Fentanyl: powerful opioid, what (side) effects?

THE Fentanyl is a opioid drug diverted from its use painkiller to be taken as dope. A truly health crisis related to misuse of opioids affects UNITED STATES since the early 2000s. “There Opioid-related mortality is increasingly due to Fentanyl” indicates an inventory published in 2021 by theFrench Observatory of Drugs and Addictive Tendencies. “He does not exist not currently in France risk of a “opioid crisis” comparable to the one in North America (…) but their strong lethal dimension nevertheless implies active surveillance” add its authors.

Definition: What is Fentanyl?

Fentanyl is a synthetic opioid analgesic (laboratory-made) derivative of phenylpiperidine. Discovered in the late 1950s, it is used as pain medication, its effect analgesic being about 80 to 100 times more potent than that of morphine and at least 50 times more potent than heroin. Fentanyl is classified as a narcotic internationally since 1964, due to its health hazards, risks in case of misuse and complexity of handling. In man, the lethal dose of fentanyl is estimated at 2 mg.

How is Fentanyl used in France?

Fentanyl has in France a marketing authorization for its medical use as an analgesic. It comes in the form of patches, lollipops, sublingual tablets, nasal spray or as an injectable solution. In France, the prescription of Fentanyl is indicated in the management of chronic pain, particularly original cancerous.

What are the effects of Fentanyl?

Opioids like Fentanyl have analgesic and sedative effects hence their use in the management of pain. Fentanyl is a strong painkiller, Tier 3, like the morphine. It aims to relieve “very intense” pain.

Why is Fentanyl taken as a drug?

Among the reasons that may lead to taking Fentanyl outside the medical framework, the fact that it provides feeling of relaxationa feeling of well-being and calmthat he alleviates anxiety, sadness and causes a euphoria. Repeated use of Fentanyl prompts increased doses to experience these effects. This is where addiction can develop.

What are the side effects of fentanyl?

The most common side effects are:

• of the nausea, constipation, drowsiness
• dizziness and headaches, breathing difficulties
• dry mouth, sweating, feeling tired
• in the mouth : pain, irritation of the oral mucosa, mouth ulcer, cavities, loss of teeth

More rarelyit is possible to see:

• hypersensitivity,
• loss of appetite or even anorexia,
• psychiatric disorders (including euphoria),
• memory loss, changes in taste,
• tremors, trouble sleeping,
• blurred vision, narrowing of the pupil,
• hypotension, hypothermia,
• various digestive disorders, skin manifestations, erectile dysfunction,
• withdrawal syndrome or accidental overdose.

Repeated use of fentanyl or its derivatives, even when prescribed by a physician, may cause risk of addiction. In case of heavy consumption, there is a risk of overdose. In case of overdose in Fentanyl (overdose), respiratory depression, shock, severe hypotension, muscle rigidity or coma can occur. These signs are to be taken seriously, they can lead to death.

Mode of action and onset of action of Fentanyl

Fentanyl acts on opioid receptors. This type of receptor present in the brain, spinal cord and digestive system module in particular the response to pain, mood, physical dependence and the 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 by the oral mucosabut 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 pill form 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).

What are the contraindications of fentanyl?

► Intraoral fentanyl is contraindicated in case 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 contraindicated in the event of simultaneous administration or within two weeks of stopping an MAOI.

► Fentanyl patches are equally contraindicated in acute or post-operative painand of severe or even fatal hypoventilation which could result. They are contraindicated when combined with buprenorphine or nalbuphine.

► The injectable form is also contraindicated in combination with agonist-antagonist opioids 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.

Prescription conditions: Fentanyl only by 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 period of 28 days, unit delivery corresponding to the exact number of doses prescribed, delivery split every 7 days unless expressly mentioned by the doctor, overlapping of prescriptions impossible unless expressly mentioned by the doctor, prescription written in full).