Sufentanil uses, doses, brand name and it effects

Description of Sufentanil 

Sufentanil is an injectable and sublingual opioid agonist of the phenylpiperidine class. Injectable sufentanil is indicated as a primary anesthetic agent for the induction and maintenance of anesthesia with 100% oxygen in patients undergoing major surgical procedures to provide favorable myocardial and cerebral oxygen balance or when extended postoperative ventilation is required, as an analgesic adjunct in the maintenance of balanced anesthesia, and for epidural anesthesia with low dose bupivacaine during labor and delivery. Sufentanil sublingual tablets are indicated for the management of acute severe pain that requires an opioid analgesic and for which alternative treatment options are inadequate in a certified, medically supervised healthcare setting. When used as balanced general anesthesia, sufentanil has been reported to be as much as 10 times as potent as fentanyl. When administered intravenously as a primary anesthetic agent with 100% oxygen, sufentanil is approximately 5 to 7 times as potent as fentanyl. Sufentanil has been shown to provide some attenuation of the sympathetic reflex activity in response to surgical stimuli, hemodynamic stability, and relatively rapid recovery.

Mechanism of Action of Sufentanil

Sufentanil is an opioid agonist and is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principle therapeutic action of sufentanil is analgesia and sedation, thought to be mediated through opioid-specific receptors throughout the central nervous system. Like all full opioid agonists, there is no ceiling effect to analgesia. When used as balanced general anesthesia, sufentanil has been reported to be as much as 10 times as potent as fentanyl. When administered intravenously as a primary anesthetic agent with 100% oxygen, sufentanil is approximately 5 to 7 times as potent as fentanyl. The response to sufentanil is dose-dependent, with analgesia predominating at intravenous doses less than 8 mcg/kg and deep anesthesia produced at doses of 8 mcg/kg or more. Sufentanil attenuates the sympathetic response to surgical stress. The catecholamine response, especially norepinephrine, is further attenuated at intravenous sufentanil doses of 25 to 30 mcg/kg, with hemodynamic stability and preservation of favorable myocardial oxygen balance. Anesthetic doses of sufentanil maintain cardiac output, with slight reduction in systemic vascular resistance during the initial postoperative period.

Pharmacokinetics

Sufentanil is administered intravenously, epidurally, or sublingually. The pharmacokinetics of sufentanil can be described as a 3-compartment model. It is 93% protein bound, primarily to alpha₁-acid glycoprotein. The liver and small intestine are the major sites of metabolism. The elimination half-life after intravenous administration is 164 minutes in adults and adolescents. The mean half-life and mean apparent plasma clearance are 13.4 hours and 108 L/hour, respectively, after a single sublingual tablet dose. Approximately 80% of intravenously administered drug is excreted within 24 hours and only 2% is eliminated as unchanged drug.

Affected cytochrome P450 isoenzymes and drug transporters: CYP3A4
Sufentanil is a substrate for cytochrome P450 (CYP) 3A4.

•Route-Specific Pharmacokinetics
Oral Route
The relative bioavailability of a single sufentanil sublingual administration to a 1-minute IV infusion of 30 mcg is 53%. Sublingual Cmax values were 17-fold lower compared to IV administration. After a single sufentanil sublingual administration, the average Cmax of 63.1 pg/mL and mean AUC of 278 hours x pg/mL occur at a median Tmax of 1 hour. After 12 multiple hourly doses over 11 hours, the geometric mean for the AUC within a dosing interval and Cmax values were increased by 3.7- and 2.3-fold compared to single-dose administration. Steady-state plasma concentrations were achieved after 7 doses.

Intravenous Route
Duration of effect is dose-related.

Other Route(s)
Epidural Route
The onset of analgesia after an epidural dose of 10 to 15 mcg sufentanil with bupivacaine 0.125% with epinephrine occurs within 10 minutes with duration of 1 to 2 hours. Subsequent equivalent doses tend to have a shorter duration. The duration of initial doses of sufentanil plus bupivacaine with epinephrine is approximately 95 minutes, and of subsequent doses, 70 minutes. After epidural administration of incremental doses totaling 5 to 40 mcg sufentanil during labor and delivery, maternal and neonatal sufentanil plasma concentrations were at or near 0.05 to 0.1 ng/mL, and were slightly higher in mothers than in their infants.

