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1.
ARS med. (Santiago, En línea) ; 48(1): 31-38, 28 mar. 2023.
Article in Spanish | LILACS-Express | LILACS | ID: biblio-1451912

ABSTRACT

Introducción: el paciente intoxicado sigue siendo un desafío para el personal de salud. La intoxicación por antidepresivos tricíclicos (ATC) es un diagnóstico frecuente y una patología que puede llegar a ser muy grave. A pesar de que ha cambiado el objetivo terapéutico de estos fármacos a lo largo de los años, la alta disponibilidad de estos hace que su uso para intento de autolisis siga presentándose. Su presentación clínica es variada y dado el riesgo de mortalidad asociada, es importante que esta patología sea rápidamente reconocida por los médicos que los reciben para iniciar un manejo oportuno y eficaz. Objetivo: presentar el enfrentamiento inicial y manejo terapéutico de la intoxicación por ATC desde la perspectiva de la medicina de urgencia. Método: se realizó una revisión bibliográfica de la literatura científica sobre el manejo de un paciente intoxicado por ATC. Se presenta la evidencia actual de las intervenciones terapéuticas más utilizadas. respecto al manejo inicial y enfrentamiento de la intoxicación por antidepresivos tricíclicos, en el contexto de la atención en un servicio de urgencia. Conclusión: la intoxicación por ATC puede presentarse con síntomas leves y signos precoces, así como con síntomas graves e incluso fatales, dados principalmente por complicaciones cardiovasculres y neurológicas. Su manejo se basa en el reconocimiento precoz, medidas de soporte y terapias específicas según la clínica que presente.


Managing poisoned patients continues to be a challenge for health personnel. Tricyclic antidepressant are a frequent diagnosis, and a pathology their can be very serious. Although the therapeutic indications for these drugs have changed over the years, their high availability means that their use for suicidal attempts continues to be present. Its clinical presentation is varied and given the mortality risk, it is crucial that this entity must be rapidly recognized by the physicians who care for them to initiate timely and effective treatment. Objective: Present the initial management and therapeutic strategies for tricyclic antidepressant intoxication, from emergency medicine perspective. Method: Bibliographic review of the scientific literature on this subject. Current evidence of the most widely used therapeutic interventions is described regarding the initial management and disposition of tricyclic antidepressant intoxication in the emergency department.

2.
Braz. J. Pharm. Sci. (Online) ; 59: e21606, 2023. tab, graf
Article in English | LILACS | ID: biblio-1447566

ABSTRACT

Abstract Amitriptyline (AMT) was developed for the treatment of chronic and neuropathic pain. There is also evidence it may be useful in the treatment of neurodegenerative disorders. In this regard, the effect of on the experimental model of seizures and memory impairment caused by seizures in rats is investigated in the present study. Seizures in Wistar rats (200-250 g) were induced by pentylenetetrazole (PTZ, 60 mg/kg, intraperitoneally (i.p.)). The anticonvulsant effect of AMT (10 and 20 mg/kg, i.p.) was evaluated in the seizure model. The effect on memory was assessed using passive avoidance (PA) learning and memory test. After behavioral tests, the animals underwent deep anesthesia and were put down painlessly. Animal serum was isolated for oxidant/antioxidant assays (malondialdehyde (MDA), and glutathione peroxidase (GPx)). Intraperitoneal injection of AMT decreased the mean number of myoclonic jerks and generalized tonic-clonic seizure (GTCS) duration and increased the mean latency of myoclonic jerk and GTCS compared to the PTZ group. Moreover, in the PA test, AMT caused a significant increase in retention latency (RL) and total time spent in the light compartment (TLC) compared to the PTZ group. Biochemical tests showed that AMT was able to significantly increase GPx serum levels and significantly reduce MDA serum levels compared to the PTZ group. Overall, this study suggests the potential neuroprotective effects of the AMT drug in a model of memory impairment caused by seizures via the mechanism of inhibition of the oxidative stress pathway.


Subject(s)
Animals , Male , Rats , Seizures/chemically induced , Memory Consolidation/classification , Amitriptyline/adverse effects , Pentylenetetrazole/agonists
3.
Article | IMSEAR | ID: sea-219151

ABSTRACT

Introduction: Antiepileptics and antidepressant medications are known for managing neuropathic pain. We aim to compare the effects of pregabalin with low‑dose amitriptyline and gabapentin with low‑dose amitriptyline in managing neuropathic pain in cancer patients undergoing palliative care. Materials and Methods: We conducted our study on 160 cancer patients who were having neuropathic pain and were undergoingpalliative care treatment in our institute. It was a hospital‑based, randomized, tertiary cancer center‑based observational study. After taking approval from the institutional ethics committee and taking written informed consent from patients, the patients were divided into two groups and the effect of medicines on incidence of neuropathic pain was observed; the incidence of burning sensation and the incidence of adverse effects of medications were also analyzed. Statistical analysis was done using paired t‑test and SPSS version 20 software. Results: The onset of relief in pain was earlier in the pregabalin group as compared to the gabapentin group. There was more reduction in a burning sensation in the pregabalin group as compared to the gabapentin group. The incidence of headaches was the same in both groups. Nausea and vomiting were more in the pregabalin group but the overall difference in adverse effects was not statistically significant (P > 0.05) Conclusions: In the management of neuropathic pain in cancer patients who are undergoing palliative care, a combination of pregabalin with amitriptyline was found to be more effective in pain relief than gabapentin with amitriptyline.

