BACKGROUND In this randomized controlled trial(RCT)comparing current acupuncture with carbamazepine for trigeminal neuralgia,meta-and sequential analyses were utilized.AIM To guide clinical decision making regarding t...BACKGROUND In this randomized controlled trial(RCT)comparing current acupuncture with carbamazepine for trigeminal neuralgia,meta-and sequential analyses were utilized.AIM To guide clinical decision making regarding the treatment of trigeminal neuralgia with carbamazepine.METHODS The RCT literature on needle comparison was searched in various Chinese biomedical databases including Chinese Biomedical Literature Database,Wanfang Data,VIP Database,as well as international databases such as Excerpt Medica Database,Cochrane Library,PubMed,and Web of Science,along with related clinical registration platforms such as World Health Organization International Clinical Trial Registry Platform,ChiCTR,and Clinical Trials up to 1 April 2020.Risk of bias was evaluated using the Cochrane Collaborative Risk Bias tool,primary outcome measures(pain reduction)were analyzed using STATA metaanalysis,outcome measures were analyzed using trial sequential analysis 0.9.5.10 Beta sequential analysis,GRADE was used to assess the evidence,and adverse reactions were documented.RESULTS This study analyzed 16 RCTs with a total of 1231 participants.The meta-analysis revealed a statistically significant difference in pain reduction between acupuncture and carbamazepine[standardized mean difference(SMD)=1.47;95%confidence interval(CI):0.99-1.95],although the quality of evidence was deemed to be of extremely low quality.Cumulative meta-analysis based on the year of publication indicated that carbamazepine treatment first demonstrated a statistically significant difference in pain reduction in 2014 and remained relatively stable over time[SMD=1.84;95%CI:0.22-3.47].Additionally,the number of adverse events associated with acupuncture was significantly lower compared to carbamazepine.CONCLUSION Acupuncture for trigeminal neuralgia is better than analgesia and safer than carbamazepine;however,firm conclusions still require a high-quality,multicenter,large-sample RCT to confirm these findings.展开更多
Standard management protocols are lacking and specific antidotes are unavailable for acute carbamazepine(CBZ)poisoning.The objective of this review is to provide currently available information on acute CBZ poisoning,...Standard management protocols are lacking and specific antidotes are unavailable for acute carbamazepine(CBZ)poisoning.The objective of this review is to provide currently available information on acute CBZ poisoning,including its management,by describing and summarizing various therapeutic methods for its treatment according to previously published studies.Several treatment methods for CBZ poisoning will be briefly introduced,their advantages and disadvantages will be analyzed and compared,and suggestions for the clinical treatment of CBZ poisoning will be provided.A literature search was performed in various English and Chinese databases.In addition,the reference lists of identified articles were screened for additional relevant studies,including non-indexed reports.Nonpeer-reviewed sources were also included.In the present review,154 articles met the inclusion criteria including case reports,case series,descriptive cohorts,pharmacokinetic studies,and in vitro studies.Data on 67 patients,including 4 fatalities,were reviewed.Based on the summary of cases reported in the included articles,the cure rate of CBZ poisoning after symptomatic treatment was 82%and the efficiency of hemoperfusion was 58.2%.Based on the literature review,CBZ is moderately dialyzable and the recommendation for CBZ poisoning is supportive management and gastric lavage.In severe cases,extracorporeal treatment is recommended,with hemodialysis as the first choice.展开更多
Epilepsy is considered as a common and diverse set of chronic neurological disorders and its symptoms can be controlled by antiepileptic drugs(AEDs). The presence of p-glycoprotein and multi-drug resistance transporte...Epilepsy is considered as a common and diverse set of chronic neurological disorders and its symptoms can be controlled by antiepileptic drugs(AEDs). The presence of p-glycoprotein and multi-drug resistance transporters in the blood-brain barrier could prevent the entry of AEDs into the brain, causing drug resistant epilepsy. To overcome this problem, we propose using carboxymethyl chitosan nanoparticles as a carrier to deliver carbamazepine(CBZ) intranasally with the purpose to bypass the blood-brain barrier thus to enhance the brain drug concentration and the treatment efficacy. Results so far indicate that the developed CBZNPs have small particle size(218.76 ± 2.41 nm) with high drug loading(around 35%) and high entrapment efficiency(around 80%). The in vitro release profiles of CBZ from the NPs are in accordance with the Korsmeyer-peppas model. The in vivo results show that both encapsulation of CBZ in nanoparticles and the nasal route determined the enhancement of the drug bioavailability and brain targeting characteristics.展开更多
Objective: To investigate the protective effect of purslane with carbamazepine treatment.Methods: Male albino rats were modulated by pilocarpine to be epileptic.Both the normal and epileptic rats were treated with car...Objective: To investigate the protective effect of purslane with carbamazepine treatment.Methods: Male albino rats were modulated by pilocarpine to be epileptic.Both the normal and epileptic rats were treated with carbamazepine, purslane or carbamazepine plus purslane, with separate non-treated control groups for both normal and epileptic rats.Results: The data from the current study showed amelioration in amino acids and electrolytes in the epileptic rats treated with purslane and carbamazepine, with this amelioration occurring without decreasing the fertility hormones(testosterone,dehydroepiandrosterone, luteinizing hormone and follicle stimulating hormone).Purslane treatments also prevented the increase in estradiol.The decreased epileptic hyperexcitability with purslane was evidenced by decreased glial fibrillary acidic protein and lipid peroxidation.Conclusions: Natural products like purslane could be used with the highly repetitive drugs like carbamazepine to reduce or prevent its side-effects.展开更多
