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[PMID]:28230244
[Au] Autor:Tayeb BO; Eidelman A; Eidelman CL; McNicol ED; Carr DB
[Ad] Endereço:Pain Research, Education and Policy (PREP) Program, Department of Public Health and Community Medicine, Tufts University School of Medicine, 136 Harrison Avenue, Stearns 203, Boston, Massachusetts, USA.
[Ti] Título:Topical anaesthetics for pain control during repair of dermal laceration.
[So] Source:Cochrane Database Syst Rev;2:CD005364, 2017 02 22.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Topical local anaesthetics provide effective analgesia for patients undergoing numerous superficial procedures, including repair of dermal lacerations. The need for cocaine in topical anaesthetic formulations has been questioned because of concern about adverse effects, thus novel preparations of cocaine-free anaesthetics have been developed. This review was originally published in 2011 and has been updated in 2017. OBJECTIVES: To assess whether benefits of non-invasive topical anaesthetic application occur at the expense of decreased analgesic efficacy. To compare the efficacy of various single-component or multi-component topical anaesthetic agents for repair of dermal lacerations. To determine the clinical necessity for topical application of the ester anaesthetic, cocaine. SEARCH METHODS: For this updated review, we searched the following databases: Cochrane Central Register of Controlled Trials (CENTRAL; 2016, Issue 11), Cumulative Index to Nursing and Allied Health Literature (CINAHL; 2010 to December 2016), Embase (2010 to December 2016) and MEDLINE (2010 to December 2016). We did not limit this search by language or format of publication. We contacted manufacturers, international scientific societies and researchers in the field. Weemailed selected journalsand reviewed meta-registers of ongoing trials. For the previous version of this review, we searched these databases to November 2010. SELECTION CRITERIA: We included randomized controlled trials (RCTs) that evaluated the efficacy and safety of topical anaesthetics for repair of dermal laceration in adult and paediatric participants. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed trial quality and extracted data. We contacted study authors for additional information when needed. We collected adverse event information from trial reports. We assessed methodological risk of bias for each included study and employed the GRADE approach to assess the overall quality of the evidence. MAIN RESULTS: The present updated review included 25 RCTs involving 3278 participants. The small number of trials in each comparison group and the heterogeneity of outcome measures precluded quantitative analysis of data for all but one outcome: pain intensity. In two pooled studies, the mean self-reported visual analogue scale (VAS; 0 to 100 mm) score for topical prilocaine-phenylephrine (PP) was higher than the mean self-reported VAS (0 to 100 mm) score for topical tetracaine-epinephrine-cocaine (TAC) by 5.59 points (95% confidence interval (CI) 2.16 to 13.35). Most trials that compared infiltrated and topical anaesthetics were at high risk of bias, which is likely to have affected their results. Researchers found that several cocaine-free topical anaesthetics provided effective analgesic efficacy. However, data regarding the efficacy of each topical agent are based mostly on single comparisons in trials with unclear or high risk of bias. Mild, self-limited erythematous skin induration occurred in one of 1042 participants who had undergone application of TAC. Investigators reported no serious complications among any of the participants treated with cocaine-based or cocaine-free topical anaesthetics. The overall quality of the evidence according to the GRADE system is low owing to limitations in design and implementation, imprecision of results and high probability of publication bias (selective reporting of data). Additional well-designed RCTs with low risk of bias are necessary before definitive conclusions can be reached. AUTHORS' CONCLUSIONS: We have found two new studies published since the last version of this review was prepared. We have added these studies to those previously included and have conducted an updated analysis, which resulted in the same review conclusions as were presented previously.Mostly descriptive analysis indicates that topical anaesthetics may offer an efficacious, non-invasive means of providing analgesia before suturing of dermal lacerations. Use of cocaine-based topical anaesthetics might be hard to justify, given the availability of other effective topical anaesthetics without cocaine. However, the overall quality of the evidence according to the GRADE system is low owing to limitations in design and implementation, imprecision of results and high probability of publication bias (selective reporting of data). Additional well-designed RCTs with low risk of bias are necessary before definitive conclusions can be reached.
