BACKGROUND Pregabalin is widely used to treat neuropathic pain associated with postherpetic neuralgia.To our knowledge,this is the first report on simultaneously occurring dose-related adverse drug reactions(ADRs)of b...BACKGROUND Pregabalin is widely used to treat neuropathic pain associated with postherpetic neuralgia.To our knowledge,this is the first report on simultaneously occurring dose-related adverse drug reactions(ADRs)of balance disorder,asthenia,peripheral edema,and constipation in an elderly patient after pregabalin.CASE SUMMARY A 76-year-old female with a history of postherpetic neuralgia was prescribed pregabalin(300 mg daily).After taking pregabalin for 7 d,the patient developed balance disorder,weakness,peripheral pitting edema(2+),and constipation.On days 8-14,the pregabalin dose was reduced to 150 mg/d based on creatinine clearance.The patient’s peripheral edema improved significantly with the disappearance of all other adverse symptoms.On day 15,the pregabalin dose was increased to 225 mg/d to relieve pain.Unfortunately,the symptoms mentioned earlier gradually reappeared after 1 wk of pregabalin treatment.However,the complaints were not as severe as when taking 300 mg/d pregabalin.The patient consulted her pharmacist by telephone and was advised to reduce the dose of pregabalin to 150 mg/d and add acetaminophen(0.5 g,q6h)to relieve pain.The patient’s ADRs gradually improved over the following week.CONCLUSION Older patients should be prescribed a lower initial dose of pregabalin.The dose should be titrated to the maximum tolerable dose to avoid dose-limiting ADR.Dose reduction and the addition of acetaminophen may help limit ADR and improve pain control.展开更多
AIM: To compare the effectiveness and tolerability of paroxetine vs pregabalin for the management of multiple sclerosis(MS)-induced neuropathic pain(NPP).METHODS: A randomized, flexible-dose open-label 8-wk study invo...AIM: To compare the effectiveness and tolerability of paroxetine vs pregabalin for the management of multiple sclerosis(MS)-induced neuropathic pain(NPP).METHODS: A randomized, flexible-dose open-label 8-wk study involving 21 relapsing-remitting MS patients with MS-induced NPP was conducted to evaluate the effectiveness and tolerability of pregabalin versus paroxetine for pain management. The trial included a 3-wk dose titration phase followed by a 5-wk stable dose phase. Primary outcome measures included daily patient-reported pain intensity as measured using a 100 mm visual analogue scale(VAS pain) and daily impact of pain on daily activities(VAS impact). Hierarchical regression modeling was conducted on each outcome to determine if within person VAS trajectory for pain and impact differed across study groups, during 56 d follow-up. RESULTS: Attrition rates were significantly greater(P < 0.001) in the paroxetine versus pregabalin study group(70% vs 18.2%, respectively). Average study duration between study groups also significantly differed(P < 0.001). Paroxetine participants completed an average of 27.3 d of treatment vs 49.5 d in the pregabalin group, with the majority of patients withdrawing due to adverse events. Due to the high attrition rates in the paroxetine study arm, the investigators stopped the study prior to achieving complete recruitment. As such, no significant differences between pregabalin and paroxetine study arms were noted for the primary outcome measures(VAS pain, VAS impact). Comparative assessment of baseline patient characteristics also revealed no significant differences between the study arms. CONCLUSION: High attrition rates associated with paroxetine use suggest that it be used with caution for MS-induced NPP. Efficacy outcomes could not be assessed due to attrition.展开更多
