Fentanyl - instructions for use, dose, side effects, contraindications

Fentanyl is an opioid analgesic of short action. Like morphine and trimeridin, fentanyl is an agonist, mainly, μ-opioid receptors. Activates the endogenous antinociceptive system and thus disrupts the interneuronal transmission of pain impulses at various levels of the central nervous system (CNS), and also changes the emotional color of the pain.

By pharmacological properties fentanyl is close to morphine: it increases the threshold of pain sensitivity with pain stimuli of different modalities, inhibits conditioned reflexes, has a depressing effect on the central nervous system, inhibits the activity of the respiratory center. It differs from morphine by a greater activity (by analgesic effect it is 100 times higher morphine), shorter duration of action and more pronounced ability to depress the respiratory center.

When parenteral administration has a rapid analgesic effect. With intravenous administration, the maximum effect develops after 1-3 min and persists for 15-20 min; with intramuscular injection, the maximum effect develops in 3-10 minutes, the duration of action is 1-2 hours.

Pharmacokinetics:

To achieve an average level of anesthesia, the concentration of fentanyl should reach 15-20 ng / ml. The connection with plasma proteins is 79-87%. The clearance is 400-500 ml / min, the half-life period is 10-30 min, the volume of distribution is 60-80 l. Rapidly redistributed from the blood and brain into muscles and adipose tissue. Metabolised in the liver (N-dealkylation and hydroxylation), kidneys, intestines and adrenal glands. It is excreted by the kidneys (75% - in the form of metabolites and 10% - unchanged) and with bile (9% - in the form of metabolites). Penetrates into breast milk.

Indications:

Pain syndrome of strong and medium intensity: postoperative pain, angina pectoris, myocardial infarction, pain in cancer patients.

Premedication before surgical operations.

As an additional analgesic for operations under local anesthesia.

Postoperative anesthesia.

Neuroleptanalgesia (in combination with droperidol).

Contraindications:

Hypersensitivity to any of the components of the drug, impaired consciousness, brain tumor; bradyarrhythmia, arterial hypotension, hepatic and / or renal insufficiency, respiratory failure (pneumonia, atelectasis and pulmonary infarction, bronchial asthma, propensity to bronchospasm); intracranial hypertension. Severe oppression of the respiratory center, acute surgical diseases of the abdominal cavity before diagnosis; cesarean section and other obstetric operations in the pre-fetal stage (threat of respiratory depression of the newborn); severe pulmonary hypertension, extrapyramidal disorders, children under 1 year of age.

Carefully:

Myasthenia gravis gravis, elderly age, weakened patients; hypothyroidism, lung disease, respiratory failure, alcoholism, renal / hepatic insufficiency, pregnancy, simultaneous intake of insulin, glucocorticosteroids and antihypertensive drugs, craniocerebral trauma, hypothyroidism, prostatic hypertrophy, urethral stricture, suicidal tendencies, hyperthermia, monoamine oxidase inhibitors (MAO).

Pregnancy and lactation:

Information about the safety of fentanyl during pregnancy is not enough. If it is necessary to introduce, the potential risk to the fetus and the possible benefits for the mother should be correlated.

Fentanyl penetrates the placenta, and the respiratory center of the fetus is particularly sensitive to narcotic analgesics, so the use of fentanyl during labor (including cesarean section) is not recommended. However, if the drug has still been introduced, it is necessary for the newborn to have antagonists of opioid receptors at the ready.

Fentanyl penetrates into breast milk. Breastfeeding should be discontinued 24 hours after the administration of fentanyl.

Dosing and Administration:

Intravenous (jet or drip), intramuscularly.

Doses are selected individually according to age, body weight, general condition, concomitant diseases, taking other medications and the type of surgery performed.

For premedication injected intramuscularly 30 minutes prior to surgery at a dose of 50-100 mcg.

For implementation of introductory anesthesia is administered intravenously at a dose of 100-200 μg.

To maintain an adequate level of analgesia After every 10-30 minutes, 50-150 μg of fentanyl (in combination with droperidol) is administered.

If the muscle relaxants are not used and neuroleptanalgesia is performed while maintaining spontaneous breathing (with short, extra-vaginal operations), after neuroleptic fentanyl injected at a dose of 50 mcg per 10-20 kg of body weight, while monitoring spontaneous breathing and maintaining readiness for intubation and artificial ventilation (IVL). In higher doses (50-100 μg / kg) fentanyl apply only for operations on the open heart.

As an additional anesthetic in operations under local anesthesia fentanyl (often with neuroleptics) is administered intramuscularly or intravenously at a dose of 25-50 μg.If necessary, repeat the injection every 20-30 minutes.

For relief of acute pain - intramuscularly or intravenously, 25-100 mcg alone or in combination with antipsychotics.

