Nerve Block for Pain Relief During Arthroscopic Rotator Cuff Repair.

BACKGROUND: Although arthroscopic rotator cuff repair (ARCR) often results in good outcomes, some patients have severe pain postoperatively. This study investigated the efficacy of nerve block for ARCR. METHODS: This study was retrospective, and consent was obtained from all patients. We divided 50 patients who had undergone ARCR into 4 groups: continuous interscalene nerve block was performed for 11 patients (continuous-injection group), single interscalene nerve block for 10 (single-injection group), suprascapular nerve block for 8 (suprascapular group), and intravenous analgesic administration for 10 (intravenous group). Eleven patients received no nerve block (control group). We evaluated diclofenac sodium and pentazocine dosing, visual analog scale (VAS) scores, and perioperative complications in each group. VAS scoring was done immediately after surgery and 1 and 6 hours and 1, 2, 3, 7, and 14 days postoperatively. RESULTS: The doses of diclofenac sodium and pentazocine did not differ between groups. VAS scores immediately after surgery and at 1 and 6 hours after surgery were significantly lower in the single-injection and continuous-injection groups than in the suprascapular, intravenous, and control groups. VAS score at 1 day postoperatively was significantly lower in the continuous-injection group than in the other groups. One patient in the continuous group reported temporary paralysis of the fingers and drug solution leakage. CONCLUSION: Interscalene nerve blocks yielded good pain relief for ARCR. Although continuous interscalene nerve block produced continuous pain relief, complications are a concern.

Enhancement of Dissolution and Skin Permeability of Pentazocine by Proniosomes and Niosomal Gel.

Proniosomes (PN) are the dry water-soluble carrier systems that may enhance the oral bioavailability, stability, and topical permeability of therapeutic agents. The low solubility and low oral bioavailability due to extensive first pass metabolism make Pentazocine as an ideal candidate for oral and topical sustained release delivery. The present study was aimed to formulate the PNs by quick slurry method that are converted to niosomes (liquid dispersion) by hydration, and subsequently formulated to semisolid niosomal gel. The PNs were found in spherical shape in the SEM and stable in the physicochemical and thermal analysis (FTIR, TGA, and XRD). The quick slurry method produced high recovery (> 80% yield) and better flow properties (θ = 28.1-37.4°). After hydration, the niosomes exhibited desirable entrapment efficiency (44.45-76.23%), size (4.98-21.3 µm), and zeta potential (- 9.81 to - 21.53 mV). The in vitro drug release (T100%) was extended to more than three half-lives (2-4 h) and showed good fit to Fickian diffusion indicated by Korsmeyer-Peppas model (n = 0.136-0.365 and R2 = 0.9747-0.9954). The permeation of niosomal gel was significantly enhanced across rabbit skin compared to the pure drug-derived gel. Therefore, the PNs are found promising candidates for oral as dissolution enhancement and sustained release for oral and topical delivery of pentazocine for the management of cancer pain.

Thiamylal Plus Pentazocine Shows Similar Efficacy as Ketamine Plus Midazolam for Painful Procedures in Children With Leukemia.

This retrospective study compared the use of thiamylal plus pentazocine (TP) to ketamine plus midazolam (KM) in children with leukemia who were undergoing bone marrow aspiration and/or intrathecal chemotherapy. A total of 268 procedures in 35 children with leukemia were retrospectively analyzed for efficacy and adverse events. All procedures were successfully completed without severe adverse events. TP induced significantly faster sedation. The incidents of desaturation were significantly greater in the TP group, but were transient and recovered by oxygen supplementation alone. Therefore, TP can be a useful combination with a similar efficacy as KM for painful procedures in children.

Diagnostic Yield and Complications of EBUS-TBNA Performed Under Bronchoscopist-directed Conscious Sedation: Single Center Experience of 1004 Subjects.

