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Objective: To evaluate clinical anesthetic effects of nalmefene hydrochloride in pediatric laryngeal mask anesthesia. Methods: Sixty pediatric patients who underwent short-time eye surgeries were randomly divided into nalmefene hydrochloride group (Group N) and the control group (Group C), 30 patients each group. At the end of the surgeries, patients of Group N and Group C were respectively given nalmefene hydrochloride at 0.25 μg/kg and 0.9% sodium chloride at the same volume intravenously. The situation of the patients' respiration recovery was recorded 1, 2, 3, 4 and 5 minutes after administration, including the time on which the patients' respiration was recovered and their laryngeal masks were removed. The sedation scores (Ramsay scores) and the incidence of adverse postoperative responses were recorded after the removal of the laryngeal mask. Results: The 5-minute respiration recovery rate was high in Group N, where the 3-minute respiration recovery rate was 83.0%, while only 16.7% in Group C. Besides, respiration recovery time [(3.17±0.78) min] and time for removing laryngeal mask [(4.10±0.95) min] in Group N were shorter than those of Group C (both P0.05). After removing laryngeal mask, the incidence of adverse responses was lower in Group N than that in Group C (P<0.05). Conclusion: Nalmefene hydrochloride is effective in shortening respiration recovery time and laryngeal masks removing time, but makes no difference in patients' sedative effects, with lower incidence of adverse postoperative respiratory responses.
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Objective·To evaluate clinical anesthetic effects of nalmefene hydrochloride in pediatric laryngeal mask anesthesia.Methods· Sixty pediatric patients who underwent short-time eye surgeries were randomly divided into nalmefene hydrochloride group (Group N) and the control group (Group C),30 patients each group.At the end of the surgeries,patients of Group N and Group C were respectively given nalmefene hydrochloride at 0.25 μg/kg and 0.9％ sodium chloride at the same volume intravenously.The situation of the patients' respiration recovery was recorded 1,2,3,4 and 5 minutes after administration,including the time on which the patients' respiration was recovered and their laryngeal masks were removed.The sedation scores (Ramsay scores) and the incidence of adverse postoperative responses were recorded after the removal of the laryngeal mask.Results· The 5-minute respiration recovery rate was high in Group N,where the 3-minute respiration recovery rate was 83.0％,while only 16.7％ in Group C.Besides,respiration recovery time [(3.17±0.78) min] and time for removing laryngeal mask [(4.10±0.95) min] in Group N were shorter than those of Group C (both P＜0.05).No significant difference was found in postoperative sedation scores between these two groups (P＞0.05).After removing laryngeal mask,the incidence of adverse responses was lower in Group N than that in Group C (P＜0.05).Conclusion· Nalmefene hydrochloride is effective in shortening respiration recovery time and laryngeal masks removing time,but makes no difference in patients' sedative effects,with lower incidence of adverse postoperative respiratory responses.
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Objective To observe the effect of Nalmefene on postoperative recovery on neonates by laparoscopic pyloromyotomy. Methods Elective laparoscopic pyloromyotomy for 60 neonates under general anestheisa, aged 15 ~ 28 days, ASA Ⅱ~Ⅲ , were randomly divided into two groups: Nalmefene group (M group) and Naloxone group (L group), 30 cases in each. Nalmefene 0.25 μg/kg and Naloxone 1.00 μg/kg were respectively administrated in M group and L group when the procedures finished. Parameters SpO2, MAP, HR and RR were measured and analyzed statistically at different times: end of surgery before drugs were used (T0), 10 min after administration (T1), 30 mins after extubation (T2) and 2 h after extubation (T3). Meanwhile observing spontaneous breathing recovery time, extubation time, residence time at PACU and adverse events 24 s after surgery. Results There were no actual differences in the value of MAP, HR and SpO2 at T0, T1, T2 and T3 times in the two groups (P > 0.05). However, the values of RR was significant faster at T1, T2 and T3 times than that at T0 in both groups (P < 0.05), compared with L group, the value of RR at T1 was much faster in M group (P < 0.05). The times of extubation and residence at PACU have significant differences in M group than that in L group (P < 0.05). The adverse events in both groups have no differences. Conclusion Nalmefene can facilitate the recovery at laparoscopic pyloromyotomy on neonates. Compared with naloxone, it can reduce the extubation time, and promote the early rehabilitation.
