Delving into the Latest Updates on Alfentanil Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Alfentanil hydrochloride (USP), Alfentanil sublingual, Alfentanyl

+ [7]

Target

Opioid receptors

Action

agonists

Mechanism

Opioid receptors agonists(Opioid receptors agonists)

Therapeutic Areas

Other Diseases

Active Indication

Anesthesia

Inactive Indication

Acute PainAnalgesia

Originator Organization

Akorn, Inc.

Active Organization

Rising Pharmaceuticals, Inc.Startup

Yichang Humanwell Pharmaceuticals Co., Ltd.

Inactive Organization

Jiangsu Nhwa Pharmaceutical Co., Ltd.

Orexo AB

Drug Highest PhaseApproved

First Approval Date

United States (29 Dec 1986),

Anesthesia

RegulationOrphan Drug (United States), Priority Review (China)

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Structure/Sequence

Molecular FormulaC21H35ClN6O4

InChIKeyYYESXRRYBUERKF-UHFFFAOYSA-N

CAS Registry70879-28-6

Currently, there is concern about food products to which new psychoactive substances (NPS) have been added illegally. However, rapid, high-sensitivity, and high-throughput screening methods for such harmful substances have not been reported yet. In this study, a high-throughput non-targeted screening strategy was developed based on UHPLC-Q/Orbitrap. First, optimized pretreatment methods for typical high-risk matrices were established. Second, an accurate, efficient, and scalable high resolution mass spectrometry database containing 206 NPS and related compounds was constructed. The fragmentation pathways of three different types of fentanyl-related compounds were then systematically investigated to enhance compound identification. Additionally, a non-targeted screening strategy was developed using warning ions derived from 24 fentanyl-related compounds, streamlining the identification of NPS. This strategy was applied to 100 food samples with possible illegal additives and demonstrated its effectiveness. In summary, this study provides robust technical support for regulatory authorities in combating the illegal addition of food products.

01 May 2025·ANESTHESIA AND ANALGESIA

A New Method for Comprehensive Analysis of Benzodiazepine, Opioid, and Propofol Interactions and Dose Selection Rationales in Gastrointestinal Endoscopy Sedation

Article

Author: Wang, Hsin-Yi ; Ting, Chien-Kun ; Tsou, Mei-Yung ; Liou, Jing-Yang ; Kuo, I-Ting ; Chang, Weng-Kuei

BACKGROUND::

The aim of this study was to explore a new method for determining optimal dosing regimens for combinations of propofol, midazolam, and an opioid to achieve rapid on- and off-set of deep sedation.

METHODS::

We simulated 16 published dosing regimens using a well-validated pharmacodynamic model. The study was divided into 2 parts. First, the regimen that best provided deep sedation and rapid recovery was selected. A deep sedation-time area-under-the-curve (AUC) method was used to compare published dosing regimens; a higher AUC indicated better sedation and faster recovery. Second, subgroup analysis of the best-performing dosing regimen was undertaken better to understand how each drug affected patient recovery.

RESULTS::

The AUC method identified a combination of midazolam 1 mg, alfentanil 500 µg, and propofol target infusion effect-site concentration (Ce) 2 µg mL−1 as the optimal regimen (P < .01). Propofol correlated with high probability of sedation and increased AUC (R2 = 0.53), whereas midazolam had a significant impact on time to return of consciousness (R2 = 0.86). Subgroup analysis indicated that regimens consisting of a fixed dose of alfentanil and either 5 µg mL−1 Ce propofol, or 1 mg midazolam with 3–5 µg mL−1 Ce of propofol, or 2 mg midazolam with 2 µg mL−1 Ce propofol provided adequate sedation and rapid recovery. Midazolam >3 mg greatly prolonged recovery.

CONCLUSIONS::

This study used a clinically relevant method and model simulation to determine suitable sedation regimens for use in gastrointestinal endoscopy. A balanced propofol, midazolam, and an opioid should be used. The AUC method was capable of providing objective assessments for model selection.

