Background:To investigate the toxicity of N-n-butyl haloperidol iodide(F2),a quaternary ammonium salt derivative of haloperidol,in mice for potential therapeutic purposes.Methods:The acute median lethal dose(LD_(50))o...Background:To investigate the toxicity of N-n-butyl haloperidol iodide(F2),a quaternary ammonium salt derivative of haloperidol,in mice for potential therapeutic purposes.Methods:The acute median lethal dose(LD_(50))of F2 was determined using the Bliss method following intravenous administration in mice.Routine surface electrocardiograms(ECGs)and arterial blood pressures(aBPs)were recorded under general anesthesia in untreated and pharmacologically vagotomized mice injected with F2.Sublethal doses of F2 were tested for their effects on aBP,heart rate,and biochemical parameters such as lactate dehydrogenase(LDH),blood urea nitrogen(BUN),and serum lactate levels.Histopathological changes in the heart,lungs,liver,and kidneys were evaluated after F2 administration.Results:The acute LD_(50)of F2 was determined to be 5.11 mg/kg.A 10 mg/kg dose of F2 caused severe hypotension,second-degree atrioventricular block,progressive prolongation of Pmurr intervals,and death due to cardiac asystole.Similar ECG and aBP changes were observed in atropine-pretreated mice,indicating that cholinergic effects do not play a major role in F2-induced toxicity.Sublethal doses of F2(1.2 and 2.4 mg/kg)caused dose-dependent decreases in aBP and increases in heart rate.F2 induced significant,dose-dependent increases in LDH,BUN,and serum lactate levels.Histopathological analysis revealed acute lung lesions at 10 mg/kg,with no significant changes observed in the heart,liver,or kidneys.Conclusion:Acute intravenous injection of F2 exhibits dose-dependent cardiopulmonary toxicity,characterized by severe hypotension,arrhythmias,and biochemical changes.These findings highlight the potential risks of F2 and the need for further evaluation of its safety profile for therapeutic use.展开更多
Objective:To investigate the effect of Rosa moschata(R.moschata)extract on haloperidol-induced Parkinson’s disease(PD)in rats.Methods:Haloperidol(1 mg/kg)was given to rats intraperitoneally for 3 weeks for induction ...Objective:To investigate the effect of Rosa moschata(R.moschata)extract on haloperidol-induced Parkinson’s disease(PD)in rats.Methods:Haloperidol(1 mg/kg)was given to rats intraperitoneally for 3 weeks for induction of PD.R.moschata extract(150,300 and 600 mg/kg)was administered orally for 21 days.The neuroprotective role of R.moschata leaf extract in PD was explored by performing neurobehavioral tests and RT-PCR analysis and measuring neurotransmitters and oxidative stress biomarkers.Results:An improvement in motor functions and muscle strength was observed in PD rats treated with R.moschata extract.The levels of dopamine,serotonin,noradrenaline,superoxide dismutase,catalase,glutathione,and superoxide dismutase were significantly increased(P<0.001),whereas acetylcholinesterase and malondialdehyde levels were markedly decreased by treatment with R.moschata extract(P<0.001).The extract also markedly downregulated the mRNA expressions of IL-1β,α-synuclein,IL-1α,and TNF-αin brain tissue.Moreover,histopathological analysis indicated that neurofibrillary tangles and plaques were noticeably decreased in a dose-dependent manner in PD rats treated with R.moschata extract.Conclusions:R.moschata extract alleviates haloperidol-induced PD in rats by reducing oxidative stress and neurodegeneration.It may be used for management and treatment of PD.However additional studies are required to confirm its efficacy and molecular mechanisms.展开更多
Background Haloperidol is the most frequently prescribed antipsycbotic for delirium symptoms. The risk of QTc prolongation often raises concerns, although the effect of haloperidol on QTc interval has not yet been inv...Background Haloperidol is the most frequently prescribed antipsycbotic for delirium symptoms. The risk of QTc prolongation often raises concerns, although the effect of haloperidol on QTc interval has not yet been investigated in a randomised placebo-controlled fixed-dose study. Methods A subanalysis of a randomised double-blind placebo-controlled study was conducted to evaluate the effect of prophylactic haloperidol 1 mg or placebo 1 mg orally twice-daily （maximum of 14 doses） on QTc interval in patients aged 70 years and over. Bedside, 12-lead ECGs were recorded before, during and after the one-week intervention period. Automatic QTc measurements were ob- tained in addition to manual measurements of QT and RR intervals, blinded for treatment status. Manual measurements were corrected （QTc） using Bazett （QTc-B）, Framingham （QTc-Fa）, Fridericia （QTc-Fi） and Hodges （QTc-H） methods. Mixed model analyses were used to test for differences in longitudinal course of QTc between patients receiving haloperidol and placebo. Results ECG recordings of 72 patients （haloperidol n = 38） were analysed, 45.8% male. Median （range） haloperidol serum concentration on day 4 was 0.71 （0.32-1.82） μg/L （n = 23）. Longitudinal course of mean QTc did not significantly differ between treatment arms for any of the automatic or manually derived QTc values. Conclusions Low dose oral haloperidol did not result in QTc prolongation in older acutely hospitalised patients. Results may not be generalizable to patients with existing ECG abnormalities such as atrial fibrillation.展开更多
