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1.
Molecules ; 29(9)2024 May 04.
Artículo en Inglés | MEDLINE | ID: mdl-38731631

RESUMEN

The participation of butyrylcholinesterase (BChE) in the degradation of atropine has been recurrently addressed for more than 70 years. However, no conclusive answer has been provided for the human enzyme so far. In the present work, a steady-state kinetic analysis performed by spectrophotometry showed that highly purified human plasma BChE tetramer slowly hydrolyzes atropine at pH 7.0 and 25 °C. The affinity of atropine for the enzyme is weak, and the observed kinetic rates versus the atropine concentration was of the first order: the maximum atropine concentration in essays was much less than Km. Thus, the bimolecular rate constant was found to be kcat/Km = 7.7 × 104 M-1 min-1. Rough estimates of catalytic parameters provided slow kcat < 40 min-1 and high Km = 0.3-3.3 mM. Then, using a specific organophosphoryl agent, echothiophate, the time-dependent irreversible inhibition profiles of BChE for hydrolysis of atropine and the standard substrate butyrylthiocholine (BTC) were investigated. This established that both substrates are hydrolyzed at the same site, i.e., S198, as for all substrates of this enzyme. Lastly, molecular docking provided evidence that both atropine isomers bind to the active center of BChE. However, free energy perturbations yielded by the Bennett Acceptance Ratio method suggest that the L-atropine isomer is the most reactive enantiomer. In conclusion, the results provided evidence that plasma BChE slowly hydrolyzes atropine but should have no significant role in its metabolism under current conditions of medical use and even under administration of the highest possible doses of this antimuscarinic drug.


Asunto(s)
Atropina , Butirilcolinesterasa , Simulación del Acoplamiento Molecular , Butirilcolinesterasa/química , Butirilcolinesterasa/metabolismo , Butirilcolinesterasa/sangre , Atropina/química , Atropina/metabolismo , Humanos , Cinética , Hidrólisis , Modelos Moleculares
2.
Harefuah ; 163(5): 278-285, 2024 May.
Artículo en Hebreo | MEDLINE | ID: mdl-38734939

RESUMEN

INTRODUCTION: The importance of myopia management lies in the desire to minimize the potential ocular risks that increase with high myopia. AIMS: To assess the decrease in myopia progression using topical low dose atropine combined with peripheral blur contact lenses (CL). METHODS: This retrospective review study included 25 children between the ages of 8.5 years to 14 years. The children all had a minimal increase in myopia of 0.75D during the year prior to treatment. The children were divided into two groups. The control group included 14 children who wore single-vision spectacles )SV) averaging 3.20±0.9D ranging from 1.5-5.3D. The study group included 11 children who wore dual-focus CL, with an average prescription of 3.4±0.7D ranging from 2.5 to 4.3D, for one year. At that point, when an additional myopia increase was observed, the children were additionally treated with topical 0.01% atropine for two years (CL+A0.01). RESULTS: There was an increase in myopia in the SV group of 1.12±0.52D, 1.08±0.56D and 0.96±0.53D in the first, second, and third years, respectively. The myopia increase in the CL+A0.01 group was 0.57±0.48D, 0.14±0.34D, and 0.17±0.29D in the first, second, and third years, respectively. CONCLUSIONS: Low-dose atropine combined with peripheral blur contact lenses was effective in decreasing myopia progression in this study. Additional, larger-scale studies are required in the future. DISCUSSION: This study found a significant decrease in myopia progression in the second and third years of treatment. The CL group showed less effectivity than the CL+A0.01 group.


Asunto(s)
Atropina , Lentes de Contacto , Progresión de la Enfermedad , Miopía , Humanos , Atropina/administración & dosificación , Niño , Miopía/terapia , Miopía/fisiopatología , Estudios Retrospectivos , Adolescente , Masculino , Femenino , Resultado del Tratamiento , Midriáticos/administración & dosificación , Soluciones Oftálmicas/administración & dosificación , Anteojos
3.
BMC Anesthesiol ; 24(1): 123, 2024 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-38561654