[Mh] Termos MeSH primário: Anestésicos Locais/administração & dosagem
Lacerações/cirurgia
Pele/lesões
[Mh] Termos MeSH secundário: Adulto
Anestésicos Locais/efeitos adversos
Anestésicos Locais/química
Criança
Cocaína/administração & dosagem
Cocaína/efeitos adversos
Combinação de Medicamentos
Epinefrina/administração & dosagem
Epinefrina/efeitos adversos
Seres Humanos
Medição da Dor
Ensaios Clínicos Controlados Aleatórios como Assunto
Suturas
Tetracaína/administração & dosagem
Tetracaína/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Drug Combinations); 0619F35CGV (Tetracaine); I5Y540LHVR (Cocaine); YKH834O4BH (Epinephrine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170614
[Lr] Data última revisão:
170614
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170224
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD005364.pub3


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[PMID]:28160271
[Au] Autor:Foster JP; Taylor C; Spence K
[Ad] Endereço:School of Nursing and Midwifery, University of Sydney, Penrith DC, Australia.
[Ti] Título:Topical anaesthesia for needle-related pain in newborn infants.
[So] Source:Cochrane Database Syst Rev;2:CD010331, 2017 02 04.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Hospitalised newborn neonates frequently undergo painful invasive procedures that involve penetration of the skin and other tissues by a needle. One intervention that can be used prior to a needle insertion procedure is application of a topical local anaesthetic. OBJECTIVES: To evaluate the efficacy and safety of topical anaesthetics such as amethocaine and EMLA in newborn term or preterm infants requiring an invasive procedure involving puncture of skin and other tissues with a needle. SEARCH METHODS: We searched the Cochrane Central Register of Controlled Trials (CENTRAL), PubMed, Embase and CINAHL up to 15 May 2016; previous reviews including cross-references, abstracts, and conference proceedings. We contacted expert informants. We contacted authors directly to obtain additional data. We imposed no language restrictions. SELECTION CRITERIA: Randomised, quasi-randomised controlled trials, and cluster and cross-over randomised trials that compared the topical anaesthetics amethocaine and eutectic mixture of local anaesthetics (EMLA) in terms of anaesthetic efficacy and safety in newborn term or preterm infants requiring an invasive procedure involving puncture of skin and other tissues with a needle DATA COLLECTION AND ANALYSIS: From the reports of the clinical trials we extracted data regarding clinical outcomes including pain, number of infants with methaemoglobin level 5% and above, number of needle prick attempts prior to successful needle-related procedure, crying, time taken to complete the procedure, episodes of apnoea, episodes of bradycardia, episodes of oxygen desaturation, neurodevelopmental disability and other adverse events. MAIN RESULTS: Eight small randomised controlled trials met the inclusion criteria (n = 506). These studies compared either EMLA and placebo or amethocaine and placebo. No studies compared EMLA and amethocaine. We were unable to meta-analyse the outcome of pain due to differing outcome measures and methods of reporting. For EMLA, two individual studies reported a statistically significant reduction in pain compared to placebo during lumbar puncture and venepuncture. Three studies found no statistical difference between the groups during heel lancing. For amethocaine, three studies reported a statistically significant reduction in pain compared to placebo during venepuncture and one study reported a statistically significant reduction in pain compared to placebo during cannulation. One study reported no statistical difference between the two groups during intramuscular injection.One study reported no statistical difference between EMLA and the placebo group for successful venepuncture at first attempt. One study similarly reported no statistically significant difference between Amethocaine and the placebo group for successful cannulation at first attempt.Risk for local redness, swelling or blanching was significantly higher with EMLA (typical risk ratio (RR) 1.65, 95% confidence interval (CI) 1.24 to 2.19; typical risk difference (RD) 0.17, 95% CI 0.09 to 0.26; n = 272; number needed to treat for an additional harmful outcome (NNTH) 6, 95% CI 4 to 11; I = 92% indicating considerable heterogeneity) although not for amethocaine (typical RR 2.11, 95% CI 0.72 to 6.16; typical RD 0.05, 95% CI -0.02 to 0.11, n = 221). These local skin reactions for EMLA and amethocaine were reported as short-lasting. Two studies reported no methaemoglobinaemia with single application of EMLA. The quality of the evidence on outcomes assessed according to GRADE was low to moderate. AUTHORS' CONCLUSIONS: Overall, all the trials were small, and the effects of uncertain clinical significance. The evidence regarding the effectiveness or safety of the interventions studied is inadequate to support clinical recommendations. There has been no evaluation regarding any long-term effects of topical anaesthetics in newborn infants.High quality studies evaluating the efficacy and safety of topical anaesthetics such as amethocaine and EMLA for needle-related pain in newborn term or preterm infants are required. These studies should aim to determine efficacy of these topical anaesthetics and on homogenous groups of infants for gestational age. While there was no methaemoglobinaemia in the studies that reported methaemoglobin, the efficacy and safety of EMLA, especially in very preterm infants, and for repeated application, need to be further evaluated in future studies.
