Sufentanil 30microgram sublingual tablets sugar free
Requires a prescription from a doctor or prescriber
Sufentanil is an opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.
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These are medicines with high potential for misuse but with accepted medical uses. Subject to the strictest controls.
Legal requirements
- Must be stored in a locked controlled drugs cabinet
- Pharmacy must keep a controlled drugs register
- Prescriptions valid for 28 days only
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- Cannot be emergency supplied by pharmacists
Other medicines in this category
Morphine, Oxycodone, Fentanyl, Methylphenidate (Ritalin), Amphetamines
Safety information for pregnancy and breastfeeding
Pregnancy
Sufentanil caused embryolethality in rats and rabbits treated for 10-30 days during pregnancy with 2.5 times the maximum human dose by intravenous administration.
May cause fetal harm [FDA label]
The Use in Lactation
Infants exposed to this drug through breast milk should be monitored for excess sedation and respiratory depression [FDA label].
Breastfeeding
May cause fetal harm [FDA label]
The Use in Lactation
Infants exposed to this drug through breast milk should be monitored for excess sedation and respiratory depression [FDA label].
Always consult your doctor or midwife before taking any medicine during pregnancy or while breastfeeding. Source: DrugBank (CC BY-NC 4.0).
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Dzuveo 30microgram sublingual tablets
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Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
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Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing all 27 studies.
Reviews & meta-analyses: 5 · Randomised trials: 9 · 2016–2026
Showing all 27 studies, sorted by most relevant.
K. Sridharan, G. Sivaramakrishnan
Current Clinical Pharmacology, 2019
- Remifentanil
- Fentanyl
- Propofol
BACKGROUND: Opioid analgesics are commonly used along with propofol during general anesthesia. Due to the dearth of data on the quality of anesthesia achieved with this combination, the present meta-analysis was carried out. METHODS: Electronic databases were searched for appropriate studies using a suitable search strategy. Randomized clinical trials comparing the combination of remifentanil/sufentanil/alfentanil with propofol with fentanyl and propofol, were included. The outcome measures were as follows: total propofol dose to achieve the desired general anesthesia; time of onset and duration of general anesthesia; depth of general anesthesia; and recovery time (time for eye-opening and time taken for extubation). Risk of bias was assessed and Forest plots were generated for eligible outcomes. The weighted mean difference [95% confidence intervals] was used as the effect estimate. RESULTS: Fourteen studies were included in the systematic review and 13 were included in the metaanalysis. Statistically significant differences were observed for remifentanil in comparison to fentanyl when combined with propofol: Propofol dose (in mg) -76.18 [-94.72, -57.64]; time of onset of anesthesia (min) -0.44 [-0.74, -0.15]; time taken for eye-opening (min) -3.95 [-4.8, -3.1]; and time for extubation (min) -3.53 [-4.37, -2.7]. No significant differences were observed for either sufentanil or alfentanil about the dose of propofol required and due to scanty data, pooling of the data could not be attempted for other outcome measures for either sufentanil or alfentanil. CONCLUSION: To conclude, we found that remifentanil has a statistically significant anesthetic profile than fentanyl when combined with propofol. Scanty evidence for both alfentanil and sufentanil precludes any such confirmation.
Abstract licence: CC BY
C. Hutchings, K. Yadav, Warren J. Cheung, et al.
The American journal of emergency medicine, 2023
- Sufentanil
- Acute Pain
- Analgesics, Opioid
Manman Yao, Baoxia Fang, Jinguo Yang, et al.
