鴉片類止痛 Severe pain, surgical analgesia & Anesthesia
藥理
Fentanyl citrate is a narcotic analgesic. A dose of 100 mcg (0.1 mg) 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.
藥動學
Absorption:
1.Onset of action: (IM) 7 to 8 minutes; (IV) Almost immediate
2. Duration: (IM) 1 to 2 hours; (IV) 0.5 to 1 hour Distribution:
1. Highly lipophilic, redistributes into muscle and fat
2. Vdss: (Children) ~15 L/kg; (Adults) 4 to 6 L/kg
3. Protein binding: 79% to 87%, primarily to alpha-1 acid glycoprotein; also binds to albumin and erythrocytes Metabolism:
Hepatic, primarily via CYP3A4 by N-dealkylation (to norfentanyl) and hydroxylation to other inactive metabolites Excretion:
Urine 75% (primarily as metabolites, <7% to 10% as unchanged drug); feces ~9%
禁忌症
1. Hypersensitivity to fentanyl or any component of the formulation
2. Known or suspected mechanical GI obstruction (eg, bowel obstruction, strictures) or any diseases/conditions that affect bowel transit (eg, ileus of any type)
3. Severe CNS depression, hemorrhage or shock
4. Concurrent use or use within 14 days of a monoamine oxidase inhibitor (MAOI)
Acute postoperative pain:
1. IV: 25 to 50 mcg every 5 minutes (moderate pain) or 50 to 100 mcg every 2 to 5 minutes (severe pain)
2. IM: 50 to 100 mcg every 1 to 2 hours as needed Note: IM route should only be used if IV administration is not available. Acute nonoperative severe pain:
IV, IM: 25 to 50 mcg or 0.35 to 0.5 mcg/kg every 30 to 60 minutes as needed Procedural sedation and analgesia:
Usual initial dose range: 0.5 to 2 mcg/kg, administered in incremental boluses of 25 to 50 mcg, titrated to effect. When used in combination with a sedative (eg, midazolam), consider dosage reduction. General anesthesia:
1. Induction: IV 25 to 100 mcg (or 0.5 to 1 mcg/kg)
2. Maintenance: 25 to 50 mcg bolus as needed OR Continuous infusion 1 to 2 mcg/kg/hour
小兒調整劑量
腎功能調整劑量
1. CrCl <50 mL/minute: No dosage adjustment necessary when single or infrequent bolus doses are used for short interventional procedures
2. Dialysis, Peritoneal dialysis, CRRT: Use lowest effective dose with gradual titration and close monitoring of response and adverse effects
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling; use with caution.