Sufentanil

Mechanism of Action

May open K+ channels and inhibit Ca++ channels, causing an increase in pain threshold and alteration in pain perception. It also inhibits ascending pain pathways

Pharmacokinetics

Half-life: 5-10hr (neonates); 55-139 min (infants and children); 164 min (adults)

Onset: 1-3 min (IV); 10 min (epidural)

Duration: 2.3-3.8 hr

Peak Plasma: 36-43 ng/mL

Protein Bound: 93% (adults); 79% (neonates)

Vd: 2.48 L/kg

Metabolism: hepatic P450 enzyme CYP3A4; (N-dealkylation, O-demethylation)

Excretion: Urine (primarily)

IV Compatibilities

Solution: D5W, NS (5 mg/L)

Additive: bupivacaine, ropivacaine

Syringe: atracurium, atropine, dexamethasone, diphenhydramine, haloperidol, hydroxyzine, ketorolac, methotrimeprazine, metoclopramide, midazolam, prochlorperazine, scopolamine

Y-site: ampho B chol SO4, atropine, bivalirudin, ceftazidime, cisatracurium, dexamethasone, dexmedetomidine, diazepam, diphenhydramine, etomidate, fenoldopam, gatifloxacin, haloperidol, Hextend, hydroxyzine, ketorolac, linezolid, methotrimeprazine, metoclopramide, midazolam, phenobarbital, prochlorperazine, propofol, remifentanil, scopolamine

IV Incompatibilities

Solution: NS (20 mg/L)

Syringe: diazepam, lorazepam, phenobarbital, phenytoin

Y-site: lorazepam, phenytoin, thiopental

IV Administration

Administer by IV injection or epidural injection

Has also been administered by IM injection or by intermittent IV infusion

Storage

Protect from light

Store at 15-25°C

Sufentanil may be found in some form under the following brand names:

• Sufenta

Sufentanil is available in the following forms:

• Injectable Solution
• Prefilled Syringe

• It is used to put you to sleep for surgery.
• It is used to ease pain.

• If you have an allergy to sufentanil or any other part of this medicine.
• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
• If you have any of these health problems: Lung or breathing problems like asthma, trouble breathing, or sleep apnea; high levels of carbon dioxide in the blood; or stomach or bowel block or narrowing.
• If you are taking any of these drugs: Buprenorphine, butorphanol, nalbuphine, or pentazocine.
• If you have taken certain drugs used for low mood (depression) like isocarboxazid, phenelzine, or tranylcypromine or drugs used for Parkinson's disease like selegiline or rasagiline in the last 14 days. Taking sufentanil within 14 days of those drugs can cause very bad high blood pressure.
• If you are taking any of these drugs: Linezolid or methylene blue.

This is not a list of all drugs or health problems that interact with this medicine.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take sufentanil with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

Sufentanil CITRATE INJECTION SHOULD BE ADMINISTERED ONLY BY PERSONS SPECIFICALLY TRAINED IN THE USE OF INTRAVENOUS AND EPIDURAL ANESTHETICS AND MANAGEMENT OF THE RESPIRATORY EFFECTS OF POTENT OPIOIDS.

AN OPIOID ANTAGONIST, RESUSCITATIVE AND INTUBATION EQUIPMENT AND OXYGEN SHOULD BE READILY AVAILABLE.

PRIOR TO CATHETER INSERTION, THE PHYSICIAN SHOULD BE FAMILIAR WITH PATIENT CONDITIONS (SUCH AS INFECTION AT THE INJECTION SITE, BLEEDING DIATHESIS, ANTICOAGULANT THERAPY, ETC.) WHICH CALL FOR SPECIAL EVALUATION OF THE BENEFIT VERSUS RISK POTENTIAL.

Intravenous Use

Intravenous administration or unintentional intravascular injection during epidural administration of Sufentanil citrate may cause skeletal muscle rigidity, particularly of the truncal muscles. The incidence and severity of muscle rigidity is dose related. Administration of Sufentanil citrate may produce muscular rigidity with a more rapid onset of action than that seen with fentanyl. Sufentanil may produce muscular rigidity that involves the skeletal muscles of the neck and extremities. As with fentanyl, muscular rigidity has been reported to occur or recur infrequently in the extended postoperative period. The incidence of muscular rigidity associated with intravenous Sufentanil can be reduced by: 1) administration of up to 1/4 of the full paralyzing dose of a non-depolarizing neuromuscular blocking agent just prior to administration of Sufentanil citrate at dosages of up to 8 mcg/kg, 2) administration of a full paralyzing dose of a neuromuscular blocking agent following loss of consciousness when Sufentanil is used in anesthetic dosages (above 8 mcg/kg) titrated by slow intravenous infusion, or, 3) simultaneous administration of Sufentanil and a full paralyzing dose of a neuromuscular blocking agent when Sufentanil is used in rapidly administered anesthetic dosages (above 8 mcg/kg).

The neuromuscular blocking agents used should be compatible with the patient's cardiovascular status. Adequate facilities should be available for postoperative monitoring and ventilation of patients administered Sufentanil. It is essential that these facilities be fully equipped to handle all degrees of respiratory depression.

The most common adverse reactions of opioids are respiratory depression and skeletal muscle rigidity, particularly of the truncal muscles. Sufentanil may produce muscular rigidity that involves the skeletal muscles of the neck and extremities. See CLINICAL PHARMACOLOGY, WARNINGS and PRECAUTIONS on the management of respiratory depression and skeletal muscle rigidity. Urinary retention has been associated with the use of epidural opioids but was not reported in the clinical trials of epidurally administered Sufentanil due to the use of indwelling catheters. The incidence of urinary retention in patients without urinary catheters receiving epidural Sufentanil is unknown; return of normal bladder activity may be delayed.

The following adverse reaction information is derived from controlled clinical trials in 320 patients who received intravenous Sufentanil during surgical anesthesia and in 340 patients who received epidural Sufentanil plus bupivacaine 0.125% for analgesia during labor and is presented below. Based on the observed frequency, none of the reactions occurring with an incidence less than 1% were observed during clinical trials of epidural Sufentanil used during labor and delivery (N=340).

In general, cardiovascular and musculoskeletal adverse experiences were not observed in clinical trials of epidural Sufentanil. Hypotension was observed 7 times more frequently in intravenous trials than in epidural trials. The incidence of central nervous system, dermatological and gastrointestinal adverse experiences was approximately 4 to 25 times higher in studies of epidural use in labor and delivery.

Probably Causally Related: Incidence Greater than 1% Derived from clinical trials (See preceding paragraph)

Probably Causally Related: Incidence Less than 1% Derived from clinical trials (Adverse events reported in post-marketing surveillance, not seen in clinical trials, are italicized.)

Sufentanil Citrate Injection is a Schedule II controlled drug substance that can produce drug dependence of the morphine type and therefore has the potential for being abused.

(soo FEN ta nil)

IV: In adult obese patients (eg, >20% above ideal body weight), use lean body weight to determine dosage.