The U.S. Drug Enforcement Agency (DEA) has previously issued public warnings regarding the use of the opioid drug fentanyl and its analogs. According to the agency, the incidents of drug overdoses and deaths relating to fentanyl have significantly increased in the last two years.
The Centers for Disease Control and Prevention (CDC) likewise reported that in 2013, about 92 fentanyl-related unintentional deaths were recorded in the state of Ohio alone. The following year, CDC data showed that the number of such incidents had increased by almost 500%. There were more than 500 fentanyl overdose deaths in 2014.
What is Fentanyl?
Fentanyl, also known as its brand names Sublimaze, Actiq, Durogesic, Duragesic, and Fentora is a potent opioid analgesic. It is estimated to be 50 times more potent than pure heroin and up to 100 times stronger than morphine. It is classified as a Schedule II prescription drug and is used in the treatment of chronic pain among patients who are non-responsive to other opioids. It is also prescribed for the management of pain associated with cancer treatments or post-surgical procedures.
At present, fentanyl is the strongest narcotic that is used in medical treatment. It has been described as potentially lethal even when administered at low doses. According to the DEA, ingestion of as low as 0.25 mg of the substance can be dangerous.
Prescription fentanyl comes in various forms. It may be administered intravenously, via injection, intranasal sprays, transdermal patches, and oral lozenges.
Non-pharmaceutical fentanyl, however, is sold on the streets where it is sold in common names such as Apache, China Girl, China White, Dance Fever, Friend, Goodfella, Jackpot, Murder 8, TNT, Tango, and Cash. Street fentanyl is produced illegally and it is often laced with other drugs including heroin and cocaine. It comes in several forms such as powder, spiked on blotter paper, and tablets that mimic other pharmaceutical products. It is abused by snorting, swallowing, or injecting. The use of recreational fentanyl has been associated with cases of drug overdose and deaths.
What are Fentanyl Analogs?
Clandestine laboratories produce variations of the drug sold in the black market. The effects can be more potent pure fentanyl itself. Some people may not even be aware that they are purchasing drugs that have been chemically adulterated. Ingesting these substances places them at a high risk of adverse effects such as respiratory depression, overdose, coma, and death.
Some of the fentanyl analogs include alfentanil (Alfenta), Brifentanil, Butyrfentanyl, 3-Allylfentanyl, 3-Methylfentanyl, 3-Methyl-thiofentanyl, 4-Phenylfentayl, Acetyl-α-methylfentanyl, Acetylfentanyl, α-Methylfentanyl, β-Hydroxy-3-methylfentanyl, β-Hydroxyfentanyl, ρ-Fluororofentanyl, Carfentanil (Wildnil), Diampromide, Lofentanil, Orcefentanil, Ohmefentanyl, Mirfentanil, Para-fluorofentanyl, Phenaridine, Remifentanil (Ultiva), Sufentanil (Sufenta, Sufentil), Thiofentanyl, and Trefentanil.
While most of these identified analogs have been banned or are currently listed among DEA’s controlled substances, some laboratories have found ways to tweak the chemical structures of the drug to come up with new versions. This makes it easy to import, market, and sell other adulterated versions of fentanyl without being detected.
In April, it was reported that a new analog called furanyl fentanyl was circulating in the U.S. In fact, it accounted for the fatal overdose of a 30-year-old man in Chicago, Illinois.
Fentanyl and the Brain
Fentanyl affects opioid receptors in the same way that heroin, morphine, and other opioids do. Such receptors are found in the brain and are responsible for controlling the response to painful stimuli. Fentanyl binds opioid receptors and causes an upsurge in dopamine levels. This results in the alteration of the user’s perception of pain and pleasure.
Taking the drug numbs the perception of pain but because of the increase in dopamine levels, it also induces feelings of euphoria and extended pleasure. Repeated exposure to the drug alters the brain’s circuits, making it dependent on the substance for the production of pleasure signals. Ingesting it over time may lead to addiction.
Fentanyl has been classified as a substance with a high potential for abuse. The addictive process is similar to that of other painkillers such as Tramadol, OxyContin, Vicodin, and morphine. Compared to the mentioned opioids, however, the addiction to fentanyl can occur very quickly given its potent properties.
Fentanyl and Respiration
Multiple opioid receptors are present in the regions of the brain that control respiration or breathing rate. When fentanyl is taken in high doses, the opioid can cause respiratory depression which can lead to death.
Some studies have shown that the administration of pharmaceutical fentanyl for the treatment of post-operative pain and cancer affects respiration. To date, while fentanyl and other opioid painkillers remain as mainstays in the management of chronic pain, the fear of the incidence of respiratory depression is still a major clinical concern. As such, the prescription of fentanyl is reserved for patients who have developed a tolerance to other opioids and whose pain conditions can no longer be managed with the use of other analgesics.
On the other hand, recreational users of fentanyl are at a high risk of experiencing this adverse side effect. Some statistics have shown that respiratory distress is a major cause of death in most fentanyl-related overdose cases.
