Fentanyl: consequences of use, side effects

Pharmacological action of Fentanyl

Fentanyl is a synthetic analgesic that has rapid, short-term sedative and analgesic effects.

The analgesic effect of Fentanyl is stronger than that of Morphine.

The pharmaceutical agent has a depressant effect on the respiratory and vasomotor centers. The drug stimulates the center of the vagus nerve and the vomiting center, helps to increase the tone of the sphincters of the gallbladder and bladder.

In addition, the medicine helps reduce:

Blood pressure
Renal blood flow
Intestinal peristalsis

Fentanyl causes euphoria and makes it easier to fall asleep.

The speed of development of physical and mental dependence and tolerance directly depends on the individual characteristics of the human body.

Unlike other opioid painkillers, the medication very rarely causes histamine reactions. The instructions note that with intravenous administration, pain relief occurs after 3 minutes, with intramuscular administration - after 30 minutes. The analgesic effect of the drug with IV is 1 hour, with IM - 2 hours, the use of a transdermal therapeutic system allows you to increase the analgesic effect to 3 days.

The effect of fentanyl

The following types of effects of fentanyl on the body can be distinguished:

sedative effect;
feeling of euphoria;
slow heart rate;
depression of the respiratory center;
pronounced analgesic, etc.

How to recognize a fentanyl addict?
This drug is most often used intravenously, as evidenced by needle marks on the skin. The following symptoms also indicate the use of this substance:

constricted pupils that do not respond to light;
slow breathing;
causeless fun, constantly high spirits;
speech disorders;
drowsiness, causeless fatigue;
lethargy, apathy;
decreased or complete lack of appetite.

Symptoms of using this drug depend on the stage of drug intoxication. For several hours after taking this drug, a person is in high spirits, enjoys every little thing, and laughs for no reason. After a few hours, when fentanyl stops working, the euphoria gives way to depression, depressed mood and apathy. It is not uncommon for drug addicts to develop psychosis after taking this drug. Call 8 (495) 150-85-96

Instructions for use

According to the instructions, Fentanyl for the relief of chronic pain should be prescribed exclusively by medical personnel who are aware of the rules of potent opioids.

When using the medication, respiratory depression may occur, so the drug is prescribed only to those who tolerate this type of pharmaceutical well. When using Fentanyl, it is important to minimize the use of other anesthetics.

The dosage of the drug is selected by the doctor individually for each patient. When prescribing medication, the doctor takes into account the previous history of taking painkillers and risk factors for drug addiction.

After starting treatment for 3 days, the doctor should carefully monitor the patient’s condition to avoid missing the occurrence of respiratory depression.

Pharmacological properties of the drug Fentanyl

fentanyl is a phenylpiperidine derivative (partially similar to trimeperidine), belongs to the group of narcotic analgesics. It has a strong (short-term when administered once) analgesic effect. Its analgesic activity is almost 100 times greater than that of morphine. The mechanism of action is due to inhibition of the thalamic centers of pain sensitivity and blocking the transmission of pain impulses to the cerebral cortex. Stimulates the vomiting center and the nucleus of the vagus nerve. When administered in high doses, it can cause short-term, mild respiratory depression. After intravenous administration of fentanyl, the maximum effect is observed after 1–3 minutes and lasts 15–30 minutes. After intramuscular administration, the maximum analgesic effect develops within 3–10 minutes.

Dosing

Before surgery, 15 minutes before anesthesia, an adult is administered intravenously 0.05-0.1 mg of the drug in combination with Droperidol (2.5-5 mg). Every 30 minutes, for surgical anesthesia, the patient is administered intravenously 0.05-0.2 mg of the substance.

Before surgery, children are administered 0.002 mg per kg of body weight. For anesthesia, a small patient is administered intramuscularly with 0.15-0.25 mg/kg or intravenously with 0.01-0.15 mg/kg.

The patch is applied to the surface of the skin with a minimum amount of hair and without irritation for 3 days. Fentanyl in the form of TTC is most often applied to the forearm, chest, and back. For children and patients with cognitive disorders, it is best to stick the patch on the back, its upper part, this will protect against improper removal. The skin where you plan to stick the medicine must first be washed with warm water; there is no need to add detergents.

Fentanyl in the form of TTC must be used immediately after removing it from the package. The pharmaceutical product should not be used if there are any irregularities on the packaging. The patch is changed every 3 days, the next one is always applied to a new area of skin.