Chemotherapy-induced neuropathy is a serious clinical problem for patients receiving cancer treatment.The aim of this study was to investigate the potential efficacy of pregabalin in chemotherapy-induced neuropathy in...Chemotherapy-induced neuropathy is a serious clinical problem for patients receiving cancer treatment.The aim of this study was to investigate the potential efficacy of pregabalin in chemotherapy-induced neuropathy in rats.A total of 35 male Sprague-Dawley rats were randomly divided into 5 groups:group 1,naive control;group 2,treated with pregabalin(30 mg/kg p.o.,for 8 days);group 3,docetaxel was given by single intravenous infusion at 10 mg/kg;groups 4 and 5,pregabalin at 10 mg/kg and 30 mg/kg respectively was orally administered for 8 days after the docetaxel treatment.On day 8,behavioral test was performed,and substance P and CGRP release in dorsal root ganglion(DRG) and sciatic nerve were analyzed by electron microscope.Our results showed that docetaxel induced mechanical allodynia,mechanical hyperalgesia,heat hypoalgesia,cold allodynia,and sciatic nerve impairment and substance P and CGRP release in DRG.However,oral administration of pregabalin(10 mg/kg and 30 mg/kg) for 8 consecutive days significantly attenuated docetaxel-induced neuropathy by ameliorating heat hypoalgesia,cold allodynia,impairment of sciatic nerve and reducing the release of substance P and CGRP.The findings in the present study reveal that pregabalin may be a potential treatment agent against chemotherapy-induced neuropathy.展开更多
Pregabalin,(S)-3-amino methyl hexanoic acid,is a structural analogue ofγ-amino butyric acid(GABA)which has been widely used to treat partial seizures and neuropathic pain[1].It is soluble in aqueous solution and spar...Pregabalin,(S)-3-amino methyl hexanoic acid,is a structural analogue ofγ-amino butyric acid(GABA)which has been widely used to treat partial seizures and neuropathic pain[1].It is soluble in aqueous solution and sparingly soluble in organic solvents such as ethanol,DMSO and DMF.Polyethylene oxide(PEO)has a strong negative effect on analysis of hydrophilic active ingredient and its relative substances due to extremely high viscosity of PEO in aqueous media.The aim of this study is to develop a fast and precise method for the determination of pregabalin and its relative substances in extended release tablets including PEO using sodium sulfate for the treatment of sample solution.展开更多
Background: Tracheal intubation is a noxious stimulus that tends to provoke a marked sympathetic response which is potentially deleterious in some patients. Various methods have been used to minimize and attenuate the...Background: Tracheal intubation is a noxious stimulus that tends to provoke a marked sympathetic response which is potentially deleterious in some patients. Various methods have been used to minimize and attenuate these potentially harmful responses. Aim of the study: The present study compared the efficacy and safety of two different doses (150 mg and 300 mg) of oral pregabalin premedication on attenuation of the hemodynamic pressor response to airway instrumentation, perioperative hemodynamic stability, preoperative sedation, and postoperative pain reduction. Patients and methods: This prospective, observational study consisted of 60 adult patients scheduled for laparoscopic cholecystectomy. The patients were randomized into three groups of 20 patients each. Group I (P0) received an oral placebo, group II (P150) received 150 mg of oral pregabalin and group III (P300) received 300 mg of oral pregabalin 1 h prior to induction. All patients were assessed for pre-operative sedation, perioperative hemodynamic changes, Post-operative pain and analgesic consumption. Results: Regarding the efficacy of the preoperative administration of oral pregabalin, a dose dependent attenuation in the increased in heart rate, systolic, and diastolic blood pressure, and mean arterial blood pressure resulting from laryngoscopy and intubation was observed (300 mg > 150 mg), along with a subsequent decrease in intraoperative fentanyl supplementation. On anxiolysis, patients were more comfortable and asleep in the pregabalin groups as compared with the control group, in which more patients were awake and agitated. Post-operative pain and analgesic consumption were effectively reduced by (150 mg and 300 mg) pregabalin in a dose-dependent manner. Postoperative nausea and vomiting were significantly lower with the administration of pregabalin compared with the placebo group (P < 0.008). Additionally, pregabalin increased the incidence of dizziness and visual disturbances in a dose-dependent manner. Conclusion: Oral pregabalin premedication adequately sedated patients and attenuated the hemodynamic pressor response to airway instrumentation in a dose-dependent manner. Premedicated patients were haemodynamically stable perioperatively without recovery time prolongation or side effects, except dizziness with 300 mg of oral pregabalin. Additionally, oral pregabalin reduced postoperative pain and analgesic consumption in a dose-dependent manner.展开更多
