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Aims To investigate the effects of high doses of pentazocine on antinociception induced by a high dose of morphine and the role of the kappa-opioid receptors (KORs) in these effects in mice. Main methods Sixty-six C57BL/6J mice were pretreated with a KOR antagonist, nor-binaltorphimine (nor-BNI) (10 mg·kg − 1 ), or a normal saline placebo. All the mice received a subcutaneous injection of morphine (10 mg·kg − 1 ) 120 min later and different doses of pentazocine (3, 10, 30, 56, 100 mg·kg − 1 ) or a normal saline placebo. A tail pressure test, hot plate test and tail flick test were performed before and at 30, 60, 90 and 120 min after the injection of morphine. Key findings The tail pressure test, hot plate test and tail flick test showed that pentazocine at doses of 10 to 100 mg·kg − 1 , but not at 3 mg·kg − 1 , had significant antagonizing effects on the antinociception induced by high-dose morphine to mechanical and thermal pain, and nor-BNI did not affect antinociception in combination with pentazocine at 10 to 100 mg·kg − 1 and morphine at 10 mg·kg − 1 . Significance High-doses of pentazocine antagonize the antinociception induced by a high-dose of morphine in a dose-dependent manner, and this antagonistic effect is not associated with the activation of KORs. [ABSTRACT FROM AUTHOR]

Background: Small Rho-GTPases are critical mediators of neuronal plasticity and are involved in the pathogenesis of several psychiatric and neurological disorders. Rac-GTPase forms a multiprotein complex with upstream and downstream regulators that are essential for the spatiotemporal transmission of Rac signaling. The sigma-1 receptor (Sig1R) is a ligand-regulated membrane protein chaperone, and multiprotein complex assembly is essential to sigma-receptor function. Results: Using immunoprecipitation techniques, we have shown that in mitochondrial membranes Sig1R could directly interact with Rac1. Besides Rac1, the Sig1R forms complexes with inositol 1,4,5-trisphosphate receptor and Bcl2, suggesting that mitochondrial associated membranes (MAM) are involved in this macromolecular complex formation. Assembly of this complex is ligand-specific and depends on the presence of sigma agonist/antagonist, as well as on the presence of GTP/GDP. Treatment of mitochondrial membranes with (+)-pentazocine leads to the (+)-pentazocine-sensitive phosphorylation of Bad and the pentazocine-sensitive NADPH-dependent production of ROS. Conclusion: We suggest that Sig1R through Rac1 signaling induces mild oxidative stress that possibly is involved in the regulation of neuroplasticity, as well as in the prevention of apoptosis and autophagy. [ABSTRACT FROM AUTHOR]

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. © 2015 S. Karger AG, Basel [ABSTRACT FROM AUTHOR]

The high-affinity sigma receptor 1 (σR1) ligand (+)-pentazocine ((+)-PTZ) affords profound retinal neuroprotection in vitro and in vivo by a yet-unknown mechanism. A common feature of retinal disease is Müller cell reactive gliosis, which includes cytokine release. Here, we investigated whether lipopolysaccharide (LPS) stimulates cytokine release by primary mouse Müller cells and whether (+)-PTZ alters release. Using a highly sensitive inflammatory antibody array we observed significant release of macrophage inflammatory proteins (MIP1γ, MIP2, MIP3α) and interleukin-12 (IL12 (p40/p70)) in LPS-treated cells compared to controls, and a significant decrease in secretion upon (+)-PTZ treatment. Müller cells from σR1 knockout mice demonstrated increased MIP1γ, MIP2, MIP3α and IL12 (p40/p70) secretion when exposed to LPS compared to LPS-stimulated WT cells. We investigated whether cytokine secretion was accompanied by cytosolic-to-nuclear NFKB translocation and whether endothelial cell adhesion/migration was altered by released cytokines. Cells exposed to LPS demonstrated increased NFKB nuclear location, which was reduced significantly in (+)-PTZ-treated cells. Media conditioned by LPS-stimulated-Müller cells induced leukocyteendothelial cell adhesion and endothelial cell migration, which was attenuated by (+)-PTZ treatment. The findings suggest that release of certain inflammatory cytokines by Müller cells can be attenuated by σR1 ligands providing insights into the retinal neuroprotective role of this receptor. [ABSTRACT FROM AUTHOR]

ABSTRACT Previous studies have shown that sigma-1 receptor chaperone (Sig-1R) ligands can regulate pain-related behaviors, and Sig-1R itself can regulate μ-opioid receptor functions as well as signal transduction. Even though (±)-pentazocine has been used clinically for the treatment of pain through opioid receptors, (+)-pentazocine is known to be a selective Sig-1R agonist. To the best of our knowledge, there is no information available regarding the involvement of Sig-1R agonistic action in the antinociceptive effects of (±)-pentazocine. Therefore, the present study was designed to investigate the effects of (+)-pentazocine on the antinociceptive effects of (-)-pentazocine in mice. Both and (-)-pentazocine induced biphasic antinociceptive effects as measured by the warm-plate test. The early phase, but not the delayed phase, of the antinociceptive effects induced by (-)-pentazocine, which are mediated by the activation of μ-opioid receptors, were suppressed by pretreatment with (+)-pentazocine. These results suggest that the innate antinociceptive action of (±)-pentazocine could be marginally reduced by the effects of (+)-pentazocine, but (+)-pentazocine can suppress the antinociceptive effects of (-)-pentazocine at certain time points. Synapse 69:166-171, 2015. © 2015 Wiley Periodicals, Inc. [ABSTRACT FROM AUTHOR]

