Dosing & Uses
Dosage Forms & Strengths
injectable solution: Schedule II
- 0.5mg/mL
Dose should be calculated based on ideal body weight
Incremental Injection: Anesthesia <30 Minutes
Maintenance: 3-5 mcg/kg IV increments q5-20min, or 0.5-1 mcg/kg/min IV
Total dose: 8-40 mcg/kg IV
Incremental Injection: Anesthesia 30-60 Minutes
Maintenance: 5-15 mcg/kg IV increments q5-20min
Total dose: Up to 75 mcg/kg IV
Anesthetic Induction: Anesthesia >45 Minutes
Maintenance: 0.5-1.5 mcg/kg/min IV or other general anesthetic
Total dose: depends on duration of operation
Continuous Infusion: For Anesthesia >45 Minutes
Maintenance: 0.5-3 mcg/kg/min IV
Total dose: depends on duration of operation
Postherpetic Neuralgia (Orphan)
Management of postherpetic neuralgia
Orphan indication sponsor
- Cinergen, LLC; 146 Medinah Drive; Blue Bell, PA 19422-3212
HIV-Associated Neuropathy (Orphan)
Treatment of painful HIV-associated neuropathy
Orphan indication sponsor
- Cinergen, LLC; 146 Medinah Drive; Blue Bell, PA 19422-3212
Administration
Total dose: depends on duration of operation
Dosage Forms & Strengths
injectable solution: Schedule II
- 0.5mg/mL
Dose should be calculated based on ideal body weight
<12 years
Anesthesia
- Not recommended
>12 years
Incremental Injection: Anesthesia <30 Minutes
- Induction: 8-20 mcg/kg IV
- Maintenance: 3-5 mcg/kg IV increments q5-20min, or 0.5-1 mcg/kg/min IV
- Total dose: 8-40 mcg/kg IV
Incremental Injection: Anesthesia 30-60 Minutes
- Induction: 20-50 mcg/kg IV
- Maintenance: 5-15 mcg/kg IV increments q5-20min
- Total dose: Up to 75 mcg/kg IV
Anesthetic Induction: Anesthesia >45 Minutes
- Induction: 130-245 mcg/kg IV
- Maintenance: 0.5-1.5 mcg/kg/min IV or other general anesthetic
- Total dose: depends on duration of operation
Continuous Infusion: For Anesthesia >45 Minutes
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Arrhythmia (14%)
Bradycardia (14%)
Chest wall rigidity (17%)
Hypertension (18%)
Nausea (28%)
Vomiting (18%)
Tachycardia (12%)
1-10%
Apnea (3-9%)
Blurred vision (1-3%)
Dizziness (3-9%)
Hypotension (10%)
Post-op respiratory depression (1-3%)
Skeletal muscle movements (3-9%)
Postoperative sedation (1-3%)
<1%
Sweating, flushing
Warmness of the face/neck/upper thorax
Pruritus
urticaria
Respiratory (undefined)
Respiratory/circulatory depression
Respiratory arrest
Shock
Cardiac arrest
Nervous System (undefined)
Dizziness
Visual disturbances
Mental clouding/depression
Sedation
Coma
Euphoria
Dysphoria
Weakness
Faintness
Agitation
Restlessness
Nervousness
Seizures
GI (undefined)
Nausea
Vomiting
Constipation
Cardiovascular (undefined)
QT-interval prolongation
Severe cardiac arrhythmias
Cardiac arrest
ST segment elevation
VTach
MI
Angina pectoris
Syncope
Genitourinary (undefined)
Urinary retention
Oliguria
Cholinergic (undefined)
Bradycardia
Dry mouth
Palpitation
Tachycardia
Warnings
Black Box Warnings
Therapy exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death; assess each patient’s risk prior to prescribing therapy, and monitor all patients regularly for the development of these behaviors and conditions
Contraindications
Hypersensitivity
Increased intracranial pressure
Severe respiratory depresssion
Cautions
Use caution in bradycardia, compromised cardiac reserve, head injury, hypothyroidism, increased ICP, intracranial lesions, renal impairment, respiratory impairment, obesicty, history of drug abuse
Concurrent administration of benzodiazepine or neuromuscular blocker will decrease chest wall rigidity
Should be administered by trained individuals
In patients who may be susceptible to intracranial effects of CO2 retention (e.g., those with evidence of increased intracranial pressure or brain tumors), therapy may reduce respiratory drive, and resultant CO2 retention can further increase intracranial pressure; monitor such patients for signs of sedation and respiratory depression, particularly when initiating therapy; opioids may obscure clinical course in a patient with a head injury; avoid the use in patients with impaired consciousness or coma
May cause spasm of sphincter of Oddi; opioids may cause increases in serum amylase; monitor patients with biliary tract disease, including acute pancreatitis, for worsening symptoms
Therapy may increase frequency of seizures in patients with seizure disorders and in other clinical settings associated with seizures; monitor patients for worsened seizure control during therapy
Life-threatening respiratory depression is more likely to occur in elderly, cachectic, or debilitated patients because they may have altered pharmacokinetics or altered clearance compared to younger, healthier patients; monitor closely
Profound sedation, respiratory depression, coma, and death may result from concomitant administration with benzodiazepines or other CNS depressants (e.g., non-benzodiazepine sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opioids, alcohol); because of these risks, reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate
Opioids can cause sleep-related breathing disorders including central sleep apnea (CSA) and sleep-related hypoxemia; opioid use increases risk of CSA in a dose-dependent fashion; in patients who present with CSA, consider decreasing opioid dosage using best practices for opioid taper
Cases of serotonin syndrome, a potentially life-threatening condition, reported with concomitant use of serotonergic drugs; this may occur within the recommended dosage range; the onset of symptoms generally occur within several hours to a few days of concomitant use, but may occur later than that; discontinue therapy immediately if serotonin syndrome is suspected