RESUMEN

BACKGROUND: Glycopyrrolate-neostigmine (G/N) for reversing neuromuscular blockade (NMB) causes fewer changes in heart rate (HR) than atropine-neostigmine (A/N). This advantage may be especially beneficial for elderly patients. Therefore, this study aimed to compare the cardiovascular effects of G/N and A/N for the reversal of NMB in elderly patients. METHODS: Elderly patients aged 65-80 years who were scheduled for elective non-cardiac surgery under general anesthesia were randomly assigned to the glycopyrrolate group (group G) or the atropine group (group A). Following the last administration of muscle relaxants for more than 30 min, group G received 4 ug/kg glycopyrrolate and 20 ug/kg neostigmine, while group A received 10 ug/kg atropine and 20 ug/kg neostigmine. HR, mean arterial pressure (MAP), and ST segment in lead II (ST-II) were measured 1 min before administration and 1-15 min after administration. RESULTS: HR was significantly lower in group G compared to group A at 2-8 min after administration (P < 0.05). MAP was significantly lower in group G compared to group A at 1-4 min after administration (P < 0.05). ST-II was significantly depressed in group A compared to group G at 2, 3, 4, 5, 6, 7, 8, 9, 11, 13, 14, and 15 min after administration (P < 0.05). CONCLUSIONS: In comparison to A/N, G/N for reversing residual NMB in the elderly has a more stable HR, MAP, and ST-II within 15 min after administration.


Asunto(s)
Sistema Cardiovascular , Retraso en el Despertar Posanestésico , Bloqueo Neuromuscular , Anciano , Humanos , Neostigmina/farmacología , Glicopirrolato , Atropina/farmacología
4.
Int J Clin Pharmacol Ther ; 62(6): 267-277, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38577753

RESUMEN

OBJECTIVES: To describe the efficacy of atropine in controlling salivary flow in patients with sialorrhea or drooling. MATERIALS AND METHODS: We included randomized controlled studies, quasi-randomized trials, case reports, clinical trials, systematic reviews, and meta-analyses assessing the use of atropine in patients with sialorrhea or drooling. The endpoints were reduction in salivary flow rate, amount of saliva secreted, reduction in clinical symptoms of sialorrhea, death rattle intensity, or reduction in drooling intensity as measured by an objective scale such as the drooling intensity scale. RESULTS: A total of 56 studies with 2,378 patients were included in the systematic review. The underlying disease states included brain injury, amyotrophic lateral sclerosis, cerebral palsy, clozapine- and perphenazine-induced sialorrhea, Parkinson's disease, and terminal illness. The routes of atropine administration included sublingual, intravenous, subcutaneous, oral tablet or solution, and direct injection of atropine into parotid glands or at the base of the tongue. The generalized estimated equation regression models showed that sublingual administration is superior to oral and subcutaneous routes. CONCLUSION: Atropine is efficacious in managing sialorrhea in most disease states. Sublingual administration of atropine is superior to other routes of administration in reducing salivary flow in patients with sialorrhea.


Asunto(s)
Atropina , Sialorrea , Sialorrea/tratamiento farmacológico , Humanos , Atropina/uso terapéutico , Resultado del Tratamiento , Salivación/efectos de los fármacos
5.
Transl Vis Sci Technol ; 13(4): 22, 2024 Apr 02.
Artículo en Inglés | MEDLINE | ID: mdl-38625083

RESUMEN

Purpose: To evaluate the effect of low-concentration (0.01% and 0.05%) atropine eyedrops on ocular surface characteristics in young adults. Methods: Twenty-six myopic students aged 18 to 30 years were randomly assigned to receive either 0.01% or 0.05% atropine once nightly for 14 days, followed by cessation, with a ≥14-day interval between each administration. Assessments were conducted one, two, seven, and 14 days after using atropine with corresponding timepoints after atropine cessation. Tear meniscus height and first and average noninvasive keratograph tear film breakup time (NIKBUT-first, NIKBUT-average) were measured using Keratograph 5M, whereas the objective scatter index (OSI) was measured by OQAS II devices; the ocular surface disease index (OSDI) score was also obtained. Results: The mean OSI peaked after two days of administration of 0.05% atropine (ß = 0.51, P = 0.001), accompanied by significant decreases in NIKBUT-first (ß = -7.73, P < 0.001) and NIKBUT-average (ß = -8.10, P < 0.001); the OSDI peaked after 14 days (ß = 15.41, P < 0.001). The above parameters returned to baseline one week after atropine discontinuation (all P > 0.05). NIKBUT-first and NIKBUT-average reached their lowest points after 14 days of 0.01% atropine administration (NIKBUT-first: ß = -4.46, P = 0.005; NIKBUT-average: ß = -4.42, P = 0.001), but those significant changes were diminished once atropine treatment stopped. Conclusions: Young adult myopes experienced a significant but temporary impact on the ocular surface with 0.05% atropine administration, whereas 0.01% atropine had a minimal effect. Translational Relevance: The investigation of the ocular surface effects of different concentrations of atropine may inform evidence-based clinical decisions regarding myopia control in young adults.