Objective:To achieve transbuccal release of carbamazepine by loading in unidirectional release mucoadhesive buccal patches.Methods:Buccal patches of carbamazepine with unidirectional drug release were prepared using h...Objective:To achieve transbuccal release of carbamazepine by loading in unidirectional release mucoadhesive buccal patches.Methods:Buccal patches of carbamazepine with unidirectional drug release were prepared using hydroxypropyl methyl cellulose,polyvinyl alcohol,polyvinyl pyrrolidone and ethyl cellulose by solvent casting method.Water impermeable backing layer(Pidilite?Biaxially-oriented polypropylene film)of patches provided unidirectional drug release.They were evaluated for thickness,mass uniformity,surface pH and folding endurance.Six formulations FA2,FA8,FA10,FBI,FB14 and FB16(folding endurance above 250)were evaluated further for swelling studies,ex vivo mucoadhesive strength,ex vivo mucoadhesion time,in vitro drug release,ex vivo permeation,accelerated stability studies and FTIR and XRD spectral studies.Results:The ex vivo mucoadhesion time of patches ranged between 109 min(FA10)to 126 min(FB14).The ex vivo mucoadhesive force was in the range of 0.278 lo 0.479 kg/m/s.The in vitro drug release studies revealed that formulation FA8 released 84%and FB16 released 99.01%of drug in140 min.Conclusions:The prepared unidirectional buccal patches of carbamazepine provided a maximum drug release within specified mucoadhesion period and it indicates a potential alternative drug delivery system for systemic denvery of carbamazepine.展开更多
Elementary osmotic pump(EOP)is a unique extended release(ER)drug delivery system based on the principle of osmosis.It has the ability to minimize the amount of the drug,accumulation and fluctuation in drug level durin...Elementary osmotic pump(EOP)is a unique extended release(ER)drug delivery system based on the principle of osmosis.It has the ability to minimize the amount of the drug,accumulation and fluctuation in drug level during chronic uses.Carbamazepine(CBZ),a poorly water-soluble antiepileptic drug,has serious side effects on overdoses and chronic uses.The aim of the present study was to design a new EOP tablet of CBZ containing a solubility enhancers and swellable polymer to reduce its side effects and enhance the patient compliance.Firstly,a combination of solubilizing carriers was selected to improve the dissolution of the slightly soluble drug.Then,designing the new EOP tablet and investigating the effect of different variables of core and coat formulations on drug release behavior by single parameter optimization and by Taguchi orthogonal design with analysis of variance(ANOVA),respectively.The results showed that CBZ solubility was successfully enhanced by a minimum amount of combined polyvinyl pyrrolidone(PVP K30)and sodium lauryl sulfate(SLS).The plasticizer amount and molecular weight(MW)together with the osmotic agent amount directly affect the release rate whereas the swellable polymer amount and viscosity together with the semi-permeable membrane(SPM)thickness inversely influence the release rate.In addition,the tendency of following zero order kinetics was mainly affected by the coat components rather than those of the core.Further,orifice size does not have any significant effect on the release behavior within the range of 0.1 mm to 0.8 mm.In this study we report the successful formulation of CBZ-EOP tablets,which were similar to the marketed product Tegretol CR 200 and able to satisfy the USP criterion limits and to deliver about 80%of CBZ at a rate of approximately zero order for up to 12 h.展开更多
BACKGROUND: It has been demonstrated that traditional antiepileptics, such as phenytoin, carbamazepine (CBZ), phenobarbital, etc., can result in the decrease of thyroid hormone of epileptic patients. However, there is...BACKGROUND: It has been demonstrated that traditional antiepileptics, such as phenytoin, carbamazepine (CBZ), phenobarbital, etc., can result in the decrease of thyroid hormone of epileptic patients. However, there is still no sufficient evidence for the studies about the effect of new-type antiepileptics, such as topiramate (TPM), on thyroid hormones. OBJECTIVE: To observe the effects of TPM and CBZ on the level of thyroid hormones in serum of adults with epilepsy. DESIGN: A comparative observation. SETTING: Department of Neurology, Sichuan Provincial People's Hospital. PARTICIPANTS: Totally 100 outpatients or inpatients newly diagnosed to have epilepsy were selected from the Department of Neurology, Sichuan Provincial People's Hospital from July 2003 to August 2005, including 60 males and 40 females, aged 18-70 years. All the patients were accorded with the standard for the classification of epilepsy set by International League Against Epilepsy (ILAE) in 1981; Had been Informed and agreed with the detection; Had no history of thyroid gland disease; Had not taken any drugs could affect the thyroid function. Meanwhile, 40 adult healthy examinees were selected from our hospital as the control group, including 24 males and 16 females, aged 18-65 years. METHODS: ① The 100 epileptic patients were randomly divided into TPM group (n =50) and CBZ group (n =50), and they were treated with TPM (Xian-Janssen Pharmaceutical, Ltd.; Batch number: 03AS032, Norm: 25 mg/tablet) and CBZ (Shanghai Sunve Pharmaceutical Co., Ltd.; Batch number: 030201, Norm: 100 mg/tablet) respectively. The initial dosage of TPM was 25 mg per day, increased by 25 mg every week, the objective dosage of 100-200 mg per day was maintained when the symptoms were satisfactorily controlled. The dosage of CBZ was 6-8 mg/kg per day. All the patients were administrated for 1 year. ② The serum levels of total thyroxine (TT4), free thyroxine (FT4), total triiodothyronine (TT3), free triiodothyronine (FT3) and thyroid stimulating hormone (TSH) in the epileptic patients were detected by means of chemiluminescence before treatment and at 3, 6 and 12 months after treatment respectively. ③Standards for judging curative effects: Controlled by without seizure, the frequency of seizure reduced by ≥ 75% was taken as significant effect, reduced by 50%-74% as effect, and reduced by < 49% as invalid, whereas increased by more than 20% was taken as aggravation. ④ The intergroup and intragroup differences of the measurement data were compared by the analysis of variance and paired t test respectively. MAIN OUTCOME MEASURES: Serum levels of thyroid hormones before treatment and at