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Fentanyl
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Restrictions
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(FEN ta nil)

U.S. Brand Names
Actiq® Oral Transmucosal; Duragesic® Transdermal; Fentanyl Oralet®; Sublimaze® Injection

Generic Available

No


Synonyms
Fentanyl Citrate

Pharmacological Index

Analgesic, Narcotic; General Anesthetic


Use

Dental: Adjunct in preoperative intravenous conscious sedation in patients undergoing dental surgery

Medical: Sedation, relief of pain, preoperative medication, adjunct to general or regional anesthesia, management of chronic pain (transdermal product)


Restrictions

C-II


Pregnancy Risk Factor

B/D (if used for prolonged periods or in high doses at term)


Contraindications

Hypersensitivity to fentanyl or any component; increased intracranial pressure; severe respiratory depression; severe liver or renal insufficiency


Warnings/Precautions

Fentanyl shares the toxic potentials of opiate agonists, and precautions of opiate agonist therapy should be observed; use with caution in patients with bradycardia; rapid I.V. infusion may result in skeletal muscle and chest wall rigidity impaired ventilation respiratory distress apnea, bronchoconstriction, laryngospasm; inject slowly over 3-5 minutes; nondepolarizing skeletal muscle relaxant may be required. Tolerance of drug dependence may result from extended use.

Topical patches: Serum fentanyl concentrations may increase approximately one-third for patients with a body temperature of 40°C secondary to a temperature-dependent increase in fentanyl release from the system and increased skin permeability. Patients who experience adverse reactions should be monitored for at least 12 hours after removal of the patch.

The elderly may be particularly susceptible to the CNS depressant and constipating effects of narcotics


Adverse Reactions

>10%:

Cardiovascular: Hypotension, bradycardia

Central nervous system: CNS depression, drowsiness, sedation

Gastrointestinal: Nausea, vomiting, constipation

Respiratory: Respiratory depression

1% to 10%:

Cardiovascular: Cardiac arrhythmias, orthostatic hypotension

Central nervous system: Confusion

Gastrointestinal: Biliary tract spasm

Ocular: Miosis

<1%: Circulatory depression, convulsions, dysesthesia, paradoxical CNS excitation or delirium; cold, clammy skin; dizziness, erythema, pruritus, rash, urticaria, itching, ADH release, urinary tract spasm, bronchospasm, laryngospasm, physical and psychological dependence with prolonged use


Overdosage/Toxicology

Symptoms of overdose include CNS depression, respiratory depression, miosis

Treatment of an overdose includes support of the patient's airway, establishment of an I.V. line, and administration of naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg


Drug Interactions

CYP3A3/4 enzyme substrate


Stability

Protect from light; incompatible when mixed in the same syringe with pentobarbital


Mechanism of Action

Binds with stereospecific receptors at many sites within the CNS, increases pain threshold, alters pain reception, inhibits ascending pain pathways


Pharmacodynamics/Kinetics

Respiratory depressant effect may last longer than analgesic effect

I.V.: Onset of analgesia: Almost immediate; Duration: 0.5-1 hour

Transmucosal:

Onset of effect: 5-15 minutes with a maximum reduction in activity/apprehension

Peak analgesia: Within 20-30 minutes

Duration: Related to blood level of the drug

Absorption: Transmucosal: Rapid, ~25% from the buccal mucosa; 75% swallowed with saliva and slowly absorbed from gastrointestinal tract

Distribution: Highly lipophilic, redistributes into muscle and fat

Metabolism: In the liver

Bioavailability: Transmucosal: ~50% (range: 36% to 71%)

Half-life: 2-4 hours

Transmucosal: 6.6 hours (range: 5-15 hours)

Elimination: In urine primarily as metabolites and 10% as unchanged drug


Usual Dosage

Doses should be titrated to appropriate effects; wide range of doses, dependent upon desired degree of analgesia/anesthesia

Sedation for minor procedures/analgesia:

I.M., I.V.: 1-2 mcg/kg/dose; may repeat at 30- to 60-minute intervals. Note: Children 18-36 months of age may require 2-3 mcg/kg/dose

Transmucosal (dosage strength is based on patient weight): 5 mcg/kg if child is not fearful; fearful children and some younger children may require doses of 5-15 mcg/kg (which also carries an increased risk of hypoventilation); drug effect begins within 10 minutes, with sedation beginning shortly thereafter

Continuous sedation/analgesia: Initial I.V. bolus: 1-2 mcg/kg then 1 mcg/kg/hour; titrate upward; usual: 1-3 mcg/kg/hour

Pain control: Transdermal: Not recommended

Children >12 years and Adults:

Sedation for minor procedures/analgesia:

I.M., I.V.: 0.5-1 mcg/kg/dose; higher doses are used for major procedures

Transmucosal: 5 mcg/kg, suck on lozenge vigorously approximately 20-40 minutes before the start of procedure, drug effect begins within 10 minutes, with sedation beginning shortly thereafter.