BACKGROUND: Endobronchial ultrasound-guided transbronchial needle aspiration (EBUS-TBNA) can be performed under either conscious sedation or general anesthesia. Herein, we describe the diagnostic yield and complications of EBUS-TBNA performed under bronchoscopist-directed conscious sedation. METHODS: This is a retrospective analysis of data collected in the bronchoscopy suite of this center on EBUS-TBNA or endoscopic ultrasound with a bronchoscope-guided fine needle aspiration (EUS-B-FNA) procedures performed between July 2011 and January 2016. All procedures were performed under bronchoscopist-directed conscious sedation with midazolam and pentazocine. The diagnostic yield, sample adequacy rate, complications, and doses of sedative agents are presented. RESULTS: Of the total 1005 EBUS-TBNA/EUS-B-FNA procedures performed during the study period, 1004 were performed under conscious sedation in spontaneously breathing subjects [mean (SD) age, 45.9 (15.8) years; 378 (37.6%) women]. The mean (SD) doses of midazolam and pentazocine used were 2.53 (1.8) mg and 30.9 (6.9) mg, respectively. The diagnostic yield of the procedure (972 subjects) was 61.2%. Complications related to EBUS were observed in 60 (5.9%) subjects. Majority of them were minor and self-limiting; major complications occurred in 11 (1.1%) subjects and included respiratory failure requiring assisted ventilation (n=6), arrhythmia (n=3), and hypotension (n=2). Escalation of the level of care was needed in only 8 (0.8%) subjects. CONCLUSION: EBUS-TBNA/EUS-B-FNA performed under bronchoscopist-guided conscious sedation was found to be safe and is associated with a reasonable diagnostic yield.

Cohort study of pain symptoms and management following impacted mandibular third molar extraction.

OBJECTIVE: The aim of this study was to investigate the possibility of intravenous sedation as a useful pain-relieving option for impacted third molar extractions. SUBJECTS AND METHODS: A prospective cohort study was conducted among patients who underwent bilateral mandibular third molar extractions under local anaesthesia and intravenous sedation (sedation group) and patients who underwent unilateral mandibular third molar extraction under local anaesthesia alone (local anaesthesia group). The frequency of use of postoperative oral analgesia and the intensity of pain assessed using the full cup test were compared between the two groups. RESULTS: The maximum pain intensity (0-100) on postoperative day 1 in the sedation and local anaesthesia groups was 72.8 ± 16.98 and 84.8 ± 15.84, respectively, and the mean pain intensity was 42.2 ± 16.00 and 49.6 ± 18.94. The maximum and mean pain intensities in the sedation group were significantly milder than those in the local anaesthesia group. The number of oral analgesic doses in the sedation group was significantly smaller on the day of surgery and on postoperative day 1 than in the local anaesthesia group. CONCLUSIONS: The results of this study suggest that bilateral impacted mandibular third molar extractions under intravenous sedation could be a recommended treatment option.

PENTAZOCINE VERSUS PENTAZOCINE WITH RECTAL DICLOFENAC FOR POSTOPERATIVE PAIN RELIEF AFTER CESAREAN SECTION- A DOUBLE BLIND RANDOMIZED PLACEBO CONTROLLED TRIAL IN A LOW RESOURCE AREA.

BACKGROUND: The unimodal approach of using pentazocine as post-cesarean section pain relief is inadequate, hence the need for a safer, easily available and more effective multimodal approach. AIM: To evaluate the effectiveness of rectal diclofenac combined with intramuscular pentazocine for postoperative pain following cesarean section. METHODS: In this double blind clinical trial, 130 pregnant women scheduled for cesarean section under spinal anesthesia were randomly assigned to two groups. Group A received 100mg diclofenac suppository and group B received placebo suppository immediately following surgery, 12 and 24h later. Both groups also received intramuscular pentazocine 30mg immediately following surgery and 6 hourly postoperatively in the first 24 h. Postoperative pain was assessed by visual analogue scale at end of surgery and 2, 12 and 24 h after surgery. Patient satisfaction scores were also assessed. RESULTS: One hundred and sixteen patients completed the study. Combining diclofenac and pentazocine had statistically significant reduction in pain intensity at 2, 12, and 24 hours postoperatively compared to pentazocine alone (p <0.05). No significant side effects were noted in both groups. The combined group also had significantly better patient satisfaction scores. CONCLUSION: The addition of diclofenac suppository to intramuscular pentazocine provides better pain relief after cesarean section and increased patient satisfaction.

Estrogen facilitates and the kappa and mu opioid receptors mediate antinociception produced by intrathecal (-)-pentazocine in female rats.

