What is the effect of Fentanyl (synthetic opioid analgesic)?

From the Guidelines

Fentanyl should only be prescribed for severe, continuous pain in patients who have received certain dosages of immediate-release opioids daily for at least 1 week, due to its high potency and risk of respiratory depression or death. Fentanyl is a potent synthetic opioid analgesic that is 50-100 times stronger than morphine, and its use has been associated with a high risk of overdose and death, particularly when used inappropriately or in combination with other substances 1. The CDC clinical practice guideline for prescribing opioids for pain recommends that extended-release/long-acting (ER/LA) opioids, such as fentanyl, should be reserved for management of pain severe enough to require daily, around-the-clock, long-term opioid treatment when alternative treatment options are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain 1.

When prescribing fentanyl, healthcare providers should exercise extreme caution and carefully individualize dosing based on patient factors, pain severity, and prior opioid exposure. The use of fentanyl should be limited to appropriate clinical scenarios, and patients should be closely monitored for signs of respiratory depression or other adverse effects. Additionally, naloxone (typically 0.4-2 mg IV/IM/intranasal) should be available to reverse fentanyl overdose, and multiple doses may be required due to fentanyl's potency.

Some key considerations when prescribing fentanyl include:

• Fentanyl should not be used to treat acute pain or for intermittent use 1
• Fentanyl should only be prescribed for patients who have received certain dosages of immediate-release opioids daily for at least 1 week 1
• Clinicians should use additional caution with ER/LA opioids and consider a longer dosing interval when prescribing to patients with renal or hepatic dysfunction 1
• Methadone and transdermal fentanyl have unique characteristics that make safe prescribing especially challenging, and clinicians should be familiar with their risk profiles and educate patients accordingly 1.

Overall, the use of fentanyl should be approached with caution, and healthcare providers should carefully weigh the potential benefits and risks of prescribing this potent opioid analgesic, as supported by the most recent and highest quality study available 1.

From the FDA Drug Label

Fentanyl is an opioid analgesic. Fentanyl interacts predominately with the opioid mu-receptor. The main effect of fentanyl is as an opioid analgesic, and it interacts with the opioid mu-receptor.

• Key points about fentanyl include:
  • It is an opioid analgesic
  • It interacts with the opioid mu-receptor
  • It has effects on the central nervous system, including analgesia, alterations in mood, euphoria, dysphoria, and drowsiness 2

From the Research

Fentanyl Overview

• Fentanyl is a powerful opioid anesthetic and analgesic that has caused an increasing public health threat in the United States and elsewhere 3.
• It was initially approved and used for the treatment of moderate to severe pain, especially cancer pain, but recent years have seen a growing concern that fentanyl and its analogs are widely synthesized in laboratories and adulterated with illicit supplies of heroin, cocaine, methamphetamine, and counterfeit pills 3.

Fentanyl-Related Overdose

• Fentanyl overdose deaths have reached "epidemic" levels in North America, with death in opioid overdose invariably resulting from respiratory depression 4.
• Fentanyl depresses both respiratory rate and tidal volume, and its potency, rate of onset, lowered sensitivity to naloxone, and lowered cross tolerance to heroin make it more likely to cause opioid overdose deaths than other commonly abused opioids 4.
• The abuse potential of fentanyl and fentanyl analogues is high, and overdose can result in serious harm and even death 5.

Treatment and Prevention

• Medication approaches to treating opioid use disorder remain the standard of care, and there are new promising pharmacological approaches to treating methamphetamine use disorder 6.
• Educating patients and physicians, making rescue kits easily accessible, developing vaccines to prevent opioid addiction, and creating new tamper-resistant fentanyl formulations may help prevent fentanyl misuse, therapeutic errors, and the repercussions that follow 5.
• Naloxone, the opioid antagonist widely used to treat opioid overdose, can reverse the depression of respiration by morphine more readily than that by fentanyl, whereas diprenorphine, a more lipophilic antagonist, is equipotent in reversing fentanyl and morphine depression of respiration 4.

Epidemiology

• Overdose due to illicit synthetic opioids, such as fentanyl and fentanyl analogs, continues to rise in the US, both preceding and during the COVID-19 pandemic 6.
• Fentanyl-related overdose is rising in new geographic areas, and stimulant-related overdose is also increasing nationwide, driven by methamphetamine and cocaine 6.
• Polysubstance use, such as the use of a stimulant along with an opioid, is driving stimulant-related overdose, and other medical consequences of injection drug use are rising, including HIV and hepatitis C infections 6.