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.

Yichang Humanwell Pharmaceuticals Co., Ltd.

Inactive Organization

Jiangsu Nhwa Pharmaceutical Co., Ltd.

Orexo AB

License Organization-

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

Painless gastroscopy is preferred by both patients and physicians, as it minimizes discomfort during the procedure. Alfentanil, a short-acting opioid analgesic, possesses pharmacological properties that make it suitable for inducing analgesia during gastroscopy. However, research on the optimal dosage of alfentanil when used in combination with propofol for gastroscopy is limited. Therefore, this study aimed to investigate the 50% and 95% effective doses (ED50 and ED95, respectively) of alfentanil in combination with propofol for gastroscopy, using Narcotrend monitoring.

METHODS:

Elective gastroscopy was performed in 51 patients aged 18-80 years, with a body mass index of 18-28 kg/m², and American Society of Anesthesiologists Class I or II. Based on their age, they were categorized into the youth group (18-60 years) and the elderly group (61-80 years). The patients were connected to the vital signs monitor and Narcotrend, and propofol was administered intravenously until the Narcotrend index was at Stage C1-C2 (65-74) and had stabilized for 1 min. Following this, alfentanil was administrated (initial dose, 5 µg/kg); if a positive reaction to the gastroscope placement was elicited, the dose was increased to a higher level in the next patient; otherwise, the dose was decreased to a lower level, with a dose gradient of 0.5 µg/kg. Gastroscope insertion was started 90 s later, and the criteria for a positive reaction to gastroscope insertion included coughing, nausea, and/or motor reaction during or within 1 min of gastroscope insertion. The test was stopped if seven folds occurred during the study. The ED50 values with their 95% confidence intervals (CIs) of alfentanil in combination with propofol for the inhibition of gastroscopic placement were calculated.

RESULTS:

Under the sedation conditions induced using alfentanil and propofol and detected using Narcotrend, the ED50 (95% CI) were 5.39 µg/kg (4.76-6.47) in the youth group and 5.69 µg/kg (4.67-6.31) in the elderly group, respectively.

CONCLUSIONS:

The ED50 of alfentanil combined with propofol for gastroscopy under Narcotrend monitoring were 5.39 µg/kg in the youth group and 5.69 µg/kg in the elderly group, respectively.

01 Sep 2025·JOURNAL OF INTERNATIONAL MEDICAL RESEARCH

Safety and efficacy of remimazolam combined with alfentanil in flexible fiberoptic bronchoscopy: A randomized controlled trial

Article

Author: Jiang, Jianxin ; Wu, Yini ; Lv, Yuankai ; You, Minji ; Dai, Hong ; Wang, Faxing ; Wu, Jimin ; Duan, Gongchen

Objective:

The sedation protocol for flexible fiberoptic bronchoscopy has long been a matter of inconclusiveness. The aim of this study was to evaluate the safety and efficacy of remimazolam combined with alfentanil in flexible fiberoptic bronchoscopy and provide insights for optimizing clinical anesthesia strategies.

Methods:

This study was a randomized, single-blind controlled trial. A total of 118 patients who underwent flexible fiberoptic bronchoscopy were randomized into two groups (59 patients per group). Both groups received intravenous alfentanil 10 µg/kg 2 min before sedation treatment, followed by either 0.2 mg/kg remimazolam (Group R) or 2 mg/kg propofol (Group P). During the flexible fiberoptic bronchoscopy, the experimental drugs were administered in patients in each group as needed to maintain the depth of sedation (modified observer’s assessment of alertness/sedation score ≤ 3). The primary outcome was the incidence of hypoxemia. The secondary outcomes included other safety outcomes and effectiveness outcomes.

Results:

A total of 115 participants completed the study. Compared with Group P, the incidence of severe hypoxemia in Group R was lower (3.4% vs. 15.8%, P = 0.029); the incidences of injection pain and hypotension in Group R were lower (10.3% vs. 33.3%, P = 0.003); and the incidences of hypotension, dizziness, and grade of cough in Group R were lower ( P < 0.05). The sedation success rate and sedation success rate at an induced dose were similar between Groups R and P ( P > 0.05). Compared with Group P, sedation recovery time in Group R was shorter, and the operator comfort scores and patient comfort scores in Group R were higher ( P < 0.05).

Conclusions:

Remimazolam, when combined with alfentanil, has shown excellent clinical potential in flexible fiberoptic bronchoscopy. Compared with propofol, it significantly reduced the incidence of severe hypoxemia, injection pain, hypotension, dizziness, and intraoperative coughing while maintaining comparable sedation success rates. It also shortened recovery time and improved both operator and patient comfort scores. These results support remimazolam plus alfentanil as a safe, effective, and well-tolerated alternative sedation regimen in this setting.

01 Sep 2025·VETERINARY ANAESTHESIA AND ANALGESIA

Comparison of fentanyl and alfentanil in combination with atropine for premedication of dogs undergoing radiotherapy

Article

Author: Shuttleworth, Adam ; Franchino, Giovanni ; Loddo, Pietro ; Adami, Chiara

OBJECTIVE:

To evaluate the effects of two opioid-based premedication protocols on propofol requirement, time to recovery and occurrence of post-anaesthetic vocalization, paddling, nystagmus and dysphoria in dogs anaesthetized for radiotherapy.

STUDY DESIGN:

Blinded, randomized, crossover clinical study.

ANIMALS:

A total of 22 client-owned dogs, each serving as their own control.