The potency of fentanyl increases the risk of overdose, especially among recreational users and those who may not be aware that the drugs they have purchased on the streets are laced with the substance. It is possible that low-grade heroin or cocaine have been mixed with versions of fentanyl to amplify the effects of the drugs.
Users who have been prescribed fentanyl should strictly follow the physician’s instructions to avoid fatal overdose. They should watch out for potential overdose symptoms that include difficulty in swallowing, extreme fatigue, fainting, dizziness, difficulty of breathing, altered consciousness, and severe confusion.
Fentanyl overdose may be reversed with the timely administration of the drug naloxone (Narcan). The drug acts as an opioid receptor antagonist and reverses the effects of the overdose. It also restores normal breathing rates.
It is imperative, however, that fentanyl overdose is treated immediately in order to effectively counter the effects and avoid fatality.
Naloxone is available in several states and is distributed to injection drug users and the general public for use in case of overdose. Some agencies and health facilities also provide information dissemination and training for the proper administration of naloxone.
Other Adverse Effects
Generally, fentanyl produces the same effects as heroin and morphine but because it is more potent, the adverse effects can occur within a shorter time and at more intense levels. Some of the adverse effects include the following:
- Abdominal pain
- Urinary retention
- Shortness of breath
- Swelling of extremities
- Dry mouth
Sudden cessation of fentanyl use can cause unpleasant withdrawal symptoms. These include the following:
- Extreme restlessness
- Watery eyes
- Runny nose
- Muscle and bone pain
- Panic attacks
- Loss of appetite
- Stomach cramps
- High blood pressure
- Intense drug cravings
Several treatment and rehabilitation centers offer structured detoxification programs that are intended to mitigate and manage the symptoms of opiate withdrawal. In most cases, in-house rehabilitation is strongly recommended because these facilities have addiction specialists, therapists, and medical professionals on duty who are trained to handle patients undergoing withdrawal symptoms.
Dangers of the Fentanyl Transdermal Patch
The use of the fentanyl patch has also shown to be habit-forming. The transdermal patch contains potent analgesic properties, which are highly addictive. As with other forms of fentanyl, it is reserved for patients who are regular users of opiates. Those with no prior exposure to other opioid drugs are at a great risk of respiratory depression and death.
Misuse and improper application of the skin patch can also result in fatal overdose. In July 2005, the U.S. Food and Drug Administration reported that there had been hundreds of fentanyl-related deaths arising from the use of skin patches. In Florida alone, the drug was accountable for 379 deaths in the years of 2003 to 2004.
In Aiken County, South Carolina, it was reported that between January 2006 and May 2008, about 11 residents died as a direct result of the misuse of fentanyl patches.
Those who intentionally misuse or abuse the fentanyl patch for the purpose of ingesting higher doses of the drug employ methods such as: placing it in the mouth, chewing, swallowing, sucking, injecting, snorting, or applying multiple patches to the body. These methods increase the risk of overdose and death.
Accidental exposure to a used patch can likewise cause fatal side effects. This is because the drug is not completely eradicated from the patch even after a three-day period of use. As such, discarded patches are often sought by some abusers.
Children are also at a risk of experiencing adverse side effects due to accidental exposure to either new or unused patches. To avoid these risks, transdermal patches should be stored or disposed of properly.
Using the patch for a longer or shorter period than prescribed is potentially fatal for a patient. Since the patch provides sustained release of the drug, wearing it longer than 72 hours or withdrawing from it before the prescribed period may result to the user’s death.
The risk of fentanyl side effects is also increased when the drug is used in conjunction with other medications such as amiodarone, amprenavir, aprepitant, carbamazepine, clarithromycin, diltiazem, erythromycin, fluconazole, fosamprenavir, itraconazole, ketoconazole, nefazodone, nelfinavir, phenytoin, rifampin, ritonavir, troleandomycin, and verapamil.
Certain pharmaceutical preparations also interact with the fentanyl patch and can cause side effects, aggravate the symptoms of existing health conditions, or affect the effectivity of the drug in some way. Some of the medicines that have been found to interact with fentanyl include phenothiazines, sodium oxybate, anticholinergics, benzodiazepines, crizotinib, fosaprepitant, other narcotic pain medicines, macrolide antibiotics, mixed agonist/antagonist pain medicines, and rifamycins.
Patients who have been prescribed fentanyl should inform their physicians of any other medication that they may be currently taking to avoid possible contraindications. Also, the patch must be used strictly as directed by the medical professionals, and in accordance with the manufacturer’s instructions or medicine guide.
The potency of fentanyl makes it one of the most dangerous drugs to be ingested. While its use as a prescription drug has become increasingly common especially among regular opioid users, care should be taken to avoid the dangers that can be brought about by incorrect administration, misuse, or abuse.
The public should likewise be warned of the grave consequences of using fentanyl non-medically or of consuming drugs that have purchased from the streets which may be laced with the substance.
As the DEA intensifies its efforts to curb the proliferation and sale of clandestine drugs in the black market, everyone should be on guard against the harmful effects of illicit drug use and prescription drug abuse.