Fentanyl maximum dose. Fentanyl patch: instructions for use of TTC, reviews. Instructions for use and method of use

To eliminate persistent pain and during certain surgical interventions, the use of Fentanyl is justified. This medicine belongs to the group of synthetic opioid narcotic analgesics, therefore it can have a narcotic effect and cause addiction. The use of the drug can be dangerous, so it is used only as prescribed by a doctor in dosages not exceeding the values specified in the instructions.

INN and tradename drug - Fentanyl. Name of the medicine on Latin- Fentanyl.

ATX

IN international classification ATC this medicine has code N01AH01.

Release forms and composition

The medicine is released in 2 dosage forms- patch (transdermal therapeutic system) and solution for intravenous and intramuscular administration. The main active ingredient of Fentanyl is the compound of the same name.

The solution for injection also includes monohydrate, lemon acid and prepared water. The patches include an adhesive layer, a backing layer and a protective film. Fentanyl solution 0.005% is available in ampoules of 2 and 10 ml. The cardboard package contains 5 or 10 ampoules. The patches are available with a contact area from 4.2 cm² to 33.6 cm². They are presented in cardboard packaging of 5 pieces.

pharmachologic effect

The analgesic activity of fentanyl at a dose of 0.1 mg is equivalent to the effect of 10 mg of morphine. The active substance of this drug affects the opioid receptors of the central nervous system and peripheral nerve fibers. The medication quickly increases pain threshold, because it suppresses the spread of impulses signaling pain along nerve fibers to the cells of the central nervous system responsible for their analysis.

This opioid medication changes the perception of pain. The medicine is mild hypnotic effect. The drug not only has a pronounced analgesic and sedative effect, it can cause a feeling of euphoria, so the development of physical and mental dependence is possible. In addition, with repeated use of the product, tolerance to the active substance Fentanyl may occur.

Pharmacokinetics

The active substance of the drug is fat-soluble. The distribution of the drug after administration is uneven, and first traces of it are found in the kidneys, liver and other organs with an active blood supply. Subsequently, it saturates other body tissues. The highest concentration of the drug in the blood is observed already 3 minutes after injection into a vein, and when injected into a muscle it reaches highest point after half an hour.

The high level of drug concentration in the blood persists for approximately 2 hours. During this period, a pronounced analgesic effect is observed. Metabolism active substance occurs in the liver. The drug is excreted primarily in the urine. Up to 10% of the dose is excreted unchanged. After a single use, the drug is completely eliminated from the body within 6-12 hours. When using the patch active substance delivered to the tissues of the central nervous system and peripheral nerves for at least 72 hours.

This method of administering the drug allows you to maintain its concentration in the blood at the same level for a long time.

Indications for use

Most frequent indication to the use of Fentanyl - neuroleptanalgesia. This is the method intravenous anesthesia, in which the patient is conscious, but does not feel pain or feel emotions. A similar method of pain relief is used for a wide range of diagnostic and surgical interventions, incl. on organs abdominal cavity.

Plasters are often used to administer local anesthesia. The medication can be used for anesthesia for people taking antipsychotics and tranquilizers, incl. Droperidol and Xanax. In addition, when a patient is put under anesthesia, a combination of Fentanyl and Propofol is possible.

The use of Fentanyl is often indicated to eliminate persistent cancer pain in adults and children. For inoperable tumors that cannot be eliminated by radiation and chemotherapy, the drug can be used in the form of a patch. In addition, it is possible to use the medication to eliminate intense pain during myocardial infarction. The use of Fentanyl is justified to eliminate chronic pain syndrome in various pathologies, if it is impossible to achieve positive effect through the use of others medicines.

Contraindications

The use of Fentanyl is unacceptable for the treatment of people suffering from bronchial asthma and severe respiratory diseases. Do not use the product if patients have a tendency to allergic reactions and hypersensitivity to individual components of the drug. The use of Fentanyl as anesthesia during obstetric operations is not recommended.

How to take Fentanyl?

Approximately 15 minutes before the patient is put under anesthesia before surgery, IV medication is administered in a dosage of 0.05 to 0.1 mg per kg of body weight. During surgical intervention intravenous administration is carried out at a dose of 0.05 to 0.2 mg per kg of body weight every 30 minutes. For pathologies accompanied by intense pain, Fentanyl patches are used, which are attached to the skin for 72 hours.

For diabetes

When administering anesthesia to patients suffering from diabetes mellitus, during anesthesia, the use of Fentanyl in combination with Propofol and Diazepam is indicated. The dose is selected individually.

Side effects

Often, when using the drug, rhythm disturbances and a decrease in blood pressure. In rare cases, due to the action this tool cardiac arrest occurs. Possible side effects and from other organs and systems.

Gastrointestinal tract

After using the medicine, there is a high probability of developing biliary colic. In addition, stool disturbances, nausea and vomiting are often observed.

Blood-forming organs

Bone marrow depression occurs extremely rarely.

central nervous system

When using Fentanyl, an increase in intracranial pressure and frequent headaches. Among other things, side effects may include drowsiness, euphoria, and visual disturbances.

From the urinary system

Rarely in patients treated with Fentanyl, there is acute delay urine.

From the respiratory system

The medication has a depressant effect on the respiratory center in the brain, so breathing may stop.

Allergies

Both when using the solution and when using patches, the appearance of skin rash and itching. In rare cases, laryngospasm and Quincke's edema occur.

special instructions

The use of Fentanyl patches requires complete refusal from sunbathing procedures. You should also avoid visiting saunas and steam baths. Cannot be used this drug for anesthesia in the absence of conditions for artificial ventilation.

Alcohol compatibility

During Fentanyl therapy, you should avoid drinking alcohol.

Impact on the ability to operate machinery

You should avoid driving a car while undergoing treatment with Fentanyl.

Use during pregnancy and lactation

Treatment with Fentanyl is unacceptable during pregnancy, since the risk to the fetus is extremely high due to increased likelihood development of severe pathologies. If a woman took this medication while pregnant, the newborn may experience severe symptoms withdrawal syndrome. If you need to use the medication after childbirth, you should stop breastfeeding your baby.

Prescription of Fentanyl for children

At surgical treatment For children, the medication is used in a dosage of 0.002 mg/kg. During surgical intervention Intravenous administration of the drug may be prescribed at a dose of 0.1 to 0.15 mg per kg. Intramuscular administration is possible in a dose of 0.15 to 0.25 mg.

Use in old age

Overdose

If you use too much of the drug, breathing problems may occur. In addition, some patients experienced hypotension and severe muscle spasms following an overdose of this opiate. IN severe cases Stupor, convulsions and coma may develop.

Interaction with other drugs

Using Fentanyl with other anti-anxiety medications hypnotic effect, as well as with opioids, increases the risk of side effects. If a patient uses CYP3A4 inhibitors while using Fentanyl, the concentration of the latter in the blood will be increased, which will increase the duration of the effect. Simultaneous administration of a CYP3A4 inducer leads to a decrease in the effectiveness of the opiate.

