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

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.

24 Jul 2025·Asian journal of anesthesiology

Effect of Sedation/Analgesia During Colonoscope on Abdominal Pain After Examination.

Article

Author: Lin, Chih-Peng ; Cheng, Ya-Jung ; Lin, Fong-Sheng ; Sun, Wei-Zen

BACKGROUND:

Sedation/analgesia (S/A) is widely used to relieve patients' anxiety and discomfort during colonoscopy. Their effects on abdominal pain after colonoscopy have never been fully investigated.

METHODS:

The prospective study consecutively recruited 494 healthy patients having a screen colonoscopy examination as part of their health checkup. They were divided into two groups based on individuals' decision to receive sedation and analgesia or not. In the S/A group, 374 patients received midazolam and alfentanil during colonoscopy with standard monitoring, while in the non-sedation/analgesia (NSA) group, 120 patients received no analgesics. Severity and duration of abdominal pain (ordinal scale: 1 = none, 4 = severe) were assessed at the end of stay in the postanesthetic care unit (the S/A group) or examination room (the NSA group) and before discharge. Side effects S/A during (hypotension, hypoxemia) and after (nausea, vomiting, dizziness) colonoscopy were also recorded. All patients were closely monitored during the whole course of the health check-up package.

RESULTS:

The mean doses of midazolam and alfentanil were 4.06 mg and 813.12 μg, respectively. Patients in the NSA group had two-fold risks of moderate to severe abdominal pain compared to those in the S/ A group (16.67% vs. 9.36%, odds ratio = 1.937, 95% confidence interval: 1.010-3.625). The NSA group also had a higher incidence of abdominal pain 120 minutes after examination (33.33% vs. 16.04%, P < 0.001). Duration of abdominal pain in those patients who did have abdominal pain was longer in the S/ A group than in the NSA group (153.3 ± 49.9 vs. 118.7 ± 47.5 minutes, P < 0.001). The incidence of hypotension and hypoxemia in the group S/A was 5.6% and 2.9%, respectively. More patients in the S/ A group felt dizzy or sleepy than those in the NSA group (14.7% vs. 3.3%, P < 0.001). The incidence of nausea and vomiting was similar between the two groups.

CONCLUSION:

Optimal S/A with midazolam and alfentanil decreases the severity and duration of postcolonoscopic abdominal pain.

19 Jul 2025·BMC Anesthesiology

The median Effective Dose (ED₅₀) and the 95% Effective Dose (ED₉₅) of alfentanil in inhibiting responses to cervical dilation when combined with ciprofol during hysteroscopic procedure: a prospective, double-blind, dose-finding clinical study.

Article

Author: Gao, Run ; Shen, Jian-Jun ; Xu, Li-Li ; Li, Shu-Xi ; Xing, Li ; Fu, Jin-Peng ; Chen, Xin-Zhong ; Zhou, Yan-Hong

BACKGROUND:

Alfentanil, a short-acting µ opioid receptor agonist, has recently been confirmed that when combined with propofol for daytime hysteroscopy, it provided more stable hemodynamics compared with sufentanil, and has a lower incidence of hypoxemia and postoperative nausea and vomiting. The object of the trial was to determine the median effective dose (ED₅₀) and the 95% effective dose (ED₉₅) of alfentanil in inhibiting responses to cervical dilation when combined with ciprofol and explore the effect of alfentanil on reducing ciprofol requirement during hysteroscopy.

METHODS:

One hundred and forty patients scheduled hysteroscopy under monitored anesthesia care were randomized to receive a bolus of 8 µg·kg^-1, 10 µg·kg^-1, 12 µg·kg^-1, 14 µg·kg^-1 intravenous alfentanil or 0.15 µg⋅kg^-1 intravenous sufentanil followed by a bolus of 0.5 mg·kg^-1 ciprofol. Whether there was loss of response to cervical dilation or not in each patient was recorded. We used the probit analysis to determine ED₅₀ and ED₉₅ of alfentanil in inhibiting responses to cervical dilation when combined with ciprofol. The requirement of ciprofol, the emergence time, the visual analogue scale score of pain at five time points, and the incidence of adverse events were recorded.

RESULTS:

The calculated ED₅₀ and ED₉₅ of alfentanil were 9.73 [95% CI 8.57 to 10.56] µg·kg^-1 and 15.02 [95% CI 13.57 to 18.12] µg·kg^-1, respectively. Ciprofol requirements were lower in patients given 10 µg·kg^-1 (0.795 [ 0.707 to 0.889] mg·kg^-1), 12 µg·kg^-1 (0.799 [0.601 to 0.913] mg·kg^-1), and 14 µg·kg^-1 (0.789 [0.660 to 0.968] mg·kg^-1) alfentanil than those given 8 µg·kg^-1 alfentanil (1.082 [ 0.853 to 1.271] mg·kg^-1) alfentanil and 0.15 µg⋅kg^-1 sufentanil (1.046 [0.861 to 1.427] mg·kg^-1) (P < 0.001). Emergence time was lower in patients given 10 µg·kg^-1 (0.9 [0.8 to 1.2] min), 12 µg·kg^-1 (0.8 [0.6 to 1.0] min) than those given 8 µg·kg^-1 (1.9 [1.0 to 2.8] min) and 14 µg·kg^-1 (1.5 [1.0 to 2.3] min) alfentanil, and 0.15 µg·kg^-1 sufentanil (1.4 [1.0 to 2.0] min) (P < 0.001). The visual analogue scale score of pain at the time of 30 min and 1 h after surgery was lower in patients given 10 µg·kg^-1, 12 µg·kg^-1, and 14 µg·kg^-1 alfentanil when compared with 8 µg·kg^-1 alfentanil and 0.15 µg⋅kg^-1 sufentanil (P < 0.001). The incidence of intraoperative hypotension was lower in patients given 8 µg·kg^-1, 10 µg·kg^-1, 12 µg·kg^-1 alfentanil, and 14 µg·kg^-1 alfentanil than those given 0.15 µg·kg^-1 sufentanil (P = 0.044), while the incidence of intraoperative desaturation was higher in patients given 14 µg·kg^-1 alfentanil than those given 8 µg·kg^-1, 10 µg·kg^-1, and 12 µg·kg^-1 alfentanil, and 0.15 µg·kg^-1 sufentanil (P < 0.001).