Dosage recommendations for transmucosal fentanyl (Oralet®) based on patient age/weight:

Children <2 years of age OR <10 kg: CONTRAINDICATED

10 kg: 5-10 mcg/kg/dose (100 mcg): 10-15 mcg/kg/dose (100 mcg)

15 kg: 5-10 mcg/kg/dose (100 mcg): 10-15 mcg/kg/dose (200 mcg)

20 kg: 5-10 mcg/kg/dose (100 or 200 mcg): 10-15 mcg/kg/dose (200 or 300 mcg)

25 kg: 5-10 mcg/kg/dose (200 mcg): 10-15 mcg/kg/dose (300 mcg)

30 kg: 5-10 mcg/kg/dose (300 mcg): 10-15 mcg/kg/dose (300 or 400 mcg)

35 kg: 5-10 mcg/kg/dose (300 mcg): 10-15 mcg/kg/dose (400 mcg)

greater than or equal to 40 kg; 5-10 mcg/dose (400 mcg): 10-15 mcg/dose (400 mcg)

Adult dose: 400 mcg

Preoperative sedation, adjunct to regional anesthesia, postoperative pain: I.M., I.V.: 50-100 mcg/dose

Adjunct to general anesthesia: I.M., I.V.: 2-50 mcg/kg

General anesthesia without additional anesthetic agents: I.V. 50-100 mcg/kg with O2 and skeletal muscle relaxant

Pain control: Transdermal: Initial: 25 mcg/hour system; if currently receiving opiates, convert to fentanyl equivalent and administer equianalgesic dosage titrated to minimize the adverse effects and provide analgesia. To convert patients from oral or parenteral opioids to Duragesic®, the previous 24-hour analgesic requirement should be calculated. This analgesic requirement should be converted to the equianalgesic oral morphine dose.

Equianalgesic doses of opioid agonists*:

Codeine: 130 mg I.M.; 200 mg oral

Hydromorphone: 1.5 mg I.M.; 7.5 mg oral

Levorphanol: 2 mg I.M.; 4 mg oral

Meperidine: 75 mg I.M.

Methadone: 10 mg I.M.; 20 mg oral

Morphine: 10 mg I.M.; 60 mg oral

Oxycodone: 15 mg I.M.; 30 mg oral

Oxymorphone: 1 mg I.M.; 10 mg rectal

*From N Engl J Med, 1985, 313:84-95.

Corresponding doses of oral/intramuscular morphine and Duragesic™*:

45-134 mg morphine oral/24 hours = 8-22 mg morphine I.M./24 hours = 25 mcg/hour Duragesic™

135-224 mg morphine oral/24 hours = 28-37 mg morphine I.M./24 hours = 50 mcg/hour Duragesic™

225-314 mg morphine oral/24 hours = 38-52 mg morphine I.M./24 hours = 75 mcg/hour Duragesic™

315-404 mg morphine oral/24 hours = 53-67 mg morphine I.M./24 hours = 100 mcg/hour Duragesic™

405-494 mg morphine oral/24 hours = 68-82 mg morphine I.M./24 hours = 125 mcg/hour Duragesic™

495-584 mg morphine oral/24 hours = 83-97 mg morphine I.M./24 hours = 150 mcg/hour Duragesic™

585-674 mg morphine oral/24 hours = 98-112 mg morphine I.M./24 hours = 175 mcg/hour Duragesic™

675-764 mg morphine oral/24 hours = 113-127 mg morphine I.M./24 hours = 200 mcg/hour Duragesic™

765-854 mg morphine oral/24 hours = 128-142 mg morphine I.M./24 hours = 225 mcg/hour Duragesic™

855-944 mg morphine oral/24 hours = 143-157 mg morphine I.M./24 hours = 250 mcg/hour Duragesic™

945-1034 mg morphine oral/24 hours = 158-172 mg morphine I.M./24 hours = 275 mcg/hour Duragesic™

1035-1124 mg morphine oral/24 hours = 173-187 mg morphine I.M./24 hours = 300 mcg/hour Duragesic™

*Product information, Duragesic™ - Janssen Pharmaceutica, January, 1991.

The dosage should not be titrated more frequently than every 3 days after the initial dose or every 6 days thereafter. The majority of patients are controlled on every 72-hour administration, however, a small number of patients require every 48-hour administration.

Elderly >65 years: Transmucosal: Dose should be reduced to 2.5-5 mcg/kg; elderly have been found to be twice as sensitive as younger patients to the effects of fentanyl

Dosing adjustment in renal impairment:

Clcr 10-50 mL/minute: Administer at 75% of normal dose

Clcr <10 mL/minute: Administer at 50% of normal dose


Dietary Considerations

Alcohol: Additive CNS effects, avoid or limit alcohol; watch for sedation

Food: Glucose may cause hyperglycemia; monitor blood glucose concentrations


Monitoring Parameters

Respiratory and cardiovascular status, blood pressure, heart rate


Mental Health: Effects on Mental Status

Drowsiness, sedation, and depression are common; may rarely cause paradoxical CNS excitement or delirium


Mental Health: Effects on Psychiatric Treatment

Concurrent use with low potency antipsychotics and TCAs may produce additive hypotension


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

While using this medication, do not use alcohol and other prescription or OTC medications (especially sedatives, tranquilizers, antihistamines, or pain medications) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). May cause hypotension, dizziness, drowsiness, impaired coordination, or blurred vision (use caution when driving, climbing stairs, or changing position - rising from sitting or lying to standing, or when engaging in tasks requiring alertness until response to drug is known); nausea or vomiting (frequent mouth care, small frequent meals, chewing gum, or sucking lozenges may help); constipation (increased exercise, fluids, or dietary fruit and fiber may help - if constipation remains an unresolved problem, consult prescriber about use of stool softeners). Report acute dizziness, chest pain, slow or rapid heartbeat, acute headache; confusion or changes in mentation; changes in voiding frequency or amount, swelling of extremities, or unusual weight gain; shortness of breath or difficulty breathing; or changes in vision. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.