Analogs

Medicines that have similar effects to Fentanyl include:

Durogesic.
Fentadol.
Fendivia.
Dolforin.
Lunaldin.

Conditions for dispensing from a pharmacy

The medication is dispensed in pharmacies with a doctor's prescription.

Can I buy it without a prescription?

When purchasing a product from unofficial sellers, there is a high probability of purchasing a counterfeit or expired drug.

Fentanyl price

In Russia, the price of Fentanyl solution ranges from 125 to 870 rubles. The cost of the patch ranges from 1800 to 4700 rubles.

Storage conditions of the drug

The optimal storage temperature for the medication is 25°C.

Best before date

The drug can be stored for no more than 4 years.

Fentanyl is a narcotic medicinal product analgesic effect; stimulates opiate receptors.

Release form and composition

Fentanyl is available in the form of a solution for intravenous and intramuscular administration, which is a colorless clear liquid(1 ml and 2 ml in ampoules, 5 ampoules in blister packs, 1 or 2 packs in a cardboard box, complete with or without an ampoule knife/scarifier, if the ampoules have rings or break points).

Composition of 1 ml solution:

active ingredient: fentanyl – 50 mcg;
auxiliary components: citric acid, water for injection.

Pharmacological properties

Pharmacodynamics

Fentanyl is an opioid analgesic short acting. It activates the analgesic (antinociceptive) system, disrupting the interneuronal transmission of pain impulses and changing the emotional coloring of pain.

According to their own pharmacological properties fentanyl is very close to morphine: it inhibits the activity of the respiratory center, increases the pain threshold for various painful stimuli, has a depressant effect on the central nervous system and inhibits conditioned reflexes. Fentanyl differs from morphine in its higher activity (the analgesic effect of fentanyl is 100 times greater than that of morphine), the ability to more strongly depress the respiratory center and the shorter duration of the therapeutic effect.

The analgesic effect of the drug develops quite quickly. With intravenous administration of Fentanyl maximum effect develops 1–3 minutes after injection and persists for 15–20 minutes; at intramuscular injection– after 3–10 minutes and persists for 1–2 hours.

Pharmacokinetics

For average analgesia, the plasma concentration of the drug should be 15–20 ng/ml. Fentanyl is 79–87% bound to plasma proteins. Its clearance is 400–500 ml/min, its volume of distribution is 60–80 liters, and its half-life is 10–30 minutes. The drug is quickly redistributed from the brain and blood to adipose tissue and muscles.

Metabolism occurs in the liver (by hydroxylation and N-dealkylation), adrenal glands, kidneys and intestines. Fentanyl is excreted by the kidneys in the form of metabolites (75%) and unchanged (10%). About 9% of the drug is excreted as metabolites in bile.

Fentanyl is able to penetrate into breast milk.

Indications for use

pain syndrome of various origins of medium and severe intensity (myocardial infarction, angina pectoris, pain in cancer patients, postoperative pain);
pain syndrome caused by spasm of smooth muscles internal organs(if the diagnosis is established); Fentanyl is used in combination with antispasmodics and atropine-like drugs;
premedication before surgical interventions;
postoperative anesthesia;
additional pain relief surgical operations under local anesthesia;
neuroleptanalgesia (combined intravenous general anesthesia simultaneously with droperidol).

Contraindications

Absolute:

arterial hypotension;
intracranial hypertension;
bradyarrhythmia;
severe hypertension of the pulmonary circulation;
severe depression of the respiratory center;
respiratory failure ( bronchial asthma, pneumonia, tendency to bronchospasm, collapse of a lung lobe or pulmonary infarction);
renal and/or liver failure;
brain tumors;
extrapyramidal disorders;
disturbances of consciousness;
obstetric operations, including surgery caesarean section before the stage of fetal extraction (due to the threat of respiratory depression of the newborn);
surgical diseases of the abdominal organs in acute stage(until an accurate diagnosis is established);
children under one year of age;
hypersensitivity to the drug.

Relative (Fentanyl is used with caution):

renal and/or hepatic colic;
hypothyroidism;
urethral strictures;
prostatic hypertrophy;
hyperthermia;
suicidal tendencies;
history of addiction to opioids;
traumatic brain injuries;
simultaneous use of glucocorticosteroids, monoamine oxidase inhibitors, insulin and antihypertensive drugs;
weakened patients;
elderly age;
period of pregnancy and lactation.

Directions for use and dosage

Fentanyl solution is intended for intravenous or intramuscular administration.

At acute pain the drug is administered in a dose of 25–100 mcg intravenously or intramuscularly (as a single agent or simultaneously with antipsychotics).

For premedication, Fentanyl is administered intramuscularly at a dose of 50–100 mcg 30 minutes before the start of surgery.

For the purpose of induction of anesthesia, the drug is administered intravenously at 100–200 mcg. Then, every 10–30 minutes, an additional 50–150 mcg is administered to maintain the required level of analgesia (in combination with droperidol).

When carrying out neuroleptanalgesia with preservation of spontaneous breathing (for example, during extracavitary and short-term operations), when muscle relaxants are not used, Fentanyl is administered after the antipsychotic at a dose of 50 mcg per 10–20 kg of body weight. In this case, spontaneous breathing should be monitored and readiness for emergency intubation and artificial ventilation should be maintained. Higher doses of Fentanyl (50–100 mcg/kg) are used exclusively during open-heart surgery.

For additional pain relief during operations under local anesthesia the drug is administered intravenously or intramuscularly at a dose of 25–50 mcg (often in combination with antipsychotics). If necessary, Fentanyl injections are repeated every 20–30 minutes.

For children, the drug is prescribed in the following doses:

preparation for surgical operations: 2 mcg/kg;
general surgical anesthesia: 150–250 mcg/kg intramuscularly or 10–150 mcg/kg intravenously;
maintaining common surgical anesthesia: 2 mcg/kg intramuscularly or 1–2 mcg/kg intravenously.

Side effects

digestive system: vomiting, nausea, hepatic colic (in patients with a history of colic), spasm of the sphincter of Oddi, constipation, flatulence;
respiratory system: laryngospasm, bronchospasm; in large doses – respiratory depression (up to respiratory arrest);
nervous system and sensory organs: convulsions, headache, increased intracranial pressure, paradoxical excitation or depression of the central nervous system, diplopia, blurred vision;
other reactions: decreased blood pressure, bradycardia (sometimes to cardiac arrest), short-term muscle rigidity, urinary retention, increased sweating, allergic reactions, tolerance, drug dependence, withdrawal syndrome.

Overdose

In case of an overdose of Fentanyl, following symptoms: apnea, depression of the respiratory center, bradycardia, decreased frequency breathing movements, muscle stiffness, low blood pressure.

Treatment of overdose consists of stopping the drug and maintaining adequate ventilation. Naloxone (a specific opioid antagonist) is administered intravenously at a dose of 0.4–2 mg; if there is no effect, then after 2-3 minutes the administration of naloxone should be repeated. It is also possible to use nalorphine at a dose of 5-10 mg intravenously or intramuscularly every 15 minutes until a total dose of 40 mg is reached. When administering nalorphine or naloxone to patients addicted to fentanyl or morphine, they may develop withdrawal symptoms; in these cases, the dose of antagonists is increased gradually.

