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S Sukhbir, S Yashpal, A Sandeep
Nefopam hydrochloride (NFH) is a non-opioid centrally acting analgesic drug used to treat chronic condition such as neuropathic pain. In current research, sustained release nefopam hydrochloride loaded nanospheres (NFH-NS) were auspiciously synthesized using binary mixture of eudragit RL 100 and RS 100 with sorbitan monooleate as surfactant by quasi solvent diffusion technique and optimized by 3(5) Box-Behnken designs to evaluate the effects of process and formulation variables. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetric (DSC) and X-ray diffraction (XRD) affirmed absence of drug-polymer incompatibility and confirmed formation of nanospheres...
September 2016: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Sung Kwan Choi, Myung Ha Yoon, Jung Il Choi, Woong Mo Kim, Bong Ha Heo, Keun Seok Park, Ji A Song
BACKGROUND: Although intraoperative opioids provide more comfortable anesthesia and reduce the use of postoperative analgesics, it may cause opioid induced hyperalgesia (OIH). OIH is an increased pain response to opioids and it may be associated with N-methyl-D-aspartate (NMDA) receptor. This study aimed to determine whether intraoperative nefopam or ketamine, known being related on NMDA receptor, affects postoperative pain and OIH after continuous infusion of intraoperative remifentanil...
October 2016: Korean Journal of Anesthesiology
Maud Pétrault, Sophie Gautier, Vincent Bérézowski, Thavarak Ouk, Michèle Bastide, Olivier Pétrault, Régis Bordet
Analgesics such as opioid agonists are usually not given during the post-operative phase of experimental stroke because they are susceptible to interfere with the evaluation of neuroprotective therapies. Here we investigate the potential of acetaminophen and nefopam, two non-opioid analgesic drugs, to exert an analgesic effect without inducing neuroprotection in a murine model of ischemic stroke. We demonstrate that acetaminophen (200 mg/kg, PO) induces a significant decrease in the infarct volume, particularly in the cortex (VEHICLE: 200...
September 30, 2016: Fundamental & Clinical Pharmacology
Daphnée Michelet, Juliette Andreu-Gallien, Alia Skhiri, Arnaud Bonnard, Yves Nivoche, Souhayl Dahmani
BACKGROUND AND AIMS: Laparoscopic pediatric surgery allows a rapid postoperative rehabilitation and hospital discharge. However, the optimal postoperative pain management preserving advantages of this surgical technique remains to be determined. This study aimed to identify factors affecting the postoperative recovery of bowel function after laparoscopic surgery in children. MATERIAL AND METHODS: A retrospective analysis of factors affecting recovery of bowel function in children and infants undergoing laparoscopic surgery between January 1, 2009 and September 30, 2009, was performed...
July 2016: Journal of Anaesthesiology, Clinical Pharmacology
Mahesh Gokara, Vidadala V Narayana, Vineet Sadarangani, Shatabdi Roy Chowdhury, Sreelaxmi Varkala, Dhevalapally B Ramachary, Rajagopal Subramanyam
In this study, molecular binding affinity was investigated for Nefopam analogues (NFs), a functionalized benzoxazocine, with human serum albumin (HSA), a major transport protein in the blood. Its binding affinity and concomitant changes in its conformation, binding site and simulations were also studied. Fluorescence data revealed that the fluorescence quenching of HSA upon binding of NFs analogues is based on a static mechanism. The three analogues of NFs binding constants (KA) are in the order of NF3>NF2>NF1 with values of 1...
July 25, 2016: Journal of Biomolecular Structure & Dynamics
Do Yun Kim, Joo Wung Chae, Chang Hun Lim, Bong Ha Heo, Keun Suk Park, Hyung Gon Lee, Jeong Il Choi, Myung Ha Yoon, Woong Mo Kim
BACKGROUND: Nefopam has been known as an inhibitor of the reuptake of monoamines, and the noradrenergic and/or serotonergic system has been focused on as a mechanism of its analgesic action. Here we investigated the role of the spinal dopaminergic neurotransmission in the antinociceptive effect of nefopam administered intravenously or intrathecally. METHODS: The effects of intravenously and intrathecally administered nefopam were examined using the rat formalin test...