BACKGROUND We report a case of lorazepam-induced agitated delirium treated with haloperidol,which in turn triggered the onset of neuroleptic malignant syndrome(NMS).The latter condition,a medical emergency,was effecti...BACKGROUND We report a case of lorazepam-induced agitated delirium treated with haloperidol,which in turn triggered the onset of neuroleptic malignant syndrome(NMS).The latter condition,a medical emergency,was effectively treated with medical treatment and dexmedetomidine,a versatile and highly selective shortacting alpha-2 adrenergic agonist with sedative-hypnotic and anxiolytic effects.CASE SUMMARY A 65-year-old man with a history of bipolar disorder presented to the emergency department with severe abdominal discomfort after binge eating.During his hospital stay,he received intravenous lorazepam for insomnia.On the next day,he became delirious and was thus treated with seven doses(5 mg each)of haloperidol over a 48 h period.Signs of NMS(hyperthermia,rigidity,myoclonus of upper limbs,impaired consciousness,tachypnea,and dark urine)became apparent and haloperidol was immediately suspended and brisk diuresis was initiated.On intensive care unit admission,he was confused,disoriented,and markedly agitated.Dexmedetomidine infusion was started with the goal of achieving a Richmond Agitation-Sedation Scale score of-1 or 0.NMS was resolved gradually and the patient stabilized,permitting discontinuation of dexmedetomidine after 3 d.CONCLUSION Dexmedetomidine may be clinically helpful for the management of NMS,most likely because of its sympatholytic activity.展开更多
Relationship between sociability and the amount of brain’s dopamine is very well known. In this study, we have examined the effect of Citrus aurantium L. essential oil on anxiety and its interaction with dopaminergic...Relationship between sociability and the amount of brain’s dopamine is very well known. In this study, we have examined the effect of Citrus aurantium L. essential oil on anxiety and its interaction with dopaminergic pathways. 70 male mice were assigned into experimental, control, and sham groups. Essential oil of Citrus aurantium L. was injected intraperitonealy at doses of 0.5%, 2.5% and 5% for 5 days. Subcutaneous injection of haloperidol was administered on the fifth day, 30 minutes before the injection of the essential oil. The anxiety-related behavior of mice was then assessed by elevated plus-maze test. The result of this study showed that the injection of Citrus aurantium L. essential oil at doses of 2.5% and 5% increased significantly the time spent in the open arms (OAT) (p < 0.001), also there was a significant increase in the number of entries into the open arms (OAE). Injection of different doses of the essential oil along with haloperidol significantly increased OAT (p < 0.001(. The results demonstrate that the essential oil of Citrus aurantium L. along with haloperidol medication reduces anxiety-related behaviors.展开更多
Objective: Intramuscular (IM) Benzodiazepines and/or Haloperidol alone or with benzodiazepines are frequently used to treat agitation. Based on emerging literature regarding Quetiapine used for the control of anxiety ...Objective: Intramuscular (IM) Benzodiazepines and/or Haloperidol alone or with benzodiazepines are frequently used to treat agitation. Based on emerging literature regarding Quetiapine used for the control of anxiety we examined Quetiapine as a possible alternative in selected cases. Methods: This study was a single-blind randomized study comparing Quetiapine PO (300 mg) with a combination of Haloperidol (5 mg), Benztropine mesylate (2 mg) and lorazepam (2 mg) administered IM to treat agitated patients seeking care in a busy psychiatric emergency setting. Male or female patients (18 - 60), deemed by the attending (admitting) psychiatrist to be indicative of agitated and/or aggressive behavior and had a Positive and Negative Syndrome Score-Excited Component (PANSS-EC), as evaluated by the Research Psychiatrist, and total score equal to or greater than 15. Patients deemed competent were randomized into one of the following treatment groups: Quetiapine 300 or Haloperidol 5 mg, benztropine mesylate, or lorazepam given by the IM route. Two scales, PANSS-EC and CGI-C were used to assess patients in the trial. The primary outcome measure PANSS-EC at 2 hours after administration of the medication. Results: Sixty-eight patients were included in the study. There were no significant treatment group differences in baseline condition. There was no significant difference between the two conditions. There was, however, a significant within-group decrease from baseline condition. Conclusion: Finding no significant differences suggests that in general the two treatments were equivalent. To sum up, Quetiapine 300 mg as a single dose appeared safe and effective in agitated patients treated in an ER. The results were similar to a comparison group receiving an intra-muscular combination of Haloperidol, Lorazepam and Benztropine. This study has significant limitations. The study was single blind and the use of a placebo would have strengthened the design but would be considered unethical. The sample size was relatively small and the group of patients who come to the ER may not be representative of the population of patients who visit across the country. And finally it was a select subgroup who made up the study population and who were probably less severely ill than other subjects who came to our ER.展开更多
