Butorphanol Group Research Articles

Evaluation of the perioperative analgesic efficacy of buprenorphine, compared with butorphanol, in cats.

To compare the analgesic effects of buprenorphine and butorphanol in domestic cats. 2-phase positive-controlled randomized masked clinical trial. 39 healthy female cats (10 in phase 1 and 29 in phase 2). Cats admitted for ovariohysterectomy received buprenorphine (4 in phase 1; 14 in phase 2) or butorphanol (6 in phase 1; 15 in phase 2). In phase 1, cats were premedicated with buprenorphine (0.02 mg/kg [0.009 mg/lb], IM) or butorphanol (0.4 mg/kg [0.18 mg/lb], IM), in combination with medetomidine. Anesthesia was induced with propofol (IV) and maintained with isoflurane in oxygen. After extubation, medetomidine was antagonized with atipamezole. A validated multidimensional composite scale was used to assess signs of pain after surgery starting 20 minutes after extubation and continuing for up to 360 minutes, and pain score comparisons were made between the 2 groups. Phase 2 proceeded similar to phase 1 with the following addition: during wound closure, cats from the butorphanol and buprenorphine groups received butorphanol (0.4 mg/kg, IM) or buprenorphine (0.02 mg/kg, IM), respectively. Phase 1 of the study was stopped after 10 cats were ovariohysterectomized because 9 of 10 cats required rescue analgesia at the first evaluation. In phase 2, at the first pain evaluation, pain scores from the buprenorphine group were lower, and all cats from the butorphanol group required rescue analgesia. None of the cats from the buprenorphine group required rescue analgesia at any time. Buprenorphine (0.02 mg/kg, IM) given before surgery and during wound closure provided adequate analgesia for 6 hours following ovariohysterectomy in cats, whereas butorphanol did not.

Continous Epidural Butorphanol Decreases the Incidence of Intrathecal Morphine-Related Pruritus After Cesarean Section: A Randomized, Double-Blinded, Placebo-Controlled Trial

This randomized, double-blinded, placebo-controlled trial investigated the effect of continuous epidural butorphanol on intrathecal morphine-related pruritus in patients undergoing cesarean section. Eighty-three patients undergoing elective cesarean section under spinal anesthesia (1.5 mL of isobaric bupivacaine 0.5 % and 0.1 mg of preservative-free morphine) were enrolled in this study. Subjects were randomized to receive epidural butorphanol (n = 43) or normal saline combined bupivacaine (n = 40). In the study group, after the umbilical cord was clamped, patients were administered an epidural loading dose of 1 mg followed by a 48-h infusion of 0.004 % butorphanol with 0.1 % bupivacaine at a rate of 2 mL/h. In the normal saline group, saline was used for the loading dose and the infusion 0.1 % bupivacaine at a same rate. Postoperatively, a blinded observer recorded the incidence/severity of pruritus, visual analog pain scores and sedation level at 1, 3, 6, 9, 12, 24 and 48 h. The 48-h consumption of breakthrough analgesic (tramadol) was also noted. The primary outcome was the incidence of pruritus at 48 h. At 48 h, the incidence of pruritus was significantly lower in the butorphanol group (16.3 vs. 52.5 %; P < 0.001). Furthermore, compared with the normal saline group, the intensity of pruritus was also decreased with epidural butorphanol at 3, 6 and 9 h (all P ≤ 0.008). The pain scores were significantly lower at 12, 24 and 48 h (all P < 0.05) in the butorphanol groups. Patients only receiving bupivacaine required a higher cumulative dose of tramadol (37.5 ± 62.8 vs. 9.3 ± 36.6; P = 0.014). In patients undergoing elective cesarean section, continuous epidural butorphanol with bupivacaine decreases the incidence and severity of intrathecal morphine-related pruritus without adversely affecting the quality of postoperative analgesia.

Efficacy and safety of intravenous acetaminophen versus intravenous butorphanol as post-operative analgesic in obstetrics and gynecology: a comparative study