Side effects

Fentanyl use can lead to a number of side effects:

Fentanyl

Patients experiencing severe side effects should be closely monitored for at least 24 hours (depending on symptoms) after removal of Fentanyl TTC, as fentanyl plasma concentrations decrease gradually and a 50% reduction is achieved within approximately 17 (13- 22) hours.

Fentanyl TTC should be kept out of the reach of children both before and after use.

Fentanyl TTC cannot be cut.

Application

in
opioid-naïve patients who are not opioid-tolerant
When using Fentanyl TTC in opioid-naïve patients, significant respiratory depression and/or death have been reported very rarely when used as initial opioid therapy. The potential for severe or life-threatening hypoventilation exists even when a minimal dose of Fentanyl TTC is used as initial opioid therapy in opioid-naïve patients. It is recommended to prescribe Fentanyl TTC to patients demonstrating opioid tolerance.

Respiratory depression

As with other narcotic analgesics, significant respiratory depression may occur in some patients when using Fentanyl TTC. Patients should be carefully monitored for such effects. Respiratory depression may continue after removal of the TTS. The degree of respiratory depression increases with increasing dose of Fentanyl TTC. Medicines that affect the central nervous system may increase respiratory depression.

Chronic lung diseases

Fentanyl can cause a number of severe side effects in patients with chronic obstructive pulmonary disease and other pulmonary diseases. In these patients, opioids may decrease respiratory excitability and increase respiratory resistance.

Increased intracranial pressure

Fentanyl TTC should be used with caution in patients who may be particularly sensitive to elevated CO2 levels. Such patients are those who have experienced increased intracranial pressure, impaired consciousness, or coma. Fentanyl TTC should be used with caution in patients with brain tumors.

Diseases of the cardiovascular system

Fentanyl may cause bradycardia and should therefore be used with caution in patients with bradyarrhythmias. Fentanyl TTS should be used with caution in patients with arterial hypotension.

Liver failure

Because fentanyl is metabolized to inactive metabolites in the liver, impaired liver function may result in delayed elimination of the drug. Patients with hepatic impairment taking Fentanyl TTC should be closely monitored for symptoms of possible fentanyl toxicity, and the dose of Fentanyl TTC should be reduced if necessary. Opioid analgesics can increase the tone of the smooth muscles of the gastrointestinal tract and biliary tract.

Fentanyl TTC should be used with caution in patients with a history of hepatic colic.

Kidney failure

Less than 10% of fentanyl is excreted unchanged by the kidneys, and fentanyl has no known active metabolites that are excreted by the kidneys. Patients with renal impairment taking Fentanyl TTC should be closely monitored for symptoms of possible fentanyl toxicity and the dose of Fentanyl TTC should be reduced if necessary.

Serotonin syndrome

Caution should be exercised when co-administering Fentanyl TTC with drugs that affect the serotonergic neurotransmitter system. Concomitant use with serotonergic drugs such as selective serotonin reuptake inhibitors (SSRIs) and serotonin norepinephrine reuptake inhibitors (SNRIs), as well as drugs that reduce serotonin metabolism (including MAO inhibitors), may lead to the development of potentially life-threatening serotonin syndrome. This syndrome may occur when taking recommended doses.

Serotonin syndrome may include psychiatric disorders (agitation, hallucinations, coma), autonomic disorders (tachycardia, blood pressure fluctuations, hyperthermia), neuromuscular disorders (hyperreflexia, incoordination, rigidity) and/or gastrointestinal disorders (nausea, vomiting, diarrhea) .

If the development of serotonin syndrome is suspected, therapy with Fentanyl TTC should be discontinued.

Interaction with inhibitors of cytochrome
CYP3A4 When CYP3A4 ,
an increase in the concentration of fentanyl in plasma is possible. The consequence of this is an increase or prolongation of both the therapeutic effect and possible side effects (respiratory depression). In these cases, the patient should be under constant medical supervision.

Therefore, the concomitant use of transdermal forms of fentanyl with inhibitors of cytochrome CYP3A4 is not recommended, unless patients are under medical supervision. If symptoms of depressed breathing occur, the dose of the drug should be reduced.

Accidental exposure to TTC

Accidental skin exposure (especially in children) to Fentanyl TTC through close physical contact with a patient using TTC may result in opioid overdose. Patients should be warned that in case of accidental exposure to the skin of a person not taking the drug, TTS should be removed immediately. For symptoms of overdose, see section "Overdose".

