Fentanyl Transdermal System
Pronunciation: (FEN-ta-nil)
Class: Opioid analgesic
Trade Names
Duragesic-12
- Transdermal System 1.25 mg
Duragesic-25
- Transdermal System 2.5 mg
Duragesic-50
- Transdermal System 5 mg
Duragesic-75
- Transdermal System 7.5 mg
Duragesic-100
- Transdermal System 10 mg
ratio-Fentanyl (Canada)
Pharmacology
A potent opiate agonist that relieves pain by stimulating opiate receptors in CNS; also causes respiratory depression and peripheral vasodilation; inhibits intestinal peristalsis and sphincter of Oddi spasm; stimulates chemoreceptors that cause vomiting; increases bladder tone.
Pharmacokinetics
Absorption
T max is 24 to 72 h. C max is about 0.3 to 2.5 ng/mL (dose dependent).
Distribution
Vd is 6 L/kg.
Metabolism
Primarily metabolized by CYP-450 3A4.
Elimination
Half-life is 17 h after removal. Approximately 75% of an administered dose of fentanyl is excreted in the urine, primarily as metabolites. About 9% of the dose is recovered in the feces, mainly as metabolites.
Special Populations
ElderlyReduced Cl and terminal half-life is prolonged.
Indications and Usage
Management of persistent moderate to severe chronic pain that requires continuous opioid administration for a prolonged period of time and cannot be managed by other means.
Contraindications
Patients who are not opioid-tolerant; management of acute pain or in patients requiring opioid analgesia for short periods of time; management of postoperative pain (including out-patient or day surgeries); management of mild pain; management of intermittent pain; situations of considerable respiratory depression, especially in unmonitored settings without resuscitative equipment; patients with acute or severe bronchial asthma; patient with paralytic ileus; hypersensitivity to fentanyl or any component of the product.
Dosage and Administration
Persistent Moderate to Severe Chronic PainAdults and Children 2 y of age and older
Transdermal Calculate dose based on previous day's opiate requirements using manufacturer's conversion charts. Max pain relief does not occur until 24 h or more after application; a short-acting opiate may be needed for breakthrough pain. Initial dose can be increased after 3 days. Further dosage increases should occur at intervals of 6 days or more. Replace patches every 3 days; some patients require new patch every 2 days.
General Advice
- Hair at the application site should be clipped (not shaved) prior to application.
- Apply only to intact, nonirritated, and nonirradiated skin on a flat surface (eg, chest, back, flank, upper arm; in young children or people with cognitive impairment, place patch on the upper back to lower the chance that the patch will be removed and placed in the mouth).
- Apply patch immediately upon removal from the sealed package and after removal of the protective liner by pressing firmly in place with the palm of the hand for 30 sec, making sure the contact is complete, especially around the edges. After removal of the patch, apply the next patch to a different skin site.
- If the site of application must be cleansed prior to application, use clear water only (do not use soaps, oils, lotions, alcohol, or any other agents that might irritate the skin or alter its characteristics); allow to dry completely prior to patch application.
- To dispose of used patch, fold (so that the adhesive side adheres to itself) and immediately flush down the toilet.
- If accidental skin contact with the gel from the patch occurs, wash the area clean with clear water (do not use soap, alcohol, or other chemicals).
Storage/Stability
Store patches in foil packets at or below 77°F. Apply immediately after removal from sealed package. Do not use if seal is broken or the patch is damaged or altered in any way.
Drug Interactions
Alcohol, drugs of abusePossible additive CNS depressant effects.
AmiodaroneProfound bradycardia, sinus arrest, and hypotension may occur.
Barbiturate anesthetics, other CNS depressantsMay have additive effects. Reduce dosage of 1 or both agents.
MAOIsNot recommended for use in patients who have received MAOIs within 14 days.
