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Zhurnal Nevrologii I Psikhiatrii Imeni... 2021This paper discusses modern approaches to the diagnosis and management of patients with piriformis syndrome. Epidemiological data on the prevalence of this syndrome in...
This paper discusses modern approaches to the diagnosis and management of patients with piriformis syndrome. Epidemiological data on the prevalence of this syndrome in neurological practice are presented. The anatomical features of this region, leading to the formation of piriformis syndrome, are described in detail. The authors provide diagnostic criteria based on neurological examination and manual muscle testing and discuss the differential diagnosis of piriformis syndrome. New possibilities of treating this syndrome using a fixed combination of diclofenac and orphenadrine registered in the Russian Federation as a drug for intravenous infusion neodolpasse are discussed in detail. The authors cite materials from their own work, a clinical case of managing a patient with piriformis syndrome using neodolpasse is analyzed.
Topics: Humans; Neurologic Examination; Piriformis Muscle Syndrome; Russia
PubMed: 34693699
DOI: 10.17116/jnevro2021121091116 -
Natural Product Research Dec 2021Roemerine is a naturally occurring aporphine alkaloid. In this study, we screened a conformer library of Food and Drug Administration (FDA)-approved drugs to identify...
Roemerine is a naturally occurring aporphine alkaloid. In this study, we screened a conformer library of Food and Drug Administration (FDA)-approved drugs to identify similar drugs that can assist in identifying the biological targets of roemerine. To assess the neuroactivity , we measured the levels of cell metabolites, Brain-Derived Neurotrophic Factor (BDNF) and serotonin (5-HT) in SH-SY5Y cell line. By means of structure-based virtual screening, we identified five drugs that are similar to roemerine; mirtazapine, atomoxetine, epinastine, diphenhydramine and orphenadrine. GC-MS metabolomics study revealed that roemerine has a high impact on alanine-aspartate-glutamate pathway in cell lysate and cultured medium. Additionally, roemerine increased intercellular 5-HT level and intracellular BDNF protein expression at 10 µM. In conclusion, roemerine - a major alkaloid in antidepressant-like effect possessing plants () - has a neuronal activity through increasing BDNF protein expression and affecting serotonergic and glutamatergic systems in SH-SY5Y cell line.
Topics: Alkaloids; Aporphines; Brain-Derived Neurotrophic Factor; Cell Line, Tumor; Humans; Plant Extracts; Serotonin
PubMed: 33025828
DOI: 10.1080/14786419.2020.1830395 -
Zhurnal Nevrologii I Psikhiatrii Imeni... 2022Evaluation of the safety and effectiveness of the use of a fixed combination of orphenadrine and diclofenac for analgesia in the early postoperative period of cardiac...
OBJECTIVE
Evaluation of the safety and effectiveness of the use of a fixed combination of orphenadrine and diclofenac for analgesia in the early postoperative period of cardiac surgery patients.
MATERIAL AND METHODS
There were two analgesia regimens evaluated in a retrospective comparative study. In 23 patients (group 1), Neodolpasse (a fixed combination of 30 mg orphenadrine and 75 mg diclofenac) was administered immediately after trachea extubation. When the severity of pain in VAS increased to more than 50 mm, so 20 mg trimeperidine was administered. In group 2 of 20 patients analgesia in group 2 was performed with patient-controlled analgesia (PCA) with Promedol (trimeperidine) as monotherapy. The intensity of pain was assessed a 100 mm visual-analog scale (VAS) and 5-channel verbal scale (VS) for assessment the severity of the pain syndrome during the patient's moving activity.
RESULTS
A decrease in the severity of the pain syndrome according to VAS from 68.31 to 21.96 mm (<0.001) was achieved by the first hour after the start of the infusion of Neodolpasse persisted for 24 hours of 65% patients. 4 patients (35%) needed the administration of the 2nd dose after 12 hours. The infusion of trimeperidine was started 2 hours after extubation, a significant decrease in pain intensity was noted only at 6th hour, and further differences in the severity of pain in the comparative groups did not significantly differ. In group 2, the observed adverse effects were associated with the use of trimeperidine and depended on its dose. No adverse effects of Neodolpasse were noted. In the Neodolpasse group no adverse effects of the treatment was noted. The total 24 hour consumption of trimeperidine at PCA averaged 72.3 mg, and in the Neodolpasse group - 6.96 mg (=0.00042).