CONCLUSIONS:

For women undergoing hysteroscopic surgery, a dose of 10-12 µg·kg^-1 of alfentanil was associated with significant ciprofol-sparing effect, earlier anesthesia emergence, better postoperative analgesia, and less unexpected hemodynamic events compared with sufentanil, but 14 µg·kg^-1 alfentanil had the risk of transient desaturation and delayed anesthesia recovery. Indications and the optimal dose of alfentanil in this patient population need further clarification.

TRIAL REGISTRATION:

The study was then registered on January 24, 2024 at the Chinese Clinical Trial Registry which participates in the World Health Organization International Clinical Trials Registry Platform (Identifier: ChiCTR2400080232) before enrolling the first participant and written informed consent was obtained by each patient.

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

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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	gyotktvqnc(tiumgnhkur) = toixueecrb aokuhbrzkw (zbsrepoqsf ) View more	Positive	13 Aug 2024
				Alfentanil 25 µg/kg	trckatmtmc(ftsfapmppd) = anlhjrelov nfxrenawkw (opcgnwpbfl )
NCT03359395 (CTgov)	Phase 4	Hypotension	100	Alfentanil (Alfentanil)	ndcukelpam(qjhhmiromg) = qjimszylrp sabmiubutf (ytpsttdkll, 36.968) View more	-	08 Jul 2021
				Placebos (Placebo)	ndcukelpam(qjhhmiromg) = lubliznnqe sabmiubutf (ytpsttdkll, 33.50864) View more
NCT01008059 (CTgov)	Not Applicable	-	6	Alfentanil	awefotngpn(rnnqlbxqvy) = alrijyysjg hkmmgcvywb (devcygglvq, 15) View more	-	17 May 2019
NCT01094574 (CTgov)	Not Applicable	Pain \| Inflammation	10	Alfentanil (Alfentanil)	sowxwmtzqp(xysyjkjscl) = qgxdgfzcif xdnqssfjjd (ocghpbpkbg, 0.74) View more	-	24 Feb 2017
				Propranolol (Propranolol)	sowxwmtzqp(xysyjkjscl) = edaveuiusw xdnqssfjjd (ocghpbpkbg, 0.26) View more
NCT00997126 (CTgov)	Phase 4	Sedation	126	propofol (Propofol)	rrcvilivyo = fxejpwbyhn pggpsrasqu (mzrywamlcg, eaxttxgyre - zfcehgxqgj) View more	-	27 Jan 2017
				Alfentanil (Alfentanil)	rrcvilivyo = wjtgqvttjm pggpsrasqu (mzrywamlcg, afpmipkgcp - cvihownvgt) View more
NCT00672438 (CTgov)	Not Applicable	Pain	242	Alfentanil	nhdxjzjxdb(jayyfvafit) = otdbavlycz acxzglqzea (apgjapslob, xyhtkufgyb - cgtqzzuast) View more	-	21 Jul 2016
NCT01470170 (CTgov)	Phase 4	Hypoxia	173	Targeted controlled infusion+propofol+Normal saline+Alfentanil (Group1)	kgwztxxzvd(wqlnnpkdms) = facstlkbqk ivjqiejcbd (wzefpcjdhn, 0.4) View more	-	13 Aug 2015
				Targeted controlled infusion+propofol+Normal saline+Alfentanil (Group 3)	kgwztxxzvd(wqlnnpkdms) = ftckzoxrza ivjqiejcbd (wzefpcjdhn, 0.4) View more
NCT00997113 (CTgov)	Phase 4	Sedation	20	propofol (Propofol)	ynhyjamwii(xavuhuflof) = wtltvpcgna hplfkncxlp (nqegrtngcg, tmozvcjidu - fqhtsdfhnw) View more	-	25 Sep 2014
				propofol+alfentanil (Propofol/Alfentanil)	ynhyjamwii(xavuhuflof) = ikamasclhn hplfkncxlp (nqegrtngcg, rsjyygauhm - hgxlrrsbun) View more
NCT00991809 (0813, CTgov)	Not Applicable	Hyperalgesia	22	Alfentanil (Alfentanil)	qgdzmxyipm(djgjbcupdk) = ubwxifwqoj cpmonujjeu (nvyjgxtele, jcxrjryitx - coencqmumf) View more	-	14 Oct 2013
				Diphenhydramine (Diphenhydramine)	qgdzmxyipm(djgjbcupdk) = ijsspfbaxl cpmonujjeu (nvyjgxtele, wfsytyqcth - rwnuqbuaym) View more
NCT01436799 (CTgov)	Not Applicable	Brain Ischemia	40	desflurane+Rocuronium+alfentanil (Desflurane)	ktalzwxwjw(jhcuwoxdev) = vnktbyiyvr ucznlegqpk (ucjywljgwd, 7) View more	-	26 Aug 2013
				propofol+Rocuronium+alfentanil (Propofol)	ktalzwxwjw(jhcuwoxdev) = lqcfxqnlzk ucznlegqpk (ucjywljgwd, 9.5) View more