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    Chemistry

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    Also known as: Sufentanyl, 56030-54-7, Sufentanilum, Sufentanilum [inn-latin], Zalviso, R-30730
    Molecular Formula
    C22H30N2O2S
    Molecular Weight
    386.6  g/mol
    InChI Key
    GGCSSNBKKAUURC-UHFFFAOYSA-N
    FDA UNII
    AFE2YW0IIZ
    Sufentanil Citrate
    An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.
    Sufentanil is an Opioid Agonist. The mechanism of action of sufentanil is as a Full Opioid Agonist.
    1 2D Structure

    Sufentanil Citrate

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    N-[4-(methoxymethyl)-1-(2-thiophen-2-ylethyl)piperidin-4-yl]-N-phenylpropanamide
    2.1.2 InChI
    InChI=1S/C22H30N2O2S/c1-3-21(25)24(19-8-5-4-6-9-19)22(18-26-2)12-15-23(16-13-22)14-11-20-10-7-17-27-20/h4-10,17H,3,11-16,18H2,1-2H3
    2.1.3 InChI Key
    GGCSSNBKKAUURC-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CCC(=O)N(C1=CC=CC=C1)C2(CCN(CC2)CCC3=CC=CS3)COC
    2.2 Other Identifiers
    2.2.1 UNII
    AFE2YW0IIZ
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Citrate, Sufentanil

