated for a longer period of time than the opioid receptor, leading to an overshoot of pain.  Increasing the opioid helps temporarily but then ultimately makes the situation worse.  This is what creates the dependence on opioids- the effect of the opioids does not significantly impact the pain for which the person is being treated, but instead may temporarily override the NMDA receptor effect of the opioids with each dose, causing chemical dependency on the opioids.  Of course in addition to this pain overshoot, tolerance to the drug develops leading to reduced effectiveness due to changes in the opioid receptors.  

 

We now have 25 studies that demonstrate by gradually taking people on high doses of opioids down to little or no opioids, the chronic pain does not worsen, and in fact in many cases, improves.  In my own patient population of chronic pain patients, I took 150 patients down from high dose to low dose opioids, and indeed their pain improved.  We also have many studies demonstrating the risk of overdose death goes up with daily dosage. By European standards, we prescribe 400% as much opioid per capita as in Europe but with no demonstrable improvement in pain.  It is estimated only 20% of those receiving long term opioids in the US actually derive any benefit from them in treating the original pain.   

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Our de-prescribing clinic, is designed to gradually get patients off opioids or move to very low levels. We do this by converting to other opioid and non-opioid pain killers that are safer, adding medications that reduce or eliminate withdrawal symptoms, and gradually ratcheting down on the dosage.  Frequently patients are alarmed at this process, exclaiming "What am I to do about my pain?" not realizing it is the high dose long term use of opioids that is responsible for continued pain.  As long as the person is taking continued opioids, the pain will persist, even for years or decades, long after the injury or surgery has healed. Moving gradually to a lower dosage or eliminating opioids improves the pain. These facts are not new-  Loeser and colleagues proved this as far back as the early 1980s, but the medical profession from 1995 onward was inundated with advertising, drug companies claiming their opioids were less addictive, strong arm pressure from other doctors with a financial interest in drug companies, and misguided federal, state, and regulatory agencies all erroneously believing chronic pain is simply an extension of acute pain and that escalation of opioid doses into the stratosphere was acceptable as a treatment to constantly chase the tolerance that was occurring with opioids.  Now we have 48,000 people a year in the US dying from opioids- an increase that is 6 fold over the past two decades, but no better pain control that with low dose opioids or no opioids.  

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THE FALLACY OF POTENCY OF OPIOIDS RELATED TO DRUG SCHEDULE

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The DEA has developed Schedules I-V for controlled substances that take into account their potential for addiction and their accepted medical use.  The Schedules include prescription drugs, street drugs, and precursors for manufacturing many of these drugs.  But the Schedules are more for legal purposes of drug diversion enforcement rather than having anything to do with potency of drugs.  Schedule I drugs are those that have a high addictive potential and are deemed by the DEA to have no legitimate medical use.  Marijuana is widely used illegally throughout the US, has a relatively low addiction potential, and has been approved by the majority of states as a medicine, yet the federal government continues to list it as a Schedule I drug.  Rather than change the drug schedule at the federal level, Congress has failed to act to change the schedule, the DEA staunchly opposes re-scheduling, and doctors and patients are left in a legal no-mans land.  Obama handled this by seditiously ignoring federal enforcement laws instructing prosecutors to not enforce the law, contrary to his Oath of Office of the President and the US Constitution.  Trump and his attorney general have reversed the Obama doctrine of selective enforcement of drug laws, but have done nothing to move to re-schedule the drug in accordance with commonly accepted medical usage.  Ironically, THC, the main active ingredient in marijuana responsible for the majority of effects, is available as a Schedule III drug, Marinol, that is outrageously expensive- approximately 10-100 times as expensive as the equivalent amount of marijuana.  Cocaine is highly addictive, but is a Schedule II drug, meaning a doctor can use cocaine on patients in clinical practice.  Similarly, methamphetamine as the prescription drug Desoxyn, is a Schedule II drug prescribed for ADHD whereas street methamphetamine is a Schedule I drug.  Buprenorphine used to be a Schedule V drug but was moved to a Schedule III when Suboxone was released.  Buprenorphine is roughly 5-10 times more potent than morphine but is a lower Schedule drug. Some narcotic pain killers such as nalbuphine (Nubain) are available as an injection but are not scheduled at all.  Some narcotic pain killers with a very low addiction and overdose potential such as tapentadol (Nucynta) are misclassified as a Schedule II drug, thereby limiting their availability that could be used as a safer alternative to oxycodone (Oxycontin) or hydromorphone (Dilaudid).   

 

Hydrocodone used to be a Schedule III drug but in October 2014 was moved to a Schedule II drug, in part due to massive overprescribing and overuse of the drug in the US with doctors prescribing it like candy since it was a lower schedule drug than morphine, yet has the exact same potency as a painkiller compared to morphine.  The US, with a population that is 6% of that of the entire world, used 95% of all hydrocodone in the world. Doctors would frequently prescribe 6-12 tablets per day of hydrocodone in the 2000-2014 era- a dosage equivalent to Oxycontin 40mg twice a day.  But because it was a Schedule III (lower abuse potential), doctors would frequently write for massive amounts on one script, then write for up to 5 refills on the prescription, meaning patients were being given 6 months of opioids equivalent to high dose Oxycontin or morphine, and were not monitored for substance abuse, drug diversion, addiction, or side effects for half a year.  This led to many problems including sharing of drugs in the workplace, selling drugs frequently, and kids having access to the huge quantities of their parents unlocked drug supply.  Some patients would call in their own prescription refills illegally and nurses and medical assistants were also calling in their own prescriptions to pharmacies for unprescribed hydrocodone.  Hydrocodone became a gateway drug for more potent prescription opioids such as Oxycontin, Opana, and Dilaudid.  Finally the DEA had enough, and in concert with the FDA made hydrocodone a Schedule II drug that could not be refilled nor called in.  This resulted in an avalanche of protests from doctor-drug dealers, primarily family physicians, that did not want to be bothered with monitoring their patients for addiction, drug diversion, or serious side effects. 

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