Background: The purpose of this study is to provide effective pain management by administration of an analgesic that gives the patients maximum satisfaction. The goal was to evaluate and compare the analgesics efficacy of acetaminophen with butorphanol; to determine if there is an overall decrease in opioid consumption and opioid-related adverse effects; and detect any adverse effects of acetaminophen as post-operative analgesics. Methods: In this randomized parallel-group controlled trial, post-operative patients were given either 1 g intravenous (IV) acetaminophen or 2 g IV butorphanol as post-operative analgesics. The post‑operative pain was evaluated by pain intensity scales and was measured at rest and during a deep breath over 24 h. If the reading in the pain intensity scale was above 5 then rescue medicine injection. Tramadol 100 mg IV SOS was given in both the groups. Any adverse effects reported by the patients were recorded. Results: The butorphanol group achieved slightly better pain ratings in the first 2 h and acetaminophen group after 6 h post-operatively. The overall visual analogue scale score across time was significantly lower for acetaminophen group than the butorphanol group (p = 0.02). The secondary outcome measure, rescue analgesic consumption (injection tramadol) was comparable between the two groups. Side-effects were less in acetaminophen than butorphanol, predominantly headache and sedation which was seen in butorphanol but was absent in acetaminophen. Conclusion: IV acetaminophen is an effective analgesic in obstetric and gynaecological surgeries with a good safety profile. When used in combination with opioids, they reduce opioid consumption, and this reduction is sufficient to reduce opioid-induced adverse effects.

A Randomized Double Blind Comparative Study of Intravenous Butorphanol and Tramadol on Haemodynamic Stress of Laproscopic Cholecystectomy

A Prospective double blind randomized study was conducted on 60 adults patients undergoing laproscpic surgery. Patients of group ? received butorphanol (25μg/kg) and patients of group II received tramadol (2mg/kg) just before induction of anaesthesia. Haemodynamic parameters including heart rate, systolic and diastolic blood pressure were recorded throughout the surgery. On statistical analysis of data, there was statistically significant increase in heart rate, systolic and diastolic blood pressure in tramadol group as compared to butorphanol group just after intubation, which got settled after 10 minutes of intubation. So, we concluded that Butorphanol (25μg/kg) is a good alternative to tramadol (2mg/Kg) as a balanced anaesthetic technique for laproscopic cholecystectomy.

Comparison of perioperative analgesic efficacy between methadone and butorphanol in cats

To compare the perioperative analgesic effect between methadone and butorphanol in cats. Randomized controlled clinical trial. 22 healthy female domestic cats. Cats admitted for ovariohysterectomy were allocated to a butorphanol group (n = 10) or methadone group (12) and premedicated with butorphanol (0.4 mg/kg [0.18 mg/lb], SC) or methadone (0.6 mg/kg [0.27 mg/lb], SC), respectively, in combination with acepromazine (0.02 mg/kg [0.01 mg/lb], SC). Anesthesia was induced with propofol (IV) and maintained with isoflurane in oxygen. A multidimensional composite scale was used to conduct pain assessments prior to premedication and 5, 20, 60, 120, 180, 240, 300, and 360 minutes after extubation or until rescue analgesia was given. Groups were compared to evaluate isoflurane requirement, propofol requirement, pain scores, and requirement for rescue analgesia. Propofol and isoflurane requirements and preoperative pain scores were not different between groups. During recovery, dysphoria prevented pain evaluation at 5 minutes. Pain scores at 20 minutes were significantly lower in the methadone group, and 6 of 10 cats in the butorphanol group received rescue analgesia, making subsequent pain score comparisons inapplicable. After 6 hours, only 3 of 12 cats in the methadone group had received rescue analgesia. In the present study, methadone appeared to be a better postoperative analgesic than butorphanol and provided effective analgesia for 6 hours following ovariohysterectomy in most cats.

English

Back ground: Laparoscopic surgeries have advantages like shorter stay and rapid return to normal activities because of small incision and les pain. Pain is an unpleasant sensation in the post-operative period. Methods: Fifty patients of American society Anesthesiologists (ASA) grade I and II, scheduled to undergo laparoscopic surgery, were randomized into butorphanol group (Group B) (n=25) and fentanyl group (Group F) (n=25). Four minutes before induction of anesthesia, Group B received inj. butorphanol 40 μg/Kg intravenously while Group F received Inj. fentanyl 2 μg/kg intravenously. All patients received general anaesthesia with controlled ventilation. Heart rate, systolic blood pressure (SBP), diastolic blood pressure (DBP), end tidal carbon dioxide (ETCO2), and oxygen saturation were monitored at different intervals. Results: The demographic data was comparable in both groups (p<0.05). There was a significant difference between the two groups in pulse rate after 12 minutes after intubation that persisted till the 2nd hour of post-operative period. There was no significant difference in DBP till 9 min after intubation, and then onwards significant changes were noted till 4th hour of post-operative period. Butorphanol provided prolonged analgesia when compared to fentanyl. Conclusions: We conclude that butorphanol is a better alternative to fentanyl for use as analgesic in laparoscopic surgeries because of its ability to produce prolonged analgesia, and less post-operative complications.