Introduction and Aims Injecting pharmaceutical opioids for non-medical purposes is a major concern globally. Though pharmaceutical opioids injection is reported in India, the exact proportion of people who inject drugs ( PWID) using pharmaceutical opioids is unknown. The objectives of this study were to describe the various types of drugs that are injected by people in India and to analyse the differences between the commonly injected drugs. Design and Methods A cross-sectional, multicentric study covering 22 harm-reduction sites from different regions of the country was conducted. First 50 subjects, chosen randomly from a list of PWIDs accessing services from each site and fulfilling study criteria, were interviewed using a structured questionnaire. Data from 902 male subjects are presented here. Results Pharmaceutical opioid injectors ( POI) accounted for 65% of PWIDs (buprenorphine: 30.8%, pentazocine: 21.8% and dextropropoxyphene: 11.9%). Heroin, injected by 34.3%, was prevalent in most states surveyed. Buprenorphine and pentazocine were not injected in the north-east region, whereas dextropropoxyphene was injected in the north-east alone. Univariate and multivariate logistic regression showed that, compared with heroin injectors, the POI group was more likely to consume alcohol and pharmaceutical opioids orally, inject frequently, share needle/syringes and develop injection-site complications. Among individual POIs, buprenorphine injectors had significantly higher proportion of subjects injecting frequently, sharing needle/syringes and developing local complications. Irrespective of the opioid type, majority of subjects were opioid dependent. Discussion and Conclusions Pharmaceutical opioids are the most common drugs injected in India currently and have greater injection-related risks and complications. Significant differences exist between different pharmaceutical opioids, which would be important considerations for interventions. [Ambekar A, Rao R, Mishra AK, Agrawal A. Type of opioids injected: Does it matter? A multicentric cross-sectional study of people who inject drugs. Drug Alcohol Rev 2015;34:97-104] [ABSTRACT FROM AUTHOR]

Objective: In this study the effect of caffeine on pentazocine analgesia in rats was assessed by “Tail-immersion test”. Methods: This study was performed by “Tail-immersion test”. Animals were juvenile M-Mari Rats (Male or female) weighing 120-160 gr. Findings: The average control latencies in “Tail-immersion test” were about 1.5-2 sec. The response latencies of rats which had been given caffeine (25, 50, 75 and 100 mg/kg I.P) or propyleneglycol (40%) were not significant comparing to those receiving an injection of the control vehicle over the 2 hours of testing period. Conclusion: The response latencies of pretreated parts with caffeine (100 mg/kg I.P) during 15, 30, 45 and 60 minutes after the injection of (10, 15, 20 and 25 mg/kg S.C) of pentazocine were significantly higher than those of control group. But injection of lower doses of caffeine and pentazocine did not show a significant analgesic effect compared with the control group.

Deafferentation pain induced by subarachnoid block (SAB) is rare, but it can appear in the form of recurrent phantom lower limb pain, new acute-onset stump pain in amputees, lower limb pain in patients with tabes dorsalis, and neuropathic pain. We have previously reported that thiopental is an effective treatment for deafferentation pain induced by therapeutic SAB applied to treat neuropathic pain of central origin. Here, we report the case of an amputee who developed new stump pain in his lower limb immediately after subarachnoid tetracaine was administered prior to appendectomy. A 51-year-old man who had previously undergone right below-knee amputation for acute arterial thrombosis, and who had not previously experienced chronic phantom limb or stump pain, was scheduled for emergency open appendectomy. For anesthesia, we induced SAB with a hyperbaric tetracaine solution. No paresthesia occurred during administration. However, the patient immediately complained of severe, lightning-bolt pain in the right lower limb stump after the SAB was established. He was given intravenous pentazocine, which promptly resolved the pain. Appendectomy was then performed under sedation using intravenous midazolam. The patient did not experience further deafferentation pain during his hospital stay and has reported no stump pain since discharge from the hospital. This case report suggests that SAB induces deafferentation pain in some patients and that this unusual pain can be treated with pentazocine. [ABSTRACT FROM AUTHOR]