Asunto(s)
Ojo , Miopía , Humanos , Adulto Joven , Atropina , Miopía/tratamiento farmacológico , Soluciones Oftálmicas
6.
Physiol Behav ; 280: 114564, 2024 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-38657747

RESUMEN

Although salivation is essential during eating behavior, little is known about the brainstem centers that directly control the salivary glands. With regard to the inferior salivatory nucleus (ISN), the site of origin of the parasympathetic preganglionic cell bodies that innervate the parotid glands, previous anatomical studies have located it within the rostrodorsal medullary reticular formation. However, to date there is no functional data that shows the secretory nature of the somas grouped in this region. To activate only the somas and rule out the activation of the efferent fibers from and the afferent fibers to the ISN, in exp. 1, NMDA neurotoxin was administered to the rostrodorsal medullary region and the secretion of saliva was recorded during the following hour. Results showed an increased secretion of parotid saliva but a total absence of submandibular-sublingual secretion. In exp. 2, results showed that the hypersecretion of parotid saliva after NMDA microinjection was completely blocked by the administration of atropine (a cholinergic blocker) but not after administration of dihydroergotamine plus propranolol (α and ß-adrenergic blockers, respectively). These findings suggest that the somata of the rostrodorsal medulla are secretory in nature, controlling parotid secretion via a cholinergic pathway. The data thus functionally supports the idea that these cells constitute the ISN.


Asunto(s)
N-Metilaspartato , Glándula Parótida , Receptores de N-Metil-D-Aspartato , Animales , Masculino , Ratas , Glándula Parótida/metabolismo , Glándula Parótida/efectos de los fármacos , Receptores de N-Metil-D-Aspartato/metabolismo , N-Metilaspartato/farmacología , N-Metilaspartato/metabolismo , Ratas Wistar , Salivación/efectos de los fármacos , Salivación/fisiología , Bulbo Raquídeo/metabolismo , Bulbo Raquídeo/efectos de los fármacos , Saliva/metabolismo , Agonistas de Aminoácidos Excitadores/farmacología , Atropina/farmacología , Propranolol/farmacología , Antagonistas Adrenérgicos beta/farmacología , Microinyecciones , Sialorrea
7.
Food Chem Toxicol ; 186: 114589, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38467298

RESUMEN

Tropane alkaloids (TA) are natural toxins found in certain plants, including cereals, of which atropine and scopolamine are the main species of concern due to their acute toxicity. This study aimed to determine the occurrence of TA in cereal foods and assess the potential health risks associated with their consumption in Korea. TA levels were analyzed in 80 raw and 71 processed cereal samples, which were distributed throughout Korea in 2021, using ultra-performance liquid chromatography-tandem mass spectrometry. At least one of the six TA species, namely atropine, scopolamine, pseudotropine, tropinone, scopine, and 6-hydroxytropinone, was detected in 10 out of the 151 samples at levels ranging from 0.12 to 88.10 µg kg-1. Dietary exposure (mean, 0.23 ng kg-1 bw day-1) to atropine and scopolamine in the Korean population was estimated to be low across all age groups. This is despite considering worst-case scenarios using the total concentrations of atropine and scopolamine in a millet sample, both of which were detected, and 95th percentile consumption for consumers of millet only. Both the hazard index and margin of exposure methods indicated that the current levels of TA exposure from millet consumption were unlikely to pose significant health risks to the Korean population.