<strong>Introduction:</strong> Because of the rising prevalence of cannabis abuse, cannabinoid hyperemesis syndrome (CHS) was recognized as a new medical diagnosis in 2004. Despite the syndrome’s growing ...<strong>Introduction:</strong> Because of the rising prevalence of cannabis abuse, cannabinoid hyperemesis syndrome (CHS) was recognized as a new medical diagnosis in 2004. Despite the syndrome’s growing prevalence, many providers are unfamiliar with its diagnosis and treatment, and there is little data to back up clinical knowledge and treatment recommendations. For many years, haloperidol has been widely used as an antiemetic, despite a lack of evidence-based clinical data on efficacy and side effects. We present the case of a female who presented to the emergency room with suspected CHS and was treated with haloperidol. <strong>Case: </strong>A 34-year-old African-American woman with diabetes and a history of marijuana use presented to the emergency department with refractory nausea and vomiting. Her urine drug screen came back positive for THC, but she denied using marijuana prior to this admission. She stated that she was following her current medication regimen. She denied drinking alcohol and smoking cigarettes. Multiple doses of ondansetron, promethazine, scopolamine, and metoclopramide had no effect on the patient. After two days of treatment with haloperidol 5 mg by mouth every 8 hours, nausea and vomiting subsided. <strong>Discussion:</strong> Haloperidol was able to control nausea and vomiting in six previous case reports of CHS. However, haloperidol was administered intravenously in five of the reports, and the route of administration was not specified in the sixth. To the best of our knowledge, we are the first to demonstrate the benefit of oral haloperidol for CHS. <strong>Conclusion:</strong> Although cessation of marijuana use is required for long-term resolution of CHS, our case and six others show the benefit of using IV haloperidol for acute management and oral for relapse prevention. More extensive clinical trials are needed to confirm haloperidol’s therapeutic role in patients presenting with CHS symptoms.展开更多
Dysphagia induces aspiration and causes aspiration pneumonia. There is no treatment for dysphagia fundamentally. Haloperidol reportedly induces dysphagia. In the present study, we established a haloperidol-induced dys...Dysphagia induces aspiration and causes aspiration pneumonia. There is no treatment for dysphagia fundamentally. Haloperidol reportedly induces dysphagia. In the present study, we established a haloperidol-induced dysphagia model in guinea pigs, and evaluated the effects of ginger, kikyoto, and a mixture of ginger and kikyoto on swallowing. Swallowing ability was evaluated using behavioral tests, computed tomography (CT), and videofluoroscopic examination of swallowing. To investigate the effect of ginger and kikyoto on swallowing, ginger, kikyoto, or a mixture of ginger and kikyoto was administered orally to guinea pigs with haloperidol-induced dysphagia. Effects of these compounds were evaluated with behavioral tests. Chronic administration of haloperidol reduced the number of swallows, as evaluated by the behavioral test and videofluoroscopic examination of swallowing. In our model, these compounds improved swallowing dysfunction. Our results suggest that this model might be useful in revealing the pathogenesis of dysphagia and evaluating compounds that might improve swallowing.展开更多
The rapid increase in consumption of herbal remedies worldwide has been stimulated by several factors, including the notion that all herbal products are safe and effective. Hyperprolactinemia is a major cause of infer...The rapid increase in consumption of herbal remedies worldwide has been stimulated by several factors, including the notion that all herbal products are safe and effective. Hyperprolactinemia is a major cause of infertility, and herbal remedies have been employed locally for treatment. This study was designed to investigate the effects of hydroethanolic extract of Solenostemon monostachyus on the reproductive hormones and metabolic parameters of haloperidol-induced hyperprolactinemic rats. Thirty six female albino rats were divided into 6 groups of 6 in each group. Groups A, B, C, D and E were given increasing doses （2, 3 and 4 mg/kg body weight in five-daily increments） of haloperidol by intramuscular injection for 15 days after which they were treated for another 15 days with either 2.5mg/kg body weight ofbromocriptine （group D only） or 75, 112.5 or 225mg/kg body weight of the extract （groups A, B and C, respectively）. Group F was given distilled water only. After treatment, the animals were sacrificed and blood was taken from each group for plasma analysis of the reproductive hormones and metabolic parameters. The total protein and the lipid profile （total cholesterol and HDL （high-density lipoprotein） and triglycerides were also determined. Phytochemical investigation revealed the