CONCLUSION
There were demonstrated safety, high analgesic efficacy and significant opioid-sparing effect of a fixed combination of Orphenadrine and Diclofenac in the early postoperative period of cardiac surgery patients within the framework of the inclusion and exclusion criteria accepted in the study.
Topics: Analgesia, Patient-Controlled; Cardiac Surgical Procedures; Diclofenac; Humans; Orphenadrine; Pain, Postoperative; Retrospective Studies
PubMed: 35271238
DOI: 10.17116/jnevro202212202161 -
Wiener Klinische Wochenschrift Feb 2023Postoperative intravenous diclofenac reduces patient opioid demand and is commonly used in surgical units. Orphenadrine is mainly used in combination with diclofenac for... (Randomized Controlled Trial)
Randomized Controlled Trial
Intravenous diclofenac and orphenadrine for the treatment of postoperative pain after remifentanil-based anesthesia : A double-blinded, randomized, placebo-controlled study.
BACKGROUND
Postoperative intravenous diclofenac reduces patient opioid demand and is commonly used in surgical units. Orphenadrine is mainly used in combination with diclofenac for musculoskeletal injuries and postoperative pain control. The objective of this study was to compare the analgesic efficacy of diclofenac-orphenadrine, diclofenac alone and saline.
METHODS
We performed a double-blind, randomized, placebo-controlled, parallel-group, single-center clinical study investigating the opioid-sparing effect of a combination of diclofenac and orphenadrine versus diclofenac alone versus isotonic saline solution. Initially 72 patients were included and received total intravenous anesthesia during cruciate ligament surgery. All patients were postoperatively treated with a patient-controlled analgesia (PCA) device containing hydromorphone. Pharmacological safety was assessed by laboratory parameters, vital signs, and delirium detection scores.
RESULTS
There was no significant difference between the groups in cumulative dose of PCA analgesics required after 24 h postsurgery, with 5.90 mg (SD ± 2.90 mg) in the placebo group, 5.73 mg (SD ± 4.75 mg) in the diclofenac group, and 4.13 mg (SD ± 2.57 mg) in the diclofenac-orphenadrine group. Furthermore, there was no significant difference between the groups in cumulative dose of PCA analgesics required 2 h postsurgery (n = 65). Mean dose of hydromorphone required after 2 h was 1.54 mg (SD ± 0.57 mg) in the placebo group, 1.56 mg (SD ± 1.19 mg) in the diclofenac-only group, and 1.37 mg (SD ± 0.78 mg) in the diclofenac-orphenadrine group. However, when comparing the diclofenac-orphenadrine group and the diclofenac group combined to placebo there was a significant reduction in PCA usage in the first 24 h postsurgery. In total, there were 25 adverse events reported, none of which were rated as severe.
CONCLUSION
Orphenadrine-diclofenac failed to significantly reduce postoperative opioid requirements. However, in an exploratory post hoc analysis the diclofenac-orphenadrine and the diclofenac group combined versus placebo showed a tendency to reduce opioid demand in postoperative pain control. Further research is required to determine the value of orphenadrine as an adjuvant in a multimodal approach for postoperative pain management.
Topics: Humans; Diclofenac; Orphenadrine; Remifentanil; Analgesics, Opioid; Hydromorphone; Pain, Postoperative; Analgesics; Anesthesia; Double-Blind Method; Anti-Inflammatory Agents, Non-Steroidal
PubMed: 36576555
DOI: 10.1007/s00508-022-02131-x -
Khirurgiia 2023To evaluate the efficacy and safety of using a fixed combination of diclofenac and orphenadrine for early postoperative pain relief in orthopedic patients following hip...