Pentazocine, a mixed-action kappa opioid receptor (KOR) agonist, has high affinity for both KOR and the mu opioid receptor (MOR), and has been shown clinically to alleviate pain with a pronounced effect in women. However, whether local application of pentazocine in the spinal cord produces antinociception and the contribution of spinal KOR and MOR in mediating the effect of pentazocine in female rats remain unknown. Also, it is not known whether pentazocine-induced antinociception in females is estrogen-dependent. Hence, we investigated whether intrathecal (i.t.) (-)-pentazocine produces thermal antinociception and whether estrogen modulates the drug effect in female rats. Only the highest dose of pentazocine (500 nmol) was effective in producing antinociception in ovariectomized (OVX) rats. In contrast, pentazocine produced antinociception in estradiol-treated ovariectomized females (OVX+E) rats with the lowest effective dose being 250nmol. KOR or MOR mediated the effect of the lowest effective dose in OVX+E rats; however, MOR blockade extended the KOR-mediated effect of 500nmol pentazocine in both groups. In normally cycling females, the 250nmol dose was effective in producing antinociception at the proestrous, but not at the diestrous stage of the estrous cycle. Thus, estrogen facilitates and KOR or MOR mediates. the antinociceptive effect of i.t. (-)-pentazocine in female rats. Selective doses of (-)-pentazocine, with or without MOR blockade, may have a therapeutic benefit.

(+)-Pentazocine reduces oxidative stress and apoptosis in microglia following hypoxia/reoxygenation injury.

BACKGROUND: Sigma-1 receptors (σ1R) are highly expressed in neurons as well as microglia and have been shown to modulate the inflammatory response in the central nervous system and thus may serve as possible target for neuroprotective strategies. The aim of the present study was to test the effect of (+)-pentazocine, a putative σ 1R agonist, in an in vitro model of microglia activation. METHODS: Microglia (BV2 cells) was exposed (3h) to 1% oxygen and reoxygenation was allowed for 24h. Cells were treated with different concentrations (1, 10, 25 and 50µM) of (+)-pentazocine in the presence or absence of NE-100 (1µM), a well established σ1R antagonist. Cell viability and apoptosis were measured by cytofluorimetric analysis, whereas oxidative stress was evaluated by reduced glutathione (GSH) content and mitochondrial potential analysis. RESULTS: Our results showed that (+)-pentazocine was able to increase cell viability and restore mitochondrial potential at all concentrations whereas only 1 and 10µM were able to reduce significantly apoptotic cell death, to restore reduced glutathione intracellular content and prevent ERK1/2 phosphorylation. All these effects were abolished by concomitant treatment with NE-100. CONCLUSIONS: (+)-pentazocine exhibits significant dose dependent protective effects in our in vitro model of microglial activation thus suggesting that σ1R may represent a possible target for neuroprotection.

Multicenter observational study comparing sedation/analgesia protocols for laser photocoagulation treatment of retinopathy of prematurity.

OBJECTIVE: The aim of this study was to identify the best sedation/analgesia protocol for laser photocoagulation (PC) of retinopathy of prematurity (ROP). STUDY DESIGN: This multicenter observational study included five hospitals, each using a specific sedation/analgesia protocol: local anesthesia with oxybuprocaine hydrochloride (Group L); intravenous pentazocine (Group P); intravenous fentanyl (Group F); air, oxygen and sevoflurane (AOS) inhalation (Group I). The groups were compared for pain responses, vital signs and adverse events. RESULTS: Heart rates and systemic blood pressures were elevated by PC in Groups L and P and Groups L, P and F, respectively. Moreover, poor analgesic efficacy was recognized in Groups L, P and F. In contrast, Group I experienced hypothermia, enteral feeding intolerance and apnea more frequently. CONCLUSION: From the viewpoint of sedation/pain relief, AOS anesthesia should be the best protocol. However, considering all the various factors together, the most reasonable one can be varied based on the patient's condition and hospital.

An effective and safe sedation technique combining target-controlled infusion pump with propofol, intravenous pentazocine, and bispectral index monitoring for peroral double-balloon endoscopy.

