Anhedonia and motivational impairments are cardinal features of depression, against which conventional antidepressants demonstrate limited efficacy. Preclinical investigations and extant clinical trial data substantiate the promise of opioid receptor modulators in addressing anhedonia, depression, and anxiety. While synthetic opioid agents like dezocine are conventionally employed for analgesia, their distinctive pharmacological profile has engendered interest in their potential antidepressant properties and translational applications. Herein, we present a case in which persistent bupropion treatment was ineffective. However, the incidental administration of a single low-dose intravenous injection of dezocine resulted in a rapid and sustained amelioration of depressive symptoms, particularly anhedonia and motivational deficits. Our findings posit a potentially novel role for the \"legacy drug\" dezocine.

Dezocine, which is well-known as an analgesic, had about 45% share of the Chinese opioid analgesic market. Since drug products containing impurities could bring serious health consequences, it was important to control the generation of impurities and degradation products in the dezocine product. In this study, two kinds of photodegradation products (i.e., degradation product 1 and degradation product 2) in the dezocine injection were isolated using high-performance liquid chromatography. The possible structures of the photodegradation products were identified using both high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy. In addition, the possible generation mechanism showed that degradation product 1 was the oxidation product of dezocine, and degradation product 2 was the coupled dimer of dezocine. Finally, we found that the degradation rate of dezocine increased with the increase in light intensity. Moreover, the degradation of dezocine easily occurred under ultraviolet light in comparison with visible light. A deeper insight into the generation of the photodegradation products in the dezocine injection would directly contribute to the safety of drug therapy based on the dezocine injection by minimizing the degradant/impurity-related adverse effects of drug preparations.

BACKGROUND: Ultrapluse CO2 fractional laser technology has emerged as an effective treatment for scar management. However, one drawback of this modality is the pain caused during the procedure. This study aims to explore the efficacy and safety of dezocine (DZC) as preemptive analgesia for reduction of pain induced by ultrapulse CO2 fractional laser treatment for acne scars.
METHODS: The study cohort included 78 outpatients with acne scars between February and April 2023. Patients were randomly assigned into three groups with intravenous injection (iv) of DZC prior to laser treatment: (1) control, iv of saline; (2) DZC group 1 (DZC_1), iv of DZC at 0.15 mg/kg; and (3) DZC_2, iv of DZC at 0.20 mg/kg. After 30 min, one session of ultrapulse CO2 fractional laser treatment on acne scars was performed. Hemodynamics, visual analogue scale (VAS), and anxiety visual analog test (AVAT) were monitored prior to, during, and after the procedure.
RESULTS: Operative success rates for patients in the control, DZC_1, and DZC_2 groups were 34.6%, 84.6%, and 100%, respectively. DZC administered with either dosage significantly reduced the VAS and AVAT scores of patients in treatment groups as compared with the subjects in the control group during the course of ultrapulse CO2 fractional laser treatment. Patients in DZC_1 and DZC_2 groups did not show any significant difference in hemodynamic parameters, VAS, and AVAT scores. Temporary adverse effects such as nausea and dizziness were observed in some subjects after treatment; the symptoms were quickly dissolved after a rest in supine position.
CONCLUSIONS: DZC as preemptive analgesia could effectively reduce pain and anxiety induced by ultrapulse CO2 fractional laser treatment in patients. This study provided an option of preemptive anesthesia to minimize the pain and discomforts associated with laser treatments in clinical practices.

Flurbiprofen axetil or dezocine monotherapy has been applied for analgesia of postoperative non-small cell lung cancer (NSCLC); however, their combination is rarely investigated. Consequently, the present study aimed to explore the effect of flurbiprofen axetil plus dezocine on postoperative pain, surgical outcomes and its safety profile in patients with NSCLC. A total of 150 patients with resectable NSCLC were enrolled and randomized into three groups: i) The flurbiprofen axetil plus dezocine group (n=50), ii) the flurbiprofen axetil group (n=51) and iii) the dezocine group (n=49). A total of 50 mg flurbiprofen axetil, 5 mg of dezocine or their combination were administered intravenously 3 h prior to surgery and subsequently every 12 h until day 3 (D3) following surgery. The postoperative pain was lower in the flurbiprofen axetil plus dezocine group compared with that of the flurbiprofen axetil group at 6 h (P=0.008), 12 h (P=0.003), day 1 (D1) (P=0.013), day 2 (D2) (P=0.036) and D3 (P=0.010); in addition, it was lower in the flurbiprofen axetil plus dezocine group compared with that of the dezocine group at 6 h (P=0.010), 12 h (P=0.012) and D1 (P=0.020). Patient-controlled analgesia consumption was also lower in the flurbiprofen axetil plus dezocine group compared with that of the flurbiprofen axetil (P=0.010) and dezocine (P=0.002) groups. Furthermore, the length of hospital stay was lower in the flurbiprofen axetil plus dezocine group compared with that of the flurbiprofen axetil (P=0.008) and dezocine (P=0.048) groups, while other surgical outcomes and adverse events were similar among these three groups. Moreover, the expression of tumor necrosis factor-α was lower in the flurbiprofen axetil plus dezocine group compared with that of the dezocine group at 12 h (P<0.001), D1 (P<0.001) and D3 (P=0.033). The data indicated that flurbiprofen axetil and dezocine combination was superior to monotherapy for postoperative analgesia in patients with resectable NSCLC.

