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Fentanyl (injection) is an analgesic opioid that is FDA approved for the treatment of general or regional anesthesia. Common adverse reactions include application site reaction, diaphoresis, pruritus, abdominal pain (transdermal, constipation (adults, , diarrhea, indigestion (transdermal, loss of appetite, nausea, vomiting, xerostomia, asthenia, confusion , dizziness, feeling nervous, headache, insomnia, somnolence, psychiatric: Anxiety, depression, euphoria, hallucinations, upper respiratory infection , influenza-like symptoms.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
- Fentanyl citrate is indicated:
- for analgesic action of short duration during the anesthetic periods, premedication, induction and maintenance, and in the immediate postoperative period (recovery room) as the need arises.
- for use as a narcotic analgesic supplement in general or regional anesthesia.
- for administration with a neuroleptic as an anesthetic premedication, for the induction of anesthesia and as an adjunct in the maintenance of general and regional anesthesia.
- for use as an anesthetic agent with oxygen in selected high risk patients, such as those undergoing open heart surgery or certain complicated neurological or orthopedic procedures.
- 50 mcg = 0.05 mg = 1 ml
- Dosage should be individualized. Some of the factors to be considered in determining the dose are age, body weight, physical status, underlying pathological condition, use of other drugs, type of anesthesia to be used and the surgical procedure involved. Dosage should be reduced in elderly or debilitated patients.
- Vital signs should be monitored routinely.
- Premedication — Premedication (to be appropriately modified in the elderly, debilitated and those who have received other depressant drugs) — 50 to 100 mcg (0.05 to 0.1 mg) (1 to 2 ml) may be administered intramuscularly 30 to 60 minutes prior to surgery.
- Adjunct to General Anesthesia
- Adjunct to Regional Anesthesia - 50 to 100 mcg (0.05 to 0.1 mg) (1 to 2 ml) may be administered intramuscularly or slowly intravenously, over one to two minutes, when additional analgesia is required.
- Postoperatively (recovery room) - 50 to 100 mcg (0.05 to 0.1 mg) (1 to 2 ml) may be administered intramuscularly for the control of pain, tachypnea and emergence delirium. The dose may be repeated in one to two hours as needed.
- Usage in Children: For induction and maintenance in children 2 to 12 years of age, a reduced dose as low as 2 to 3 mcg/kg is recommended.
As a General Anesthetic
- When attenuation of the responses to surgical stress is especially important, doses of 50 to 100 mcg/kg (0.05 to 0.1 mg/kg) (1 to 2 ml/kg) may be administered with oxygen and a muscle relaxant. This technique has been reported to provide anesthesia without the use of additional anesthetic agents. In certain cases, doses up to 150 mcg/kg (0.15 mg/kg) (3 ml/kg) may be necessary to produce this anesthetic effect. It has been used for open heart surgery and certain other major surgical procedures in patients for whom protection of the myocardium from excess oxygen demand is particularly indicated, and for certain complicated neurological and orthopedic procedures.
- As noted above, it is essential that qualified personnel and adequate facilities be available for the management of respiratory depression.
- Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
Off-Label Use and Dosage (Adult)
There is limited information regarding Off-Label Guideline-Supported Use of Fentanyl (injection) in adult patients.
There is limited information regarding Off-Label Non–Guideline-Supported Use of Fentanyl (injection) in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding FDA-Labeled Use of Fentanyl (injection) in pediatric patients.
Off-Label Use and Dosage (Pediatric)
There is limited information regarding Off-Label Guideline-Supported Use of Fentanyl (injection) in pediatric patients.
There is limited information regarding Off-Label Non–Guideline-Supported Use of Fentanyl (injection) in pediatric patients.
- Fentanyl citrate is contraindicated in patients with known intolerance to the drug or other opioid agonists.
- Fentanyl citrate SHOULD BE ADMINISTERED ONLY BY PERSONS SPECIFICALLY TRAINED IN THE USE OF INTRAVENOUS ANESTHETICS AND MANAGEMENT OF THE RESPIRATORY EFFECTS OF POTENT OPIOIDS.