presence of saponins, phenols, alkaloids, fiavonoids, and tannins. The result of endocrine investigation showed a dose-dependent, statistically significant reduction in prolactin and testosterone （P 〈 0.05） level by the extract with statistical significant increase （P 〈 0.05） in the levels of the follicle stimulating hormone, LH （luteinizing hormone） and estrogen. There was also a decrease in the levels of the triglycerides and total cholesterol while HDL was increased （P 〉 0.05）. It can be concluded from this study, that hydroethanolic extract has a prolactin reducing activity compared with Bromocriptine and exhibited a corresponding statistical significant difference in other reproductive hormones, with no detectable alteration on metabolic parameters such as＂ albumin, total cholesterol, and high density lipoprotein.展开更多
In the present study,haloperidol(HP)-loaded solid lipid nanoparticles(SLNs)were prepared to enhance the uptake of HP to brain via intranasal(i.n.)delivery.SLNs were prepared by a modified emulsification-diffusion tech...In the present study,haloperidol(HP)-loaded solid lipid nanoparticles(SLNs)were prepared to enhance the uptake of HP to brain via intranasal(i.n.)delivery.SLNs were prepared by a modified emulsification-diffusion technique and evaluated for particle size,zeta potential,drug entrapment efficiency,in vitro drug release,and stability.All parameters were found to be in an acceptable range.In vitro drug release was found to be 94.1674.78%after 24 h and was fitted to the Higuchi model with a very high correlation coefficient(R2¼0.9941).Pharmacokinetics studies were performed on albino Wistar rats and the concentration of HP in brain and blood was measured by high performance liquid chromatography.The brain/blood ratio at 0.5 h for HP-SLNs i.n.,HP sol.i.n.and HP sol.i.v.was 1.61,0.17 and 0.031,respectively,indicating direct nose-to-brain transport,bypassing the blood-brain barrier.The maximum concentration(Cmax)in brain achieved from i.n.administration of HP-SLNs(329.17720.89 ng/mL,Tmax 2 h)was significantly higher than that achieved after i.v.(76.9577.62 ng/mL,Tmax 1 h),and i.n.(90.1376.28 ng/mL,Tmax 2 h)administration of HP sol.The highest drug-targeting efficiency(2362.43%)and direct transport percentage(95.77%)was found with HP-SLNs as compared to the other formulations.Higher DTE(%)and DTP(%)suggest that HP-SLNs have better brain targeting efficiency as compared to other formulations.展开更多
Objectives To explore the association between schizophrenic symptoms and superoxide dismutase (SOD), and to investigate the effect of classic antipsychotic haloperidol plus the extract of Ginkgo biloba (EGb) on S...Objectives To explore the association between schizophrenic symptoms and superoxide dismutase (SOD), and to investigate the effect of classic antipsychotic haloperidol plus the extract of Ginkgo biloba (EGb) on SOD Methods In 54 patients with chronic refractory schizophrenia, 27 were treated with haloperidol plus EGb (group 1), and the rest received haloperidol plus placebo (group 2) Superoxide dismutase (SOD) levels of these patients were measured before and after treatment and compared with the levels of 25 healthy volunteers Therapeutic efficacy was equated with a change in clinical rating scores assessed by standardized measurement tools including the Scale for Assessment of Positive Symptoms (SAPS) and the Scale for Assessment of Negative Symptoms (SANS) Results Patients in group 1 improved significantly as demonstrated by scores from both SAPS and SANS, while those in group 2 only by scores from SANS Assessed by SAPS, the response of patients receiving haloperidol plus EGb was more significant than those receiving haloperidol only SOD levels before treatment in all patients were significantly higher than those in normal controls After treatment, SOD levels decreased significantly in group 1 but not in group 2 In addition, before treatment, SOD levels in all patients correlated significantly with SAPS score The levels of SOD measured before treatment were also correlated with the improvement of patients as measured by SAPS and SANS after 12 weeks Conclusions EGb may enhance the efficacy of classic antipsychotic haloperidol on schizophrenia, especially on positive symptoms It may work through an antioxidant efficacy that is involved in the therapeutic mechanism展开更多
目的:探究阿立哌唑、利培酮与氟哌啶醇治疗儿童抽动障碍的效果及安全性。方法:选取2021年3月—2024年3月于昭通市中医医院诊治的96例儿童抽动障碍患儿,随机分为阿立哌唑组、利培酮组、氟哌啶醇组,各32例。比较三组抽动严重程度[耶鲁综...目的:探究阿立哌唑、利培酮与氟哌啶醇治疗儿童抽动障碍的效果及安全性。方法:选取2021年3月—2024年3月于昭通市中医医院诊治的96例儿童抽动障碍患儿,随机分为阿立哌唑组、利培酮组、氟哌啶醇组,各32例。比较三组抽动严重程度[耶鲁综合抽动严重程度量表(Yale global tic severity scale,YGTSS)]、临床疗效及不良反应。结果:三组治疗前、治疗4周后、治疗8周后YGTSS评分比较,差异无统计学意义(P>0.05);三组治疗4周、8周后YGTSS评分低于治疗前,且三组治疗8周后YGTSS评分低于治疗4周后,差异有统计学意义(P<0.05)。三组临床总有效率比较,差异无统计学意义(P>0.05)。三组不良反应发生率比较,差异有统计学意义(P<0.05)。结论:阿立哌唑、利培酮与氟哌啶醇应用于儿童抽动障碍,均有利于改善患儿抽动症状,但相较于利培酮与氟哌啶醇,阿立哌唑治疗后不良反应较小,更具安全性。展开更多
