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Sufentanil, sold under the brand names Dsuvia and Sufenta, is a synthetic opioid analgesic drug approximately 5 to 10 times more potent than its parent drug, fentanyl, and 500 times as potent as morphine. Structurally, sufentanil differs from fentanyl through the addition of a methoxymethyl group on the piperidine ring (which is believed to reduce duration of action^[2]), and the replacement of the phenyl ring by thiophene. Sufentanil first was synthesized at Janssen Pharmaceutica in 1974.^[3]

Sufentanil is marketed for use by specialist centers^{[clarification needed]} under different trade names, such as Sufenta and Sufentil. Sufentanil with and without lidocaine or mepivacaine is available as a transdermal patch similar to Duragesic in Europe under trade names such as Chronogesic. It is available as a sublingual tablet under the trade name Dsuvia.^[4]

Medical uses

The main use of this medication is in operating suites and critical care where pain relief is required for a short period of time. It also offers properties of sedation and this makes it a good analgesic component of anesthetic regimen during an operation.^[5]

Because of its extremely high potency, it is often used in surgery and post-operative pain management for patients that are heavily opioid dependent/opioid tolerant because of long term opiate use for chronic pain or illicit opiate use. Currently sufentanil is the most potent opioid painkiller available for use in humans. Although more potent narcotic pain medications do exist, all medications stronger than sufentanil are approved for veterinary use only. It is also used in surgery and post operative pain control in patients that are taking high dose buprenorphine for chronic pain because it is the only opioid that has a potency and binding affinity strong enough to displace buprenorphine from the opioid receptors in the central nervous system and provide analgesia.^[6]

In 2018, the Food and Drug Administration (FDA) approved Dsuvia, a sublingual tablet form of the drug, that was developed in a collaboration between AcelRx Pharmaceuticals and the United States Department of Defense for use in battlefield settings where intravenous (IV) treatments may not be readily available.^[7] The decision to approve this new potent synthetic opioid came under criticism from politicians and from the chair of the FDA advisory committee, who fear that the tablets will be easily diverted to the illegal drug market.^[8]

Side effects

It is essential for the administering medical professional to be trained in airway management with readily available airway equipment because the drug causes significant respiratory depression and may cause respiratory arrest if given too rapidly or in too high a dose. Other opioid side effects such as heart rhythm irregularity, blood pressure changes and nausea/vomiting can also be present in patients given this drug and should be dealt with accordingly.

Sufentanil has been associated with extremely rare instances of life-threatening anaphylaxis.^{[citation needed]}

Overdose

Management

Because sufentanil is very potent, practitioners must be prepared to reverse the effects of the drug should the patient exhibit symptoms of overdose such as respiratory depression or respiratory arrest. As for all other opioid-based medications, naloxone (trade name Narcan) is the definitive antidote for overdose. Depending on the amount administered, it can reverse the respiratory depression and, if enough is administered, completely reverse the effects of sufentanil.^[9]^[10]^{[medical citation needed]}

References

^ Shaw, Leslie M. (2001). The clinical toxicology laboratory : contemporary practice of poisoning evaluation. Washington, DC: AACC Press. p. 89. ISBN 9781890883539.
^ Vucković S, Prostran M, Ivanović M, Dosen-Mićović Lj, Todorović Z, Nesić Z, Stojanović R, Divac N, Miković Z (2009). "Fentanyl analogs: structure-activity-relationship study". Curr Med Chem. 16 (9): 2468–2474. PMID 19601792.
^ Niemegeers CJ, Schellekens KH, Van Bever WF, Janssen PA (1976). "Sufentanil, a very potent and extremely safe intravenous morphine-like compound in mice, rats and dogs". Arzneimittel-Forschung. 26 (8): 1551–6. PMID 12772.
^ Silverman, Ed (November 2, 2018). "Despite criticism and concerns, FDA approves a new opioid 10 times more powerful than fentanyl". Pharmalot. Retrieved November 2, 2018.
^ Savoia G, Loreto M, Gravino E (September 2001). "Sufentanil: an overview of its use for acute pain management". Minerva Anestesiologica. 67 (9 Suppl 1): 206–216. PMID 11778119.
^ "Fentanyl Citrate - Drug Summary". pdr.net. Retrieved 23 October 2015.
^ Davio, Kelly (November 5, 2018). "FDA Approves Painkiller Dsuvia Amid Criticism". American Journal of Managed Care.
^ Goodnough, Abby (November 2, 2018). "F.D.A. Approves Powerful New Opioid Despite Warnings of Likely Abuse". The New York Times. Retrieved November 2, 2018.
^ "Sufenta (Sufentanil Citrate Injection) Drug Information: Overdosage and Contraindications - Prescribing Information at RxList". RxList. Retrieved 23 October 2015.
^ "The First and Only Naloxone Auto-Injector EVZIO® (naloxone HCl injection)". evzio.com. Retrieved 23 October 2015.

