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Aim To provide scientific evidence for clinical drug combination by exploring the analgesic effect of aspirin combined with Kv7 channel openers, retigabine and flupirtine. Methods The mice were randomly divided into control group, aspirin group, flupirtine group, retigabine group, aspirin + flupirtine group and aspirin + retigabine group. To assess the antinociceptive effects of each group, the acetic acid-induced abdominal constriction test and the hot-plate test were used. Results In the acetic acid-induced abdominal constriction test, compared to aspirin group, the amount of abdominal constriction in aspirin + flupirtine group was significantly reduced (P <0.01). The latent period of abdominal constriction in aspirin + retigabine group was significantly prolonged ( P < 0. 01) and the number of abdominal constriction was significantly reduced (P < 0. 01). In the hot-plate test, compared to aspirin group, the increment percentage of latent period in aspirin + flupirtine group and aspirin + retigabine group showed an increased trend. Among them, the increment percentage of latent period 30 and 60 minutes after injections in aspirin + retigabine group had a significant difference from that in aspirin group (P <0. 05). Conclusion Kv7 channel openers, retigabine and flupirtine, can enhance the analgesic effect of aspirin.
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Background: Osteoarthritis (OA) is a chronic, degenerative joint disorder responsible for considerable morbidity, particularly in old age. Flupirtine, a new centrally acting analgesic, is devoid of the adverse effects of NSAIDs and opioid analgesics. In this study author compared the effectiveness and safety of flupirtine with tramadol in knee OA.Methods: An open label, randomized, controlled trial was done with patients of primary knee OA of both sexes, age >50 years. Patients were recruited from Rheumatology OPD of SSKM Hospital. A minimum WOMAC score of 35 was essential for recruitment. Patients with serious comorbidities were excluded. They were treated orally with either flupirtine (100mg thrice daily) or tramadol (50mg thrice daily) for 12 weeks.Results: Ninety patients were recruited and data of 42 on flupirtine and 41 on tramadol were analysed. There was significant improvement in pain, stiffness and physical function compared to baseline in both the groups. However, there was no significant difference between groups at 4, 8 and 12 weeks. Responder rate (50% reduction in pain score from baseline) was 66.67% with flupirtine and 48.78% with tramadol (p = 0.122). Flupirtine caused 4 adverse events compared to 16 with tramadol. However, both the drugs were well-tolerated.Conclusions: The effectiveness of flupirtine in knee OA is comparable to tramadol, while causing minimal adverse effects. Long-term benefits need to be explored.
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Background: Postoperative pain after laparoscopic surgery limits the function and mobility of patients in postoperative period. Aim: The aim of present study is to study Flupirtine regarding its efficacy as preemptive analgesic in elective laparoscopic surgeries. Methods: In this randomized prospective study 100 patients were divided into two groups. Group-F received two capsules of Oral Flupirtine 100 mg each and group- P received two multivitamin capsules(placebo) with sip of water 2 hour before the expected time of induction of anaesthesia. Time for requirement of first dose of rescue analgesic post operatively, VAS score and dose of rescue analgesic used in first 24 hours post operatively were assessed. Results: Group F had lower visual analogue score(VAS) score in comparison to P group. Time for requirement of first dose of rescue analgesic in P group was less compared to F group. Consumption of rescue analgesic was less in F group in comparison to P group. Conclusion: Flupirtine as preemptive analgesic produced prolonged postoperative analgesia compared to placebo.