Asunto(s)
Grano Comestible , Tropanos , Atropina , Grano Comestible/química , República de Corea , Medición de Riesgo , Escopolamina/toxicidad , Tropanos/análisis , Tropanos/química , Alcaloides/análisis , Alcaloides/química
8.
Dig Dis Sci ; 69(4): 1156-1168, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38448762

RESUMEN

BACKGROUND/AIMS: We examined the involvement of cholecystokinin (CCK) in the exacerbation of indomethacin (IND)-induced gastric antral ulcers by gastroparesis caused by atropine or dopamine in mice. METHODS: Male mice were fed for 2 h (re-feeding) following a 22-h fast. Indomethacin (IND; 10 mg/kg, s.c.) was administered after re-feeding; gastric lesions were examined 24 h after IND treatment. In another experiment, mice were fed for 2 h after a 22-h fast, after which the stomachs were removed 1.5 h after the end of the feeding period. Antral lesions, the amount of gastric contents, and the gastric luminal bile acids concentration were measured with or without the administration of the pro- and antimotility drugs CCK-octapeptide (CCK-8), atropine, dopamine, SR57227 (5-HT3 receptor agonist), apomorphine, lorglumide (CCK1 receptor antagonist), ondansetron, and haloperidol alone and in combination. RESULTS: IND produced severe lesions only in the gastric antrum in re-fed mice. CCK-8, atropine, dopamine, SR57227 and apomorphine administered just after re-feeding increased bile reflux and worsened IND-induced antral lesions. These effects were significantly prevented by pretreatment with lorglumide. Although atropine and dopamine also increased the amount of gastric content, lorglumide had no effect on the delayed gastric emptying provoked by atropine and dopamine. Both ondansetron and haloperidol significantly inhibited the increase of bile reflux and the exacerbation of antral lesions induced by atropine and dopamine, respectively, but did not affect the effects of CCK-8. CONCLUSIONS: These results suggest that CCK-CCK1 receptor signal increases bile reflux during gastroparesis induced by atropine and dopamine, exacerbating IND-induced antral ulcers.


Asunto(s)
Reflujo Biliar , Gastroparesia , Úlcera Gástrica , Ratones , Masculino , Animales , Indometacina , Úlcera , Receptor de Colecistoquinina A , Sincalida/efectos adversos , Apomorfina/efectos adversos , Dopamina , Haloperidol/efectos adversos , Ondansetrón , Úlcera Gástrica/inducido químicamente , Colecistoquinina/efectos adversos , Receptores de Colecistoquinina , Atropina/efectos adversos
9.
Planta Med ; 90(6): 426-439, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38452806

RESUMEN

Plants are an incredible source of metabolites showing a wide range of biological activities. Among these, there are the alkaloids, which have been exploited for medical purposes since ancient times. Nowadays, many plant-derived alkaloids are the main components of drugs used as therapy for different human diseases. This review deals with providing an overview of the alkaloids used to treat eye diseases, describing the historical outline, the plants from which they are extracted, and the clinical and molecular data supporting their therapeutic activity. Among the different alkaloids that have found application in medicine so far, atropine and pilocarpine are the most characterized ones. Conversely, caffeine and berberine have been proposed for the treatment of different eye disorders, but further studies are still necessary to fully understand their clinical value. Lastly, the alkaloid used for managing hypertension, reserpine, has been recently identified as a potential drug for ameliorating retinal disorders. Other important aspects discussed in this review are different solutions for alkaloid production. Given that the industrial production of many of the plant-derived alkaloids still relies on extraction from plants, and the chemical synthesis can be highly expensive and poorly efficient, alternative methods need to be found. Biotechnologies offer a multitude of possibilities to overcome these issues, spanning from genetic engineering to synthetic biology for microorganisms and bioreactors for plant cell cultures. However, further efforts are needed to completely satisfy the pharmaceutical demand.