As a supporting and symptomatic therapy muscle relaxants are prescribed, and for bradycardia - a 1% atropine solution in a dose of 0.5–1 ml.

special instructions

Fentanyl can only be used in specialized inpatient conditions. The drug should be administered by highly qualified specialists.

It is necessary to establish careful monitoring of the patient in the postoperative period.

In patients with reduced weight, long-term surgical operations or frequent repeated use of the drug, the duration of its action may increase.

For renal, hepatic and gastric colic, Fentanyl is used simultaneously with antispasmodic and atropine-like drugs, and the patient must be closely monitored.

Impact on the ability to drive vehicles and complex mechanisms

Use during pregnancy and lactation

During pregnancy, Fentanyl is used only in cases where the expected benefit to the mother exceeds potential risk for the fetus and newborn.

The drug passes into breast milk, so while using Fentanyl breast-feeding should be stopped.

Women reproductive age During the period of use of the drug, contraceptives should be selected with particular care.

Drug interactions

When using Fentanyl simultaneously with antihistamines, which have a sedative effect, and ethanol increase the risk of side effects.

Benzodiazepines prolong the patient's recovery from neuroleptanalgesia; Beta blockers may reduce the frequency and severity of hypertensive reactions when fentanyl is used in cardiac surgery, but increase the likelihood of bradycardia.

When used simultaneously with monoamine oxidase inhibitors, the risk increases severe complications; With antihypertensive drugs– the effect of the latter is enhanced.

At joint use with muscle relaxants, muscle stiffness is prevented or eliminated; muscle relaxants with vagolytic activity reduce the risk of hypotension and bradycardia, and may increase the risk of hypertension and tachycardia; muscle relaxants that do not have vagolytic activity do not reduce the risk of hypotension and bradycardia, and increase the likelihood of severe adverse reactions from the outside of cardio-vascular system.

Fentanyl should be used with caution against the background of the effects of hypnotics, antipsychotics and drugs for general anesthesia to avoid suppression of the activity of the respiratory center, and excessive depression of the central nervous system. Dinitrogen oxide increases muscle stiffness, and tricyclic antidepressants increase the likelihood of suppression of the respiratory center.

The drug should not be used in combination with narcotic analgesics from the group of opioid receptor agonists-antagonists (tramadol, nalbuphine and butorphanol) and partial agonists (buprenorphine), since there is a risk of weakening analgesia.

When concomitantly treated with antihypertensive drugs, glucocorticosteroids and insulin, Fentanyl should be used in reduced doses. The analgesic effect and side effects of other opioid agonists (promedol, morphine) in the therapeutic dose range are summarized with the action and effects of fentanyl.

Analogs

Analogues of Fentanyl are: Dolforin, Lunaldin, Fentadol Matrix, Fentadol Reservoir, Fendivia.

Terms and conditions of storage

Store at a temperature of no more than 25 °C in specially equipped rooms (if you have the appropriate license). Keep away from children.

Shelf life – 4 years.

Conditions for dispensing from pharmacies

The drug is intended exclusively for hospitals.

Pharmacological properties

Pharmacodynamics

Fentanyl is an opioid analgesic with high affinity for the mu-opioid receptor.

Fentanyl can be used as an analgesic component during general anesthesia or on your own. Fentanyl may reduce cardiac output by slowing down the heart rate, which is an advantage of the drug in conditions of the cardiovascular system when it is desirable to reduce the stress response. 100 mcg of fentanyl (2 ml) is approximately equivalent in analgesic activity to 10 mg of morphine. The drug exhibits its effect quickly, but the maximum analgesic effect and inhibitory effect on the respiratory center occurs only after a few minutes. The duration of the analgesic effect with a single intravenous dose of up to 100 mcg is about 30 minutes. The depth of analgesia depends on the dose of the drug and can be adjusted according to the intensity pain. Fentanyl has a high therapeutic breadth. In rats, the therapeutic index (LD 50 /ED 50) for the lowest degree of analgesia is 277, compared with 69.5 and 4.6 for morphine and pethidine, respectively.

Like other opioid analgesics, fentanyl, depending on the dose and rate of administration, can cause muscle rigidity, euphoria, miosis and bradycardia.

Histamine release assays and skin prick tests in humans, as well as in vivo tests in dogs, have shown that clinically significant histamine release is rare with fentanyl use. The specific opioid antagonist for fentanyl is naloxone.

Pharmacokinetics

Fentanyl is a lipid-soluble drug and its pharmacokinetics can be described using a three-compartment model. After intravenous administration, high concentrations fentanyl occurs rapidly in well-perfused tissues such as the lungs, kidneys, and brain. Subsequently, the drug is redistributed to other tissues. It accumulates slowly in skeletal muscle and at an even slower rate in adipose tissue, from which it is gradually released into the blood. Up to 80% of fentanyl is bound to blood plasma proteins.

Fentanyl is primarily metabolized in the liver, probably by N-dealkylation, and is excreted primarily in the urine. Less than 10% is excreted unchanged. The half-life of fentanyl is 3.7 hours.

Indications for use

Fentanyl is used for neuroleptanalgesia (in combination with droperidol), for premedication (as part of certain regimens), for induction of anesthesia, for pain relief (during short-term extracavitary operations), as additional means during operations under local anesthesia, with pain syndrome strong and moderate intensity for myocardial infarction, renal and hepatic colic.

Fentanyl is used to relieve persistent moderate to severe chronic pain that require constant, 24-hour prescription of opioids over a long period of time and cannot be treated in another way (for example, non-steroidal anti-inflammatory drugs (or in patients with a contraindication to the use of drugs of this group), a combination of opioids, or immediate-release opioid drugs).

It is not recommended to use fentanyl for the relief of postoperative pain, except when following palliative surgery. oncological diseases requires the introduction of drugs with a high antinociceptive effect.

Patients who tolerate opioid therapy are those who have been taking at least 60 mg of morphine per day, at least 30 mg of oral oxycodone per day, or at least 8 mg of hydromorphone per day for a week or more.

Directions for use and dosage regimen

Fentanyl should only be used by highly trained personnel and in conditions where mechanical ventilation is available.

The dose of the drug should be selected individually according to age, body weight, physical condition and the underlying disease of the patient, and it also depends on the type of surgery performed and anesthesia, and the use of other medications.

The initial dose should be reduced in elderly and debilitated patients. The effect of the initial dose must be taken into account when determining maintenance doses.

Fentanyl can be administered intravenously and intramuscularly. The drug can be administered intravenously to children and adults as a bolus or as an infusion.

Standard dosage regimen:

Adults and children over 12 years of age:

Doses greater than 200 mcg are used exclusively for anesthesia.

For premedication, 1-2 ml of the drug is administered intramuscularly before induction of anesthesia.