BACKGROUND/AIMS: Because peroral double-balloon endoscopy (DBE) is a time-consuming, painful procedure, sedation with analgesics, and/or anesthetics is generally required. The aim of this prospective study was to investigate the safety and efficacy of our sedation protocol for peroral DBE, which consisted of target-controlled infusion (TCI) anesthesia with propofol, an intravenous bolus of pentazocine, and bispectral index (BIS) monitoring. METHODS: A total of 34 consecutive patients who underwent DBE by the oral approach were enrolled. Patients were primarily sedated with a continuous infusion of propofol and adjusted in accordance with the BIS levels. The bolus infusion of pentazocine was performed when the propofol infusion was insufficient. The primary outcome measure of this study was to ensure the safety and efficacy of this sedation technique. The secondary purpose was to identify the characteristics of the patient who required the bolus infusion of pentazocine. RESULTS: Five patients (14.7%) required a reduction in the dose of propofol. However, no patient experienced any serious adverse events. All patients (100%) and 80.6% (25/31) of endoscopists answered that the sedation protocol was 'excellent' or 'enough' for peroral DBE. Eleven patients (32.3%) required a bolus injection of pentazocine. Age <60 years and a total procedure time of >70 min were significant risk-factors for pentazocine use. CONCLUSIONS: A combination of propofol via TCI pump, bolus injection of pentazocine as needed, and BIS monitoring was a safe and effective procedure for peroral DBE. Reasonable satisfaction indices were obtained from both patients and endoscopists. Pentazocine was required for young patients and in cases with longer procedure times.

[Anesthetic management for caesarean delivery in a parturient with achondroplasia].

A 27-year-old parturient (height, 130 cm; weight, 43 kg) with achondroplasia, which is characterized by rhizomeric short stature, large head and frontal bossing, was scheduled for elective caesarean section (C/S) because of her contracted pelvis. Her first delivery had been performed by C/S under general anesthesia at a regional hospital 6 years before. Preoperative airway assessment showed normal mouth opening and mobile cervical spine. Since she had anxiety about needle puncture and refused neuraxial blockade and since we considered the trachea could be intubated, we decided to perform C/S under general anesthesia at 37 weeks of gestation. The patient and baby had an uneventful perioperative course. Underdevelopment of bone formation results in characteristic craniofacial and vertebral abnormalities in patients with achondroplasia. Anesthetic management of achondroplastic parturients should be specified to individual basis based on careful preoperative assessment of craniofacial and vertebral deformities.

[Treatment of intrathecal fentanyl-induced itch with pentazocine: a case report].

Pentazocine has activities both of kappa-opioid receptor agonist and weak micro-opioid receptor antagonist. Recent study has suggested that kappa-opioid receptor agonists have antipruritic effects. We experienced a case of pentazocine inhibiting itch evoked by intrathecal fentanyl in a patient with idiopathic pulmonary fibrosis (IPF). A 50-year-old woman with IPF was diagnosed with fallopian tube abscess and which necessitated emergency surgery. We mainly performed regional anesthetic management to prevent acute exacerbation of IPF by tracheal intubation under general anesthesia. About 30 minutes after intrathecal administration of a combination of bupivacaine and fentanyl, she began to complain of itch. Although propofol was given intravenously, pruritus still recurred. Following that, when pentazocine was administered intravenously, pruritus disappeared immediately and then never recurred. Therefore, it is suggested that pentazocine can be useful in reducing pruritus on intrathecal opioid-induced itch. Future studies are necessary to evaluate the efficacy of pentazocine for the treatment and prevention of opioid-induced itch.

First report of hepatectomy without endotracheal general anesthesia.

BACKGROUND: Local anesthesia, including epidural anesthesia, has much merit over general anesthesia for the reduction of perioperative cardiac and respiratory complications. Liver operations commonly require general anesthesia. This is the first report of hepatectomy performed under epidural anesthesia with conscious sedation to avoid general anesthesia with endotracheal intubation. STUDY DESIGN: We devised the following protocol for hepatectomy under epidural anesthesia with conscious sedation: the patient receives 10 mg diazepam orally 1 hour before surgery, followed by 10 mg diazepam and 15 mg pentazocine intravenously just before surgery. An epidural catheter is inserted via the thoracic vertebra 7 to 9 interspaces. Intraoperatively, the patient receives a bolus of 7 mL 2% mepivacaine hydrochloride every 40 minutes through the epidural catheter. We conducted 4 left hepatectomies, 1 left lateral sectorectomy, and 5 partial hepatectomies under this protocol. We assessed the efficacy and safety of hepatectomy under epidural anesthesia with conscious sedation in terms of mortality rate, surgical time, amount of bleeding, and central venous pressure during the procedure. RESULTS: Every patient was managed without endotracheal intubation and laryngeal masks. There was no perioperative mortality. Median intraoperative blood loss was 453.0 mL (range 144.0 to 1292.0 mL) and median surgical time was 273.0 minutes (range 137.0 to 440.0 minutes). Median total amount of 2% mepivacaine hydrochloride used was 52.0 mL (range 23.0 to 95.0 mL). Central venous pressure values were significantly lower during the Pringle maneuver than at preclamp. CONCLUSIONS: The traditional belief is that liver resection should be performed under general anesthesia. We report the world's first series of liver resections for malignant tumors performed under epidural anesthesia with conscious sedation to avoid general anesthesia with endotracheal intubation.