Gabapentin, and pregabalin had been used in analgesic field some studies. This double blind randomized clinical trial was conducted to evaluate the pre-emptive use of gabapentin 900 mg and pregabalin 300 mg in reducin...Gabapentin, and pregabalin had been used in analgesic field some studies. This double blind randomized clinical trial was conducted to evaluate the pre-emptive use of gabapentin 900 mg and pregabalin 300 mg in reducing postoperative pain. Methods: A total number of 75 patients undergoing lower gynecological procedures were prospectively randomized, into three groups (group A, B and C), each group including 25 patients with total 75 patients. Pregabalin, gabapentin or placebo, the pain was assessed on a visual analogue scale (VAS) at 0, 6, 12, 18 & 24 hours postoperatively. Duration of effective analgesia was documented, and administration of extra analgesic doses of meperedine required in the first 24 hours. Results: Patients in the gabapentin or pregabalin had significantly lower VAS scores at 6, 12, 18 and 24 hours, than those in the placebo group. As for rescue analgesia with mepredine consumed in the gabapentin, and pregabalin were significantly less than in the placebo. As for the complications, both drugs had increased incidence of nausea, vomiting and dizziness postoperatively, while no significance was found between all groups as regard hypotension, bradycardia and shivering. Conclusion: Preoperative use of pregabalin or gabapentin provides comparable but significant prolonged postoperative analgesia, less nausea and vomiting compared to placebo after gynecological surgeries. However, it was associated with increased incidence of postoperative dizziness.展开更多
Pain is defined as an unpleasant sensory and emotional experience, associated with actual or potential tissue damage. According to its neurobiological mechanism, pain is classified into nociceptive, inflammatory, dysf...Pain is defined as an unpleasant sensory and emotional experience, associated with actual or potential tissue damage. According to its neurobiological mechanism, pain is classified into nociceptive, inflammatory, dysfunctional, and neuropathic. Neuropathic pain (NP) is caused by a lesion or disease of the somatosensory nervous system. Both pregabalin and gabapentin are pharmaceuticals used as validation drugs in experimental models of NP. Pregabalin was shown to produce significant antihyperalgesic and antiallodynic effects. Gabapentin is used as a reference compound for new analgesics and reduces tactile allodynia in rats. The aim of this work is to evaluate pregabalin and gabapentin effects on nociceptive behaviors induced by spinal nerve ligation (SNL). Female Wistar rats of 140 - 160 g were used, divided into five groups: Naive, SHAM, SNL rats treated with saline solution, SNL rats treated with pregabalin 30 mg/kg p.o., SNL rats treated with gabapentin 300 mg/kg p.o. Nociceptive behaviors were determined by the up and down method. In the establishment of SNL-induced allodynic behavior, a reduction in paw withdrawal threshold was observed in the time course, which was present from day 1 and it was maintained for 28 days post-ligation. With the administration of pregabalin and gabapentin, anti-allodynic behavior was observed in the time course and in the areas under the curve (AUC) of the time course of anti-allodynic behavior, significant difference was observed between pregabalin, and gabapentin groups compared to vehicle with a value of p < 0.0001. The results showed pregabalin and gabapentin induce an antinociceptive effect in rats subjected to SNL.展开更多