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Objective To study the protective effect of nalmefene hydrochloride on lung ischemia-reperfusion injury and its mechanism.Methods 40 rats were randomly divided into model group,high dose of nalmefene group,low dose nalmefene group and sham operation group equally(n =10).The lung ischemia-reperfusion model was established by occlusion of the left pulmonary hilum.The intravenous injection of nalmefene (20,10 μg·kg-1) was applied at 10 minutes before occlusion of the left pulmonary hilum in the high dose of nalmefene group and the low dose of nalmefene group,respectively.The sham operation group without occlusion of the left pulmonary hilum was not given any treatment.At 2 h after reperfusion,all rats were detected arterial blood gas value and then sacrificed.The specimens from the upper lobe of the left lung tissue were preserved to observe pulmonary lesions,detect the ratio of wet / dry weight and the expressions of β-endorphin and interleukin(IL)-17.Results Compared with the model group,the value of PCO2,the degree of pulmonary lesions,the ratio of wet / dry weight and the expressions of β-endorphin and IL-17 in lung tissue were significantly decreased (P ＜ 0.01),while the value of PO2 was significantly increased (P ＜ 0.01) in the low dose of nalmefene group.Compared with the low dose of nalmefene group,thevalue of PCO2,the degree of pulmonary lesions,the ratio of wet/dry weight and the expressions of β-endorphin and IL-17 in lung tissue were significantly decreased (P ＜ 0.01),while the value of PO2was significantly increased (P ＜ 0.01) in the high dose of nalmefene group.Conclusion Nalmefene hydrochloride may prevent lung ischemia-reperfusion injury in a dose dependent manner by reducing the production of β-endorphin and inhibiting the expression of IL-17 in lung tissue.
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Objective To establish a high performance liquid chromatography(HPLC)method for the determination of disodi-um edetate(EDTA-2Na)in nalmefene hydrochloride injection. Methods Content of EDTA-2Na in nalmefene hydrochloride injection was determined by HPLC. C18 Column was used. The mobile phase consisted of 0.3%tetrabutylammonium hydroxide solution-water-acetonitrile(20:45:35)with a flow rate of 1.0 ml/min,and the detection wavelength was 254 nm. The column temperature was 30℃and the injection volume was 20μl. Results The quantification limit and detection limit were 0.199 and 0.060μg/ml,respectively;the linear equation for the disodium edetate was Y=10.125X-0.216,and the calibration curves were linear within the range of 2.4593~7.3780 μg/ml(r=1.000). Each concentration of the average recovery was between 98~102%(n=9)(RSD%=0.58%). Conclusion The method can be used for the determination of EDTA-2Na in nalmefene hydrochloride injection,which is convenient,fast,sensitive and reproducible,with good precision,specificity and accuracy.
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Objective: To investigate the clinical efficacy of nalmefene hydrochloride in the treatment of patients with traumatic shock. Methods:Totally 62 cases of patients with traumatic shock were randomly divided into nalmefene treatment group (n=31) and the control group ( n =31 ) according to the random number table. The control group was given the conventional treatment, while nalmefene treatment group was treated with nalmefene hydrochloride additionally. The changes of hemodynamics, plasma TNF-αand vas-cular endothelial function index were compared between the groups. Results:The mean arterial pressure in 24h after the treatment signifi-cantly decreased when compared with that in 12h after the treatment of nalmefene treatment group, and the difference was statistically sig-nificant (P<0. 05);the heart rate in 12h and 24h after the treatment in nalmefene treatment group significantly decreased when com-pared with that before the treatment, and the differences were statistically significant (P<0. 05);the plasma TNF-αlevels in 24h after the treatment in nalmefene treatment group significantly decreased when compared with that in 12h after the treatment, and the difference was statistically significant (P<0. 05), and there was no significant difference in plasma TNF-α levels before the treatment and in 12h after the treatment (P<0. 05);the plasma NO and ET in 24h after the treatment in nalmefene treatment group significantly decreased when compared with that in 12h after the treatment, and the difference were statistically significant (P<0. 05);and there was no signifi-cant difference in plasma NO and ET before the treatment and in 24h after the treatment (P<0. 05);abnormality in electrocardiogram, routine blood tests, routine urine and liver and renal function examinations were not found, and no obvious adverse drug reactions were shown during the treatment course. Conclusion:Nalmefene hydrochloride combined with the conventional treatment in the patients with traumatic shock shows striking efficiency with notable effects on hemodynamics ( heart rate and mean arterial pressure) , which can reduce plasma TNF-α, NO and ET levels and shows significant research significance.