    2. Curasan, Sufentanil

    3. R 30730

    4. R-30730

    5. R30730

    6. Sufenta

    7. Sufentanil Citrate

    8. Sufentanil Curasan

    9. Sufentanil Hameln

    10. Sufentanil Ratiopharm

    11. Sufentanil-hameln

    12. Sufentanil-ratiopharm

    13. Sufentanilhameln

    14. Sufentanilratiopharm

    15. Sulfentanil

    16. Sulfentanyl

    2.3.2 Depositor-Supplied Synonyms

    1. Sufentanyl

    2. 56030-54-7

    3. Sufentanilum

    4. Sufentanilum [inn-latin]

    5. Zalviso

    6. R-30730

    7. N-(4-(methoxymethyl)-1-(2-(2-thienyl)ethyl)-4-piperidyl)propionanilide

    8. N-(4-(methoxymethyl)-1-(2-(2-thienyl)ethyl)-4-piperidinyl)-n-phenylpropanamide

    9. Chebi:9316

    10. Afe2yw0iiz

    11. N-[4-(methoxymethyl)-1-(2-thiophen-2-ylethyl)piperidin-4-yl]-n-phenylpropanamide

    12. Chronogesic

    13. Ids-ns-001

    14. R 30,730

    15. Propanamide, N-(4-(methoxymethyl)-1-(2-(2-thienyl)ethyl)-4-piperidinyl)-n-phenyl-

    16. Propanamide, N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-n-phenyl-

    17. N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidyl]propionanilide

    18. R 30730

    19. Hsdb 6760

    20. Unii-afe2yw0iiz

    21. Sufentanil (usan/inn)

    22. Sufentanil [usan:inn:ban]

    23. Sufentanil Base

    24. N-[4-(methoxymethyl)-1-{2-(2-thienyl)ethyl}-4-piperidinyl]-n-phenylpropanamide

    25. Dsuvia (brand Name)

    26. Sufenta (brand Name)

    27. Sufentanil [mi]

    28. Sufentanil [inn]

    29. Sufentanil [hsdb]

    30. Sufentanil [usan]

    31. Sufentanil [vandf]

    32. Chembl658

    33. Epitope Id:153513

    34. Sufentanil [mart.]

    35. Arx04

    36. Sufentanil [who-dd]

    37. Oprea1_120838

    38. Oprea1_246787

    39. Schembl26728

    40. Cid_65494

    41. Arx 04

    42. Gtpl3534

    43. Dtxsid6023604

    44. Bdbm94503

    45. Sufentanil [ep Monograph]

    46. Zinc538386

    47. Pdsp1_001741

    48. Pdsp2_001724

    49. Db00708

    50. N-{4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]piperidin-4-yl}-n-phenylpropanamide

    51. N-{4-[(methyloxy)methyl]-1-[2-(2-thienyl)ethyl]piperidin-4-yl}-n-phenylpropanamide

    52. Ncgc00247355-01

    53. Hy-13754

    54. C08022

    55. D05938

    56. L000580

    57. Q417915

    58. N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]propionalnalide

    59. Citric Acid;n-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidyl]-n-phenyl-propionamide

    60. N-(4-(methoxymethyl)-1-(2-(thiophen-2-yl)ethyl)piperidin-4-yl)-n-phenylpropionamide

    61. N-(4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl)-n-phenylpropanamide #

    62. N-[4-(methoxymethyl)-1-[2-(thiophen-2-yl)ethyl]piperidin-4-yl]-n-phenylpropanamide

    63. 2-hydroxypropane-1,2,3-tricarboxylic Acid;n-[4-(methoxymethyl)-1-(2-thiophen-2-ylethyl)-4-piperidinyl]-n-phenylpropanamide

    64. N-[4-(methoxymethyl)-1-(2-thiophen-2-ylethyl)piperidin-4-yl]-n-phenyl-propanamide;2-oxidanylpropane-1,2,3-tricarboxylic Acid

    2.4 Create Date
    2005-03-28
    3 Chemical and Physical Properties
    Molecular Weight 386.6 g/mol
    Molecular Formula C22H30N2O2S
    XLogP34
    Hydrogen Bond Donor Count0
    Hydrogen Bond Acceptor Count4
    Rotatable Bond Count8
    Exact Mass386.20279938 g/mol
    Monoisotopic Mass386.20279938 g/mol
    Topological Polar Surface Area61 Ų
    Heavy Atom Count27
    Formal Charge0
    Complexity459
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Therapeutic Uses

    Analgesics, Opioid; Adjuvants, Anesthesia; Narcotics; Anesthetics, Intravenous

    National Library of Medicine's Medical Subject Headings. Sufentanil. Online file (MeSH, 2017). Available from, as of April 26, 2017: https://www.nlm.nih.gov/mesh/2017/mesh_browser/MBrowser.html

    /CLINICAL TRIALS/ ClinicalTrials.gov is a registry and results database of publicly and privately supported clinical studies of human participants conducted around the world. The Web site is maintained by the National Library of Medicine (NLM) and the National Institutes of Health (NIH). Each ClinicalTrials.gov record presents summary information about a study protocol and includes the following: Disease or condition; Intervention (for example, the medical product, behavior, or procedure being studied); Title, description, and design of the study; Requirements for participation (eligibility criteria); Locations where the study is being conducted; Contact information for the study locations; and Links to relevant information on other health Web sites, such as NLM's MedlinePlus for patient health information and PubMed for citations and abstracts for scholarly articles in the field of medicine. Sufentanil is included in the database.

    NIH/NLM; ClinicalTrials.Gov. Available from, as of June 20, 2017: https://clinicaltrials.gov/

    Sufentanil Citrate Injection is indicated for intravenous administration in adults and pediatric patients as an analgesic adjunct in the maintenance of balanced general anesthesia in patients who are intubated and ventilated. /Included in US product label/

    NIH; DailyMed. Current Medication Information for Sufentanil Citrate Injection (Updated: December 2016). Available from, as of May 2, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=95e639db-1ca3-4328-b347-7ea348f6cc72

    Sufentanil Citrate Injection is indicated for intravenous administration in adults and pediatric patients ... as a primary anesthetic agent for the induction and maintenance of anesthesia with 100% oxygen in patients undergoing major surgical procedures, in patients who are intubated and ventilated, such as cardiovascular surgery or neurosurgical procedures in the sitting position, to provide favorable myocardial and cerebral oxygen balance or when extended postoperative ventilation is anticipated. /Included in US product label/

    NIH; DailyMed. Current Medication Information for Sufentanil Citrate Injection (Updated: December 2016). Available from, as of May 2, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=95e639db-1ca3-4328-b347-7ea348f6cc72

    For more Therapeutic Uses (Complete) data for Sufentanil (7 total), please visit the HSDB record page.

    4.2 Drug Warning

    /BOXED WARNING/ WARNING: ADDICTION, ABUSE, AND MISUSE. 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.