different time points after treatment of TPM and CBZ. RESULTS: All the 100 epileptic patients and 40 healthy subjects were involved in the analysis of results. ① Changes of serum levels of thyroid hormones: The serum levels of TT3, TT4, FT3, FT4 and TSH were close between the epileptic patients and normal subjects before treatment (P > 0.05). In the CBZ group, the serum levels of FT4 at 3, 6 and 12 months after treatment [(16.87±3.77), (16.34±3.98) , (16.97±3.95) pmol/L] were significantly decreased as compared with those before treatment [(18.00±3.54) pmol/L, t =2.74, 3.50, 2.26, P < 0.05]; The levels of TT3 at 3, 6 and 12 months [(2.09±0.54), (1.99±0.49), (1.84±0.47) nmol/L] were significantly decreased as compared with those before treatment [(2.22±0.63) nmol/L, t =2.73, 2.78, 5.18, P < 0.05]. The levels of TT3 at 6 and 12 months [(109.65±23.98), (107.72±23.90) nmol/L] were significantly decreased as compared with those before treatment [(118.98±28.48) nmol/L, t =3.11, 3.30, P < 0.05]. TT4 level in serum at 3 months and the levels of FT3 and TSH at each time point after CBZ treatment had no obvious changes as compared with those before treatment (P > 0.05). In the TPM group, the levels of thyroid hormones at each time point had no obvious changes as compared with those before treatment (P > 0.05). ② Curative effects: Of the 100 epileptic patients, it was controlled in 12 cases, significantly effective in 30 cases, effective in 39 cases and invalid in 19 cases, the total effective rate was 81% (81/100). CONCLUSION: CBZ treatment can lead to the decreases of thyroid hormones in adult epileptic patients. Epilepsy itself and TPM treatment cannot change the thyroid hormones in adult epileptic patients, which suggests that TPM treatment is safer for the thyroid function of adult epileptic patients.展开更多
The degradation of carbamazepine (CBZ) and ibuprofen (IBP) in aqueous matrices was investigated by TiO2 and ZnO photocatalysis initiated by UV-A and visible-light irradiation. Emphasis was given on the effect of opera...The degradation of carbamazepine (CBZ) and ibuprofen (IBP) in aqueous matrices was investigated by TiO2 and ZnO photocatalysis initiated by UV-A and visible-light irradiation. Emphasis was given on the effect of operating parameters on the degradation effectiveness, such as catalyst type and loading (50 - 500 mg/L), initial drug concentration (10, 40, 80 mg/L) and wavelength of irradiation (200 - 600 nm). In an effort to understand the photocatalytic pathway for CBZ and IBP removal in terms of primary oxidants, the contribution of HO· was evaluated. With this scope, the radical-mediated process was suppressed by addition of an alcohol scavenger, isopropanol, (i-PrOH), described as the best free hydroxyl radical quencher. The photodegradation rate of the pharmaceuticals was monitored by high performance liquid chromatography (HPLC). According to the results, visible-light exposure, at λexc > 390 nm, takes place as a pure photocatalytic degradation reaction for both compounds. IBP was found to have overall high conversion rates, compared to CBZ. IBP oxidized fast under photocatalytic conditions, regardless the adverse effect of the increase of initial drug concentration, or low catalyst load, irradiation upon visible-light, by either titania or zinc oxide. Finally, addition of isopropanol showed a significant inhibition effect on the CBZ degradation, taken as an evidence of a solution-phase mechanism. In the case though of IBP degradation, the hole mechanism may be prevailing, suggested by the negligible effect upon addition of isopropanol indicating a direct electron transfer between holes (h+) and surface-bound IBP molecules. A plausible mechanism of IBP and CBZ photocatalysis was proposed and described.展开更多
In this work,the solubilities of carbamazepine(CBZ)(form III)in ethyl acetate,methyl acetate,ethylene glycol,chloroform and cyclohexylamine were determined by laser monitoring techniques at pressure above sea level,an...In this work,the solubilities of carbamazepine(CBZ)(form III)in ethyl acetate,methyl acetate,ethylene glycol,chloroform and cyclohexylamine were determined by laser monitoring techniques at pressure above sea level,and the solubility data of CBZ(form III)in different pure solvents were fitted by the Modified Apelblat model andλh model.The result shows that the solubility of CBZ(form III)in five solvents increases as temperature rises,and the solubility in chloroform was the largest.The experimental solubility values of CBZ(form III)in ethyl acetate,methyl acetate,chloroform and cyclohexylamine were in better agreement with the simulated fitting values of theλh model.For ethylene glycol,the r value was much larger than the other four solvents,and it can be seen from theλh model that ethylene glycol was closer to the ideal solution system than the other four solvents.展开更多
Purpose:To observe the efficacy of the combined treatment of carbamazepine and botulinum toxin A for blepharospasm and hemifacial spasm. Methods:Fifty-eight patients with either blepharospasm or hemifacial spasm were ...Purpose:To observe the efficacy of the combined treatment of carbamazepine and botulinum toxin A for blepharospasm and hemifacial spasm. Methods:Fifty-eight patients with either blepharospasm or hemifacial spasm were randomly divided into treatment and control groups. In the treatment group, 30 patients were administered with local intramuscular injections of botulinum toxin A and oral carbamazepine 100 mg/time,3 times/day for 60 days. Twenty-eight subjects in the control group under-went local intramuscular injections of botulinum toxin A only. Results:After combined treatment, the complete remission rate was 90%, which was significantly higher than that of the of the control group (67.9% , P<0.05,χ2 =4.733). However, no statistical significance was noted regarding the duration of therapeutic effects between the treatment group (range 14~40 weeks; 19.2 weeks on average) and control group (range 12~36 weeks; 18 weeks on average). Conclusion:The combined therapy of carbamazepine and topical injections of botulinum toxin A had increased efficacy in the treatment of blepharospasm or hemifacial spasm, but had no significant effect in terms of the duration of the therapeutic effect.展开更多