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OBJECTIVE:To observe the clinical efficacy and safety of flupirtine maleate combined with amitriptyline in the treatment of thalamic pain after stroke. METHODS:A total of 70 patients with thalamic pain after stroke in our hospital during Jan. 2016-Aug. 2017 were divided into control group(34 cases)and observation group(36 cases)according to random number table. Both groups received secondary prevention therapy of stroke. Based on it,control group was given Amitriptyline hydrochloride tablet 25 mg/time orally,tid. Observation group was additionally given Flupirtine maleate capsule 0.1 g/time orally,tid,on the basis of control group. Treatment course of 2 groups lasted for 4 weeks. VAS,HAMD17 and HAMA14 scores of 2 groups evaluated before treatment,after 1,2,3,4 weeks of treatment Clinical efficacies and the occurrence of ADR were observed in 2 groups. RESULTS:Before treatment,there was no statistical significance in the scores of VAS,HAMD17 or HAMA14 between 2 groups(P>0.05). VAS score and HAMD17 score of observation group after 1,2,3,4 weeks of treatment,those of control group after 2,3 and 4 weeks of treatment were significantly lower than before treatment;the observation group was significantly lower than the control group at different time periods(P<0.05 or P<0.01). HAMA14 score of 2 groups after 2,3,4 weeks of treatment were significantly lower than before treatment;the observation group was significantly lower than the control group at different time periods(P<0.05 or P<0.01). Total efficiency rate(91.67%)of observation group were significantly higher than that(67.65%)of control group(P<0.05). There was no statistical significance in the incidence of ADR between 2 groups (11.76% vs. 11.11%)(P>0.05). CONCLUSIONS:Flupirtine maleate combined with amitriptyline can effectively relieve thalamic pain after stroke,and improve post-stroke,anxiety depression,which are better than control group,and the incidence of ADR is familar to control group.
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Objective To investigate the treatment effect of flupirtine maleate on postherpetic trigeminal neuralgia and the subsequent effects on patient quality of life.Methods Forty patients with postherpetic trigeminal neuralgia were selected at our hospital from December 2015 to December 2016,and they were randomized and divided into a control group and an observation group.Patients in the control group were treated with gabapentin and oxycodone-acetaminophen,and the patients in the observation group were treated with flupirtine maleate on the basis of the control group.Visual analogue scale (VAS) scores,quality of life scores (SF-36 scale),and clinical effective rate were compared between the two groups before and after treatment.Results There was a significant decrease (P ＜ 0.05) in the VAS scores of the two groups after treatment when compared to those before treatment.The VAS score of the patients in the observation group was significantly lower than that of the patients in the control group (P ＜ 0.05).The scores for each dimension in the observation group were significantly higher than those in the control group (P ＜ 0.05).Conclusion When combined with the basic conventional treatment,flupirtine maleate can effectively improve the treatment effects in postherpetic trigeminal neuralgia and effectively relieve pain,thereby improving the quality of life.
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Vasoconstriction is regulated by various ion channels expressed in the plasma membrane of vascular smooth muscle cells. In particular, potassium (K+) channel activity determines resting membrane potential and regulates intracellular calcium (Ca2+) signaling. A number of studies have suggested that dysregulation of K+ channel activity is associated with increased myogenic tone or diminished vasorelaxation. Among the various families of K+ channels, voltage-dependent K+ channels (Kv channels) encoded by the KCNQ gene family (Kv7 channels or M channels) are widely expressed in various blood vessels isolated from mouse, rat, and human. Recent studies have demonstrated that a subunit of the Kv7 channel, Kv7.4, is down-regulated in the aorta and mesenteric and renal arteries of the Spontaneously Hypertensive Rat (SHR) model. Previous studies have also suggested that Kv7 channels play an important role in the regulation of vasorelaxation/vasoconstriction in response to activators/blockers. In addition, previous studies have indicated that hypertension, diabetes mellitus, and cerebrovascular disease result in development of vascular dysfunction associated with Kv7 abnormalities in various animal models. This review focuses on the potential role of the Kv7 channel in vascular dysfunction.