Asunto(s)
Alcaloides , Oftalmopatías , Humanos , Alcaloides/farmacología , Alcaloides/aislamiento & purificación , Alcaloides/química , Oftalmopatías/tratamiento farmacológico , Atropina/farmacología , Pilocarpina , Plantas Medicinales/química , Cafeína/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Reserpina/farmacología
10.
J Pharm Biomed Anal ; 243: 116029, 2024 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-38457866

RESUMEN

Atropine (ATR) intoxication is a recurrent case in emergency departments. The diagnosis is dependent on clinical evaluation and is supported by analytical assessment. The assay is limited by the rapid degradation/metabolism of ATR into TRP as well as the preanalytical factors impairing correct detection and diagnosis. In this study, an HPLC-MS/MS method was optimized for the simultaneous determination of ATR and TRP. The effect of analytical matrix and the impact of blood-collection tube type on the ATR analytical signal were investigated. Separation was achieved using water: 0.01% formic acid acidified methanol (40: 60, v/v) as a mobile phase and Inertsil® C18 column (5 µm; 4.6*150 mm) as a stationary phase. The retention-times were 2.6 and 6.5 min for ATR and TRP, respectively. A chromatographic shift (0.4 min) in ATR peak, but not TRP, was observed in biological samples from neat ones. The best analytical signal was observed when heparinized blood collection tubes were employed. The method was linear, accurate and precise in the ATR toxicity range enabling the detection of ATR intoxication down to a concentration of 0.1 ng/mL by applying a simple sample clean-up procedure. In conclusion, an HPLC-MS/MS method for the simultaneous determination of ATR and TRP is presented. The method highlights the chromatographic shift of ATR peak in biological samples that may induce false-negative detection and poses TRP as an alternative toxicological marker for ATR toxicity. Meanwhile the study recommends heparin tubes for blood-sample collection.


Asunto(s)
Cromatografía Líquida con Espectrometría de Masas , Espectrometría de Masas en Tándem , Cromatografía Liquida/métodos , Espectrometría de Masas en Tándem/métodos , Atropina , Reproducibilidad de los Resultados , Cromatografía Líquida de Alta Presión/métodos
11.
Optom Vis Sci ; 101(3): 134-142, 2024 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-38546754

RESUMEN

SIGNIFICANCE: The availability of a range of effective myopia control modalities enables the clinician to exercise judgment when discussing the treatment plan with the patient and their parents. This article outlines important considerations beyond efficacy.Clinically meaningful myopia control may be attained with some spectacle lenses, select soft contact lenses, some concentrations of atropine, and overnight orthokeratology. Given that satisfactory efficacy can be achieved with a range of modalities, other factors should be considered when deciding upon the best intervention for a given child. Four key factors-compliance, quality of vision, quality of life, and safety-are discussed in this review. Compliance directly impacts efficacy regardless of the modality and is the most important consideration, as it is influenced by quality of vision and comfort. Daily disposal myopia control contact lenses and overnight orthokeratology are generally associated with high compliance, provide better vision-related quality of life than spectacles, and carry a very low risk when used appropriately. A further benefit of overnight orthokeratology is the elimination of a need for optical correction during the day.


Asunto(s)
Lentes de Contacto Hidrofílicos , Miopía , Niño , Humanos , Calidad de Vida , Miopía/terapia , Atropina , Ejercicio Físico
12.
Hipertens. riesgo vasc ; 41(1): 58-61, Ene-Mar, 2024. ilus
Artículo en Inglés | IBECS | ID: ibc-231667

RESUMEN

Atropine, a competitive antagonist of acetylcholine muscarinic receptors, is commonly used to treat severe bradycardia by blocking parasympathetic activity. We present a rare case of hypertensive emergency following atropine administration, with only one previous report in the literature. A 78-year-old woman with essential hypertension and hypercholesterolemia was admitted to the cardiac intensive care unit for non-ST segment elevation myocardial infarction. During coronary angiography, an occlusion of the right coronary artery was identified. While removing the diagnostic catheter through the right radial artery, the patient experienced intense pain and discomfort, accompanied by a vasovagal reflex characterized by bradycardia and hypotension. Intravenous atropine (0.5mg) was administered, leading to a rapid rise in heart rate with frequent ventricular ectopy. Subsequently, a progressive and exaggerated elevation in arterial blood pressure occurred, peaking at 294/121mmHg approximately 10min after atropine administration. The patient developed hypertensive acute pulmonary edema, successfully treated with intravenous nitroglycerine (10mg) and furosemide (60mg). Blood pressure normalized after approximately 14min. The exact mechanism of atropine-induced hypertensive emergency remains unknown. While hypertensive emergencies with atropine are exceedingly rare, healthcare professionals should be aware of this potential effect and be prepared for prompt intervention.(AU)