Sulfation of buprenorphine, pentazocine, and naloxone by human cytosolic sulfotransferases.

Buprenorphine, pentazocine, and naloxone are opioid drugs used for the treatment of pain and opioid dependence or overdose. Sulfation as catalyzed by the cytosolic sulfotransferases (SULTs) is involved in the metabolism of a variety of xenobiotics including drug compounds. Sulfation of opioid drugs has not been well investigated. The current study was designed to examine the sulfation of three opioid drugs, buprenorphine, pentazocine, and naloxone, in HepG2 human hepatoma cells and to identify the human SULT(s) responsible for their sulfation. Analysis of the spent media of HepG2 cells, metabolically labeled with [(35)S]sulfate in the presence of each of the three opioid drugs, showed the generation and release of their [(35)S]sulfated derivatives. A systematic analysis using eleven known human SULTs revealed SULT1A3 and SULT2A1 as the major responsible SULTs for the sulfation of, respectively, pentazocine and buprenorphine; whereas three other SULTs, SULT1A1, SULT1A2, and SULT1C4, were capable of sulfating naloxone. Enzymatic assays using combinations of these opioid drugs as substrates showed significant inhibitory effects in the sulfation of buprenorphine and pentazocine by naloxone. Differential sulfating activities toward the three opioid drugs were detected in cytosol or S9 fractions of human lung, liver, kidney, and small intestine. Collectively, these results imply that sulfation may play a role in the metabolism of buprenorphine, pentazocine, and naloxone in vivo.

[Effect of pentazocine on the bispectral index during nitrous oxide-sevoflurane anesthesia].

BACKGROUND: The effect of pentazocine on the bispectral index (BIS) has not been reported. In this study, we have examined whether pentazocine alters the bispectral index during nitrous oxide-sevoflurane anesthesia. METHODS: Thirty surgical patients were enrolled in this double-blind, randomized study. Anesthesia was induced with thiopental and vecuronium and maintained with nitrous oxide-sevoflurane with the bispectral index maintained at approximate 40. Under stable anesthetic condition before surgery, patients were assigned to receive either a bolus of pentazocine 0.3 mg x kg(-1), 0.6 mg x kg(-1) or the same volume of saline 15 min after induction. Blood pressure (BP), heart rate (HR) and BIS were measured every 2.5 min from 2.5 min before induction until 30 min after induction. RESULTS: BP and HR showed no changes after pentazocine administration compared with control group. BIS showed no significant change in the saline group, but it increased significantly in the pentazocine group. When pentazocine was administered 15 min after induction, BIS increased significantly 20, 22.5, 25, 27.5 and 30 min after induction compared with the control group. The increase of BIS by pentazocine showed no dose-dependent effect in our present study. CONCLUSIONS: We observed that intravenous pentazocine caused a significant increase in BIS under nitrous oxide-sevoflurane anesthesia. The depth of sedation should be assessed carefully using a bispectral index monitor when pentazocine is used together.

Pentazocine increases bispectral index without surgical stimulation during nitrous oxide-sevoflurane anesthesia.

Although there have been a large number of reports on the effects of opioids on the bispectral index (BIS) during anesthesia, the effects of pentazocine on the BIS have not been reported. In this study, 60 patients scheduled for elective oral surgery [30 females, 30 males; all American Society of Anesthesiologists Physical Status (ASA PS) category 1] were enrolled in the trials. Maintaining gender parity, we randomly assigned the patients to one of three groups: pentazocine group (0.3 mg/kg; n = 20), fentanyl group (1 µg/kg; n = 20), or saline group (n = 20); these opioids were administered intravenously 15 min after the intubation. Anesthesia was induced with thiopental and vecuronium bromide and maintained with nitrous oxide (4 l/min)-oxygen (2 l/min)-sevoflurane (1%). At 15 min after the intubation, mean arterial blood pressure (MAP), heart rate (HR), and BIS index were recorded as baseline values. MAP, HR, and BIS values were measured at 2.5-min after the intubation up to 30 min. All data were expressed as the mean ± standard deviation. Differences in BIS values, MAP, and HR among the three groups throughout the experiment were analyzed using two-way repeated-measures analysis of variance (ANOVA), and demographic data among the three groups were analyzed using one-way ANOVA. Post hoc comparisons were performed using Fisher's protected least significant difference test. A P value of <0.05 was considered to indicate statistically significance. MAP and HR showed no significant differences among the three groups during the study. BIS values significantly increased between 5 and 15 min after the intubation relative to the baseline value in the pentazocine group (P < 0.001), and BIS values in this group were significantly during this time period than those in the fentanyl and saline group (P < 0.001). BIS values were not significantly different between the fentanyl group and saline group. These results indicated that pentazocine, but not fentanyl, under nitrous oxide-sevoflurane anesthesia caused a statistically significant increase in BIS in our patients.