When given intravenously in patients without premedication, 2 mL of fentanyl can provide adequate analgesia for 10 to 20 minutes for low-pain surgeries. A bolus of 10 ml fentanyl can provide analgesia for about 1 hour, which is used in surgical procedures. medium intensity pain. Administration of fentanyl at a dose of 50 mcg/kg provides analgesia for 4–6 hours for operations with high pain intensity.

Fentanyl can also be given by intravenous infusion.

In mechanically ventilated patients, fentanyl may be given a loading dose of fentanyl rapidly at a rate of approximately 1 mcg/kg/min over the first 10 minutes, followed by a loading dose of approximately 0.1 mcg/kg/min. An alternative route of loading loading dose administration may be bolus administration. The infusion rate should be titrated according to the individual patient's response; it may be necessary to reduce the rate of administration. Administration should be stopped approximately 40 minutes before the end of surgery, unless it is planned to continue artificial ventilation lungs and after surgery.

If spontaneous breathing persists, more low speeds administration of fentanyl, for example, 0.05 - 0.08 mcg/kg/min. Higher rates of drug administration (up to 3 mcg/kg/min) are used for cardiac surgery.

To determine the required dose of fentanyl, it is important to correctly assess the possible degree of pain intensity, the effect of medications used for premedication, and the duration of the procedure.

Use in children. For children over 12 years of age, the dosage regimen is the same as for adults.

Standard dosage regimen for children from 2 to 12 years of age:

In children, it is used for analgesia during surgery, enhancing anesthesia while maintaining spontaneous breathing.

Analgesia in spontaneously breathing children should only be used as an adjunct to anesthetic management or as an adjunct to sedation (or as part of a sedation/analgesia technique), provided that qualified personnel and equipment are available to perform tracheal intubation and artificial respiration.

Side effect

To assess the frequency of occurrence of the following adverse reactions, the following gradations were used: very often (≥1/10), often (from ≥1/100 to<1/10), нечасто (от ≥ 1/1 000 до <1/100), редко (от ≥ 1/10 000 до < 1/1 000), очень редко (<1/10 000), неизвестно – частота не может быть оценена на основании имеющихся данных.

From the immune system: unknown – hypersensitivity (anaphylactic shock, anaphylactic reactions, urticaria).

Mental disorders: infrequently - euphoria.

From the nervous system: often – dyskinesia, sedation, dizziness; infrequently – headache; unknown – convulsions, loss of consciousness, myoclonus.

From the senses: often - impaired visual perception.

From the cardiovascular system: often – bradycardia, tachycardia, arrhythmia, hypotension, hypertension, pain along the vein; infrequently – phlebitis, fluctuations in blood pressure; unknown - cardiac arrest.

From the respiratory system: often – laryngospasm, bronchospasm, apnea; infrequently – hyperventilation, hiccups; unknown - respiratory depression.

From the gastrointestinal tract: very often - nausea, vomiting.

From the skin: often – allergic dermatitis; unknown - itching.

From the musculoskeletal system: very often – muscle rigidity (including the chest).

Others: often – postoperative confusion; uncommon – hypothermia, chills, postoperative agitation, complications of anesthesia from the respiratory tract.

When fentanyl is used together with antipsychotics, the following adverse reactions may occur: chills and/or myoclonus, anxiety, postoperative hallucinations and extrapyramidal symptoms.

Contraindications

Hypersensitivity to any component of the drug, obstetric operations (before extraction of the fetus), severe hypertension in the pulmonary circulation, depression of the respiratory center, pneumonia, atelectasis and pulmonary infarction, bronchial asthma, tendency to bronchospasm, diseases of the extrapyramidal system, intracranial hypertension, intestinal obstruction, drug dependence, alcoholism, drug addiction, pregnancy, lactation (breastfeeding must be stopped), use in patients after surgical interventions on the biliary tract, relief of short-term and mild pain.

Overdose

Symptoms: dizziness, drowsiness, nervousness, general weakness, depression of the cardiovascular system, decreased blood pressure, bradycardia, clammy sweat, miosis, muscle rigidity, depression of the respiratory center, bradypnea, apnea.

Treatment: administration of a specific antagonist - naloxone; symptomatic therapy that supports vital functions (including the administration of muscle relaxants, artificial ventilation, for bradycardia - the administration of atropine, for a pronounced decrease in blood pressure - replenishment of circulating blood volume).

Precautionary measures

Fentanyl should only be used by highly qualified personnel. Fentanyl should be prescribed only by specialists who are knowledgeable in the management of long-term opioid analgesic therapy, identification and recovery from hypoventilation, including, if necessary, treatment with opioid receptor antagonists.

Fentanyl, like other opioid analgesics, can be subject to abuse both when used in accordance with its indications for use and when the drug is obtained illicitly. This risk must be taken into account when prescribing, prescribing and dispensing a drug in cases where there are concerns about misuse, abuse and other violations.

Patients at increased risk for opioid abuse include those with a family history of addiction (including drug or alcohol addiction) or certain mental health disorders (eg, major depression). Before prescribing opioid analgesics to a patient, the clinical risk of developing opioid dependence should be assessed. All patients receiving opioids should be monitored for signs of misuse, abuse, and dependence. Patients at increased risk for opioid abuse are recommended to remain on modified-release opioid formulations; These patients require constant monitoring for signs of opioid abuse.

Concerns about abuse, dependence, and inappropriate use should not be a reason for not providing appropriate pain management.

However, all patients receiving opioid analgesics require careful monitoring for signs of dependence and abuse, as there is a risk of developing dependence even with the proper use of opioid analgesics.

Fentanyl should not be used to relieve short-term or mild pain.

Concomitant use of drugs that affect the central nervous system requires special assessment and monitoring.

The use of fentanyl can cause respiratory depression, which is dose-dependent and can be relieved by the administration of a specific antagonist, naloxone. Additional doses of naloxone may be required because respiratory depression may last longer than the duration of action of the antagonist. Respiratory depression is one of the most dangerous complications of therapy with opioid agonists, which include fentanyl. The risk of developing respiratory depression is greater in elderly and debilitated patients, usually after a large initial dose in opioid-naïve patients or when opioids are co-administered with other drugs that depress respiratory function. Opioid-induced respiratory depression is manifested by decreased respiratory stimulation and decreased respiratory rate, often resulting in abnormal breathing (deep inspiration interrupted by an atypically long pause). Carbon dioxide retention due to respiratory depression may enhance the sedative effects of opioids. In this regard, overdose of drugs with sedative properties and opioids is especially dangerous.

Profound analgesia is accompanied by severe respiratory depression, which may persist or recur in the postoperative period. For this reason, careful monitoring of patients is necessary, as well as the availability of the necessary equipment and a specific antagonist for resuscitation measures. Hyperventilation during anesthesia may alter the patient's response to CO2 concentrations and cause respiratory depression in the postoperative period.

Fentanyl should be prescribed with extreme caution in patients with obstructive pulmonary disease or cor pulmonale, as well as in patients with a significant decrease in residual lung volume, hypoxia, hypercapnia, or a history of respiratory depression. In these patients, even normal therapeutic doses of fentanyl can significantly suppress respiratory function to the point of apnea. For these patients, alternative non-opioid therapy should be considered, and opioids should be prescribed only under close medical supervision and at the lowest effective dose.