UpToDate Contents

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1. 周術期に成人に静脈内投与するオピオイド鎮痛薬perioperative uses of intravenous opioids in adults [show details]
…effects of sufentanil are similar to those of other lipophilic opioids . Synergistic effects occur with coadministration of sufentanil and other anesthetic agents . Pharmacokinetics for sufentanil are summarized …
2. 急性周術期疼痛のマネージメントmanagement of acute perioperative pain [show details]
…fentanyl has been associated with the development of acute tolerance . Sufentanil and alfentanil are derivatives of fentanyl. Sufentanil is 10 times more potent than fentanyl, whereas alfentanil has about …
3. Anesthesia and cancer recurrenceanesthesia and cancer recurrence [show details]
…recurrence rates in patients who received intraoperative ketorolac compared with those who received sufentanil, ketamine, or clonidine . In one small prospective trial, 38 patients were randomly assigned to…
4. 全身麻酔：維持general anesthesia maintenance [show details]
…maintenance of general anesthesia are described separately ( and and and ): Remifentanil Fentanyl Sufentanil Alfentanil Hydromorphone Morphine Dexmedetomidine is a highly selective alpha₂…
5. 脊髄麻酔：手技spinal anesthesia technique [show details]
…monitoring are discussed in more detail separately. Fentanyl and sufentanil – Lipid-soluble opioids such as fentanyl (10 to 25 mcg) and sufentanil (2.5 to 10 mcg) are commonly added to intrathecal LA to improve …

English Journal

Abstracts.

Lunn TH.SourceDepartment of Anaesthesiology and Orthopaedic Surgery, Hvidovre University Hospital; Section for Surgical Pathophysiology, Rigshospitalet - Copenhagen University Hospital and The Lundbeck Centre for Fast-Track Hip and Knee Arthroplasty, Copenhagen, Denmark.
Acta anaesthesiologica Scandinavica.Acta Anaesthesiol Scand.2013 Oct;57(9):1207-9. doi: 10.1111/aas.12161. Epub 2013 Jul 19.
BACKGROUND: Total hip and knee arthroplasty (THA and TKA) are frequently performed surgical procedures with excellent long-term functional outcomes. However, pain is pronounced in the early post-operative phase, especially after TKA. Glucocorticoids have proven to relieve post-operative pain, but a
PMID 23865612

Effects of caudal sufentanil supplemented with levobupivacaine on blocking spermatic cord traction response in pediatric orchidopexy.

Wang T, Xiang Q, Liu F, Wang G, Liu Y, Zhong L.SourceDepartment of Anesthesia, Wuhan Children's Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.
Journal of anesthesia.J Anesth.2013 Oct;27(5):650-6. doi: 10.1007/s00540-013-1613-9. Epub 2013 Apr 23.
PURPOSES: Caudal block is one of the most commonly used anesthetic techniques in subumbilical and genitourinary procedures. However, traditional administration of caudal levobupivacaine was inadequate on blocking peritoneal response during spermatic cord traction. The aim of this study was to evalua
PMID 23608774

Intranasal sufentanil/ketamine analgesia in children.