[Mh] Termos MeSH primário: Anestesia Local
Anestésicos Locais/administração & dosagem
Dor/prevenção & controle
Punções/efeitos adversos
Tetracaína/administração & dosagem
[Mh] Termos MeSH secundário: Anestesia Local/efeitos adversos
Anestesia Local/métodos
Anestésicos Locais/efeitos adversos
Cateterismo/efeitos adversos
Combinação de Medicamentos
Seres Humanos
Recém-Nascido
Recém-Nascido Prematuro
Agulhas
Dor/etiologia
Medição da Dor
Flebotomia/efeitos adversos
Ensaios Clínicos Controlados Aleatórios como Assunto
Punção Espinal/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; REVIEW
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Drug Combinations); 0619F35CGV (Tetracaine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170912
[Lr] Data última revisão:
170912
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170205
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD010331.pub2


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[PMID]:28130888
[Au] Autor:Cozzi G; Borrometi F; Benini F; Neri E; Rusalen F; Celentano L; Zanon D; Schreiber S; Ronfani L; Barbi E
[Ad] Endereço:Institute for Maternal and Child Health, IRCCS Burlo Garofolo, Trieste, Italy.
[Ti] Título:First-time success with needle procedures was higher with a warm lidocaine and tetracaine patch than an eutectic mixture of lidocaine and prilocaine cream.
[So] Source:Acta Paediatr;106(5):773-778, 2017 May.
[Is] ISSN:1651-2227
[Cp] País de publicação:Norway
[La] Idioma:eng
[Ab] Resumo:AIM: More than 50% of children report apian during venepuncture or intravenous cannulation and using local anaesthetics before needle procedures can lead to different success rates. This study examined how many needle procedures were successful at the first attempt when children received either a warm lidocaine and tetracaine patch or an eutectic mixture of lidocaine and prilocaine (EMLA) cream. METHODS: We conducted this multicentre randomised controlled trial at three tertiary-level children's hospitals in Italy in 2015. Children aged three to 10 years were enrolled in an emergency department, paediatric day hospital and paediatric ward and randomly allocated to receive a warm lidocaine and tetracaine patch or EMLA cream. The primary outcome was the success rate at the first attempt. RESULTS: The analysis included 172 children who received a warm lidocaine and tetracaine patch and 167 who received an EMLA cream. The needle procedure was successful at the first attempt in 158 children (92.4%) who received the warm patch and in 142 children (85.0%) who received the cream (p = 0.03). The pain scores were similar in both groups. CONCLUSION: This study showed that the first-time needle procedure success was 7.4% higher in children receiving a warm lidocaine and tetracaine patch than EMLA cream.
[Mh] Termos MeSH primário: Anestésicos Locais/administração & dosagem
Lidocaína/administração & dosagem
Dor/prevenção & controle
Flebotomia/efeitos adversos
Prilocaína/administração & dosagem
Tetracaína/administração & dosagem
[Mh] Termos MeSH secundário: Cateterismo Periférico/efeitos adversos
Criança
Pré-Escolar
Feminino
Temperatura Alta
Seres Humanos
Masculino
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (EMLA); 046O35D44R (Prilocaine); 0619F35CGV (Tetracaine); 98PI200987 (Lidocaine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170129
[St] Status:MEDLINE
[do] DOI:10.1111/apa.13764


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[PMID]:28060026
[Au] Autor:Ethington J; Goldmeier D; Gaynes BI
[Ad] Endereço:Department of Ophthalmology, Stritch School of Medicine, Loyola University Chicago, Maywood, IL.
