- Fentanyl: mechanism of action
- Fentanyl: application
- Fentanyl: contraindications
- Fentanyl: interactions
- Fental: side effects
- Fentanyl: use during pregnancy and lactation
- Fentanyl as a drug: victim of Prince and 30 million Americans
- Fenantyl and terrorism
- Fentanyl and the death pen alty
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Fentanyl belongs to the group of opioid analgesics and is available in many different forms - there are both intravenous fentanyl preparations on the market as well as agents containing this substance in the form of sprays or patches applied to the skin. In medicine, this drug is primarily used to relieve severe pain, but fentanyl is also used outside medicine - it's a drug that is killing America.
Fentanylwas discovered in Belgium in 1959 - this discovery is attributed to Paul Janssen. Pretty soon, less than 10 years later, in 1968, this compound was approved for medical use in the United States.
Over the years, this preparation has gained more and more popularity - according to statistics from 2022, fentanyl is the most commonly used synthetic opioid in medicine.
Estimates of how much fentanyl are consumed annually around the world are far more astonishing.
Well, just as patients are administered only micrograms of this drug (e.g. 200 micrograms) at a time, according to statistics - more than one and a half tons of fentanyl was used worldwide in 2015.
Fentanyl: mechanism of action
Fentanyl is an agonist of µ-opioid receptors. By binding with these structures, the preparation reduces the intracellular calcium level, which ultimately reduces the release of neurotransmitters related to the perception of pain from the cells.
It is clearly visible what the effect of taking fentanyl is - this agent reduces the feeling of pain and its effect is up to 100 times stronger than morphine.
This dependence results, among others, from because fentanyl accumulates in adipose tissue, from which it is gradually released into the blood, and because this drug - thanks to its lipophilicity - much easier than morphine than morphine crosses the blood-brain barrier and thus easily penetrates the central system nervous.
In medicine, fentanyl has found several different uses. First of all, this agent is used in patients with chronic pain caused by cancer.
For this purpose, patients may take the drug in the following forms:
- buccal tablets
- nasal spray
- transdermal patches
The last form of fentanyl-containing drugs is often appreciated by patients - the patch stuck to the skin is changed only after 72 hours, during which the painkiller is evenly released from the patch into the patient's body (it is undoubtedly the convenient method of administering the drug).
Fentanyl is sometimes administered to patients also intravenously - this route of administration is used primarily during various surgical procedures, where the drug can be used both for analgesia (i.e. pain relief) and anesthesia.
In the intravenous form, fentanyl is also used in the treatment of acute pain, e.g. postoperative pain or accompanying a heart attack.
As a pain reliever or in surgical procedures, fentanyl can work perfectly well, but it should be emphasized here that there are some contraindications to its use. Among them, the following are mainly mentioned:
- breathing disorders (fentanyl - especially in high doses - may lead to respiratory arrest)
- the patient's use of monoamine oxidase inhibitors, i.e. MAO inhibitors (administering fentanyl to the patient who takes these drugs may cause him to develop serotonin syndrome)
- existence in the patient of some respiratory disease with obstruction of the respiratory tract (e.g. chronic obstructive pulmonary disease)
- hypersensitivity to fentanyl
There are also a number of problems where fentanyl should be used with extreme caution in patients. I am talking about:
- a heart disorder involving a slow heartbeat (known as bradyarrhythmias)
- renal and hepatic dysfunction
- disturbed consciousness
The dosage of fentanyl may require modification in the above-mentioned conditions, but also in the case of its use in elderly patients.
Before recommending a patient to use fentanyl, it is important to know if they are taking any other medications - the opioid painkiller can interact in various ways with other medications.
The most important are the interactions of fentanyl with those preparations that depress the activity of the central nervous system - such areamong others :
Fental: side effects
Like any other drug, fentanyl and its use can lead to certain side effects. Among the most common side effects of taking fentanyl are
- respiratory depression
- drop in blood pressure
- muscle stiffness
Patients who are prescribed fentanyl (especially those who can use it for a long time, e.g. because of pain associated with cancer) should be warned against the fact that the drug may lead to a deterioration of psychomotor performance. Therefore, you should not drive while taking this opioid.
Fentanyl: use during pregnancy and lactation
The FDA classifies fentanyl as a category C drug, so it is not used during pregnancy, unless there are clear indications for it.
The use of fentanyl during labor - due to the risk of respiratory depression in the child - is also not recommended.
In lactating women, if necessary, painkillers other than fentanyl are used, because these substances penetrate into the breast milk (if a woman takes fentanyl, she must withhold daily feeding when administered orally, and in the case of using fentanyl). using the patch with this drug, a break in feeding should last at least 3 days after removing the patch from the skin).
Fentanyl as a drug: victim of Prince and 30 million Americans
Fentanyl is used not only in medicine, but also - unfortunately - also for completely different purposes. This drug is sometimes used as a psychoactive substance - it is used as a substitute for heroin. Recreational fentanyl can lead to feelings of euphoria, relaxation and well-being, but also a feeling that any problems are not really important at all.
As a drug, fentanyl is sometimes taken orally and intravenously, and people sometimes smoke it.
Each addiction to psychoactive substances is very dangerous, addiction to fentanyl is special - an overdose of this substance (which is not difficult to do) can lead to the patient's death in a short time (mainly due to the possibility of depression respiratory).
The problem is serious, as reported by the Americanshe alth organizations, nearly 30 million people died from fentanyl use in 2022.
The examples of deaths caused by the abuse of fentanyl do not need to be looked for in any particular way - we can mention here, for example, the American musician, Prince, who died in 2016, who - after his death - was found to have died due to an overdose of fentanyl.
Fenantyl and terrorism
Non-medically, fentanyl has other uses as well. As another example, we can describe the terrorist attack that took place in 2002 in Moscow.
Teatr na Dubrowce was seized by terrorists on October 23 of the above-mentioned year - there were almost 1,000 people in the building at that time.
The hostages were held there for 3 consecutive days, until finally, on October 26, Russian special forces launched an assault on the theater.
Before entering it, however, sleeping gas was introduced into the building - the goal was, among others, euthanizing the victims there, which would reduce the number of potential losses in people.
The expected effect was not fully achieved - not only terrorists were eventually killed, but also over 100 hostages who poisoned themselves with the gas released into the theater. One of the substances that this gas contained was fentanyl.
Fentanyl and the death pen alty
Yet another use of fentanyl is the use of the preparation to carry out the death pen alty. For the first time, an execution with the use of this drug in the United States was carried out in 2022.
It should be emphasized, however, that the prisoner was then given (apart from fentanyl, which was to lead primarily to respiratory depression) also other drugs, which were diazepam, cisatracurium and potassium chloride.