RESUMO
REASONS FOR PERFORMING STUDY: Short duration of analgesia is among the limitations of a single epidural injection with lidocaine in horses. OBJECTIVES: To evaluate the effectiveness and safety of epidural lidocaine in combination with either tramadol or neostigmine for perineal analgesia in horses. METHODS: Epidural catheters were placed in 6 saddle horses that then were given 3 treatments: 2% lidocaine (0.2 mg/kg bwt) alone, 2% lidocaine (0.2 mg/kg bwt) plus tramadol (0.5 mg/kg bwt), and 2% lidocaine (0.2 mg/kg bwt) plus neostigmine (1.0 µg/kg bwt). The order of treatments was randomised. Haemodynamic variables, respiratory rate, rectal temperature, analgesia, motor block and behaviour scores were compared among the 3 treatments. These parameters were determined before drug administration (baseline), at 5, 10, 15, 30, 45, 60, 75 and 90 min, and every 30 min thereafter until loss of analgesia. RESULTS: Duration of analgesia was longer with lidocaine plus tramadol (210 ± 12 min) compared with lidocaine plus neostigmine (150 ± 35 min) or lidocaine alone (70 ± 12 min; P<0.05). All treatments produced mild or moderate motor block without behavioural changes. Other adverse effects were not observed in any of the horses. CONCLUSION AND POTENTIAL RELEVANCE: Further studies are required to demonstrate whether tramadol or neostigmine have a role in the management of post operative pain when coadministered with lidocaine.
Assuntos
Analgesia/veterinária , Doenças dos Cavalos/prevenção & controle , Lidocaína/farmacologia , Neostigmina/farmacologia , Períneo , Tramadol/farmacologia , Analgésicos Opioides/administração & dosagem , Analgésicos Opioides/farmacologia , Anestésicos Locais/administração & dosagem , Anestésicos Locais/farmacologia , Animais , Estudos Cross-Over , Quimioterapia Combinada , Cavalos , Lidocaína/administração & dosagem , Neostigmina/administração & dosagem , Dor/prevenção & controle , Dor/veterinária , Parassimpatomiméticos/administração & dosagem , Parassimpatomiméticos/farmacologia , Tramadol/administração & dosagemRESUMO
BACKGROUND: A case of severe constipation is described in a 75-year- old cancer patient receiving methadone for pain. Her constipation was refractory to the current treatment and she suffered severe discomfort and cognitive impairment. Due to the severity of the clinical situation and after excluding mechanical obstruction, low doses of subcutaneous neostigmine were administered, having bowel movements with evacuation of stools in a few hours after its administration. DISCUSSION: The results suggest that subcutaneous neostigmine could be an alternative choice in a group of selected patients with advanced cancer and opioid-induced constipation.
Assuntos
Constipação Intestinal/tratamento farmacológico , Metadona/efeitos adversos , Neoplasias/complicações , Neostigmina/uso terapêutico , Dor/tratamento farmacológico , Idoso , Analgésicos Opioides/efeitos adversos , Analgésicos Opioides/uso terapêutico , Constipação Intestinal/induzido quimicamente , Feminino , Humanos , Injeções Subcutâneas , Metadona/uso terapêutico , Neoplasias/tratamento farmacológico , Neostigmina/administração & dosagem , Parassimpatomiméticos/administração & dosagem , Parassimpatomiméticos/uso terapêuticoRESUMO
The aim of this study was to evaluate the participation of central cholinergic transmission in the regulation of metabolic rate, core temperature, and heat storage in untrained rats submitted to exercise on a treadmill (20 m/min, 5% inclination) until fatigue. The animals were separated into eight experimental groups, and core temperature or metabolic rate was measured in the rats while they were exercising or while they were at rest after injection of 2 microl of 5 x 10(-3) M physostigmine (Phy) or 0.15 M NaCl solution (Sal) into the lateral cerebral ventricle. Metabolic rate was determined by the indirect calorimetry system, and colonic temperature was recorded as an index of core temperature. In resting animals, Phy induced only a small increase in metabolic rate compared with Sal injection, without having any effect on core temperature. During exercise, the Phy-treated animals showed a lower core heating rate (0.022 +/- 0.003 degrees C/min Phy vs. 0.033 +/- 0.003 degrees C/min Sal; P < 0.02), lower heat storage (285 +/- 37 cal Phy vs. 436 +/- 34 cal Sal; P < 0.02) and lower core temperature at fatigue point than the Sal-treated group (38.5 +/- 0.1 degrees C Phy vs. 39.0 +/- 0.1 degrees C Sal; P < 0.05). However, despite the lower core heating rate, heat storage, and core temperature at fatigue, the Phy-treated rats showed a similar running time compared with the Sal-treated group. We conclude that the activation of the central cholinergic system during exercise increases heat dissipation and attenuates the exercise-induced increase in core temperature without affecting running performance.
