Fentanyl is a synthetic opioid analgesic that has a very rapid onset of effectiveness and a short duration. The primary use of fentanyl is a pain reliever, but it is also used as an anesthetic.

Fentanyl has a number of different modes of administration and goes under a number of different brand names that include Durogesic, Sublimaze, Actiq, Fentora, Matrifen, Haldid, Onsolis, and several others.  Fentanyl is far more potent than the major opioid drugs that are used for pain control and also abused such, as morphine.

Development and Modes of Administration

Fentanyl was first synthesized in the 1960s and eventually introduced in a patch form, in lollipops, in lozenge forms, and more recently in a spray form, along with the more standard forms of administration, such as injections and pills.

The transdermal patch is applied to the skin and can provide potent and consistent relief of pain for as long as 72 hours. Lozenges dissolve in the mouth and are used in the treatment of breakthrough pain for patients that are already taking other opiates for severe pain, whereas the injected solution form can be used for pain relief and sedation during surgery.

The DEA lists fentanyl as a Schedule II controlled substance, indicating it has a high potential for abuse and addiction. It can only be legally purchased with a prescription from a physician.

The half-life of fentanyl depends on its mode of administration.

  • Its transdermal patch half-life is around 20-27 hours.
  • The half-life of sublingual doses ranges from 5.4 to 6.3 hours.
  • Half-life of the nasal spray is only a few moments (mean of about 6.5 minutes).

 

How Fentanyl Works

 

Fentanyl is an opioid agonist.  The specific action of opioid agonists is not yet fully understood; however, the brain has built-in receptors for endogenous opioids, which are neurotransmitters that are very similar to opioid drugs in their chemical structure. They function in the control of pain and fatigue, and experiencing pleasure.  It is believed that opioid agonists bind to these same sites on neurons in the central nervous system and produce their effects.

When opiate drugs like fentanyl bind to these receptor cites, they also increase the production of the neurotransmitter dopamine, particularly in areas of the brain that are associated with reinforcement or feeling rewarded for repeating a behavior. This increase in dopamine-binding in these areas produces a state of euphoria and relaxation. The association of these pleasurable feelings increases the incentive to repeat the action linked to the feeling in order to achieve this sensation.

The major action of fentanyl is painkilling without inducing a loss of consciousness. Thus, fentanyl is an effective painkiller that had many practical uses in its many different forms; however, its potential to produce the euphoric feelings associated with opioid drugs also opens up the potential for abuse.

 

How Fentanyl Affects the Mind and Body

 
Similar to other opiate drugs, the major pleasurable symptoms of fentanyl include euphoria, a pleasurable form of drowsiness or lethargy, and a pervasive mellowness.

There are a number of potential side effects that can occur with fentanyl use. The most commonly reported side effects include:

  • Blurred vision
  • Sunken eyes
  • Pale skin or changes in pallor
  • Dry mouth or excessive thirst
  • Ringing or pounding in the ears
  • Cough
  • Labored breathing
  • Dizziness
  • Fainting spells
  • Wrinkled skin
  • Unusual tiredness or weakness
  • Black, tarry stools
  • Chest pain
  • Back pain
  • Pain or cramps in other areas of the body
  • Constipation or decreased urine production
  • Painful urination
  • Nausea or vomiting
  • Irregular heartbeat
  • Unusual bleeding or bruising
  • Chest tightness
  • Fever, chills, or numbness in the hands or feet (or other areas)
  • Loss of appetite
  • Mental status changes, such as confusion, anxiety, or mood changes
  • Convulsions
  • Swelling of the ankles, feet, hands, or lower legs
  • Ulcers, sores, or white spots in the mouth

 
Signs of overdose with Fentanyl are commonly listed as:

  • Significant respiratory slowing
  • Clammy skin
  • Seizures
  • Pinpoint pupils
  • Slowed heartbeat
  • Low blood pressure
  • Severe drowsiness or inability to be awakened

 

Fentanyl Abuse

 

Male Addict Syringe And Heroin In A Spoon In The Shape Of A CrossStreet versions of fentanyl are commonly administered similar to how heroin is administered. The drug is often sold in a powder form and either injected into a vein, snorted, or smoked. Because it is water-soluble, it can be stirred into a solution immediately without any special preparations, like how heroin must be heated and melted. Fentanyl on the street is far more potent than heroin and results in many cases of overdose.