Head injuries and increased intracranial pressure

Fentanyl should not be prescribed to patients who may be particularly sensitive to the intracranial effects of elevated CO2 levels. This category of patients includes those with signs of increased intracranial pressure, impaired consciousness, or coma. Opioids may complicate the clinical assessment of patients with traumatic brain injury. Fentanyl should be administered with caution to patients with a brain tumor.

Muscle stiffness, including the pectoral muscles, may occur, which can be avoided by taking the following measures: slow intravenous administration, premedication with benzodiazepines and the use of muscle relaxants.

Myoclonic movements of a non-epileptogenic nature may occur. Bradycardia, including cardiac arrest, may occur if the patient has received an insufficient amount of anticholinergic drug or when fentanyl is used in combination with muscle relaxants that do not have vagolytic activity. Bradycardia can be treated with atropine.

With long-term use of fentanyl, tolerance and drug dependence may develop.

Opioids may cause hypotension, especially in hypovolemic patients. Necessary measures must be taken to maintain stable blood pressure.

Rapid bolus injections of opioid drugs should be avoided in patients with altered cerebral vascular elasticity: in such patients, a transient decrease in mean arterial pressure is sometimes accompanied by a transient decrease in cerebral perfusion pressure.

Patients on long-term opioid therapy or with opioid dependence may require higher doses of fentanyl.

The use of fentanyl requires caution in patients with the following conditions: uncontrolled hypothyroidism, pulmonary disease, reduced tidal volume, alcoholism, impaired liver or kidney function. Such patients also require long-term postoperative monitoring.

When using fentanyl together with antipsychotics (such as droperidol), it is necessary to take into account the difference in the duration of action of these drugs. When used simultaneously, the risk of hypotension increases. Antipsychotics may cause extrapyramidal symptoms, which can be controlled with antiparkinsonian drugs.

As with other opioids, due to its anticholinergic effects, the use of fentanyl can lead to increased pressure in the bile duct and, in isolated cases, spasms of the sphincter of Oddi may occur.

In patients with myasthenia gravis, careful consideration should be given to the use of certain anticholinergics and neuromuscular blocking agents before and during general anesthesia, which includes intravenous fentanyl.

Use of fentanyl during labor may cause respiratory depression in the newborn.

Interactions with alcohol and drugs of abuse

Fentanyl may have additive CNS depressant effects when administered in conjunction with alcohol, other opioids, or illicit drugs with similar CNS effects.

Use in children. The safety of fentanyl has not been demonstrated in children under 2 years of age. Fentanyl should only be prescribed to children over 2 years of age who have demonstrated opioid tolerance.

Use in the elderly. Data from studies of intravenous fentanyl suggest that elderly patients may have decreased clearance and prolonged half-life and may be more sensitive to fentanyl than younger patients. Elderly patients should be closely monitored for symptoms of possible fentanyl overdose, which will require a reduction in the fentanyl dose.

Use during pregnancy and lactation. There is insufficient data regarding the use of fentanyl in pregnant women. Fentanyl crosses the placenta in early pregnancy. Animal studies have shown reproductive toxicity, but the implications for humans are unknown. Long-term use of fentanyl during pregnancy can lead to neonatal withdrawal syndrome, which can be life-threatening if left untreated. If it is necessary to take opioids for an extended period of time during pregnancy, the patient should be warned of the risk of neonatal withdrawal syndrome and ensure that appropriate treatment will be available.

The use of fentanyl (IV or IM) during childbirth (including cesarean section) is not recommended because fentanyl crosses the placenta and also because the fetal respiratory center is particularly sensitive to opiates. If a decision is made to use fentanyl, a ready-to-use antidote must be available.

Fentanyl is excreted in breast milk and may cause sedation/respiratory depression in infants, so do not breastfeed for 24 hours after taking the drug. The risk/benefit ratio of breastfeeding after fentanyl use should be considered.

Serotonin syndrome

Caution should be exercised when concomitantly using fentanyl with drugs that affect the serotonergic neurotransmitter system.

Concomitant use with serotonergic drugs, such as selective serotonin reuptake inhibitors, serotonin and norepinephrine reuptake inhibitors, as well as drugs that affect serotonin metabolism (including monoamine oxidase inhibitors), can lead to the development of life-threatening serotonin syndrome.

The development of serotonin syndrome can occur when medications are used in recommended doses.

The clinical picture of serotonin syndrome may include the following symptoms:

Changes in mental status (anxiety, hallucinations, coma);

Disorders of the autonomic nervous system (tachycardia, labile blood pressure, hyperthermia);

Neuromuscular disorders (hyperreflexia, lack of coordination, muscle rigidity);

Gastrointestinal symptoms (eg, nausea, vomiting, diarrhea).

If serotonin syndrome is suspected, fentanyl use should be discontinued immediately.

Impact on the ability to drive vehicles and other potentially dangerous mechanisms. Driving and engaging in other potentially hazardous activities are only possible if a sufficient amount of time has passed after using the drug.

Interaction with other drugs

Effects of other drugs on fentanyl

Barbiturates, benzodiazepines, antipsychotics, halogen gases, and other non-selective CNS depressants (eg, alcohol) may potentiate respiratory depression when used together with fentanyl. When using such drugs, the dose of fentanyl should be reduced.

Fentanyl is a drug with high clearance and is rapidly and extensively metabolized, mainly by CYP3A4.

Concomitant use of fentanyl with strong inhibitors of the cytochrome P450CYP3A4 isoenzyme (ritonavir, ketoconazole, itraconazole, troleandomycin, clarithromycin, nelfinavir and nefazodone) may lead to increased plasma concentrations of fentanyl, which increases the risk of adverse reactions, including life-threatening respiratory depression, or prolongs the symptoms of adverse reactions. reactions. Patients receiving fentanyl and strong CYP3A4 inhibitors concomitantly should be carefully monitored over an extended period of time, with dosage adjustments being made if necessary.

When fluconazole or voriconazole and fentanyl are used together, the duration of action of fentanyl may be prolonged.

It is recommended to stop using MAO inhibitors two weeks before surgery or anesthesia. However, there are several reports of the use of fentanyl without consequences during surgery or anesthesia in patients who were on therapy with MAO inhibitors.

The combined use of fentanyl and muscle relaxants that do not have vagolytic properties can lead to bradycardia, including cardiac arrest.

Concomitant use of fentanyl and droperidol increases the risk of hypotension.

Pre-administration or concomitant use of cimetidine may increase plasma concentrations of fentanyl with repeated use of these drugs.

Bradycardia may be aggravated by previous or concomitant use of drugs such as beta-blockers, suxamethonium, halothane, vecuronium, which themselves have the ability to cause bradycardia.

Effects of fentanyl on other drugs

When fentanyl is used concomitantly with other CNS depressants, the dose of the latter should be reduced.

Fentanyl increases plasma concentrations of etomidate and increases its half-life during the elimination phase.