4.
Rev. gastroenterol. Peru ; 42(4)oct. 2022.
Article in English | LILACS-Express | LILACS | ID: biblio-1423951

ABSTRACT

Cyclic vomiting syndrome is a benign, chronic, functional gastrointestinal pathology that manifests clinically with intense nausea and vomiting interspersed with asymptomatic periods. Its diagnosis is made according to the Rome IV criteria, which require the presence of at least 2 episodes of vomiting in the past 6 months or 3 or more episodes in the past year, with the corresponding exclusion of secondary causes that can explain the vomiting. We present the case of a 44-year-old man who consulted for intermittent nausea and vomiting of 1 year evolution with hydroelectrolytic repercussion and multiple emergency consultations. The diagnosis of cyclic vomiting syndrome was made and treatment with amitriptyline was started due to its neuromodulatory effect to prevent the recurrence of episodes. After 6 months of establishing it, the patient is asymptomatic.


El síndrome de vómitos cíclicos es una patología gastrointestinal funcional crónica, benigna, que se manifiesta clínicamente con náuseas y vómitos intensos que intercalan con periodos asintomáticos. Su diagnóstico se realiza de acuerdo con los criterios de Roma IV, que requieren la presencia de al menos 2 episodios de vómitos en los últimos 6 meses o 3 o más episodios en el último año, con la correspondiente exclusión de causas secundarias que puedan explicar los síntomas. Se presenta el caso de un hombre de 44 años que consulta por náuseas y vómitos intermitentes de 1 año de evolución, con repercusión hidroelectrolítica y múltiples consultas en emergencia. Se realiza el diagnóstico de síndrome de vómitos cíclicos y se inicia tratamiento con amitriptilina, por su efecto neuromodulador para prevenir la recurrencia de los episodios. Luego de 6 meses de instaurado el mismo, el paciente se presenta asintomático.

5.
Arq. Asma, Alerg. Imunol ; 6(3): 404-408, Jul.Set.2022. ilus
Article in English, Portuguese | LILACS | ID: biblio-1452538

ABSTRACT

Introdução: A rinite vasomotora (RVM), também denominada idiopática, é um tipo de rinite não alérgica. Pode ser muitas vezes ativada por mudanças de temperatura, especialmente com o ar frio e outras irritantes de vias aéreas. A dosagem de IgE e o citograma nasal são normais, e os testes de inalantes são negativos. A etiologia pode estar associada à desregulação de nervos simpáticos e parassimpáticos da mucosa nasal, onde aumenta a rinorreia e a obstrução nasal. Objetivo: Avaliar a eficácia da amitriptilina no controle da rinorreia vasomotora. Método: Através de estudo retrospectivo, avaliaram-se pacientes com RVM (n = 110), no qual um grupo de n = 12 (11%) apresentava rinorreia profusa há mais de um ano, não controlada, na sua totalidade, com corticosteroide nasal. Usou-se a amitriptilina, um antidepressivo tricíclico, com intensa atividade anticolinérgica com dose de 25 mg/50 mg diária para a rinorreia nesses pacientes. Resultados: Foram avaliados através de uma escala de sintomas (modificada de Wilson AM): 0 = ausente, 1 = leve, bem tolerado, 2 = desconforto interferindo com a concentração, 3 = forte intensidade interferindo no sono e na concentração. Dez pacientes catalogados apresentaram sintomas no grau 3, e dois, no grau 2. A pontuação foi reduzida para grau 0-1 após 4-6 semanas com o uso de amitriptilina por sintomas reflexivos matinais e noturnos. Conclusão: Futuros estudos controlados e com maior número de pacientes seriam necessários para confirmação do efeito farmacológico da amitriptilina na rinorreia da RVM.


Background: Vasomotor rhinitis (VMR), also referred to as idiopathic rhinitis, is a type of nonallergic rhinitis. It can often be triggered by changes in temperature, especially with cold air and other airway irritants. Immunoglobulin E (IgE) levels and nasal cytograms are normal, and inhalant skin tests are negative. The etiology may be associated with dysregulation of the sympathetic and parasympathetic nervous systems in the nasal mucosa, with increased rhinorrhea and nasal obstruction. Objective: To evaluate the efficacy of amitriptyline in the control of VMR-related rhinorrhea. Method: We retrospectively evaluated 110 patients with VMR, of whom 12 (11%) had profuse rhinorrhea for more than 1 year, not completely controlled with nasal corticosteroids. In these 12 patients, rhinorrhea was treated with amitriptyline, a tricyclic antidepressant with intense anticholinergic activity, at a daily dose of 25 mg/50 mg. Results: Patients were evaluated using a symptom scale (modified from Wilson AM): 0 = absent; 1 = mild, well tolerated; 2 = discomfort interfering with concentration; and 3 = severe intensity interfering with sleep and concentration. Ten patients had grade 3 symptoms, and 2 had grade 2 symptoms. The score decreased to grade 0-1 after 4-6 weeks of amitriptyline use for reflex symptoms in the morning and at night. Conclusion: Further controlled studies with a larger sample size are needed to confirm the pharmacological effect of amitriptyline on VMRrelated rhinorrhea.