OBJECTIVE
To evaluate the efficacy and safety of using a fixed combination of diclofenac and orphenadrine for early postoperative pain relief in orthopedic patients following hip prosthetics.
MATERIAL AND METHODS
A prospective comparative study enrolled 65 patients with primary total hip replacement in the setting of spinal bupivacaine anesthesia. Patients were divided into 2 groups - study (39 patients) and control (26 people). The study group underwent Neodolpasse infusion (orphenadrine 30 mg + diclofenac 75 mg) after the end of surgery and morphine infusion in a patient-controlled analgesia (PKA) regimen. The control group underwent morphine monotherapy in the PKA regimen. The intensity of pain syndrome was compared on a visual-analog scale (VAS) from 0 to 100, the total amount of morphine administered, the number of bolus requests, the change in kidney function and the side effect were assessed.
RESULTS
In the control group, the duration of the intervention was shorter and amounted to 70 [59; 82] minutes, in the study group - 83 [65; 94] minutes (=0.05). No significant difference was found in the number of bolus requests (32 [22; 38] and 23 [15; 36], =0.085 and pain intensity 2 and 12 hours after the start of therapy (5 [4; 6] and 3 [2; 4] and 5 [4; 6] and 2 [2; 3] points) in the control group and in the study group. When assessing the intensity of pain syndrome 24 hours after the start of therapy, differences were found in the groups - in the control group 30 [2; 3] mm, in the study group 20 [2; 3] mm (=0.05). There was no nephrotoxic effect on Neodolpasse. Complications of analgesic therapy in the form of nausea, vomiting, pruritus were recorded in both groups in equal amounts, which is explained by the administration of morphine in both groups.
CONCLUSION
1. The use of a fixed combination of orphenadrine 30 mg + diclofenac 75 mg as part of postoperative pain relief after operations of primary hip prosthetics improves the quality of postoperative pain relief according to the subjective assessment of patients. 2. The use of a fixed combination of orphenadrine 30 mg + diclofenac 75 mg did not lead to the development of side effects and complications.
Topics: Humans; Diclofenac; Orphenadrine; Anti-Inflammatory Agents, Non-Steroidal; Prospective Studies; Pain, Postoperative; Morphine
PubMed: 37850894
DOI: 10.17116/hirurgia202304149 -
The Journal of the American Academy of... Sep 2023Posterior lumbar fusion surgery has become more common amid an aging population, with degenerative disease as its most common indication. Historically, postoperative... (Randomized Controlled Trial)
Randomized Controlled Trial
INTRODUCTION
Posterior lumbar fusion surgery has become more common amid an aging population, with degenerative disease as its most common indication. Historically, postoperative pain control for spine surgery has relied on opioids. However, opioid use is associated with adverse effects such as dependence, respiratory depression, and altered cognition. Our study aimed to determine whether an opioid-sparing multimodal analgesia regimen (ketorolac, orphenadrine, and gabapentin) could be a viable alternative to diminish opioid use compared with a standard opioid-based regimen in Hispanic patients undergoing posterior lumbar spinal fusion.
METHODS
This was a randomized controlled trial of Hispanic patients scheduled to undergo elective posterior spinal fusion. Inclusion criteria included age 30 to 85 years, Hispanic ethnicity, lumbar stenosis between L1 and S1, elective posterior spinal fusion with instrumentation, American Society of Anesthesiologists Score <2, and consent to participate in the study. Patients were randomized into two groups, an experimental multimodal analgesia and control (opioid-based) treatment groups, and outcomes such as morphine milligram equivalents used, visual analog scale score, and length of hospital stay were compared between the groups.
RESULTS
The MMA experimental group used significantly lower amounts of opioid (measured with morphine milligram equivalent) than the opioid-based group during the 12-hour and 24-hour postoperative periods ( P -value = 0.023 and P -value = 0.033, respectively). No statistically significant difference was observed in opioid use in the 48-hour postoperative period between both groups ( P -value = 0.066). The MMA group had significantly lower VAS scores reported at the 12-hour, 24-hour, and 48-hour postoperative periods compared with the opioid-based group ( P -values = 0.016, 0.020, and 0.020, respectively). No difference was observed in the length of hospital stay between groups ( P -value = 0.169).