[Ti] Título:Exponential Decay Metrics of Topical Tetracaine Hydrochloride Administration Describe Corneal Anesthesia Properties Mechanistically.
[So] Source:Cornea;36(3):363-366, 2017 Mar.
[Is] ISSN:1536-4798
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To identify pharmacodynamic (PD) and pharmacokinetic (PK) metrics that aid in mechanistic understanding of dosage considerations for prolonged corneal anesthesia. METHODS: A rabbit model using 0.5% tetracaine hydrochloride was used to induce corneal anesthesia in conjunction with Cochet-Bonnet anesthesiometry. Metrics were derived describing PD-PK parameters of the time-dependent domain of recovery in corneal sensitivity. Curve fitting used a 1-phase exponential dissociation paradigm assuming a 1-compartment PK model. Derivation of metrics including half-life and mean ligand residence time, tau (τ), was predicted by nonlinear regression. Bioavailability was determined by area under the curve of the dose-response relationship with varying drop volumes. RESULTS: Maximal corneal anesthesia maintained a plateau with a recovery inflection at the approximate time of predicted corneal drug half-life. PDs of recovery of corneal anesthesia were consistent with a first-order drug elimination rate. The mean ligand residence time (tau, τ) was 41.7 minutes, and half-life was 28.89 minutes. The mean estimated corneal elimination rate constant (ke) was 0.02402 minute. Duration of corneal anesthesia ranged from 55 to 58 minutes. There was no difference in time domain PD area under the curve between drop volumes. CONCLUSIONS: Use of a small drop volume of a topical anesthetic (as low as 11 µL) is bioequivalent to conventional drop size and seems to optimize dosing regiments with a little effect on ke. Prolongation of corneal anesthesia may therefore be best achieved with administration of small drop volumes at time intervals corresponding to the half-life of drug decay from the corneal compartment.
[Mh] Termos MeSH primário: Anestesia Local
Anestésicos Locais/administração & dosagem
Anestésicos Locais/farmacocinética
Córnea/metabolismo
Tetracaína/administração & dosagem
Tetracaína/farmacocinética
[Mh] Termos MeSH secundário: Administração Tópica
Animais
Disponibilidade Biológica
Córnea/efeitos dos fármacos
Modelos Animais
Soluções Oftálmicas
Coelhos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Ophthalmic Solutions); 0619F35CGV (Tetracaine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170107
[St] Status:MEDLINE
[do] DOI:10.1097/ICO.0000000000001125


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[PMID]:28017670
[Au] Autor:Piao LH; Fujita T; Yu T; Kumamoto E
[Ad] Endereço:Department of Physiology, Saga Medical School, 5-1-1 Nabeshima, Saga 849-8501, Japan.
[Ti] Título:Presynaptic facilitation by tetracaine of glutamatergic spontaneous excitatory transmission in the rat spinal substantia gelatinosa - Involvement of TRPA1 channels.
[So] Source:Brain Res;1657:245-252, 2017 Feb 15.
[Is] ISSN:1872-6240
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The amide-type local anesthetic (LA) lidocaine activates transient receptor potential (TRP) ankyrin-1 (TRPA1) channels to facilitate spontaneous l-glutamate release onto spinal substantia gelatinosa (SG) neurons, which play a crucial role in regulating nociceptive transmission. In contrast, the ester-type LA procaine reduces the spontaneous release of l-glutamate in SG neurons. In order to determine whether TRPA1 activation by LAs is specific to amide-types, we examined the actions of tetracaine, another ester-type LA, and other amide-type LAs on glutamatergic spontaneous excitatory transmission in SG neurons by focusing on TRP activation. Whole-cell patch-clamp recordings were performed on SG neurons of adult rat spinal cord slices at a holding potential of -70mV. Bath-applied tetracaine increased spontaneous excitatory postsynaptic current (sEPSC) frequency in a concentration-dependent manner. Tetracaine activity was resistant to the voltage-gated Na -channel blocker tetrodotoxin, the TRP vanilloid-1 antagonist capsazepine, and the TRP melastatin-8 antagonist BCTC, but was inhibited by the non-selective TRP antagonist ruthenium red and the TRPA1 antagonist HC-030031. With respect to amide-type LAs, prilocaine had a tendency to increase sEPSC frequency, while ropivacaine and levobupivacaine reduced the frequency. In conclusion, tetracaine facilitated spontaneous l-glutamate release from nerve terminals by activating TRPA1 channels in the SG, resulting in an increase in the excitability of SG neurons. TRPA1 activation was not specific to amide-type or ester-type LAs. The facilitatory action of LAs may be involved in pain occurring after recovery from spinal anesthesia.