Subject(s)
Humans , Retrospective Studies
6.
Journal of Clinical Hepatology ; (12): 99-104, 2021.
Article in Chinese | WPRIM | ID: wpr-862552

ABSTRACT

ObjectiveTo investigate the effect of amitriptyline on lipid deposition and biochemical metabolism in a cell model of nonalcoholic fatty liver disease (NAFLD) by regulating the acid sphingomyelinase (ASM)/ceramide (CE) pathway. MethodsHepG2 and L02 cells were cultured in vitro to establish a cell model of NAFLD. MTT colorimetry was used to measure cell proliferation rate, and oil red O staining was used to observe the change of lipid droplets in cells. In the experiment, the cells were divided into normal control group, model group, Ami group, TNFα group, and Ami+TNFα group. An automatic biochemical analyzer was used to measure the levels of triglyceride (TG) and total cholesterol (TC) in cells and the levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in supernatant; ELISA was used to measure the levels of CE and ASM in cells; Western blot was used to measure the protein expression ASM in cells, and RT-PCR was used to measure the mRNA expression of ASM in cells. A one-way analysis of variance was used for comparison of continuous data between multiple groups, and the Turkey test was used for further comparison between two groups. ResultsCompared with the normal control group, the NAFLD model group had significant increases in the protein and mRNA expression of ASM and the levels of CE, TG, TC, ALT, and AST (all P<0.05). Compared with the model group, the Ami group had significant reductions in the protein and mRNA expression of ASM and the levels of CE, TG, TC, ALT, and AST (all P<0.05), and the TNFα group had significant increases in the protein and mRNA expression of ASM and the levels of CE, TG, ALT, and AST (all P<0.05). Compared with the TNFα group, the Ami+TNFα group had significant reductions in the protein and mRNA expression of ASM and the levels of CE, TG, TC, ALT, and AST (all P<0.05). ConclusionThe ASM/CE pathway promotes lipid accumulation and may lead to hepatocyte steatosis, and amitriptyline can alleviate lipid deposition in NAFLD hepatocytes by inhibiting the ASM/CE pathway.

7.
Braz. J. Pharm. Sci. (Online) ; 56: e18852, 2020. tab, graf
Article in English | LILACS | ID: biblio-1249150

ABSTRACT

Rheumatoid arthritis (RA) is a chronic inflammatory disorder that causes pain, systemic complications and premature mortality. Depression has also been identified as a problem for persons with RA. This association remaining significant even after the degree of disease activity is controlled. In the present study, the efficacy of combination therapeutic effect of antidepressant (amitriptyline) with Disease Modifying Anti rheumatoid drug (leflunomide) was determined in rheumatoid arthritis pain associated depression in Freund's complete adjuvant (FCA) induced arthritic rats. Drug treatment was started 9 days after induction of FCA induced arthritis in rats. The antiarthritic activity was assessed by measuring paw volume, weight-bearing, hematological, biochemical, serological parameters, Radiographic analysis and Histopathology of tibiotarsal joints. The antidepressant activity was assessed by Forced swimming test, Rota-rod test and confirmed by estimation of brain neuro transmitters (serotonin and norepinephrine) level. Results of this study revealed that leflunomide and amitriptyline combination showed more significant (p<0.001) antiarthritic and antidepressant action and leflunomide alone treatment showed significant (p<0.001) antiarthritic activity only as compared to arthritic control. The leflunomide and low dose amitriptyline combination found to be more effective in pain associated depression in rheumatoid arthritic rats


Subject(s)
Animals , Male , Rats , Arthritis , Depression/chemically induced , Antidepressive Agents/analysis , Arthritis, Rheumatoid/classification , Pharmaceutical Preparations/administration & dosage , Antirheumatic Agents/analysis
8.
Adv Rheumatol ; 60: 35, 2020. tab, graf
Article in English | LILACS | ID: biblio-1130787

ABSTRACT

Abstract Background: Duloxetine and amitriptyline are antidepressants used in the treatment of fibromyalgia. In published systematic reviews, there is no agreement about which drug is more effective and safer. This study aimed to compare evidence of the efficacy and safety of duloxetine compared with amitriptyline in the treatment of adult patients with fibromyalgia. This work contributes to guiding clinicians on the use of duloxetine or amitriptyline for the treatment of fibromyalgia and provides information for public health decision-makers. Methods: Overview of systematic reviews of clinical trials comparing duloxetine and amitriptyline in the treatment of fibromyalgia. The reviews were screened in Cochrane, PubMed, EMBASE, and SRDR with no restrictions on language and year of publication, considering that the research was conducted in July 2018 and updated until May 2020. The selection was based on the following criteria: adult patients with a diagnosis of fibromyalgia treated with duloxetine or amitriptyline, comparing the efficacy and safety in pain, fatigue, sleep, and mood disorder symptoms and quality of life, in addition to the acceptability of these antidepressants. The methodological quality and strength of evidence were assessed using the AMSTAR and GRADE instruments. Results: Eight systematic reviews were selected. Amitriptyline had low evidence for pain, moderate evidence for sleep and fatigue, and high evidence for quality of life. Duloxetine had high quality of evidence in patients with mood disorders. With low evidence, duloxetine has higher acceptability, but is safer in older patients, while amitriptyline is safer for non-elderly individuals. Conclusion: Both antidepressants are effective in the treatment of fibromyalgia, differing according to the patient's symptoms and profile. Registration: PROSPERO: CRD42019116101.(AU)


