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Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.
Life-threatening adverse reactions caused by furanylfentanyl use have been observed in Sweden and Canada. At least seven deaths in Cook County, Illinois, have been linked to furanylfentanyl in 2016, with additional deaths in suburban Chicago in 2017.
Furanylfentanyl may be measured in blood or urine to monitor for use, confirm a diagnosis of poisoning, or assist in a medicolegal death investigation. Commercially available immunoassays are often used as initial screening tests, but chromatographic techniques are generally used for confirmation and quantitation. Blood furanylfentanyl concentrations are expected to be in a range of 1-45 μg/L in victims of fatal overdosage.
Opioids are substances that, when reaching opioid receptors, have effects similar to those of morphine. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, restless leg syndrome, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids derived from opium are used recreationally by some, at first for their euphoric effects and then to react to withdrawal.
Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use and frequent, escalating recreational use of opioids typically results in addiction. An overdose or concurrent use with other depressant drugs like benzodiazepines or alcohol commonly results in death from respiratory depression.
Opioids act by binding to opioid receptors. They are found principally in the central and peripheral nervous system and the gastrointestinal tract. These receptors mediate both the psychoactive and the somatic effects of opioids. Opioid drugs include partial agonists, like the anti-diarrhea drug loperamide and antagonists like naloxegol for opioid-induced constipation. They do not cross the blood-brain barrier, but can displace other opioids from binding to those receptors.
Because opioids are addictive and may result in fatal overdose, most are controlled substances. In 2013, between 28 and 38 million people used opioids illicitly (0.6% to 0.8% of the global population between the ages of 15 and 65). In 2011, an estimated 4 million people in the United States used opioids recreationally or were dependent on them. As of 2015, increased rates of recreational use and addiction were attributed to over-prescription of opioid medications and inexpensive illicit heroin. Conversely, fears about over-prescribing, exaggerated side effects, and addiction from opioids are similarly blamed for under-treatment of pain.
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The weak opioid codeine, in low doses and combined with one or more other drugs, is commonly available without a prescription and can be used to treat mild pain. Other opioids are usually reserved for the relief of moderate to severe pain.
Opioids are effective for the treatment of acute pain (such as pain following surgery). For immediate relief of moderate to severe acute pain, opioids are frequently the treatment of choice. This is due to their rapid onset, efficacy, and reduced risk of dependence. However, a new report showed a clear risk of prolonged opioid use when opioid analgesics are initiated for an acute pain management following surgery or trauma. They have also been found to be important in palliative care to help with the severe, chronic, disabling pain that may occur in some terminal conditions such as cancer and degenerative conditions such as rheumatoid arthritis. In many cases, opioids are a successful long-term care strategy for those with chronic cancer pain.