UNASSIGNED: To analyze the application of Dezocine combined with psychological care in the postoperative pain management.
UNASSIGNED: This is a retrospective study. A total of 186 HFS patients who underwent Microvascular Decompression (MVD) at First People\'s Hospital of Zunyi between January 2020 and January 2022 were selected as the study subjects. Patients were divided into two groups based on different treatment interventions. The control group (n = 93) received routine perioperative care without preemptive analgesia, while the observation group (n = 93) received preemptive analgesia and combined psychological care on the basis of the control group\'s intervention.
UNASSIGNED: At 30 min post-laryngeal mask removal (T3), no significant difference in Ramsay Sedation Scale scores existed between control and observation groups (p > 0.05). The observation group showed significantly lower RSS scores at immediate mask removal (T2) and VAS scores at T3 compared to controls (p < 0.05). Following intervention, the observation group had notably lower SAS and SDS scores than controls (p < 0.05). Baseline (T0) and 5 min pre-removal (T1) exhibited no significant differences in mean arterial pressure (MAP) and heart rate (HR) values between groups (p > 0.05). However, at T2 and T3, the observation group displayed significantly lower MAP and HR values than controls (p < 0.05). No significant differences in pulse oxygen saturation (SpO2) values existed between groups at any time point (p > 0.05).
UNASSIGNED: Compared to standard perioperative care alone, Dezocine combined with preemptive analgesia and psychological care effectively reduces postoperative pain during the awakening period, lowers the risk of immediate extubation-related agitation, and maintains stable hemodynamics in the postoperative period.

This commentary discusses the issues related to the current pharmacotherapy using super long-acting opioids (for the potential convenience for both patients and medical providers) for opioid addiction and argues for the potential to use a non-scheduled short-acting opioid to taper off opioids to reduce total number of patients on opioids and ultimately reduce opioid-related death. This article also proposes to develop short-acting opioids for addiction management instead of the current long-acting regimen. The authors further suggest that dezocine, a previously FDA approved medication for perioperative pain management and a non-scheduled opioid, be brought back to clinical practice in the US as a potential alternative addiction management medication, especially for those who are highly motivated to quit opioids completely using a taper off strategy.

BACKGROUND: Sufentanil in combination with dezocine or esketamine is often used for postoperative analgesia. However, there is a lack of clinical evidence of efficacy. This study compares the analgesic effects of esketamine and dezocine combined with sufentanil for relieving pain after laparoscopic cholecystectomy(LC).
METHODS: A total of 58 patients were randomly assigned to the esketamine group (ES group) and dezocine group (DE group). In the ES group, 1.5 mg/kg esketamine was used. In the DE group, 0.3 mg/kg dezocine was used. Primary outcome measures were Visual Analog Scale (VAS) score at 4 h, 8 h, 24 h and 48 h after surgery. The second outcome measures were Interleukin-6 (IL-6) and C-reactive protein (CRP) levels in the serum 10 minutes before anesthesia induction, and at 24 h and 48 h after surgery.
RESULTS: The VAS scores at 4 h, 8 h, 24 h and 48 h after the surgery in the ES group vs DE group were 2.70 vs 3.50(P=0.013),2.35 vs 3.15(P=0.004),1.69 vs 2.58(P=0.002), and 1.50 vs 2.26(P=0.002), respectively. The serum IL-6 concentrations 10 minutes before anesthesia induction, and at 24 h and 48 h after surgery in the ES group and DE group were 34.39 and 34.12(P=0.901),112.33 and 129.60(P=0.014), and 89.69 and 108.46(P<0.001), respectively. The CRP levels in serum 10 minutes before anesthesia induction, and at 24 h and 48 h after the surgery in the ES group and DE group were 5.99 and 5.86(P=0.639), 28.80 and 35.37(P<0.001), and 23.17 and 30.11(P<0.001), respectively.
CONCLUSIONS: For postoperative pain after LC, 1.5mg/kg esketamine provided better analgesia and reduced inflammation levels than 0.3mg/kg dezocine.
BACKGROUND: This trial was registered in the China Clinical Research Information Center in 31/05/2023 : https://www.chictr.org.cn/bin/home (Registration number: ChiCTR2300072011).