Potent CYP3A4 inhibitors (eg, clarithromycin, diltiazem, erythromycin, ketoconazole, nefazodone, protease inhibitors [eg, ritonavir]), other CNS depressants (eg, alcohol, barbiturates, benzodiazepines, general anesthetics, other opioids, phenothiazines, sedating antihistamines, sedatives/hypnotics, skeletal muscle relaxants, tranquilizers)Increased depressant effects; hypoventilation, hypotension, profound sedation, and life-threatening respiratory depression may occur.
Adverse Reactions
Cardiovascular
Arrhythmias, chest pain, hypertension, syncope, tachycardia (at least 1%).
CNS
Asthenia, fatigue, headache, insomnia, nervousness, somnolence (3% to 10%); agitation, anxiety, confusion, convulsions, depression, dizziness, hallucinations, paranoid reaction, speech disorder, stupor, tremor (at least 10%).
Dermatologic
Sweating (at least 10%); application-site reaction, pruritus (3% to 10%); erythematous rash, increased sweating, localized skin reaction, rash (at least 1%).
EENT
Rhinitis (at least 10%); blurred vision (postmarketing).
GI
Constipation, dry mouth, nausea, vomiting (at least 10%); anorexia, diarrhea, dyspepsia (3% to 10%); flatulence (at least 1%).
Genitourinary
Urinary retention (3% to 10%); micturition disorder (at least 1%); anorgasmia, decreased libido, ejaculatory difficulty (postmarketing).
Local
Application-site reaction including edema, erythema, itching, papules (at least 1%).
Metabolic
Weight loss (postmarketing).
Musculoskeletal
Back pain, rigors (at least 1%).
Respiratory
Coughing, dyspnea, respiratory depression (at least 10%); apnea, hypoventilation (3% to 10%); bronchitis, hiccups, rhinitis, sinusitis, upper respiratory tract infection (at least 1%).
Miscellaneous
Abdominal pain, pain (3% to 10%); accidental injury, allergic reaction, fever, flushing, influenza-like symptoms (at least 1%); edema (postmarketing).
Precautions
WarningsOnly for chronic pain in patients who are already receiving continuous opioid therapy, are opioid tolerant, and cannot be managed by lesser means. Risk of potentially fatal hypoventilation contraindicates use in patients who are not opioid tolerant; acute, mild, or postoperative pain; patients who require opioid analgesia for a short period of time; intermittent pain. Concomitant use of fentanyl and potent CYP3A4 inhibitors may result in an increase in fentanyl plasma concentrations, which could increase or prolong adverse drug effects and cause fatal respiratory depression. Fentanyl transdermal system should only be used in children 2 y of age and older who are opioid tolerant. Fentanyl patches can be abused in a manner similar to other legal or illicit opioid agonists. Assess patients for clinical risk of opioid abuse or addiction. Use of damaged or cut patches can lead to rapid release of contents and absorption of a potentially fatal dose of fentanyl. |
MonitorMonitor patients who have experienced a serious adverse reaction, including overdose, for at least 24 h. |
Pregnancy
Category C .
Lactation
Excreted in breast milk.
Children
Safety and efficacy not established in children younger than 2 y of age.
Renal Function
Fentanyl is renally excreted. Use with caution.
Hepatic Function
Fentanyl is hepatically metabolized. Use with caution.
Special Risk Patients
Use with caution in elderly, debilitated, or cachetic patients or patients with myxedema, acute alcoholism, acute abdominal conditions, biliary tract disease (including acute pancreatitis), ulcerative colitis, head injury or increased intracranial pressure, brain tumors, supraventricular tachycardia, depleted blood volume, or circulatory shock.
Hazardous Tasks
May impair physical or mental abilities required to perform potentially dangerous tasks.
Cardiac disease
May cause bradycardia. Use with caution in patients with bradyarrhythmias.
Drug dependence
Fentanyl has abuse potential.
Exposure to external heat
Direct contact with heating pads, electric blankets, saunas, or hot tubs could increase fentanyl absorption.