Background Intravenous drug abuse (IVDA) is a common problem; there were more than 16 million users worldwide in 2008. Numerous reports highlight the infectious skeletal complication associated with IVDA. Objective To determine septic arthritis pathogens in IVDA in a U.S. hospital and compare the current causative organisms to a cohort from the 1980s at the same institution. Methods An institutional review board-approved retrospective cohort study compared a consecutive series of IVDA septic arthritis patients over a 10-year period, 1999–2008 (Group B), with an IVDA septic arthritis database that was collected in the 1980s (Group A). Endpoints were: bacterial species and staph species antibiotic susceptibility. Results Group B included 58 patients (35 men, 23 women) with a median age of 46.5 years. Group A included 38 patients (30 men, 8 women), with a median age of 32.5 years. The sets were significantly different in pathogens ( p = 0.0443). The most common organisms were Staphylococcus (staph) species (B 74.51%, A 52.63%), followed by Streptococcus (strep) species (B 7.84%, A 31.58%), Pseudomonas (B 13.73%, A 13.16%), and Serratia (B 3.92%, A 2.63%). Of the total number of septic joints, methicillin-resistant Staphylococcus aureus (MRSA) made up 39% of Group B and 34% of Group A. However, within the staph species, MRSA made up 53% of Group B and 65% of Group A. Strep species made up 7.84% (Group B) vs. 31.58% (Group A), and Pseudomonas (13%) and Serratia (3–4%) were similar. In the Group B cohort, methicillin-susceptible Staphylococcus aureus (MSSA) had a predilection to infect the knee (94.4%), whereas MRSA was found more often in the hip (57.1%). Conclusions In IVDAs, MRSA is the most common pathogen causing septic arthritis. The ratio of staph species in septic joints is increasing, and the ratio of MRSA to MSSA remains high (>50%). Strep species are much less common. [ABSTRACT FROM AUTHOR]

Objective: Bridelia micrantha is among the commonly used herbs in the traditional management of disease conditions. This study aimed to evaluate the antinociceptive and antioxidant effects of the hydromethanolic extract of B. micrantha stem bark. Methods: The acute oral toxicity of the extract was evaluated using up and down method. The antinociceptive effects of B. micrantha extract at the doses of 50, 100 and 200 mg/kg were investigated using acetic acid-induced writhing reflex and tail flick method. The effect of B. micrantha on thiopentone-induced narcosis was also investigated. The antioxidant effect of B. micrantha was investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) photometric assay. Results: The extract was well-tolerated at the high dose (2000 mg/kg) used for the acute toxicity study. The extract produced a significant dose-dependent decrease in the mean number of abdominal constriction in the acetic acid-induced writhing reflex when compared to the negative control. Both the extract (200 mg/kg) and paracetamol (400 mg/kg) produced 61.85 and 73.08% inhibition of writhing reflex, respectively. B. micrantha and pentazocine (3 mg/kg) caused a significant increase in the pain reaction time (PRT) in treated rats when compared to the negative control group in tail flick method. The pretreatment of the rats with B. micrantha at different doses increased the normal sleeping time of thiopentone from 69.33 ± 7.31 min to an average of 105.33 ± 11.88 min. The extract also produced concentration-dependent increase in percentage antioxidant activity in DPPH photometric assay. Conclusion: This study demonstrates that B. micrantha possess potent antinociceptive and antioxidant activities, which validate its use in folkloric medicine for this purpose. [ABSTRACT FROM AUTHOR]

The article offers information on a study on the efficacy of ketamine combined with pentazocine and meperidine as epidural anaesthesia for dogs. Topics include clinico-anaesthetic changes caused by the drug combination, and the results which show significant alteration in rectal temperature, respiration and heart rate in the initial observation intervals. Other results include quicker analgesia onset and markedly longer duration of analgesia, standing time, and recovery time.

Introduction: Pain is a very well-known signal of ill health and analgesics are the drugs that are used to relieve pain. The main problem with these drugs remains that of side effects. Safer alternatives are natural herbs. Guduchi (Tinospora cordifolia) is one such plant with analgesic potential but few studies are there. Objective: To evaluate the analgesic activity of commercially available extract of Guduchi (T. cordifolia). Materials and Methods: For this purpose commercially available extract of Guduchi (T. cordifolia) by Himalaya Drug Company, Bangalore was used. Albino rats were divided randomly in three groups of six rats each. Group 1 (control) received distilled water orally, group 2 (test) received T. cordifolia extract in dose of 300 mg/kg orally and group 3(standard) received Pentazocine in dose 10mg/kg intraperitoneally. Analgesic activity was evaluated using hot plate and abdominal writhing method. All the observations were analysed statistically using student's t-test. Observation and Results: T. cordifolia extract significantly (p<0.05) increased the response time and decreased the number of writhes in hot plate method and abdominal writhing method respectively, on comparison with the control group. Conclusions: The above findings suggest that this commercially available extract of Guduchi (T. cordifolia) possess analgesic activity. This analgesic activity probably involves peripheral as well as central mechanisms as the extract showed analgesic activity in both hot plate and abdominal writhing method. [ABSTRACT FROM AUTHOR]

Abstract: The potent orexigenic peptide neuropeptide Y (NPY) has been considered as a possible endogenous ligand for a subpopulation of sigma receptors (SigR). However, their mutual interaction with reference to feeding behavior remains poorly understood. In the present study, we explored the possible interaction between sigma1 receptors (Sig1R) agonist, pentazocine, and NPY on food intake in satiated rats. While pentazocine dose-dependently reduced the food intake, NPY significantly increased it at 2, 4 and 6h post injection time points. In combination studies, pretreatment with NPY (0.1nmol/rat, intra-PVN) normalized the inhibitory effect of pentazocine (60μg/rat, intra-PVN) on food intake. Similarly, pre-treatment with pentazocine (30μg/rat, intra-PVN) significantly antagonized the orexigenic effect of NPY (0.5 and 1.0nmol/rat, intra-PVN). Moreover, pentazocine treatment decreased NPY immunoreactivity in arcuate (ARC), paraventricular (PVN), dorsomedial (DMH) and ventromedial (VMH) nuclei of hypothalamus. However, no change was observed in lateral hypothalamus (LH). Study implicates the reduced NPY immunoreactivity for the anorectic effect observed following pentazocine injections. Therefore, the concomitant activation of the NPYergic system along with the Sig1R agonist treatment may serve a useful purpose in the management of the unwanted side effects related to energy homeostasis. [Copyright &y& Elsevier]