An ultra-sensitive LC method for the simultaneous quantitation of paracetamol, carbamazepine, losartan and ciprofloxacin have been developed and validated following the ICH guidelines at isobestic point and by program...An ultra-sensitive LC method for the simultaneous quantitation of paracetamol, carbamazepine, losartan and ciprofloxacin have been developed and validated following the ICH guidelines at isobestic point and by programming the detector at individual wavelength of each component. The components were eluted by 50:50 v/v acetonitrile-water (pH 3.0) using a Bondapak, C18 (10 μm, 25 × 0.46 cm) column at flow rate of 1.0 mL·min-1 with detection wavelength 240 nm at isobestic point and 245, 230, 206 and 272 nm for paracetamol, carbamazepine, losartan potassium and ciprofloxacin respectively by programming the detector. Linearity was found to be 0.5 - 24, 0.25 - 8.0, 0.4 - 12 and 0.75 - 10 μg·mL-1 (R2 > 0.999) with detection limits 99, 20, 30 and 6.0 ng·mL-1 respectively. Comparison study with time program method showed more sensitivity with calibration range of 0.4 - 12, 0.2 - 6.0, 0.1 - 3.0 and 0.25 - 8.0 μg·mL-1 (R2 > 0.999) and LOD values 29, 11, 2.0 and 5.0 ng·mL-1 respectively. Percent recoveries >98.37% from pharmaceutical formulation and human serum samples and RSD 2% for inter-day and intra-day assay were obtained. The method was found to be robust and can be successfully applied for the determination of studied drugs in, pharmaceutical formulations and human serum without interference of excipients or endogenous components of serum.展开更多
This work presents a simple and sensitive flow injection fluorimetric method for the determination of carbamazepine (CBZ) in pharmaceutical samples. It is based on the fluorescence signal measurement of the product ge...This work presents a simple and sensitive flow injection fluorimetric method for the determination of carbamazepine (CBZ) in pharmaceutical samples. It is based on the fluorescence signal measurement of the product generated by photoinduced (λex = 251 nm;λem = 434 nm) using a flow injection manifold containing an online homemade photoreactor. In order to optimize the experimental setup, the variable conditions were studied using a multivariate optimization method, thus finding the set of optimum parameters according to the evaluated responses (sensitivity and sampling frequency) and minimizing the number of experiments performed. Under optimal experimental conditions, linear relationship with good correlation coefficient (0.9956) was found between the fluorescence intensity and CBZ concentration in the range of 0.13 - 40 μg·mL-1. The limit of detection was 0.04 μg·mL-1. The precision of the method was satisfactory;the values of relative standard deviations were better than 4.36%. The proposed method was validated and successfully applied to the determination of CBZ in pharmaceuticals with good accuracy;being the recovery values from 89.45% - 112.20%.展开更多
The objective of this study was to develop novel transanasl microemulsion containing carbamazepine for treatment of epilepsy.Oleic acid was selected as oil while Tween 80 and propylene glycol were selected as surfacta...The objective of this study was to develop novel transanasl microemulsion containing carbamazepine for treatment of epilepsy.Oleic acid was selected as oil while Tween 80 and propylene glycol were selected as surfactant and cosurfactant respectively based on solubility results.Optimized ratio of Tween 80:propylene glycol was selected after developing pseudoternary phase diagrams for different ratio and microemulsions were prepared.The prepared microemulsions were evaluated for globule size,viscosity,pH,conductivity and%transmittance.Exvivo diffusion study for optimized microemulsion was performed through sheep nasal mucosa wherein diffusion flux and permeability coefficients were determined.Further pharmacodynamic performance was evaluated in rats by electrically induced seizures.It was found that optimized microemulsion was stable and transparent with average globule size of 190 nm and diffusion flux of 75.77 mg cm2 min1 and showed no toxicity during histopathological evaluation on sheep nasal mucosa.Pharmacodynamic evaluation also indicated lesser intensity of seizures in rats treated with optimized formulation in comparison to rats treated with oral carbamazepine microemulsion and nasal carbamazepine solution which suggested carbamazepine transnasal delivery system as an effective alternate therapy for treatment of epilepsy.展开更多
Carbamazepine (CBZ) is an antiepileptic drug which has multiple mechanisms of action including stabilization of the inactivated stage of the voltage-gated sodium channels, potentiating gamma-amino butyric acid (GABA) ...Carbamazepine (CBZ) is an antiepileptic drug which has multiple mechanisms of action including stabilization of the inactivated stage of the voltage-gated sodium channels, potentiating gamma-amino butyric acid (GABA) receptors as a GABA antagonist, as well as the serotonin releasing affect. It is effective in neuropathic pain syndromes such as post-herpetic neuralgia and trigeminal neuralgia, as well as epilepsy. We presented a 29-year-old female patient with the diagnosis of trigeminal neuralgia (TN) who experienced a reactivation of the latent Ebstein-Barr Virus (EBV) infection in terms of anticonvulsant hypersensitivity syndrome after CBZ use, who gave her approval to publish her data. Since the clinical and serological findings of EBV re-infection resolved after the discontinuation of the drug, this clinical and serological manifestation was attributed to CBZ. Since common side-effects of CBZ are drowsiness, dizziness, headaches, skin reactions, cognitive dysfunctions, we reported an activation of EBV infection due to CBZ consumption as a rare side-effect of the drug.展开更多
CBZ (carbamazepine), CBZ-epox (carbamazepine-10,11-epoxide), TPR (topiramate) and ethanol were detected in 37-year-old woman buried in the wall founded eighteen months after death. The woman was in treatment wit...CBZ (carbamazepine), CBZ-epox (carbamazepine-10,11-epoxide), TPR (topiramate) and ethanol were detected in 37-year-old woman buried in the wall founded eighteen months after death. The woman was in treatment with anticonvulsants. The cause of death was strangulation investigated by immunohistochemical with GPA (glycophorin A). Routine analyses for drugs of abuse, therapeutic drugs and volatiles were conducted. Carbamazepine, Topiramate and Alcohol were quantified in abdominal effusion, gastric wall, spleen, douglas fluid, skeletal muscles, endothoracic fluid, kidney, liver, heart and bone marrow. CBZ, CBZ-epox and TPR were recovered in samples deproteinized by acetonitrile spiked with DNSnVal as Internal Standard. Compounds were detected by HPLC-MS/MS. Alcohol was detected in any specimens by HS-GC/FID. CBZ concentrations were ranged from 0.49 in liver to 13.6 ~tg/g in endothoracic fluid; CBZ-Epox 0.46 in skeletal muscle, and 1.13 pg/g in Douglas fluid; TPR 0.11 in gastric wall and 1.23 Ixg/g in endothoracic fluid; alcohol from 0.17 in bone marrow to 0,75 mg/g in Douglas fluid. To our knowledge this is the first report of the presence of carbamazepine, topiramate, and alcohol in post mortem putrefied specimens.展开更多