Fever
May increase absorption of fentanyl; monitor for adverse reactions.
Respiratory depression
Serious or life-threatening hypoventilation may occur, especially during the initial 24 to 72 h and following increases in dose. Use with extreme caution in patients with COPD or cor pulmonale, or in patients having a substantially decreased respiratory reserve, hypoxia, hypercapnia, or preexisting respiratory depression.
Tolerance
May occur.
Overdosage
Symptoms
Cardiopulmonary arrest, circulatory collapse, CNS depression, death, hypoventilation, miosis, respiratory depression, seizures.
Patient Information
- Caution patient or caregiver that medication may impair mental and/or physical abilities required for the performance of potentially hazardous tasks (eg, driving, operating machinery) and to use caution until tolerance is determined.
- Caution patient or caregiver to avoid alcohol and other depressants (eg, sleep medications, tranquilizers) because dangerous additive effects may occur, resulting in serious injury or death.
- Remind patient or caregiver that fentanyl is a medication with high potential for abuse and to protect the systems from theft or misuse in the work or home environment.
- Warn patient or caregiver that transdermal system should never be used by anyone other than the individual for whom it was prescribed because of the risk of death or other serious medical problems.
- Caution patient or caregiver that medication can cause severe constipation and to use stool softeners, dietary fiber, and adequate fluids. Advise patient or caregiver to notify health care provider if severe constipation develops.
- Caution patient or caregiver to notify health care provider if a high fever develops because there is a potential for temperature-dependent increase in fentanyl release from the system that could result in fentanyl overdose.
- Advise patient that patches contain fentanyl, a potent opioid pain medicine similar to morphine, hydromorphone, methadone, oxycodone, and oxymorphone.
- Advise patient or caregiver that each patch may be worn continuously for 72 h before removal and to apply the replacement patch to a different skin site.
- Ensure patient or caregiver understands how to apply patch: apply only to intact, nonirritated, and nonirradiated skin on a flat surface (eg, back, chest, flank, upper arm). In young children or people with cognitive impairment, secure the patch on the upper back to lower the chance that it will be removed and placed in the mouth. Hair at the application site should be clipped (not shaved) prior to patch application; if the site of application must be cleansed prior to application of the patch, do so with clear water (do not use soaps, oils, lotions, alcohol, or any other agents that might irritate the skin or alter its characteristics) and allow to dry completely prior to patch application; apply patch immediately upon removal from the sealed package and after removal of the protective liner by pressing firmly in place with the palm of the hand for 30 sec, making sure the contact is complete, especially around the edges. Caution patient not to fold the patch so that only part of the patch is exposed.
- Caution patient or caregiver not to apply the patch if the seal is broken, or if the patch is altered, cut, or damaged in any way. Advise patient that this could lead to the rapid release and absorption of the contents of the patch resulting in serious side effects or death.
- Caution patient or caregiver to avoid exposing the application site to direct external heat sources (eg, heating pads, electric blankets, heat lamps, saunas, hot tubs, heated water beds) while wearing the patch.
- Instruct patient or caregiver that if the gel from the patch accidentally contacts the skin, to wash the area with clear water. Soap, alcohol, or other chemicals should not be used because these products may increase the ability of fentanyl to go through the skin.
- Caution patient or caregiver not to change the dose or stop using unless advised by health care provider. Advise patient that suddenly stopping therapy after long-term use could cause narcotic withdrawal symptoms and that the dose will usually be slowly reduced if therapy needs to be discontinued.
- Caution patient or caregiver to keep patches in a safe place out of the reach of children because of the high risk of fatal respiratory depression.
- Instruct patient or caregiver that when patches are either used or no longer needed, to remove the used patch from the skin or the unused patches from their pouches, fold so that the adhesive side of the patch adheres to itself, and flush down the toilet.
Copyright © 2009 Wolters Kluwer Health.