The σ1 receptor is an integral membrane protein that shares no homology with other receptor systems, has no unequivocally identified natural ligands, but appears to play critical roles in a wide variety of cell functions. While the number of reports of the possible functions of the σ1 receptor is increasing, almost no information about the three-dimensional structure of the receptor and/or possible modes of interaction of the σ1 protein with its ligands have been described. Here we performed an in vitro/in silico investigation to analyze the molecular interactions of the σ1 receptor with its prototypical agonist (+)-pentazocine. Accordingly, 23 mutant σ1 isoforms were generated, and their interactions with (+)-pentazocine were determined experimentally. All direct and/or indirect effects exerted by the mutant residues on the receptor–agonist interactions were reproduced and rationalized in silico, thus shining new light on the three-dimensional structure of the σ1 receptor and its ligand binding site. [ABSTRACT FROM AUTHOR]

Background and Aim A double-balloon ( DB) endoscope can be selectively inserted into the afferent loop to carry out endoscopic retrograde cholangiopancreatography ( ERCP) in patients with surgically altered anatomy, allowing various types of endoscopic treatments for pancreaticobiliary diseases to be successfully carried out. In order to make such a lengthy procedure more comfortable and safe, sedatives and carbon dioxide ( CO2) insufflation are widely used for gastrointestinal endoscopy. However, these techniques can increase the risk of CO2 retention. Recently, a new sensor for transcutaneous measurement of partial pressure of carbon dioxide ( PCO2) has been introduced. The aim of the present study was to evaluate the changes in transcutaneous PCO2 ( PtcCO2) during DB-ERCP with CO2 insufflation under conscious sedation and assess any complications related to sedation and CO2 insufflation. Methods A total of 312 patients underwent DB-ERCP with CO2 insufflation at our hospital between March 2009 and December 2012. The patients were moderately sedated using midazolamwith or without pentazocine. PtcCO2 was measured by a non-invasive sensor throughout DB-ERCP in all patients. Results The mean peak PtcCO2 during the procedure was significantly higher than the mean PtcCO2 value before and after DB-ERCP. Body mass index, procedure time and dose of pentazocine were significantly higher in the CO2 retention group (peak PtcCO2 ≥ 50 mm Hg). CO2 narcosis was observed in one case. Conclusions DB-ERCP with CO2 insufflation under conscious sedation might have the potential to increase the risk of CO2 retention. Hence, non-invasive and continuous PtcCO2 measurement is useful for early detection of hypercapnia. [ABSTRACT FROM AUTHOR]

The present study was designed to formulate buccal bioadhesive patches of pentazocine hydrochloride employing aminated and sulfated derivatives of tamarind seed polysaccharide (TSP). The patches were evaluated for their physicomechanical characteristics, swelling index,in vitrorelease, andin vivorelease profiles. Thein vitrorelease of the drug was found to depend on the swelling index of the polymers. The sulfated TSP patches were releasing drug at a faster rate as compared to aminated TSP patches. The oral administration of aminated patches to rats was found to enhance the bioavailability of pentazocine hydrochloride 2.8 times as compared to oral solution. [ABSTRACT FROM AUTHOR]

Background: Pain relief remains the most fundamental and consequential aspect of surgery for patients throughout perioperative period. Dexmedetomidine has created an interest in α2-adrenoceptor agonists in the management of pain and hence the aim of this study was to evaluate the effectiveness of the drug in hilly population of North India. Materials and Methods: Patients, irrespective of gender, were randomly allocated to two groups, control and test, each having 30 patients. Test group received an infusion of dexmedetomidine at a rate of 0.5 µg/kg/h 30 min before induction and 0.6 µg/kg/h after inducing anesthesia. Control patients received a volume-matched infusion of normal saline as placebo. Approximately 2 min before induction, analgesia was provided in the form of pentazocine, 0.5 mg/kg in control and 0.3 mg/kg in the test group. Induction was performed by 2 mg/kg thiopentone sodium supplemented with intravenous boluses of 25 mg thiopentone sodium every 15 s until loss of eyelid reflex (determined every 15 s). Induction dose of thiopentone sodium and total pentazocine dose were recorded. Recovery was assessed on the clinical recovery score (CRS) scale. Results: Infusion of dexmedetomidine decreased the induction dose of thiopentone approximately by 33% and of pentazocine dose by approximately 39% in patients undergoing laparoscopic cholecystectomy. Moreover, incidence of pain was also decreased significantly. Improved CRS from 4.33 to 6.87 was noticed immediately post-operatively in dexmedetomidine group of patients. Conclusion: Infusion of dexmedetomidine during the laparoscopic cholecystectomy decreases the requirement of thiopentone sodium and pentazocine and leads to early recovery of patients. [ABSTRACT FROM AUTHOR]