Frontiers in Pharmacology, 2024
Objective: Patient-controlled intravenous analgesia (PCIA) can alleviate pain to some extent, and several randomized controlled trials (RCTs) have examined the efficacy of esketamine-assisted sufentanil in postoperative PCIA. In this research, we conducted a meta-analysis of relevant RCTs to compare the effect and safety of esketamine-sufentanil versus sufentanil alone for postoperative PCIA. Methods: We systematically searched the Cochrane Library, PubMed, Embase, Web of Science, CNKI, and other libraries up to December 2023 to screen out RCTs examining the use of esketamine combined with sufentanil for PCIA. We analysed analgesia scores, sedation scores, adverse drug reactions and postpartum depression scores as outcome indicators. Results: This meta-analysis included 32 RCTs. The results of the meta-analysis were as follows. 1) Visual Analog Scale: The VAS scores at 6, 12, 24, and 48 h were lower in the esketamine-sufentanil group than in the sufentanil alone group, and significant differences were found at all time points ( p < 0.05). 2) Ramsay Sedation Scale: The sedation score of the esketamine-sufentanil group at 48 h after surgery was higher than that of the sufentanil group alone [mean difference (MD) = −0.09 points, confidence interval ( CI ): (−0.26, −0.07), p = 0.27], but this difference was not significant ( p > 0.05). 3) Safety: Compared with sufentanil alone, the incidence rates of postoperative nausea-vomiting, dizziness-headache, skin pruritus and respiratory depression were significantly lower in the esketamine-sufentanil group. 4) Postartum depression: The reduction in postpartum depression scores were significantly greater in the esketamine-sufentanil group than in the sufentanil alone group at 3 days [MD = −1.35 points, CI : (−1.89, −0.81), p < 0.00001] and 7 days [MD = −1.29 points, CI : (−2.42, −0.16), p = 0.03]. Conclusion: The meta-analysis showed that the use of esketamine combined with sufentanil for postoperative PCIA could improve postoperative analgesia, alleviate postpartum depression and reduce the rate of postoperative adverse reactions, but there was no significant difference in sedation.
Abstract licence: CC BY
Neuber Martins Fonseca, G. Guimarães, J. Pontes, et al.
Brazilian journal of anesthesiology, 2021
- Anesthesia, Spinal
- Fentanyl
- Analgesics, Opioid
INTRODUCTION: Spinal infusions of either fentanyl or sufentanil have been reported in international reports, articles, and scientific events worldwide. This study aimed to determine whether intrathecal fentanyl or sufentanil offers safety in mortality and perioperative adverse events. METHODS: MEDLINE (via PubMed), EMBASE, CENTRAL (Cochrane library databases), gray literature, hand-searching, and clinicaltrials.gov were systematically searched. Randomized controlled trials with no language, data, or status restrictions were included, comparing the effectiveness and safety of adding spinal lipophilic opioid to local anesthetics (LAs). Data were pooled using the random-effects models or fixed-effect models based on heterogeneity. RESULTS: The initial search retrieved 4469 records; 3241 records were eligible, and 3152 articles were excluded after reading titles and abstracts, with a high agreement rate (98.6%). After reading the full texts, 76 articles remained. Spinal fentanyl and sufentanil significantly reduced postoperative pain and opioid consumption, increased analgesia and pruritus. Fentanyl, but not sufentanil, significantly reduced both postoperative nausea and vomiting, and postoperative shivering; compared to LAs alone. The analyzed studies did not report any case of in-hospital mortality related to spinal lipophilic opioids. The rate of respiratory depression was 0.7% and 0.8% when spinal fentanyl or sufentanil was added and when it was not, respectively. Episodes of respiratory depression were rare, uneventful, occurred intraoperatively, and were easily manageable. CONCLUSION: There is moderate to high quality certainty that there is evidence regarding the safety and effectiveness of adding lipophilic opioids to LAs in spinal anesthesia.
Abstract licence: CC BY
Baoguo Wang, Fang Luo, Bin Yu, et al.
