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Fentanyl - Fentanyl

Generality

Fentanyl - also known as fentanyl or fentanyl - is an opiate drug derived from morphine, the famous alkaloid extracted from opium poppy. Compared to its precursor - which already has marked analgesic properties - it has an effect 30-80 times higher, but a shorter half-life (about an hour against the three of morphine).

Fentanyl - Chemical Structure

Fentanyl is generally administered before or after surgery - as an anesthetic or as a post-operative sedative / analgesic - and in the treatment of chronic pain of tumor origin.

Fentanyl is available in pharmaceutical formulations suitable for oral administration, inhalation, transdermal (through the application of a transdermal patch) and parenterally.

Examples of medicinal specialties containing Fentanyl

  • Effentora ®
  • Durogesic ®
  • Instanyl ®
  • Ionsys ®
  • PecFent ®

Therapeutic indications

The use of fentanyl is indicated for:

  • Treatment of breakthrough pain in patients with neoplastic diseases who are already on therapy with other opioid analgesics for the treatment of chronic cancer pain. Episodic intense pain is a sudden exacerbation of pain that already afflicts cancer patients;
  • Treatment of chronic neoplastic pain.

Furthermore, as mentioned, fentanyl is used in the anesthetic field before surgery and as a post-operative sedative and / or analgesic.

Warnings

Before taking fentanyl, you must tell your doctor if:

  • There is a head injury;
  • You suffer from respiratory diseases;
  • You are suffering from myasthenia gravis;
  • It is hypothesis and / or bradycardia;
  • You are suffering from liver and / or kidney diseases;
  • You are suffering from brain tumors or if you suffer from intracranial hypertension.

Simultaneous intake of fentanyl and alcohol should be avoided, as this increases fentanyl-induced drowsiness.

When using the fentanyl-based transdermal patch, it is necessary to inform your doctor if fever occurs. This is because the rate of drug release from the patch increases if the patient has a high body temperature. When the body temperature exceeds 39 ° C the resulting overdose could significantly depress the center of the breath and make the patient enter a coma. For the same reason, exposure to heat sources, including artificial ones (electric blankets, saunas, hot baths, direct and prolonged exposure to sunlight) should be avoided. To reduce the risk of overdose, the patient must also strictly comply with what the doctor has prescribed and the warnings on the information leaflet.

Fentanyl may decrease the ability to drive and / or operate machinery, therefore, these activities should be avoided.

For those who do sports, the use of fentanyl without therapeutic necessity is doping and in any case can determine positivity to doping tests even when the drug is taken for therapeutic purposes.

Interactions with other drugs

Concomitant use of fentanyl and the following drugs may increase the effects of fentanyl itself:

  • Azole antifungals, such as ketoconazole, itraconazole, etc .;
  • Macrolides, antibiotic drugs;
  • Some antivirals, such as, for example, ritonavir;
  • Monoamine oxidase inhibitors (or MAOIs), drugs used in the treatment of Parkinson's disease and depression;
  • Drugs containing alcohol .

In contrast, concomitant administration of fentanyl and buprenorphine or pentazocine may reduce the effects of fentanyl itself.

Furthermore, fentanyl may intensify the effect of drugs that are able to induce sleepiness. Among these, we recall:

  • Other opioid painkillers ;
  • General anesthetics ;
  • Muscle relaxants ;
  • Antidepressants ;
  • Anxiolytics ;
  • Antipsychotics ;
  • Some antihistamines ;
  • Clonidine, an antihypertensive drug.

However, it is always good to inform your doctor if you are taking - or if you have recently been - medications of any kind, including over-the-counter medicines and herbal and homeopathic products.

Side effects

Fentanyl can cause several side effects, although not all patients experience them.

Listed below are some of the major adverse effects that may occur during drug therapy.

Nervous system disorders

Treatment with fentanyl may cause:

  • Excessive sleepiness;
  • dizziness;
  • Headache;
  • Fatigue;
  • Lack of energy;
  • Weakness;
  • Alteration of the sense of taste;
  • Alteration of the sense of smell.

Psychiatric disorders

Fentanyl therapy may cause:

  • Euphoria;
  • Depression;
  • Paranoia;
  • Confusion;
  • Disorientation;
  • Sleep disorders;
  • Anxiety;
  • Restlessness;
  • Mood swings.

Gastrointestinal disorders

Treatment with fentanyl may cause nausea, vomiting and constipation.

