SUFentanil

Brand name: Sufenta
Drug class: Opiate Agonists
VA class: CN101
Chemical name: N-[4-(Methoxymethyl)-1-[2-(2-thieyl)ethyl]-4-piperidinyl]-N-phenylpropanamide2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Molecular formula: C₂₂H₃₀N₂O₂S•O₆H₈O₇
CAS number: 60561-17-3

Medically reviewed by Drugs.com on Jul 14, 2022. Written by ASHP.

Introduction

Opiate agonist; synthetic phenylpiperidine derivative.

Uses for SUFentanil

Anesthesia

As the analgesic component in the maintenance of balanced anesthesia (e.g., IV hypnotic and/or inhalation anesthetic, analgesic, skeletal muscle relaxant).

As the primary anesthetic agent for induction and maintenance of general anesthesia when used in conjunction with 100% oxygen and a skeletal muscle relaxant (e.g., pancuronium bromide, succinylcholine chloride).

Particularly useful when postoperative ventilation is anticipated and in providing favorable myocardial and cerebral oxygen balance.

Cardiovascular parameters generally are more stable intraoperatively with use of sufentanil compared with inhalation agents. Incidence of postoperative hypertension and requirements for vasoactive agents or postoperative analgesics generally are decreased following use of moderate or high doses of sufentanil as compared with use of inhalation agents.

Pain

Obstetric analgesia during labor and vaginal delivery.

SUFentanil Dosage and Administration

General

Premedication

• Selection of preanesthetic medication(s) should be based on the individual needs of the patient.

Administration

Administer by IV injection, intermittent or continuous IV infusion, or epidural injection.

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administration of small volumes may require use of a tuberculin syringe or equivalent.

Rate of Administration

Administer by slow injection or intermittent or continuous infusion; individualize rate based on patient’s needs.

Concomitant Administration of a Neuromuscular Blocking Agent

Risk of muscular rigidity (particularly of the truncal muscles) is related to the dose and rate of the infusion; however, administration of a neuromuscular blocking agent prior to sufentanil therapy can reduce the risk.

The neuromuscular blocking agent used should be compatible with the patient’s condition, taking into account the hemodynamic effects of the drug, the cardiovascular status of the patient, existing drug therapy (e.g., preoperative use of β-adrenergic blocking agents), and the degree of skeletal muscle relaxation required.

Epidural Administration

For drug compatibility information, see Compatibility under Stability.

Specialized techniques are required for epidural administration; administration should be performed only by qualified individuals familiar with the techniques of administration, dosages, and special patient management problems associated with epidural administration.

Dosage

Available as sufentanil citrate; dosage expressed in terms of sufentanil.

Adjust dosage carefully according to body weight, individual requirements and response, physical status and underlying pathologic condition, premedication or concomitant medication(s), the anesthetic(s) being used, and the nature and duration of the surgery.

Administer additional doses when patient movement and/or changes in vital signs indicate surgical stress or lightening of analgesia, and adjust according to individual requirements, response, and the anticipated remaining duration of the surgical procedure.

Pediatric Patients

Anesthesia

General Anesthesia (as sole anesthetic agent) for Cardiovascular Surgery

IV

Children <12 years of age: Initially, 10–25 mcg/kg in conjunction with 100% oxygen and a skeletal muscle relaxant. Additional doses of up to 25–50 mcg each (or, alternatively, 1–2 mcg/kg each) may be given as needed based on response to the initial dose and as determined by changes in vital signs that indicate surgical stress or lightening of anesthesia.

Neonates: Reduce dosage, especially in those with cardiovascular disease, according to the decrease in clearance. (See Pediatric Use under Cautions.)

Adults

Anesthesia

Analgesic Component of General Anesthesia

IV

Minor surgical procedures (expected duration of anesthesia is 1–2 hours): Total dosage of 1–2 mcg/kg in conjunction with nitrous oxide and oxygen; ≥75% of the total dosage may be given by slow injection or infusion prior to intubation. May administer supplemental doses of 10–25 mcg or administer intermittent or continuous maintenance infusions as necessary when movement and/or changes in vital signs indicate surgical stress or lightening of anesthesia; adjust maintenance infusion rate so that total dosage does not exceed 1 mcg/kg per hour of expected surgical time.