Assuntos
Regulação da Temperatura Corporal/efeitos dos fármacos , Regulação da Temperatura Corporal/fisiologia , Parassimpatomiméticos/farmacologia , Fisostigmina/farmacologia , Corrida/fisiologia , Animais , Injeções Intraventriculares , Cinética , Masculino , Metabolismo/efeitos dos fármacos , Metabolismo/fisiologia , Fadiga Muscular/efeitos dos fármacos , Fadiga Muscular/fisiologia , Consumo de Oxigênio/efeitos dos fármacos , Consumo de Oxigênio/fisiologia , Parassimpatomiméticos/administração & dosagem , Fisostigmina/administração & dosagem , Ratos , Ratos WistarRESUMO
BACKGROUND: The purpose of this study was to determine whether combination of 1-5 microg intrathecal neostigmine would enhance analgesia from a fixed intrathecal dose of morphine. METHODS: A total of 60 patients undergoing gynecologic surgery were randomized to one of five groups. Patients received 15 mg bupivacaine plus 2 ml of the test drug intrathecally (saline, 100 microg morphine, or 1-5 microg neostigmine). The control group received spinal saline as the test drug. The morphine group received spinal morphine as test drug. The morphine + 1 microg neostigmine group received spinal morphine and 1 microg neostigmine. The morphine + 2.5 microg neostigmine group received spinal morphine and 2.5 microg neostigmine. Finally, the morphine + 5 microg neostigmine group received spinal morphine and 5 microg neostigmine. RESULTS: The groups were demographically similar. The time to first rescue analgesic (minutes) was longer for all patients who received intrathecal morphine combined with 1-5 microg neostigmine (median, 6 h) compared with the control group (median, 3 h) (P < 0.02). The morphine group (P < 0.05) and the groups that received the combination of 100 microg intrathecal morphine combined with neostigmine (P < 0.005) required less rescue analgesics in 24 h compared with the control group. The incidence of perioperative adverse effects was similar among groups (P > 0.05). CONCLUSIONS: The addition of 1-5 microg spinal neostigmine to 100 microg morphine doubled the duration to first rescue analgesic in the population studied and decreased the analgesic consumption in 24 h, without increasing the incidence of adverse effects. The data suggest that low-dose spinal neostigmine may improve morphine analgesia.
Assuntos
Analgésicos Opioides/uso terapêutico , Procedimentos Cirúrgicos em Ginecologia , Morfina/uso terapêutico , Neostigmina/uso terapêutico , Dor Pós-Operatória/tratamento farmacológico , Parassimpatomiméticos/uso terapêutico , Adulto , Analgésicos Opioides/administração & dosagem , Raquianestesia , Relação Dose-Resposta a Droga , Método Duplo-Cego , Quimioterapia Combinada , Feminino , Humanos , Injeções Espinhais , Pessoa de Meia-Idade , Morfina/administração & dosagem , Neostigmina/administração & dosagem , Medição da Dor/efeitos dos fármacos , Parassimpatomiméticos/administração & dosagemRESUMO
A study was carried out relating to the anticholinergic action of clonidine on the cardiovascular responses to i.c.v. injection of neostigmine, a quaternary anticholinesterase, in conscious sham-operated animals and rats with sinoaortic denervation, 7 days after the corresponding operation. Neostigmine (0.1-1 micrograms i.c.v.) induced a dose-dependent pressor and bradycardic responses in sham-operated rats but induced only an increase in blood pressure in sinoaortic-denervated animals. However, the pressor response in sinoaortic-denervated rats was significantly greater than in sham-operated animals. Clonidine (10 micrograms kg-1 i.v.) induced a fall in mean arterial pressure in sinoaortic-denervated rats but not in sham-operated animals. Moreover, sinoaortic denervation reduced the bradycardic action of this antihypertensive drug. The anticholinesterase activity of clonidine (10 micrograms kg-1 i.v.), given 30 min previously, prevented the bradycardic action of neostigmine (0.1-1 micrograms i.c.v.) but failed to modify the pressor effect in sham-operated rats. This alpha2-adrenergic agent reduced the pressor response to i.c.v. administration of neostigmine in sinoaortic-denervated rats. Alternatively, the i.c.v. administration of clonidine (3 micrograms i.c.v.), given either 15 or 30 min before neostigmine, only prevented the bradycardic effect of the anticholinesterase (0.3 micrograms i.c.v.) in sham-operated rats but not the pressor action of this drug. In sinoaortic denervated rats, 3 micrograms of clonidine i.c.v. reduced an increase in blood pressure by i.c.v. injection of the anticholinesterase. The results suggest different central cholinergic mechanisms and different cholinergic-adrenergic interactions on the cardiovascular responses elicited by centrally injected neostigmine in sinoaortic denervated rats.