    NIH; DailyMed. Current Medication Information for Sufentanil Citrate Injection (Updated: December 2016). Available from, as of May 2, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=95e639db-1ca3-4328-b347-7ea348f6cc72

    Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids, even when used as recommended. Respiratory depression, if not immediately recognized and treated, may lead to respiratory arrest and death. Sufentanil Citrate Injection should be administered only by persons specifically trained in the use of anesthetic drugs and the management of the respiratory effects of potent opioids, including respiration and cardiac resuscitation of patients in the age group being treated. Such training must include the establishment and maintenance of a patent airway and assisted ventilation. Adequate facilities should be available for postoperative monitoring and ventilation of patients administered anesthetic doses of Sufentanil Citrate Injection. It is essential that these facilities be fully equipped to handle all degrees of respiratory depression. Management of respiratory depression may include close observation, supportive measures, and use of opioid antagonists, depending on the patient's clinical status. Carbon dioxide (CO2) retention from opioid-induced respiratory depression can exacerbate the sedating effects of opioids.

    NIH; DailyMed. Current Medication Information for Sufentanil Citrate Injection (Updated: December 2016). Available from, as of May 2, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=95e639db-1ca3-4328-b347-7ea348f6cc72

    Sufentanil should be used with caution in patients with head injuries, since the drug may obscure the clinical course in these patients. The drug should be used with caution in patients with pulmonary disease, decreased respiratory reserve, or potentially compromised respiratory function, since opiate agonists may cause additional decreases in respiratory function and increases in airway resistance in these patients. These adverse respiratory effects can be managed by using assisted or controlled respiration during anesthesia. Sufentanil-induced respiratory depression can be reversed by administration of an opiate antagonist (e.g., naloxone); however, the duration of respiratory depression produced by sufentanil may be longer than the duration of the opiate antagonist and, therefore, appropriate patient monitoring should be continued following apparent initial reversal.

    American Society of Health-System Pharmacists 2017; Drug Information 2017. Bethesda, MD. 2017, p. 2279

    The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for Sufentanil Citrate Injection and any potential adverse effects on the breastfed infant from Sufentanil Citrate Injection or from the underlying maternal condition.

    NIH; DailyMed. Current Medication Information for Sufentanil Citrate Injection (Updated: December 2016). Available from, as of May 2, 2017: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=95e639db-1ca3-4328-b347-7ea348f6cc72

    For more Drug Warnings (Complete) data for Sufentanil (22 total), please visit the HSDB record page.

    4.3 Drug Indication

    The indications for this drug are as follows: 1. As an analgesic adjunct in the maintenance of balanced general anesthesia in patients who are intubated and ventilated. 2. As a primary anesthetic agent for the induction and maintenance of anesthesia with 100% oxygen in patients undergoing major surgical procedures, in patients who are intubated and ventilated, such as cardiovascular surgery or neurosurgical procedures in the sitting position, to provide favorable myocardial and cerebral oxygen balance or when extended postoperative ventilation is anticipated. 3. For epidural administration as an analgesic combined with low dose (usually 12.5 mg per administration) bupivacaine usually during labor and vaginal delivery 4. The sublingual form is indicated for the management of acute pain in adults that is severe to warrant the use of an opioid analgesic in certified medically supervised healthcare settings, including hospitals, surgical centers, and emergency departments.

    FDA Label

    Zalviso is indicated for the management of acute moderate to severe post-operative pain in adult patients.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    **Effect on the Central Nervous System (CNS)** In clinical settings, sufentanil exerts its principal pharmacologic effects on the central nervous system. Its primary therapeutic actions are analgesia and sedation. Sufentanil may increase pain tolerance and decrease the perception of pain. This drug depresses the respiratory centers, depresses the cough reflex, and constricts the pupils,. When used in 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. High doses of intravenous sufentanil have been shown to cause muscle rigidity, likely as a result of an effect on the substantia nigra and the striate nucleus in the brain. Sleep-inducing (hypnotic) activity can be demonstrated by EEG alterations. **Effects on the Respiratory System** Sufentanil may cause respiratory depression. **Effects on the Cardiovascular System** Sufentanil causes peripheral vasodilation which may result in orthostatic hypotension or syncope. Bradycardia may also occur. Clinical signs or symptoms of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes and sweating and/or orthostatic hypotension. **Effects on the Gastrointestinal Tract** Sufentanil causes a reduction in motility associated with an increase in smooth muscle tone in both the antrum of the stomach and duodenum. Digestion of food in the small intestine may be delayed and propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, while tone may be increased and lead to spasm, resulting in constipation. Other opioid-induced effects may include a reduction in biliary and pancreatic secretions, spasm of the sphincter of Oddi, as well as temporary elevations in serum amylase.