Major surgical procedures (expected duration of anesthesia is 2–8 hours): Total dosage of 2–8 mcg/kg in conjunction with nitrous oxide and oxygen; ≤75% of the total dosage may be given by slow injection or infusion prior to intubation. May administer supplemental doses of 10–50 mcg or administer intermittent or continuous maintenance infusions as necessary when movement and/or changes in vital signs indicate surgical stress or lightening of anesthesia; adjust maintenance infusion rate so that total dosage does not exceed 1 mcg/kg per hour of expected surgical time.

General Anesthesia (as sole anesthetic agent)

IV

Total dosage of 8–30 mcg/kg (by slow injection, infusion, or injection followed by infusion) in conjunction with oxygen and a skeletal muscle relaxant. Depending on the initial dose, may administer additional incremental doses of 0.5–10 mcg/kg by slow injection in anticipation of surgical stress (e.g., incision, sternotomy, cardiopulmonary bypass). Alternatively, may administer intermittent or continuous maintenance infusions as necessary as determined by changes in vital signs that indicate surgical stress and lightening of anesthesia; adjust maintenance infusion rate so that total dosage for the procedure does not exceed 30 mcg/kg.

Pain

Obstetric Analgesia

Epidural

10–15 mcg (in combination with 10 mL of bupivacaine 0.125% with or without epinephrine). Doses may be repeated twice (for a total of 3 doses) at ≥1-hour intervals until delivery.

Prescribing Limits

Adults

Anesthesia

Analgesic Component of General Anesthesia

IV

Minor or major surgical procedures: Total dose of ≤1 mcg/kg per hour of expected surgical time.

General Anesthesia (as sole anesthetic agent)

IV

Total dose for procedure: ≤ 30 mcg/kg.

Special Populations

Hepatic Impairment

Adjust dosage carefully; elimination of the drug may be decreased.

Renal Impairment

Adjust dosage carefully; elimination of the drug may be decreased.

Geriatric and Debilitated Patients

Reduce initial dosage; adjust additional doses according to the initial response and desired effect.

Obese Patients

Base dosage on an estimate of ideal (lean) body weight if body weight exceeds ideal weight by >20%.

Cautions for SUFentanil

Contraindications

• Known hypersensitivity to sufentanil or intolerance to other opiate agonists.

Warnings/Precautions

Warnings

Shares the toxic potentials of the opiate agonists; observe the usual precautions of opiate agonist therapy.

Respiratory Depression

Respiratory function can be severely compromised.

Consider the possibility of a recurrence of respiratory depression during recovery. A secondary rise in plasma concentrations may occur during the recovery period as blood perfusion to peripheral tissues increases and drug redistribution occurs.

Administration of an opiate antagonist (e.g., naloxone) can reverse respiratory depression. The duration of respiratory depression produced by sufentanil may be longer than the duration of the opiate antagonist; therefore, continue appropriate patient monitoring following apparent initial reversal.

Concomitant Use with Benzodiazepines or Other CNS Depressants

Concomitant use of sufentanil and benzodiazepines or other CNS depressants (e.g., anxiolytics, sedatives, hypnotics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opiate agonists, alcohol) may result in hypotension, decreased pulmonary arterial pressure, profound sedation, respiratory depression, coma, and death. (See Specific Drugs under Interactions.)

Supervised Administration

Should be administered only by individuals experienced in the use of parenteral anesthetics and in the maintenance of an adequate airway and respiratory support.

Opiate antagonist (e.g., naloxone) and facilities for intubation, administration of oxygen, and assisted or controlled respiration should be immediately available.

Monitor vital signs routinely during administration; facilities for postoperative monitoring and assisted or controlled respiration should be available following administration of anesthetic doses of the drug (i.e., ≥8 mcg/kg).

Major Toxicities

Musculoskeletal Effects

Possible skeletal muscle rigidity (e.g., of the truncal muscles); onset may be more rapid than with fentanyl. Administration of a neuromuscular blocking agent may be necessary. (See Concomitant Administration of a Neuromuscular Blocking Agent under Dosage and Administration.)

Adrenal Insufficiency

Adrenal insufficiency reported in patients receiving opiate agonists or opiate partial agonists. Manifestations are nonspecific and may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and hypotension.