文摘BACKGROUND In this randomized controlled trial(RCT)comparing current acupuncture with carbamazepine for trigeminal neuralgia,meta-and sequential analyses were utilized.AIM To guide clinical decision making regarding the treatment of trigeminal neuralgia with carbamazepine.METHODS The RCT literature on needle comparison was searched in various Chinese biomedical databases including Chinese Biomedical Literature Database,Wanfang Data,VIP Database,as well as international databases such as Excerpt Medica Database,Cochrane Library,PubMed,and Web of Science,along with related clinical registration platforms such as World Health Organization International Clinical Trial Registry Platform,ChiCTR,and Clinical Trials up to 1 April 2020.Risk of bias was evaluated using the Cochrane Collaborative Risk Bias tool,primary outcome measures(pain reduction)were analyzed using STATA metaanalysis,outcome measures were analyzed using trial sequential analysis 0.9.5.10 Beta sequential analysis,GRADE was used to assess the evidence,and adverse reactions were documented.RESULTS This study analyzed 16 RCTs with a total of 1231 participants.The meta-analysis revealed a statistically significant difference in pain reduction between acupuncture and carbamazepine[standardized mean difference(SMD)=1.47;95%confidence interval(CI):0.99-1.95],although the quality of evidence was deemed to be of extremely low quality.Cumulative meta-analysis based on the year of publication indicated that carbamazepine treatment first demonstrated a statistically significant difference in pain reduction in 2014 and remained relatively stable over time[SMD=1.84;95%CI:0.22-3.47].Additionally,the number of adverse events associated with acupuncture was significantly lower compared to carbamazepine.CONCLUSION Acupuncture for trigeminal neuralgia is better than analgesia and safer than carbamazepine;however,firm conclusions still require a high-quality,multicenter,large-sample RCT to confirm these findings.
基金Science and Public Welfare Research Fund of Liaoning Province,No.2022JH4/10100075and National Nature Science Foundation of China,No.81772056.
文摘Standard management protocols are lacking and specific antidotes are unavailable for acute carbamazepine(CBZ)poisoning.The objective of this review is to provide currently available information on acute CBZ poisoning,including its management,by describing and summarizing various therapeutic methods for its treatment according to previously published studies.Several treatment methods for CBZ poisoning will be briefly introduced,their advantages and disadvantages will be analyzed and compared,and suggestions for the clinical treatment of CBZ poisoning will be provided.A literature search was performed in various English and Chinese databases.In addition,the reference lists of identified articles were screened for additional relevant studies,including non-indexed reports.Nonpeer-reviewed sources were also included.In the present review,154 articles met the inclusion criteria including case reports,case series,descriptive cohorts,pharmacokinetic studies,and in vitro studies.Data on 67 patients,including 4 fatalities,were reviewed.Based on the summary of cases reported in the included articles,the cure rate of CBZ poisoning after symptomatic treatment was 82%and the efficiency of hemoperfusion was 58.2%.Based on the literature review,CBZ is moderately dialyzable and the recommendation for CBZ poisoning is supportive management and gastric lavage.In severe cases,extracorporeal treatment is recommended,with hemodialysis as the first choice.
基金the Academic Research Fund,Faculty of Science,National University of Singapore,R148-000-180-112
文摘Epilepsy is considered as a common and diverse set of chronic neurological disorders and its symptoms can be controlled by antiepileptic drugs(AEDs). The presence of p-glycoprotein and multi-drug resistance transporters in the blood-brain barrier could prevent the entry of AEDs into the brain, causing drug resistant epilepsy. To overcome this problem, we propose using carboxymethyl chitosan nanoparticles as a carrier to deliver carbamazepine(CBZ) intranasally with the purpose to bypass the blood-brain barrier thus to enhance the brain drug concentration and the treatment efficacy. Results so far indicate that the developed CBZNPs have small particle size(218.76 ± 2.41 nm) with high drug loading(around 35%) and high entrapment efficiency(around 80%). The in vitro release profiles of CBZ from the NPs are in accordance with the Korsmeyer-peppas model. The in vivo results show that both encapsulation of CBZ in nanoparticles and the nasal route determined the enhancement of the drug bioavailability and brain targeting characteristics.
文摘Objective: To investigate the protective effect of purslane with carbamazepine treatment.Methods: Male albino rats were modulated by pilocarpine to be epileptic.Both the normal and epileptic rats were treated with carbamazepine, purslane or carbamazepine plus purslane, with separate non-treated control groups for both normal and epileptic rats.Results: The data from the current study showed amelioration in amino acids and electrolytes in the epileptic rats treated with purslane and carbamazepine, with this amelioration occurring without decreasing the fertility hormones(testosterone,dehydroepiandrosterone, luteinizing hormone and follicle stimulating hormone).Purslane treatments also prevented the increase in estradiol.The decreased epileptic hyperexcitability with purslane was evidenced by decreased glial fibrillary acidic protein and lipid peroxidation.Conclusions: Natural products like purslane could be used with the highly repetitive drugs like carbamazepine to reduce or prevent its side-effects.