    5.2 MeSH Pharmacological Classification

    Adjuvants, Anesthesia

    Agents that are administered in association with anesthetics to increase effectiveness, improve delivery, or decrease required dosage. (See all compounds classified as Adjuvants, Anesthesia.)

    Anesthetics, Intravenous

    Ultrashort-acting anesthetics that are used for induction. Loss of consciousness is rapid and induction is pleasant, but there is no muscle relaxation and reflexes frequently are not reduced adequately. Repeated administration results in accumulation and prolongs the recovery time. Since these agents have little if any analgesic activity, they are seldom used alone except in brief minor procedures. (From AMA Drug Evaluations Annual, 1994, p174) (See all compounds classified as Anesthetics, Intravenous.)

    Narcotics

    Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS. (See all compounds classified as Narcotics.)

    Analgesics, Opioid

    Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS. (See all compounds classified as Analgesics, Opioid.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    SUFENTANIL
    5.3.2 FDA UNII
    AFE2YW0IIZ
    5.3.3 Pharmacological Classes
    Opioid Agonist [EPC]; Full Opioid Agonists [MoA]
    5.4 ATC Code

    N01AH03

    N01AH03

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    N - Nervous system

    N01 - Anesthetics

    N01A - Anesthetics, general

    N01AH - Opioid anesthetics

    N01AH03 - Sufentanil

    5.5 Absorption, Distribution and Excretion

    Absorption

    Bioavailability of a single sublingual tablet was 52%, decreasing to 35% with repeat dosing. 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 the 0.05 to 0.1 ng/mL limit of detection, and were slightly higher in mothers than in their infants.

    Route of Elimination

    Approximately 80% of the administered dose is excreted within 24 hours and only 2% of the dose is eliminated as unchanged drug.

    Volume of Distribution

    Sufentanil has a distribution time of 1.4 minutes and redistribution time of 17.1 minutes. The central volume of distribution after intravenous application of sufentanil is approximately 14 L and the volume of distribution at steady state is approximately 350 L.

    Clearance

    The total plasma clearance after single intravenous administration is about 917 l/min. The clearance of sufentanil in healthy neonates is approximately one-half that in adults and children. The clearance rate of sufentanil can be further reduced by up to a third in neonates with cardiovascular disease.

    This randomized double-blind investigation was designed to study the placental transfer and neonatal effects of epidural sufentanil and fentanyl infused with bupivacaine for labor analgesia. Healthy parturient women (n = 36) received epidural bupivacaine alone (group B) or with fentanyl (group B-F) or sufentanil (group B-S). Group B received a 12-ml bolus of 0.25% bupivacaine followed by a 10 mL/hr infusion of 0.125% bupivacaine. Groups B-F and B-S received a 12-mL bolus of 0.125% bupivacaine with 75 ug fentanyl or 15 ug sufentanil, respectively, followed by 10 mL/hr of 0.125% bupivacaine with fentanyl 1.5 ug/mL or sufentanil 0.25 ug/mL. Maternal venous (MV) and umbilical arterial (UA) and umbilical venous (UV) bupivacaine and opioid plasma concentrations were determined. Neonatal assessment included Apgar scores, umbilical cord blood gas analyses, and neurobehavioral testing at delivery and at 2 and 24 hr of life using the Neurologic and Adaptive Capacity Score (NACS). The mean total dose of fentanyl was 136.6 +/- 13.1 micrograms (SEM), and of sufentanil, 23.8 +/- 1.8 micrograms. Although administered in a ratio of 5.7:1, fentanyl and sufentanil MV plasma concentrations were in the ratio of 27:1. UV/MV ratios were 0.37 for fentanyl and 0.81 for sufentanil. Fentanyl was detected in most UA samples, whereas sufentanil was present in only one sample. Neonatal condition was good and generally similar in all groups, with the exception of a lower NACS at 24 h in group B-F. Although the degree of placental transfer of sufentanil appeared greater than that of fentanyl, lower MV sufentanil concentrations resulted in less fetal exposure to sufentanil. The lower NACS at 24 hr in group B-F may reflect the continued presence of fentanyl in the neonate.