目的比较普瑞巴林与加巴喷丁治疗带状疱疹后神经痛(PHN)的效果与安全性。方法选择72例PHN患者为研究对象,随机分为普瑞巴林组与加巴喷丁组,每组36例。普瑞巴林组在常规治疗的基础上加用普瑞巴林,加巴喷丁组在常规治疗的基础上加用加巴...目的比较普瑞巴林与加巴喷丁治疗带状疱疹后神经痛(PHN)的效果与安全性。方法选择72例PHN患者为研究对象,随机分为普瑞巴林组与加巴喷丁组,每组36例。普瑞巴林组在常规治疗的基础上加用普瑞巴林,加巴喷丁组在常规治疗的基础上加用加巴喷丁。比较两组基线及治疗后不同时间点视觉模拟评分法(VAS)评分、睡眠障碍指数(SPI)与不良反应发生情况、临床疗效。结果两组组基线、治疗后3 d VAS评分无统计学差异(P>0.05)。两组患者VAS评分均随着时间推移呈下降趋势,普瑞巴林组治疗后7、14、28及56 d VAS评分分别为(4.0±0.8)、(2.8±0.7)、(2.2±0.6)、(1.6±0.5)分,均显著低于加巴喷丁组的(4.6±1.3)、(3.5±1.1)、(2.8±1.2)、(2.1±0.8)分,差异有统计学意义(P<0.05)。两组基线SPI无统计学差异(P>0.05);两组患者SPI均随着时间推移呈下降趋势,普瑞巴林组治疗后28、56 d SPI分别为(23.3±5.6)、(16.2±4.1)分,均低于加巴喷丁组的(29.4±6.0)、(21.6±5.7)分,差异有统计学意义(P<0.05)。普瑞巴林组与加巴喷丁组有效率分别为94.4%与86.1%,组间比较无统计学差异(P>0.05);普瑞巴林组优良率86.1%显著高于加巴喷丁组的63.9%,差异有统计学意义(P<0.05)。两组头晕、头痛、视物模糊、嗜睡、口干、外周水肿发生率比较无统计学差异(P>0.05)。结论普瑞巴林与加巴喷丁治疗PHN效果显著,但普瑞巴林治疗效果更佳,二者安全性相当。展开更多
文摘BACKGROUND Pregabalin is widely used to treat neuropathic pain associated with postherpetic neuralgia.To our knowledge,this is the first report on simultaneously occurring dose-related adverse drug reactions(ADRs)of balance disorder,asthenia,peripheral edema,and constipation in an elderly patient after pregabalin.CASE SUMMARY A 76-year-old female with a history of postherpetic neuralgia was prescribed pregabalin(300 mg daily).After taking pregabalin for 7 d,the patient developed balance disorder,weakness,peripheral pitting edema(2+),and constipation.On days 8-14,the pregabalin dose was reduced to 150 mg/d based on creatinine clearance.The patient’s peripheral edema improved significantly with the disappearance of all other adverse symptoms.On day 15,the pregabalin dose was increased to 225 mg/d to relieve pain.Unfortunately,the symptoms mentioned earlier gradually reappeared after 1 wk of pregabalin treatment.However,the complaints were not as severe as when taking 300 mg/d pregabalin.The patient consulted her pharmacist by telephone and was advised to reduce the dose of pregabalin to 150 mg/d and add acetaminophen(0.5 g,q6h)to relieve pain.The patient’s ADRs gradually improved over the following week.CONCLUSION Older patients should be prescribed a lower initial dose of pregabalin.The dose should be titrated to the maximum tolerable dose to avoid dose-limiting ADR.Dose reduction and the addition of acetaminophen may help limit ADR and improve pain control.
文摘AIM: To compare the effectiveness and tolerability of paroxetine vs pregabalin for the management of multiple sclerosis(MS)-induced neuropathic pain(NPP).METHODS: A randomized, flexible-dose open-label 8-wk study involving 21 relapsing-remitting MS patients with MS-induced NPP was conducted to evaluate the effectiveness and tolerability of pregabalin versus paroxetine for pain management. The trial included a 3-wk dose titration phase followed by a 5-wk stable dose phase. Primary outcome measures included daily patient-reported pain intensity as measured using a 100 mm visual analogue scale(VAS pain) and daily impact of pain on daily activities(VAS impact). Hierarchical regression modeling was conducted on each outcome to determine if within person VAS trajectory for pain and impact differed across study groups, during 56 d follow-up. RESULTS: Attrition rates were significantly greater(P < 0.001) in the paroxetine versus pregabalin study group(70% vs 18.2%, respectively). Average study duration between study groups also significantly differed(P < 0.001). Paroxetine participants completed an average of 27.3 d of treatment vs 49.5 d in the pregabalin group, with the majority of patients withdrawing due to adverse events. Due to the high attrition rates in the paroxetine study arm, the investigators stopped the study prior to achieving complete recruitment. As such, no significant differences between pregabalin and paroxetine study arms were noted for the primary outcome measures(VAS pain, VAS impact). Comparative assessment of baseline patient characteristics also revealed no significant differences between the study arms. CONCLUSION: High attrition rates associated with paroxetine use suggest that it be used with caution for MS-induced NPP. Efficacy outcomes could not be assessed due to attrition.