BMJ Open, 2023
- Pain, Postoperative
- Postoperative Pain
- Drug-Related Side Effects and Adverse Reactions
INTRODUCTION: Patients undergoing major spine surgery usually experience moderate-to-severe postoperative pain. It has been shown that dexamethasone as an adjunct to local anaesthesia (LA) infiltration presented a superior analgesic benefit compared with LA alone in various types of surgeries. However, a recent meta-analysis reported that the overall benefits of dexamethasone infiltration were marginal. Dexamethasone palmitate (DXP) emulsion is a targeted liposteroid. Compared with dexamethasone, DXP has a stronger anti-inflammatory effect, longer duration of action and fewer adverse effects. We hypothesised that the additive analgesic effects of DXP on local incisional infiltration in major spine surgery may have better postoperative analgesic effect, compared with local anaesthetic alone. However, no study has evaluated this so far. The purpose of this trial is to determine whether pre-emptive coinfiltration of DXP emulsion and ropivacaine at surgical site incision will further reduce postoperative opioid requirements and pain scores after spine surgery than that with ropivacaine alone. METHODS AND ANALYSIS: This is a prospective, randomised, open-label, blinded endpoint, multicentre study. 124 patients scheduled for elective laminoplasty or laminectomy with no more than three levels will be randomly allocated in a 1:1 ratio into two groups: the intervention group will receive local incision site infiltration with ropivacaine plus DXP; the control group will receive infiltration with ropivacaine alone. All participants will complete a 3 months follow-up. The primary outcome will be the cumulative sufentanil consumption within 24 hours after surgery. The secondary outcomes will include further analgesia outcome assessments, steroid-related side effects and other complications, within the 3 months follow-up period. ETHICS AND DISSEMINATION: This study protocol has been approved by the Institutional Review Board of Beijing Tiantan Hospital (KY-2019-112-02-3). All participants will provide a written informed consent. The results will be submitted for publication in a peer-reviewed journals. TRIAL REGISTRATION NUMBER: NCT05693467.
Abstract licence: CC BY-NC
Yuhao Zhang, Guangyou Duan, Shanna Guo, et al.
Medicine, 2016
- Analgesics, Opioid
- Feasibility Studies
- Pain Measurement
Preoperative identification of individual sensitivity to opioid analgesics could improve the quality of postoperative analgesia. We explored the feasibility and utility of a real-time assessment of sufentanil sensitivity in predicting postoperative analgesic requirement.Our primary study included 111 patients who underwent measurements of pressure and quantitative pricking pain thresholds before and 5 minutes after sufentanil infusion. Pain intensity was assessed during the first 24-hour postsurgery, and patients who reported inadequate levels of analgesia were excluded from the study. The sufentanil requirement for patient-controlled analgesia was recorded, and a subsequent exploratory study of 20 patients facilitated the interpretation of the primary study results. In the primary study, experimental pain thresholds increased (P < 0.001) 5 minutes after sufentanil infusion, and the percent change in pricking pain threshold was positively associated with sufentanil requirement at 12 and 24 hours after surgery (β = 0.318, P = 0.001; and β = 0.335, P = 0.001). A receiver-operating characteristic curve analysis showed that patients with a change in pricking pain threshold >188% were >50% likely to require more sufentanil for postoperative pain control. In the exploratory study, experimental pain thresholds significantly decreased after the operation (P < 0.001), and we observed a positive correlation (P < 0.001) between the percent change in pricking pain threshold before and after surgery. Preoperative detection of individual sensitivity to sufentanil via the above described real-time method was effective in predicting postoperative sufentanil requirement. Thus, percent change in pricking pain threshold might be a feasible predictive marker of postoperative analgesia requirement.
Abstract licence: CC BY
Zhonglan Lin, Shuxin Li, Yun Zhou, et al.
BMC Anesthesiology, 2023
- Analgesia
- Anesthesia
- Lung Neoplasms
OBJECTIVE: To observe and evaluate the effectiveness and safety of Esketamine or Sufentanil combined with Dexmedetomidine for sedation and analgesia in lung tumor percutaneous radiofrequency ablation (PRFA) to provide a clinical basis for the optimization of sedation and analgesia in lung tumor PRFA protocols outside the operating room. METHODS: In this trial, 44 patients aged 37 to 84 undergoing lung tumor PRFA were enrolled and assigned to Group E (n = 22, Esketamine 0.2 mg/kg) or Group S (n = 22,Sufentanil 0.1 μg/kg ). Dexmedetomidine was infused intravenously as a sedative in both groups. The modified observer's assessment of alertness and sedation scale (MOAAS), physical movement pain scale, intraoperative vital signs, anesthesia recovery time, radiologist and patient satisfaction rates, incidence of respiratory depression, and incidence of postoperative nausea and vomiting were recorded. RESULTS: Although there was no significant difference in the physical movement pain scale, blood oxygen saturation or incidence of perioperative adverse events between the two groups during ablation, the MOAAS, mean arterial pressure (MAP) and heart rate (HR) were higher in Group E than in Group S. The anesthesia recovery time was shorter in Group E than in Group S, and radiologist satisfaction was better in Group E than in Group S, but there was no significant difference between the two groups in terms of patient satisfaction. CONCLUSION: Esketamine or Sufentanil combined with Dexmedetomidine is safe for lung tumor PRFA. However, in elderly patients with multiple underlying diseases, low-dose Esketamine combined with Dexmedetomidine has fewer hemodynamic effects on patients, milder respiratory depression, shorter recovery time, and better radiologist satisfaction because of its better controllability of sedation depth. TRIAL REGISTRATION: Chinese Clinical Trial Registry (Registration number#ChiCTR ChiCTR21000500 21); Date of Registration: 16/08/2021.
