Fentanyl

Fentanyl was developed by Paul Janssen in 1960 and was the first anilinopiperidine at the time. By modifying the molecular formula, it has since been possible to develop some derivatives from fentanyl that are more controllable.

What is fentanyl?

At Fentanyl It is a synthetic opiod that is used in anesthesia as a potent pain reliever and in the treatment of chronic pain as a transdermal therapeutic system.

It acts as a so-called agonist. In Germany and Switzerland, fentanyl falls under the Narcotics Act, in Austria under the Narcotics Act.

Pharmacological effect

Fentanyl primarily has an analgesic (strong pain reliever) and sedative (calming) effect. It is 120 times more potent than morphine, which leads to greater effectiveness and a shorter duration of action.

When administered intravenously, fentanyl takes effect after two to five minutes, and the so-called half-life is around three to twelve hours. The dose for effective treatment is 0.01 mg per kilogram of body weight, the dose that leads to death 3.1 mg per kilogram of body weight, the last figure referring to rats. Even lower doses can therefore lead to death in humans due to respiratory depression.

The side effects can, however, generally be compared with those of morphine. Fentanyl dissolves well in fat and can therefore be distributed well in fatty tissue. It is mainly metabolized in the liver, less than ten percent is excreted unchanged via the kidneys. Depending on the patient's condition and the dose administered, fentanyl can impair cognitive abilities, have a calming effect, lead to impaired consciousness or induce a sleep-like state. The latter point is the reason for its use in anesthesia.

Fentanyl is mainly used in operations in conjunction with a sleeping pill as a pain reliever and can optionally also be used as a muscle relaxant. Since fentanyl is stored and released again with difficulty in a controlled manner in adipose tissue due to its lipophilicity, the substances remifentanil, alfentanil or sufentanil are often used as alternatives.

Fentanyl has a calming effect; this effect can be increased by other sedatives as well as alcohol or reduced by taking other opioids. Serious circulatory and respiratory disorders can occur in connection with the intake of so-called monoamine oxidase inhibitors, which is why there should be a period of at least 14 days between each intake.

When using pain patches, there may also be an interaction with preparations such as omeprazole, furosemide or glibenclamide. There may also be interactions with preparations containing St. John's wort. For smokers, it may be necessary to adjust the dose of fentanyl.

If a drug containing fentanyl is taken together with a drug with a serotonergic effect, it can lead to a dangerous serotonin syndrome, the symptoms of which can be blood pressure crises, hallucinations or a coma.

Medical application & use

Fentanyl is used as fentanyl dihydrogen citrate in three forms: as a transdermal therapeutic system, as intravenous administration in anesthesia and emergency medicine, and as an oral-transmucosal therapeutic system (as a lozenge for breakthrough pain). Nycomed's Instanyl, the first approved fentanyl nasal spray in the EU, has been approved for breakthrough pain since September 1, 2009.

This drug is suitable for the treatment of breakthrough pain in adult patients who are already receiving basic therapy with an opioid for chronic cancer pain. Fentanyl has a strong analgesic effect and is therefore usually used perioperatively (before an operation) or after an operation.

In the case of severe, chronic pain in cancer patients, it is used in the form of a skin patch as an analgesic, and it can also be used in analgesia for chronic pain that is not related to a tumor. The emergency doctor may use fentanyl in the case of acute pain in the rescue service.

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Risks & side effects

As a side effect of Fentanyl It can lead to impaired breathing and even respiratory depression. Furthermore, side effects such as cramped or rigid muscles, slowed heart activity, euphoria or even anxiety, constricted pupils, vomiting, nausea and constipation are possible. If the injection is given quickly, it can, in rare cases, lead to a brief urge to cough.