Nursing Implications

May cause rebound respiratory depression postoperatively

Patients with increased temperature may have increased fentanyl absorption transdermally, observe for adverse effects, dosage adjustment may be needed

Pharmacologic and adverse effects can be seen after discontinuation of transdermal system, observe patients for at least 12 hours after transdermal product removed; keep transdermal product (both used and unused) out of the reach of children

Do not use soap, alcohol, or other solvents to remove transdermal gel if it accidentally touches skin as they may increase transdermal absorption, use copious amounts of water. For patients who have received transmucosal product within 6-12 hours, it is recommended that if other narcotics are required, they should be used at starting doses 1/4 to 1/3 those usually recommended.


Dosage Forms

Injection, as citrate: 0.05 mg/mL (2 mL, 5 mL, 10 mL, 20 mL, 50 mL)

Lozenge, oral transmucosal (raspberry flavored):

Fentanyl Oralet®: 100 mcg, 200 mcg, 300 mcg, 400 mcg, 600 mcg, 800 mcg, 1200 mcg, 1600 mcg

Actiq®: 100 mcg, 200 mcg, 300 mcg, 400 mcg

Transdermal system: 25 mcg/hour [10 cm2]; 50 mcg/hour [20 cm2]; 75 mcg/hour [30 cm2]; 100 mcg/hour [40 cm2] (all available in 5s)


References

Baraka A, "Fentanyl-Induced Laryngospasm Following Tracheal Extubation in a Child," Anaesthesia, 1995, 50(4):375.

Bedforth NM and Lockey DJ, "Raynaud's Syndrome Following Intravenous Induction of Anaesthesia," Anaesthesia, 1995, 50(3):248-9.

Billmire DA, Neale HW, and Gregory RO, "Use of I.V. Fentanyl in the Outpatient Treatment of Pediatric Facial Trauma," J Trauma, 1985, 25(11):1079-80.

Chaturvedi AK, Rao NG, and Baird JR, "A Death Due to Self-Administered Fentanyl," J Anal Toxicol, 1990, 14(6):385-7.

"Drugs for Pain," Med Lett Drugs Ther, 1998, 40(1033):79-84.

Fine PG, "Fentanyl in the Treatment of Cancer Pain," Semin Oncol, 1997, 24(5 Suppl 16):S16-20-7.

Furuya H and Okumura F, "Hemolysis After Administration of High Dose Fentanyl," Anesth Analg, 1986, 65(2):207-8.

Jeal W and Benfield P, "Transdermal Fentanyl. A Review of Its Pharmacological Properties and Therapeutic Efficacy in Pain Control," Drugs, 1997, 53(1):109-38.

Katz R, Kelly HW, and Hsi A, "Prospective Study on the Occurrence of Withdrawal in Critically Ill Children Who Receive Fentanyl by Continuous Infusion," Crit Care Med, 1994, 22(5):763-7.

Leuschen MP, Willett LD, Hoie EB, et al, "Plasma Fentanyl Levels in Infants Undergoing Extracorporeal Membrane Oxygenation," J Thorac Cardiovasc Surg, 1993, 105(5):885-91.

Maurer PM and Bartkowski RR, "Drug Interactions of Clinical Significance With Opiad Analgesics," Drug Saf, 1993, 8(1):30-48.

Poklis A, "Fentanyl: A Review for Clinical and Analytical Toxicologists," J Toxicol Clin Toxicol, 1995, 33(5):439-47.

Roth B, Schlunder C, Houben F, et al, "Analgesia and Sedation in Neonatal Intensive Care Using Fentanyl by Continuous Infusion," Dev Pharmacol Ther, 1991, 17(3-4):121-7.

Schechter NL, Weisman SJ, Rosenblum M, et al, "The Use of Oral Transmucosal Fentanyl Citrate for Painful Procedures in Children," Pediatrics, 1995, 95(3):335-9.

Scholz J, Steinfath M, and Schulz M, "Clinical Pharmacokinetics of Alfentanil, Fentanyl, and Sufentanil. An Update," Clin Pharmacokinet, 1996, 31(4):275-92.

Stoukides CA and Stegman M, "Diffuse Rash Associated With Transdermal Fentanyl," Clin Pharm, 1992, 11(3):222.

Zeltzer LK, Altman A, Cohen D, et al, "Report of the Subcommittee on the Management of Pain Associated With Procedures in Children With Cancer," Pediatrics, 1990, 86(5 Pt 2):826-31.


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