Background. Parenteral opioids, thus, are still popular for pain relief in labor in many countries throughout the world. Aim. To evaluate and compare the efficacy of intramuscular tramadol and pentazocine in the first stage of labor. Method. Sixty-five patients were divided into pentazocine group and tramadol group. Subjects received either 30 mg pentazocine or 1 mg/kg tramadol intramuscularly. Pain was assessed using visual analog scale (VAS) before the administration of the drug, at 1 h, 2 h, 4 h, and at full dilatation. Maternal and neonatal side effects were determined. Results. Analgesic effect of the two drugs was not significantly different. Neither of these analgesics was effective towards the end of the first stage. However, in the tramadol group, the majority of women (55%) rated pain as severe, whereas in the pentazocine group, the majority of women (60%) rated pain as moderately severe. There were not many side effects with either of the drug in the given dosage. Mean injection to delivery interval was significantly shorter in the tramadol group as compared to the pentazocine group. Conclusion. Pentazocine or tramadol can be given for labor pain relief as an alternative to epidural analgesia in resource poor setting. [ABSTRACT FROM AUTHOR]

Although pentazocine binds to σ1-receptor (σ1R) with high affinity, the physiological relevance of its binding remains unclear. We first confirmed that σ1R stimulation with pentazocine rescues contractile dysfunction following pressure overload (PO)-induced cardiac hypertrophy ovariectomized (OVX) female rats. In in vivo studies, vehicle, pentazocine (0.5-1.0 mg/kg ip), and NE-100 (1.0 mg/kg po), a σ1R antagonist, were administered for 4 wk (once daily) starting from the onset of aortic banding after OVX. We also examined antihypertrophic effects of pentazocine (0.5-1 μM) in cultured cardiomyocytes exposed to angiotensin II. Pentazocine administration significantly inhibited PO-induced cardiac hypertrophy and rescued hypertrophyinduced impairment of cardiac dysfunctions such as left ventricular end-diastolic pressure, left ventricular developed pressure, and left ventricular contraction and relaxation (±dp/dt) rates. Coadministration of NE-100 with pentazocine eliminated pentazocine-induced amelioration of heart dysfunction. Interestingly, pentazocine administration inhibited PO-induced σ1R reduction and inositol-1,4,5-trisphosphate (IP3) receptor type 2 (IP3R2) upregulation in heart. Therefore, the reduced mitochondrial ATP production following PO was restored by pentazocine administration. Furthermore, we found that σ1R binds to the ryanodine receptor (RyR) in addition to IP3 receptor (IP3R) in cardiomyocytes. The σ1R/RyR complexes were decreased following OVX-PO and restored by pentazocine administration. We noticed that pentazocine inhibits the ryanodine-induced Ca2+ release from sarcoplasmic reticulum (SR) in cultured cardiomyocytes. Taken together, the stimulation of σ1R by pentazocine rescues cardiac dysfunction by restoring IP3R-mediated mitochondrial ATP production and by suppressing RyR-mediated Ca2+ leak from SR in cardiomyocytes. [ABSTRACT FROM AUTHOR]

Abstract: Objective: To evaluate the anti-inflammatory and analgesic activities of methanolic leaf extract of Indigofera cassioides (I. cassioides) (MEIC) using various animal models. Methods: Anti-inflammatory and analgesic activities of MEIC was assessed by using different animal models. Anti-inflammatory activity of the extract was evaluated by using carrageenan-induced rat paw edema and cotton pellet granuloma method. Anti-nociceptive activity of the extract was evaluated for its central and peripheral pharmacological actions by using Eddy's hot plate method and acetic acid-induced writhing respectively. The study was carried out using dose of 200 & 400 mg/kg orally. Aceclofenac, aspirin and pentazocine was used as standard drugs to evaluate anti-inflammatory and analgesic activities, respectively. Results: Treatment with MEIC significantly (P<0.001) decrease the paw volume and weight of cotton pellet in the tested models. It also exhibit potent analgesic activity on chemical and thermal induced pain in mice. MEIC exhibit potent and dose dependent anti-inflammatory and analgesic activities in all the tested animal models. Conclusions: All the results obtained revealed that the extract MEIC showed potent anti-inflammatory and anti-nociceptive activity against all the tested models and the results obtained were comparable with the standards used. The activity of the extract may be due to the presence of terpenoids, flavonoids and other phytochemicals. [Copyright &y& Elsevier]