Subject(s)
Humans , Fibromyalgia/drug therapy , Duloxetine Hydrochloride/therapeutic use , Amitriptyline/therapeutic use , Quality of Life , Treatment Outcome
9.
Article | IMSEAR | ID: sea-183635

ABSTRACT

Introduction: Diabetes mellitus frequently leads to development of peripheral neuropathies in almost 30-50% of patients and the most common type of neuropathy associated with this condition is Distal Symmetric Sensorimotor Polyneuropathy (DSPN). Gabapentin and Amitriptyline are two drugs frequently used for the treatment of neuropathic pain associated with type 2 diabetes. Aim of the study: The aim of this study was to compare efficacy and safety of Gabapentin and Amitriptyline in subjects of Type 2 diabetes mellitus with peripheral neuropathic pain. Material and Methods: A prospective, open, randomized, parallel group, comparative study was conducted in 60 patients coming to Department of Medicine, Rajindra Hospital attached to Government Medical College Patiala, to evaluate the efficacy and safety of Gabapentin and Amitriptyline in patients with diabetic peripheral neuropathic pain. The patients fulfilling the inclusion criteria were included in the study after taking written informed consent. The patients were divided into two groups of 30 cases each by simple randomization. Group I patients received Gabapentin 300 mg HS by oral route. Group II patients received Amitriptyline 25 mg HS by oral route. Therapeutic efficacy of both drugs, by using Michigan Neuropathy Screening Instrument (MNSI) was compared at the baseline and at the end of 4 months. Any adverse drug reactions of the respective drug observed in patient were also noted. All the observations thus made were statistically analysed using appropriate tests. Results: Baseline characteristics of the patients in two groups such as age, sex, duration of diabetes were similar (p>0.05). The mean age in group I and group II were 53.40±8.41 years and 57.17±8.55 years, respectively. There was statistically significant reduction in mean MNSI scores in questionnaire part and physical examination part in both the groups. Also, there was statistically significant difference between the two drugs in reducing mean MNSI score. Mean difference between two drugs in reducing MNSI score in history part (0.77±0.16, p<0.01) and physical examination part (0.75±0.19, p<0.01) favoured Gabapentin. No. of adverse drug reactions reported were significantly higher in Amitriptyline group, p value (<0.05) for the difference in ADRs between two drugs was statistically significant. Conclusion: In this study, we concluded that both drugs lead to improvement in signs and symptoms of diabetic neuropathy. Gabapentin was proved to be more efficacious than Amitriptyline. Gabapentin treated patient’s mean MNSI score at the study end point was significantly lower as compared to the Amitriptyline treated patient’s end-point score. Adverse drug reactions reported in our study were mild in both the groups and a significantly higher number of adverse effects were reported in the amitriptyline group. Dizziness and somnolence were two most commonly reported adverse drug reactions.

10.
Article | IMSEAR | ID: sea-200255

ABSTRACT

Background: Pain is one of the most frequent reasons for visiting a doctor. Large-scale studies in Western countries have shown that a fifth of the adult population suffer from chronic pain. Treatment of pain, still a major problem in clinical practice. Despite several available analgesics, unrelieved pain remains a major health care issue. Amitriptyline is a tricyclic antidepressant drug, which is regarded as adjuvant analgesic. There is a common consensus among the researchers on analgesic effect of amitriptyline which is mediated by central pathway but for the peripheral mechanism no conclusive evidence exists till now.Methods: To establish the analgesic mechanism of amitriptyline we tried to evaluate the analgesic activity on different mice models for central (Radiant heat tail flick test and Haffner’s tail clip method) and peripheral analgesia (Writhing test). We also compare the effects of amitriptyline with standard drugs for central and peripheral analgesia.Results: Both in Radiant heat tail flick test and Haffner’s tail clip method we found that the amitriptyline showed significant (p<0.05 to p<0.001) activity as compared to control and diclofenac group. But in comparison to pentazocin group amitriptyline didn’t show significant difference in the reaction time. In acetic acid induced writhing test amitriptyline group mice showed 41.09% reduction in number of writhes as compared to control group. While the standard control (Diclofenac) showed reduction of 65.17% as compared to control. So, amitriptyline showed comparable efficacy towards reduction in number of writhes with that of diclofenac.Conclusions: The results revealed that amitriptyline has significant analgesic activity which is mediated by modulation of both the central and peripheral pathways.