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Objective To establish a high performance liquid chromatography (HPLC) method for the determination of disodium edentate (EDTA-2Na) in nalmefene hydrochloride injection. Methods Content of EDTA-2Na in nalmefene hydrochloride injection was determined by HPLC. C18 Column was used. The mobile phase consisted of 0.3% tetrabutylammonium hydroxide solution-wateracetonitrile (20: 45: 35) with a flow rate of 1.0 ml/min, and the detection wavelength was 254 nm. The column temperature was 30°C and the injection volume was 20 µl. Results The quantification limit and detection limit were 0.199 and 0.060 µg/ml, respectively; the linear equation for the disodium edetate was Y=10.125X-0.216, and the calibration curves were linear within the range of 2.4593~ 7.3780 µg/ml (r=1.000). Each concentration of the average recovery was between 98~102% (n=9) (RSD%=0.58%). Conclusion The method can be used for the determination of EDTA-2Na in nalmefene hydrochloride injection, which is convenient, fast, sensitive and reproducible, with good precision, specificity and accuracy.
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Objective:To investigate the preventive effect of nalmefene on sufentanil-induced cough in the patients with general anesthesia. Methods:Eighty patients with general anesthesia were randomly divided into the control group and the nalmefene group. The nalmefene group was intravenously given 0. 25μg·kg-1 hydrochloric acid natrium nalmefene 5 minutes before the induction, and physiological saline with the same capacity was given in the control group. Cough number and intensity in one minute after the injection of nalmefene were observed, and the changes of hemodynamic indices such as the blood pressure, heart rate and pulse oxygen satura-tion before the anesthesia induction (T0), 1min after sufentanil injection (T1) and after the intubation (T2) were observed and com-pared between the groups. Results:The incidence rate of cough was 37. 5% in the control group and 0% in the nalmefene group, and the incidence rate and strength of cough in nalmefene group were both lower than those in the control group (P0. 05). Conclusion:Pretreatment with hydrochloric acid natrium nalmefene can prevent sufentanil-induced cough response during the induction of anesthesia without weakening the inhibitory effect of sufentanil on intubation response.
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OBJECTIVE:To explore the clinical efficacy and safety of nalmefene combined with monosialotetrahexosylganglio-side sodium in the treatment of patients in brain tumor operation. METHODS:64 patients in brain tumor operation were randomly divided into observation group and control group,32 cases in each group. Control group received brain cell protection,reducing in-tracranial pressure,anti-infective,vasodilator and other conventional treatment;observation group additionally received 0.7μg/(kg· h) nalmefene combined with 100 mg/d monosialotetrahexosylganglioside sodium from the first day of operation,for continuous 7 d. The plasma cortisol,adrenocorticotropic hormone (ACTH) before and 3,7 d after treatment,changes of serum IL-6,TNF-αand Barthel index (BI) in 2 groups were observed,improvement of neurological function and ADR were observed;Karnofsky (KPS)score was determined after 90 d follow-up used to assess the patient’s ability to take care of themselves. RESULTS:After treatment,plasma cortisol and ACTH content,serum TNF-αand IL-6 levels in 2 groups significantly decreased than before,the dif-ference was statistically significant(P<0.05);cortisol,ACTH and TNF-α levels 3,7 d after treatment,IL-6 level 7 d after treat-ment in observation group decreased more significantly than control group,the differences were statistically significant(P<0.05). After treatment,BI score in 2 groups significantly increased,and observation group increased more significantly than control group,the differences were statistically significant (P<0.05). 7 d after treatment,improvement rate of neurological function was 50.00%,which was significantly higher than that of the control group(18.75%),the difference was statistically significant(P<0.05). There was no significant ADR occurred of 2 groups in the study. Following-up for 90 d,the KPS score in observation group with not less than 70 points accounted for 71.88%,which was significantly higher than the control group(46.87%),the difference was statistically significant (P<0.05). CONCLUSIONS:Nalmefene combined with monosialotetrahexosylganglioside sodium can promote the recovery of patients in brain tumor operation,reduce cortisol,ACTH,IL-6 and TNF-α levels and improve prognosis of patients.