基金supported by the National Natural Science Foundation of China (Grant No. 81172187)
文摘Chemotherapy-induced neuropathy is a serious clinical problem for patients receiving cancer treatment.The aim of this study was to investigate the potential efficacy of pregabalin in chemotherapy-induced neuropathy in rats.A total of 35 male Sprague-Dawley rats were randomly divided into 5 groups:group 1,naive control;group 2,treated with pregabalin(30 mg/kg p.o.,for 8 days);group 3,docetaxel was given by single intravenous infusion at 10 mg/kg;groups 4 and 5,pregabalin at 10 mg/kg and 30 mg/kg respectively was orally administered for 8 days after the docetaxel treatment.On day 8,behavioral test was performed,and substance P and CGRP release in dorsal root ganglion(DRG) and sciatic nerve were analyzed by electron microscope.Our results showed that docetaxel induced mechanical allodynia,mechanical hyperalgesia,heat hypoalgesia,cold allodynia,and sciatic nerve impairment and substance P and CGRP release in DRG.However,oral administration of pregabalin(10 mg/kg and 30 mg/kg) for 8 consecutive days significantly attenuated docetaxel-induced neuropathy by ameliorating heat hypoalgesia,cold allodynia,impairment of sciatic nerve and reducing the release of substance P and CGRP.The findings in the present study reveal that pregabalin may be a potential treatment agent against chemotherapy-induced neuropathy.
文摘Pregabalin,(S)-3-amino methyl hexanoic acid,is a structural analogue ofγ-amino butyric acid(GABA)which has been widely used to treat partial seizures and neuropathic pain[1].It is soluble in aqueous solution and sparingly soluble in organic solvents such as ethanol,DMSO and DMF.Polyethylene oxide(PEO)has a strong negative effect on analysis of hydrophilic active ingredient and its relative substances due to extremely high viscosity of PEO in aqueous media.The aim of this study is to develop a fast and precise method for the determination of pregabalin and its relative substances in extended release tablets including PEO using sodium sulfate for the treatment of sample solution.
文摘Background: Tracheal intubation is a noxious stimulus that tends to provoke a marked sympathetic response which is potentially deleterious in some patients. Various methods have been used to minimize and attenuate these potentially harmful responses. Aim of the study: The present study compared the efficacy and safety of two different doses (150 mg and 300 mg) of oral pregabalin premedication on attenuation of the hemodynamic pressor response to airway instrumentation, perioperative hemodynamic stability, preoperative sedation, and postoperative pain reduction. Patients and methods: This prospective, observational study consisted of 60 adult patients scheduled for laparoscopic cholecystectomy. The patients were randomized into three groups of 20 patients each. Group I (P0) received an oral placebo, group II (P150) received 150 mg of oral pregabalin and group III (P300) received 300 mg of oral pregabalin 1 h prior to induction. All patients were assessed for pre-operative sedation, perioperative hemodynamic changes, Post-operative pain and analgesic consumption. Results: Regarding the efficacy of the preoperative administration of oral pregabalin, a dose dependent attenuation in the increased in heart rate, systolic, and diastolic blood pressure, and mean arterial blood pressure resulting from laryngoscopy and intubation was observed (300 mg > 150 mg), along with a subsequent decrease in intraoperative fentanyl supplementation. On anxiolysis, patients were more comfortable and asleep in the pregabalin groups as compared with the control group, in which more patients were awake and agitated. Post-operative pain and analgesic consumption were effectively reduced by (150 mg and 300 mg) pregabalin in a dose-dependent manner. Postoperative nausea and vomiting were significantly lower with the administration of pregabalin compared with the placebo group (P < 0.008). Additionally, pregabalin increased the incidence of dizziness and visual disturbances in a dose-dependent manner. Conclusion: Oral pregabalin premedication adequately sedated patients and attenuated the hemodynamic pressor response to airway instrumentation in a dose-dependent manner. Premedicated patients were haemodynamically stable perioperatively without recovery time prolongation or side effects, except dizziness with 300 mg of oral pregabalin. Additionally, oral pregabalin reduced postoperative pain and analgesic consumption in a dose-dependent manner.