BACKGROUND:Agitation is a common presentation within emergent departments(EDs).Agitation during pregnancy should be treated as an obstetric emergency,as the distress may jeopardize both the patient and fetus.The safet...BACKGROUND:Agitation is a common presentation within emergent departments(EDs).Agitation during pregnancy should be treated as an obstetric emergency,as the distress may jeopardize both the patient and fetus.The safety of psychotropic medications in the reproductive age female has not been well established.This review aimed to explore a summary of general agitation recommendations with an emphasis on ED management of agitation during pregnancy.METHODS:A literature review was conducted to explore the pathophysiology of acute agitation and devise a preferred treatment plan for ED management of acute agitation in the reproductive age or pregnant female.RESULTS:While nonpharmacological management is preferred,ED visits for agitation often require medical management.Medication should be selected based on the etiology of agitation and the clinical setting to avoid major adverse effects.Adverse effects are common in pregnant females.For mild to moderate agitation in pregnancy,diphenhydramine is an effective sedating agent with minimal adverse effects.In moderate to severe agitation,high-potency typical psychotropics are preferred due to their neutral effects on hemodynamics.Haloperidol has become the most frequently utilized psychotropic for agitation during pregnancy.Second generation psychotropics are often utilized as second-line therapy,including risperidone.Benzodiazepines and ketamine have demonstrated adverse fetal outcomes.CONCLUSION:While randomized control studies cannot be ethically conducted on pregnant patients requiring sedation,animal models and epidemiologic studies have demonstrated the effects of psychotropic medication exposure in utero.As the fetal risk associated with multiple doses of psychotropic medications remains unknown,weighing the risks and benefits of each agent,while utilizing the lowest effective dose remains critical in the treatment of acute agitation within the EDs.展开更多
基金National Natural Science Foundation of China,Grant/Award Number:81903613。
文摘Background:To investigate the toxicity of N-n-butyl haloperidol iodide(F2),a quaternary ammonium salt derivative of haloperidol,in mice for potential therapeutic purposes.Methods:The acute median lethal dose(LD_(50))of F2 was determined using the Bliss method following intravenous administration in mice.Routine surface electrocardiograms(ECGs)and arterial blood pressures(aBPs)were recorded under general anesthesia in untreated and pharmacologically vagotomized mice injected with F2.Sublethal doses of F2 were tested for their effects on aBP,heart rate,and biochemical parameters such as lactate dehydrogenase(LDH),blood urea nitrogen(BUN),and serum lactate levels.Histopathological changes in the heart,lungs,liver,and kidneys were evaluated after F2 administration.Results:The acute LD_(50)of F2 was determined to be 5.11 mg/kg.A 10 mg/kg dose of F2 caused severe hypotension,second-degree atrioventricular block,progressive prolongation of Pmurr intervals,and death due to cardiac asystole.Similar ECG and aBP changes were observed in atropine-pretreated mice,indicating that cholinergic effects do not play a major role in F2-induced toxicity.Sublethal doses of F2(1.2 and 2.4 mg/kg)caused dose-dependent decreases in aBP and increases in heart rate.F2 induced significant,dose-dependent increases in LDH,BUN,and serum lactate levels.Histopathological analysis revealed acute lung lesions at 10 mg/kg,with no significant changes observed in the heart,liver,or kidneys.Conclusion:Acute intravenous injection of F2 exhibits dose-dependent cardiopulmonary toxicity,characterized by severe hypotension,arrhythmias,and biochemical changes.These findings highlight the potential risks of F2 and the need for further evaluation of its safety profile for therapeutic use.
基金This work was supported by the Princess Nourah bint Abdulrahman University Researchers Supporting Project number(PNURSP2025R73)Princess Nourah bint Abdulrahman University,Riyadh,Saudi Arabia,and researchers supporting project number(RSPD2025R885)at King Saud University Riyadh Saudi Arabia。
文摘Objective:To investigate the effect of Rosa moschata(R.moschata)extract on haloperidol-induced Parkinson’s disease(PD)in rats.Methods:Haloperidol(1 mg/kg)was given to rats intraperitoneally for 3 weeks for induction of PD.R.moschata extract(150,300 and 600 mg/kg)was administered orally for 21 days.The neuroprotective role of R.moschata leaf extract in PD was explored by performing neurobehavioral tests and RT-PCR analysis and measuring neurotransmitters and oxidative stress biomarkers.Results:An improvement in motor functions and muscle strength was observed in PD rats treated with R.moschata extract.The levels of dopamine,serotonin,noradrenaline,superoxide dismutase,catalase,glutathione,and superoxide dismutase were significantly increased(P<0.001),whereas acetylcholinesterase and malondialdehyde levels were markedly decreased by treatment with R.moschata extract(P<0.001).The extract also markedly downregulated the mRNA expressions of IL-1β,α-synuclein,IL-1α,and TNF-αin brain tissue.Moreover,histopathological analysis indicated that neurofibrillary tangles and plaques were noticeably decreased in a dose-dependent manner in PD rats treated with R.moschata extract.Conclusions:R.moschata extract alleviates haloperidol-induced PD in rats by reducing oxidative stress and neurodegeneration.It may be used for management and treatment of PD.However additional studies are required to confirm its efficacy and molecular mechanisms.