Concomitant use of fentanyl and intravenous midazolam results in an increase in the half-life and a decrease in the overall clearance of midazolam. When using the above drugs together with fentanyl, their dose may need to be reduced.

Serotonergic drugs: Concomitant use of fentanyl with serotonergic drugs, such as selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, monoamine oxidase inhibitors, may increase the risk of developing serotonin syndrome.

Storage conditions

Narcotic drug.

In a dark place at a temperature from 15 0 C to 25 0 C.

Keep out of the reach of children.

Best before date

Do not use after the expiration date stated on the packaging.

Package

In ampoules of 2 ml in blister packs No. 5×1, No. 5×2.

Release from pharmacies

Description

Transparent colorless solution.

Composition per ampoule

active substance: fentanyl - 0.1 mg;

Excipients: citric acid monohydrate - 0.068 mg, water for injection - up to 2 ml.

Pharmacotherapeutic group

Opioid analgesics. Phenylpiperidine derivatives. ATS code: N02AB03.

Pharmacological properties

Pharmacodynamics

Fentanyl is an opioid analgesic with high affinity for the mu-opioid receptor.

Fentanyl can be used as an analgesic component during general anesthesia or alone. Fentanyl may reduce cardiac output by slowing the heart rate, which is an advantage for cardiovascular conditions where it is desirable to reduce the stress response. 100 mcg of fentanyl (2 ml) is approximately equivalent in analgesic activity to 10 mg of morphine. The drug exhibits its effect quickly, but the maximum analgesic effect and inhibitory effect on the respiratory center occurs only after a few minutes. The duration of the analgesic effect with a single intravenous dose of up to 100 mcg is about 30 minutes. The depth of analgesia depends on the dose of the drug and can be adjusted according to the intensity of pain. Fentanyl has a high therapeutic breadth. In rats, the therapeutic index (LD50/ED50) for the lowest degree of analgesia is 277, compared with 69.5 and 4.6 for morphine and pethidine, respectively.

Like other opioid analgesics, fentanyl, depending on the dose and rate of administration, can cause muscle rigidity, euphoria, miosis and bradycardia.

Histamine release tests and prick tests in humans, as well as tests performed on dogs in vivo, showed that clinically significant histamine release is rare with fentanyl use. The specific opioid antagonist for fentanyl is naloxone.

Pharmacokinetics

Fentanyl is a lipid-soluble drug and its pharmacokinetics can be described using a three-compartment model. Following intravenous administration, high concentrations of fentanyl occur rapidly in well-perfused tissues such as the lungs, kidneys, and brain. Subsequently, the drug is redistributed to other tissues. It accumulates slowly in skeletal muscle and at an even slower rate in adipose tissue, from which it is gradually released into the blood. Up to 80% of fentanyl is bound to blood plasma proteins.

Fentanyl is primarily metabolized in the liver, probably by N-dealkylation, and is excreted primarily in the urine. Less than 10% is excreted unchanged. Fentanyl has a half-life of 3.7 hours.

Indications for use

Fentanyl is used for neuroleptanalgesia (in combination with droperidol), for premedication (as part of certain regimens), for induction of anesthesia, for pain relief (during short-term extracavitary operations), as an additional agent during operations under local anesthesia, for pain syndrome of strong and moderate intensity. with myocardial infarction, renal and hepatic colic.

Fentanyl is used to relieve constant (persistent) moderate to severe chronic pain that requires constant, round-the-clock prescription of opioids over a long period of time and cannot be relieved in another way (for example, non-steroidal anti-inflammatory drugs (or in patients with contraindications to the use of drugs of this group) ), a combination of opioids or immediate-release opioid preparations).

It is not recommended to use fentanyl for the relief of postoperative pain, except in cases where the administration of drugs with a high antinociceptive effect is required after palliative operations for cancer.

Directions for use and dosage regimen

Fentanyl should only be used by highly trained personnel and in conditions where mechanical ventilation is available.

The dose of the drug should be selected individually in accordance with the age, body weight, physical condition and underlying disease of the patient, and it also depends on the type of surgery and anesthesia performed, and the use of other medications.

The initial dose should be reduced in elderly and debilitated patients. The effect of the initial dose must be taken into account when determining maintenance doses. Fentanyl can be administered intravenously and intramuscularly. The drug can be administered intravenously to children and adults as a bolus or as an infusion.

Standard dosage regimen:

Adults and children over 12 years of age:

Doses greater than 200 mcg are used exclusively for anesthesia.

For premedication, 1-2 ml of the drug is administered intramuscularly before induction of anesthesia.

When given intravenously in patients without premedication, 2 mL of fentanyl can provide adequate analgesia for 10 to 20 minutes for low-pain surgeries. Bolus administration. 10 ml of fentanyl can provide analgesia for about 1 hour, which is used during operations with moderate pain intensity. Administration of fentanyl at a dose of 50 mcg/kg provides analgesia for 4-6 hours for operations with high pain intensity.

Fentanyl can also be given by intravenous infusion.

In mechanically ventilated patients, a loading dose of fentanyl can be given rapidly at a rate of approximately 1 mcg/kg/minute over the first 10 minutes, followed by a loading dose of approximately 0.1 mcg/kg/minute. An alternative route of loading loading dose administration may be bolus administration. The infusion rate should be titrated according to the individual patient's response; it may be necessary to reduce the rate of administration. Administration should be stopped approximately 40 minutes before the end of surgery, unless it is planned to continue artificial ventilation after surgery.

Lower rates of fentanyl administration, such as 0.05-0.08 mcg/kg/minute, may be required if spontaneous breathing is maintained. Higher rates of drug administration (up to 3 mcg/kg/minute) are used for cardiac surgery.

Use in children. For children over 12 years of age, the dosage regimen is the same as for adults. Standard dosage regimen for children from 2 to 12 years of age:

In children, it is used for analgesia during surgery, enhancing anesthesia while maintaining spontaneous breathing.

Side effect

To assess the frequency of occurrence of the following adverse reactions, the following gradations were used: very often (≥1/10), often (from ≥1/100 to

From the immune system: unknown - hypersensitivity (anaphylactic shock, anaphylactic reactions, urticaria).

Mental disorders: infrequently - euphoria.

From the nervous system: often - dyskinesia, sedation, dizziness; infrequently - headache; unknown - convulsions, loss of consciousness, myoclonus.

From the senses: often - impaired visual perception.

From the cardiovascular system: often - bradycardia, tachycardia, arrhythmia, hypotension, hypertension, pain along the vein; infrequently - phlebitis, fluctuations in blood pressure; unknown - cardiac arrest.

From the respiratory system: often - laryngospasm, bronchospasm, apnea; infrequently - hyperventilation, hiccups; unknown - respiratory depression.

From the gastrointestinal tract: very often - nausea, vomiting.

From the skin: often - allergic dermatitis; unknown - itching.

From the musculoskeletal system: very often - muscle rigidity (including the chest).

From the reproductive system: unknown - decreased libido, impotence, erectile dysfunction, lack of menstruation, infertility. If these adverse reactions develop, it is necessary to evaluate the level of sex hormones.