基金supported by RR college of Pharmacy affiliated to Rajiv Gandhi University of Health Sciences,Bangalore,India(Grant No.RRCP\PCEUTICS\IHR&D\231)
文摘Objective:To achieve transbuccal release of carbamazepine by loading in unidirectional release mucoadhesive buccal patches.Methods:Buccal patches of carbamazepine with unidirectional drug release were prepared using hydroxypropyl methyl cellulose,polyvinyl alcohol,polyvinyl pyrrolidone and ethyl cellulose by solvent casting method.Water impermeable backing layer(Pidilite?Biaxially-oriented polypropylene film)of patches provided unidirectional drug release.They were evaluated for thickness,mass uniformity,surface pH and folding endurance.Six formulations FA2,FA8,FA10,FBI,FB14 and FB16(folding endurance above 250)were evaluated further for swelling studies,ex vivo mucoadhesive strength,ex vivo mucoadhesion time,in vitro drug release,ex vivo permeation,accelerated stability studies and FTIR and XRD spectral studies.Results:The ex vivo mucoadhesion time of patches ranged between 109 min(FA10)to 126 min(FB14).The ex vivo mucoadhesive force was in the range of 0.278 lo 0.479 kg/m/s.The in vitro drug release studies revealed that formulation FA8 released 84%and FB16 released 99.01%of drug in140 min.Conclusions:The prepared unidirectional buccal patches of carbamazepine provided a maximum drug release within specified mucoadhesion period and it indicates a potential alternative drug delivery system for systemic denvery of carbamazepine.
基金This work was financially supported by the major project of the National Science and Technology of China for new drugs development(2009ZX09310-004).
文摘Elementary osmotic pump(EOP)is a unique extended release(ER)drug delivery system based on the principle of osmosis.It has the ability to minimize the amount of the drug,accumulation and fluctuation in drug level during chronic uses.Carbamazepine(CBZ),a poorly water-soluble antiepileptic drug,has serious side effects on overdoses and chronic uses.The aim of the present study was to design a new EOP tablet of CBZ containing a solubility enhancers and swellable polymer to reduce its side effects and enhance the patient compliance.Firstly,a combination of solubilizing carriers was selected to improve the dissolution of the slightly soluble drug.Then,designing the new EOP tablet and investigating the effect of different variables of core and coat formulations on drug release behavior by single parameter optimization and by Taguchi orthogonal design with analysis of variance(ANOVA),respectively.The results showed that CBZ solubility was successfully enhanced by a minimum amount of combined polyvinyl pyrrolidone(PVP K30)and sodium lauryl sulfate(SLS).The plasticizer amount and molecular weight(MW)together with the osmotic agent amount directly affect the release rate whereas the swellable polymer amount and viscosity together with the semi-permeable membrane(SPM)thickness inversely influence the release rate.In addition,the tendency of following zero order kinetics was mainly affected by the coat components rather than those of the core.Further,orifice size does not have any significant effect on the release behavior within the range of 0.1 mm to 0.8 mm.In this study we report the successful formulation of CBZ-EOP tablets,which were similar to the marketed product Tegretol CR 200 and able to satisfy the USP criterion limits and to deliver about 80%of CBZ at a rate of approximately zero order for up to 12 h.
文摘BACKGROUND: It has been demonstrated that traditional antiepileptics, such as phenytoin, carbamazepine (CBZ), phenobarbital, etc., can result in the decrease of thyroid hormone of epileptic patients. However, there is still no sufficient evidence for the studies about the effect of new-type antiepileptics, such as topiramate (TPM), on thyroid hormones. OBJECTIVE: To observe the effects of TPM and CBZ on the level of thyroid hormones in serum of adults with epilepsy. DESIGN: A comparative observation. SETTING: Department of Neurology, Sichuan Provincial People's Hospital. PARTICIPANTS: Totally 100 outpatients or inpatients newly diagnosed to have epilepsy were selected from the Department of Neurology, Sichuan Provincial People's Hospital from July 2003 to August 2005, including 60 males and 40 females, aged 18-70 years. All the patients were accorded with the standard for the classification of epilepsy set by International League Against Epilepsy (ILAE) in 1981; Had been Informed and agreed with the detection; Had no history of thyroid gland disease; Had not taken any drugs could affect the thyroid function. Meanwhile, 40 adult healthy examinees were selected from our hospital as the control group, including 24 males and 16 females, aged 18-65 years. METHODS: ① The 100 epileptic patients were randomly divided into TPM group (n =50) and CBZ group (n =50), and they were treated with TPM (Xian-Janssen Pharmaceutical, Ltd.; Batch number: 03AS032, Norm: 25 mg/tablet) and CBZ (Shanghai Sunve Pharmaceutical Co., Ltd.; Batch number: 030201, Norm: 100 mg/tablet) respectively. The initial dosage of TPM was 25 mg per day, increased by 25 mg every week, the objective dosage of 100-200 mg per day was maintained when the symptoms were satisfactorily controlled. The dosage of CBZ was 6-8 mg/kg per day. All the patients were administrated for 1 year. ② The serum levels of total thyroxine (TT4), free thyroxine (FT4), total triiodothyronine (TT3), free triiodothyronine (FT3) and thyroid stimulating hormone (TSH) in the epileptic patients were detected by means of chemiluminescence before treatment and at 3, 6 and 12 months after treatment respectively. ③Standards for judging curative effects: Controlled by without seizure, the frequency of seizure reduced by ≥ 75% was taken as significant effect, reduced by 50%-74% as effect, and reduced by < 49% as invalid, whereas increased by more than 20% was taken as aggravation. ④ The intergroup and intragroup differences of the measurement data were compared by the analysis of variance and paired t