- AN OPIOID ANTAGONIST, RESUSCITATIVE AND INTUBATION EQUIPMENT AND OXYGEN SHOULD BE READILY AVAILABLE.
- If fentanyl citrate is administered with a tranquilizer, the user should become familiar with the special properties of each drug, particularly the widely differing duration of action. In addition, when such a combination is used, fluids and other countermeasures to manage hypotension should be available.
- As with other potent narcotics, the respiratory depressant effect of fentanyl citrate may persist longer than the measured analgesic effect. The total dose of all narcotic analgesics administered should be considered by the practitioner before ordering narcotic analgesics during recovery from anesthesia. It is recommended that narcotics, when required, should be used in reduced doses initially, as low as ¼ to ⅓ those usually recommended.
- Fentanyl citrate may cause muscle rigidity, particularly involving the muscles of respiration. This rigidity has been reported to occur or recur infrequently in the extended postoperative period usually following high dose administration. In addition, skeletal muscle movements of various groups in the extremities, neck and external eye have been reported during induction of anesthesia with fentanyl; these reported movements have, on rare occasions, been strong enough to pose patient management problems. This effect is related to the dose and speed of injection and its incidence can be reduced by: 1) administration of up to ¼ of the full paralyzing dose of a non-depolarizing neuromuscular blocking agent just prior to administration of fentanyl citrate; 2) administration of a full paralyzing dose of a neuromuscular blocking agent following loss of eyelash reflex when fentanyl citrate is used in anesthetic doses titrated by slow intravenous infusion; or, 3) simultaneous administration of fentanyl citrate and a full paralyzing dose of a neuromuscular blocking agent when fentanyl citrate is used in rapidly administered anesthetic dosages. The neuromuscular blocking agent used should be compatible with the patient's cardiovascular status.
- Adequate facilities should be available for postoperative monitoring and ventilation of patients administered anesthetic doses of fentanyl citrate. Where moderate or high doses are used (above 10 mcg/kg), there must be adequate facilities for postoperative observation, and ventilation if necessary, of patients who have received fentanyl citrate. It is essential that these facilities be fully equipped to handle all degrees of respiratory depression.
- Fentanyl citrate may also produce other signs and symptoms characteristic of narcotic analgesics including euphoria, miosis, bradycardia and bronchoconstriction.
- Severe and unpredictable potentiation by MAO inhibitors has been reported for other narcotic analgesics. Although this has not been reported for fentanyl, there are insufficient data to establish that this does not occur with fentanyl. Therefore, when fentanyl is administered to patients who have received MAO inhibitors within 14 days, appropriate monitoring and ready availability of vasodilators and beta-blockers for the treatment of hypertension is indicated.
- Head Injuries and Increased Intracranial Pressure
- Fentanyl citrate should be used with caution in patients who may be particularly susceptible to respiratory depression, such as comatose patients who may have a head injury or brain tumor. In addition, fentanyl citrate may obscure the clinical course of patients with head injury.
Clinical Trials Experience
- As with other narcotic analgesics, the most common serious adverse reactions reported to occur with fentanyl citrate are respiratory depression, apnea, rigidity, and bradycardia; if these remain untreated, respiratory arrest, circulatory depression or cardiac arrest could occur. Other adverse reactions that have been reported are hypertension, hypotension, dizziness, blurred vision, nausea, emesis, diaphoresis, pruritus, urticaria, laryngospasm and anaphylaxis.
- It has been reported that secondary rebound respiratory depression may occasionally occur postoperatively. Patients should be monitored for this possibility and appropriate countermeasures taken as necessary.
- When a tranquilizer is used with fentanyl citrate, the following adverse reactions can occur: chills and/or shivering, restlessness, and postoperative hallucinatory episodes (sometimes associated with transient periods of mental depression); extrapyramidal symptoms (dystonia, akathisia, and oculogyric crisis) have been observed up to 24 hours postoperatively. When they occur, extrapyramidal symptoms can usually be controlled with anti-parkinson agents. Postoperative drowsiness is also frequently reported following the use of neuroleptics with fentanyl citrate.