Assuntos
Antagonistas Colinérgicos/farmacologia , Clonidina/farmacologia , Nó Sinoatrial/fisiologia , Animais , Barorreflexo/efeitos dos fármacos , Pressão Sanguínea/efeitos dos fármacos , Denervação , Relação Dose-Resposta a Droga , Frequência Cardíaca/efeitos dos fármacos , Injeções Intraventriculares , Masculino , Neostigmina/administração & dosagem , Neostigmina/antagonistas & inibidores , Neostigmina/farmacologia , Parassimpatomiméticos/administração & dosagem , Parassimpatomiméticos/antagonistas & inibidores , Parassimpatomiméticos/farmacologia , Ratos , Ratos WistarRESUMO
BACKGROUND AND OBJECTIVES: Intraspinal administration of neostigmine has been shown to prevent induction of hypotension in rats by bupivacaine spinal block, and thus to provide greater hemodynamic stability. This study was undertaken to determine whether subarachnoid neostigmine would prevent bupivacaine spinal anesthesia from causing hypotension or bradycardia in patients undergoing abdominal hysterectomy. METHODS: Of 40 patients scheduled for abdominal hysterectomy under spinal anesthesia, 20 were randomly assigned to each of two groups. The control group (CG) received 1.5 mL subarachnoid saline followed by 15 mg (3 mL) of hyperbaric bupivacaine 0.5%. The neostigmine group (NG) received 75 micrograms (1.5 mL) of subarachnoid neostigmine followed by 15 mg (3 mL) of hyperbaric bupivacaine 0.5%. No preload was given. Hypotension was treated with 4-mg intravenous boluses of ephedrine to keep blood pressure above 75% of the baseline value. The skin body temperature was measured with probes at the suprascapular region and at the foot. RESULTS: Spinal neostigmine (75 micrograms) failed to prevent bupivacaine-induced hypotension. There was no statistical difference in the incidence of brady-cardia between the groups (NG, 2/20; CG 1/20), although the bradycardia appeared to be qualitatively different, being somewhat delayed in the NG. Spinal neostigmine did not alter the onset or duration of sensory block and did not affect skin body temperature in either anesthetized or unanesthetized sites. The incidence of intraoperative nausea was 20% in the NG and 5% in the CG. CONCLUSION: A 75-micrograms subarachnoid neostigmine dose does not affect blood pressure or heart rate during bupivacaine spinal anesthesia.