test respectively. MAIN OUTCOME MEASURES: Serum levels of thyroid hormones before treatment and at different time points after treatment of TPM and CBZ. RESULTS: All the 100 epileptic patients and 40 healthy subjects were involved in the analysis of results. ① Changes of serum levels of thyroid hormones: The serum levels of TT3, TT4, FT3, FT4 and TSH were close between the epileptic patients and normal subjects before treatment (P > 0.05). In the CBZ group, the serum levels of FT4 at 3, 6 and 12 months after treatment [(16.87±3.77), (16.34±3.98) , (16.97±3.95) pmol/L] were significantly decreased as compared with those before treatment [(18.00±3.54) pmol/L, t =2.74, 3.50, 2.26, P < 0.05]; The levels of TT3 at 3, 6 and 12 months [(2.09±0.54), (1.99±0.49), (1.84±0.47) nmol/L] were significantly decreased as compared with those before treatment [(2.22±0.63) nmol/L, t =2.73, 2.78, 5.18, P < 0.05]. The levels of TT3 at 6 and 12 months [(109.65±23.98), (107.72±23.90) nmol/L] were significantly decreased as compared with those before treatment [(118.98±28.48) nmol/L, t =3.11, 3.30, P < 0.05]. TT4 level in serum at 3 months and the levels of FT3 and TSH at each time point after CBZ treatment had no obvious changes as compared with those before treatment (P > 0.05). In the TPM group, the levels of thyroid hormones at each time point had no obvious changes as compared with those before treatment (P > 0.05). ② Curative effects: Of the 100 epileptic patients, it was controlled in 12 cases, significantly effective in 30 cases, effective in 39 cases and invalid in 19 cases, the total effective rate was 81% (81/100). CONCLUSION: CBZ treatment can lead to the decreases of thyroid hormones in adult epileptic patients. Epilepsy itself and TPM treatment cannot change the thyroid hormones in adult epileptic patients, which suggests that TPM treatment is safer for the thyroid function of adult epileptic patients.
文摘The degradation of carbamazepine (CBZ) and ibuprofen (IBP) in aqueous matrices was investigated by TiO2 and ZnO photocatalysis initiated by UV-A and visible-light irradiation. Emphasis was given on the effect of operating parameters on the degradation effectiveness, such as catalyst type and loading (50 - 500 mg/L), initial drug concentration (10, 40, 80 mg/L) and wavelength of irradiation (200 - 600 nm). In an effort to understand the photocatalytic pathway for CBZ and IBP removal in terms of primary oxidants, the contribution of HO· was evaluated. With this scope, the radical-mediated process was suppressed by addition of an alcohol scavenger, isopropanol, (i-PrOH), described as the best free hydroxyl radical quencher. The photodegradation rate of the pharmaceuticals was monitored by high performance liquid chromatography (HPLC). According to the results, visible-light exposure, at λexc > 390 nm, takes place as a pure photocatalytic degradation reaction for both compounds. IBP was found to have overall high conversion rates, compared to CBZ. IBP oxidized fast under photocatalytic conditions, regardless the adverse effect of the increase of initial drug concentration, or low catalyst load, irradiation upon visible-light, by either titania or zinc oxide. Finally, addition of isopropanol showed a significant inhibition effect on the CBZ degradation, taken as an evidence of a solution-phase mechanism. In the case though of IBP degradation, the hole mechanism may be prevailing, suggested by the negligible effect upon addition of isopropanol indicating a direct electron transfer between holes (h+) and surface-bound IBP molecules. A plausible mechanism of IBP and CBZ photocatalysis was proposed and described.
基金The authors would like to thank the Science Foundation of Henan University of Technology (2017RCJH09,2017QNJH29)Science Foundation of Henan Province (202102310208,182102210399) for their financial assistance in this project。
文摘In this work,the solubilities of carbamazepine(CBZ)(form III)in ethyl acetate,methyl acetate,ethylene glycol,chloroform and cyclohexylamine were determined by laser monitoring techniques at pressure above sea level,and the solubility data of CBZ(form III)in different pure solvents were fitted by the Modified Apelblat model andλh model.The result shows that the solubility of CBZ(form III)in five solvents increases as temperature rises,and the solubility in chloroform was the largest.The experimental solubility values of CBZ(form III)in ethyl acetate,methyl acetate,chloroform and cyclohexylamine were in better agreement with the simulated fitting values of theλh model.For ethylene glycol,the r value was much larger than the other four solvents,and it can be seen from theλh model that ethylene glycol was closer to the ideal solution system than the other four solvents.
基金The Science and Technology Projects of GuangdongProvince,China (2010B060500006)
文摘Purpose:To observe the efficacy of the combined treatment of carbamazepine and botulinum toxin A for blepharospasm and hemifacial spasm. Methods:Fifty-eight patients with either blepharospasm or hemifacial spasm were randomly divided into treatment and control groups. In the treatment group, 30 patients were administered with local intramuscular injections of botulinum toxin A and oral carbamazepine 100 mg/time,3 times/day for 60 days. Twenty-eight subjects in the control group under-went local intramuscular injections of botulinum toxin A only. Results:After combined treatment, the complete remission rate was 90%, which was significantly higher than that of the of the control group (67.9% , P<0.05,χ2 =4.733). However, no statistical significance was noted regarding the duration of therapeutic effects between the treatment group (range 14~40 weeks; 19.2 weeks on average) and control group (range 12~36 weeks; 18 weeks on average). Conclusion:The combined therapy of carbamazepine and topical injections of botulinum toxin A had increased efficacy in the treatment of blepharospasm or hemifacial spasm, but had no significant effect in terms of the duration of the therapeutic effect.