La atropina, un antagonista competitivo de los receptores muscarínicos de acetilcolina, se utiliza comúnmente para tratar la bradicardia severa al bloquear la actividad parasimpática. Presentamos un caso raro de emergencia hipertensiva después de la administración de atropina, con solo un informe previo en la literatura. Una mujer de 78 años con hipertensión esencial e hipercolesterolemia fue ingresada en la unidad de cuidados intensivos cardíacos por infarto agudo de miocardio sin elevación del segmento ST. Durante la angiografía coronaria, se identificó una oclusión de la arteria coronaria derecha. Mientras se retiraba el catéter diagnóstico a través de la arteria radial derecha, la paciente experimentó un intenso dolor y malestar, acompañado de un reflejo vasovagal caracterizado por bradicardia e hipotensión. Se administró atropina intravenosa (0,5 mg), lo que provocó un rápido aumento de la frecuencia cardíaca con frecuente ectopia ventricular. Posteriormente, ocurrió una elevación progresiva y exagerada de la presión arterial, alcanzando un máximo de 294/121 mmHg aproximadamente 10 minutos después de la administración de atropina. La paciente desarrolló edema pulmonar agudo hipertensivo, tratado con éxito con nitroglicerina intravenosa (10 mg) y furosemida (60 mg). La presión arterial se normalizó después de aproximadamente 14 minutos. El mecanismo exacto de la emergencia hipertensiva inducida por atropina sigue siendo desconocido. Aunque las emergencias hipertensivas con atropina son excepcionalmente raras, los profesionales de la salud deben estar al tanto de este efecto potencial y estar preparados para intervenir rápidamente.(AU)


Asunto(s)
Humanos , Femenino , Anciano , Atropina/administración & dosificación , Atropina/efectos adversos , Bradicardia , Hipercolesterolemia , Angiografía Coronaria , Efectos Colaterales y Reacciones Adversas Relacionados con Medicamentos , Pacientes Internos , Examen Físico , Hipertensión , Presión Arterial
13.
Eur Rev Med Pharmacol Sci ; 28(5): 2068-2083, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38497888

RESUMEN

OBJECTIVE: Methyl-2-(4-chloro- phenyl)-5-benzoxazoleacetate (MCBA), a synthetic benzoxazole derivative with established antipsoriatic efficacy, was investigated for potential antinociceptive effects. This study employs various nociceptive assays in mice to elucidate MCBA's antinociceptive mechanisms. MATERIALS AND METHODS: MCBA's antinociceptive potential was tested against various nociception models induced by formalin, glutamate, capsaicin, a transient receptor potential vanilloid 1 (TRPV1) receptor agonist, and phorbol 12-myristate 13-acetate, a protein kinase C (PKC) activator. It was then assessed using the hot plate test and examined within the acetic acid-induced writhing test. During the acetic acid-induced writhing test, MCBA was pre-challenged against selective receptor antagonists such as naloxone, caffeine, atropine, yohimbine, ondansetron, and haloperidol. It was also pre-challenged with ATP-sensitive potassium channel inhibitor (glibenclamide) to further elucidate its antinociceptive mechanism. RESULTS: The results showed that oral administration of MCBA led to a dose-dependent and significant inhibition (p < 0.05) of nociceptive effects across all evaluated models at doses of 60, 120, and 240 mg/kg. Moreover, the efficacy of MCBA's antinociceptive potential was significantly counteracted (p < 0.0001) by specific antagonists: (i) directed at adenosinergic, alpha-2 adrenergic, and cholinergic receptors using caffeine, yohimbine, and atropine, respectively; and (ii) targeting ATP-sensitive potassium channels, employing glibenclamide. Antagonists aimed at opioidergic and serotoninergic receptors (naloxone and ondansetron, respectively) had poor utility in inhibiting antinociceptive activity. Conversely, the dopaminergic receptor antagonist haloperidol potentiated locomotor abnormalities associated with MCBA treatment. CONCLUSIONS: MCBA-induced antinociception involves modulation of glutamatergic-, TRVP1 receptors- and PKC-signaling pathways. It impacts adenosinergic, alpha-2 adrenergic, and cholinergic receptors and opens ATP-sensitive potassium channels.


