Fentanyl-containing Analgesics: Effects, Uses & Risks

Painkillers containing fentanyl are some of the strongest painkillers available in pharmacies. The active ingredient is used to treat rheumatism and cancer, among other conditions, as well as during surgical procedures. It can be administered in various forms. It also came to sad prominence in the summer of 2016, when it became known that the musician Prince died from an overdose of this drug.

What are painkillers containing fentanyl?

Fentanyl is among the most effective painkillers (analgesics). For example, its effects are considered 50 to 100 times more potent than those of morphine. The opioid requires a prescription and is available only upon presentation of a prescription. In addition, the analgesic falls under the Narcotics Act (BtMG). This means that the prescription of fentanyl finished medicines is exclusively via a BtM prescription. Fentanyl was developed in 1959 by the Belgian chemist and pharmaceutical entrepreneur Paul Janssen (1926-2003). The analgesic entered the market in the 1960s. Over time, the molecular structure of the active ingredient was modified several times, resulting in the development of derivatives that could be better controlled. Thus, in the 1990s, a pain patch was available that was also suitable for the treatment of chronic pain. Later, fentanyl also became available in the form of buccal tablets placed on the mucous membrane of the cheek, lozenges, nasal sprays and oral sprays. One drawback of the drug, however, is that it carries addictive potential.

Pharmacological action

Fentanyl belongs to the opioid group of drugs. These are derived from the opiates found in the poppy plant. They have the property of having an inhibitory effect on the sensation of pain. Opioids are chemically synthesized substances that are produced in the same way as opiates. They have the same mechanism of action as opiates. Fentanyl is one of these opioids. When absorbed into the body, it can rapidly cross the bloodbrain barrier and binds to the opioid receptors in the brain and spinal cord, where it stops pain signals from being transmitted. In this way, the brain is no longer able to register the pain. The analgesic effect of fentanyl is so strong that even small amounts are sufficient to suppress the pain. A variety of dosage forms allow the drug to enter the body in different ways. An almost immediate effect can be achieved by fentanyl injection. It can also be absorbed through the mucous membranes of the mouth and nose, which means that the pain-relieving effect sets in after just a few minutes. If the patient applies the fentanyl to the skin, it takes several hours for the effect to begin. The breakdown of fentanyl takes place in the liver, where it is metabolized into ineffective breakdown products. Out of the body, the opioid passes through the kidneys. After about 7 hours, about 50 percent of the painkiller is excreted from the body. When retard tablets are taken, this process takes longer.

Medical use and application

Fentanyl is administered to treat severe to very intense pain. In most cases, the patient is given a special patch. This delivers the drug evenly over the course of several days. This treatment method is primarily used for the treatment of cancer and is suitable for the control of continuous pain. However, pain patches are not suitable for acute pain or wound pain after operations. In such cases, injection solutions are administered by syringe. Fentanyl is also used to induce anesthesia, in combination with a sleeping pill. For acute pain, lozenges or nasal sprays are also administered, since a rapid onset of action is also possible with these preparations. As a rule, the opioid is only taken for a short time in acute cases. The individual dose is determined by the physician. If chronic pain has to be treated with a fentanyl patch, the medical staff cleans the selected skin area, which should be unharmed and hairless, with water. After drying, the patch is lightly pressed on for about 30 seconds and remains on the skin for three days until it is replaced by another patch elsewhere.The treated area needs at least a week off before a fentanyl patch can be applied there again.

Risks and side effects

There is a risk of a variety of unwanted side effects from taking fentanyl. These primarily include restlessness, drowsiness, headache, dizziness, skin rash, itching, sweating, constipation, nausea, vomiting, changes in mood, dry mouth, a slowing of the heartbeat, disturbances in bladder emptying, diarrhea, flushing of the skin, digestive problems, confusion, anxiety, nervousness, depression, and hallucinations. Occasionally, tremors, sensitivity problems, memory problems, low blood pressure, sleep problems, breathing problems, heart palpitations, high blood pressure, or speech disorders are also possible. In addition, there is a risk that the patient may become dependent on fentanyl. If hypersensitivity to fentanyl or dependence on opioid painkillers is present, the active substance must not be administered. The same applies if there is severe impairment of brain function. Careful consideration of the risks and benefits of fentanyl treatment is required if the patient suffers from cardiac arrhythmias with slowed heartbeat, increased intracranial pressure, impaired consciousness, COPD or other diseases of the lungs, as well as limitations of kidney and liver function. Under no circumstances should fentanyl be administered during pregnancy. In this way, the child is already at risk of becoming dependent in the womb. This becomes noticeable through withdrawal symptoms after birth. In addition, fentanyl can restrict the child’s respiratory functions. Because the drug passes into breast milk, it should also not be used during breastfeeding. In principle, however, fentanyl is suitable for treating children.