Others: often - postoperative confusion; uncommon - hypothermia, chills, postoperative agitation, complications of anesthesia from the respiratory tract.

When fentanyl is used together with antipsychotics, the following adverse reactions may occur: chills and/or myoclonus, anxiety, postoperative hallucinations and extrapyramidal symptoms.

When fentanyl is used concomitantly with serotonergic drugs, patients should be carefully monitored if the following symptoms develop: agitation, hallucinations, rapid heartbeat, fever, increased sweating, chills or tremors, muscle twitching (muscle cramps) or rigidity (stiffness), loss of coordination, nausea, vomiting or diarrhea (see section "Precautions" - Serotonin syndrome).

Contraindications

Overdose

Precautionary measures

Fentanyl, like other opioid analgesics, can be subject to abuse both when used in accordance with its indications for use and when the drug is obtained illicitly. This risk must be taken into account when prescribing, prescribing and dispensing a medicinal product in cases where there are concerns about misuse, abuse or otherwise. violations.

Concerns about abuse, dependence, and inappropriate use should not be a reason for not providing appropriate pain management. However, all patients receiving opioid analgesics require careful monitoring for signs of dependence and abuse, as there is a risk of developing dependence even with the proper use of opioid analgesics.

Fentanyl should not be used to relieve short-term or mild pain.

Concomitant use of drugs that affect the central nervous system requires special assessment and monitoring.

Head injuries and increased intracranial pressure

With long-term use of fentanyl, tolerance and drug dependence may develop.

Opioids may cause hypotension, especially in hypovolemic patients. Necessary measures must be taken to maintain stable blood pressure.

Patients on long-term opioid therapy or with opioid dependence may require higher doses of fentanyl.

As with other opioids, due to its anticholinergic effects, the use of fentanyl can lead to increased pressure in the bile duct and, in isolated cases, spasms of the sphincter of Oddi may occur.

Use of fentanyl during labor may cause respiratory depression in the newborn.

Interactions with alcohol and drugs of abuse

Fentanyl may have additive CNS depressant effects when administered in conjunction with alcohol, other opioids, or illicit drugs with similar CNS effects.

Use during pregnancy during pregnancy and lactation

There is insufficient data regarding the use of fentanyl in pregnant women. Fentanyl crosses the placenta in early pregnancy. Animal studies have shown reproductive toxicity, but the implications for humans are unknown. Long-term use of fentanyl during pregnancy can lead to neonatal withdrawal syndrome, which can be life-threatening if left untreated. If it is necessary to take opioids for an extended period of time during pregnancy, the patient should be warned of the risk of neonatal withdrawal syndrome and ensure that appropriate treatment will be available.

Serotonin syndrome

Caution should be exercised when concomitantly using fentanyl with drugs that affect the serotonergic neurotransmitter system.

The development of serotonin syndrome can occur when medications are used in recommended doses.

The clinical picture of serotonin syndrome may include the following symptoms:

Changes in mental status (anxiety, hallucinations, coma); disorders of the autonomic nervous system (tachycardia, labile blood pressure, hyperthermia); neuromuscular disorders (hyperreflexia, lack of coordination, muscle twitching (muscle cramps) or muscle rigidity); gastrointestinal symptoms (eg, nausea, vomiting, diarrhea).

Symptoms typically develop within hours to several days of starting concomitant opioid therapy with other drugs. However, symptoms may develop later, especially after increasing the dose of drugs.

If serotonin syndrome is suspected, discontinue opioids and/or other concomitant medications.

Adrenal insufficiency

Patients should be closely monitored if symptoms of adrenal insufficiency occur, such as nausea, vomiting, loss of appetite, fatigue, weakness, dizziness, or low blood pressure. If adrenal insufficiency is suspected, diagnostic testing should be performed. If necessary, if the test result is positive, it is necessary to prescribe treatment with corticosteroids and discontinue opioids. If opioids are discontinued, a follow-up evaluation of adrenal function should be performed to determine the need to continue or discontinue corticosteroid therapy.

Androgen deficiency

Chronic use of opioids can affect the hypothalamic-pituitary-gonadal axis, which can lead to androgen deficiency, which manifests as low libido, impotence, erectile dysfunction, amenorrhea and infertility. If symptoms or signs of androgen deficiency appear, laboratory diagnosis should be performed.

Impact on the ability to drive vehicles and other potentially dangerous mechanisms

Driving and engaging in other potentially hazardous activities are only possible if a sufficient amount of time has passed after using the drug.

Interaction with other drugs

The effects of other drugs onfentanyl

Fentanyl is a highly cleared drug that is rapidly and extensively metabolized, primarily by CYP3A4.

When fluconazole or voriconazole and fentanyl are used together, the duration of action of fentanyl may be increased.

The combined use of fentanyl and muscle relaxants that do not have vagolytic properties can lead to bradycardia, including cardiac arrest.

Concomitant use of fentanyl and droperidol increases the risk of hypotension.

Pre-administration or concomitant use of cimetidine may increase plasma concentrations of fentanyl during repeated use of these drugs. Bradycardia may be aggravated by previous or concomitant use of drugs such as beta-blockers, suxamethonium, halothane, vecuronium, which themselves have the ability to cause bradycardia.

Impactfentanylfor other medicines

When fentanyl is used concomitantly with other CNS depressants, the dose of the latter should be reduced.

Fentanyl increases plasma concentrations of etomidate and increases its half-life during the elimination phase.

Serotonergicmedicines: Concomitant use of fentanyl with serotonergic drugs, such as selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, monoamine oxidase inhibitors, may increase the risk of developing serotonin syndrome. If concomitant use of opioids and serotonergic drugs is indicated, patients should be monitored closely, particularly during treatment initiation and dose increases (see Precautions). - Serotonin syndrome).

st. Fabricius, 30, t./f.: (+37517)22037 16,

e-mail: [email protected]

Fentanyl

International nonproprietary name

Fentanyl

Dosage form

Solution for injection, 0.005% 2 ml

Compound

1 ml of solution contains

active substance - fentanyl 0.05 mg,

Excipients - citric acid, monohydrate; water for injections.

Description

Transparent colorless liquid.

Pharmacotherapeutic group

Anesthetics. General anesthetics. Opioid analgesics. Fentanyl.

ATX code N01A H01

Pharmacological properties

Pharmacokinetics

Rapidly redistributed from the blood and brain to muscle and fat tissue. Plasma protein binding reaches 79%. Metabolized in the liver by N-dealkylation and hydroxylation, as well as in the kidneys, intestines and adrenal glands. Clearance is 0.4 - 0.5 l/min, half-life is 10 - 30 min, volume of distribution is 60 - 80 l. It is excreted by the kidneys (about 75% in the form of metabolites and 10% unchanged) and intestines (9% in the form of metabolites). Passes into breast milk.

Pharmacodynamics

Opioid analgesic. Has a pronounced analgesic effect. Its analgesic activity is significantly higher than that of morphine.