Abstract licence: CC BY
Tao Zhang, Yulong Yu, Wang Zhang, et al.
Drug Design, Development and Therapy, 2019
- Anesthesia, Local
- Labor, Obstetric
- Analgesia, Epidural
Background: The epidural dexmedetomidine combined with ropivacaine has been successfully used for labor analgesia. We compared the effects of dexmedetomidine and sufentanil as adjuvants to local anesthetic for epidural labor analgesia. Methods: Eighty nulliparous women were enrolled in the double-blind study and randomly divided into two groups. Group D received 0.5 µg/mL dexmedetomidine with 0.1% ropivacaine for epidural labor analgesia, and group S (control group) received 0.5 µg/mL sufentanil with 0.1% ropivacaine for labor analgesia. Hemodynamic parameters were monitored. Pain was assessed using a visual analog scale. The onset of epidural analgesia, duration of stages of labor, Ramsay Sedation Scale, blood loss, neonatal Apgar scores, umbilical artery blood pH and adverse effects, such as respiratory depression, nausea, vomiting, pruritus, and bradycardia, were recorded. Results: Compared with the control group, visual analog scale values after cervical dilation >3 cm were lower in group D ( P <0.05) and first-stage labor duration was shorter in group D (378.5±52.6 vs 406.5±58.2, P <0.05). Ramsay Sedation Scale values were higher in group D compared to the control group (2.8±0.6 vs 2.4±0.5, P <0.05). No significant differences in side effects were observed between the groups. Conclusion: Dexmedetomidine is superior to sufentanil in analgesic effect and duration in first-stage labor during epidural analgesia when combined with 0.1% ropivacaine (www.chictr.org.cn, registration ChiCTR-OPC-16008548). Keywords: dexmedetomidine, sufentanil, epidural, analgesia, labor
Abstract licence: CC BY-NC
Tao Han, Qing Chen, Jie Huang, et al.
Frontiers in Endocrinology, 2023
- Analgesia
- Diabetes, Gestational
- Ketamine
Background: Pregnant women with gestational diabetes mellitus (GDM) require more analgesics after cesarean delivery than those who do not have GDM. Uncontrolled pain following cesarean delivery is a major problem in women with GDM. We investigate the efficacy of low-dose esketamine combined with sufentanil intravenous patient-controlled analgesia (PCA)for postcesarean analgesia in women with GDM. Methods: One hundred forty pregnant women with GDM were enrolled participate in this randomized controlled trial and were randomized into two groups (70 in each group). The esketamine (S) group was given esketamine +sufentanil + ondansetron, and the control (C) group was given sufentanil +ondansetron. The primary outcome is sufentanil consumption at 24 hours postoperatively, the secondary outcomes are sufentanil consumption at 6 hours postoperatively, pain scores at 6, 24 and 48 hours postoperatively. Results: Compared with group C, group S had significantly lower sufentanil consumption at 6 and 24 hours postoperatively (P= 0.049 and P<0.001), significantly lower activities VAS(pain during activities)scores at 6 hours postoperatively, rest and activities VAS (pain at rest and pain during activities)scores at 24 hours postoperatively, and activities VAS scores at 48 hours postoperatively(P=0.022, P =0.002, P=0.001 and P=0.007). Compared to group C, the time to bowel function return was significantly shorter in group S. There was no significant difference in rest VAS (pain at rest) scores at 6 and 48 hours postoperatively (P>0.05). The time to first lactation was not significantly different between the two groups (P>0.05). There was no significant difference in neonatal neurobehavioral scores between the two groups (P>0.05). Conclusion: Compared to sufentanil PCA, adding low dose of esketamine significantly reduced the consumption of sufentanil while providing equally effective post cesarean analgesia in the patients with gestational diabetes.