Use in elderly patients

Data from studies of intravenous fentanyl suggest that elderly patients will have decreased clearance and prolonged half-life and may be more sensitive to fentanyl than younger patients. Elderly patients taking Fentanyl TTC should be closely monitored for symptoms of possible fentanyl overdose and, if necessary, the dose of Fentanyl TTC should be reduced.

Effect on the gastrointestinal tract

Opioids increase the tone and reduce propulsive contractions of the smooth muscles of the gastrointestinal tract. As a result, gastrointestinal transit time increases, which can cause constipation. Patients should be informed about measures to prevent constipation and the prophylactic use of laxatives. Additional precautions should be taken in patients suffering from chronic constipation. If paralytic ileus is present or suspected, treatment with Fentanyl TTC should be discontinued.

Application

in
depleted and debilitated patients
Since clearance may be reduced in depleted and debilitated patients and the half-life of the drug may be prolonged, depleted and debilitated patients should be under constant medical supervision to identify symptoms of a possible overdose, in which case the dose of Fentanyl TTC should be reduced.

Drug dependence and potential for abuse

With repeated administration of opioids, tolerance and physical and psychological dependence can develop. Iatrogenic dependence with opioid use is rare.

As with other opioid agonists, there is a potential for abuse of fentanyl. Abuse or intentional misuse of Fentanyl TTC can lead to overdose and/or death. Patients at increased risk for opioid abuse may still receive adequate treatment with modified-release narcotic analgesics but should be closely monitored for possible signs of off-label use, abuse, or dependence.

Fever / external heat sources

A pharmacokinetic model suggests that serum fentanyl concentrations may increase by approximately one-third if body temperature rises to 40°C. Therefore, patients with fever should be closely monitored for opioid-specific side effects and subsequent dose adjustments if necessary. There has been an increase in the release of fentanyl from TTS with increasing temperature, which can result in overdose and death of the patient. A study on healthy volunteers showed that when heated with fentanyl TTC, there was an increase in mean AUC values by 120% and Cmax by 61%. All patients should avoid direct exposure of the Fentanyl TTC application site to external heat sources, such as heat lamps, tanning lamps, intense sunbathing, heating pads, saunas, solariums, hot water baths, etc.

Discontinuation of the drug

If it is necessary to discontinue the use of Fentanyl TTC, replacing this drug with other opioids should be done gradually, starting with low doses. This drug change regimen is necessary because fentanyl concentrations gradually decrease after TTC removal, with a 50% reduction in serum fentanyl concentrations taking 17 hours. Withdrawal of opioid analgesia should always be gradual to prevent the development of a withdrawal syndrome.

Instructions for disposal of Fentanyl TTS

Unused TTS must be returned to the attending physician for disposal. Used TTS should be folded in half with the sticky side inward and disposed of independently.

Use in drug addicts

Enterprising drug addicts inject drugs intravenously to obtain a narcotic effect. The drug, like heroin, can be snorted or inhaled through the nose.

Fentanyl use is highly addictive. To get a “high”, a small dose is enough, but due to the short duration of action, it is not particularly used in its pure form. Dealers most often use the drug in the manufacture of other drugs or simply mix it with heroin. Unfortunately, without laboratory tests it is impossible to understand what is added to the drug.

Consequences of use

Using a serious pharmaceutical for non-medical purposes has a negative impact on physical and psychological health. Dependence on an analgesic forms quickly, sometimes 5-7 doses are enough. The lethal dose of Fentanyl is 2 mg.

Side effects:

Hallucinations
Nausea, vomiting
Problems with urination
Pulmonary edema
Decreased blood pressure
Amnesia
Sudden cardinal death

Fentanyl is a narcotic drug that is indispensable for patients with severe pathologies, but it is often used for recreational purposes.

If drug addiction occurs, it is important to seek medical help as soon as possible.

Fentanyl - what is it?

Fentanyl is an opioid analgesic used in anesthesiology.
Long-term use of fentanyl solution or tablets is fraught with the development of drug addiction. Today, the drug fentanyl, as well as its various derivatives, are among the most powerful synthetic drugs. The drug fentanyl comes in the form of a white crystalline powder or liquid solution for injection. It was first received by Paul Janssen in 1959. Soon after this, the drug began to be used in medicine as a highly effective pain reliever, replacing some non-narcotic analgesics. In the 90s of the last century, a patch made on the basis of this substance appeared on the market. It was intended to relieve point pain following injuries. Soon, doctors noticed that those patients who were administered fentanyl began to develop dependence on it and experienced withdrawal symptoms. Therefore, restrictions were placed on the distribution of this substance. Some countries have completely banned its use.

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