    PMID:7631952 Loftus JR et al; Anesthesiology 83 (2): 300-8 (1995)

    The effects of cirrhosis on the elimination kinetics and plasma protein binding of sufentanil were evaluated in 12 anesthetized patients with uncomplicated cirrhosis and these findings were compared with data from age-matched control anesthetized patients with normal hepatic and renal function. Sufentanil 3 ug/kg was given iv as a bolus injection and venous plasma concentrations were measured at intervals up to 10 hr. The average (+ or - standard deviation) elimination half life was 3.5 + or - 0.9 hr in controls and did not differ in cirrhotics: 4.1 + or - 0.6 hr. The plasma clearance did not differ between the two groups: 11.3 + or - 2.5 ml/min kg in controls and 10.8 + or - 4.6 ml/min kg in cirrhotic patients. The sufentanil free fraction was also similar in controls (8.3 + or - 1.5%) and in cirrhotic patients (9.6 + or - 1.8%). These data suggest that sufentanil in a single dose should have a similar duration of action in patients with uncomplicated cirrhosis and in normal patients.

    PMID:2521279 Chauvin M et al; Anesth Analg 68 (1): 1-4 (1989)

    The in vitro plasma protein binding and distribution in blood of fentanyl and three analogues were studied in rats, dogs and healthy volunteers. In human plasma, 84.4% of fentanyl was bound, 92.5% of sufentanil, 92.1% of alfentanil and 93.6% of lofentanil. Plasma protein binding of the four analgesics was independent of their concentration over the whole therapeutic range. Plasma protein binding of alfentanil was much less pH dependent than that of the three other analgesics. Attention was drawn to the possible contribution of the "acute phase' protein alpha 1-acid glycoprotein (alpha 1-AGP), of lipoproteins and of blood cells to the binding of fentanyl and its analogues in blood.

    PMID:6214227 Meuldermans WE et al; Arch Int Pharmacodyn Ther. 1982 May;257(1):4-19 (1982)

    The aim of this study was to compare the pharmacokinetics of fentanyl, alfentanil, and sufentanil in isoflurane-anesthetized cats. Six adult cats were used. Anesthesia was induced and maintained with isoflurane in oxygen. End-tidal isoflurane concentration was set at 2% and adjusted as required due to spontaneous movement. Fentanyl (10 ug/kg), alfentanil (100 ug/kg), or sufentanil (1 ug/kg) was administered intravenously as a bolus, on separate days. Blood samples were collected immediately before and for 8 hr following drug administration. Plasma drug concentration was determined using liquid chromatography/mass spectrometry. Compartment models were fitted to concentration-time data. A 3-compartment model best fitted the concentration-time data for all drugs, except for 1 cat in the sufentanil group (excluded from analysis). The volume of the central compartment and the volume of distribution at steady-state (L/kg) [mean +/- SEM (range)], the clearance (mL/min/kg) [harmonic mean +/- pseudo-SD (range)], and the terminal half-life (min) [median (range)] were 0.25 +/- 0.04 (0.09-0.34), 2.18 +/- 0.16 (1.79-2.83), 18.6 +/- 5.0 (15-29.8), and 151 (115-211) for fentanyl; 0.10 +/- 0.01 (0.07-0.14), 0.89 +/- 0.16 (0.68-1.83), 11.6 +/- 2.6 (9.2-15.8), and 144 (118-501) for alfentanil; and 0.06 +/- 0.01 (0.04-0.10), 0.77 +/- 0.07 (0.63-0.99), 17.6 +/- 4.3 (13.9-24.3), and 54 (46-76) for sufentanil. Differences in clearance and volume of distribution result in similar terminal half-lives for fentanyl and alfentanil, longer than for sufentanil.

    PMID:23895731 Pypendop BH et al; J Vet Pharmacol Ther 37 (1): 13-7 (2014)

    For more Absorption, Distribution and Excretion (Complete) data for Sufentanil (18 total), please visit the HSDB record page.