[Mh] Termos MeSH primário: Ácido Glutâmico/metabolismo
Neurotransmissores/farmacologia
Terminações Pré-Sinápticas/efeitos dos fármacos
Substância Gelatinosa/efeitos dos fármacos
Canais de Cátion TRPC/metabolismo
Tetracaína/farmacologia
[Mh] Termos MeSH secundário: Acetanilidas/farmacologia
Amidas/farmacologia
Anestésicos Locais/farmacologia
Animais
Bupivacaína/análogos & derivados
Bupivacaína/farmacologia
Capsaicina/análogos & derivados
Capsaicina/farmacologia
Potenciais Pós-Sinápticos Excitadores/efeitos dos fármacos
Potenciais Pós-Sinápticos Excitadores/fisiologia
Masculino
Dor/metabolismo
Técnicas de Patch-Clamp
Terminações Pré-Sinápticas/metabolismo
Prilocaína/farmacologia
Purinas/farmacologia
Pirazinas/farmacologia
Piridinas/farmacologia
Ratos Sprague-Dawley
Rutênio Vermelho/farmacologia
Substância Gelatinosa/metabolismo
Canal de Cátion TRPA1
Tetrodotoxina/farmacologia
Técnicas de Cultura de Tecidos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropylphenyl)acetamide); 0 (Acetanilides); 0 (Amides); 0 (Anesthetics, Local); 0 (N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide); 0 (Neurotransmitter Agents); 0 (Purines); 0 (Pyrazines); 0 (Pyridines); 0 (TRPA1 Cation Channel); 0 (TRPC Cation Channels); 0 (Trpa1 protein, rat); 046O35D44R (Prilocaine); 0619F35CGV (Tetracaine); 11103-72-3 (Ruthenium Red); 3KX376GY7L (Glutamic Acid); 4368-28-9 (Tetrodotoxin); 7IO5LYA57N (ropivacaine); A5H73K9U3W (levobupivacaine); LFW48MY844 (capsazepine); S07O44R1ZM (Capsaicin); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161227
[St] Status:MEDLINE


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[PMID]:27957755
[Au] Autor:Opstrup MS; Sørensen HB; Zachariae C
[Ad] Endereço:Department of Dermato-Allergology, Copenhagen University Hospital Gentofte, 2900, Hellerup, Denmark.
[Ti] Título:Occupational allergic contact dermatitis caused by tetracaine in an otorhinolaryngologist.
[So] Source:Contact Dermatitis;76(1):55-57, 2017 Jan.
[Is] ISSN:1600-0536
[Cp] País de publicação:England
[La] Idioma:eng
[Mh] Termos MeSH primário: Anestésicos Locais/efeitos adversos
Dermatite Alérgica de Contato/etiologia
Dermatite Ocupacional/etiologia
Dermatoses da Mão/induzido quimicamente
Otolaringologia
Tetracaína/efeitos adversos
[Mh] Termos MeSH secundário: Seres Humanos
Masculino
Meia-Idade
Testes do Emplastro
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anesthetics, Local); 0619F35CGV (Tetracaine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170418
[Lr] Data última revisão:
170418
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161214
[St] Status:MEDLINE
[do] DOI:10.1111/cod.12645


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[PMID]:27557558
[Au] Autor:Jalili S; Saeedi M
[Ad] Endereço:Department of Chemistry, K. N. Toosi University of Technology, Tehran, P.O. Box 15875-4416, Iran. sjalili@kntu.ac.ir.
[Ti] Título:Study of procaine and tetracaine in the lipid bilayer using molecular dynamics simulation.