文摘Background Haloperidol is the most frequently prescribed antipsycbotic for delirium symptoms. The risk of QTc prolongation often raises concerns, although the effect of haloperidol on QTc interval has not yet been investigated in a randomised placebo-controlled fixed-dose study. Methods A subanalysis of a randomised double-blind placebo-controlled study was conducted to evaluate the effect of prophylactic haloperidol 1 mg or placebo 1 mg orally twice-daily （maximum of 14 doses） on QTc interval in patients aged 70 years and over. Bedside, 12-lead ECGs were recorded before, during and after the one-week intervention period. Automatic QTc measurements were ob- tained in addition to manual measurements of QT and RR intervals, blinded for treatment status. Manual measurements were corrected （QTc） using Bazett （QTc-B）, Framingham （QTc-Fa）, Fridericia （QTc-Fi） and Hodges （QTc-H） methods. Mixed model analyses were used to test for differences in longitudinal course of QTc between patients receiving haloperidol and placebo. Results ECG recordings of 72 patients （haloperidol n = 38） were analysed, 45.8% male. Median （range） haloperidol serum concentration on day 4 was 0.71 （0.32-1.82） μg/L （n = 23）. Longitudinal course of mean QTc did not significantly differ between treatment arms for any of the automatic or manually derived QTc values. Conclusions Low dose oral haloperidol did not result in QTc prolongation in older acutely hospitalised patients. Results may not be generalizable to patients with existing ECG abnormalities such as atrial fibrillation.
基金Supported by National Taiwan University Hospital Fund,No.MS 213.
文摘BACKGROUND We report a case of lorazepam-induced agitated delirium treated with haloperidol,which in turn triggered the onset of neuroleptic malignant syndrome(NMS).The latter condition,a medical emergency,was effectively treated with medical treatment and dexmedetomidine,a versatile and highly selective shortacting alpha-2 adrenergic agonist with sedative-hypnotic and anxiolytic effects.CASE SUMMARY A 65-year-old man with a history of bipolar disorder presented to the emergency department with severe abdominal discomfort after binge eating.During his hospital stay,he received intravenous lorazepam for insomnia.On the next day,he became delirious and was thus treated with seven doses(5 mg each)of haloperidol over a 48 h period.Signs of NMS(hyperthermia,rigidity,myoclonus of upper limbs,impaired consciousness,tachypnea,and dark urine)became apparent and haloperidol was immediately suspended and brisk diuresis was initiated.On intensive care unit admission,he was confused,disoriented,and markedly agitated.Dexmedetomidine infusion was started with the goal of achieving a Richmond Agitation-Sedation Scale score of-1 or 0.NMS was resolved gradually and the patient stabilized,permitting discontinuation of dexmedetomidine after 3 d.CONCLUSION Dexmedetomidine may be clinically helpful for the management of NMS,most likely because of its sympatholytic activity.
文摘Relationship between sociability and the amount of brain’s dopamine is very well known. In this study, we have examined the effect of Citrus aurantium L. essential oil on anxiety and its interaction with dopaminergic pathways. 70 male mice were assigned into experimental, control, and sham groups. Essential oil of Citrus aurantium L. was injected intraperitonealy at doses of 0.5%, 2.5% and 5% for 5 days. Subcutaneous injection of haloperidol was administered on the fifth day, 30 minutes before the injection of the essential oil. The anxiety-related behavior of mice was then assessed by elevated plus-maze test. The result of this study showed that the injection of Citrus aurantium L. essential oil at doses of 2.5% and 5% increased significantly the time spent in the open arms (OAT) (p < 0.001), also there was a significant increase in the number of entries into the open arms (OAE). Injection of different doses of the essential oil along with haloperidol significantly increased OAT (p < 0.001(. The results demonstrate that the essential oil of Citrus aurantium L. along with haloperidol medication reduces anxiety-related behaviors.
文摘Objective: Intramuscular (IM) Benzodiazepines and/or Haloperidol alone or with benzodiazepines are frequently used to treat agitation. Based on emerging literature regarding Quetiapine used for the control of anxiety we examined Quetiapine as a possible alternative in selected cases. Methods: This study was a single-blind randomized study comparing Quetiapine PO (300 mg) with a combination of Haloperidol (5 mg), Benztropine mesylate (2 mg) and lorazepam (2 mg) administered IM to treat agitated patients seeking care in a busy psychiatric emergency setting. Male or female patients (18 - 60), deemed by the attending (admitting) psychiatrist to be indicative of agitated and/or aggressive behavior and had a Positive and Negative Syndrome Score-Excited Component (PANSS-EC), as evaluated by the Research Psychiatrist, and total score equal to or greater than 15. Patients deemed competent were randomized into one of the following treatment groups: Quetiapine 300 or Haloperidol 5 mg, benztropine mesylate, or lorazepam given by the IM route. Two scales, PANSS-EC and CGI-C were used to assess patients in the trial. The primary outcome measure PANSS-EC at 2 hours after administration of the medication. Results: Sixty-eight patients were included in the study. There were no significant treatment group differences in baseline condition. There was no significant difference between the two conditions. There was, however, a significant within-group decrease from baseline condition. Conclusion: Finding no significant differences suggests that in general the two treatments were equivalent. To sum up, Quetiapine 300 mg as a single dose appeared safe and effective in agitated patients treated in an ER. The results were similar to a comparison group receiving an intra-muscular combination of Haloperidol, Lorazepam and Benztropine. This study has significant limitations. The study was single blind and the use of a placebo would have strengthened the design but would be considered unethical. The sample size was relatively small and the group of patients who come to the ER may not be representative of the population of patients who visit across the country. And finally it was a select subgroup who made up the study population and who were probably less severely ill than other subjects who came to our ER.