Abstract licence: CC BY
Mengyue Fu, Rui Xu, Guizhen Chen, et al.
Heliyon, 2024
Background: Pain management after lung resection plays a crucial role in reducing postoperative pulmonary complications (PPCs). This study aimed to examine the effect of postoperative esketamine infusion as an adjunct to opioid analgesia on ventilation and pulmonary complications in patients underwent lung resection. Methods: Patients undergoing video-assisted thoracoscopic lung resection were randomly assigned to either the esketamine group or the control group. The esketamine group received a 24-h infusion of 1.5 mcg/ml sufentanil combined with 0.75 mcg/ml esketamine after surgery, while the control group received 1.5 mcg/ml sufentanil alone. The primary outcome measure was low minute ventilation, and the secondary outcome measures were hypoxemia, PaO2/FiO2 levels, postoperative pulmonary complications, hospital stay duration, ambulation time, Visual Analogue Scale (VAS) score, depression and anxiety levels, sleep quality, and analgesia satisfaction. Results: 80 patients were randomly divided into two groups: the esketamine group (n = 40) and the control group (n = 40). The esketamine group exhibited notably reduced incidence of low minute ventilation (P = 0.014), lower occurrence of postoperative pulmonary complications (PPCs) compared to the control group (P = 0.039), and decreased incidence of hypoxemia (P = 0.003). Furthermore, the esketamine group showed improved outcomes with lower VAS scores on the second postoperative day and enhanced sleep quality (P < 0.001) after the surgery. Conclusions: Postoperative esketamine infusion with opioids improved ventilation and reduced PPCs after lung resection, warranting further clinical studies. Trial registration: This study was registered on ClinicalTrials.gov (Trial ID: NCT05458453, https://clinicaltrials.gov/ct2/show/NCT05458453).
Abstract licence: CC BY-NC-ND
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
64 found
Half-life
164 minutes
Mechanism
Sufentanil is a synthetic, potent opioid with highly selective binding to μ-opioid receptors [F2009].
Food interactions
2 warnings
Human targets
3 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
52%
[A39629]
After…
Half-life
164 minutes
Protein binding
93%
Volume of distribution
1.4 minutes
Metabolism
Sufentanil…
Elimination
80%
Clearance
917 l
The…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Also known as Dsuvia, the sublingual form is used for the management of acute pain in adults that is severe to warrant the use of an opioid analgesic in certified medically supervised healthcare settings, including hospitals, surgical centers, and emergency departments [L4717]. Consideration may be made in the future for the use of the sublingual form in the US military in cases where analgesia is required immediately [L4718].
The sublingual form, manufactured by AcelRx Pharmaceuticals, Inc. (AcelRx), was approved on November 2, 2018 [L4717].
This route of administration is intended to be a simple, effective, non-invasive analgesic option to enable healthcare professionals to rapidly manage acute pain without difficult intravenous or epidural administration [L4717], [A39633].
1. As an analgesic adjunct in the maintenance of balanced general anesthesia in patients who are intubated and ventilated.
2. As a primary anesthetic agent for the induction and maintenance of anesthesia with 100% oxygen in patients undergoing major surgical procedures, in patients who are intubated and ventilated, such as cardiovascular surgery or neurosurgical procedures in the sitting position, to provide favorable myocardial and cerebral oxygen balance or when extended postoperative ventilation is anticipated.
3.
For epidural administration as an analgesic combined with low dose (usually 12.5 mg per administration) bupivacaine usually during labor and vaginal delivery
4. The sublingual form is indicated for the management of acute pain in adults that is severe to warrant the use of an opioid analgesic in certified medically supervised healthcare settings, including hospitals, surgical centers, and emergency departments.