• Sufentanil Citrate

• Sufenta
• Dsuvia

• Analgesic
• Opioid

• Analgesia in labor, In combination with bupivacaine: Adult
• General anesthesia: Adult
• General anesthesia: Pediatric
• Maintenance of general anesthesia – No sensitivity to pain; Adjunct: Adult
• Maintenance of general anesthesia – No sensitivity to pain; Adjunct: Pediatric
• Pain, acute (Severe), Severe enough to require an opioid analgesic: Adult: yes (sublingual tablet only)

• Dermatologic: Pruritus (Analgesia, 0.5% or greater ; Anesthesia, 25% )
• Gastrointestinal: Nausea (Analgesia, 29% ; anesthesia, 3% to 9% ; ), Vomiting (3% to 9% )
• Musculoskeletal: Muscle rigidity, Chest Wall (3% to 9% )
• Neurologic: Dizziness (Analgesia, 5.6% ), Headache (Analgesia, 12.1% ), Somnolence (Analgesia, 0.1% or greater ; anesthesia, 3% to 9% )

• Cardiovascular: Bradyarrhythmia (Analgesia, 0.1% or greater ; anesthesia, 3% to 9% ), Cardiac arrest, Hypertension (3% to 9% ), Hypotension (3% to 9% )
• Immunologic: Anaphylaxis
• Musculoskeletal: Muscle rigidity
• Neurologic: Seizure
• Respiratory: Apnea (Up to 1% ), Respiratory depression (0.3 to 1% ), Sleep apnea
• Other: Drug dependence, Opioid withdrawal, Serotonin syndrome

• (Injection) For IV or epidural use
• (Tablet) For sublingual use only
• Intravenous: Use a tuberculin syringe or equivalent for the accurate administration of small volumes .
• Intravenous: Administer via slow IV injection or infusion .
• Intravenous: (Maintenance infusion) Adjust the rate of infusion based upon the induction dose so that total dose does not exceed 1 mcg/kg per hour of expected surgical time .
• Epidural: Use a tuberculin syringe or equivalent for the accurate administration of small volumes ..
• Epidural: Mix sufentanil and bupivacaine prior to administration .
• Epidural: Administer by slow injection .
• Sublingual: Must be administered by a healthcare provider in a certified medically supervised healthcare setting .
• Sublingual: Not for home use. Discontinue before patients leave the supervised healthcare setting .
• Sublingual: Administer via single-dose applicator to sublingual space .
• Sublingual: Wear gloves when administering .
• Sublingual: Do not chew or swallow tablet .
• Sublingual: Do not eat or drink and minimize talking for 10 minutes after receiving tablet .