Background: Narcotic drugs have been used to attenuate laryngoscopy and intubation induced circulatory responses, but are not always available due to tough narcotics laws. Nalbuphine a synthetic opioid, free from restrictions has been in use for post-operative pain relief. Hence, we decided to compare nalbuphine and pentazocine for attenuation of hemodynamic effects during larygoscopy and endotracheal intubation in a randomized, double-blind clinical study. Materials and Methods: A total of 60 patients (ASA I and II) of either sex, between 18 years and 50 years were given either nalbuphine 0.2 mg/kg (group N, n = 30) or pentazocine 0.5 mg/kg (group P, n = 30) 5 min before induction of general anesthesia. After, induction with thiopentone and endotracheal intubation with succinylcholine balanced anesthesia was maintained with O2:N2O, 0.2% halothane and non-depolarizing relaxants for surgical duration. Changes in heart rate (HR), systolic blood pressure (SBP), diastolic pressure, mean arterial pressure, and rate pressure product calculated by HR x SBP were recorded at various time intervals. Results: A non-significant fall (P > 0.05) up to 3 min and thereafter a significant rise (P < 0.05) in all the parameters were observed throughout the remaining study period with nalbuphine, whereas a continuous and significant (P < 0.05) rise in these parameters were observed with pentazocine. Maximum rise in both the group was observed immediately after larygoscopy and intubation and these started to return toward the basal values at the end of the study period, but remained above the initial values. (pentazocine > nalbuphine P = <0.01). Conclusion: Nalbuphine effectively reduces the tachycardia, hypertension, and cardiac workload associated with laryngoscopy and endotracheal intubation. [ABSTRACT FROM AUTHOR]

Background: Postoperative pain leads to patient discomfort, decreased level of satisfaction, prolonged recovery, and higher health costs. Acute pain control therefore improves the overall quality of life in patients undergoing cesarean section. Pain relief is a fundamental human right, but there is no gold standard for post-cesarean section pain management. Objective: To compare the efficacy of pentazocine and tramadol used in unimodal and multimodal (in combination with piroxicam) approach, in the management of post-cesarean section pain. Materials and methods: This study employed a random allocation design to compare the effectiveness of intramuscular pentazocine (60 mg) or tramadol (100 mg) as single analgesic agent and in combination with daily intramuscular piroxicam 20 mg, for the management of post-cesarean section pain during the immediate 12 hours after surgery. The primary outcome measure was control of postoperative pain, while the secondary outcome measures were the analgesic agent onset of action, duration of action, patient satisfaction, and maternal and neonatal adverse outcomes. Data obtained were entered into a predesigned sheet and analyzed with the Statistical Package for Social Sciences version 17. Means ± standard deviation (SD) were calculated for the quantitative variables, and the difference between two independent groups was compared using unpaired Student's t-test. The level of significance was set at 0.05. Results: A total of 120 patients were equally and randomly allocated to four study groups - two that received unimodal analgesia (the pentazocine group and the tramadol group) and two that received multimodal analgesia (the pentazocine-piroxicam group and the tramadol-piroxicam group). Among the unimodal groups, tramadol had a faster onset of action, but pentazocine had a longer duration of action and provided better control of pain. Among the multimodal groups, the combination of pentazocine with piroxicam was superior to the tramadol with piroxicam combination, and it was also more effective than pentazocine alone. Conclusion: The multimodal approach of combining pentazocine with piroxicam is a safe, effective, and an acceptable mode of analgesia for post-cesarean section pain management, especially in a resource-constrained setting. [ABSTRACT FROM AUTHOR]

To assess the efficiency and safety of parenteral analgesics for pain relief in acute pancreatitis. We carried out an electronic search of PubMed, Cochrane Library, EMBASE, WEIPU, CNKI and CBM and a manual search for eligible studies. The methodological quality of included trials and quality of evidence were examined by the Cochrane Collaboration's tool for assessing risk of bias and GRADE, respectively. The data were mainly analyzed descriptively and some were pooled by Review manager 5. Eight randomized controlled trials with a total of 356 patients were finally included in this systematic review. Compared with procaine, pentazocine led to lower pain severity: day 1, Mean Difference (MD), 95%CI: 40.0 [35.3, 44.7]; day 2, MD, 95%CI: 24.00 [20.88, 27.12]; day 3, MD, 95%CI: 5.00 [2.17, 7.83], and it decreased the requirement for additional analgesics, Relative Risk, 95%CI: 2.23 [1.63, 3.05]. The combination of fentanyl, atropine, droperidol and lidocaine rendered lower pain score: day 1, MD, 95%CI: −5.46 [−6.95, −3.97]; day 2, MD, 95%CI: −5.78 [−7.39, −4.17]. Patients treated with metamizole tended to had lower pain than those treated with morphine, MD, 95%CI: −2.60 [−2.95, −2.25]. Nausea, emesis and vomiting were the common adverse events reported and there was almost no significant difference between different agents on safety. The systemic review showed that the randomized controlled trials comparing different analgesics were of low quality and did not favor clearly any particular analgesic for pain relief in acute pancreatitis. [ABSTRACT FROM AUTHOR]

Abstract: A number of laboratory studies have confirmed the efficacy of opioid medication in reducing pain generated by a number of psychophysical modalities. However, one implicit assumption of clinical and experimental pain testing of analgesics is that the analgesic response is stable and will be comparable across repeated administrations. In the current study, the repeatability of opioid analgesia was assessed in a randomized, double-blinded study using 3 psychophysical pain modalities (e.g., thermal, pressure, and ischemic) over 4 medication sessions (2 with active drug, 2 with placebo). Psychophysical responses were evaluated before and after intravenous administration of either morphine (0.08mg/kg; n=52) or pentazocine (0.5mg/kg; n=49). To determine the ability of a drug to reduce pain, 4 analytic methods (i.e., absolute change, percent change, ratio, and residualized change scores) were calculated to generate separate analgesic index scores for each measure and drug condition. All analgesic index scores demonstrated a greater analgesic response compared to saline for both medications, but stability (i.e., test-retest correlations) of the opioid analgesic indices depended on the pain measurement. Ischemic pain outcomes were moderately stable across sessions for both opioid medications; however, heat and pressure analgesic index scores were moderately stable for only morphine and pentazocine, respectively. Finally, within stimulus modalities, analgesic index scores were highly correlated with each other, suggesting that the different methods for computing analgesic responses provided comparable results. These results suggest that analgesic measures are able to distinguish between active drugs. In addition, analgesic responses to morphine and pentazocine demonstrate at least moderate reliability. [Copyright &y& Elsevier]