The myocardial protection of polarizing cardioplegia combined with delta-opioid receptor agonist in swine.

BACKGROUND: The purpose of this study was to determine whether polarized arrest using adenosine/lidocaine cold crystalloid cardioplegia in combination with the hibernation inductor δ-opioid receptor agonist pentazocine would give satisfactory myocardial protection rather than using depolarized supranormal potassium cardioplegia, supranormal potassium cardioplegia with pentazocine, or adenosine/lidocaine cardioplegia. METHODS: Twenty pigs were randomly divided into four groups (n=5 each) to receive the four types of cold crystalloid cardioplegia with an aortic cross-clamp time of 1 hour. Hemodynamic data were continuously measured, as was the left ventricular end-diastolic pressure (LVEDP), left ventricular end-systolic pressure (LVESP), plus or minus derivative of change in diastolic pressure over time (±dp/dt), cardiac output, pulmonary artery pressure, pulmonary capillary wedge pressure, cardiac troponin I, and left ventricular ultrastructure. RESULTS: Both the adenosine/lidocaine/pentazocine group and the adenosine/lidocaine group got significantly better results than the hyperkalemic and hyperkalemic pentazocine groups in improving hemodynamic values, pulmonary capillary wedge pressure, LVEDP, LVESP, ±dp/dt, cardiac output, cardiac troponin I values, and left ventricular ultrastructure. There were no statistical differences between the adenosine/lidocaine/pentazocine group and the adenosine/lidocaine group at 1 hour after cross-clamp removal; but at 2 hours after cross-clamp removal, the adenosine/lidocaine/pentazocine group stands out (LVEDP 3.3±0.5, LVESP 122.5±18.9, +dp/dt 2.9±0.1, -dp/dt 2.0±0.6, cardiac output 2.6±0.4, and troponin I 4.9±0.5), with significant differences from the adenosine/lidocaine group (LVEDP 5.8±1.0, LVESP 98.5±10.1, +dp/dt 2.5±0.2, -dp/dt 1.0±0.2, cardiac output 2.2±0.2, troponin I 8.2±0.8; p<0.05). The defibrillation rate was largely decreased after the cross-clamp was released in the group containing pentazocine in cardioplegia. CONCLUSIONS: Adenosine/lidocaine/pentazocine cold crystalloid cardioplegia gave satisfactory cardiac arrest and better myocardial protection than the other three groups, especially with regard to improving prolonged postoperative cardiac function.

Estimating attractiveness for abuse of a not-yet-marketed "abuse-deterrent" prescription opioid formulation.