文摘<strong>Introduction:</strong> Because of the rising prevalence of cannabis abuse, cannabinoid hyperemesis syndrome (CHS) was recognized as a new medical diagnosis in 2004. Despite the syndrome’s growing prevalence, many providers are unfamiliar with its diagnosis and treatment, and there is little data to back up clinical knowledge and treatment recommendations. For many years, haloperidol has been widely used as an antiemetic, despite a lack of evidence-based clinical data on efficacy and side effects. We present the case of a female who presented to the emergency room with suspected CHS and was treated with haloperidol. <strong>Case: </strong>A 34-year-old African-American woman with diabetes and a history of marijuana use presented to the emergency department with refractory nausea and vomiting. Her urine drug screen came back positive for THC, but she denied using marijuana prior to this admission. She stated that she was following her current medication regimen. She denied drinking alcohol and smoking cigarettes. Multiple doses of ondansetron, promethazine, scopolamine, and metoclopramide had no effect on the patient. After two days of treatment with haloperidol 5 mg by mouth every 8 hours, nausea and vomiting subsided. <strong>Discussion:</strong> Haloperidol was able to control nausea and vomiting in six previous case reports of CHS. However, haloperidol was administered intravenously in five of the reports, and the route of administration was not specified in the sixth. To the best of our knowledge, we are the first to demonstrate the benefit of oral haloperidol for CHS. <strong>Conclusion:</strong> Although cessation of marijuana use is required for long-term resolution of CHS, our case and six others show the benefit of using IV haloperidol for acute management and oral for relapse prevention. More extensive clinical trials are needed to confirm haloperidol’s therapeutic role in patients presenting with CHS symptoms.
文摘Dysphagia induces aspiration and causes aspiration pneumonia. There is no treatment for dysphagia fundamentally. Haloperidol reportedly induces dysphagia. In the present study, we established a haloperidol-induced dysphagia model in guinea pigs, and evaluated the effects of ginger, kikyoto, and a mixture of ginger and kikyoto on swallowing. Swallowing ability was evaluated using behavioral tests, computed tomography (CT), and videofluoroscopic examination of swallowing. To investigate the effect of ginger and kikyoto on swallowing, ginger, kikyoto, or a mixture of ginger and kikyoto was administered orally to guinea pigs with haloperidol-induced dysphagia. Effects of these compounds were evaluated with behavioral tests. Chronic administration of haloperidol reduced the number of swallows, as evaluated by the behavioral test and videofluoroscopic examination of swallowing. In our model, these compounds improved swallowing dysfunction. Our results suggest that this model might be useful in revealing the pathogenesis of dysphagia and evaluating compounds that might improve swallowing.
文摘The rapid increase in consumption of herbal remedies worldwide has been stimulated by several factors, including the notion that all herbal products are safe and effective. Hyperprolactinemia is a major cause of infertility, and herbal remedies have been employed locally for treatment. This study was designed to investigate the effects of hydroethanolic extract of Solenostemon monostachyus on the reproductive hormones and metabolic parameters of haloperidol-induced hyperprolactinemic rats. Thirty six female albino rats were divided into 6 groups of 6 in each group. Groups A, B, C, D and E were given increasing doses （2, 3 and 4 mg/kg body weight in five-daily increments） of haloperidol by intramuscular injection for 15 days after which they were treated for another 15 days with either 2.5mg/kg body weight ofbromocriptine （group D only） or 75, 112.5 or 225mg/kg body weight of the extract （groups A, B and C, respectively）. Group F was given distilled water only. After treatment, the animals were sacrificed and blood was taken from each group for plasma analysis of the reproductive hormones and metabolic parameters. The total protein and the lipid profile （total cholesterol and HDL （high-density lipoprotein） and triglycerides were also determined. Phytochemical investigation revealed the presence of saponins, phenols, alkaloids, fiavonoids, and tannins. The result of endocrine investigation showed a dose-dependent, statistically significant reduction in prolactin and testosterone （P 〈 0.05） level by the extract with statistical significant increase （P 〈 0.05） in the levels of the follicle stimulating hormone, LH （luteinizing hormone） and estrogen. There was also a decrease in the levels of the triglycerides and total cholesterol while HDL was increased （P 〉 0.05）. It can be concluded from this study, that hydroethanolic extract has a prolactin reducing activity compared with Bromocriptine and exhibited a corresponding statistical significant difference in other reproductive hormones, with no detectable alteration on metabolic parameters such as＂ albumin, total cholesterol, and high density lipoprotein.