Opiate receptor agonist, interacts primarily with mu receptors in the central nervous system, spinal cord and peripheral tissues. Increases the activity of the antinociceptive system, increases the threshold of pain sensitivity. It disrupts the transmission of excitation along specific and nonspecific pain pathways to the nuclei of the thalamus, hypothalamus and amygdala complex. Reduces the emotional assessment of pain, causes euphoria, which contributes to the formation of addiction (mental and physical). By reducing the excitability of pain centers, it has a hypnotic effect.

With repeated administration, tolerance and drug dependence may develop.

It depresses the respiratory center, stimulates the vomiting center and the centers of the vagus nerve, causing the appearance of bradycardia. Increases the tone of the smooth muscles of internal organs, as well as the sphincters of the urethra, bladder, sphincter of Oddi, biliary tract and gastrointestinal tract with simultaneous inhibition of peristalsis, improves the absorption of water from the gastrointestinal tract. Reduces the intensity of renal blood flow. Leads to an increase in amylase and lipase levels in the blood.

The analgesic effect when administered intravenously develops after 1 - 3 minutes, reaching a maximum after 5 - 7 minutes; when administered intramuscularly, the effect begins within 10 - 15 minutes; The duration of the effect with a single injection is about 30 minutes.

Indications for use

neuroleptanalgesia (as an analgesic and additional agent)

general anesthesia and as an anesthetic for induction during anesthesia

as a respiratory depressant in intensive care.

Directions for use and doses

Fentanyl is used only in a hospital setting under the supervision of a physician. The dose of fentanyl must be selected individually (depending on the clinical situation).

Fentanyl is administered intravenously and intramuscularly.

Adults: for premedication and in the postoperative period - intramuscularly, 1 - 2 ml (0.05 - 0.1 mg of fentanyl);

for induction anesthesia - 2 - 4 ml (0.1 - 0.2 mg of fentanyl) intravenously;

neuroleptanalgesia - 4 - 12 ml (0.2 - 0.6 mg fentanyl) intravenously, the administration is repeated every 20 minutes;

during operations under local anesthesia - 0.5 - 1 ml (0.025 - 0.05 mg of fentanyl) intramuscularly or intravenously, possibly repeated administration every 20 - 30 minutes;

to reduce severe pain - intramuscularly or intravenously, 0.5 - 1 - 2 ml (0.025 - 0.05 - 0.1 mg of fentanyl).

Doses exceeding 200 mcg are used exclusively for anesthesia.

Children from 2 to 12 years old are administered intramuscularly at 0.04 ml/kg (0.002 mg/kg) body weight.

Side effects

- drowsiness

Paradoxical stimulation of the central nervous system

Confusion, hallucinations

Euphoria

Muscle stiffness

- bradycardia, tachycardia

- hypoventilation, shortness of breath, respiratory depression to the point of stopping (when administered in large doses), bronchospasm, laryngospasm, cough

- nausea, vomiting

Constipation, spasm of the sphincter of Oddi

Increased sweating

Hepatic colic

- obstruction of urine outflow

- visual impairment, miosis

Possible toxic reactions: itching, erythema with subcutaneous injection, bleeding with injection into the submucosa, acute toxic delirium with subcutaneous injection, anaphylactic shock

Dry mouth

Headache, dizziness

Biliary spasm, liver enzyme fluctuations

Orthostatic hypotension, cardiac arrest

Libido and potency disorders

Increased intracranial pressure

Convulsions (in children), loss of consciousness, myoclonus

Postoperative disorientation in time and space

Chills, hypothermia, postoperative agitation

Air embolism

Spasm of the ureters, urinary retention (in patients with prostatic hypertrophy)

Extrapyramidal symptoms

Contraindications

Breathing disorders due to depression of the respiratory center, bronchial asthma, obstructive airway diseases

For patients after surgical interventions on the biliary tract

Addiction

Cranial hypertension

Severe liver failure

Pregnancy and lactation (breastfeeding excluded)

Increased individual sensitivity to the components of the drug, other opioid anesthetics and muscle relaxants

Caesarean section operations before fetal extraction, other obstetric operations (possible depression of the fetal respiratory center)

Concomitant use with MAO inhibitors and for 2 weeks after its cessation

Children under 2 years of age.

Drug interactions

Buprenorphine reduces the effect of the drug. When used simultaneously with other drugs that have a depressive effect on the central nervous system (opiates, sedatives, hypnotics, phenothiazines, tranquilizers, muscle relaxants, antihistamines that cause sedation, alcohol, etc.), a mutual increase in side effects is possible (depression of the central nervous system , hypoventilation, hypotension, etc.). With systematic use of barbiturates (especially phenobarbital), the analgesic effect of narcotic analgesics may be reduced. Long-term use of barbiturates or narcotic analgesics causes the development of cross-tolerance. Benzodiazepines prolong recovery from neuroleptanalgesia. Nitrous oxide increases muscle rigidity, antihypertensive drugs increase hypotension, and monoamine oxidase inhibitors increase the risk of severe complications.

Naloxone reverses the respiratory depression and analgesia caused by narcotic analgesics. Nalorphine reverses the respiratory depression caused by narcotic analgesics while maintaining their analgesic effect.

special instructions

The use of fentanyl is recommended in conditions of resuscitation readiness and only in the presence of an anesthesiologist. With repeated use, addiction and drug dependence may develop. Euphoria is possible. The drug is withdrawn gradually.

Use with caution in cases of impaired liver and kidney function, hypothyroidism, adrenal insufficiency, prostate hypertrophy, shock, myasthenia gravis, inflammatory diseases of the gastrointestinal tract, as well as in patients over 60 years of age. When using high doses in depleted and asthenic patients, secondary respiratory depression may develop, associated with the release of fentanyl 1 to 2 hours after administration into the gastric lumen and subsequent resorption.

During the treatment period, avoid drinking alcohol.

If side effects develop, activated charcoal can be used in conscious patients.

One must be especially careful when using Fentanyl, in particular in patients with myasthenia gravis, where there is rigidity of the respiratory muscles. There is information about contraindications for the use of Fentanyl in opioid-dependent patients; this can lead to the development of fatal respiratory depression. Due to postoperative depression after the use of Fentanyl, patients require care after surgery. In the presence of respiratory depression, an opioid antagonist, naloxone, is used. All patients require observation for 6 hours after the last dose of naloxone. Respiratory stimulation is carried out by administering Doxapram, which does not affect analgesia. Elderly patients have muscle sensitivity to Fentanyl, so they need to use a lower dose.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms.

During the treatment period, you should not engage in potentially hazardous activities that require rapid psychomotor reactions.

Overdose

Symptoms: the earliest and most dangerous manifestation is depression of the respiratory center.

Treatment: general resuscitation measures, oxygen inhalation, prescription of antagonists and agonist-antagonists of opiate receptors (naloxone, nalorphine), respiratory analeptics.

Release form and packaging

2 ml in glass ampoules.

5 ampoules are placed in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

20 contour cell packages together with instructions for medical use in the state and Russian languages and a ceramic cutting disc or ceramic ampoule knife are placed in a cardboard box.