Effectiveness of butorphanol as an adjuvant to lidocaine for haematoma or periosteal block: A prospective, randomised, double blind study

Background:The peripheral nerve endings carrying pain contains opiod receptors. Blocking these receptors during haematoma block or periosteal block may provide better analgesia.Aim:Evaluation of effectiveness and safety of butorphanol as an adjuvant to lidocaine for haematoma block.Settings and Design:This is a two centre, prospective, individually randomised, two group, parallel, double-blind clinical trial.Methods:In this study, 115 American society of anaesthesiologist grade I and II adult patients scheduled for closed reduction of fractures were randomly allocated into two groups; Group A received 1% lidocaine (2 mg/kg) where as Group B received 1% lidocaine (2 mg/kg) with butorphanol (0.02 mg/kg) during haematoma block. Pain was assessed before, during and after manipulation of fracture by using visual analogue scale (VAS 0-10). Onset time of block, time for first rescue analgesic, 24 hour analgesic requirement and sedation levels were noted.Statistical Analysis:Data analysed with the unpaired t-test with Welch correction assuming unequal variances and Fisher's exact test using Graph pad Prism 5.02 version.Results:Onset time of haematoma block was significantly less in the butorphanol group compared to the lidocaine group (P=0.0003). The mean time for first rescue analgesic was significantly higher and total analgesic requirement was significantly lower in the butorphanol group (P<0.0001). Mean VAS scores were lower and sedation scores were higher in the butorphanol group.Conclusions:Addition of butorphanol to lidocaine quickens onset of haematoma block, provides excellent post manipulation analgesia and decreases 24 hour total analgesic requirement without excessive sedation.

Intravenous butorphanol administration reduces intrathecal morphine-induced pruritus after cesarean delivery: a randomized, double-blind, placebo-controlled study

Pruritus associated with intrathecal opioid administration is a common side effect. There is evidence that κ-opioid receptor agonists have antipruritic activity. Butorphanol has agonist actions at both κ-opioid and μ-opioid receptors. This study was designed to evaluate the antipruritic efficacy of butorphanol after intrathecal morphine administration in the setting of a randomized, double-blind study of parturients undergoing cesarean section. Ninety-one women who received combined spinal-epidural anesthesia with 1.2 ml 0.5 % isobaric bupivacaine and 0.1 mg preservative-free morphine were included in this study. After delivery of the baby, the parturients were randomly allocated to two groups: butorphanol group (n = 46) and physiological saline group (n = 45). In the butorphanol group, parturients received an intravenous loading dose of 1 mg butorphanol followed by infusion of 0.2 mg/h butorphanol. The physiological saline group received an infusion of the same volume of physiological saline. The presence of pruritus, visual analog scores for pain, sedation scores, and adverse effects were recorded 1, 2, 4, 6, 8, 10, 12, and 24 h after intrathecal morphine administration. The incidence of pruritus at 24 h was significantly more frequent in the physiological saline group than in the butorphanol group (48.9 vs. 13.0 %, P < 0.001). The severity of pruritus was significantly greater in the saline group than in the butorphanol group 2, 4, 6, 8 and 10 h after intrathecal morphine injection (P = 0.004, 0.001, 0.002, and 0.003, respectively). The visual analog scale scores at 24 h were significantly lower in the butorphanol group than in physiological saline group (P < 0.001). The Ramsay sedation score in the butorphanol group was significantly higher than that in the physiological saline group after 1, 2, 4, 6, 8, 10, 12, and 24 h (P < 0.05). There were no significant differences between the two groups in nausea/vomiting and other adverse effects. Administration of intravenous butorphanol after delivery of the baby can reduce pruritus that has been induced by intrathecal morphine administration in cesarean delivery with combined spinal-epidural anesthesia.

