Fentanyl is a very potent opiate drug. Its primary use is to treat moderate to intense pain. The fentanyl transdermal patch, Duragesic, is most commonly used for the control of pain that has not responded to other interventions, including other opiates.
Fentanyl is believed to attach to neurons in the brain and spinal cord that are specialized for endorphins and enkephalins, neurotransmitters that are involved in the control of physical pain, exertion, stress, etc. In fact, these neurotransmitters are often referred to as endogenous opiate substances because of their chemical similarity to opiate drugs. All opiate drugs are processed from opium, found in the Asian poppy plant, or they are synthetic substances that mimic the chemical structure of substances found in opium.
Fentanyl is a controlled substance that is classified in the highest level of control for a drug that can be attained via a prescription from a physician, Schedule II. The United States Drug Enforcement Administration (DEA) categorizes substances in this category as significant potential substances of abuse and liable to produce physical dependence in individuals who use them for any purpose. They can only be safely taken while under the direct supervision of a physician. Thus, fentanyl is considered to be a potentially dangerous drug of abuse, and this is confirmed by numerous reports in the media of fatal overdoses on the drug over the past few years.
Tolerance and the Fentanyl Patch
The development of tolerance to any medication is not necessarily a problem when the medication is being used according to its instructions and under the supervision of a physician. In fact, it is expected that many individuals will develop some level of tolerance to a great deal of the medications they use for medical reasons, and physicians can monitor the situation, adjust doses as needed, and ensure that the medication continues to work. The level of tolerance that develops as a result of medicinal use is typically not at the same level of severity as that which occurs in individuals who abuse drugs because these people take much higher amounts and often take them more frequently.
Transdermal patches release fentanyl at a very slow rate. Patches of varying sizes release different amounts of fentanyl per hour with the formula being about 25 micrograms of fentanyl released per hour for each 10.5 cm² of the patch. Thus, larger patches release more fentanyl per hour.
There is an extended risk for the misuse of opiate drugs when they are prescribed for pain, particularly the fentanyl patch, because of several reasons:
- Because the patch is designed to be used by individuals for whom other opiate drugs have not worked for their pain, these individuals often have significant emotional issues and high sensitivity to pain and will attempt to use more of any drug they are prescribed.
- Many people who have not previously been taking opiate drugs develop tolerance at a rapid rate when prescribed the patch and attempt to self-administer more of the drug to get the effects they initially got.
- The recommended doses of the patch are often not sufficient to control the subjective experience of pain that many patients endure, and this leads to people re-administering the patch before they are supposed to do so.
- The end dose effects of the patch often appear to be less effective at controlling pain, and individuals may attempt to re-administer a new patch before they are supposed to do so. The end dose effects are the effects that occur near the end of the duration of time that an individual is prescribed to wear any specific patch, which is most often 72 hours.
- In general, there are greater risks for overdosing and experiencing negative effects with extended-release opiate formulations compared to immediate-release formulations.
Thus, the development of tolerance to fentanyl is a normal consequence of its medicinal use. There are numerous complications that can occur as a result of using fentanyl in the treatment of chronic pain.
There are some claims by researchers that the majority of individuals who are prescribed the fentanyl patch for pain control have been prescribed them inappropriately:
- Physicians may not be familiar with the proper protocol for prescribing the patch.
- The patch may be prescribed individuals who have not been exposed other opiates; thus, they have not developed tolerance.
- Physicians may prescribe the patch in either too little or too high of the dose.
- Patients should be evaluated for past substance abuse or their potential to abuse drugs before being prescribed opiates; many times, this is not adequately done.
- Patients are not fully instructed regarding the expectations they should have of the patch’s effectiveness.
Tolerance figures into these problems when a person who has never used opiates is prescribed the patch and develops rapid tolerance to fentanyl because they are what is termed opiate-naïve patients. This means that their system has never been exposed to opiates and has not developed any level of tolerance; thus, these individuals may develop tolerance to fentanyl very rapidly and may experience a need for more of the drug very early in its administration, resulting in them misusing the fentanyl patch to control their pain.
On the other hand, individuals who have developed tolerance to opiates may not respond to the initial doses of the patch that are prescribed by physicians, and this may lead to the same types of issues. Thus, issues with tolerance can be problematic for the medicinal use of the drug in certain individuals and with physicians who are not experienced in prescribing this medication. Moreover, physicians may not be aware of issues associated with prescribing the fentanyl patch and may inadvertently make errors in judgment when prescribing it to certain individuals.
According to information from the book Opiate Receptors and Antagonists: From Bench to Clinic, fentanyl is extremely potent, and overdoses can occur at exposures to the drug that are minute and significantly lower than doses for other drugs like morphine. This makes the development of tolerance to fentanyl an even greater issue when individuals attempt to alter the amount of the drug they are taking because the therapeutic window and the potential for overdose are very small, even for individuals who have developed tolerance to the drug. Simply self-adjusting the amount of fentanyl one uses by changing the patch too often or wearing more than one patch simultaneously can lead to a potentially serious situation that can lead to overdose effects. Of course, overdoses on fentanyl can be fatal.
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There are several conclusions that should be drawn from the research information regarding the use of the fentanyl patch:
- The development of a substance use disorder should never be considered the fault of the drug; it is associated with individual differences in behavior, outlook, emotional makeup, and access to drugs.
- Fentanyl is an extremely potent drug that does have potential medicinal uses for the treatment of pain, but it should be used judiciously.
- Tolerance to fentanyl is a normal and often expected occurrence.
- It appears that the prescription practices associated with use of the fentanyl patch can be better implemented by physicians.
- Individuals should never adjust the dose of fentanyl that they are using by changing patches too quickly unless they discuss the situation with their physician.
- The development of tolerance to fentanyl or even a lack of tolerance can be problematic for some individuals who are using the fentanyl patch.
- Education, close monitoring, and continued reassessment and evaluation of the patient should be standard practice when the fentanyl patch is prescribed.
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