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Objective:To compare the clinical efficacy and safety of nalmefene hydrochloride injections and Naofukang injections in the treatment of the patients with severe head injury. Methods:Totally 60 cases of patients with severe head injury were randomly divided into the observation group and the control group. The two groups were all given the conventional therapy, such as dehydration, expansion and anti-infective therapy. On the basis of the conventional therapy, the observation group was treated with nalmefene hydro-chloride injections, 0. 4-0. 6 mg in 0. 9% sodium chloride injections, ivd, qd, while the control group was given Naofukang injections, 4-9 g in 5% or 10% glucose injections, ivd, qd. The treatment course was 2 weeks. After the 3-day treatment, the heart rhythm, the incidence of respiratory abnormalities and intracranial pressure were compared between the two groups. After the 10-day treatment, the total efficacy and complications in the two groups were also recorded and compared. Results:After the 3-day treatment, the incidence of abnormal heart rhythm and respiratory abnormalities in the observation group were significantly lower than that in the control group (P<0. 05), the intracranial pressure in the observation group was better than that in the control group (P<0. 05). After the 10-day treatment, the total effective rate of the observation group was 93. 3%, which was much higher than that in the control group ( P<0. 05). After the treatment, the incidence of respiratory infections, acid-base unbalance and upper gastrointestinal bleeding in the ob-servation group was significantly lower than that in the control group (P <0.05). Conclusion: The clinical efficacy of nalmefene hydrochloride injections in the treatment of patients with severe traumatic brain injury is significant with promising safety, which is bet-ter than that of Naofukang injections.
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Objective To analyse effect of nalmefene hydrochloride adjuvant therapy on serum nitric oxide(NO), endothelin (ET) and cardiac troponin I ( cTnI) in patients with traumatic shock.Methods 48 patients who were diagnosed with traumatic shock were collected.All patients were randomly divided into experimental group and control group, 24 cases in each group.On the basis of conventional anti shock treatment, the control group were treated with naloxone, the patients in experimental group received nalmefene hydrochloride treatment, after treatment, the serum levels of NO, endothelin and cardiac troponin I were detected in all patients.Results After treatment, compared with control group, the serum level of NO was lower in experimental group(P<0.05);the serum level of ET was lower in experimental group(P<0.05);the serum level of cTnI was lower in experimental group(P<0.05).Conclusions Nalmefene hydrochloride adjuvant therapy could significantly reduce the serum levels of NO, ET and cTnI in patients with traumatic shock,control the development of the disease, prevent myocardial injury.
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Objective To investigate the effect of nalmefene on sufentanil and propofol anesthesia for abortion and its impact on BIS. Methods One hundred and twenty patients undergoing abortion patients were randomly divided into group A, B, C, and D (n = 30 each). Patients in group A and B received 0.2 μg/kg or 0.3 μg/kg sufentanil, respectively, followed with 1.5 mg/kg propofol for induction of anesthesia post-pretreatment with 0.2 μg/kg nalmefene. Patients in group C and D received induction of anesthesia as patients in group A and B. According to the BIS and fluctuation of hemodynamic , the amount of propofol was adjusted. If necessary, additional single intravenous injection of 0.5 mg/kg propofol. The mean arterial pressure (MAP), heart rate (HR), pulse oxygen saturation (SpO2) and respiratory rate (RR) in patient before injection (T1), the eyelash reflex (T2), dilatation (T3), curettage (T4) and surgery awake (T5) were detected. The additional amount of propofol , operation time , recovery time of surgery , the steward score of orientation recovery after 1min of surgery , body movement reaction , cough , respiratory depression , postoperative visual analog digital score (VAS) 15 min later were also recorded in each group. Results Compared with group A, propofol could reduce the intraoperative body movement reaction rate , with lower postoperative VAS in group B and group D (P 0.05). The rapid recovery, surgery within 1 min orientation recovery were higher in group B, C, D compared with group A (P <0.05). However, orientation recovery score in group D was higher than that in group B (P < 0.05); The respiratory depression and choking were higher in group A and B than those in group C , D (P < 0.05, respectively). Conclusion The doses of 0.2 μg/kg nalmefene can effectively antagonize the respiratory depression , delay recovery and other adverse reactions in painless which induced by sufentanil , and the dose of nalmefene in this study failed to enhance the effect of analgesic and change the BIS values.