Analgesic Efficacy of Tramadol and Butorphanol in Mandibular Third Molar Surgery: A Comparative Study

Butorphanol tartrate, a mixed synthetic agonistantagonist opioid analgesic has been used for management of postoperative pain in minor and major surgical procedures.(14,20) Tramadol hydrochloride is a centrally acting opioid which is effectively used in postoperative pain in various minor and major surgeries. Twenty subjects selected randomly received butorphanol tartrate 1 mg intramuscular and 20 subjects received tramadol hydrochloride 50 mg intramuscular after the removal of mandibular third molars. Time of injection, amount of anesthetic injected, duration of surgery, adverse effects were recorded.(21) The mean amount of LA administered in butorphanol group was 2.6450 ml and in tramadol group was 2.640 ml respectively, the mean duration for surgery was 56.75 and 53.5 minutes for butorphanol and tramadol groups respectively which was statistically not significant. Pain assessment was done with VAS which showed mean of 19.2 and 15.5 mm (p = 0.001) which was significant for butorphanol and tramadol respectively after 12 hours. The mean time for rescue medication requirement was 5.9 hours (for tramadol) and 8.4 hours (for butorphanol). Effective analgesic activity was seen by butorphanol 1 mg intramuscular then tramadol 50 mg. Butorphanol 1 mg was more effective than tramadol 50 mg in respect to postoperative analgesia.

The effect of epidural injections with different dose of butorphanol on the rats' serum myelin basic protein and spinal cord morphology

Objective To observe the effect of epidural injection with different dose of tartrate-butorphanol(butorphanol)on the rats' serum myelin basic protein(MBP)and spinal cord morphology.Methods A PE-530 catheter was inserted into the epidural space of each Sprague-Dawley rat(male,weighting 180 g-210 g)at L1-2 level,and three days later,a total of 32 rats without any motor dysfunction were divided into 4 groups by random number table method as follow:saline group(group NS,n=8)and butorphanol group(B1,n=8;B2,n=8;B3,n=8).Rats in group NS were epidurally injected NS 30 μl each,and rats in group B1,B2 and B3 were respectively epidurally injected butorphanol 60,120 μg and 240 μg(all diluted to 30 μl with NS)1 time per day 5 d,the serum MBP of rats were measured before injection(T0),6(T1),24(T2)and 72 h(T3)after the last injection.At T3,the lumbar enlargement of the spinal cord was taken for detecting the morphology and apoptosis with optical microscope and electron microscope.Results There was no significant difference between each group in content of the serum MBP(P＜0.05).In group B2(21.2±2.6)and B3(25.3±3.1),compared with group NS(39.2±3.4)and B1(35.1±2.7),the number of nissl body in the neurons were decrease(P＜0.05).In group B2(36.3±7.2)and B3(48.2±8.5),compared with group NS(10.6±1.6)and B1(13.4±2.1),the expression of the Bcl-2 decreased obviously(P＜0.05).In group B2(37.9 ±7.6)and B3(45.2 ±8.3),compared with group NS(8.6 ±2.5)and B1(10.2 ±3.1),the expression of the Bax increased obviously(P＜0.05).In group B2(15.7±2.6)and B3(18.8±3.2),compared with group NS(6.1 ±2.5)and B1(9.7±2.9),the number of apoptosis neurons increased obviously(P＜0.05).In the electron microscope,the structure of myelins was destroyed,but not demyelinated.Conclusion Repeated epidural injection of butorphanol 60 pg has no influence on spinal cord morphology of rats,while injection of 120 μg and 240 μg can impair the spinal cord morphology. Key words: Butorphanol ; Epidural ; Myelin basic protein ; Morphology ;

Hemodynamic effects of butorphanol in desflurane-anesthetized dogs

ObjectiveTo evaluate the effects of butorphanol on cardiopulmonary parameters in dogs anesthetized with desflurane and breathing spontaneously. Study designProspective, randomized experimental trial. AnimalsTwenty dogs weighing 12 ± 3 kg. MethodsAnimals were distributed into two groups: a control group (CG) and butorphanol group (BG). Propofol was used for induction and anesthesia was maintained with desflurane (10%). Forty minutes after induction, the dogs in the CG received sodium chloride 0.9% (0.05 mL kg−1 IM), and dogs in the BG received butorphanol (0.4 mg kg−1 IM). The first measurements of body temperature (BT), heart rate (HR), arterial pressures (AP), cardiac output (CO), cardiac index (CI), central venous pressure (CVP), stroke volume index (SVI), pulmonary arterial occlusion pressure (PAOP), mean pulmonary arterial pressure (mPAP), left ventricular stroke work (LVSW), systemic (SVR) and pulmonary (PVR) vascular resistances, respiratory rate (fR), and arterial oxygen (PaO2) and carbon dioxide (PaCO2) partial pressures were taken immediately before the administration of butorphanol or sodium chloride solution (T0) and then at 15-minute intervals (T15–T75). ResultsIn the BG, HR, AP, mPAP and SVR decreased significantly from T15 to T75 compared to baseline. fR was lower at T30 than at T0 in the BG. AP and fR were significantly lower than in the CG from T15 to T75. PVR was lower in the BG than in the CG at T30, while PaCO2 was higher compared with T0 from T30 to T75 in the BG and significantly higher than in the CG at T30 to T75. Conclusions and clinical relevanceAt the studied dose, butorphanol caused hypotension and decreased ventilation during desflurane anesthesia in dogs. The hypotension (from 86 ± 10 to 64 ± 10 mmHg) is clinically relevant, despite the maintenance of cardiac index.

