Fentanyl

Fentanyl is a narcotic-type painkiller.

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Indications Fentanyl

It is used in the following situations:

• pain relief for a short period of time - as anesthesia during induction or premedication, and also as a maintenance measure in the period after a surgical procedure;
• to provide a strong analgesic effect, in addition to local or general anesthesia;
• in combination with neuroleptics (for example, with droperidol) during premedication, and also as an adjuvant drug during local or general anesthesia;
• as an anesthetic in people with an increased risk of complications during major surgeries (for example, in the heart area).

In addition, Fentanyl can be used during orthopedic or neurological procedures - it is prescribed as an adjuvant analgesic.

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Release form

It is released in the form of an injection liquid (in a 50 ml bottle), as well as in the form of a transdermal treatment system - 5 special packets inside a box.

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Pharmacodynamics

The drug has a sedative and analgesic effect. During use, it is necessary to remember that changes in the ventilation of the pulmonary alveoli and respiratory rate may be longer lasting than the analgesic effect.

When the dose is increased, pulmonary exchange is weakened. When too large doses are used, apnea may develop.

Fentanyl has a less pronounced emetic effect than substances such as meperidine or morphine.

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Pharmacokinetics

The distribution period of the substance is 1.7 minutes, and the redistribution period is 13 minutes. The half-life of the drug is 219 minutes.

The distribution volume of the drug is 4 l/kg. The ability of plasma protein to synthesize decreases as the ionization of the drug increases. Changes in pH values can affect the distribution processes of the drug between the CNS and plasma.

The active component accumulates inside the skeletal muscles and fatty tissues, and then is released at a low speed, penetrating into the blood. The drug is converted inside the liver at a high frequency.

Approximately 75% of the intravenously administered dose is excreted in the urine (mostly as breakdown products). Less than 10% of the unchanged element is excreted in the urine. Approximately 9% of the drug dose is excreted (as breakdown products) in the feces.

The active effect of Fentanyl begins to manifest itself almost immediately after intravenous injection. However, the maximum intensity of pain relief lasts no more than a few minutes. On average, the analgesic effect lasts about 0.5-1 hour (with intravenous injection of a dosage of up to 2 ml of solution (100 mcg)). With an intramuscular injection, the drug begins to act 7-8 minutes after the procedure, and the total duration of the medicinal effect is about 2 hours.

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Dosing and administration

The drug may only be prescribed by physicians who have knowledge and experience in handling powerful opioid drugs when used to treat chronic pain.

Since there is a possibility of respiratory depression, the drug is prescribed only to those individuals who have good tolerance of such drugs. During the use of Fentanyl, it is necessary to reduce the use of other anesthetics to a minimum.

People who have previously taken at least 60 mg of morphine, 30 mg of oxycodone, 8 mg of hydromorphone, or other opioid drugs daily for 7 days or longer are considered to be resistant to the effects of opioids.

The selection of doses for each patient is carried out individually, taking into account the existing history of analgesic use during therapy, as well as risk factors for the development of drug addiction in a person.

After prescribing any dose of the drug, the physician should carefully monitor the patient's reaction, for example, suppression of respiratory activity, especially during the first 24-72 hours from the start of the course, when the drug reaches its maximum in the serum.

Dosage portion sizes.

When preparing an adult for a surgical procedure, 0.05-0.1 mg of the drug is administered intravenously (in combination with droperidol (2.5-5 mg)). This should be done approximately 15 minutes before the administration of anesthesia. As a surgical anesthesia: 0.05-0.2 mg of the substance is administered intravenously every 30 minutes.

In case of preparation of a child for a surgical procedure, 0.002 mg/kg of the drug should be administered. For surgical anesthesia, an intravenous dosage of 0.01-0.15 mg/kg or an intramuscular injection of 0.15-0.25 mg/kg is required. To maintain surgical anesthesia, an intramuscular injection of 0.001-0.002 mg/kg of the drug is required.

The patch must be applied to the epidermis (flat area) for 72 hours. An important condition for the procedure is a minimum amount of hair in the treatment area, as well as the absence of noticeable signs of allergic irritation.

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Use Fentanyl during pregnancy

Fentanyl should not be used during lactation or pregnancy.

Contraindications

Main contraindications:

• the presence of intolerance to opioid drugs;
• bronchial asthma;
• drug addiction;
• conditions in which suppression of the respiratory center function is observed;
• performing obstetric procedures;
• respiratory failure;
• there is a suspicion of intestinal obstruction.

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Side effects Fentanyl

The medication can cause a variety of negative effects:

• in case of excessive or prolonged use of drugs, drug addiction may develop;
• severe forms of respiratory disorders;
• decrease in blood pressure values;
• bradycardia;
• short-term muscle rigidity;
• moderate bronchoconstriction.

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Overdose

In acute poisoning, a feeling of drowsiness, suppression of respiratory activity, muscle spasm, comatose state or stupor, decreased blood pressure and bradycardia are observed.

Rarely, an overdose of the drug can cause death of the patient.

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Interactions with other drugs

Combination with antidepressants.

Combination with other drugs that affect the central nervous system (including tranquilizers, hypnotics or sedatives, opioids and general anesthetics) may increase the likelihood of respiratory system dysfunction, development of deep sedation and coma, and even death. When used simultaneously with any of the above drugs, the dosage of one of them should be reduced.

Medicines that inhibit CYP3A4 activity.

Because CYP3A4 is an important part of drug metabolism, drugs that inhibit its activity may decrease Fentanyl clearance values, resulting in increased plasma levels and prolonged opioid effects. These effects may be more pronounced when combined with 3A4 inhibitors.

Substances that induce CYP3A4 function.

Elements that induce CYP450 3A4 are capable of causing the process of drug metabolism, due to which its clearance increases, and the level in plasma, on the contrary, decreases. As a result, there is a lack of medicinal effectiveness or the possible occurrence of withdrawal syndrome in people who subsequently acquire drug addiction.

Combination with MAOIs.

The combination of the drug with MAOIs has not yet been sufficiently studied, which is why the simultaneous use of these substances is completely prohibited.

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Storage conditions

Fentanyl should be stored in a dry, dark place, out of the reach of small children. The temperature should not exceed 25°C.

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Shelf life

Fentanyl can be used within 24 months from the date of manufacture of the drug.

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Application for children

It is prohibited to prescribe the medicine to children under 2 years of age.

Analogues

Analogues of the drug are Lunaldin with Dolforin, Fentadol with Durogesic Matrix, and Fendivia.

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Reviews

Fentanyl receives quite different reviews regarding the nature of its medicinal effect. Often, patients who have used it are unable to adequately assess its effectiveness, which is due to the severity of the pathologies for which the drug is prescribed.

But most experts consider the drug to be quite effective, because it very effectively eliminates severe pain during treatment, as well as after surgical procedures.