If adrenal insufficiency is suspected, perform appropriate laboratory testing promptly and provide physiologic (replacement) dosages of corticosteroids; taper and discontinue the opiate agonist or partial agonist to allow recovery of adrenal function. If the opiate agonist or partial agonist can be discontinued, perform follow-up assessment of adrenal function to determine if corticosteroid replacement therapy can be discontinued. In some patients, switching to a different opiate improved symptoms.

General Precautions

CNS Effects

Caution in patients with head injuries; sufentanil may obscure the clinical course.

Impaired Respiration

Caution in patients with pulmonary disease, decreased respiratory reserve, or potentially compromised respiratory function. Further decreases in respiratory function and increases in airway resistance may occur.

Cardiovascular Effects

Generally produces few cardiovascular effects. Possible hypotension or hypertension. Bradycardia occurs infrequently during anesthesia and may be corrected by administration of atropine.

Hypogonadism

Hypogonadism or androgen deficiency reported in patients receiving long-term opiate agonist or opiate partial agonist therapy; causality not established. Manifestations may include decreased libido, impotence, erectile dysfunction, amenorrhea, or infertility. Perform appropriate laboratory testing in patients with manifestations of hypogonadism.

Specific Populations

Pregnancy

Category C.

Used epidurally for analgesia during labor and delivery. Not recommended for IV use during labor and delivery; avoid epidural dosages in excess of the recommended dosage.

Lactation

Not known whether sufentanil is distributed into milk. Caution if used in nursing women.

Pediatric Use

Safety and efficacy documented in a limited number of children ≥1 day of age undergoing cardiovascular surgery.

Use with caution in neonates because decreased clearance may result in increased blood concentrations of the drug. Clearance in healthy neonates is approximately one-half that reported in adults and children; may be further reduced by up to one-third in neonates with cardiovascular disease.

Geriatric Use

Consider dosage reduction. (See Geriatric and Debilitated Patients under Dosage and Administration.)

Hepatic Impairment

Use with caution, since the drug undergoes metabolism in the liver.

Renal Impairment

Use with caution, since the drug and its metabolites are eliminated mainly by the kidneys.

Common Adverse Effects

Respiratory depression, skeletal muscle rigidity (e.g., truncal muscles, neck, extremities).

Interactions for SUFentanil

Drugs Associated with Serotonin Syndrome

Risk of serotonin syndrome when used with other serotonergic drugs. May occur at usual dosages. Symptom onset generally occurs within several hours to a few days of concomitant use, but may occur later, particularly after dosage increases. (See Advice to Patients.)

If concomitant use of other serotonergic drugs is warranted, monitor patients for serotonin syndrome, particularly during initiation of therapy and dosage increases.

If serotonin syndrome is suspected, discontinue sufentanil, other opiate therapy, and/or any concurrently administered serotonergic agents.

Specific Drugs

SUFentanil Pharmacokinetics

Absorption

Onset

Following IV administration, the onset of action as determined by time to unconsciousness (i.e., loss of response to voice command) is 1.2–3 minutes.

Following epidural administration of 10–15 mcg and 0.125% bupivacaine with epinephrine 1:200,000 during the first stage of labor, the onset of action occurs within 10 minutes.

Duration

The mean duration of anesthesia is 40 minutes following initial IV dose of 0.4 mcg/kg and 41–44 minutes following additional doses of 0.1 mcg/kg. Following administration of anesthetic doses (about 13–19 mcg/kg total), patient response to verbal command and adequate ventilation occurs at 0.6–1.8 and 5.6 hours, respectively.

Following IM administration of single doses of 0.15, 0.3, or 0.5 mcg/kg in patients with pain, the approximate duration of detectable analgesia was 2.3, 3.7, and 3.8 hours, respectively.

Following epidural administration of 10–15 mcg and 0.125% bupivacaine with epinephrine 1:200,000 during the first stage of labor, the duration of action was 1–2 hours.

Distribution

Extent

Distribution into human body tissues and fluids has not been fully characterized; however, the drug is highly lipophilic and is rapidly and extensively distributed in animals.

Not known whether sufentanil crosses the placenta or distributes into milk.