• Dsuvia: Sublingual Tablet: 30 MCG

• Injection Solution: 1 MG/1 ML, 50 MCG/1 ML

• Important Note: Beers Criteria: Use caution or avoid use as potentially inappropriate in older adults .
• Analgesia in labor, In combination with bupivacaine: Prior to initiation, verify proper placement of the needle or catheter in the epidural space
• Analgesia in labor, In combination with bupivacaine: Individualize dosage based on patient age, weight, physical status, underlying conditions, and medication use .
• Analgesia in labor, In combination with bupivacaine: 10 to 15 mcg administered epidurally with 10 mL bupivacaine 0.125% with or without epinephrine; may repeat twice at not less than 1-hour intervals until delivery; MAX 3 doses
• General anesthesia: Individualize dosage based on patient age, weight, physical status, underlying conditions, and medication use, as well as the specific surgical procedure and type of anesthesia to be used. Base preanesthetic medication selection on individual needs .
• General anesthesia: (Incremental IV) Maintenance dosage, 0.5 to 10 mcg/kg IV in anticipation of surgical stress, such as incision, sternotomy, or cardiopulmonary bypass. Total dosage, 8 to 30 mcg/kg; MAX, 30 mcg/kg
• General anesthesia: (IV infusion) Maintenance dosage, administer via intermittent or continuous IV infusion as needed for signs of analgesia lightening; titrate downward in the absence of lightening until there is some response to surgical stimulation. Total dosage, 8 to 30 mcg/kg; MAX, 30 mcg/kg
• Maintenance of general anesthesia – No sensitivity to pain; Adjunct: Individualize dosage based on patient age, weight, physical status, underlying conditions, and medication use, as well as the specific surgical procedure and type of anesthesia to be used. Base preanesthetic medication selection on individual needs .
• Maintenance of general anesthesia – No sensitivity to pain; Adjunct: (Incremental IV) Expected anesthesia duration of 1 to 2 hours: Maintenance dosage, 10 to 25 mcg IV in increments as needed for movement or vital sign changes indicating surgical stress or lightening of analgesia; individualize and adjust doses based on anticipated remaining operative time. Total dosage, 1 to 2 mcg/kg; may give 75% or more of total dose prior to intubation by slow injection or infusion titrated to clinical response .
• Maintenance of general anesthesia – No sensitivity to pain; Adjunct: (Incremental IV) Expected anesthesia duration of 2 to 8 hours: Maintenance dosage, 10 to 50 mcg IV in increments as needed for movement or vital sign changes indicating surgical stress or lightening of analgesia; individualize and adjust doses based on anticipated remaining operative time. Total dosage, 2 to 8 mcg/kg; may give 75% or more of total dose prior to intubation by slow injection or infusion titrated to clinical response .
• Maintenance of general anesthesia – No sensitivity to pain; Adjunct: (IV Infusion) Expected anesthesia duration of 1 to 2 hours: Maintenance dosage, administer via intermittent or continuous IV infusion as needed for signs of analgesia lightening; titrate downward in the absence of lightening until there is some response to surgical stimulation. MAX total dosage, 1 mcg/kg/hr of expected surgical time; may give 75% or more of total dose prior to intubation by slow injection or infusion titrated to clinical response .
• Maintenance of general anesthesia – No sensitivity to pain; Adjunct: (IV Infusion) Expected anesthesia duration of 2 to 8 hours: Maintenance dosage, administer via intermittent or continuous IV infusion as needed for signs of analgesia lightening; titrate downward in the absence of lightening until there is some response to surgical stimulation. MAX total dosage, 1 mcg/kg/hr of expected surgical time; may give 75% or more of total dose prior to intubation by slow injection or infusion titrated to clinical response .
• Pain, acute (Severe), Severe enough to require an opioid analgesic: 30 mcg sublingually as needed with a minimum of 1 hour between doses; MAX, 12 tablets in 24 hours (360 mcg cumulative daily dose); do not use for more than 72 hours .

• Important Note: Beers Criteria: Use caution or avoid use as potentially inappropriate in older adults .
• General anesthesia: Individualize dosage based on patient age, weight, physical status, underlying conditions, and medication use, as well as the specific surgical procedure and type of anesthesia to be used. Base preanesthetic medication selection on individual needs .
• General anesthesia: (Younger than 12 years) Cardiovascular surgery: Induction and maintenance, 10 to 25 mcg/kg IV; maintenance dosage, 25 to 50 mcg IV as needed based for vital sign changes indicating surgical stress or lightening of analgesia and based on response to initial dose

• Injection (Solution): Sufentanil citrate injection exposes users to risks of addiction, abuse, and misuse, which can lead to overdose and death. Assess patient’s risk before prescribing and monitor regularly for these behaviors and conditions .
• Sublingual (Tablet): Accidental exposure to or ingestion of sufentanil sublingual tablets, especially in children, can result in respiratory depression and death. Because of the potential for life-threatening respiratory depression due to accidental exposure, sufentanil sublingual tablets are only available through a restricted program called the Dsuvia REMS Program. Sufentanil sublingual tablets must only be dispensed to patients in a certified medically supervised healthcare setting. Discontinue use of sufentanil sublingual tablets prior to discharge or transfer from the certified medically supervised healthcare setting.
• Sublingual (Tablet): Serious, life-threatening, or fatal respiratory depression may occur with the use of sufentanil sublingual tablets. Monitor for respiratory depression, especially during initiation of sufentanil sublingual tablets.
• Sublingual (Tablet): Sufentanil sublingual tablets 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 sufentanil sublingual tablets, and monitor all patients regularly for the development of these behaviors or conditions.
• Sublingual (Tablet): Concomitant use with CYP3A4 inhibitors (or discontinuation of CYP3A4 inducers) can result in a fatal overdose of sufentanil.
• Sublingual (Tablet): Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants including alcohol, may result in profound sedation, respiratory depression coma, and death. Reserve concomitant prescribing for use in patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required. Follow patients for signs and symptoms of respiratory depression and sedation .