11.
Rev. bras. cir. cardiovasc ; 34(3): 290-296, Jun. 2019. tab, graf
Article in English | LILACS | ID: biblio-1013469

ABSTRACT

Abstract Objective: In this study, we aimed to examine the effects of amitriptyline, fluoxetine, tranylcypromine and venlafaxine on saphenous vein grafts in coronary artery bypass graft surgeries. Methods: 59 patients (40 males and 19 females; mean age 65.1 years, distribution: 45-84 years) who had coronary artery bypass graft surgery between February 2014 and May 2016 were included in the study. After the saphenous vein grafts with intact and denuded endothelium were precontracted with 3×10-6M phenylephrine, amitriptyline, fluoxetine and tranylcypromine were cumulatively added to isolated organ baths in the range of 10-11-3x10-5M, while venlafaxine was added in the range of 10-9-3×10-5M. Then, the antidepressant-induced relaxation responses were recorded isometrically. Results: While the relaxation response of amitriptyline at -6.42 (Log M) was 74.6%, the response at -6.32 (Log M) was 75.5%. While the relaxation response at -6.46 (Log M) of fluoxetine was 68.02%, the response at -6.02 (Log M) was 72.12%. While the relaxation response of tranylcypromine at -7.53 (Log M) was 61.13%, the response at -7.23 (Log M) was 65.53%. While the relaxation response of venlafaxine at -6.21 (Log M) was 29.98%, the response at -5.90 (Log M) was 32.96%. Conclusion: The maximum relaxation at minimum and maximum therapeutic concentrations was obtained with amitriptyline, fluoxetine and tranylcypromine, and the minimum relaxation was obtained with venlafaxine. The relaxation responses were independent of the endothelium.


Subject(s)
Humans , Male , Female , Middle Aged , Aged , Aged, 80 and over , Saphenous Vein/drug effects , Saphenous Vein/transplantation , Tranylcypromine/pharmacology , Fluoxetine/pharmacology , Amitriptyline/pharmacology , Antidepressive Agents/pharmacology , Reference Values , Vasodilation/drug effects , Endothelium, Vascular/drug effects , Coronary Artery Bypass/methods , Analysis of Variance , Transplants/drug effects , Venlafaxine Hydrochloride/pharmacology , Muscle, Smooth, Vascular/drug effects
12.
Chinese Journal of Primary Medicine and Pharmacy ; (12): 2332-2335, 2019.
Article in Chinese | WPRIM | ID: wpr-753790

ABSTRACT

To investigate the clinical effect of amitriptyline combined with Xiaoyao Powder in the treatment of postpartum depression.Methods From January 2018 to February 2018,128 patients with postpartum depression in the Second People's Hospital of Lishui were selected.The patients were randomly divided into observation group and control group according to the digital table ,with 64 cases in each group.The observation group was treated with Chinese and western medicine (amitriptyline combined with Xiaoyao Powder ),and the control group was treated with amitriptyline alone.The self-rating anxiety scale ( SAS),self-rating depression scale (SDS) score,and the concise health survey scale ( SF -36) score before and after treatment were compared between the two groups. Results The SDS scores of the two groups were decreased after treatment (t=4.564,3.656,P=0.012,0.027), and the SDS score of the observation group was lower than that of the control group ,the difference was statistically significant (P=0.035).The SDS scores had no statistically significant difference between the two groups before treatment (P=0.961).The SAS scores in the two groups were decreased after treatment ( t=4.352,3.432,P=0.015,0.029).The SAS score of the observation group was lower than that of the control group ,and the difference was statistically significant (t=3.021,P=0.038).After treatment,the scores of SF -36 in the observation group were significantly increased (all P<0.05),and the comparison of various indicators :emotional function (t=2.951, P=0.048),vitality (t=3.012,P=0.042),mental health (t=3.131,P=0.043),social function (t=2.967,P=0.048),physical pain (3.320,P=0.039),physiological function ( t=3.467,P=0.038),physiological function (t=3.986, P =0.035), overall health ( t =4.045, P =0.021 ), which had statistically significant differences compared with the control group.Conclusion Amitriptyline combined with Xiaoyao Powder in the treatment of postpartum depression can significantly improve the quality of life and improve the anxiety and depressive symptoms of patients,which is better than amitriptyline alone.