文摘Gabapentin, and pregabalin had been used in analgesic field some studies. This double blind randomized clinical trial was conducted to evaluate the pre-emptive use of gabapentin 900 mg and pregabalin 300 mg in reducing postoperative pain. Methods: A total number of 75 patients undergoing lower gynecological procedures were prospectively randomized, into three groups (group A, B and C), each group including 25 patients with total 75 patients. Pregabalin, gabapentin or placebo, the pain was assessed on a visual analogue scale (VAS) at 0, 6, 12, 18 & 24 hours postoperatively. Duration of effective analgesia was documented, and administration of extra analgesic doses of meperedine required in the first 24 hours. Results: Patients in the gabapentin or pregabalin had significantly lower VAS scores at 6, 12, 18 and 24 hours, than those in the placebo group. As for rescue analgesia with mepredine consumed in the gabapentin, and pregabalin were significantly less than in the placebo. As for the complications, both drugs had increased incidence of nausea, vomiting and dizziness postoperatively, while no significance was found between all groups as regard hypotension, bradycardia and shivering. Conclusion: Preoperative use of pregabalin or gabapentin provides comparable but significant prolonged postoperative analgesia, less nausea and vomiting compared to placebo after gynecological surgeries. However, it was associated with increased incidence of postoperative dizziness.
文摘Pain is defined as an unpleasant sensory and emotional experience, associated with actual or potential tissue damage. According to its neurobiological mechanism, pain is classified into nociceptive, inflammatory, dysfunctional, and neuropathic. Neuropathic pain (NP) is caused by a lesion or disease of the somatosensory nervous system. Both pregabalin and gabapentin are pharmaceuticals used as validation drugs in experimental models of NP. Pregabalin was shown to produce significant antihyperalgesic and antiallodynic effects. Gabapentin is used as a reference compound for new analgesics and reduces tactile allodynia in rats. The aim of this work is to evaluate pregabalin and gabapentin effects on nociceptive behaviors induced by spinal nerve ligation (SNL). Female Wistar rats of 140 - 160 g were used, divided into five groups: Naive, SHAM, SNL rats treated with saline solution, SNL rats treated with pregabalin 30 mg/kg p.o., SNL rats treated with gabapentin 300 mg/kg p.o. Nociceptive behaviors were determined by the up and down method. In the establishment of SNL-induced allodynic behavior, a reduction in paw withdrawal threshold was observed in the time course, which was present from day 1 and it was maintained for 28 days post-ligation. With the administration of pregabalin and gabapentin, anti-allodynic behavior was observed in the time course and in the areas under the curve (AUC) of the time course of anti-allodynic behavior, significant difference was observed between pregabalin, and gabapentin groups compared to vehicle with a value of p < 0.0001. The results showed pregabalin and gabapentin induce an antinociceptive effect in rats subjected to SNL.
文摘目的比较普瑞巴林与加巴喷丁治疗带状疱疹后神经痛(PHN)的效果与安全性。方法选择72例PHN患者为研究对象,随机分为普瑞巴林组与加巴喷丁组,每组36例。普瑞巴林组在常规治疗的基础上加用普瑞巴林,加巴喷丁组在常规治疗的基础上加用加巴喷丁。比较两组基线及治疗后不同时间点视觉模拟评分法(VAS)评分、睡眠障碍指数(SPI)与不良反应发生情况、临床疗效。结果两组组基线、治疗后3 d VAS评分无统计学差异(P>0.05)。两组患者VAS评分均随着时间推移呈下降趋势,普瑞巴林组治疗后7、14、28及56 d VAS评分分别为(4.0±0.8)、(2.8±0.7)、(2.2±0.6)、(1.6±0.5)分,均显著低于加巴喷丁组的(4.6±1.3)、(3.5±1.1)、(2.8±1.2)、(2.1±0.8)分,差异有统计学意义(P<0.05)。两组基线SPI无统计学差异(P>0.05);两组患者SPI均随着时间推移呈下降趋势,普瑞巴林组治疗后28、56 d SPI分别为(23.3±5.6)、(16.2±4.1)分,均低于加巴喷丁组的(29.4±6.0)、(21.6±5.7)分,差异有统计学意义(P<0.05)。普瑞巴林组与加巴喷丁组有效率分别为94.4%与86.1%,组间比较无统计学差异(P>0.05);普瑞巴林组优良率86.1%显著高于加巴喷丁组的63.9%,差异有统计学意义(P<0.05)。两组头晕、头痛、视物模糊、嗜睡、口干、外周水肿发生率比较无统计学差异(P>0.05)。结论普瑞巴林与加巴喷丁治疗PHN效果显著,但普瑞巴林治疗效果更佳,二者安全性相当。