A comparison of epidural butorphanol and tramadol for postoperative analgesia using CSEA technique

Post operative analgesia in patients undergoing lower limb surgery is very essential for immediate postoperative pain relief which can be provided by oral or parentral medication, epidural analgesia, local blocks etc.The study was designed to evaluate the efficacy of epidural butorphanol and tramadol for postoperative pain relief. PATIENTS #ENTITYSTARTX00026; This was randomized, prospective, double blind study was conducted on 60 patients, ASA grade I&II, age 18-60 undergoing lower limb surgeries after approval from hospital ethics committee. Group allocation - Group I I (n=30) received 2 mg butorphanol as bolus epidurally, 1 mg for top up dose. Group II (n=30) received 100mg tramadol as bolus, 50 mg for top up. All the drugs were diluted to 10 ml normal saline & the observer was blinded to the drugs given. Postoperatively VAS, sedation score, vitals & side effects were observed. Top ups were given on achieving VAS>4. Diclofenac 75mg was given as rescue analgesia. Duration of analgesia was 5.35±0.29 hr and 6.25±1.58 hrs in Butorphanol and Tramadol groups respectively and the difference was found to be statistically significant. Pain scores were also significantly lower statistically in Group I as compared to Group II. Sedation scores were significantly higher in butorphanol group, whereas nausea vomiting was seen in tramadol group only (4 patients).No other side effects were observed. Both butorphanol and tramadol were effective for relieving postoperative pain, however quality of analgesia & patient satisfaction was more with butorphanol.

Comparison of postoperative analgesia with epidural butorphanol/bupivacaine versus fentanyl/bupivacaine following pediatric urological procedures

The aim of this retrospective study is to compare safety and efficacy of postoperative epidural butorphanol/bupivacaine with the gold-standard epidural analgesic infusion fentanyl/bupivacaine in children. With the Institutional Review Board's approval, the authors searched their Pain Management Database and divided children who received epidural analgesia into two groups. Each butorphanol group subject was matched with two fentanyl group subjects. Demographic data, pain scores, epidural interventions, epidural side effects, use of rescue opioid analgesia and adjuvant analgesics, causes of epidural failure, time of first oral intake and ambulation, and length of stay were statistically compared. A total of 191 patients were identified between 2000 and 2007; 58 in epidural butorphanol/bupivacaine and 133 in fentanyl/bupivacaine groups. Demographic data were comparable between the groups. The number of children with good pain control on postoperative days 1 and 2 in butorphanol (84 and 82 percent) and fentanyl (93 and 91 percent) groups were statistically similar (p = 0.06 and 0.13, respectively). Incidences of epidural side effects, especially pruritus, were significantly higher in the fentanyl group. Significantly more children in the butorphanol group required epidural rate changes when compared with those in the fentanyl group. Incidence of failed epidurals was significantly higher in the fentanyl group when compared with that in the butorphanol group. Clinically significant respiratory depression occurred in two children in the fentanyl group and in none of the children in the butorphanol group (p > 0.99). Epidural butorphanol provided similar analgesia to epidural fentanyl after urological procedures in children, but butorphanol caused less pruritus than fentanyl. Epidural analgesia with butorphanol/bupivacaine is effective in children undergoing urological procedures. When compared with epidural fentanyl, epidural butorphanol causes significantly less itching.