13.
Korean Journal of Anesthesiology ; : 60-67, 2019.
Article in English | WPRIM | ID: wpr-759498

ABSTRACT

BACKGROUND: The pain-relief properties of tricyclic antidepressants can be attributed to several actions. Recent observations suggest that adenosine is involved in the antinociceptive effect of amitriptyline. The A3 adenosine receptor (A3AR) is the only adenosine subtype overexpressed in inflammatory and cancer cells. This study was performed to investigate the role of A3AR in the anti-nociceptive effect of amitriptyline. METHODS: Spinal nerve-ligated neuropathic pain was induced by ligating the L5 and L6 spinal nerves of male Sprague-Dawley rats. The neuropathic rats were randomly assigned to one of the following three groups (8 per group): a neuropathic pain with normal saline group, a neuropathic pain with amitriptyline group, and a neuropathic pain with amitriptyline and 3-ethyl-5-benzyl- 2-methyl-4-phenylethynyl-6-phenyl-1,4-(±)-dihydropyridine-3,5-dicarboxylate (MRS) group. Amitriptyline or saline was administered intraperitoneally and 3-ethyl-5-benzyl-2-methyl-4-phenylethynyl-6-phenyl-1,4-(±)-dihydropyridine-3,5-dicarboxylate (MRS-1191), an A3AR antagonist, was injected subcutaneously immediately before amitriptyline administration. The level of extracellular signal-regulated kinase P44/42 (ERK1/2), cyclic AMP response element-binding protein (CREB), and proinflammatory cytokines were assessed using immunoblotting or reverse-transciption polymerase chain reaction. RESULTS: Amitriptyline increased the mechanical withdrawal threshold of the neuropathic rats. The level of phospho-ERK1/2 and phospho-CREB proteins, and proinflammatory cytokines produced by spinal nerve ligation were significantly reduced by amitriptyline administration. However, the use of MRS-1191 before amitriptyline administration not only reduced the threshold of mechanical allodynia, but also increased the signaling protein and proinflammatory cytokine levels, which were reduced by amitriptyline. CONCLUSIONS: The results of this study suggest that the anti-nociceptive effect of amitriptyline involves the suppression of ERK1/2 and CREB signaling proteins, and A3AR activation also affects the alleviation of the inflammatory response.


Subject(s)
Animals , Humans , Male , Rats , Adenosine , Amitriptyline , Antidepressive Agents, Tricyclic , Cyclic AMP Response Element-Binding Protein , Cytokines , Hyperalgesia , Immunoblotting , Ligation , Neuralgia , Phosphotransferases , Polymerase Chain Reaction , Rats, Sprague-Dawley , Receptors, Purinergic P1 , Spinal Nerves
14.
Chinese Journal of Primary Medicine and Pharmacy ; (12): 2332-2335, 2019.
Article in Chinese | WPRIM | ID: wpr-803040

ABSTRACT

Objective@#To investigate the clinical effect of amitriptyline combined with Xiaoyao Powder in the treatment of postpartum depression.@*Methods@#From January 2018 to February 2018, 128 patients with postpartum depression in the Second People's Hospital of Lishui were selected.The patients were randomly divided into observation group and control group according to the digital table, with 64 cases in each group.The observation group was treated with Chinese and western medicine (amitriptyline combined with Xiaoyao Powder), and the control group was treated with amitriptyline alone.The self-rating anxiety scale (SAS), self-rating depression scale (SDS) score, and the concise health survey scale (SF-36) score before and after treatment were compared between the two groups.@*Results@#The SDS scores of the two groups were decreased after treatment (t=4.564, 3.656, P=0.012, 0.027), and the SDS score of the observation group was lower than that of the control group, the difference was statistically significant (P=0.035). The SDS scores had no statistically significant difference between the two groups before treatment (P=0.961). The SAS scores in the two groups were decreased after treatment (t=4.352, 3.432, P=0.015, 0.029). The SAS score of the observation group was lower than that of the control group, and the difference was statistically significant (t=3.021, P=0.038). After treatment, the scores of SF-36 in the observation group were significantly increased (all P<0.05), and the comparison of various indicators: emotional function (t=2.951, P=0.048), vitality (t=3.012, P=0.042), mental health (t=3.131, P=0.043), social function (t=2.967, P=0.048), physical pain (3.320, P=0.039), physiological function (t=3.467, P=0.038), physiological function (t=3.986, P=0.035), overall health (t=4.045, P=0.021), which had statistically significant differences compared with the control group.@*Conclusion@#Amitriptyline combined with Xiaoyao Powder in the treatment of postpartum depression can significantly improve the quality of life and improve the anxiety and depressive symptoms of patients, which is better than amitriptyline alone.

15.
Chinese Journal of Anesthesiology ; (12): 578-581, 2019.
Article in Chinese | WPRIM | ID: wpr-755609

ABSTRACT

Objective To evaluate the effect of amitriptyline on the phosphorylation of histone deacetylase 5 (HDAC5) in the basolateral amygdala (BLA) of rats with neuropathic pain.Methods Thirty healthy male Wistar rats,weighing 250-300 g,were divided into 3 groups (n=10 each) using a random number table method:sham operation group (S group),neuropathic pain group (NP group) and amitriptyline group (A group).Spared nerve injury was produced by exposing the sciatic nerve and its branches and ligation and transection of tibial nerve and common fibular nerve in anesthetized rats.Amitriptyline 10 mg/kg was intraperitoneally injected every day on 14-35 days after establishing the model in group A,while the equal volume of normal saline was given instead of amitriptyline in S and NP groups.The mechanical paw withdrawal threshold (MWT) was measured on 3,7,14,21,28 and 35 days after establishing the model in each group.The forced swimming test was performed on day 36 after establishing the model,and immobility time,climbing time and swimming time were recorded.The rats were then sacrificed,and brain tissues in BLA were obtained for determination of the expression of HDAC5 and phosphorylated HDAC5 (p-HDAC5) (by Western blot) and expressionof HDAC5 mRNA (by real-time quantitative polymerase chain reaction).Results Compared with group S,the MWT was significantly decreased at each time point,the immobility time was prolonged,and the swimming time and climbing time were shortened in group NP,and the MWT was significantly decreased on days 14,21 and 28 after establishing the model,the expression of p-HDAC5 was down-regulated,and the expression of HDAC5 mRNA was up-regulated in group A (P<0.05).Compared with group NP,the MWT was significantly increased on days 21,28 and 35 after establishing the model,the immobility time was shortened,the climbing time was prolonged,the expression of p-HDAC5 was up-regulated,and the expression of HDAC5 mRNA was down-regulated in group A (P<0.05or 0.01).Conclusion The mechanism by which amitriptyline improves depression is associated with promoting the phosphorylation of HDAC5 in BLA of rats with NP.