[FDA label]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 1430 interactions
A Note on Respiratory Depression
Major, life-threatening, or fatal respiratory depression has been reported with the use of opioids, even in cases where it is used as recommended. Respiratory depression may lead to respiratory arrest and death if not diagnosed and treated appropriately. This drug should be administered only by persons specifically trained in the use of anesthetic drugs and the management of the respiratory effects of potent opioids, including respiration and cardiac resuscitation of patients in the age group being treated.
This training must include the establishment and maintenance of a patent airway and assisted ventilation [FDA label].
Carcinogenesis
Long-term studies in animals to evaluate the carcinogenic potential of sufentanil have not been conducted [FDA label].
Mutagenesis
Sufentanil was not found to be genotoxic in the in vitro bacterial reverse mutation assay (Ames assay) or in the in vivo rat bone marrow micronucleous assay [FDA label].
Reproductive Toxicity
Sufentanil caused embryolethality in rats and rabbits treated for 10-30 days during pregnancy with 2.5 times the maximum human dose by intravenous administration. The embryolethal effect was thought to be secondary to the toxicity for the mother animal model. No negative effects were noted in another study in rats that were treated with 20 times the maximum human dose in the period of organogenesis.
The preclinical effects were only seen following administrations of levels significantly above the maximum human dose, which is therefore of minimal relevance for clinical use F2009.
Pregnancy
May cause fetal harm [FDA label]
The Use in Lactation
Infants exposed to this drug through breast milk should be monitored for excess sedation and respiratory depression [FDA label].
In general, opioids decrease cAMP (affecting neural signaling pathways), decrease neurotransmitter release, and cause membrane hyperpolarization, all of which contribute to the relief of painful symptoms [A39637].
Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic neural transmission via G-proteins that activate effector proteins. Binding of the opiate receptor leads to the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP, located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. The release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is then inhibited [A39637].
Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist), also preventing neurotransmitter release [A39637].
Sufentanil and other opioids open calcium-dependent inwardly rectifying potassium channels, resulting in hyperpolarization and reduced neuronal excitability [A39636], [A39637].
In clinical settings, sufentanil exerts its principal pharmacologic effects on the central nervous system. Its primary therapeutic actions are analgesia and sedation. Sufentanil may increase pain tolerance and decrease the perception of pain. This drug depresses the respiratory centers, depresses the cough reflex, and constricts the pupils F2009, [A39637]. When used in balanced general anesthesia, sufentanil has been reported to be as much as 10 times as potent as fentanyl. When administered intravenously as a primary anesthetic agent with 100% oxygen, sufentanil is approximately 5 to 7 times as potent as fentanyl [FDA label]. High doses of intravenous sufentanil have been shown to cause muscle rigidity, likely as a result of an effect on the substantia nigra and the striate nucleus in the brain. Sleep-inducing (hypnotic) activity can be demonstrated by EEG alterations [FDA label].
Effects on the Respiratory System
Sufentanil may cause respiratory depression [FDA label].
Effects on the Cardiovascular System
Sufentanil causes peripheral vasodilation which may result in orthostatic hypotension or syncope. Bradycardia may also occur F2009. Clinical signs or symptoms of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes and sweating and/or orthostatic hypotension [FDA label].
Effects on the Gastrointestinal Tract
Sufentanil causes a reduction in motility associated with an increase in smooth muscle tone in both the antrum of the stomach and duodenum. Digestion of food in the small intestine may be delayed and propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, while tone may be increased and lead to spasm, resulting in constipation. Other opioid-induced effects may include a reduction in biliary and pancreatic secretions, spasm of the sphincter of Oddi, as well as temporary elevations in serum amylase [FDA label].
How the body processes this drug — absorption, distribution, metabolism, and elimination
[A39629]
After epidural administration of incremental doses totaling 5 to 40 mcg sufentanil during labor and delivery, maternal and neonatal sufentanil plasma concentrations were at or near the 0.05 to 0.1 ng/mL limit of detection, and were slightly higher in mothers than in their infants [FDA label].
