Fentanyl is a very powerful and potentially fatal opioid pain reliever. It was an overdose of fentanyl that caused the death of American singers Prince (2016) and Coolio (2022).
[Mise à jour le 7 avril 2023 à 15h48] THE fentanyl is a medicine very powerful painkiller. After being at theorigin of the death of singer Prince in 2016, fentanyl would also have caused the death of American rapper Coolio in September 2022, according to the report of the medical examiner published Thursday, April 6, 2023 by the county of Los Angeles, relayed by Reuters. Coolio would have made a accidental overdosehe suffered from heart disease and asthma.
Definition: what is fentanyl?
Fentanyl is a synthetic opioid analgesic derived from phenylpiperidine, which acts primarily on μ-type morphine receptors. Discovered in the late 1950s, it is used as pain medication, its effect analgesic being about 100 times more potent than that of morphine and at least 50 times more potent than that of heroin. This medicine is on the list of narcotics, because of its health hazards, the risks in the event of misuse and the resulting complexity of handling. In man, the lethal dose of fentanyl is estimated at 2 mg.
Indications: why take fentanyl?
Fentanyl may be indicated in the management of bouts of paroxysmal pain (stronger and transient bouts of pain that is already present and stable) of origin cancerousin postoperative analgesia, intense chronic pain, anesthesia and neuroleptanalgesia (anesthesia caused by both an analgesic and a neuroleptic).
How does fentanyl work?
Fentanyl is a pure morphinomimetic agonist, i.e. it acts on morphine receptors, and more particularly on the μ morphine receptor. This type of receptor present in the brain, spinal cord and digestive system module including the rresponse to pain, mood, physical dependence and gastrointestinal motility. The sought-after therapeutic action of fentanyl is above all a analgesia (pain relief). Fentanyl is a lipophilic molecule (with high affinity for fatty substances and low affinity for aqueous substances) and its absorption is very rapid through the oral mucosa, but it can also be administered by injection or transdermally. The action of fentanyl on pain is rapid, just like its duration of action, it depends on the dose administered and thus on its plasma concentration.
Fentanyl in patch: when, what delay of action?
Fentanyl patches (transdermal patches) are indicated for adults in the treatment of severe chronic pain which require long-term continuous administration of opioids, as well as for severe chronic pain in children (from 2 years of age) receiving opioid treatment. The patches allow a continuous release of fentanyl into the blood, by transdermal passage, for 72 hours, i.e. the duration of application of the patch. After applying a first patch, the maximum effect is observed after 12 to 24 hours. The effect then remains stable during subsequent applications (every 72 hours) of patches of the same size. On the other hand, in the event of a change in dosage, a delay of 12 to 24 hours is again necessary after the placement of the patch.
Fentanyl in tablets: when, what delay of action?
Fentanyl in tablet form (sublingual, buccogingival or with buccal applicator) is a fast-acting analgesicit is used in the treatment of bouts of paroxysmal pain in adult patients who are already using opioids as disease-modifying drugs to treat chronic cancer pain. It is absorbed by the oral mucosa in about 30 minutes and its effect on pain is observed between 20 minutes and 4 hours after administration of the drug. The maximum effect is sometimes reached in less than an hour, and up to 8 hours in some cases.
What drugs contain fentanyl?
There are various fentanyl-based drugs on the pharmaceutical market, for which the galenic forms differ. Are marketed:
- Abstral® in sublingual tablet (100 mcg, 200 mcg, 300 mcg, 400 mcg, 600mcg and 800 mcg) as well as its generics,
- Actiq® tablet with buccal applicator (200 mcg, 400 mcg, 600 mcg, 800 mcg, 1200 mcg and 1600 mcg),
- Breakyl® orodispersible film (200 mcg and 400 mcg),
- Durogesic® transdermal device or patch (12 mcg/h, 25 mcg/h, 50 mcg/h, 75 mcg/h and 100 mcg/h) and its generics fentanyl and Matrifen®,
- Effentora® oral-gingival tablet (100 mcg, 200 mcg, 400 mcg, 600 mcg, 800 mcg) and its generics fentanyl,
- Fentanyl Piramal® solution for injection in ampoule (100 mcg/2ml and 500 mcg/10 ml) and its generic fentanyl,
- Fentanyl Renaudin® solution for injection IV/epidural in ampoule (50 mcg/ml),
- Instanyl® solution for nasal spray in a single-dose container or in a multi-dose container (50 mcg, 100 mcg, 200 mcg),
- Pecfent® solution for nasal spray (100 mcg/pulv, 400 mcg/pulv),
- Recivit® sublingual tablet (133 mcg, 267 mcg, 400 mcg, 533 mcg and 800 mcg).
Available with or without a prescription?
Fentanyl can only be obtained through a medical prescription. To be issued, it must also be prescribed on a secure prescription because it is part of the narcotic drugs, for which the regulations are strict and very supervised (maximum prescription duration of 28 days, unit delivery corresponding to the exact number of doses prescribed, split delivery every 7 days unless expressly mentioned by the doctor, overlapping of prescriptions impossible unless expressly mentioned by the doctor, prescription written in full ).
What are the side effects of fentanyl?
The most common side effects are nausea, constipation, drowsiness, dizziness and headache, difficulty breathing, dry mouth, sweating and feeling tired. More rarely, it is possible to observe hypersensitivity, loss of appetite or even anorexia, psychiatric disorders (including euphoria), memory loss, changes in taste, tremors, sleep disorders, vision blurred, narrowing of the pupil, hypotension, hypothermia, various digestive disorders, skin manifestations, erectile dysfunction, withdrawal syndrome or accidental overdose. In the event of an overdose of fentanyl (overdose), respiratory depression, shock, severe hypotension, muscle rigidity or coma can occur. These signs are to be taken seriously, and in some cases can lead to death. Other deleterious effects of fentanyl are tolerance (need higher doses over time) and physical dependencewhich vary greatly from person to person.
What are the contraindications of fentanyl?
Intraoral fentanyl is contraindicated in allergy fentanyl or an excipient contained in the drug, in the absence of background morphine treatment (increased risk of respiratory depression), apart from paroxysmal painful attacks, in case of severe respiratory depressionin case of pulmonary pathology obstructive disease as well as in the event of simultaneous treatment with a medicinal product containing sodium oxybate. The buccogingival film form (Breakyl®) is also contraindicated in the event of simultaneous administration or within two weeks of stopping an MAOI. Fentanyl patches are also contraindicated in acute or postoperative pain due to the impossibility of achieving dose titration in short-term treatment, and severe or even fatal hypoventilation which could result. They are contraindicated when combined with buprenorphine or nalbuphine. The injectable form is also contraindicated in the event of association with opioid agonists-antagonists or naltrexone. Finally, increased vigilance is required when taking fentanyl because of the addiction risk physical, psychic and the abuses that it can entail, as well as the risk of withdrawal syndrome (including neonatal), serotonin syndrome, and risks associated with concomitant intake of sedative drugs and alcohol.