01 May 2025·JOURNAL OF CARDIOTHORACIC AND VASCULAR ANESTHESIA

Application of Alfentanil Combined With Dexmedetomidine for Conscious Sedation of Patients During Transesophageal Echocardiography Examination

Article

Author: Huang, Yushan ; Wang, Jiagao ; Xiao, Bin ; Zhao, Xiang ; RanRan ; Zhuang, Zelong

OBJECTIVES:

To investigate the efficacy and safety of combining alfentanil with dexmedetomidine for conscious sedation in outpatients undergoing transesophageal echocardiography (TEE).

DESIGN:

Prospective, randomized, double-blind clinical trial.

SETTING:

University-affiliated teaching hospital.

PARTICIPANTS:

We recruited 80 patients scheduled to undergo transesophageal echocardiography examinations from May 2023 to July 2023.

INTERVENTIONS:

Eighty patients were randomly assigned into 2 groups, namely, the alfentanil + dexmedetomidine (AD) group (n = 40) and the oropharyngeal topical anesthesia with dyclonine + midazolam + dexmedetomidine (MD) group (n = 40).

MEASUREMENTS AND MAIN RESULTS:

Suppression of the patient's pharyngeal reflexes was assessed, and the hemodynamic parameters, along with the incidence of intraoperative adverse events, were also documented. The primary outcome was the initial sedation success rate, defined as achieving a pharyngeal reflex grade of less than 3, no excessive sedation (Ramsay sedation scores >4), and no serious adverse effects. This rate was significantly higher in the AD group (85%) compared with the MD group (35%) (p < .001). Compared with the MD group (47.5%), the incidence of hypotension in AD group (25.0%) decreased significantly (p < .05). Although the incidence of respiratory depression in AD group (42.5%) was higher than that in MD group (15.0%) (p < .01), no hypoxia and asphyxia occurred in either group. The recovery time of AD group (626.25 ± 295.80) was significantly shorter than that of MD group (768.33 ± 310.43) (p < .05). No serious complications occurred in either group.

CONCLUSIONS:

Intravenous alfentanil combined with dexmedetomidine effectively inhibits pharyngeal reflexes and demonstrates a favorable safety profile, with fewer incidents of hypotension but a higher incidence of manageable respiratory depression compared with the MD protocol.

2

News (Medical) associated with Alfentanil Hydrochloride

14 Mar 2025

·www.echemi.com

5 Key Updates on China's Fentanyl Control Amid US Tariffs

On February 1st, the United States announced a 10% tariff on products imported from China, citing concerns over the fentanyl crisis. In response, a spokesperson from the Ministry of Public Security emphasized that China maintains one of the strictest drug control policies in the world. As a signatory to the three UN drug control conventions, China has consistently upheld its international obligations and actively collaborates with countries, including the US, on drug enforcement efforts. In 2019, China took a humanitarian step by becoming the first country to classify all fentanyl-related substances under stringent controls, responding to US requests. Since this classification, China has not received reports of these substances being seized in the US. On March 12th, the National Medical Products Administration (NMPA) shared insights regarding China's management of fentanyl substances through a recently released white paper. The spokesperson addressed concerns about the production and export of fentanyl-related pharmaceuticals. Currently, four fentanyl-related drugs are approved for clinical use in China: fentanyl, sufentanil, remifentanil, and alfentanil. Three companies have been authorized to produce raw materials, while five are permitted to manufacture formulations. In 2024, China produced 100 kilograms of fentanyl raw materials, primarily for domestic medical use and export, with only 12.3 kilograms exported to countries like South Korea, Vietnam, and the Philippines. Notably, China has never exported fentanyl products to North America. All fentanyl-related drugs in China are classified as controlled narcotics, subjected to stringent regulations. The production and distribution of these drugs are closely monitored, with specific companies designated for manufacturing and fixed sales channels established. Export controls require permits, and international verification ensures the legality of trade before issuing export licenses. The NMPA will continue to enhance the supervision of fentanyl-related drug production and strictly regulate exports to prevent illegal channels and misuse, ensuring that medical needs are met responsibly.

