Fentanyl - Overview

Overview

Fentanyl is an extremely powerful opioidA substance created in a laboratory to mimic the effects of naturally occurring opiates such as heroin and morphine. that relieves pain like the various drugs created from the opium poppy plant. Opiate use extends back to ancient times, when people in the Middle East and northern Africa learned that certain poppies produce a fluid that causes euphoria, or a state of extreme happiness and well-being; drowsiness; and pain relief.

Transdermal patches containing fentanyl are applied directly to the patients skin. The medication is released through the skin at a rate of about 75 micrograms per hour. Samuel Ashfield/Photo Researchers, Inc.
Transdermal patches containing fentanyl are applied directly to the patient's skin. The medication is released through the skin at a rate of about 75 micrograms per hour. Samuel Ashfield/Photo Researchers, Inc.

A document dated to 1552 BCE in the ancient Egyptian city of Thebes lists more than 700 uses for opium gum. Abuse of opium and its derivatives heroin, codeine, and morphine, has occurred throughout recorded history. But the drugs have also been recognized for their ability to ease pain. After the hypodermic needle was invented in 1848, injected morphine made surgery far less traumatic to a patient and eased the suffering during recovery.

Opiates, such as heroin and morphine, could not be used without difficulties, however. The substances cause addiction and problems with the stomach and intestines. In the twentieth century, scientists began to experiment with chemical compounds that would carry the analgesicPain relievers or the qualities of pain relief. benefits of morphine without the side effects such as addiction and constipation. Fentanyl was developed in the 1950s in Belgium. Its use as a quick-acting painkiller and relaxant attracted the interest of the medical community. First marketed under the brand name Sublimaze, the compound went into widespread use in the 1960s.

Doctors have found many uses for such a powerful painkiller. Fentanyl is one of the ingredients given to women during childbirth to ease the pain of contractions. Oral surgeons use it during tooth extraction. Heart surgeons use it in the most delicate operations, because even patients who have been "put to sleep" with nitrous oxideA gas given to surgical patients to induce sleep. or some other agent can react to surgical tools. A vast majority of people facing any kind of surgery receives at least one shot of fentanyl at the beginning stages of a procedure, to ease the tension of general anesthesia (being "put to sleep"). The drug's effectiveness against the most extreme pain in terminal cancer is well established.

The Dangers of Fentanyl

Despite its effective use as a painkiller, synthetic fentanyl carries with it some of the worst side effects of its natural cousins, heroin and morphine. It is highly addictive, and its withdrawalThe process of gradually cutting back on the amount of a drug being taken until it is discontinued entirely; also the accompanying physiological effects of terminating use of an addictive drug. symptoms are even worse than those of heroin. Like its cousins as well, fentanyl affects the part of the brain that controls breathing. Doctors use it in surgery with great care, closely monitoring patients for suffocation. Some people who have abused fentanyl have stopped breathing with the needles still in their arms. The drug works that fast.

Faced with these dangerous side effects, the federal government and the medical community have tried to balance fentanyl's beneficial uses against its potential for addiction and death. Pharmaceutical fentanyl—such medications as Sublimaze, Duragesic, and Actiq—are Schedule II controlled substances. Even this level of care has not eliminated the abuse of legal fentanyl, however.

Fast Fentanyl Facts

Fentanyl is a human-made (synthetic) substance that mimics the behavior of opiates in the brain and central nervous system. It is 80 to 100 times more powerful than morphine.

Beginning in the late 1970s, illegally synthesized fentanyl analogs (using slightly different molecules) began appearing as "club drugs" that could be snorted, injected, or taken as tablets. Drug dealers

After Chechen rebels took an entire theater of people hostage in Moscow in 2002, they released eight children. The fate of some of the other child hostages was not the same, however. To end the standoff, the Russian government flooded the theat
After Chechen rebels took an entire theater of people hostage in Moscow in 2002, they released eight children. The fate of some of the other child hostages was not the same, however. To end the standoff, the Russian government flooded the theater with gas containing fentanyl, killing many hostages (men, women, and children) as well as the terrorists. AP/Wide World Photos.

touted fentanyl as a "safer" heroin. The substance is also harder to detect in urine drug tests. Various people tried the drug, and deaths and emergency room visits from fentanyl analog abuse began immediately. In 1984, the Food and Drug Administration (FDA) declared all fentanyl analogs to be Schedule I substances (completely illegal and useless for medical purposes). According to the Journal of Toxicology: Clinical Toxicology, by 1995 over 100 deaths had been attributed to illegal fentanyl analogs. The vast majority of these deaths occurred because the analogs were so powerful that users just stopped breathing.

The 1990s also saw the invention of a berry-flavored lollipop containing fentanyl. This Schedule II product was introduced to ease "breakthrough pain" in cancer patients already on strong painkillers. Breakthrough pain is defined as a bout of intense pain that occurs rapidly and lasts several hours, despite the patient's use of longer-acting pain medicine. Despite the tight controls on the lollipops, they have been found for sale on the black marketThe illegal sale or trade of goods; drug dealers are said to carry out their business on the 'black market.' in Pennsylvania, Connecticut, and other states.

In 2002, fentanyl was again the subject of news stories and debate. In October of that year the Russian government used a fentanyl gas to end a hostage crisis at a theater in Moscow. As many as 117 people died from the gas; many others were hospitalized.

On July 15, 2005, the FDA issued a public health advisory about the use of fentanyl skin patches. The warning appeared on the FDA's Web site as follows: "FDA is investigating reports of death and other serious side effects from overdoses of fentanyl in patients using fentanyl transdermal (skin) patches for pain control. … The directions for using the fentanyl skin patch must be followed exactly to prevent death or other serious side effects from overdosing with fentanyl." The agency also noted: "The FDA is conducting an investigation into the deaths associated with these patches. The Agency has been examining the circumstances of product use to determine if the reported adverse events may be related to inappropriate use of the patch or factors related to the quality of the product. It is possible that some patients and their health care providers may not be completely aware of the dangers of these potent narcotic drug products and the important recommendations regarding their safe use."

Fentanyl's Analogs

Chemists tinker with the fentanyl compound to create "analogs" with similar characteristics but greater strength. Some of these fentanyl analogs have names such as: acetyl-alpha-methylfentanyl; betahydroxyfentanyl; and Remifentanil. All of these analogs are produced illegally and are Schedule I controlled substances, which means that they have no recognized medical use. Because the strengths and chemical by-products vary so much, a single use of any of these analogs can prove deadly.