How does fentanyl compare to heroin or other opiates?

You can access naloxone from most pharmacists in the U.S. without a prescription. If you, a family member, or a friend take illegal drugs, it is important to have immediate access to naloxone to help possibly save a life. One 2 milligram (mg) dose of fentanyl is enough to kill an adult, but may be more or less depending upon your body size, opioid tolerance, and former usage. Fentanyl can kill you within a matter of 2 minutes, usually due to respiratory failure (breathing that has stopped).

Other drugs may interact with fentanyl, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Oxycodone is an opioid pain medication used to treat moderate to severe pain. Naloxone (Narcan nasal spray, Kloxxado nasal spray, Zimhi injection, Naloxone injection) is a safe and easily accessible medication used to reverse an opioid overdose and help restore breathing by blocking or reversing the opioid effects. It is not currently possible to predict the occurrence of secondary plasma peaks, and it is not known if secondary peaking in the plasma affects IMF-related withdrawal presentation or contributes to late-onset overdose risk via respiratory depression. It must be introduced into the bloodstream or a mucus membrane in order for someone to feel the effects.

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Another report has implicated fentanyl as a potential cause of pulsus alternans in a patient with aortic stenosis and congestive heart failure. Use with CYP3A4 inhibitors or inducers may change fentanyl plasma levels resulting in a fatal overdose of fentanyl and monitoring is recommended. Pinpoint pupils, medically termed miosis, refer to abnormally small, constricted pupils that do not dilate appropriately in low light. This symptom is a significant clinical clue and can be caused by various drugs and toxins. Some examples include opioids, clonidine, buspirone, and metoclopramide. Fentanyl sublingual spray should be used together with other non-fentanyl narcotic pain medicines that are used around the clock.

1. Absorption and Applications to IMF:

• They are less potent but can still be deadly due to respiratory depression (breathing that has slowed or stopped) if recommended doses are exceeded, or they are combined with alcohol, benzodiazepines or other CNS depressant drugs.
• Using this medicine while you are pregnant may cause serious unwanted effects in your newborn baby.
• Some other ways to spot fentanyl-laced weed include smelling it or examining it closely for the common signs of a laced joint.
• It is therefore imperative to know what fentanyl-laced weed is, and how to tell if weed is laced with fentanyl.

It has a rapid onset (within 2 min following intravenous administration) and short serum half-life (~1 h). In order to avoid precipitating severe withdrawal, the American Heart Association recommends starting with a small dose of naloxone (0.4 mg intramuscularly or 2 mg intranasally). However, recent reports suggest that higher doses or repeated dosing of naloxone (due to recurrence of respiratory depression) may be required to reverse fentanyl-induced respiratory depression (Fairbairn et al., 2017; Lynn and Galinkin, 2018; Somerville et al., 2017). The reason that higher doses of naloxone may be required is not entirely clear. Possibilities are that a large dose of naloxone is needed simply because a large dose of fentanyl was used, a fentanyl analog was used that is not sensitive to naloxone, or, because the onset of fentanyl-induced respiration is so rapid, the naloxone was administered after the individual was already deceased. Another possibility is that fentanyl and naloxone may share an influx transporter into the brain and that when high doses of fentanyl are used, the transporter becomes saturated, so naloxone is not able to cross the blood-brain barrier (Lynn and Galinkin, 2018; Suzuki et al., 2010).

• If you, a family member, or a friend take illegal drugs, it is important to have immediate access to naloxone to help possibly save a life.
• Fentanyl is a synthetic opioid medicine that is up to 100 times stronger than other opioids like morphine, heroin, or oxycodone.
• This is further compounded by fentanyl’s metabolic profile, which is characterized by a major metabolite (norfentanyl) and an array of minor metabolites that may themselves be able to confer opioid effects, which is important to consider in future research with persons who use IMF regularly.
• Discontinue all other extended-release opioids when beginning therapy.

2. Plasma Protein Binding and Implications for IMF:

Systemic injection of a high-efficacy agonist such as fentanyl was more potent at blocking the depression of ICSS caused by an acute pain stimulus (Altarifi et al., 2015). A previous study reported similar findings for heroin (Ewan and Martin, 2011a). Interestingly, morphine failed to facilitate ICSS in the presence of chronic neuropathic pain (Ewan and Martin, 2011b) or in an acute model of acute visceral pain (Altarifi et al., 2015). Participants who were maintained on morphine (30 mg orally, given 4 times per day) reported that they would pay $8.50 for a fentanyl dose of 250 μg/70 kg i.v. Compared to $2.50 for saline, and ratings of “bad drug effects” and “nauseated” were not significantly different from saline (Comer et al., 2008).