Assuntos
Raquianestesia , Pressão Sanguínea/efeitos dos fármacos , Bupivacaína , Frequência Cardíaca/efeitos dos fármacos , Neostigmina/administração & dosagem , Parassimpatomiméticos/administração & dosagem , Adulto , Raquianestesia/efeitos adversos , Bradicardia/induzido quimicamente , Bradicardia/etiologia , Bradicardia/prevenção & controle , Bupivacaína/efeitos adversos , Feminino , Humanos , Hipotensão/induzido quimicamente , Hipotensão/etiologia , Hipotensão/prevenção & controle , Histerectomia , Injeções Espinhais , Pessoa de Meia-Idade , Temperatura Cutânea , Espaço SubaracnóideoRESUMO
Two patients suffering with severe pain due to metastatic abdominal neoplasm were selected to examine whether subarachnoid neostigmine provided effective pain relief. Neostigmine was injected through a catheter introduced into the subarachnoid space at L4-L5. Patients were monitored for changes in arterial blood pressure, cardiac and respiratory rates, body temperature, level of consciousness and neurologic change. Pain was classified by the patients on a verbal four-grade scale, and analgesia was classified on a verbal three-grade scale. Complete pain relief was obtained 2 h after neostigmine (0.2 mg) in one patient and 4 h after neostigmine (0.1 mg) in the second patient. Pain of mild intensity returned 20 and 22 h after drug administration, respectively. Gastrointestinal discomfort was observed in both cases, but nausea and vomiting occurred only in the patient treated with the highest dose of neostigmine. No significant change in the monitored parameters was observed, except for a 6-h period of decreased blood pressure in the patient treated with the lower dose of neostigmine which required no specific treatment. The results obtained in these anecdotal cases indicate that subarachnoid neostigmine may provide analgesia in patients with pain arising from neoplasia, but further studies using controlled trials are needed before the drug is brought into clinical use.
Assuntos
Neoplasias Abdominais/complicações , Neostigmina/uso terapêutico , Dor/tratamento farmacológico , Parassimpatomiméticos/uso terapêutico , Neoplasias Abdominais/secundário , Cateterismo , Doença Crônica , Hemodinâmica/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Neostigmina/administração & dosagem , Dor/etiologia , Parassimpatomiméticos/administração & dosagem , Neoplasias Retais/patologia , Neoplasias Gástricas/patologia , Espaço SubaracnóideoRESUMO
This study was designed to qualitatively evaluate the analgesic actions of intrathecal neostigmine alone and with intravenous (IV) N-butyl-scopolamine on somatic and visceral pain. Twenty-seven patients scheduled for both tubal ligation and vaginoplasty were divided into three groups. Patients received a standard anesthetic with thiopental, atracurium, and N2O/O2/enflurane. N-butyl-scopolamine, 20 mg, or saline was administered as a 2-mL IV bolus 20 min before the end of the surgical procedure. The control group (CG) received spinal and IV saline; the neostigmine group (NG), spinal neostigmine and IV saline; and the neostigmine-N-butyl-scopolamine group (NSG), spinal neostigmine and IV N-butyl-scopolamine. Postoperatively, patients assessed their pain on a 10-cm visual analog scale (VAS). The CG had both visceral and somatic pain at the first 30-min assessment, and all patients requested morphine. Patients from the NG had only visceral pain from the first assessment; however, they had lower VAS scores (P = 0.026) and requested less morphine (P = 0.037). Patients from the NSG were pain free during all assessment times (P < 0.0001). Neostigmine was more effective for somatic pain than visceral pain. N-butyl-scopolamine administration acted peripherally as an effective complement for treatment of visceral pain, reflecting an association between central cholinergic effects and peripheral anticholinergic effects in the treatment of visceral postoperative pain.
Assuntos
Analgesia , Brometo de Butilescopolamônio/administração & dosagem , Antagonistas Colinérgicos/administração & dosagem , Neostigmina/administração & dosagem , Dor Pós-Operatória/prevenção & controle , Parassimpatolíticos/administração & dosagem , Parassimpatomiméticos/administração & dosagem , Adulto , Analgésicos/administração & dosagem , Método Duplo-Cego , Feminino , Humanos , Injeções Intravenosas , Injeções Espinhais , Morfina/administração & dosagem , Medição da Dor , Estudos Prospectivos , Esterilização Tubária , Vagina/cirurgia , VíscerasRESUMO
Microinjections of carbachol (50 nmol) or neostigmine (25 nmol) in 0.5 ml saline into the ventromedial nucleus of the hypothalamus (VMH) (but not into the lateral hypothalamic area) of fed, conscious rats produced marked increases in plasma glucose and lactate, which were suppressed or markedly reduced by previous adrenodemedullation. The rate of incorporation of 14C from infused bicarbonate (0.60 microliter, 0.20 microCi/min), an index of gluconeogenic activity, increased significantly after VMH administration of neostigmine. The data suggest that cholinergic synapses in the VMH participate of a central glucoregulatory system that increases hepatic glucose production mainly through a stimulation of adrenal medulla epinephrine secretion.