Effects of butorphanol tartrate on cytokines in septic shock rats

Objective To investigate the effects of butorphanol tartrate(B)on inflammatory cytokines in septic shock rats.Method Eighty adult male SD rats,weighing 200-250 g,were randomly(random number)divided into sham-operated group(group C,n=20),model group Ⅰ(group CLP,n=20),model group Ⅱ(group CLP+B,n=20)and butorphanol group(group B,n=20).Septic shock model was induced by cecal ligature puncture(CLP).Thirty minutes before CLP,5 mL/kg saune and 0.5 mg/kg butorphanol were injected intravenously in group CLP and group CLP+B,respectively.Sham-operated and butorphanol groups only received saune(5 mL/kg)and butorphanol(0.5 mg/kg),respectively.The mortauty rates were observed during 48 hours in 10 rats of all groups.In other 10 rats of all groups,the mean arterial pressure(MAP)and heart rates were monitored via the right femoral artery every 2 hours during 2-20 period after CLP.Tumor necrosis factor-α(TNF-α),interleukin-6(IL-6)and interleukin-10(IL-10)in serum were measured 4,12 and 20 hours after CLP.Analysis was made using SPSS version 17.0 software.Results The mortauty rate of rats in group CLP was higher than those in group C and group CLP+B(P＜0.05).MAPs progressively decreased after CLP in group CLP and group CLP+B,while HR increased at fast and descended afterwards in group CLP.The decrease in MAP was limited,and changes of HR in group CLP+B were slight.TNF-a and IL-6 in serum in group CLP and group CLP+B increased at first and then decreased to lower levels than those in group C and group B after CLP(P＜0.05).While TNF-α and IL-6 levels in group CLP+B were lower than those in group CLP(P＜0.05).Serum IL-10 increased to higher level 4 hours after CLP in group CLP and group CLP+B than that in group C and group B(P＜0.05).IL-10 level in group CLP+B were higher than that in group CLP(P＜0.05).There were no significant differences in mortauty rate,MAP,HR,TNF-α,IL-6 and IL-10 levels between group C and group B(P＞0.05).Conclusions Butorphanol tamale has protective effects on mrs with septic shock by inhibiting the production of pro-inflammatory cytokines TNF-a and IL-6,and increasing anti-irflammatory cytokine IL-10 level.Butorphanol tartrate has no significant effect on the serum TNF-α,IL-6 and IL-10 levels of normal rats. Key words: Butorphanol tartrate; Septic shock; Cytokine; TNF-α; IL-6; IL-10; Rat; Mortauty rate

The influence of using the Butorphanol to prevent the catheter-related bladder discomfort at post-operation

目的 观测术中应用布托啡诺对术后导尿管相关膀胱刺激征(Catheter-related bladder discomfort,CRBD)的影响.方法 选取60例ASAI～Ⅲ全麻下行经尿道前列腺电切术(transurethral resection of the prostate,TURP)患者,随机分为对照组(n=30)和治疗组(n=30),治疗组在预计拔管前45分钟静脉注射布托啡诺注射液0.02 mg/kg,对照组为等体积生理盐水,观测患者CRBD发生率与严重程度以及术后VAS评分.观察记录患者恶心呕吐、口干、嗜睡等不良反应发生率.手术前1天及术后24小时进行2分钟步行测验(2MWT).结果 各个时间点治疗组出现CRBD发生率和程度均低于对照组(P值 0.05),治疗组发生低氧血症4例,对照组1例,P值<0.05,但经对症处理后无明显并发症,不影响布托啡诺的治疗疗效.结论 术中给予布托啡诺可有效预防和降低导管相关膀胱刺激征,促进术后恢复,且无严重不良反应。

Comparison of fentanyl and butorphanol for postoperative pain relief with intravenous patient controlled analgesia

Opioids are very effective as postoperative analgesics, influencing emotional aspects of pain as well as reducing the actual pain threshold. Fentanyl, a phenylpiperidine derivative and potent opioid agonist, has already been studied for postoperative analgesia. Butorphanol, a synthetic morphinan derivative – agonist–antagonist, has few studies to substantiate its use. The present study was undertaken to compare the effects of the two drugs on postoperative pain relief in terms of efficacy and safety. A prospective, randomized controlled study of 100 patients [ASA I and II] undergoing total abdominal hysterectomies was conducted. Group F of 50 patients received fentanyl [0.4 μg/kg/h] and group B received butorphanol [4 μg/kg/h] as postoperative pain treatment via intravenous patient controlled analgesia [i.v. PCA]. Parameters monitored were pain score [VAS], pulse, blood pressure, respiratory rate, sedation score and side effects. The infusion rate, number of boluses, PCA demands and requirement of rescue analgesia were noted. Butorphanol had a better maintenance phase than fentanyl. The VAS scores were found to be reduced in the butorphanol group when compared with fentanyl group, significantly at 8 h [F: 1.16 ± 1.037; B: 0.78 ± 0.582; p-value: 0.026]. The incidences of complications were comparable in both the groups. Both the drugs are equally effective and safe as postoperative analgesics with i.v. PCA. The dose of 4 μg/kg/h of butorphanol appeared effective but the dosage of fentanyl used, 0.4 μg/kg/h, was not as effective as evidenced by the increased number of boluses taken by patients and needs to be increased.