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Animals , Humans , Mice , Rats , Aorta , Blood Vessels , Calcium , Cell Membrane , Diabetes Mellitus , Hypertension , Ion Channels , Membrane Potentials , Models, Animal , Muscle, Smooth, Vascular , Potassium , Rats, Inbred SHR , Renal Artery , Vasoconstriction , VasodilationABSTRACT
Objective:To prepare flupirtine maleate dry suspension and establish its quality control method. Methods: The dry suspension was prepared by a powder direct mixing method. With the sedimentation and redispersibility as the indices,the suspending effect of the hydrophilic polymers HPMC and CMC-Na was investigated. The optimal formula was obtained. The viscosity was deter-mined by a rotary viscometer. An HPLC fluorescence method was used to determine the content of main component. Results:The sedi-mentation ratio of flupirtine maleate dry suspension was 1 in 3h with good redispersibility and liquidity. The cumulative dissolution in 30min was above 80%. Conclusion:The quality of the prepared flupirtine maleate dry suspension is stable and controllable, and the production process is feasible, which provides basis for the research and development of new preparation of flupirtine maleate.
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Background: Low back pain is a common musculoskeletal symptom caused by a variety of disorders that affect the lumbar spine. The most frustrating aspect in the treatment of low back pain is that there is “no magic bullets”. The objective of the study was to compare the efficacy and safety of flupirtine versus piroxicam in patients with back pain. Methods: This was prospective, open labeled, randomized, comparative clinical study conducted by the Departments Orthopedics and Pharmacology, BMC&H, Chitradurga. Study was conducted on 60 patients of either sex, aged above 18 years with low back pain. Assessments were done for Finger-to-Floor Distance (FFD), lumbar pain, Lasegue’s sign, tenderness of vertebral muscles, pain & sensory disturbance in lower limbs and response to therapy for efficacy. Parametric data was analyzed by t-test and proportions were compared using Chi-square test. Results: 74 patients were randomized to 2 groups of 37 each. Group I patients received flupirtine maleate 100 mg twice daily and Group II patients received piroxicam 20 mg twice daily for 14 days. 30 patients in each group completed the study and were analysed. On intergroup comparison, there was no statistical difference (p>0.05) in the efficacy parameters of finger-to-floor distance (FFD), lumbar pain, Lasegue’s sign, tenderness of vertebral muscles, sensory disturbance in lower limbs, VAS scores & global assessment of response to therapy. 13.3% in flupirtine group and 16.6% in piroxicam group reported adverse events. Conclusions: Both flupiritine and piroxicam were equally effective but flupirtine was better tolerated than piroxicam.
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OBJECTIVE:To observe clinical efficacy and safety of flupirtine maleate for pain caused by acute lumbar sprain. METHODS:60 patients with acute lumbar sprain were selected and divided into trial group and control group according to even and odd-numbered admission order. Trial group received flupirtine maleate capsule,1 piece/time,3 times/d;control group was giv-en codeine sustained-release tablet,2 tablets/time,2 times/d. The VAS score,clinical efficacy and ADR were compared between 2 groups. RESULTS:The VAS score of treatment group after treatment was significantly lower than that of control group,with statis-tical significance(t=2.375,P=0.013). The clinical efficacy of trial group was significantly higher than that of control group,with statistical significance (u=9.431,P=0.024). The ADR of trial group was mild,and there was no significant difference between two groups(χ2=0.131,P=0.717). CONCLUSIONS:Flupirtine maleate has a good clinical efficacy and safety in the treatment of pain caused by acute lumbar sprain.
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Objective:To determine the content of methanol, alcohol and isopropanol in flupirtine maleat by headspace gas chro-matography. Methods:The capillary gas chromatography with programming temperature was established with an FID detector and a DB-624(30 m × 0. 53 mm,3. 0 μm) capillary column. The temperature of the injector and the detector was 200℃ and 250℃, respec-tively. The residual organic solvents were determined by an external standard method. Results: Methanol, alcohol and isopropanol showed good linearity within the range of 2. 182~152. 74(r=0. 999 1), 3. 546-248. 22(r=0. 9998)and 4. 082-285. 74 μg·ml-1(r=0. 999 7) with the average recovery of 97. 7%(RSD=1. 5%),99. 0%(RSD=1. 1%)and 98. 8%(RSD=1. 1%)(n=5), respec-tively. Conclusion:The method is simple, sensitive and accurate, and can be used in the residual solvents detection for flupirtine mal-eat.