Assuntos
Gluconeogênese/efeitos dos fármacos , Hiperglicemia/induzido quimicamente , Região Hipotalâmica Lateral/efeitos dos fármacos , Hipotálamo Médio/efeitos dos fármacos , Lactatos/sangue , Parassimpatomiméticos/administração & dosagem , Medula Suprarrenal/fisiologia , Animais , Carbacol/administração & dosagem , Alimentos , Ácido Láctico , Masculino , Microinjeções , Neostigmina/administração & dosagem , Ratos , Ratos Wistar , Fatores de TempoRESUMO
Se evaluó en lactantes asmáticos el efecto de un agente proquinético: cisapride. Cuarenta pacientes asmáticos, cuyas edades estaban comprendidas entre 2 y 11 meses, fueron estudiados durante 4 semanas. Se conformaron dos grupos de 20 casos cada uno. En cada grupo había tres lactantes con reflujo gastroesofágico. Todos los niños fueron estudiados al comienzo del ensayo y controlados cada 7 días. Tos, sibilancia, disnea y reflujo gastroesofágico fueron evaluados clínicamente. Los lactantes del grupo I fueron tratados con Cisapride oral con una dosis de 0,2mg/kg tres veces por día. Los lactantes del grupo II sirvieron como controles. La intensidad y la frecuencia de los síntomas fueron evaluados por medio de un sistema de puntaje de 0 a 4 cruces. La tos diurna mejoró (p<0.01) durante la primera semana de tratamiento. La sibilancia nocturna disminuyó durante la segunda y tercera semana (p<0.008 y p<0.01 respectivamente). La disnea disminuyó en el transcurso de la primera semana (p<0.008). La mejoría de la enfermedad asmática se observó al finalizar el estudio (p<0.002). El reflujo gastroesofágico desapareció dentro de las 72 horas después de iniciado el tratamiento. Estos resultados indican una significativa mejoría en el grupo que recibió Cisapride (grupo I). Este colinomimético indirecto, que actúa sobre el sistema vagal, incrementa la actividad del neurotransmisor VIP y se sabe que VIP ejerce una potente actividad broncodilatadora
Assuntos
Humanos , Masculino , Feminino , Lactente , Asma/tratamento farmacológico , Parassimpatomiméticos/uso terapêutico , Asma/etiologia , Asma/fisiopatologia , Tosse/tratamento farmacológico , Tosse/etiologia , Tosse/fisiopatologia , Parassimpatomiméticos/administração & dosagem , Refluxo Gastroesofágico/complicações , Refluxo Gastroesofágico/tratamento farmacológicoRESUMO
Se evaluó en lactantes asmáticos el efecto de un agente proquinético: cisapride. Cuarenta pacientes asmáticos, cuyas edades estaban comprendidas entre 2 y 11 meses, fueron estudiados durante 4 semanas. Se conformaron dos grupos de 20 casos cada uno. En cada grupo había tres lactantes con reflujo gastroesofágico. Todos los niños fueron estudiados al comienzo del ensayo y controlados cada 7 días. Tos, sibilancia, disnea y reflujo gastroesofágico fueron evaluados clínicamente. Los lactantes del grupo I fueron tratados con Cisapride oral con una dosis de 0,2mg/kg tres veces por día. Los lactantes del grupo II sirvieron como controles. La intensidad y la frecuencia de los síntomas fueron evaluados por medio de un sistema de puntaje de 0 a 4 cruces. La tos diurna mejoró (p<0.01) durante la primera semana de tratamiento. La sibilancia nocturna disminuyó durante la segunda y tercera semana (p<0.008 y p<0.01 respectivamente). La disnea disminuyó en el transcurso de la primera semana (p<0.008). La mejoría de la enfermedad asmática se observó al finalizar el estudio (p<0.002). El reflujo gastroesofágico desapareció dentro de las 72 horas después de iniciado el tratamiento. Estos resultados indican una significativa mejoría en el grupo que recibió Cisapride (grupo I). Este colinomimético indirecto, que actúa sobre el sistema vagal, incrementa la actividad del neurotransmisor VIP y se sabe que VIP ejerce una potente actividad broncodilatadora