Fentanyl is commonly administered in oral forms such as lollipops, pills, or lozenges. Transdermal fentanyl patches, lozenges, and lollipop forms are also abused frequently. The lollipop forms are particularly useful in the treatment of cancer pain for children; however, they are subject to abuse. Users typically try and extract the drug out of the patch and either inject or inhale it, whereas lozenge and lollipop forms are often used in conjunction with other drugs and often taken in large quantities.

People who abuse the drug by taking it without supervision are putting themselves at great risk. Due to the potency of fentanyl, the difference between the dose that is used for therapeutic reasons and a potentially fatal overdose is actually very small.  Moreover, fentanyl users very quickly experience tolerance to even high doses, so doses that might produce a satisfactory high one week may not result in the same experience even just a few days later.  This situation is further complicated by individuals who mix fentanyl with heroin or cocaine, as this significantly intensifies the potencies of the drugs as well as their potential dangers.

 

How Does Fentanyl Addiction Begin?

 

Because fentanyl is a pure opioid agonist, it is not unusual for anyone who uses the drug for any significant period of time for any reason to develop at least a low-level physical dependence to the drug. Though having a physical dependence to fentanyl is not necessarily the same thing is being addicted to it, physical dependence often leads to abusive use of the drug and eventually addiction.

Tolerance and withdrawal develop relatively quickly with full opioid agonists. A person may begin using fentanyl legitimately, but increase use of the substance as tolerance develops. As the person begins using the substance outside of the prescription parameters, abuse takes hold. Coupled with the physical dependence, it often doesn’t take long before the person is struggling with full-blown addiction.

 
Behavioral Signs of Addiction

  • Spending a great deal of time trying to get, using, or recovering from using the drug
  • Taking fentanyl in larger amounts or over a longer time period of time than intended
  • Use of fentanyl leads to the inability to fulfill major life obligations
  • Use of the drug in dangerous situations
  • Desiring to decrease use but being unsuccessful at doing so
  • Continuing to use in spite of negative repercussions socially, academically, or at work
  • Giving up activities that were once important
  • Continuing to use the drug, resulting in worsening physical or psychological problems
  • Forging prescriptions
  • Seeing different doctors to get different prescriptions for the medication
  • Financial problems
  • Stealing or borrowing money to pay for fentanyl
  • Experiencing issues in one’s personal relationships as a result of fentanyl use

 

Psychological Symptoms of Addiction

  • Difficulty concentrating
  • Depressed or elevated mood
  • Anxiety
  • Confusion

Medical Detox

Anyone who is going to attempt to discontinue fentanyl use should do so under the supervision of a physician in a professional medical detox program. With all opiate addictions, individuals should never simply attempt to stop taking the drugs cold turkey. Medical detox is necessary.

A medical detox program will generally initiate a tapering dosage of the opiate to slowly ease individuals off the drug over a scheduled period of time. In some instances, replacement medications, such as methadone or buprenorphine, may be used; however, such use is determined on an individual basis.

The timeline for fentanyl withdrawal varies greatly according to a plethora of individual circumstances, such as the length of the addiction, dosage levels taken, co-occurring mental health issues, and other physical and mental factors.

 

Treatment beyond Just Medical Detox

 

While necessary and the first step in opiate addiction treatment, medical detox does not constitute treatment on its own. In order to achieve recovery, people struggling with fentanyl addiction must address the underlying issues that let to their abuse of the drug in the first place. Without comprehensive therapeutic care, individuals will likely relapse to opiate use after detox.

Treatment for opiate addiction takes many forms, such as Cognitive Behavioral Therapy, Motivational Interviewing, adventure therapy, individual therapy, and holistic treatment approaches. It’s imperative to choose a treatment program that caters care to each individual. Treatment should also be adjusted as needed throughout the recovery process.