16.
Article | IMSEAR | ID: sea-194007

ABSTRACT

Background: Painful diabetic neuropathy is a common complication of long standing diabetes mellitus. Amitriptyline is commonly used to treat painful diabetic neuropathy. Pregabalin has been shown to be effective in the treatment of painful diabetic neuropathy with lesser adverse effects. Sustained release (SR) of pregabalin has the advantage of once daily dosing and a better patient compliance. Hence, this study was planned to compare the efficacy and safety of pregabalin-SR with amitriptyline in painful diabetic neuropathy.Methods: It is a prospective, open labelled, randomized controlled study. A total of 80 patients diagnosed with painful diabetic neuropathy based on Diabetic neuropathy symptom score and Michigan neuropathy screening instrument, were randomized into two groups to receive amitriptyline and pregabalin SR. Amitriptyline was started at 25mg OD and pregabalin SR 75mg OD for 6 weeks with optional dose titration. Patients were assessed for pain relief by using visual analogue scale and an overall improvement in their general condition by patient’s global impression of change scale. Adverse drug reactions were recorded on each follow up.Results: All patients had significant improvement in pain relief in both the treatment groups. The median VAS (visual analogue scale) score was slightly higher in pregabalin SR group (25 vs 22) however it was not statistically significant. Intergroup comparison did not show any significant differences between the treatment groups. Good and moderate pain relief were noted in 37(92.5%) and 3(7.5%) patients on amitriptyline and 36 (90%) and 4 (10%) patients on pregabalin SR respectively. The common adverse effects reported in amitriptyline group were drowsiness (27.5%) and dry mouth (17.5%) and in pregabalin-SR group were drowsiness (15%) and dizziness (5%). No serious adverse event was reported in either of the groups.Conclusions: In patients with painful diabetic neuropathy both amitriptyline and pregabalin-SR are equally effective in alleviating pain and improving the patient’s general condition, but pregabalin-SR has the advantage of fewer adverse effects and convenient dosage timing.

17.
Arq. neuropsiquiatr ; 76(4): 213-218, Apr. 2018. tab, graf
Article in English | LILACS | ID: biblio-888380

ABSTRACT

ABSTRACT Objectives: Nonpharmacological treatments, such as the Nociceptive Trigeminal Inhibition Tension Suppression System (NTI-tss), are approved for migraine prophylaxis. We aimed at evaluating the effectiveness of the NTI-tss and to compare its efficacy with amitriptyline and with a sham intraoral device in the preventive treatment of migraine. Methods: Consecutive patients with migraine were randomized to receive 25 mg of amitriptyline/day (n = 34), NTI-tss (n = 33) and a non-occlusal splint (n = 30). The headache frequency was evaluated at six and 12 weeks. Results: The amitriptyline group showed, respectively, 60% and 64% reduction in attack frequency at six and 12 weeks (P = 0.000). In the NTI-tss and non-occlusal splint groups, reduction was 39% and 30%, respectively, at six weeks and 48% for both groups at 12 weeks. Conclusions: Amitriptyline proved superior to the NTI-tss and the non-occlusal splint. Despite its approval by the United States Food and Drug Administration, the NTI-tss was not superior to a sham device.


RESUMO Objetivo: Tratamentos não farmacológicos como o Nociceptive Trigeminal Inhibition Tension Suppression System (NTI-tss), são aprovados para a prevenção da migrânea. Avaliamos a eficácia do NTI-tss no tratamento preventivo da migrânea e comparamos sua eficácia com a de um medicamento tradicional (amitriptilina) e com um dispositivo intraoral que não interfere com a oclusão (placa palatina). Métodos: Pacientes consecutivos com migrânea foram randomizados e receberam 25mg de amitriptilina/dia (n = 34), NTI-tss (n = 33) ou placa palatina não oclusal (n = 30). A frequência da cefaleia foi comparada após seis e 12 semanas. Resultados: No grupo da amitriptilina houve redução de 60% em seis semanas e de 64% em 12 semanas (P = 0.000). Nos grupos do NTI-tss e da placa não oclusal a redução foi respectivamente de 39% e 30% após seis semanas, e de 48% para ambos em 12 semanas. Conclusões: Amitriptilina foi superior ao NTI-tss e à placa palatina no tratamento da migrânea sem aura. O NTI-tss obteve resultados similares aos da placa não oclusal.


