Sufentanil Citrate

Sufentanil Citrate

Cat Number
API0232119
CAS Number
60561-17-3

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CAS Number
60561-17-3
EINECS
262-295-4
Synonyms
SUFENTA, Fentatienil, Sufentanil citrate cii
Molecular Formula
C28H38N2O9S
Molecular Weight
578.68
Smiles
CCC(=O)N(C1=CC=CC=C1)C2(CCN(CC2)CCC3=CC=CS3)COC.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Appearance
White to off-white crystalline powder
Melting Point
96.6℃
Boiling Point
493.1℃
General Description
Sufentanil citrate is the citrate salt form of sufentanil, a synthetic opioid analgesic belonging to the phenylpiperidine class and structurally related to fentanyl. As a Schedule II controlled substance, it is approximately 5 to 10 times more potent than fentanyl and is characterized by rapid onset and predictable duration of action.
Mechanism of Action
Sufentanil is a highly selective agonist at the mu-opioid receptor, producing potent analgesia through G-protein-mediated inhibition of nociceptive pathways. Receptor activation results in analgesia, respiratory depression, miosis, reduced gastrointestinal motility, and euphoria. The drug exhibits high lipophilicity and approximately 93% plasma protein binding, with rapid redistribution and hepatic metabolism primarily via CYP3A4, yielding an elimination half-life of approximately 164 minutes in adults.
Application
Sufentanil citrate is indicated for intravenous use as an analgesic adjunct in balanced general anesthesia and as a primary anesthetic agent for induction and maintenance in major surgical procedures including cardiovascular and neurosurgery. It is also indicated for epidural administration combined with low-dose bupivacaine for analgesia during labor and vaginal delivery.

van de Donk T, et al. examined the pharmacology and clinical evidence for a novel sufentanil sublingual tablet system (15 μg tablets, patient-controlled at 20-minute intervals) for managing moderate-to-severe postoperative pain. Clinical studies involving over 600 patients have demonstrated the efficacy and safety of this system, providing effective pain relief while allowing early patient mobility and analgesic control. The authors conclude that although this system represents a promising patient-controlled analgesic option, further independent studies are needed to definitively establish its role among existing postoperative pain management strategies.

Fig. 1 Plasma concentration (Cp) of sufentanil following the administration of a 15-μg dose given via the intravenous (orange), sublingual (blue) or oral (green) routes. (van de Donk T, <i>et al</i>., 2018) Fig. 1 Plasma concentration (Cp) of sufentanil following the administration of a 15-μg dose given via the intravenous (orange), sublingual (blue) or oral (green) routes. (van de Donk T, et al., 2018)

References

  1. van de Donk T, et al. Pharmacokinetics and pharmacodynamics of sublingual sufentanil for postoperative pain management. Anaesthesia. 2018;73(2):231-237.

Wu Q, et al. investigated the cardioprotective mechanism of sufentanil preconditioning using in vivo rat models of myocardial ischemia-reperfusion injury and in vitro cardiomyocyte hypoxia-reoxygenation models. Sufentanil pretreatment suppressed myocardial damage by inhibiting oxidative stress and mitochondrial autophagy. Mechanistically, these protective effects were mediated through upregulation of miR-125a, which directly targeted and suppressed damage-regulated autophagy regulator 2 (DRAM2). Knockdown experiments confirmed that the miR-125a/DRAM2 axis is essential for the cardioprotective actions of sufentanil.

Fig. 2 Sufentanil alleviated myocardial IRI in rats by regulating miR-125a. (Wu Q, <i>et al</i>, 2021) Fig. 2 Sufentanil alleviated myocardial IRI in rats by regulating miR-125a. (Wu Q, et al, 2021)

References

  1. Wu Q, et al. Sufentanil preconditioning protects against myocardial ischemia/reperfusion injury via miR-125a/DRAM2 axis. Cell Cycle. 2021;20(4):383-391.

What are the specific storage conditions for Sufentanil Citrate as a highly potent opioid?

It must be stored in a secure, locked facility with limited access, in accordance with controlled substance regulations. Temperature should be maintained at 20-25°C.

Does Sufentanil Citrate require any special packaging to prevent adsorption during transport?

Yes, due to its high potency and low dose, we use containers that minimize surface adsorption. Glass vials or specially treated plastic liners are used for small-quantity shipments.

Is Sufentanil Citrate stable in solution for extended periods?

In aqueous solution, it has limited stability. We recommend storing the API in lyophilized powder form and reconstituting immediately before use. Stability data for reconstituted solutions is available.

How can I verify the chain of custody for a Sufentanil Citrate shipment?

We provide a complete audit trail, including signed delivery receipts and temperature logs, to ensure full regulatory compliance from dispatch to final destination.
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