- Cases of cardiac dysrhythmias, cardiac arrest, and death have been reported following the use of fentanyl citrate with a neuroleptic agent.
There is limited information regarding Postmarketing Experience of Fentanyl (injection) in the drug label.
- Other CNS depressant drugs (e.g. barbiturates, tranquilizers, narcotics and general anesthetics) will have additive or potentiating effects with fentanyl citrate. When patients have received such drugs, the dose of fentanyl citrate required will be less than usual. Following the administration of fentanyl citrate, the dose of other CNS depressant drugs should be reduced.
Use in Specific Populations
- Fentanyl citrate has been shown to impair fertility and to have an embryocidal effect in rats when given in doses 0.3 times the upper human dose for a period of 12 days. No evidence of teratogenic effects have been observed after administration of fentanyl citrate to rats. There are no adequate and well-controlled studies in pregnant women. Fentanyl citrate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
- Australian Drug Evaluation Committee (ADEC) Pregnancy Category
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Fentanyl (injection) in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Fentanyl (injection) during labor and delivery.
There is no FDA guidance on the use of Fentanyl (injection) with respect to nursing mothers.
- The safety and efficacy of fentanyl citrate in children under two years of age have not been established.
- Rare cases of unexplained clinically significant methemoglobinemia have been reported in premature neonates undergoing emergency anesthesia and surgery which included the combined use of fentanyl, pancuronium and atropine. A direct cause and effect relationship between the combined use of these drugs and the reported cases of methemoglobinemia has not been established.
There is no FDA guidance on the use of Fentanyl (injection) with respect to geriatric patients.
There is no FDA guidance on the use of Fentanyl (injection) with respect to specific gender populations.
There is no FDA guidance on the use of Fentanyl (injection) with respect to specific racial populations.
There is no FDA guidance on the use of Fentanyl (injection) in patients with renal impairment.
There is no FDA guidance on the use of Fentanyl (injection) in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Fentanyl (injection) in women of reproductive potentials and males.
There is no FDA guidance one the use of Fentanyl (injection) in patients who are immunocompromised.
Administration and Monitoring
There is limited information regarding Monitoring of Fentanyl (injection) in the drug label.
There is limited information regarding IV Compatibility of Fentanyl (injection) in the drug label.
- The manifestations of fentanyl citrate overdosage are an extension of its pharmacologic actions (see CLINICAL PHARMACOLOGY) as with other opioid analgesics. The intravenous LD50 of fentanyl citrate is 3 mg/kg in rats, 1 mg/kg in cats, 14 mg/kg in dogs and 0.03 mg/kg in monkeys.
- In the presence of hypoventilation or apnea, oxygen should be administered and respiration should be assisted or controlled as indicated. A patent airway must be maintained; an oropharyngeal airway or endotracheal tube might be indicated. If depressed respiration is associated with muscular rigidity, an intravenous neuromuscular blocking agent might be required to facilitate assisted or controlled respiration. The patient should be carefully observed for 24 hours; body warmth and adequate fluid intake should be maintained. If hypotension occurs and is severe or persists, the possibility of hypovolemia should be considered and managed with appropriate parenteral fluid therapy. A specific narcotic antagonist such as nalorphine, levallorphan or naloxone should be available for use as indicated to manage respiratory depression. This does not preclude the use of more immediate countermeasures. The duration of respiratory depression following overdosage of fentanyl citrate may be longer than the duration of narcotic antagonist action. Consult the package insert of the individual narcotic antagonists for details about use.
|Systematic (IUPAC) name|
|ATC code||N01 N02AB03 (WHO)|
|Mol. mass||336.471 g/mol|
|Melt. point||87.5 °C (190 °F)|
|Metabolism||hepatic, primarily by CYP3A4|
|Half life||(IV)= 10-20 mins (T1/2 β)|
2-4 hours (T1/2 ɣ)
Intranasal = 6.5 mins
Transdermal = 20–27 h
|Excretion||60% Urinary (metabolites, <10% unchanged drug)|
|Dependence Liability||Moderate – high|
|Routes||TD, IM, IV, oral transmucosal, sublingual, buccal|
Mechanism of Action
- Fentanyl is a pure opioid agonist whose principal therapeutic action is analgesia. Other members of the class known as opioid agonists include substances such as morphine, oxycodone, hydromorphone, codeine, and hydrocodone.