July 2016: Korean Journal of Pain
Hyun Seung Jin, Yong Chul Kim, Yongjae Yoo, Changsoon Lee, Chan Woo Cho, Won-Joong Kim
OBJECTIVES: A double-blind randomised study to evaluate the opioid sparing effect and safety of nefopam when administered via intravenous patient controlled analgesia (PCA) with fentanyl. METHODS: Patients planned for elective open laparotomy, were randomly assigned to receive into fentanyl 25 µg/ml (SF group) or nefopam 2.4 mg/ml plus fentanyl 25 µg/ml (NF group). Patients were assessed before surgery and for 24 h postoperatively. RESULTS: Total PCA fentanyl consumption was significantly lower in the NF group (n = 35) than the SF group (n = 36)...
August 2016: Journal of International Medical Research
Laurence Dangers, Louis Laviolette, Bény Charbit, Thomas Similowski, Capucine Morélot-Panzini
BACKGROUND: Dyspnoea is a distressing and debilitating symptom with a major impact on quality of life. Alleviation of dyspnoea therefore constitutes a major clinical challenge. When causative physiological disorders cannot be corrected ("persistent dyspnoea"), nonspecific treatment must be considered. Morphine alleviates dyspnoea but has numerous side-effects including ventilatory depression, which justifies looking for alternatives. Certain forms of dyspnoea involve C-fibres, and can be attenuated by C-fibres blockade...
August 2016: Pulmonary Pharmacology & Therapeutics
Won Uk Koh, Jin Woo Shin, Ji-Yeon Bang, Sae Gyeol Kim, Jun-Gol Song
BACKGROUND: Nefopam hydrochloride is a centrally acting compound that induces antinociceptive and antihyperalgesic properties in neuropathic pain models. Previous reports have shown that activation of adenosine triphosphate (ATP)-sensitive and calcium-activated potassium (KATP and KCa2+) channels has antiallodynic effects in neuropathic pain. In the present study, we evaluated the relationship between potassium channels and nefopam to determine whether the antiallodynic effects of nefopam are mediated by potassium channels in a neuropathic pain model...
September 2016: Anesthesia and Analgesia
Hyo-Seok Na, Ah-Young Oh, Bon-Wook Koo, Dae-Jin Lim, Jung-Hee Ryu, Ji-Won Han
Breast cancer surgery is known to cause severe acute postoperative pain, which can persist for a long time. We administered nefopam preventively to patients undergoing lumpectomy with axillary lymph node dissection or sentinel lymph node biopsy, and evaluated its efficacy on acute and chronic postoperative pain.Enrolled patients were assigned to the nefopam (n = 41) or the control (n = 42) group. Before initiating the operation, 20 mg of nefopam was given to the patients of the nefopam group, and normal saline was used in the control group...
May 2016: Medicine (Baltimore)
Jee Youn Moon, Sang Sik Choi, Shin Young Lee, Mi Kyung Lee, Jung Eun Kim, Ji Eun Lee, So Hyun Lee
BACKGROUND: Nefopam is a non-opioid, non-steroidal, centrally acting analgesic drug. The concomitant use of opioids and nefopam is believed to have many advantages over the administration of opioids alone for postoperative pain management. We conducted a randomized, double-blind study to determine the fentanyl-sparing effect of co-administration of nefopam with fentanyl for postoperative pain management via patient controlled analgesia (PCA). METHODS: Ninety female patients who underwent laparoscopic total hysterectomy under general anesthesia were randomized into 3 groups, Group A, fentanyl 1,000 µg; Group B, fentanyl 500 µg + nefopam 200 mg; and Group C, fentanyl 500 µg + nefopam 400 mg, in a total volume of 100 ml PCA to be administered over the first 48 h postoperatively without basal infusion...
April 2016: Korean Journal of Pain
Jeong Il Choi
No abstract text is available yet for this article.
April 2016: Korean Journal of Pain
Ji-Uk Yoon, Gyeong-Jo Byeon, Ji-Hyun Cheon, Yoon-Mi Choi, Hyun-Su Ri, Seong-Wan Baik
BACKGROUND: Nefopam is a non-opioid non-steroidal centrally acting analgesic. This study was conducted to assess the analgesic efficacy of intravenous patient-controlled analgesia (IV-PCA) using nefopam alone, compared with a combination of morphine and ketorolac, after laparoscopic gynecologic surgery. METHODS: Sixty patients undergoing laparoscopic gynecologic surgery received IV-PCA. Group A (n = 30) received IV-PCA with a combination of morphine 60 mg and ketorolac 180 mg, while group B (n = 30) received nefopam 200 mg (basal rate 1 ml/h, bolus 1 ml, and lockout time 15 min for both)...