Fentanyl Use and Overdose Prevention Tips

Although later reports described non-medical use of the fentanyl transdermal patch by patients and/or individuals with substance use disorders (Jumbelic, 2010), overall prevalence rates of non-medical use of FDA-approved fentanyl products remained low. But in 2006, a surge in fentanyl-related overdose deaths and Drug Enforcement Agency (DEA) seizures of illicitly manufactured fentanyl occurred in the U.S. This “crisis” was attributed to fentanyl being mixed into heroin (Drug Enforcement Administration, 2016). The origin of this crisis was traced to a single clandestine laboratory that was manufacturing fentanyl illicitly, and when the laboratory was shut down, fentanyl overdose deaths and DEA seizures of fentanyl rapidly declined.

At intravenous (i.v.) doses up to approximately 250 μg/70 kg, fentanyl increased positive subjective effects in 4 studies (e.g., it increased ratings of euphoria, feelings of well-being, or pleasantness of drug effects in Hoehe, 1988; Hoehe et al., 1988; Manner et al., 1987; and Matussek and Hoehe, 1989). Fentanyl doses ranging between 50 μg/70 kg and approximately 200 μg/70 kg, fentanyl did not increase positive subjective responses (Ghoneim et al., 1975; Scamman et al., 1984; fentanyl laced weed : an overview Zacny et al., 1996a), and in 2 additional studies, the positive subjective effects produced by fentanyl were equivocal (Zacny et al., 1992a, b). The negative findings reported by Ghoneim et al. (1975) and Scamman et al. (1984) were possibly due to the fact that the peak effects of fentanyl were missed because measurements of subjective responses did not begin until 30 min after drug administration.

Clinical pharmacology of fentanyl: focus on abuse potential

After naloxone is given, the person giving it must call emergency services. Human drug administration studies align with these rodent studies. Fentanyl is a synthetic opioid that may be prescribed for difficult-to-treat pain. The prescription version may come in the form of a tablet, lozenge, or patch, but fentanyl may be used illegally to lace other substances, such as cocaine.Note that doses are not equivalent between the different formulations (for example a 25mcg fentanyl patch DOES NOT EQUAL 25mcg of fentanyl injection). The substitution of one fentanyl product for a different type of fentanyl product (for example Subsys for Duragesic) may result in a fatal overdose. Opioids were involved in 68,630 overdose deaths in 2020 (74.8% of all drug overdose deaths).

Assess risk prior to initiation and monitor for signs of misuse, abuse, and addiction during treatment. The emergency and referral resources listed above are available to individuals located in the United States and are not operated by the National Institute on Drug Abuse (NIDA). NIDA is a biomedical research organization and does not provide personalized medical advice, treatment, counseling, or legal consultation.

Has a currently accepted medical use in treatment in the United States or a currently accepted medical use with severe restrictions. The risk of death can be higher with the use of fentanyl compared to heroin due to its high potency. Errors during illicit production can occur due to the small microgram (mcg) dose.

Supporting the hypothesis that pain negatively influences the abuse potential of opioid analgesics are reports that non-contingent delivery of analgesics such as indomethacin (Lyness et al., 1989) or dexamethasone (Colpaert et al., 2001) decreased intravenous morphine or oral fentanyl self-administration, respectively. However, others have reported an increase in oral fentanyl consumption in a model of polyarthritis compared to pain-free or chronic neuropathic pain in rats (Kupers and Gybels, 1995). Fentanyl is highly lipophilic, lending itself to rapid absorption by highly-perfused tissues (including the brain) before redistributing from these tissues to muscle and fat. Fentanyl is eliminated primarily by metabolism and urinary excretion of metabolites (norfentanyl and other minor metabolites). Fentanyl has a long terminal elimination, with a documented secondary peaking phenomenon that can manifest as “fentanyl rebound”. Clinical implications in overdose (respiratory depression, muscle rigidity and “wooden chest syndrome”) and opioid use disorder treatment (subjective effects, withdrawal and buprenorphine-precipitated withdrawal) are discussed.