Drug Approval

21 Jan 2025

·www.echemi.com

Humanwell Healthcare Secures Major Investment: A New Era Begins with Strategic Backing

After a three-month hiatus, leading domestic anesthetics producer Humanwell Healthcare has officially been "acquired" by a state-backed entity. On January 15, the company announced that it had signed a restructuring investment agreement with Zhaoshang Innovation Technology Group Co., Ltd. and its management team. This collaboration involves an investment of ¥11.8 billion, positioning Zhaoshang Innovation as the new controlling shareholder, with a 23.70% stake in Humanwell Healthcare. The restructuring investment will be executed in two phases. The first phase, covering 60% of the investment, will be paid upon the approval of the restructuring plan by the Wuhan Intermediate People’s Court. The remaining 40% will be paid after the completion of stock and voting rights transfers. Once this restructuring plan is finalized, Humanwell Healthcare will officially transition to state-owned control, a move that has significantly boosted its stock price, reaching ¥23.6 per share and a market capitalization of ¥38.52 billion. A Shift in Leadership: Hope for the "Anesthetic King" Founded in 1993, Humanwell Healthcare was once the dominant force in the anesthetic drugs sector. However, it has faced unprecedented challenges due to its former major shareholder, Dandai Technology, being mired in a debt crisis. Previously, six potential restructuring investors had passed the initial review, including three state-owned enterprises and three large local state-owned enterprises. Dandai Technology’s 23.7% stake in Humanwell Healthcare is currently frozen due to judicial actions. The entry of Zhaoshang Innovation brings a glimmer of hope, with the investment structured in three parts: Direct acquisition of 6% of Humanwell Healthcare’s shares. Indirect acquisition of another 6% through a new limited partnership in the Donghu New Technology Development Zone, with Zhaoshang Innovation as the general partner. Trust plan acquiring 11.70% of shares, with all voting rights delegated to Zhaoshang Innovation. Zhaoshang Innovation is controlled by China Merchants Group, a significant state-owned enterprise headquartered in Hong Kong. In 2023, China Merchants Group reported revenues of ¥924.4 billion and a net profit of ¥191.1 billion, showcasing its robust financial standing. Strategic Investment Amid Market Challenges Zhaoshang Innovation's substantial investment indicates its strategic interest in Humanwell Healthcare's industry-leading position in the pharmaceutical sector. Humanwell Healthcare is one of the few companies capable of producing a full range of fentanyl products and has established a strong foothold in various segments, including anesthetics and steroid hormones. According to the latest data, Humanwell Healthcare holds a 25.9% market share in the anesthetics market, making it the leading player. Its products, including alfentanil and hydromorphone, have a 100% market share, illustrating its dominance. In the past five years, Humanwell Healthcare has invested ¥4.6 billion in research and development, reflecting a commitment to innovation. In 2023, R&D expenses surpassed ¥1 billion, with a 9.2% increase in the first three quarters of 2024. The company has received approval for 1 traditional Chinese medicine and 17 chemical drug products, indicating a robust pipeline for future growth. Despite these positive developments, challenges remain. The competitive landscape is fierce, and the company must ensure that its R&D investments yield proportional returns. The support from Zhaoshang Innovation may provide the necessary impetus for Humanwell Healthcare to navigate these challenges successfully and emerge stronger. With Zhaoshang Innovation taking a controlling stake, Humanwell Healthcare's ownership issue has reached a significant resolution. This strategic investment from a state-owned entity sends positive signals to the market. However, the company still faces challenges related to market competition and R&D efficiency. Observers will be keen to see if Humanwell Healthcare can leverage this new partnership to overcome its obstacles and achieve a successful turnaround.