UNASSIGNED: The application of sedation and analgesia in spinal anesthesia has many benefits, but the risk of respiratory depression (RD) caused by opioids cannot be ignored. We aimed to observe the effect of dezocine, a partial agonist of μ-receptor, on the median effective dose (ED50) of sufentanil-induced RD in patients undergoing spinal anesthesia combined with low-dose dexmedetomidine.
UNASSIGNED: Sixty-two patients were randomly assigned to dezocine group (DS) and control group (MS). After spinal anesthesia, mask oxygen (5 L/min) and dexmedetomidine (0.1 ug/kg) were given. Five minutes later, patients in the DS group received an Intravenous (IV) bolus of sufentanil and 0.05mg/kg dezocine, while patients in the MS group only received an IV bolus of sufentanil.
UNASSIGNED: ED50 of DS group was 0.342 ug/kg, 95% confidence interval (CI) was (0.269, 0.623) ug/kg, and the ED50 of MS group was 0.291 ug/kg, 95% CI was (0.257, 0.346) ug/kg. There was no difference in the type and treatment measures of RD and hemodynamic changes between the two groups, and no serious adverse reactions occurred in either group.
UNASSIGNED: Dezocine can improve RD induced by sufentanil in patients with spinal anesthesia combined with low-dose dexmedetomidine, and increase the safety window of sufentanil use.

UNASSIGNED: Comprehensive data on the risk of hospital-acquired (HA) acute kidney injury (AKI) among adult users of opioid analgesics are lacking. This study aimed to systematically compare the risk of HA-AKI among the users of various opioid analgesics.
UNASSIGNED: This multicenter, retrospective real-world study analyzed 255,265 adult hospitalized patients who received at least one prescription of opioid analgesic during the first 30 days of hospitalization. The primary outcome was the time from the first opioid analgesic prescription to HA-AKI occurrence. 12 subtypes of opioid analgesics were analyzed, including 9 for treating moderate-to-severe pain and 3 for mild-to-moderate pain. We examined the association between the exposure to each subtype of opioid analgesic and the risk of HA-AKI using Cox proportional hazards models, using the most commonly used opioid analgesic as the reference group.
UNASSIGNED: As compared to dezocine, the most commonly used opioid analgesic for treating moderate-to-severe pain, exposure to morphine, but not the other 7 types of opioid analgesics, was associated with a significantly increased risk of HA-AKI (adjusted hazard ratio: 1.56, 95% confidence interval: 1.40-1.78). The association was consistent in stratified analyses and in a propensity-matched cohort. There were no significant differences in the risk of HA-AKI among the opioid analgesic users with mild-to-moderate pain after adjusting for confounders.
UNASSIGNED: The use of morphine was associated with an increased risk of HA-AKI in adult patients with moderate-to-severe pain. Opioid analgesics other than morphine should be chosen preferentially in adult patients with high risk of HA-AKI when treating moderate-to-severe pain.

Dezocine is a partial mu opioid receptor agonist previously used as an analgesic for perioperative acute pain in the US and is now the most used perioperative analgesic in China. In general, dezocine is well-tolerated, with relatively minimal risk of fatal respiratory depression. To our knowledge, there are no reports of dezocine addiction, which suggests that the abuse liability of dezocine is low. The overarching goal of this study was to determine the efficacy of a novel formulation of dezocine (Cyc-dezocine), developed for intraperitoneal or intranasal administration, to reduce voluntary opioid taking in rats. One cohort of male rats self-administered intravenous oxycodone on a fixed-ratio 5 schedule of reinforcement. Once oxycodone taking stabilized, rats were pretreated with systemic injections of vehicle or Cyc-dezocine. Cyc-dezocine dose-dependently reduced intravenous oxycodone self-administration. A second cohort of male and female rats self-administered oral oxycodone from drinking water. Once oxycodone taking stabilized, rats were pretreated with intra-nasal Cyc-dezocine. Consistent with the effects of i.p. Cyc-dezocine in our intravenous oxycodone studies, intra-nasal Cyc-dezocine attenuated oral oxycodone self-administration. Together, these findings support the need for further studies investigating the therapeutic potential of Cyc-dezocine for treating opioid use disorder.