Nielsen BN, Friis SM, Rømsing J, Schmiegelow K, Anderson BJ, Ferreirós N, Labocha S, Henneberg SW.SourceDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark; Paediatric Pain Service, Department of Anaesthesiology, The Juliane Marie Centre, Copenhagen University Hospital Rigshospitalet, Copenhagen, Denmark.
Paediatric anaesthesia.Paediatr Anaesth.2013 Oct 1. doi: 10.1111/pan.12268. [Epub ahead of print]
BACKGROUND: The management of procedural pain in children ranges from physical restraint to pharmacological interventions. Pediatric formulations that permit accurate dosing, are accepted by children and a have a rapid onset of analgesia are lacking.OBJECTIVES: To investigate a pediatric formulation
PMID 24118506

Japanese Journal

By regulating miR-182-5p/BCL10/CYCS, sufentanil reduces the apoptosis of umbilical cord mesenchymal stem cells caused by ropivacaine

Li Lisha,Sun Yan,Zhang Na,Qiu Xuemin,Wang Ling,Luo Qingyan
BioScience Trends 13(1), 49-57, 2019
… Sufentanil is a type of opioid analgesic and is usually used to facilitate painless labor in combination with the local anesthetic ropivacaine. … One aim of the current study was to investigate the effects of sufentanil and ropivacaine on umbilical cord mesenchymal stem cells (UCMSCs). … A second aim of this study was to determine whether sufentanil attenuated the cytotoxicity of ropivacaine in vitro. …
NAID 130007613103

Effects of pretreatment with a small dose of dexmedetomidine on sufentanil-induced cough during anesthetic induction

SUN Shen,HUANG Shao-qiang
Journal of anesthesia 27(1), 25-28, 2013-02-20
NAID 10031165378

Circumstantial and toxicological features of deaths from self-administered intravenous anesthetic/narcotic agents

HAYASHI Takahito,BUSCHMANN Claas,RIESSELMANN Benno,ROSCHER Sonja,TSOKOS Michael
Forensic Science, Medicine, and Pathology 9(2), 138-144, 2013
… Despite suspected usage, remifentanil was not detected due to its rapid metabolism by elastases in one case, and sufentanil was undetectable due to putrefaction in another, but death was attributed to their potent respiratory depressant effects without respiratory assistance. …
NAID 120005447080

Related Pictures

★リンクテーブル★

リンク元	「オピオイド」「スフェンタニル」
拡張検索	「sufentanil citrate」

「オピオイド」

Sufentanil
Clinical data
Trade names	Dsuvia, Sufenta
Synonyms	R30730
AHFS/Drugs.com	Monograph
License data	EU EMA: by INN;
Pregnancy; category	US: C (Risk not ruled out) ; ;
Routes of; administration	IV, IM, SQ, epidural, intrathecal, transdermal patch (in clinical trials)
ATC code	N01AH03 (WHO) ;
Legal status
Legal status	AU: S8 (Controlled) ; CA: Schedule I ; DE: Anlage III (Special prescription form required) ; UK: Class A ; US: Schedule II ; In general: ℞ (Prescription only);
Pharmacokinetic data
Elimination half-life	162 minutes
Duration of action	30 to 60 min
Identifiers
	IUPAC name N-[4-(Methoxymethyl)-1-(2-thiofuran-2-ylethyl)-4-piperidyl]-N-phenylpropanamide;
CAS Number	56030-54-7 ;
PubChem CID	41693;
IUPHAR/BPS	3534;
DrugBank	DB00708 ;
ChemSpider	38043 ;
UNII	AFE2YW0IIZ;
KEGG	D05938 ;
ChEBI	CHEBI:9316 ;
ChEMBL	ChEMBL658 ;
CompTox Dashboard (EPA)	DTXSID6023604 ;
ECHA InfoCard	100.168.858
Chemical and physical data
Formula	C22H30N2O2S
Molar mass	386.552 g/mol g·mol−1
3D model (JSmol)	Interactive image;
Melting point	97 °C (207 °F)
	SMILES O=C(N(c1ccccc1)C2(COC)CCN(CC2)CCc3sccc3)CC;
	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 ; Key:GGCSSNBKKAUURC-UHFFFAOYSA-N ;
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　　[★]

英: opioid
同: 類麻薬
関: オピオイド受容体

オピオイド受容体に結合するモルフィン様物質のことを指す。

内因性のオピオイドペプチドが発見され、これらは内因性オピオイドペプチドと呼ばれるようになった。

作用

縮瞳

モルフィンと多くのμ,κアゴニストは瞳孔の縮小を引き起こす。これは瞳孔を支配する副交感神経の興奮による。μアゴニストを中毒量投与すると縮瞳し、pinpoints pupupilsはpathognomonicである。(GOO.559)