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Objective To develop a headspace GC method for simultaneously determining the residual organic solvents Ethanol, Diethyl ether, Acetone, Dichloromethane, Ethyl acetate, and Tetrahydrofuran in Nalmefene Hydrochloride. Methods Samples dissolved in DMF and six organic residual organic solvents were separated on a DB 624 capillary column (30.0 m×0.32 mm,1.8μm) with a FID detector. The inlet temperature was 220℃and the FID detector temperature was 250℃. The column temperature rose by program:the initial temperature was 35℃, maintained for 8 min, raise to 180cwith a rate of 30℃/min, maintained for 5 min. The heated temperature of the headspace oven was 80℃, the heated time lasted 30 min, and the injection volume was 1.0 mL. Results Six residual orgamic solvents, including Ethanol, Diethyl ether, Acetone, Dichloromethane, Ethyl acetate, and Tetrahydrofuran in Nalmefene Hydrochloride were completely separated. It was appeared to present a good linearity within the experimental concentration. The limit of detection for Ethanol, Diethyl ether, Acetone, ichloromethane, Ethyl acetate, and Tetrahydrofuran were 0.25,0.076,0.15,0.55,0.26 and 0.30μg?mL-1.The method has a good average recovery. Conclusion The method is proved to be accurate and sensitive after validation. It is suitable to determine the residual orgamic solvents in Nalmefene Hydrochloride .
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Objective To observe the changes of TNF-α and NF-κB after different doses of nalmefene hydrochloride (NAL) therapy for traumatic brain injury (TBI) in an effort to identify the effect of NAL on TBI-induced inflammatory response and the possible mechanism.Methods A model of TBI in the rat was produced using the improved Feeney' s free-fall impact method.The animals were randomly divided into sham group,TBI group,TBI + large dose of NAL (ip,0.2 mg/kg) group (TBI + NAL1group),TBI + medial dose of NAL (ip,0.14 mg/kg) group (TBI + NAL2 group),TBI + small dose of NAL (ip,0.07 mg/kg) group (TBI + NAL3 group).Form of brain tissues in each group was observed and mRNA levels of TNF-α and NF-κB were measured by real-time quantitative PCR assay.Results HE staining revealed severe injury and inflammatory infiltration of brain parenchyma in TBI group ;on the contrary,the situation ameliorated in TBI + NAL1 group,TBI + NAL2 group and TBI + NAL3group,with especially obvious improvement in TBI + NAL2 group.In PCR assay,significant expression of NF-κB and TNF-α was observed at post-TBI days 1,3,5 and 7 (P ＜ 0.05),followed by great reverse after NAL therapy (P ＜ 0.05),particularly in TBI + NAL2 group.Conclusions NAL can reduce the inflammation response to TBI and promote post-injury recovery.Moreover,there exists a NAL concentration window.