There is limited information regarding Pharmacodynamics of Fentanyl (injection) in the drug label.
- Fentanyl citrate is a narcotic analgesic. A dose of 100 mcg (0.1 mg) (2.0 ml) is approximately equivalent in analgesic activity to 10 mg of morphine or 75 mg of meperidine. The principal actions of therapeutic value are analgesia and sedation. Alterations in respiratory rate and alveolar ventilation, associated with narcotic analgesics, may last longer than the analgesic effect. As the dose of narcotic is increased, the decrease in pulmonary exchange becomes greater. Large doses may produce apnea. Fentanyl citrate appears to have less emetic activity than either morphine or meperidine. Histamine assays and skin wheal testing in man indicate that clinically significant histamine release rarely occurs with fentanyl citrate. Recent assays in man show no clinically significant histamine release in dosages up to 50 mcg/kg (0.05 mg/kg) (1 ml/kg). Fentanyl citrate preserves cardiac stability, and blunts stress-related hormonal changes at higher doses.
- The pharmacokinetics of fentanyl citrate can be described as a three-compartment model, with a distribution time of 1.7 minutes, redistribution of 13 minutes and a terminal elimination half-life of 219 minutes. The volume of distribution for fentanyl citrate is 4 L/kg.
- Fentanyl citrate plasma protein binding capacity decreases with increasing ionization of the drug. Alterations in pH may affect its distribution between plasma and the central nervous system. It accumulates in skeletal muscle and fat, and is released slowly into the blood. Fentanyl citrate, which is primarily transformed in the liver, demonstrates a high first pass clearance and releases approximately 75% of an intravenous dose in urine, mostly as metabolites with less than 10% representing the unchanged drug. Approximately 9% of the dose is recovered in the feces, primarily as metabolites.
- The onset of action of fentanyl citrate is almost immediate when the drug is given intravenously; however, the maximal analgesic and respiratory depressant effect may not be noted for several minutes. The usual duration of action of the analgesic effect is 30 to 60 minutes after a single intravenous dose of up to 100 mcg (0.1 mg) (2.0 ml). Following intramuscular administration, the onset of action is from seven to eight minutes, and the duration of action is one to two hours. As with longer acting narcotic analgesics, the duration of the respiratory depressant effect of fentanyl citrate may be longer than the analgesic effect. The following observations have been reported concerning altered respiratory response to CO2 stimulation following administration of fentanyl citrate to man.
- DIMINISHED SENSITIVITY TO CO2 STIMULATION MAY PERSIST LONGER THAN DEPRESSION OF RESPIRATORY RATE. (Altered sensitivity to CO2 stimulation has been demonstrated for up to four hours following a single dose of 600 mcg (0.6 mg) (12 ml) fentanyl citrate to healthy volunteers.) Fentanyl citrate frequently slows the respiratory rate, duration and degree of respiratory depression being dose related.
The peak respiratory depressant effect of a single intravenous dose of fentanyl citrate is noted 5 to 15 minutes following injection.
There is limited information regarding Nonclinical Toxicology of Fentanyl (injection) in the drug label.
There is limited information regarding Clinical Studies of Fentanyl (injection) in the drug label.
Store at 20° to 25°C (68° to 77°F)
Package and Label Display Panel
Patient Counseling Information
There is limited information regarding Patient Counseling Information of Fentanyl (injection) in the drug label.
Precautions with Alcohol
- Alcohol-Fentanyl (injection) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Look-Alike Drug Names
There is limited information regarding Fentanyl (injection) Look-Alike Drug Names in the drug label.
The contents of this FDA label are provided by the National Library of Medicine.