Effect of intrathecal administration of a mixture of butorphanol and ketamine on cAMP-PKA-CREB signal transduction pathway in spinal dorsal horn of rats with inflammatory pain

Objective To investigate the effect of intrathecal administration of a mixture of butorphanol and ketamine on cAMP-PKA-CREB signal transductian pathway in the spinal dorsal ham of the rats with inflammatory pain. Methods Twenty-four male SD rats, weighing 240-280 g,in which intrathecal catheters were successfully placed, were divided into 4 groups randomly (n = 6 each): inflammatory pain group (group IP), butorphanol group (group B), ketamine group (group K), and butorphanol + ketamine group (group BK). The inflammatory pain was induced by injection of 5% formalin 50 μl into the plantar surface of left hind paw. Normal saline 10 μl, butorphannl 12.5 μg, ketamine 50 μg, and a mixture of butorphanol 12.5 μg and ketamine 50 μg was injected intrathecally 30 min before subcutaneous injection of formalin in group IP, B, K and BK respectively.Pain intensity score (PIS) was used to assess pain behavior every 5 min within an hour after subcutaneous injection of formalin. The animals were killed at 2 h after subcutaneous injection of formalin, and the L5 segment of the spinal cord was removed for determination of protein kinase A (PKA) and phosphorylated cAMP response element binding protein (p-CREB) expression using immunohistochemistry. Results Fonnahn administration induced pain behaviour expressed as two phases. PIS scores, PKA and p-CBEB expression, and staining scores were significantly lower during the fast and second phases in group BK than in group IP (P 0.05). Conclusion lntrathecal injection of a mixture of butorphanol and ketamine can reduce inflammatory pain in rats, and the mechanism may be related to the cAMP-PKA-CREB signal transduction pathway. Key words: Butorphanol; Ketamine; Cyclic AMP; Cyclic AMP-dependent protein kinnses; Cyclic AMP response element-binding protein; Pain; Injections, spinal

Effect of a Novel NOP Receptor Agonist (SCH 225288) on Guinea Pig Irritant-Evoked, Feline Mechanically Induced and Canine Infectious Tracheobronchitis Cough

Background: Previous studies have demonstrated that nociceptin/orphanin FQ (N/OFQ), the endogenous peptide ligand for the G-protein-coupled NOP receptor, inhibits cough in experimental models. SCH 225288 is a nonpeptide, orally active NOP agonist that may provide the foundation for the development of novel treatments for cough. Methods: First we characterized the selectivity of SCH 225288 in human receptor binding assays. Afterwards, the antitussive activity of SCH 225288 was studied in three mechanistically distinct cough models. Specifically, we observed the cough-suppressant effect of SCH 225288 in a guinea pig capsaicin irritant-evoked cough model, a feline mechanically induced cough model and finally in a canine Bordetella bronchiseptica disease model. Results: SCH 225288 selectively binds human NOP receptor (K_i = 0.38 ± 0.02 nmol/l) over classical opioid receptors (COR). In a guinea pig capsaicin cough model, SCH 225288 (0.1–1 mg/kg) suppressed cough at 2, 4, and 6 h after oral administration. The antitussive effect of SCH 225288 (3.0 mg/kg, p.o.) was blocked by the NOP antagonist J113397 (12 mg/kg, i.p.) but not by the classical opioid receptor (COR) antagonist, naltrexone (3.0 mg/kg, i.p.). In the anesthetized cat, we evaluated the effects of SCH 225288 given either intravenously or via the intravertebral artery against the increases in cough number and respiratory expiratory and inspiratory muscle (rectus abdominis and parasternal) electromyographic (EMG) activities due to perturbations of the intrathoracic trachea. SCH 225288 (0.03–3.0 mg/kg, i.v.) inhibited both cough number and abdominal EMG amplitudes. Similarly, SCH 225288 (0.001–0.3 mg/kg) administered intra-arterially also diminished cough number and abdominal EMG amplitudes. No significant effect of the drug was noted on parasternal EMG activity. Finally, we studied the antitussive actions of SCH 225288 (1.0 mg/kg) in a canine B. bronchiseptica disease model. In this model, dogs were challenged intranasally with B. bronchiseptica. Comparisons were made between a vehicle group, an SCH 225288 (1.0 mg/kg, p.o., q.d.) and a butorphanol (0.6 mg/kg, p.o., b.i.d.) group on the mean change in cough scores from baseline values and days 6–9 after B. bronchiseptica challenge. SCH 225288 (1.0 mg/kg, p.o., q.d.) displayed a positive antitussive tendency (p = 0.06) to inhibit B. bronchiseptica cough whereas butorphanol (0.6 mg/kg, p.o., b.i.d.) was devoid of antitussive activity. Conclusions: Taken together, the present data show that SCH 225288 is a potent and effective antitussive agent in animal models of cough. Furthermore, these findings indicate that NOP agonists represent a promising new therapeutic approach for the treatment of cough without the side effect liabilities associated with opioid antitussives.

