alfentanil (Rx)

>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

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

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

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.

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

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