AcquisitionDrug Approval

100 Deals associated with Alfentanil Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00835	Alfentanil Hydrochloride	N01AH02	DB00802

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Anesthesia	United States	Rising Pharmaceuticals, Inc.Startup	29 Dec 1986

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Analgesia	Phase 3	China	Jiangsu Nhwa Pharmaceutical Co., Ltd.	06 Jun 2018
Acute Pain	Phase 3	Czechia	Orexo AB	08 Oct 2012

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ChiCTR2200062034 (Pubmed \| BMC Anesthesiol)	Phase 1	-	96	Alfentanil 20 µg/kg	mvsbadfgxz(nvithqilho) = gflmnwzyee lexjuxdmjw (wwpiakbwsf ) View more	Positive	13 Aug 2024
				Alfentanil 25 µg/kg	axyhtxfgdl(mhlnvqnghy) = tfcqnbfhvv lgauzbvnjh (ilpcjftsru )
NCT03359395 (CTgov)	Phase 4	-	100	Alfentanil (Alfentanil)	nldnnaebxd(bkcnbszgtd) = wnfzhgwdab tjthaybidx (pczvnxitrs, 36.968) View more	-	08 Jul 2021
				Placebos (Placebo)	nldnnaebxd(bkcnbszgtd) = bzxmrbdnlg tjthaybidx (pczvnxitrs, 33.50864) View more
NCT01008059 (CTgov)	Not Applicable	-	6	Alfentanil	rvmmnqfygg(nfkbdpltuy) = iugdjoxnby ndghuiykaz (ogjbtrojmw, 15) View more	-	17 May 2019
NCT01094574 (CTgov)	Not Applicable	Pain \| Inflammation	10	Alfentanil (Alfentanil)	isgxartwdl(wlkpdhhiuq) = ifxzvobylm nslzyrjdjo (cggsfkejiv, 0.74) View more	-	24 Feb 2017
				Propranolol (Propranolol)	isgxartwdl(wlkpdhhiuq) = ysoxngkvlf nslzyrjdjo (cggsfkejiv, 0.26) View more
NCT00997126 (CTgov)	Phase 4	Sedation	126	Propofol (Propofol)	kmumfwurqf = mgkfosiomh nxofgqzvzp (louxqonxdc, hjlmitvcrr - ekmmuzxsyi) View more	-	27 Jan 2017
				Alfentanil (Alfentanil)	kmumfwurqf = bllbkyjbsc nxofgqzvzp (louxqonxdc, ldclsworrv - natjdcqrtz) View more
NCT00672438 (CTgov)	Not Applicable	Pain	242	Alfentanil	blfmlcnazw(ctnlrwvnrx) = kfovjzbkem asypzmyrbs (glwfgezftq, dneicjwvec - amkqhwwyuw) View more	-	21 Jul 2016
NCT01470170 (CTgov)	Phase 4	Hypoxia	173	Targeted controlled infusion+Propofol+normal saline+Alfentanil (Group1)	tnkmxypxur(dpqqntmhhc) = nawdoltmkr ogvjigockn (woylgkexdv, 0.4) View more	-	13 Aug 2015
				Targeted controlled infusion+Propofol+normal saline+Alfentanil (Group 3)	tnkmxypxur(dpqqntmhhc) = tpvdrbzwjx ogvjigockn (woylgkexdv, 0.4) View more
NCT00997113 (CTgov)	Phase 4	Sedation	20	propofol (Propofol)	bcdwszigkm(lnfkccchdu) = padqhjhjkw hyorpmzkpp (qdzqjptuvh, muswqbxaey - tpdfkotpnz) View more	-	25 Sep 2014
				propofol+alfentanil (Propofol/Alfentanil)	bcdwszigkm(lnfkccchdu) = mncfmyvlrv hyorpmzkpp (qdzqjptuvh, opaiwqjznd - xbbfzmwfgg) View more
NCT00538850 (CTgov)	Phase 3	Cancer Pain \| Neoplasms	130	Placebo+Fentanyl sublingual spray	uzdzcietxp(gkazmjtfct) = aisuzpsfty yezumnuumq (iwavubppyp, 458.8) View more	-	05 Mar 2014
Pubmed \| Clin J Pain	Not Applicable	Pain	-	Alfentanil 15 mcg/kg	pgsxhsseuq(bfwaodfnex) = sdcayillem ntphhheanv (lqejaphiof, ±26.5)	-	01 Jan 2014