1. Onset of action: (Analgesic) 6 hours
2. Duration: Related to blood level; some effects may last 72 to 96 hours due to extended half-life and absorption from the skin, fentanyl concentrations decrease by ~50% in 20 to 27 hours
3. Distribution: Highly lipophilic, redistributes into muscle and fat
4. Metabolism: Hepatic, primarily via CYP3A4 by N-dealkylation (to norfentanyl) and hydroxylation to other inactive metabolites
5. Half-life elimination: 20 to 27 hours (apparent half-life is influenced by continued fentanyl absorption from skin)
6. Time to peak: 20 to 72 hours; steady state serum concentrations are reached after two sequential 72-hour applications
7. Excretion: Urine 75% (primarily as metabolites, <7% to 10% as unchanged drug); feces ~9%
禁忌症
1. Hypersensitivity (eg, anaphylaxis, hypersensitivity) to fentanyl or any component of the formulation.
2. Patients requiring short-term therapy, management of acute or intermittent pain, postoperative or mild pain.
3. Other: Significant respiratory depression; gastrointestinal obstruction, including paralytic ileus; patients who are not opioid tolerant.
懷孕分類
Prolonged use of fentanyl during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated. If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available.
哺乳分類
When opioids are needed in breastfeeding women, the lowest effective dose for the shortest duration of time should be used to limit adverse events
1. To convert from oral or parenteral opioids, a 24-hour analgesic requirement should be calculated. Dosing conversion strategy based on a 2:1 ratio of oral morphine to transdermal fentanyl.
2. Change patch every 72 hours.
3. Do not titrate more frequently than every 3 days after the initial application or every 6 days thereafter.
小兒調整劑量
腎功能調整劑量
1. CrCl >50 mL/minute: No dosage adjustment necessary.
2. CrCl 10-50 mL/minute: (Initial) 75% of normal dose.
3. CrCl <10 mL/minute, dialysis: (Initial) 50% of normal dose.
肝功能調整劑量
1. Mild to moderate impairment: Reduce dose by 50%.
2. Severe impairment: Use not recommended.