文摘An ultra-sensitive LC method for the simultaneous quantitation of paracetamol, carbamazepine, losartan and ciprofloxacin have been developed and validated following the ICH guidelines at isobestic point and by programming the detector at individual wavelength of each component. The components were eluted by 50:50 v/v acetonitrile-water (pH 3.0) using a Bondapak, C18 (10 μm, 25 × 0.46 cm) column at flow rate of 1.0 mL·min-1 with detection wavelength 240 nm at isobestic point and 245, 230, 206 and 272 nm for paracetamol, carbamazepine, losartan potassium and ciprofloxacin respectively by programming the detector. Linearity was found to be 0.5 - 24, 0.25 - 8.0, 0.4 - 12 and 0.75 - 10 μg·mL-1 (R2 > 0.999) with detection limits 99, 20, 30 and 6.0 ng·mL-1 respectively. Comparison study with time program method showed more sensitivity with calibration range of 0.4 - 12, 0.2 - 6.0, 0.1 - 3.0 and 0.25 - 8.0 μg·mL-1 (R2 > 0.999) and LOD values 29, 11, 2.0 and 5.0 ng·mL-1 respectively. Percent recoveries >98.37% from pharmaceutical formulation and human serum samples and RSD 2% for inter-day and intra-day assay were obtained. The method was found to be robust and can be successfully applied for the determination of studied drugs in, pharmaceutical formulations and human serum without interference of excipients or endogenous components of serum.
文摘This work presents a simple and sensitive flow injection fluorimetric method for the determination of carbamazepine (CBZ) in pharmaceutical samples. It is based on the fluorescence signal measurement of the product generated by photoinduced (λex = 251 nm;λem = 434 nm) using a flow injection manifold containing an online homemade photoreactor. In order to optimize the experimental setup, the variable conditions were studied using a multivariate optimization method, thus finding the set of optimum parameters according to the evaluated responses (sensitivity and sampling frequency) and minimizing the number of experiments performed. Under optimal experimental conditions, linear relationship with good correlation coefficient (0.9956) was found between the fluorescence intensity and CBZ concentration in the range of 0.13 - 40 μg·mL-1. The limit of detection was 0.04 μg·mL-1. The precision of the method was satisfactory;the values of relative standard deviations were better than 4.36%. The proposed method was validated and successfully applied to the determination of CBZ in pharmaceuticals with good accuracy;being the recovery values from 89.45% - 112.20%.
基金This study was supported by a grant from Gujarat Council of Scientific Technology(GUJCOST),Ahmedabad.
文摘The objective of this study was to develop novel transanasl microemulsion containing carbamazepine for treatment of epilepsy.Oleic acid was selected as oil while Tween 80 and propylene glycol were selected as surfactant and cosurfactant respectively based on solubility results.Optimized ratio of Tween 80:propylene glycol was selected after developing pseudoternary phase diagrams for different ratio and microemulsions were prepared.The prepared microemulsions were evaluated for globule size,viscosity,pH,conductivity and%transmittance.Exvivo diffusion study for optimized microemulsion was performed through sheep nasal mucosa wherein diffusion flux and permeability coefficients were determined.Further pharmacodynamic performance was evaluated in rats by electrically induced seizures.It was found that optimized microemulsion was stable and transparent with average globule size of 190 nm and diffusion flux of 75.77 mg cm2 min1 and showed no toxicity during histopathological evaluation on sheep nasal mucosa.Pharmacodynamic evaluation also indicated lesser intensity of seizures in rats treated with optimized formulation in comparison to rats treated with oral carbamazepine microemulsion and nasal carbamazepine solution which suggested carbamazepine transnasal delivery system as an effective alternate therapy for treatment of epilepsy.
文摘Carbamazepine (CBZ) is an antiepileptic drug which has multiple mechanisms of action including stabilization of the inactivated stage of the voltage-gated sodium channels, potentiating gamma-amino butyric acid (GABA) receptors as a GABA antagonist, as well as the serotonin releasing affect. It is effective in neuropathic pain syndromes such as post-herpetic neuralgia and trigeminal neuralgia, as well as epilepsy. We presented a 29-year-old female patient with the diagnosis of trigeminal neuralgia (TN) who experienced a reactivation of the latent Ebstein-Barr Virus (EBV) infection in terms of anticonvulsant hypersensitivity syndrome after CBZ use, who gave her approval to publish her data. Since the clinical and serological findings of EBV re-infection resolved after the discontinuation of the drug, this clinical and serological manifestation was attributed to CBZ. Since common side-effects of CBZ are drowsiness, dizziness, headaches, skin reactions, cognitive dysfunctions, we reported an activation of EBV infection due to CBZ consumption as a rare side-effect of the drug.
文摘CBZ (carbamazepine), CBZ-epox (carbamazepine-10,11-epoxide), TPR (topiramate) and ethanol were detected in 37-year-old woman buried in the wall founded eighteen months after death. The woman was in treatment with anticonvulsants. The cause of death was strangulation investigated by immunohistochemical with GPA (glycophorin A). Routine analyses for drugs of abuse, therapeutic drugs and volatiles were conducted. Carbamazepine, Topiramate and Alcohol were quantified in abdominal effusion, gastric wall, spleen, douglas fluid, skeletal muscles, endothoracic fluid, kidney, liver, heart and bone marrow. CBZ, CBZ-epox and TPR were recovered in samples deproteinized by acetonitrile spiked with DNSnVal as Internal Standard. Compounds were detected by HPLC-MS/MS. Alcohol was detected in any specimens by HS-GC/FID. CBZ concentrations were ranged from 0.49 in liver to 13.6 ~tg/g in endothoracic fluid; CBZ-Epox 0.46 in skeletal muscle, and 1.13 pg/g in Douglas fluid; TPR 0.11 in gastric wall and 1.23 Ixg/g in endothoracic fluid; alcohol from 0.17 in bone marrow to 0,75 mg/g in Douglas fluid. To our knowledge this is the first report of the presence of carbamazepine, topiramate, and alcohol in post mortem putrefied specimens.