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

Fentanyl is an opioid analgesic of short action. Like morphine and promedol, fentanyl is an agonist, mainly of mu-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% - in unchanged form) 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);

- pain syndrome associated with a spasm of smooth muscles of internal organs (with the established diagnosis it is used in combination with atropine-like and antispasmodics).

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 hypertension of the small circle of blood circulation, extrapyramidal disorders, children under 1 year old.

Carefully:

Pregnancy, lactation, elderly; patients with a history of guest indication addiction to opioids, liver and / or renal colic, simultaneous reception of insulin, glucocorticoid and antihypertensive drugs, craniocerebral trauma, hypothyroidism, weakened patients, prostatic hypertrophy, stricture of the urethra, suicide, hyperthermia, administration of MAO inhibitors.

Pregnancy and lactation:

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

Dosing and Administration:

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, 50-150 μg of fentanyl (in combination with droperidol) is administered every 10-30 minutes.

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 for 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:

- when preparing for a surgical operation - 2 μg / kg;

- for general anesthesia - 10-150 mcg / kg intravenously or 150-250 mcg / kg intramuscularly;

- to maintain anesthesia - 1-2 mcg / kg intravenously or 2 mcg / kg intramuscularly.

Side effects:

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

From the nervous system and sense organs: headache, depression, or paradoxical excitation of the central nervous system, 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: bradypnea, apnea, rigidity of muscles, depression of the respiratory center, lowering of arterial pressure, bradycardia.

Treatment: cessation of the administration of the drug, maintenance of adequate pulmonary ventilation. Intravenous introduction of a specific opioid antagonist - naloxone in doses from 0.4 mg to 2 mg; in the absence of effect after 2-3 minutes, the administration of naloxone is repeated. It is possible to use nalorphine: 5-10 mg intramuscularly or intravenously every 15 minutes to a total dose of 40 mg. It is necessary to consider the possibility of developing a withdrawal syndrome with the administration of naloxone or nalorphinepatients with 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 of a 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 (including 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 vagolytic activity (including pancuronium bromide) reduce the risk of bradycardia and hypotension (especially when using beta-blockers and other vasodilators) and may increase the risk of tachycardia and hypertension; muscle relaxants that do not possess vagolytic activity (including succinylcholine) do not reduce the risk of bradycardia and hypotension (especially in the background of a burdened cardiological history) 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, promedol) 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.

With pain caused by a spasm of smooth muscles of the internal organs (liver, kidney, stomach cramps), fentanyl should be combined with atropinopodobnymi and spasmolytic drugs with careful monitoring of the patient's condition.

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

During treatment it is not recommended to engage in potentially dangerous activities requiring concentration of attention and psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection, 50 μg / ml.

Packaging:

In ampoules of 1 ml and 2 ml.

5 ampoules per contour cell packaging made of polyvinylchloride film and aluminum foil.

For 1 or 2 contour packs with instruction on the use of the drug, a knife or scarifier ampullum in a pack of cardboard.

For 20, 50 or 100 contour mesh packages, together with an equal number of instructions for use, respectively, with knives or scarifiers ampoule into boxes of cardboard or into boxes of corrugatedcardboard.

When packing ampoules with rings or break points, knives or scarifier ampoules do not.

Storage conditions:

List II. "List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation", in specially equipped premises with a license for the specified type of activity. At a temperature of no higher than 25 ° C. In a place inaccessible to children.

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 N000266 / 01

Date of registration:10.10.2011

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Representation: & nbspMOSCOW ENDOCRINE FACTORY FGUP MOSCOW ENDOCRINE FACTORY FGUP Russia

Information update date: & nbsp21.09.2015

Illustrated instructions

Instructions

Fentanyl (Fentanyl)