Subject(s)
Humans , Male , Female , Adult , Occlusal Splints , Analgesics, Non-Narcotic/therapeutic use , Amitriptyline/therapeutic use , Migraine Disorders/prevention & control , Treatment Outcome
18.
Article | IMSEAR | ID: sea-199579

ABSTRACT

Background: Several generations of antidepressant medication which act by distinct pharmacological mechanisms have been introduced for the treatment of depression; tricyclic antidepressants (TCAs) were first line of treatment for many years. However, over the last decade, selective serotonin reuptake inhibitors (SSRIs) have displaced TCAs, mainly because of better side effect profile. There are no references in literature on comparison of efficacy of TCAs and SSRIs in Nepalese population. This study attempted to compare the efficacy of amitriptyline, a reference standard TCA with escitalopram, a newer SSRI in Nepalese population.Methods: An open level, randomised, prospective study was conducted for one year duration. Eighty outpatients suffering from major depression who met inclusion and exclusion criteria were randomly assigned to either amitriptyline or escitalopram group for four week study. Seventy one patients (amitriptyline N: 36, escitalopram N: 35) completed the study. Hamilton Depression Rating Scale (HDRS) was used to measure the antidepressant effect. Antidepressant efficacy was evaluated on reduction of HDRS score before and after therapy (End of four weeks).Results: In amitriptyline group, mean percentage reduction in HDRS score was 58.29% (13.5 points), while in escitalopram group was 60.78% (14.03 points). Both the drugs significantly improved the HDRS score at the end of the study (p<0.05). On intergroup comparison, antidepressant efficacy of amitriptyline and escitalopram did not differ significantly from each other (p>0.05).Conclusions: This study suggests that escitalopram is effective in the treatment of depression and its efficacy appears to be comparable to amitriptyline at the end of four weeks.

19.
The Korean Journal of Physiology and Pharmacology ; : 585-595, 2018.
Article in English | WPRIM | ID: wpr-727865

ABSTRACT

Amitriptyline, a tricyclic antidepressant, is commonly used to treat depression and neuropathic pain, but its mechanism is still unclear. We tested the effect of amitriptyline on 5-hydroxytryptamine 3 (5-HT₃) receptor currents and studied its blocking mechanism because the clinical applications of amitriptyline overlapped with 5-HT₃ receptor therapeutic potentials. Using a whole-cell voltage clamp method, we recorded the currents of the 5-HT₃ receptor when 5-HT was applied alone or co-applied with amitriptyline in cultured NCB-20 neuroblastoma cells known to express 5-HT₃ receptors. To elucidate the mechanism of amitriptyline, we simulated the 5-HT₃ receptor currents using Berkeley Madonna® software and calculated the rate constants of the agonist binding and receptor transition steps. The 5-HT₃ receptor currents were inhibited by amitriptyline in a concentration-dependent, voltage-independent manner, and a competitive mode. Amitriptyline accelerated the desensitization of the 5-HT₃ receptor. When amitriptyline was applied before 5-HT treatment, the currents rose slowly until the end of 5-HT treatment. When amitriptyline was co-applied with 5-HT, currents rose and decayed rapidly. Peak current amplitudes were decreased in both applications. All macroscopic currents recorded in whole cell voltage clamping experiments were reproduced by simulation and the changes of rate constants by amitriptyline were correlated with macroscopic current recording data. These results suggest that amitriptyline blocks the 5-HT₃ receptor by close and open state blocking mechanisms, in a competitive manner. We could expand an understanding of pharmacological mechanisms of amitriptyline related to the modulation of a 5-HT₃ receptor, a potential target of neurologic and psychiatric diseases through this study.


Subject(s)
Amitriptyline , Constriction , Depression , Methods , Neuralgia , Neuroblastoma , Serotonin
20.
Chinese Journal of Primary Medicine and Pharmacy ; (12): 1052-1055, 2018.
Article in Chinese | WPRIM | ID: wpr-701889

ABSTRACT

Objective To observe and analyze the clinical efficacy of amitriptyline combined with domperidone in the treatment of functional dyspepsia ( FD) .Methods 156 patients with FD were selected as the study subjects , and they were randomly divided into the observation group and the control group ,78 cases in each group .The patients in the control group were treated with domperidone ,and the patients in the observation group were given amitriptyline combined with domperidone .The changes of clinical symptoms scores and the occurrence of adverse reactions were observed before and after treatment in both two groups ,and the clinical curative effect was compared .Results After treatment,the total effective rate of the observation group was 93.59%,which was significantly higher than 76.92%of the control group,and there was significant difference between the two groups (χ2 =10.59,P<0.01).The early satiety,postprandial bloating,nausea and vomiting,epigastric distending pain,belching and other clinical symptoms scores in two groups were significantly reduced ( tobservation group =21.95,33.78,42.12,37.58,42.64, tcontrol group =17.54,8.88,16.43,10.98,15.06,all P<0.01),and the clinical symptoms of the observation group improved more significantly (t=9.89,9.79,8.47,9.99,18.52,all P<0.01).The incidence rate of adverse reactions in the obser-vation group was 16.67%,which in the control group was 23.08%,the difference between the two groups was not statistically significant (χ2 =1.09,P>0.05).After the treatment,the adverse reactions disappeared spontaneously . Conclusion Compared with the use of domperidone alone , the clinical efficacy of amitriptyline combined with domperidone in the treatment of FD patients is significant with good safety ,and is conducive to improve the clinical symptoms of patients ,increase the efficacy and worthy of clinical application .

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