Asunto(s)
Cafeína , Gliburida , Animales , Ratones , Haloperidol , Nocicepción , Ondansetrón , Adrenérgicos , Atropina , Canales KATP , Naloxona/farmacología , Receptores Colinérgicos , Yohimbina , Analgésicos/farmacología , Acetatos
14.
Sci Rep ; 14(1): 5926, 2024 03 11.
Artículo en Inglés | MEDLINE | ID: mdl-38467744

RESUMEN

Cardioneuroablation (CNA) is currently considered as a promising treatment option for patients with symptomatic bradycardia caused by vagotonia. This study aims to further investigate its safety and efficacy in patients suffering from vagal bradycardia. A total of 60 patients with vagal bradycardia who underwent CNA in the First Affiliated Hospital of Xinjiang Medical University from November 2019 to June 2022. Preoperative atropine tests revealed abnormal vagal tone elevation in all patients. First, the electroanatomic structures of the left atrium was mapped out by using the Carto 3 system, according to the protocol of purely anatomy-guided and local fractionated intracardiac electrogram-guided CNA methods. The upper limit of ablation power of superior left ganglion (SLGP) and right anterior ganglion (RAGP) was not more than 45W with an ablation index of 450.Postoperative transesophageal cardiac electrophysiological examination was performed 1 to 3 months after surgery. The atropine test was conducted when appropriate. Twelve-lead electrocardiogram, Holter electrocardiogram, and skin sympathetic nerve activity were reviewed at 1, 3, 6 and 12 months after operation. Adverse events such as pacemaker implantation and other complications were also recorded to analyze the safety and efficacy of CNA in the treatment of vagus bradycardia. Sixty patients were enrolled in the study (38 males, mean age 36.67 ± 9.44, ranging from 18 to 50 years old). None of the patients had a vascular injury, thromboembolism, pericardial effusion, or other surgical complications. The mean heart rate, minimum heart rate, low frequency, low/high frequency, acceleration capacity of rate, and skin sympathetic nerve activity increased significantly after CNA. Conversely, SDNN, PNN50, rMSSD, high frequency, and deceleration capacity of rate values decreased after CNA (all P < 0.05). At 3 months after ablation, the average heart rate, maximum heart rate, and acceleration capacity of heart rate remained higher than those before ablation, and the deceleration capacity of heart rate remained lower than those before ablation and the above results continued to follow up for 12 months after ablation (all P < 0.05). There was no significant difference in other indicators compared with those before ablation (all P > 0.05). The remaining 81.67% (49/60) of the patients had good clinical results, with no episodes of arrhythmia during follow-up. CNA may be a safe and effective treatment for vagal-induced bradycardia, subject to confirmation by larger multicenter trials.


Asunto(s)
Bradicardia , Ablación por Catéter , Masculino , Humanos , Adulto , Persona de Mediana Edad , Adolescente , Adulto Joven , Bradicardia/etiología , Bradicardia/terapia , Bradicardia/diagnóstico , Estudios Prospectivos , Electrocardiografía , Atrios Cardíacos , Atropina , Ablación por Catéter/efectos adversos , Ablación por Catéter/métodos
15.
Braz J Biol ; 83: e277354, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38452187

RESUMEN

This study aimed to explore the diuretic activity of linalyl acetate (LA). LA is an essential oil, it is an integral phyto-constituent of various plants. In this study, acute and chronic diuretic activities were explored by measuring the levels of different electrolytes and pH in the urine of experimental rats. Rats were divided into five groups. The control group was given 10 mg/kg normal saline, the treated group was given 10 mg/kg furosemide, and the remaining 3 groups received different doses of LA including 25, 50, and 75 mg/kg through intraperitoneal route, to determine its diuretic potential. Urine volume for acute diuretic activity was measured for 6 hours however for chronic diuretic activity was measured for 6 days. For a comparative study of LA with a control group and treated group with reference drug, diuretic index was used. Moreover, the underlying mechanism of the diuretic activity was also explored by comparing atropine, L-NAME, and indomethacin. The results of each group with 6 rats in each group were obtained by ± standard error of the mean of every group. Analysis of Variance (ANOVA) was used for statistical analysis. Results revealed that the LA 75 mg/kg dose showed comparable results as of furosemide. Moreover, this study revealed the involvement of muscarinic receptors to produce diuresis in comparison with atropine with very little involvement of prostanoids and no effect on NO pathway induced by indomethacin and L-NAME respectively. It is concluded that LA possess anti-diuretic potential. Muscarinic receptors might be involved in producing diuretic effects.