After a single administration of a 15 microgram sufentanil sublingual tablet, mean terminal phase half-lives in the range of 6-10 hours have been observed. After multiple administrations, a longer average terminal half-life of up to 18 hours was measured, owing to the higher plasma concentrations of sufentanil achieved after repeated dosing and due to the possibility to quantify these concentrations over a longer time period F2009.
The central volume of distribution after intravenous application of sufentanil is approximately 14 L and the volume of distribution at steady state is approximately 350 L F2009.
Sufentanil is rapidly metabolized to a number of inactive metabolites, with oxidative N- and O-dealkylation being the major routes of elimination F2009.
The clearance of sufentanil in healthy neonates is approximately one-half that in adults and children. The clearance rate of sufentanil can be further reduced by up to a third in neonates with cardiovascular disease [FDA label].
Proteins and enzymes this drug interacts with in the body
PMID:10529478 PMID:12589820 PMID:7891175 PMID:7905839 PMID:7957926 PMID:9689128
Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone .
PMID:10529478 PMID:10836142 PMID:12589820 PMID:19300905 PMID:7891175 PMID:7905839 PMID:7957926 PMID:9689128
Also activated by enkephalin peptides, such as Met-enkephalin or Met-enkephalin-Arg-Phe, with higher affinity for Met-enkephalin-Arg-Phe (By similarity). Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors .
PMID:7905839
The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extent to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15 .
PMID:12068084
They mediate an array of downstream cellular responses, including inhibition of adenylate cyclase activity and both N-type and L-type calcium channels, activation of inward rectifying potassium channels, mitogen-activated protein kinase (MAPK), phospholipase C (PLC), phosphoinositide/protein kinase (PKC), phosphoinositide 3-kinase (PI3K) and regulation of NF-kappa-B (By similarity). Also couples to adenylate cyclase stimulatory G alpha proteins (By similarity).
The selective temporal coupling to G-proteins and subsequent signaling can be regulated by RGSZ proteins, such as RGS9, RGS17 and RGS4 (By similarity). Phosphorylation by members of the GPRK subfamily of Ser/Thr protein kinases and association with beta-arrestins is involved in short-term receptor desensitization (By similarity). Beta-arrestins associate with the GPRK-phosphorylated receptor and uncouple it from the G-protein thus terminating signal transduction (By similarity).
The phosphorylated receptor is internalized through endocytosis via clathrin-coated pits which involves beta-arrestins (By similarity). The activation of the ERK pathway occurs either in a G-protein-dependent or a beta-arrestin-dependent manner and is regulated by agonist-specific receptor phosphorylation (By similarity). Acts as a class A G-protein coupled receptor (GPCR) which dissociates from beta-arrestin at or near the plasma membrane and undergoes rapid recycling (By similarity).
Receptor down-regulation pathways are varying with the agonist and occur dependent or independent of G-protein coupling (By similarity). Endogenous ligands induce rapid desensitization, endocytosis and recycling (By similarity). Heterooligomerization with other GPCRs can modulate agonist binding, signaling and trafficking properties (By similarity)
Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine
Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain.
Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions
Enzymes involved in drug metabolism — important for understanding drug interactions
ATC N01AH03
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Sufentanil
Additional database identifiers
Drugs Product Database (DPD)
12343
ChemSpider
38043
BindingDB
94503
Guide to Pharmacology
3534
ZINC
ZINC000000538386
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8156
GenAtlas
OPRM1
GeneCards
OPRM1
GenBank Gene Database
L25119
GenBank Protein Database
452073
Guide to Pharmacology
319
UniProt Accession
OPRM_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8153
GenAtlas
OPRD1
GeneCards
OPRD1
GenBank Gene Database
U07882
GenBank Protein Database
27545517
Guide to Pharmacology
317
UniProt Accession
OPRD_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8154
GenAtlas
OPRK1
GeneCards
OPRK1
GenBank Gene Database
U11053
GenBank Protein Database
532060
Guide to Pharmacology
318
UniProt Accession
OPRK_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
DrugBank citations
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Structured knowledge from the free knowledge base
ATC classifications (Wikidata)
Linked open data from Wikidata (Q417915), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication. WHO INN from the World Health Organization.