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Objective To evaluate the efficacy of nalmefene antagonizing postoperative respiratory depression induced by opioids.Methods Two hundred and forty ASA Ⅰ orⅡpatients aged 18-64 yr with body weight fluctuating within 20% of the standard body weight were included in this multicenter,randomized,double-blind,positive drug-controlled study.Anesthesia was induced with etomidate 0.3 mg/kg and TCI of sufentanil(effect-site concentration 0.4.ng/ml).Tracheal intubation was facilitated with vecuronium 0.1 mg/kg or rocuronium 0.6mg/kg.The patients were mechanically ventilated.PETCO2 was maintained at 35-45 mm Hg.Anesthesia was maintained with sevoflurane+ sufentanil TCI(Ce=0.1-0.4 ng/ml).Patients undergoing neurosurgery and liver or kidney operation were excluded.The operation time was within 3 h.The residual effects of muscle relaxants were reversed after operation.The patients were randomly divided into 2 groups(n=120 each):group Ⅰneloxone andgroup Ⅱ nalmefene.Naloxone 0.1 mg or nalmefene 0.25 μg/kg was injected iv over 30 s and was repeated 5 min later if necessary until the respiratory rate＞10 bpm,PETCO2＜45 mm Hg and apnea time＜15 s.The total amount of naloxone was≤0.4 mg while that of nalmefene≤1 μg/kg.BP,HR,SpO2,PETCO2,respiratory rate and apnea time were recorded immediately before and at 2 and 5 min after haloxone/nalmefene administration and then every 5 min until 5 min after extubation.The recovery of spontaneous breathing within 30 min after naloxone/nalmefene administration,extubation time and Ramsay sedation score at 5 min after extubation were recorded.The patients were also observed for adverse reactions.Results Spontaneous breathing recovered within 30 min after naloxone/nalmefene administration in all patients in both groups.The extubation time was significantly shorter in nalmefene group than in naloxone group.There was no significant difference in Ramsay sedation score,BP,HR,SpO2 and incidence of adverse reactions between the 2 groups.Conclusion Nalmefene is better than naloxone in antagonizing opioid-induced postoperative respiratory depression.
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Objective:To study the phamacokinetics of Nalmefene hydrochloride. Methods:30 healthy Chinese volunteers were assigned to 3 groups according to randomized design, and each group were given respectively a single intravenous administration dose of 0.5 mg, 1mg and 2mg of Nalmefene hydrochloride. The electrospray ionization positive selected reaction monitoring detections for Nalmefene hydrochloride and allyln-oroxymorphone (the internal standard) in the plasma and in the urine were used. The pharmaceutical parameters were calculated by 3P87 software. Results: The limit of the detection for Nalmefene hydrochloride was 0.0008 ng/ml in plasma and 0.0003 ng/ml in urine. There were good linear relationship range from 0.04 to 625ng/ml in plasma and 0.2 to 625 ng/ml in the urine. The variation coefficient in day and days, and the recoveries fitted the clinical pharmacokinetic study requirements. After a single intravenous administration of 0.5 mg,1mg, and 2mg of Na-lmefene hydrochloride, the obtained pharmacokinetic parameters were respectively as follows:Cmax were(1.74?0.48)?g/L,(4.17?1.08) ?g/L,(7.88?2.89) ?g/L;t1/2? were(12.83?3.98) h,(12.6?6.4) h, (10.58?3.74) h;V were (3.45?0.16) L/kg;(4.11?0.0716)L/kg、(4.25?0.56)L/kg;CL were (0.81?0.11) L/(h?kg), (0.85?0.15)L/(h?kg), (0.87?0.11) L/(h?kg);AUC0-∞ were (21.62?9.34) (ng/L)*h,(24.89?8.52) (ng/L)*h, (35?11.2) ng/L)*h;the urine accumulatived exc-retory rate were (78?21)%,(71?29)%,(78?19)%. Conclusion: The determination method for Nalmefene hydro-chloride in the plasma and in the urine by the electrosprayionization positive selected reaction monitoring detections is exclusive, accurate, sensitive and suitable. Pharmacokinetic characteristics in 3 groups of human treated with intravenous administration were described by a two-compartment model. The pharmaceutical characteristics of doxycycline hydrochloride in human body were linear in the range of 0.5~2.0 mg.
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OBJECTIVE: To study the clinical efficacy of Nalmefene in the treatment of chronic type Ⅱrespiratory failure. METHODS: A total of 40 patients with chronic type Ⅱ respiratory failure were randomly divided into treatment group and the control group: the treatment group received Nalmefene (1.0 mg) plus 5% GS (250 mL) q.d by iv gtt. in addition to the routine treatment, and the control group received 1.875 g Nikethamide plus 5% GS (250 mL) q.d by iv gtt. After 5-day treatment, the clinical symptom, physical signs, adverse drug reactions, lung function testing and blood gas analysis in two groups were evaluated. RESULTS: The overall response rate was 95.0% in the treatment group vs. 60.0% in the control group(P