DISCUSSION
Implementing an MMA protocol in Hispanic patients undergoing posterior lumbar fusion resulted in decreased overall opioid use and decreased pain intensity compared with the opioid-based group. MMA is an effective alternative for pain control in patients who want to avoid opioid use.
CLINICAL TRIAL REGISTRATION
Identifier: NCT05413902.
Topics: Adult; Aged; Aged, 80 and over; Humans; Middle Aged; Analgesia; Analgesics, Opioid; Hispanic or Latino; Morphine Derivatives; Pain, Postoperative; Spinal Fusion
PubMed: 37192425
DOI: 10.5435/JAAOS-D-22-00878 -
Environmental Science and Pollution... Mar 2024The uptake, translocation, and metabolization of four widely used drugs, amitriptyline, orphenadrine, lidocaine, and tramadol, were investigated in a laboratory study....
The uptake, translocation, and metabolization of four widely used drugs, amitriptyline, orphenadrine, lidocaine, and tramadol, were investigated in a laboratory study. Cress (Lepidium sativum L.) and pea (Pisum sativum L.) were employed as model plants. These plants were grown in tap water containing the selected pharmaceuticals at concentrations ranging from 0.010 to 10 mg L, whereby the latter concentration was employed for the (tentative) identification of drug-related metabolites formed within the plant. Thereby, mainly phase I metabolites were detected. Time-resolved uptake studies, with sampling after 1, 2, 4, 8, and 16 days, revealed that all four pharmaceuticals were taken up by the roots and further relocated to plant stem and leaves. Also in these studies, the corresponding phase I metabolites could be detected, and their translocation from root to stem (pea only) and finally leaves could be investigated.
Topics: Amitriptyline; Pisum sativum; Brassicaceae; Orphenadrine; Tramadol; Lidocaine; Plants; Vegetables; Pharmaceutical Preparations; Plant Roots
PubMed: 38363510
DOI: 10.1007/s11356-024-32379-x -
Journal of Pain Research 2024Skeletal muscle relaxants (SMRs) are widely used in treating musculoskeletal conditions. All SMRs, with the exception of baclofen and tizanidine, are on the list of 2023... (Review)
Review
BACKGROUND
Skeletal muscle relaxants (SMRs) are widely used in treating musculoskeletal conditions. All SMRs, with the exception of baclofen and tizanidine, are on the list of 2023 American Geriatrics Society Beers Criteria for potentially inappropriate medication use in older adults. In our geriatric practice, off-label use of tizanidine as preemptive analgesia drove us to find recent advances in its pharmacology and therapeutics. An update review of tizanidine was thus presented, aiming to bring the latest knowledge to clinicians and promote further research and practical exploration.
METHODS
Relevant literature up to December 2023 was identified through searches of PubMed, Web of Science, and Embase.
RESULTS
Tizanidine, a centrally acting alpha-2 adrenoceptor agonist with both antispastic and antispasmodic activity, shows efficacy in the common indications for all SMRs. From the perspective of drug safety, tizanidine has lower incidences of adverse events (injury, delirium, encephalopathy, falls, and opioid overdose) compared to baclofen, no association with risk of Alzheimer's disease as with orphenadrine, no risk of serotonin syndrome like metaxalone when comedicated with serotonergic drugs, no significant pharmacokinetic changes in CYP2C19 poor metabolizers unlike diazepam and carisoprodol, and no physically addictive or abuse properties like carisoprodol and diazepam. From the perspective of new and potential therapeutic uses, tizanidine has additional benefits (eg, gastroprotection that can improve patient tolerance to nonsteroidal anti-inflammatory agents, anti-neuropathic pain, a key component of multimodal analgesia strategy to reduce early postoperative pain, and anti-tumor effects). New delivery systems of tizanidine are developing to improve the pharmacokinetics of oral products, including buccal patches, transdermal delivery systems, nasal spray, and in situ rectal gel.