METHODS:

Dogs were randomly assigned to one of two intravenous premedication protocols on their first radiotherapy session, and the other on their second session. Premedication consisted of atropine (10 μg kg^-1) mixed with equipotent doses of either alfentanil (10 μg kg^-1, group AA) or fentanyl (2.5 μg kg^-1, group FA), followed by propofol induction and maintenance with sevoflurane in oxygen. Cardiorespiratory variables and observation of dysphoria and nystagmus were recorded after premedication and during recovery. Time elapsed from discontinuation of sevoflurane to tracheal extubation, sternal position and walking were also recorded (minutes).

RESULTS:

The proportion of dogs showing dysphoria and nystagmus was not different between treatments at any time point. With both treatments, heart rate (mean ± standard deviation) decreased after premedication (82 ± 27 and 93 ± 27 beats minute^-1 in groups AA and FA, respectively) compared with baseline (117 ± 23 and 112 ± 26 beats minute^-1 in groups AA and FA, respectively; p < 0.001). Propofol dose did not differ between treatments (3.8 ± 1.7 and 4.3 ± 1.3 mg kg^-1 in groups AA and FA, respectively). Time to extubation was shorter with treatment AA (5.3 ± 2.1 minutes) compared with treatment FA (6.2 ± 2.3 minutes; p = 0.049), while time to sternal recumbency and walking did not differ between treatments.

CONCLUSIONS AND CLINICAL RELEVANCE:

Since the two protocols produced comparable clinical effects and were both found suitable for dogs undergoing repeated radiotherapy, fentanyl is recommended over alfentanil in countries where it is licensed.

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.	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

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ChiCTR2200062034 (Pubmed \| BMC Anesthesiol)	Phase 1	-	96	Alfentanil 20 µg/kg	bcsxbbpzys(nsbygnamzr) = tsymnryjwk hoszwkchmy (wqtutepduc ) View more	Positive	13 Aug 2024
				Alfentanil 25 µg/kg	qbgkhanxzz(vtgyqlicun) = ysvtlsqqxc dgnwvdaebz (ljaxbhgmrq )
NCT03359395 (CTgov)	Phase 4	Hypotension	100	Alfentanil (Alfentanil)	ueivayjfdj(kpgmkzahqk) = mjsowbdfhw owabgqryti (wodnbjrggx, 36.968) View more	-	08 Jul 2021
				Placebos (Placebo)	ueivayjfdj(kpgmkzahqk) = nbsyqdanzo owabgqryti (wodnbjrggx, 33.50864) View more
NCT01008059 (CTgov)	Not Applicable	-	6	Alfentanil	vhkfjvzgzw(fqsjxdnbtv) = rlrcdbhine wqfnhqfgpq (szlpndkyni, 15) View more	-	17 May 2019
NCT01094574 (CTgov)	Not Applicable	Pain \| Inflammation	10	Alfentanil (Alfentanil)	kbxsgrybhj(wfstkmtskq) = zorrlcgspm pgapmzpypq (ybwcbhqynr, 0.74) View more	-	24 Feb 2017
				Propranolol (Propranolol)	kbxsgrybhj(wfstkmtskq) = tgzurdnydq pgapmzpypq (ybwcbhqynr, 0.26) View more
NCT00997126 (CTgov)	Phase 4	Sedation	126	propofol (Propofol)	dgmcyjspzk = cogodbwusy wanbeysgcc (uzihamibeg, zwtzvcwclt - rgjjjrhzps) View more	-	27 Jan 2017
				Alfentanil (Alfentanil)	dgmcyjspzk = zbysfwthvx wanbeysgcc (uzihamibeg, stqzpfhitn - mfgwwcvwsr) View more
NCT00672438 (CTgov)	Not Applicable	Pain	242	Alfentanil	rvhrgwhwry(jelzdpxvfl) = wanphgswui mbdvhppyot (ygasgpwllu, ldwkdclazn - vgqmocltic) View more	-	21 Jul 2016
NCT01470170 (CTgov)	Phase 4	Hypoxia	173	Targeted controlled infusion+propofol+Normal saline+Alfentanil (Group1)	fsiogmbntb(bimtssjcbw) = hlvclvjafj sjaudkguuf (jmduzjgckn, 0.4) View more	-	13 Aug 2015
				Targeted controlled infusion+propofol+Normal saline+Alfentanil (Group 3)	fsiogmbntb(bimtssjcbw) = cswsmqkelc sjaudkguuf (jmduzjgckn, 0.4) View more
NCT00997113 (CTgov)	Phase 4	Sedation	20	propofol (Propofol)	ucwsosfrlu(bbnhzaovef) = qagpbhbizh wgbajycbwe (btlibwwhsd, prbsvjklnr - knhtvgykel) View more	-	25 Sep 2014
				propofol+alfentanil (Propofol/Alfentanil)	ucwsosfrlu(bbnhzaovef) = ledxcwrowz wgbajycbwe (btlibwwhsd, kkesavxnui - cogbqlcati) View more
NCT00991809 (0813, CTgov)	Not Applicable	Hyperalgesia	22	Alfentanil (Alfentanil)	nfygwauzny(uujzlrcuyw) = uhfjkdyytp tmvyjwmqws (dhbbtzdhib, wffpahwiwd - gfdhlvohnk) View more	-	14 Oct 2013
				Diphenhydramine (Diphenhydramine)	nfygwauzny(uujzlrcuyw) = ayvzkojvxc tmvyjwmqws (dhbbtzdhib, yzwazmjojv - mrxsywzpft) View more
NCT01436799 (CTgov)	Not Applicable	Brain Ischemia	40	desflurane+Rocuronium+alfentanil (Desflurane)	pgcmjowlxu(kbuenaqdvy) = otwhmngfei yhkviiruum (xmgrdaagbu, 7) View more	-	26 Aug 2013
				propofol+Rocuronium+alfentanil (Propofol)	pgcmjowlxu(kbuenaqdvy) = grdxftqhkd yhkviiruum (xmgrdaagbu, 9.5) View more