 redirect アルフェンタニル

(合成麻薬性鎮痛薬;神経遮断麻酔薬)ルフェンタニル

関: alfentanil hydrochloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/15 09:03:57」(JST)

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Alfentanil (R-39209, trade name Alfenta, Rapifen in Australia) is a potent but short-acting synthetic opioid analgesic drug, used for anaesthesia in surgery. It is an analogue of fentanyl with around 1/4 to 1/10 the potency of fentanyl and around 1/3 of the duration of action, but with an onset of effects 4x faster than fentanyl.^[2] Alfentanil has a pKa of approximately 6.5, which leads to a very high proportion of the drug being uncharged at physiologic pH. This unique characteristic is responsible for its rapid onset. It is an agonist at mu opioid receptors.

While alfentanil tends to cause fewer cardiovascular complications than other similar drugs such as fentanyl and remifentanil, it tends to give stronger respiratory depression and so requires careful monitoring of breathing and vital signs. Almost exclusively used by anesthesia providers during portions of a case where quick, fast acting (though not long lasting) pain control is needed (i.e. during a nerve block, head pinning etc..) Alfentanil is administered by the parenteral (injected) route for fast onset of effects and precise control of dosage.

Alfentanil is a restricted drug which is classified as Schedule II in the USA, according to the U.S. DEA website.^[3]

Alfentanil was discovered at Janssen Pharmaceutica in 1976.

Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.^[4]

References

^ Shaw, Leslie M. (2001). The clinical toxicology laboratory : contemporary practice of poisoning evaluation. Washington, DC: AACC Press. p. 89. ISBN 9781890883539.
^ Jacob Mathew, J. Kendall Killgore. Methods for the synthesis of alfentanil, sufentanil, and remifentanil. US Patent 7,208,604
^ From DEA website, accessed 23 Jan 2007
^ Jane Mounteney, Isabelle Giraudon, Gleb Denissov, Paul Griffiths (July 2015). "Fentanyls: Are we missing the signs? Highly potent and on the rise in Europe.". The international journal of drug policy. 26 (7): 626–631. doi:10.1016/j.drugpo.2015.04.003. PMID 25976511.

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1. 術後疼痛のマネージメント management of postoperative pain
2. 成人における処置時の鎮静 procedural sedation in adults
3. 危篤状態の成人における鎮静鎮痛剤：特性、投与レジメン、および副作用 sedative analgesic medications in critically ill adults properties dosage regimens and adverse effects
4. 陣痛および分娩に対する硬膜外・脊椎麻酔：薬 neuraxial analgesia and anesthesia for labor and delivery drugs
5. 高齢患者における緊急気道マネージメント emergency airway management in the geriatric patient

English Journal

Analgesia without sedatives during colonoscopies: worth considering?

Eberl S, Preckel B, Fockens P, Hollmann MW.SourceDepartment of Anesthesiology, Academic Medical Center, University of Amsterdam, Meibergdreef 9, 1100 DD, Amsterdam, The Netherlands, S.Eberl@amc.uva.nl.
Techniques in coloproctology.Tech Coloproctol.2012 Aug;16(4):271-6. Epub 2012 Jun 6.
Colonoscopy is a proven method for bowel cancer screening and is often experienced as a painful procedure. Today, there are two main strategies to facilitate colonoscopy. First, deep sedation results in satisfied patients but increases sedation-associated risks and raises costs for healthcare provid
PMID 22669482

Miniaturized hollow fibre assisted liquid-phase microextraction and gas chromatography for determination of trace concentration of sufentanil and alfentanil in biological samples.

Fakhari AR, Tabani H, Nojavan S.SourceDepartment of Chemistry, Faculty of Sciences, Shahid Beheshti University, G.C., PO Box 19396-4716, Evin, Tehran, Iran.
Drug testing and analysis.Drug Test Anal.2012 Jul 12. doi: 10.1002/dta.1387. [Epub ahead of print]
A simple and highly sensitive method that involves miniaturized hollow fibre assisted liquid-phase microextraction with gas chromatography-flame ionization detector was developed for the determination of trace concentration of sufentanil and alfentanil in biological samples. These drugs were extract
PMID 22786780

Japanese Journal

The effect of alfentanil versus ketamine on the intubation condition and hemodynamics with low-dose rocuronium in children

KIM Ji Young,LEE Jong Seok,PARK Hee Yeon,KIM Yong Beom,KWON Youngjun,KWAK Hyun Jeong
Journal of anesthesia 27(1), 7-11, 2013-02-20
NAID 10031165375

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
… Alongside the 2 propofol-detected cases, there was one case where a higher-than-therapeutic level of piritramide and a therapeutic level of alfentanil was identified. …
NAID 120005447080

Highly sensitive gas chromatographic-mass spectrometric screening method for the determination of picogram levels of fentanyl, sufentanil and alfentanil and their major metabolites in urine of opioid exposed workers

VAN NIMMEN Nadine F. J.,POELS Katrien L. C.,VEULEMANS Hendrik A. F.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 804(2), 375-387, 2004-05-25
NAID 10016550256

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Alfentanil
Systematic (IUPAC) name
	N-{1-[2-(4-ethyl-5-oxo-4,5-dihydro-1H-1,2,3,4-tetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl}-N-phenylpropanamide
Clinical data
Trade names	Alfenta
AHFS/Drugs.com	Micromedex Detailed Consumer Information
MedlinePlus	a601130
Legal status	AU: Controlled (S8); DE: Anlage III; UK: Class A; US: Schedule II;
Routes of; administration	Intravenous
Pharmacokinetic data
Bioavailability	100%
Protein binding	92%
Metabolism	Hepatic
Biological half-life	90–111 minutes
Duration of action	15 min
Identifiers
CAS Registry Number	71195-58-9
ATC code	N01AH02
PubChem	CID: 51263
IUPHAR/BPS	7108
DrugBank	DB00802
ChemSpider	46451
UNII	1N74HM2BS7
KEGG	D07122
ChEBI	CHEBI:2569
ChEMBL	CHEMBL634
Chemical data
Formula	C21H32N6O3
Molecular mass	416.517 g/mol
	SMILES O=C1N(\N=N/N1CC)CCN3CCC(N(c2ccccc2)C(=O)CC)(CC3)COC ;
	InChI InChI=1S/C21H32N6O3/c1-4-19(28)27(18-9-7-6-8-10-18)21(17-30-3)11-13-24(14-12-21)15-16-26-20(29)25(5-2)22-23-26/h6-10H,4-5,11-17H2,1-3H3 ; Key:IDBPHNDTYPBSNI-UHFFFAOYSA-N ;
Physical data
Melting point	140.8 °C (285.4 °F)
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英: alfentanil、alfentanil hydrochloride
関: 塩酸アルフェンタニル

-alfentanil

[1] Shaw, Leslie M. (2001). The clinical toxicology laboratory : contemporary practice of poisoning evaluation. Washington, DC: AACC Press. p. 89. ISBN 9781890883539.

[2] Jacob Mathew, J. Kendall Killgore. Methods for the synthesis of alfentanil, sufentanil, and remifentanil. US Patent 7,208,604

[http:.2F.2Fwww.deadiversion.usdoj.gov.2Fschedules.2Flistby_sched.2Fsched2.htm-3] From DEA website, accessed 23 Jan 2007

[4] Jane Mounteney, Isabelle Giraudon, Gleb Denissov, Paul Griffiths (July 2015). "Fentanyls: Are we missing the signs? Highly potent and on the rise in Europe.". The international journal of drug policy. 26 (7): 626–631. doi:10.1016/j.drugpo.2015.04.003. PMID 25976511.

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alfentanil