Children only intravenously. In spontaneous breathing, the initial dose is 3-5 μg / kg, repeated (additional) - 1 μg / kg; with an auxiliary ventilation, the initial dose is 15 μg / kg, repeated (additional) -1-3 μg / kg.

Side effects:

From the respiratory system: bronchospasm, laryngospasm, respiratory depression right up to the stop (large doses).

From the nervous system and sensory organs: headache, depression or paradoxical CNS excitement, convulsions, blurred vision, diplopia, increased intracranial pressure.

From the digestive system: nausea, vomiting, constipation, hepatic colic (in patients who had it in the anamnesis), flatulence, spasm of sphincter of Oddi.

Other: allergic reactions of varying severity, bradycardia (up to cardiac arrest), lowering of blood pressure, urinary retention, short-term stiffness of muscles (including breast), increased sweating, drug dependence, tolerance, withdrawal syndrome.

Overdose:

Symptoms: depression of the respiratory center, apnea, rigidity of muscles, lowering of arterial pressure, bradycardia.

Treatment: discontinuation of the drug, with hypoventilation and apnea appointed oxygen, Mechanical ventilation. With respiratory depression, intravenous injection of a specific opioid receptor antagonist - naloxone in doses from 0.4 mg to 2.0 mg; in the absence of effect after 2-3 minutes, the administration of naloxone is repeated; holding your breath. It is possible to use nalorphine: 5-10 mg intramuscularly or intravenously every 15 minutes to a total dose of 40 mg. Consideration should be given to the possibility of developing a withdrawal syndrome when naloxone or nalorphine is administered to patients with a dependence on morphine or fentanyl; In such cases, the doses of antagonists should be increased gradually. Symptomatic and maintenance therapy: the introduction of muscle relaxants, with bradycardia - the introduction of 0.5-1 ml 1% solution of atropine.

Interaction:

Ethanol and antihistamines, which have a sedative effect, increase the likelihood of side effects.

Enhances the effect of antihypertensive drugs. Beta-adrenoblockers can reduce the frequency and severity of hypertensive reaction in cardiac surgery (incl.with sternotomy), but increase the risk of bradycardia.

Benzodiazepines prolong the yield of neuroleptanalgesia.

MAO inhibitors increase the risk of serious complications.

Muscle relaxants prevent or eliminate muscle rigidity; muscle relaxants with m-cholinoblocking activity (including pancuronium bromide) reduce the risk of bradycardia and hypotension (especially when using beta-adrenoblockers and other vasodilators) and may increase the risk of tachycardia and hypertension; muscle relaxants that do not possess m-cholinoblocking activity (including suxamethonium) do not reduce the risk of bradycardia and hypotension (especially in the background of a burdened cardiological anamnesis) and increase the risk of serious side effects from the cardiovascular system.

Fentanyl should be used with caution against the background of the funds for general anesthesia, hypnotics and antipsychotics to avoid excessive CNS suppression and inhibition of respiratory center activity. Tricyclic antidepressants also increase the risk of suppression of the respiratory center. Dinitrogen oxide (nitrous oxide) increases muscle rigidity.

Fentanyl do not do it combine with narcotic analgesics from the group of partial agonists (buprenorphine) and opioid receptor antagonist agonists (nalboufine, butorphanol, tramadol) because of the danger of weakening analgesia.

When carrying out concomitant treatment with insulin preparations, antihypertensive drugs and glucocorticosteroids fentanyl should be used in reduced doses.

The analgesic effect and side effects of opioid agonists (morphine, trimiperidine) in the therapeutic dose range are summarized with the effects of fentanyl.

Special instructions:

Fentanyl should only be used by highly qualified personnel in a specialized hospital setting.

In the postoperative period, the patient must be carefully monitored.

In patients with reduced body weight, with prolonged operations, or in the case of frequent repeated use of fentanyl, an increase in the duration of its action is possible.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Effect on the ability to drive transp. cf. and fur:

The patient is not recommended to drive vehicles and engage in other activities.potentially dangerous activities requiring increased concentration and speed of psychomotor reactions, within 24 hours after the administration of fentanyl.

Form release / dosage:Solution for intravenous and intramuscular injection, 50 μg / ml.

Packaging:

Ampoules of 1 ml or 2 ml; on 5 ampoules in a planar cell package. 20, 30, 40, 50 or 100 contour mesh packages together with instructions for use, with ampoules or scarifiers, if necessary for ampoules of this type, in a cardboard box (for hospitals).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children. List II of the "List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation", approved by the Government of the Russian Federation of June 30, 1998, No. 681.

Shelf life:

4 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:For hospitals

Registration number:P N002020 / 01

Date of registration:10.12.2008

The owner of the registration certificate:GosMPS, FSUE GosMPS, FSUE Russia

Manufacturer: & nbsp

GosMPS, FSUE Russia

Information update date: & nbsp21.09.2015

Illustrated instructions

Instructions

Fentanyl (Phentanyl)