Cerebrovascular disorders contribute to the morbidity and disability associated with illicit drug use. Drug abusers have an increased risk of both hemorrhagic and ischemic stroke. In geographic areas with a high prevalence of illicit drug use, drug abuse is a frequent cause of stroke in the young adult. The illicit drugs more commonly associated with stroke are psychomotor stimulants, such as amphetamine and cocaine. Less commonly implicated are opioids and psychotomimetic drugs, including cannabis. Toxicology screening for illicit drugs should be done in young patients with stroke with no obvious cause, or if suggested by history or examination. Although in some patients the mechanism of stroke is identified using neuroimaging and other modern diagnostic tools, in a sizeable fraction of cases the mechanism of stroke remains unclear. Further studies are needed to elucidate the role of hemodynamic and immunologic mechanisms in these cases. [ABSTRACT FROM AUTHOR]

Context: The administration of opioids intrathecally as a sole anesthetic has proven to be effective in providing adequate surgical anesthesia without much hemodynamic instability. Aim: This study aims to determine the efficacy and safety of intrathecal pentazocine as a sole anesthetic drug in patients undergoing lower limb surgeries. Settings and Design: It was a randomized single blinded study conducted in 60 patients undergoing lower limb surgeries. Subjects and Methods: The patients were randomly divided into 2 groups of 30 patients in each group. Group A received 2 ml (60 mg) intrathecal pentazocine and Group B received 2 ml intrathecal 0.5% bupivacaine heavy before surgery. Duration of surgery, onset of sensory, and motor blockade and their duration, heart rate (HR), mean arterial pressure (MAP), and time for first rescue analgesia were statistically analyzed. Results: Group B showed a statistically significant earlier onset of sensory (2.54 ± 0.87 vs. 3.66 ± 1.10 min) and motor blocks (2.22 ± 0.77 vs. 3.29 ± 1.06 min).The majority of patients in the group A (30%) attained the highest level of sensory block of T11, whereas the majority in group B (33.3%) attained the highest level of sensory block of T8. Majority in the Group A (60%) showed a motor block of Bromage scale Grade III at the beginning of surgery, whereas the majority in Group B (80%) showed a motor block of Bromage scale Grade IV. Duration of sensory block was significantly prolonged in group B (124.33 ± 14.84 vs. 115.60 ± 18.39 min). However, duration of motor blockade was similar in both groups. Group B patients required first analgesia earlier than Group A (5.24 ± 1.98 h vs. 2.48 ± 0.51 h) which was significant. There was no difference between groups with regard to HR intra-operatively. On comparison of the pre-induction MAP between 2 groups, there was no difference. But later on at 1, 3, 5 min intervals, the MAP was less in group B. But at 10 and 15 min there was no significant difference between groups. The significantly reduced MAP in group B was evident again at 30, 45, and 60 min. There was no difference between groups at 90 and 120 min. Group B required first analgesia earlier than group A which was statistically significant. Conclusions: Because of adequate surgical anesthesia, intraoperative hemodynamic stability and prolonged post-operative analgesia, we recommend the use of intrathecal pentazocine as a sole anesthetic agent for lower limb surgeries. [ABSTRACT FROM AUTHOR]

We experienced an unreported rare case with an adnexal mass causing severe acute abdomen during pregnancy. A 30-year-old Japanese pregnant woman was transported to our hospital for her right lower abdominal pain at 30 weeks of gestation. Magnetic resonance imaging and ultrasound demonstrated a cyst measuring 3-4 cm in diameter adjacent to the right ovary, and a parovarian cyst was considered to be the most probable diagnosis. We strongly suspected torsion of the ovarian pedicle or fallopian tube in conjunction with her clinical symptoms. Laparotomy revealed that the elongated right fallopian tube accompanied by a paratubal cyst was coiling tightly 2.5 times round the right ovary, causing apparent congestion and enlargement of the right ovary. Soon after we released the congested right ovary from the coiling of the fallopian tube, the congestion subsided. The postoperative course was favorable, and pregnancy and delivery were uneventful. [ABSTRACT FROM AUTHOR]