April 2016: Korean Journal of Anesthesiology
V V Balandin, E S Gorobec
62 adult patients had highly traumatic cancer head and neck surgery under multimodal non-opioid general anesthesia consisted of dexmedetomidine, lidocane, nefopam and sevoflurane. 18 patients had been intubatedwith fiber optic bronchoscope because of II-IV grade trismus. 10 patients with laryngeal stenosis had been tracheotomizedfor intubation. All these 28 patients had been sedated with dexmedetomidine, lidocane and small doses (10-20 mg) ketamine additionally to local anesthesia. All these patients maintained consciousness and breathed spontaneously...
November 2015: Anesteziologiia i Reanimatologiia
Jian Yu, Eric Solon, Helen Shen, Nishit B Modi, Aravind Mittur
1. This study examined the pharmacokinetics, distribution, metabolism, and excretion of [(14)C] nefopam in rats after a single oral administration. Blood, plasma, and excreta were analyzed for total radioactivity, nefopam, and metabolites. Metabolites were profiled and identified. Radioactivity distribution was determined by quantitative whole-body autoradiography. 2. The pharmacokinetic profiles of total radioactivity and nefopam were similar in male and female rats. Radioactivity partitioned approximately equally between plasma and red blood cells...
November 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
S Mazouz Dorval, J Salleron, Y Guenane, V Nguyen Van Nuoi, C Ozil, M Revol, T Sorin
INTRODUCTION: Bilateral reduction mammaplasty (BRM) is a common procedure in plastic surgery. Our study aims to determine whether single-shot infiltration with ropivacaine during surgery reduces postoperative pain and decreases analgesic consumption. METHODS: In a prospective and monocentric study, all women operated by a single senior plastic surgeon, for whom BRM had been performed were included. The same surgical technique was performed for all patients (a superior pedicle, wise-pattern BRM with a closed-suction drainage)...
April 2016: Annales de Chirurgie Plastique et Esthétique
Jules Greze, Arnaud Vighetti, Pascal Incagnoli, Jean-Louis Quesada, Pierre Albaladejo, Olivier Palombi, Jerome Tonetti, Jean-Luc Bosson, Jean-Francois Payen
PURPOSE: There has been a growing interest in continuous local anaesthetic wound infiltration as a non-opioid technique for postoperative pain relief. The impact of this modality on baseline analgesia after spinal fusion surgery has however been inconclusive. We tested whether continuous wound infiltration with ropivacaine can enhance postoperative analgesia compared to a baseline intravenous multimodal analgesia protocol after spinal fusion surgery. METHODS: In this randomized, double-blinded, placebo-controlled study, a multiholed 19-gauge catheter was placed at the end of the surgical procedure through the wound to permit the continuous administration (8 ml/h) of ropivacaine 0...
February 10, 2016: European Spine Journal
Young Min Ok, Ji Hyun Cheon, Eun Ji Choi, Eun Jung Chang, Ho Myung Lee, Kyung Hoon Kim
BACKGROUND: Neuropathic pain, including paresthesia/dysesthesia in the lower extremities, always develops and remains for at least one month, to variable degrees, after percutaneous endoscopic lumbar discectomy (PELD). The recently discovered dual analgesic mechanisms of action, similar to those of antidepressants and anticonvulsants, enable nefopam (NFP) to treat neuropathic pain. This study was performed to determine whether NFP might reduce the neuropathic pain component of postoperative pain...
January 2016: Korean Journal of Pain
Madhu Sanga, John Banach, Aaron Ledvina, Nishit B Modi, Aravind Mittur
1. The disposition of nefopam, a serotonin-norepinephrine reuptake inhibitor, was characterized in eight healthy male volunteers following a single oral dose of 75 mg [(14)C]-nefopam (100 μCi). Blood, urine, and feces were sampled for 168 h post-dose. 2. Mean (± SD) maximum blood and plasma radioactivity concentrations were 359 ± 34.2 and 638 ± 64.7 ngEq free base/g, respectively, at 2 h post-dose. Recovery of radioactive dose was complete (mean 92.6%); a mean of 79.3% and 13.4% of the dose was recovered in urine and feces, respectively...
November 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Hue Jung Park, Je Uk Park, Woojoo Yoo, Young Eun Moon
PURPOSE: Many studies have examined the postoperative analgesic effects of nefopam in various settings. However, although nefopam is expected to be useful in bimaxillary osteotomy, no published data are available. MATERIAL AND METHODS: We divided 42 patients into nefopam [n = 21, nefopam 20 mg intravenous (i.v.) 30 min before surgery, followed by an i.v. infusion (5 mg/h) beginning immediately postoperatively for 24 h] and control [n = 21, normal saline] groups...
February 2016: Journal of Cranio-maxillo-facial Surgery
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