Dosing and uses of Sublimaze (fentanyl)
Adult dosage forms and strengths
injection solution: Schedule II
- 0.05mg/mL
Surgery Premedication
50-100 mcg/dose IM or slow IV 30-60 min prior to surgery
Adjunct to regional anesthesia: 25-100 mcg/dose slow IV over 1-2 min
General Anesthesia
Minor surgical procedures: 0.5-2 mcg/kg/dose IV
Major surgery: 2-20 mcg/kg/dose initially; 1-2 mcg/kg/hr maintenance infusion IV; discontinue infusion 30-60 min prior to end of surgery; limit total fentanyl doses to 10-15 mcg/kg for fast tracking and early extubation
Adjunct to general anesthesia (rarely used): 20-50 mcg/kg/dose IV
Analgesia (Off-label)
Analgesia: 1-2 mcg/kg IV bolus or 25-100 mcg/dose PRN or 1-2 mcg/kg/hr by continuous IV infusion or 25-200 mcg/hr
Severe pain: 50-100 mcg/dose IV/IM q1-2hr PRN (patients with prior opioid exposure may tolerate higher initial doses)
Patient controlled anesthesia (PCA): 10 mcg/mL IV (usual concentration); 20 mcg demand dose with 5-10 min lockout time interval and base rate of ≤50mcg/hr
Pediatric dosage forms and strengths
injection solution: Schedule II
- 0.05mg/mL
Surgery Premedication (Off-label)
1-12 years: 0.5-2 mcg/kg IV given 3 min prior to procedure; may repeat q1-2hr
>12 years: 0.5-2 mcg/kg/dose; not to exceed 50 mcg/dose; give 3 min prior to procedure; may repeate in 5 min if necessary; if more than two doses needed, may repeat up to 5 times at 25 mcg/dose maximum
Continuous Sedation/Analgesia
0.5-2 mcg/kg/hr; titrate to desired effect
Adjunct Anesthesia
<2 years: Safety and efficacy not established
>2 years: 2-3 mcg/kg IV/IM q1-2hr PRn
Geriatric dosage forms and strengths
Elderly patients are twice as sensitive to effects of fentanyl as young patients are; take into account weight and physical status when administering the drug
Sublimaze (fentanyl) adverse (side) effects
Frequency not defined
Asthenia
Confusion
Constipation
Dry mouth
Nausea
Somnolence
Sweating
Vomiting
Abdominal pain
Anorexia
Anxiety
Apnea
Depression
Diarrhea
Dizziness
Dyspepsia
Dyspnea
Euphoria
Fatigue
Hallucinations
Headache
Hemoptysis
Hypoventilation
Influenzalike symptoms
Nervousness
Pharyngitis
Pruritus
Upper respiratory tract infection
Urinary retention
Abnormal coordination, thinking, gait, dreams
Accidental injury
Agitation
Amnesia
Angina pectoris
Application-site reaction
Back pain
Bradycardia
Bronchitis
Cardiac arrest
Coma
Dysphoria
Faintness
Fever
Flatulence
Flushing
Hiccups
Mental clouding
Micturition disorder
Myocardial infarction (MI)
Oliguria
Paranoid reaction
Paresthesia
QT-interval prolongation
Rash
Respiratory arrest
Respiratory/circulatory depression
Rhinitis
Sedation
Seizures
Severe cardiac arrhythmias
Shock Sinusitis
Speech disorder
ST-segment elevation
Sweating
Syncope
Tremor
Urinary retention
Ventricular tachycardia
Visual disturbances
Warmness of face/neck/upper thorax, urticaria
Weakness
Warnings
Contraindications
Hypersensitivity
Within 2 weeks of monoamine oxidase inhibitor (MAOI) use
Cautions
Caution in acute pancreatitis, Addison disease, benign prostatic hyperplasia, cardiac arrhythmias, central nervous system (CNS) depression, drug abuse or dependence, emotional lability, gallbladder disease, gastrointestinal (GI) disorder, pseudomembranous colitis, GI surgery, head injury, hypothyroidism or untreated myxedema, intracranial hypertension, brain tumor, toxic psychosis, urethral stricture, urinary tract surgery, seizures, acute alcoholism, delirium tremens, shock, cor pulmonale, chronic pulmonary disease, emphysema, hypercapnia, kyphoscoliosis, severe obesity, renal or hepatic impairment, elderly or debilitated patients
Concurrent administration of benzodiazepine or neuromuscular blocker will decrease chest wall rigidity
Caution in toxin-mediated diarrhea (until toxins are cleared), paralytic ileus, respiratory depression, acute/severe bronchial asthma
Risks of potentially fatal respiratory depression, pruritus (despite little histamine release), and abuse or addiction
May produce bradycardia, which may be treated with atropine
Can produce drug dependence
Safety and efficacy in children not established
Pregnancy and lactation
Pregnancy category: C
Lactation: Drug enters breast milk; use not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Sublimaze (fentanyl)
Mechanism of action
Narcotic agonist-analgesic of opiate receptors; inhibits ascending pain pathways, thus altering response to pain; increases pain threshold; produces analgesia, respiratory depression, and sedation
Absorption
Bioavailability: 50%
Onset: IV, immediate; IM, 7-15 min
Duration: IV, 0.5-1 hr; IM, 1-2 hr
Peak plasma time: IV (≤100 mcg), 30-60 min; IM, 1-2 hr
Concentration: 0.2-2 ng/mL (adverse effects occur at >2 ng/mL)
Distribution
Protein bound: 80-85%
Vd: 4-6 L/kg
Metabolism
Metabolized in liver by CYP3A4
Elimination
Half-life: 2-4 hr
Total plasma clearance: 8.3 mL/min/kg
Excretion: Urine (75%), feces (9%)
Administration
IV Incompatibilities
Additive: Fluorouracil, lidocaine(?), methohexital, pentobarbital, thiopentaL
Syringe: Methohexital, pentobarbital, thiopentaL
Y-site: Azithromycin, methohexital(?), phenytoin, pentobarbital(?), thiopental(?)
IV Compatibilities
Solution: D5W, Ns
Additive: Bupivacaine, bupivacaine-clonidine, ropivacaine
Syringe (partial list): Atropine, chlorpromazine, dimenhydrinate, diphenhydramine, heparin, hydroxyzine, meperidine, metoclopramide, midazolam, morphine, ondansetron, prochlorperazine, promethazine, ranitidine
Y-site (partial list): Amiodarone, amphotericin B cholesteryl sulfate, atropine, bivalirudin, dexamethasone sodium phosphate, diazepam, diltiazem, diphenhydamine, dobutamine, dopamine, epinephrine, esmolol, furosemide, haloperidol, heparin, hydrocortisone, labetalol, lorazepam, metoclopramide, midazolam, morphine, nitroglycerin, norepinephrine, potassium chloride, propofol, vitamins B and C
IV Preparation
Use undiluted or diluted in 250 mL of D5W
IV/IM Administration
IM: Injection
IV: Injection or continuous infusion