Skin and subcutaneous tissue disorders

Fentanyl therapy may promote the onset of:

  • Skin eruptions;
  • Itch;
  • Sweating.

Other side effects

Other side effects that may occur during treatment with fentanyl include:

  • Tolerance and dependence;
  • Allergic reactions in sensitive individuals;
  • Dyspnea or wheezing;
  • Respiratory depression;
  • Dry mouth and inflammation of the oral mucosa;
  • Joint pain;
  • Joint and muscle stiffness;
  • Loss of appetite;
  • Visual disturbances;
  • Reactions at the site of administration.

Overdose

If overdoses of fentanyl are taken, symptoms such as:

  • Respiratory depression;
  • bradycardia;
  • Severe drowsiness;
  • Moist and cold skin;
  • Difficulty walking or talking;
  • Dizziness;
  • Confusion.

If a fentanyl overdose is suspected, it is necessary to inform the doctor immediately and seek medical assistance.

Action mechanism

Fentanyl performs its pain-relieving action by interacting with opioid μ receptors.

These receptors are located along the pain pathways of our body and their task is precisely to modulate the neurotransmission of painful stimuli. More in detail, when these receptors are stimulated, analgesia is induced.

Fentanyl - as an opioid receptor agonist μ - is able to activate them thus exerting its potency analgesic action.

Method of use and dosage

Fentanyl is available for:

  • Oral administration in the form of pharmaceutical formulations that allow the absorption of the drug in the oral cavity, such as orosoluble tablets, sublingual tablets, orosoluble tablets for oral mucosa and buccal film.
  • Administration by inhalation in the form of a nasal spray.
  • Transdermal administration in the form of a transdermal patch.
  • Parenteral administration in the form of a solution for injection.

To avoid the appearance of dangerous adverse reactions, during treatment with the drug, it is necessary to scrupulously follow all the indications provided by the doctor, both as regards the amount of fentanyl to be taken, both as regards the frequency of administration and the duration of treatment.

Treatment of breakthrough pain

For the treatment of breakthrough pain, fentanyl is usually administered orally or by inhalation.

The dose of the drug to be administered must be established by the doctor on an individual basis. Generally, treatment with low doses of fentanyl is started and will be gradually increased until the ideal dosage is reached.

It is important to remember that fentanyl should not be used for the treatment of episodic acute pain in patients who do not regularly take opioid drugs or who have not taken them for at least a week, since, in these cases, the administration of the drug may increase the risk of onset of respiratory depression and / or respiratory arrest.

Furthermore, it is good to know that the use of the nasal spray is contraindicated in patients suffering from frequent episodes of blood to the nose.

Treatment of chronic pain

For the treatment of chronic pain, the fentanyl-based transdermal patch is used.

The transdermal patches are equipped with a central tank containing the drug; there are patches with different dosages and each of them releases a very precise quantity (directly proportional to its surface) of fentanyl for about 72 hours.

After the first application of fentanyl patches, sufficient plasma concentrations for optimal analgesia are reached only after 10-14 hours.

Again, the doctor will determine the optimal dosage to be used in each patient.

Use of fentanyl in the anesthetic field or as a post-operative sedative / analgesic

When used in the anesthetic field or as a post-operative sedative / analgesic, fentanyl is administered intramuscularly or intravenously.

The medicine will be administered only and exclusively by highly specialized personnel.

Pregnancy and breastfeeding

The use of fentanyl in pregnancy is not recommended, except when the doctor does not consider it absolutely necessary. In particular, the use of the drug during birth is contraindicated, since it can cause respiratory depression in the newborn.

Fentanyl is excreted in breast milk, therefore breast-feeding mothers should not take the drug. If fentanyl is still necessary, breastfeeding must be stopped, both during the treatment and for a period of 48-72 hours from the end of the treatment.

In any case, pregnant women and breastfeeding mothers should always consult their doctor before using any type of medication.

Contraindications

The use of fentanyl is contraindicated in the following cases:

  • In patients with known hypersensitivity to the same fentanyl;
  • In patients suffering from short-term pain other than episodic intense pain and due to other causes, such as lesions, headache surgery or migraines (only when fentanyl is used for the treatment of breakthrough pain);
  • In patients with respiratory depression or chronic obstructive pulmonary disease (COPD);
  • In pregnancy (especially during labor);
  • During breastfeeding.

Furthermore, when used for the treatment of pain, fentanyl is contraindicated in children and adolescents under 18 years of age; when, on the other hand, the drug is used in the anesthetic field, its use is contraindicated in children under two years of age.

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