Continuous infusion of butorphanol combined with intravenous morphine patient-controlled analgesia after total abdominal hysterectomy: a randomized, double-blind controlled trial

Postoperative pain therapy is still a problem for clinicians. Continuous basal infusion of drugs combined with standard patient-controlled analgesia (PCA) is considered to be an effective means of postoperative acute pain management. This study was designed to investigate the analgesic efficacy, morphine-sparing effects and side effects of butorphanol delivered as a continuous infusion adjunct to intravenous morphine PCA after abdominal hysterectomy. One hundred and eighty-six ASA physical status I-II patients, undergoing total abdominal hysterectomy, were allocated to this randomized double-blind controlled study and assigned to one of two groups. In the butorphanol (n = 96) group, patients received an intravenous loading dose of 10 microg kg(-1) butorphanol followed by infusion of 2 microg kg(-1) h(-1) butorphanol combined with intravenous PCA set at a bolus of 0.02 mg kg(-1) morphine after surgery. The control group (n = 90) received a physiological saline infusion combined with the same morphine PCA. Pain intensity on movement and at rest, sedation, satisfaction with analgesia, morphine consumption and side effects were recorded. A total of 164 patients completed the study. The butorphanol group had analgesia superior to the physiological saline control (P < 0.001). The butorphanol infusion group produced higher sedation ratings (P < 0.001) and better satisfaction (P < 0.05) and a lower incidence of side effects (P < 0.001) with the exception of sweating and dry mouth (P < 0.05) than the physiological saline group. The butorphanol group consumed less morphine over 48 h, 24.6 mg (95% confidence interval, 18.7-46.6), than the physiological saline group, 58.5 mg (95% confidence interval, 41.5-79.2; P = 0.006). There were no differences between urinary catheterization of more than 24 h, first time out of bed and time to discharge to home. Basal infusion of butorphanol combined with intravenous morphine PCA in patients undergoing abdominal hysterectomy shows effective analgesia with sedation and fewer side effects.

A Double‐blind Randomized Clinical Trial Evaluating the Analgesic Efficacy of Ketorolac versus Butorphanol for Patients with Suspected Biliary Colic in the Emergency Department

Patients presenting to the emergency department (ED) with suspected biliary colic often require intravenous (IV) analgesia. The choice of IV analgesia typically includes opioids and ketorolac. Although ultrasound (US) is the initial diagnostic study in these patients, nondiagnostic scans and a high clinical suspicion may require the patient to undergo hepatobiliary scintigraphy (HIDA). Opioids such as morphine interfere with the HIDA scan and thus may limit its value as an analgesic in the ED for these patients. Analgesics that do not interfere with HIDA scanning include ketorolac and butorphanol, an opioid agonist-antagonist. This study evaluates the efficacy of IV ketorolac compared to butorphanol for the treatment of biliary colic pain in the ED. Between June 2005 and February 2007, a convenience sample of patients presenting to the ED with abdominal pain suspected to be biliary colic were randomized to receive either 30 mg of IV ketorolac or 1 mg of IV butorphanol. Pain level was assessed using a 1 to 10 "faces" visual analog pain scale initially, as well as 15 and 30 minutes after medication infusion. Side effect profiles and the need for rescue analgesia were also assessed. Patients and clinicians were blinded to the study drug given. Forty-six patients were enrolled in the study. Both groups had similar demographics and baseline pain scores. The mean (+/-standard deviation [SD]) pain score in the butorphanol group decreased from 7.1 (+/-1.7) to 2.1 (+/-2.2) after 30 minutes. The mean (+/-SD) pain score in the ketorolac group decreased from 7.4 (+/-2.0) to 3.1 (+/-3.3) after 30 minutes. Both groups had similar needs for rescue analgesia. Side effects included dizziness and sedation with butorphanol and nausea with ketorolac. Although limited by small sample size and convenience sample, this study demonstrates that both ketorolac and butorphanol provide pain relief in biliary colic. Both agents should be considered reasonable options in the ED treatment of biliary colic, especially in patients that may undergo HIDA.