Plasma Protein Binding

Approximately 93% bound at plasma pH 7.4 (mainly to albumin; α-, α₁-, β-, and γ-globulins; and α₁-acid glycoprotein).

Because a large portion of the drug appears to be bound to α₁-acid glycoprotein, binding may be affected by disease states in which this protein is altered.

Binding in plasma is independent of plasma drug concentration within the therapeutic range (i.e., 0.1–10 ng/mL); however, binding is affected by changes in plasma pH. Increases in plasma pH from 7.4 to 7.8 increase sufentanil binding by about 30%; decreases in plasma pH from 7.4 to 7 decrease binding by about 30%.

Elimination

Metabolism

Appears to be metabolized mainly in the liver and small intestine via N-dealkylation and O-demethylation.

The O-demethylated metabolite appears to have about 10% of the analgesic activity of the unchanged drug.

Elimination Route

Excreted principally in urine and also in feces via biliary elimination; only 2% of a dose is excreted unchanged in urine and feces.

Half-life

Triphasic; plasma concentrations decline rapidly secondary to redistribution.

In adults with normal renal and hepatic function, the plasma half-life averages 0.72–1.2 minutes in the initial (distribution) phase, 13.7–17 minutes in the second (redistribution) phase, and 140–158 minutes in the terminal (elimination) phase.

Elimination half-life is longer (434 minutes) in neonates but shorter in infants and children (97 minutes), compared with adults and adolescents.

Stability

Storage

Parenteral

Injection

15–25°C; protect from light.

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Sufentanil citrate is hydrolyzed in acidic solutions.

Solution CompatibilityHID

Drug Compatibility

Actions

• A potent analgesic; shares the actions of the opiate agonists.

• Precise mechanism of action has not been fully elucidated; opiate agonists act at several CNS sites, involving several neurotransmitter systems to produce analgesia.

• Pain perception is altered in the spinal cord and higher CNS levels (e.g., substantia gelatinosa, spinal trigeminal nucleus, periaqueductal gray, periventricular gray, medullary raphe nuclei, hypothalamus).

• Opiate agonists do not alter the threshold or responsiveness of afferent nerve endings to noxious stimuli, nor peripheral nerve impulse conduction.

• Opiate agonists act at specific receptor binding sites in the CNS and other tissues; opiate receptors are concentrated in the limbic system, thalamus, striatum, hypothalamus, midbrain, and spinal cord.

• High affinity and selectivity for the μ-opiate receptor in the CNS; reportedly is more selective and binds more tightly to this receptor than does fentanyl.

• Produces dose-related analgesia; at doses up to 8 mcg/kg, the drug has a potent analgesic effect, but higher doses usually produce substantial CNS depression resulting in hypnosis and anesthesia.

• Analgesic potency appears to be 5–12 times that of fentanyl on a weight basis.

• Appears to have little effect on histamine release.

• May have a centrally mediated vagal effect.

Advice to Patients

• Risk of potentially fatal additive effects (e.g., profound sedation, respiratory depression, coma) if used concomitantly with benzodiazepines or other CNS depressants, including alcohol and other opiates, either therapeutically or illicitly. Importance of advising patients to avoid alcohol following sufentanil administration.

• Potential risk of serotonin syndrome with concurrent use of sufentanil and other serotonergic agents. Importance of immediately contacting clinician if manifestations of serotonin syndrome (e.g., agitation, hallucinations, tachycardia, labile BP, fever, excessive sweating, shivering, shaking, muscle stiffness, twitching, loss of coordination, nausea, vomiting, diarrhea) develop.

• Potential risk of adrenal insufficiency. Importance of contacting clinician if manifestations of adrenal insufficiency (e.g., nausea, vomiting, loss of appetite, fatigue, weakness, dizziness, hypotension) develop.

• Possible risk (although causality not established) of hypogonadism or androgen deficiency with long-term opiate agonist or partial agonist use. Importance of informing clinician if decreased libido, impotence, erectile dysfunction, amenorrhea, or infertility occurs following therapy.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Subject to control under the Federal Controlled Substances Act of 1970 as a schedule II (C-II) drug.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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Frequently asked questions

• What is the Dsuvia REMS program?
• How do you take the Dsuvia (sufentanil) tablet?
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