CONCLUSION
Tizanidine is an SMR with unique features and may be an optimal initial choice for older adults. There would be more scientific studies, wider therapeutic applications, and new drug formulations in the future.
PubMed: 38529017
DOI: 10.2147/JPR.S461032 -
Environmental Science and Pollution... Dec 2022The pollution of the surface waters by pharmaceuticals and personal care products (PPCPs) has attracted worldwide attention, but data regarding their occurrence and...
The pollution of the surface waters by pharmaceuticals and personal care products (PPCPs) has attracted worldwide attention, but data regarding their occurrence and potential risks for the aquatic biota on tropical coastal rivers of South America are still scarce. In this context, the occurrence and the preliminary ecological risk assessment of eleven pharmaceuticals of various therapeutic classes (including cocaine and its primary metabolite, benzoylecgonine) were investigated, for the first time, in five rivers of São Paulo, southeast Brazil, covering a coastline of about 140 km, namely Perequê River, Itinga River, Mongaguá River, Itanhaém River and Guaraú River. Although these five rivers are born in well-preserved areas of the Atlantic rainforest biome, on its way to sea and when they cross the urban perimeter, they receive untreated sewage discharges containing a complex mixture of contaminants. In addition, a "persistence, bioaccumulation and toxicity" (PBT) approach allowed to pre-select the priority PPCPs to be monitored in this coastline. Identification of several PPCPs in the samples was done using liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS). Ten PPCPs were successfully quantified in all five rivers, namely caffeine (9.00-560.00 ng/L), acetaminophen (
orphenadrine ( orphenadrine were also classified as priority compounds, followed by furosemide, acetaminophen, cocaine and losartan (all in second position) and caffeine, atenolol, diclofenac and benzoylecgonine (all in third position). This study provides valuable information to reinforce the importance of continuous monitoring of the coastal rivers of South America (containing PPCPs and illicit drugs) whose diffuse loads flow continuously into the marine ecosystems. Furthermore, ecotoxicological studies (especially with tropical marine organisms) to assess the long-term toxicity of these bioactive compounds are urgent. Topics: Environmental Monitoring; Water Pollutants, Chemical; Chromatography, Liquid; Caffeine; Brazil; Diclofenac; Ecosystem; Atenolol; Orphenadrine; Acetaminophen; Losartan; Furosemide; Tandem Mass Spectrometry; Rivers; Illicit Drugs; Cocaine; Risk Assessment; Carbamazepine; Pharmaceutical Preparations
PubMed: 35857165
DOI: 10.1007/s11356-022-21945-w -
European Journal of Gastroenterology &... Aug 2020Many patients of liver cirrhosis are complaining of muscle cramps, which are annoying to them. There is no effective treatment for muscle cramps in cirrhotic patients... (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE
Many patients of liver cirrhosis are complaining of muscle cramps, which are annoying to them. There is no effective treatment for muscle cramps in cirrhotic patients till now. This study purposed to evaluate efficacy and safety of orphenadrine in the treatment of muscle cramps in cirrhotic patients.
METHODS
One hundred and twenty four patients who had muscle cramps three or more times weekly were included. They were divided into two arms: 62 patients administrated orphenadrine and 62 administrated placebo. They were followed up till 2 weeks after the end of therapy. Muscle cramps were evaluated using questionnaire as regards severity, duration, and frequency. Also, side effects of orphenadrine were recorded.
RESULTS
Frequency, duration of muscle cramps, and pain score improved significantly after 1 month of orphenadrine therapy in comparison to placebo. Few side effects were recorded in the form of dry mouth, drowsiness, and nausea.
CONCLUSION
Orphenadrine is considered as promising safe drug for treatment of muscle cramps associated with liver cirrhosis.
Topics: Humans; Liver Cirrhosis; Muscle Cramp; Orphenadrine; Pain; Treatment Outcome
PubMed: 31834056
DOI: 10.1097/MEG.0000000000001622