Aim The aim of the present study was to evaluate the efficacy and safety of giving pentazocine as an analgesic with benzodiazepine during endoscopic retrograde cholangiopancreatography ( ERCP). Methods The paradoxical reactions ( PR) incidence was evaluated as an indicator of usefulness. Transcutaneous arterial carbon dioxide tension ( PtcCO2) was evaluated as an indicator of safety. Atotal of 160 patients were enrolled. Subjects were randomly divided into two groups; group 1 sedated with midazolam only and group 2 sedated both with midazolam and pentazocine (7.5 mg). Results The initial dosage introduced sedation before procedure was significantly higher in group 1. The occurrence rate of PR's in group 1 was significantly higher compared to that in group2 ( P = 0.0108). Although maximum PtcCO2 observed during sedation did not differ between the two groups (48.7 ± 7.2, 50.3 ± 7.6 mmHg, respectively),maximum PtcCO2 during the first 15 min after the start of sedation was significantly higher in group 2 than in group 1 ( P = 0.0294). In multivariate analysis, procedure duration (odds ratio [ OR] = 1.048) and midazolam dose ( OR = 1.221) were predictive factors for PR. Conclusion The administration of pentazocine is significantly reduced the incidence of PR's in patients under midazolaminduced sedation during ERCP. [ABSTRACT FROM AUTHOR]

Background and Aim: Radiofrequency ablation (RFA) therapy is frequently used as first-line treatment for small hepatocellular carcinoma (HCC). RFA is often associated with pain; however, no definitive solution has been established for its relief. We retrospectively analyzed the safety and efficacy of the combination of pentazocine and midazolam to relieve pain experienced by HCC patients undergoing RFA., Methods: We studied 77 patients with 98 HCCs treated with RFA between January 2015 and August 2019. Patients were divided into two groups: the sedative-free group, which included those who received pentazocine alone, and the pentazocine-midazolam group, which included those who received a combination of pentazocine and midazolam. The degrees of analgesia and sedation were evaluated using the numerical rating scale (NRS) and the Richmond Agitation-Sedation Scale (RASS), respectively. Other parameters such as treatment time, awakening time, midazolam dosage, vital signs, local recurrence rate, and time to recurrence were also examined., Results: The median NRS score and RASS score were significantly lower in the pentazocine-midazolam group. Ninety-five percent of patients in the pentazocine-midazolam group had no memory of the RFA session. The treatment time and awakening time were prolonged for the pentazocine-midazolam group. No significant differences in oxygen saturation, recurrence rates, and time to local recurrence were observed between groups., Conclusion: A combination of pentazocine and midazolam is safe and effective for pain and anxiety relief experienced by patients undergoing RFA for local treatment of HCC., (© 2022 The Authors. JGH Open published by Journal of Gastroenterology and Hepatology Foundation and John Wiley & Sons Australia, Ltd.)

The standard assay for the determination of σ1 receptor affinities of novel compounds is a competitive binding assay using [3H]-(+)-pentazocine as radioligand and membrane preparations from guinea pig brain. Herein, a novel competitive binding assay was developed employing the hematopoietic cell line of human multiple myeloma (RPMI 8226), which expresses a large amount of the human σ1 receptor. Membrane fragments of RPMI 8226 cells were prepared and characterized. A Western blot analysis confirmed the high density of σ1 receptors in this cell line. Assay conditions were carefully optimized leading to an incubation period of 120 min, an incubation temperature of 37°C, and receptor material for each well was prepared from 300,000 cells. It was shown that a large excess (10 μM) of (+)-pentazocine, haloperidol, and di-o-tolylguanidine provided the same results during determination of the nonspecific binding. Saturation experiments with the radioligand [3H]-(+)-pentazocine led to a K d -value of 36±0.3 nM and a B max -value of 477±7 fmol/mg protein. These data resulted in approximately 122,000 σ1 binding sites per cell. The assay was validated by using six known σ1 ligands and eight σ1 ligands prepared in our lab. The K i -values determined with RPMI 8226-derived receptor material are in good accordance with the K i -values obtained with guinea pig brain membrane preparations. Compared with guinea pig brain preparations, the RPMI 8226-derived receptor material represents a better standardized receptor material with a high density of human σ1 receptors. [ABSTRACT FROM AUTHOR]

Abstract: Several lines of evidence suggest that σ1 receptors regulate intracellular calcium concentration [Ca2+]i. However, no previous studies have demonstrated a consistent role for these receptors in the modulation of extracellular calcium entry through plasmalemmal voltage-dependent calcium channels (VDCCs). To search for evidence of such a role we compared [Ca2+]i under basal conditions and after depolarization with KCl in fura-2-loaded synaptosomes from wild-type and σ1 receptor knockout (σ1R-KO) mice. We also tested the effects of the selective σ1 receptor agonists PRE-084 and (+)-pentazocine and antagonists BD-1047 and NE-100 on the increase in [Ca2+]i induced by depolarization with 60mM KCl. Mibefradil, a nonselective blocker of VDCCs, was used as a positive control. Basal [Ca2+]i and the increase in [Ca2+]i caused by KCl-induced depolarization were similar in brain synaptosomes from both wild-type and σ1R-KO mice. Mibefradil (1–30μM) and all σ1 receptor ligands studied (3–100μM) inhibited the KCl-induced increase in [Ca2+]i in a concentration-dependent way. The order of maximum inhibition for the ligands compared here was NE-100>BD-1047=PRE 084>(+)-pentazocine. There were no appreciable differences in their effects between wild-type and σ1R-KO mice. These findings indicate that σ1 receptors are not involved in calcium influx through VDCCs or in the inhibitory effects of these σ1 ligands on Ca2+ channels. [Copyright &y& Elsevier]