Muscle rigidity occurring during induction of can be treated by decreasing rate or discontinuing infusion of drug or by administering a neuromuscular blocking agent; neuromuscular blocking agents used should be compatible with patient's cardiovascular status
Not to be administered into same IV tubing with blood due to potential inactivation by nonspecific esterases in blood products
Proper placement of needle or catheter in epidural space should be verified before drug is injected to assure that unintentional intravascular or intrathecal administration does not occur; unintentional intravascular injection of sufentanil could result in a potentially serious overdose, including acute truncal muscular rigidity and apnea; unintentional intrathecal injection of sufentanil/bupivacaine epidural doses and volume could produce effects of high spinal anesthesia including prolonged paralysis and delayed recovery; if analgesia is inadequate, placement and integrity of catheter should be verified prior to administration of any additional epidural medications; administer epidurally by slow injection
Bradycardia may occur; monitor heart rate during dosage initiation and titration; responsive to ephedrine or anticholinergic drugs
Therapy may cause severe hypotension including orthostatic hypotension and syncope in ambulatory patients; there is increased risk in patients whose ability to maintain blood pressure has already been compromised by a reduced blood volume or concurrent administration of certain CNS depressant drugs (e.g., phenothiazines or general anesthetics); monitor patients for signs of hypotension after initiating or titrating dosage; in patients with circulatory shock, therapy may cause vasodilation that can further reduce cardiac output and blood pressure; avoid therapy in patients with circulatory shock
Pregnancy & Lactation
Pregnancy
Prolonged use of opioid analgesics during pregnancy may cause neonatal opioid withdrawal syndrome; available data in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage
Labor or delivery
- Opioids cross placenta and may produce respiratory depression and psycho-physiologic effects in neonates; an opioid antagonist, such as naloxone, must be available for reversal of opioid induced respiratory depression in neonate; drug is not recommended for use in women during and immediately prior to labor, when use of shorter-acting analgesics or other analgesic techniques are more appropriate; opioid analgesics can prolong labor through actions that temporarily reduce strength, duration, and frequency of uterine contractions; however, this effect is not consistent and may be offset by an increased rate of cervical dilatation, which tends to shorten labor; monitor neonates exposed to opioid analgesics during labor for signs of excess sedation and respiratory depression
Lactation
The developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy; capsules and any potential adverse effects on breastfed infant from therapy or from underlying maternal condition
Monitor infants exposed to drug through breast milk for excess sedation and respiratory depression; withdrawal symptoms can occur in breastfed infants when maternal administration of an opioid analgesic is stopped, or when breast- feeding is stopped
Withdrawal signs can occur in breast-fed infants when maternal administration of an opioid analgesic is stopped or when breastfeeding is stopped; naloxone may precipitate opioid withdrawal in a breast-fed infant whose mother received opioid analgesics
Lactation: use with caution
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
Mechanism of Action
Narcotic agonist analgesic; increases pain threshold, inhibits ascending pain pathways, alters pain perception
Pharmacokinetics
Half-life: 5.33-8.75 hr (prematures, newborns); 40-60 min (children); 83-97 min (adults)
Onset: Immediate
Duration: 30-60 min
Vd: 1 L/kg (premature, newborns); 0.163-0.48 L/kg (children); 0.46 L/kg (adults)
Peak Plasma: distributed in decreasing order of concentration into skeletal muscle, kidneys, liver, intestinal tract, lungs, spleen, and brain
Bioavailability: Varies
Metabolism: liver (hepatic P450 enzyme CYP3A4), CNS, kidneys, lungs, and placenta (conjugation with glucuronic acid, hydrolysis, oxidation, N-dealkylation)
Excretion: urine, feces
Administration
IV Compatibilities
Solution: D5W
Syringe: atracurium, midazolam, ondansetron
Y-site: bivalirudin, cisatracurium, dexmedetomidine, etomidate, fenoldopam, gatifloxacin, Hextend, linezolid, propofol, remifentanil
IV Incompatibilities
Y-site: amphotericin B cholSO4, thiopental
IV Preparation
Add 20 mL to 230 mL of diluent for a final concentration of 40 mg/mL
IV Administration
Keep Naloxone and resuscitation equip available
By incremental injection as analgesic adjunct to anesthesia with barbiturate/nitrous oxide/oxygen for short surgical procedures (expected duration <1 hr)
By continuous infusion as a maintenance analgesic with nitrous oxide/oxygen for general surgical procedures
By IV injection in aesthetic doses for anesthesia induction for general surgical procedures with a minimum expected duration of 45 min
By IV inj as the analgesic component for monitored anesthesia care (MAC)
Storage
Protect from light
Store at controlled room temp
Images
Patient Handout
Formulary
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