[So] Source:Eur Biophys J;46(3):265-282, 2017 Apr.
[Is] ISSN:1432-1017
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Despite available experimental results, the molecular mechanism of action of local anesthetics upon the nervous system and contribution of the cell membrane to the process are still controversial. In this work, molecular dynamics simulations were performed to investigate the effect of two clinically used local anesthetics, procaine and tetracaine, on the structure and dynamics of a fully hydrated dimyristoylphosphatidylcholine lipid bilayer. We focused on comparing the main effects of uncharged and charged drugs on various properties of the lipid membrane: mass density distribution, diffusion coefficient, order parameter, radial distribution function, hydrogen bonding, electrostatic potential, headgroup angle, and water dipole orientation. To compare the diffusive nature of anesthetic through the lipid membrane quantitatively, we investigated the hexadecane/water partition coefficient using expanded ensemble simulation. We predicted the permeability coefficient of anesthetics in the following order: uncharged tetracaine > uncharged procaine > charged tetracaine > charged procaine. We also shown that the charged forms of drugs are more potent in hydrogen bonding, disturbing the lipid headgroups, changing the orientation of water dipoles, and increasing the headgroup electrostatic potential more than uncharged drugs, while the uncharged drugs make the lipid diffusion faster and increase the tail order parameter. The results of these simulation studies suggest that the different forms of anesthetics induce different structural modifications in the lipid bilayer, which provides new insights into their molecular mechanism.
[Mh] Termos MeSH primário: Anestésicos Locais/metabolismo
Anestésicos Locais/farmacologia
Bicamadas Lipídicas/metabolismo
Procaína/metabolismo
Procaína/farmacologia
Tetracaína/metabolismo
Tetracaína/farmacologia
[Mh] Termos MeSH secundário: Anestésicos Locais/química
Membrana Celular/química
Membrana Celular/efeitos dos fármacos
Membrana Celular/metabolismo
Difusão
Dimiristoilfosfatidilcolina/metabolismo
Bicamadas Lipídicas/química
Conformação Molecular
Simulação de Dinâmica Molecular
Procaína/química
Tetracaína/química
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Lipid Bilayers); 0619F35CGV (Tetracaine); 4Z8Y51M438 (Procaine); U86ZGC74V5 (Dimyristoylphosphatidylcholine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160826
[St] Status:MEDLINE
[do] DOI:10.1007/s00249-016-1164-8


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[PMID]:27436060
[Au] Autor:Cacek AT; Gobburu JV; Gopalakrishnan M
[Ad] Endereço:ContractKinetica, Columbia, MO, USA.
[Ti] Título:Population Pharmacokinetics of an Intranasally Administered Combination of Oxymetazoline and Tetracaine in Healthy Volunteers.
[So] Source:J Clin Pharmacol;57(2):247-254, 2017 Feb.
[Is] ISSN:1552-4604
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The primary objective of the current investigation was to establish the pharmacokinetic characteristics of oxymetazoline and tetracaine's primary metabolite, para-butylaminobenzoic acid (PBBA), after the intranasal administration of oxymetazoline/tetracaine. Thirty-six subjects contributing a total of 1791 plasma concentration results from 2 open-label trials were utilized. Model development was achieved using data from the second trial (N = 24) in which 0.3 mg oxymetazoline/18 mg tetracaine was administered. External model validation utilized data from the first trial (N = 12), which included doses of 0.3 mg oxymetazoline/18 mg tetracaine and 0.6 mg oxymetazoline/36 mg tetracaine. Oxymetazoline and PBBA dispositions were described by a 2-compartment model with first-order absorption. An allometric model for body weight was included on volumes and clearances to describe unexplained between-subject variability. The final oxymetazoline parameter estimates were k 4.41 h ; peripheral volume 418 L; clearance 66.4 L/h; central volume 6.97 L; and intercompartmental clearance 419 L/h for a 70-kg subject. The final PBBA parameter estimates were k 8.51 h ; peripheral volume 32.0 L; clearance 16.7 L/h; central volume 29.8 L; and intercompartmental clearance 2.43 L/h for a 70-kg subject. Between-subject variability ranged from 14% to 39% for oxymetazoline and from 10% to 94% for PBBA.