OBJECTIVE: The present study builds on research to model abusers' perceptions of particular analgesics' attractiveness for abuse and extends these methods to derive an estimate of attractiveness for abuse of a not-yet-marketed abuse-deterrent formulation (ADF) of a prescription opioid (Remoxy), Pain Therapeutics, Inc., San Mateo, CA, and King Pharmaceuticals, Inc., Bristol, TN). In a previous study, the Opioid Attractiveness Technology Scaling (OATS) method identified, from a drug abuser's point of view, the particular features of a prescription opioid relevant to its attractiveness for recreational use. A second online sample rated the extent to which these features applied to particular products they had actually used/abused. These data were used to model the abusers' overall preference for prescription opioids they had used/abused. DESIGN: In the present study, this method was applied to a not-yet-marketed ADF using substance abuse counselors as proxies for prescription opioid abusers. Thirty-eight counselors were given materials describing the new ADF along with four known products. RESULTS: Thirty-two counselors demonstrated sufficient agreement with abusers' ratings of the overall attractiveness of these drugs. The overall model yielded a significant pseudo R(2) of 0.15 (P < 0.001), with increasing model fit based on preferred route of administration, from swallowing whole (pseudo R(2) = 0.06; P < 0.001) and best for those who preferred to inject (pseudo R(2) = 0.40; P < 0.001). Data from a cross-validation group of 16 counselors/proxies were used to calculate the OATS scores for the five rated drugs and revealed significant differences between the ADF and OxyContin (Purdue Pharma LP, Stamford, CT), Percocet (Endo Pharmaceuticals, Chadds Ford, PA), and Vicodin (Abbott Laboratories, Abbott Park, IL), but not Talwin NX (Sanofi-aventis, Bridgewater, NJ), which was identified in the prior study as a highly unattractive drug for recreational purposes. CONCLUSIONS: The OATS method shows promise for providing pre-marketing estimates of attractiveness for abuse of not-yet-marketed ADFs.

Cognitive-affective and somatic side effects of morphine and pentazocine: side-effect profiles in healthy adults.

OBJECTIVE: The side effects of opioids have been widely investigated, but it is unknown whether the subjective effects of mu agonists and mixed action opioids produce similar symptom profiles. This study examined the structure and predictive validity of somatic and cognitive/affective side-effect profiles of morphine and pentazocine using the Somatic Side Effects Questionnaire and the Cognitive and Affective Side Effects Questionnaire. DESIGN: The subjects were 122 female and 90 male healthy volunteers that received an intravenous bolus administration of either 0.08 mg/kg of morphine or 0.5 mg/kg pentazocine. Pre- and post-drug experimental pain testing was also performed. Exploratory and confirmatory factor analysis resulted in similar factor structures for both drugs. RESULTS: The most frequently reported side effects across both drugs involved feeling relaxed, sedation, and feeling in control. At equianalgesic doses, pentazocine had greater aversive side effects than morphine, whereas morphine was more associated with feelings of control and euphoria. For both drugs, females reported greater frequency of negative side effects than males. Using cluster analysis, we identified similar symptom profiles for each drug. These drug-related side-effect profiles were linked with analgesic responses. Specifically, groups that had a more positive side-effect profile experienced the greatest analgesic effect based on changes in ischemic pain sensitivity. CONCLUSIONS: These findings have implications for decisions regarding opioid management of acute, chronic, and malignant pain conditions.

Comparison of efficacy of oral drotaverine plus mefenamic acid with paracervical block and with intravenous sedation for pain relief during hysteroscopy and endometrial biopsy.

BACKGROUND: Office hysteroscopy with endometrial biopsy is usually the first investigation for abnormal uterine bleeding and other uterine diseases. AIMS: To evaluate the effect of oral drotaverine with mefenamic acid on pain perception during hysteroscopy and endometrial biopsy and to compare it with that of paracervical block using 1% lignocaine and with that of intravenous sedation using diazepam with pentazocine. SETTINGS AND DESIGN: Outpatient gynecological department and open randomized trial. MATERIALS AND METHODS: One hundred twenty women undergoing hysteroscopy and endometrial biopsy were randomized into 3 groups. Group I received tablet containing drotaverine hydrochloride (80 mg)+mefenamic acid (250 mg), group II received lignocaine paracervically and group III received intravenous diazepam. The intensity of pain during the procedure, 30 and 60 minutes later on visual analog scale (VAS) was assessed. STATISTICAL ANALYSIS: Statistical analysis was performed using Kruskal-Wallis test, with the Bonferroni correction, the t test, and the chi2 test. RESULTS: Groups were similar in age, parity, vaginal birth or relevant medical history. A statistically significant difference in pain scores was noted among the 3 groups during the procedure (group I, 4.13+/-1.28; group II, 5.93+/-1.26; group III, 5.58+/-1.51), (P<0.001); as well as 30 minutes later (group I, 1.78+/-0.89; group II, 2.53+/-0.81; group III, 2.23+/-0.94), (P<0.001) and 60 minutes later (group I, 1.2+/-0.46; group II, 1.98+/-0.83; group III, 1.68+/-0.75), (P<0.001). VAS at different time intervals among the groups was also statistically significant. No adverse effects were observed. CONCLUSIONS: Oral drotaverine with mefenamic acid is effective in women undergoing hysteroscopy and endometrial biopsy.