Asunto(s)
Diuréticos , Furosemida , Monoterpenos , Ratas , Animales , Furosemida/farmacología , NG-Nitroarginina Metil Éster/farmacología , Diuréticos/farmacología , Indometacina/farmacología , Atropina/farmacología , Extractos Vegetales/farmacología , Receptores Muscarínicos
16.
Optom Vis Sci ; 101(1): 37-43, 2024 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-38350056

RESUMEN

SIGNIFICANCE: Popularity of publicly searched myopia terminologies is reported, for example, myopia control over myopia management and myopia over nearsighted or shortsighted. Insights are also provided for searches on specific myopia control interventions. The findings offer an evidence-based starting point for public messaging and communications by clinicians, policymakers, and other industry leaders. PURPOSE: Public understanding of myopia can be difficult to ascertain for clinicians. Although small-scale studies provide valuable snapshots of data, findings tend to be population-specific and thus difficult to extrapolate to global audiences. In this study, big data were used to provide a more comprehensive depiction of global market interest in myopia. METHODS: Google Trends data were used to analyze searches relating to myopia between January 2004 and August 2023. Data extracted were related to use of the terms myopia control and myopia management, with further searches executed for common myopia control interventions: orthokeratology, contact lenses, atropine, and glasses. Analysis into the search interest of other refractive error states, hyperopia and astigmatism, was also undertaken along with alternative terms that may be used to describe myopia. Where relevant, search trends were considered worldwide, by country, and over time. RESULTS: Myopia was a more popular search term than common layman alternatives such as nearsighted or shortsighted. Myopia control was found to be more popular than myopia management, and of the specific myopia interventions, atropine was most popular. Compared with astigmatism and hyperopia, relative search volumes were greatest for myopia, on average accounting for approximately 50% of the relative search volume at the country level. CONCLUSIONS: The differences identified in both popularity of myopia-related search terms and specific interventions may provide the basis for improvements in public messaging and facilitate patient-practitioner communication.


Asunto(s)
Astigmatismo , Hiperopía , Miopía , Humanos , Macrodatos , Miopía/epidemiología , Miopía/terapia , Atropina
20.
Hipertens Riesgo Vasc ; 41(1): 58-61, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38403566

RESUMEN

Atropine, a competitive antagonist of acetylcholine muscarinic receptors, is commonly used to treat severe bradycardia by blocking parasympathetic activity. We present a rare case of hypertensive emergency following atropine administration, with only one previous report in the literature. A 78-year-old woman with essential hypertension and hypercholesterolemia was admitted to the cardiac intensive care unit for non-ST segment elevation myocardial infarction. During coronary angiography, an occlusion of the right coronary artery was identified. While removing the diagnostic catheter through the right radial artery, the patient experienced intense pain and discomfort, accompanied by a vasovagal reflex characterized by bradycardia and hypotension. Intravenous atropine (0.5mg) was administered, leading to a rapid rise in heart rate with frequent ventricular ectopy. Subsequently, a progressive and exaggerated elevation in arterial blood pressure occurred, peaking at 294/121mmHg approximately 10min after atropine administration. The patient developed hypertensive acute pulmonary edema, successfully treated with intravenous nitroglycerine (10mg) and furosemide (60mg). Blood pressure normalized after approximately 14min. The exact mechanism of atropine-induced hypertensive emergency remains unknown. While hypertensive emergencies with atropine are exceedingly rare, healthcare professionals should be aware of this potential effect and be prepared for prompt intervention.


Asunto(s)
Hipertensión , Crisis Hipertensiva , Femenino , Humanos , Anciano , Atropina/efectos adversos , Bradicardia/inducido químicamente , Hipertensión/tratamiento farmacológico , Frecuencia Cardíaca
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