文摘In the present study,haloperidol(HP)-loaded solid lipid nanoparticles(SLNs)were prepared to enhance the uptake of HP to brain via intranasal(i.n.)delivery.SLNs were prepared by a modified emulsification-diffusion technique and evaluated for particle size,zeta potential,drug entrapment efficiency,in vitro drug release,and stability.All parameters were found to be in an acceptable range.In vitro drug release was found to be 94.1674.78%after 24 h and was fitted to the Higuchi model with a very high correlation coefficient(R2¼0.9941).Pharmacokinetics studies were performed on albino Wistar rats and the concentration of HP in brain and blood was measured by high performance liquid chromatography.The brain/blood ratio at 0.5 h for HP-SLNs i.n.,HP sol.i.n.and HP sol.i.v.was 1.61,0.17 and 0.031,respectively,indicating direct nose-to-brain transport,bypassing the blood-brain barrier.The maximum concentration(Cmax)in brain achieved from i.n.administration of HP-SLNs(329.17720.89 ng/mL,Tmax 2 h)was significantly higher than that achieved after i.v.(76.9577.62 ng/mL,Tmax 1 h),and i.n.(90.1376.28 ng/mL,Tmax 2 h)administration of HP sol.The highest drug-targeting efficiency(2362.43%)and direct transport percentage(95.77%)was found with HP-SLNs as compared to the other formulations.Higher DTE(%)and DTP(%)suggest that HP-SLNs have better brain targeting efficiency as compared to other formulations.
文摘Objectives To explore the association between schizophrenic symptoms and superoxide dismutase (SOD), and to investigate the effect of classic antipsychotic haloperidol plus the extract of Ginkgo biloba (EGb) on SOD Methods In 54 patients with chronic refractory schizophrenia, 27 were treated with haloperidol plus EGb (group 1), and the rest received haloperidol plus placebo (group 2) Superoxide dismutase (SOD) levels of these patients were measured before and after treatment and compared with the levels of 25 healthy volunteers Therapeutic efficacy was equated with a change in clinical rating scores assessed by standardized measurement tools including the Scale for Assessment of Positive Symptoms (SAPS) and the Scale for Assessment of Negative Symptoms (SANS) Results Patients in group 1 improved significantly as demonstrated by scores from both SAPS and SANS, while those in group 2 only by scores from SANS Assessed by SAPS, the response of patients receiving haloperidol plus EGb was more significant than those receiving haloperidol only SOD levels before treatment in all patients were significantly higher than those in normal controls After treatment, SOD levels decreased significantly in group 1 but not in group 2 In addition, before treatment, SOD levels in all patients correlated significantly with SAPS score The levels of SOD measured before treatment were also correlated with the improvement of patients as measured by SAPS and SANS after 12 weeks Conclusions EGb may enhance the efficacy of classic antipsychotic haloperidol on schizophrenia, especially on positive symptoms It may work through an antioxidant efficacy that is involved in the therapeutic mechanism
文摘目的:探究阿立哌唑、利培酮与氟哌啶醇治疗儿童抽动障碍的效果及安全性。方法:选取2021年3月—2024年3月于昭通市中医医院诊治的96例儿童抽动障碍患儿,随机分为阿立哌唑组、利培酮组、氟哌啶醇组,各32例。比较三组抽动严重程度[耶鲁综合抽动严重程度量表(Yale global tic severity scale,YGTSS)]、临床疗效及不良反应。结果:三组治疗前、治疗4周后、治疗8周后YGTSS评分比较,差异无统计学意义(P>0.05);三组治疗4周、8周后YGTSS评分低于治疗前,且三组治疗8周后YGTSS评分低于治疗4周后,差异有统计学意义(P<0.05)。三组临床总有效率比较,差异无统计学意义(P>0.05)。三组不良反应发生率比较,差异有统计学意义(P<0.05)。结论:阿立哌唑、利培酮与氟哌啶醇应用于儿童抽动障碍,均有利于改善患儿抽动症状,但相较于利培酮与氟哌啶醇,阿立哌唑治疗后不良反应较小,更具安全性。
文摘BACKGROUND:Agitation is a common presentation within emergent departments(EDs).Agitation during pregnancy should be treated as an obstetric emergency,as the distress may jeopardize both the patient and fetus.The safety of psychotropic medications in the reproductive age female has not been well established.This review aimed to explore a summary of general agitation recommendations with an emphasis on ED management of agitation during pregnancy.METHODS:A literature review was conducted to explore the pathophysiology of acute agitation and devise a preferred treatment plan for ED management of acute agitation in the reproductive age or pregnant female.RESULTS:While nonpharmacological management is preferred,ED visits for agitation often require medical management.Medication should be selected based on the etiology of agitation and the clinical setting to avoid major adverse effects.Adverse effects are common in pregnant females.For mild to moderate agitation in pregnancy,diphenhydramine is an effective sedating agent with minimal adverse effects.In moderate to severe agitation,high-potency typical psychotropics are preferred due to their neutral effects on hemodynamics.Haloperidol has become the most frequently utilized psychotropic for agitation during pregnancy.Second generation psychotropics are often utilized as second-line therapy,including risperidone.Benzodiazepines and ketamine have demonstrated adverse fetal outcomes.CONCLUSION:While randomized control studies cannot be ethically conducted on pregnant patients requiring sedation,animal models and epidemiologic studies have demonstrated the effects of psychotropic medication exposure in utero.As the fetal risk associated with multiple doses of psychotropic medications remains unknown,weighing the risks and benefits of each agent,while utilizing the lowest effective dose remains critical in the treatment of acute agitation within the EDs.