    5.6 Metabolism/Metabolites

    The liver and small intestine are the major sites of biotransformation. Sufentanil is rapidly metabolized to a number of inactive metabolites, with oxidative N- and O-dealkylation being the major routes of elimination.

    Although the metabolic fate of sufentanil in humans has not been fully characterized, the drug appears to be metabolized mainly in the liver and small intestine via N-dealkylation at the piperidine nitrogen and O-demethylation. The O-demethylated metabolite appears to have about 10% of the analgesic activity of the unchanged drug. The hepatic extraction ratio of the drug (EH) has been reported to be about 0.72 following IV administration of a single 5-mcg/kg dose.

    American Society of Health-System Pharmacists 2017; Drug Information 2017. Bethesda, MD. 2017, p. 2281

    5.7 Biological Half-Life

    The elimination half-life is 164 minutes in adults when administered intravenously (IV). The elimination half-life of sufentanil is shorter (e.g. 97 +/- 42 minutes) in infants and children, and longer in neonates (e.g. 434 +/- 160 minutes) compared to that of adolescents and adults. After a single administration of a 15 microgram sufentanil sublingual tablet, mean terminal phase half-lives in the range of 6-10 hours have been observed. After multiple administrations, a longer average terminal half-life of up to 18 hours was measured, owing to the higher plasma concentrations of sufentanil achieved after repeated dosing and due to the possibility to quantify these concentrations over a longer time period.

    In adults with normal renal and hepatic function, the plasma half-life in the initial (distribution) phase averages 0.72-1.2 minutes, the plasma half-life in the second (redistribution) phase averages 13.7-17 minutes, and the plasma half-life in the terminal (elimination) phase averages 140-158 minutes. The elimination half-life is longer (434 minutes) in neonates but shorter in infants and children (97 minutes), compared with adults and adolescents.

    American Society of Health-System Pharmacists 2017; Drug Information 2017. Bethesda, MD. 2017, p. 2281

    5.8 Mechanism of Action

    Sufentanil is a synthetic, potent opioid with highly selective binding to -opioid receptors. These receptors are widely distributed in the human brain, spinal cord, and other tissues,. In general, opioids decrease cAMP (affecting neural signaling pathways), decrease neurotransmitter release, and cause membrane hyperpolarization, all of which contribute to the relief of painful symptoms. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic neural transmission via G-proteins that activate effector proteins. Binding of the opiate receptor leads to the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP, located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. The release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is then inhibited. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist), also preventing neurotransmitter release. Sufentanil and other opioids open calcium-dependent inwardly rectifying potassium channels, resulting in hyperpolarization and reduced neuronal excitability,.

    We determined the binding domains of sufentanil and lofentanil in the mu opioid receptor by comparing their binding affinities to seven mu/delta and six mu/kappa chimeric receptors with those to mu, delta and kappa opioid receptors. TMHs 6 and 7 and the e3 loop of the mu opioid receptor were important for selective binding of sufentanil and lofentanil to the mu over the kappa receptor. TMHs 1-3 and the e1 loop of the mu opioid receptor conferred binding selectivity for sufentanil over the delta receptor. Thus, the region that conferred binding selectivity for sufentanil differs, depending on chimeras used. In addition, the interaction TMHs 1-3 and TMHs 6-7 was crucial for the high affinity binding of these two ligands. These two regions are likely to contain sites of interaction with the ligands or to confer conformations specific to the mu receptor.

    PMID:8612823 Zhu J et al; FEBS Lett 384 (2): 198-202 (1996)

    Opioids are the most effective and widely used drugs in the treatment of severe acute and chronic pain. They act through opioid receptors that belong to the family of G protein-coupled receptors. Three classes of opioid receptors (mu, delta, kappa), expressed in the central and peripheral nervous system, have been identified. The analgesic effect of opioids is mediated through multiple pathways of opioid receptor signaling (e.g., G(i/o) coupling, cAMP inhibition, Ca(++) channel inhibition). The standard exogenous opioid analgesics used in the operating room are fentanyl, sufentanil, morphine, alfentanil, and remifentanil.

    PMID:18685878 Zollner C, Schafer M; Anaesthesist 57 (7): 729-40 (2008)

    API SUPPLIERS

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