[Mh] Termos MeSH primário: Anestésicos Locais/farmacocinética
Descongestionantes Nasais/farmacocinética
Oximetazolina/farmacocinética
Tetracaína/farmacocinética
[Mh] Termos MeSH secundário: Administração Intranasal
Adulto
Algoritmos
Anestésicos Locais/administração & dosagem
Biotransformação
Combinação de Medicamentos
Feminino
Voluntários Saudáveis
Seres Humanos
Masculino
Descongestionantes Nasais/administração & dosagem
Sprays Nasais
Oximetazolina/administração & dosagem
População
Tetracaína/administração & dosagem
Adulto Jovem
para-Aminobenzoatos/sangue
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Drug Combinations); 0 (Nasal Decongestants); 0 (Nasal Sprays); 0 (para-Aminobenzoates); 0619F35CGV (Tetracaine); 4740-24-3 (4-n-butylaminobenzoic acid); 8VLN5B44ZY (Oxymetazoline)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170816
[Lr] Data última revisão:
170816
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160721
[St] Status:MEDLINE
[do] DOI:10.1002/jcph.799


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[PMID]:27377616
[Au] Autor:Greveling K; Prens EP; Ten Bosch N; van Doorn MB
[Ad] Endereço:Department of Dermatology, Erasmus MC University Medical Centre Rotterdam, Rotterdam, the Netherlands.
[Ti] Título:Comparison of lidocaine/tetracaine cream and lidocaine/prilocaine cream for local anaesthesia during laser treatment of acne keloidalis nuchae and tattoo removal: results of two randomized controlled trials.
[So] Source:Br J Dermatol;176(1):81-86, 2017 Jan.
[Is] ISSN:1365-2133
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Pain is a common adverse effect of dermatological laser procedures. Currently, no standard topical anaesthetic cream exists for deeper dermal laser procedures. OBJECTIVES: To compare the efficacy of lidocaine/tetracaine cream and lidocaine/prilocaine cream in reducing self-reported pain during deeper dermal laser treatment of acne keloidalis nuchae (AKN) and tattoos. METHODS: We conducted two randomized, double-blind, controlled clinical trials with intrapatient, split-lesion designs: study A included patients with AKN (n = 15); study B included patients with black tattoos (n = 15). The primary end point was the patients' self-reported pain on a 10-cm visual analogue scale (VAS). Secondary objectives were the percentage of patients with adequate pain relief, willingness to pay €25 for the cream that provided the best pain relief and safety of the creams. RESULTS: In both studies, VAS scores were lower for lidocaine/prilocaine cream, with a mean VAS difference in study A of 1·9 [95% confidence interval (CI) 1·0-2·8] and in study B of 0·6 (95% CI -0·7 to 1·9). In study A, adequate pain relief was achieved in 13% (n = 2) with lidocaine/tetracaine cream vs. 73% (n = 11) with lidocaine/prilocaine cream (P = 0·004), and in study B in 53% (n = 8) vs. 80% (n = 12), respectively (P = 0·289). In study A, 47% (n = 7) were willing to pay an additional €25 vs. 73% (n = 11) in study B. No serious adverse events occurred. CONCLUSIONS: Lidocaine/prilocaine cream under plastic occlusion is the preferred topical anaesthetic during painful laser procedures targeting dermal chromophores.
[Mh] Termos MeSH primário: Acne Queloide/terapia
Dor Aguda/prevenção & controle
Anestésicos Combinados/administração & dosagem
Anestésicos Locais/administração & dosagem
Terapia a Laser/efeitos adversos
Tatuagem
[Mh] Termos MeSH secundário: Adulto
Técnicas Cosméticas
Método Duplo-Cego
Feminino
Seres Humanos
Terapia a Laser/métodos
Lidocaína/administração & dosagem
Masculino
Prilocaína/administração & dosagem
Tetracaína/administração & dosagem
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Anesthetics, Combined); 0 (Anesthetics, Local); 046O35D44R (Prilocaine); 0619F35CGV (Tetracaine); 98PI200987 (Lidocaine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171003
[Lr] Data última revisão:
171003
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160706
[St] Status:MEDLINE
[do] DOI:10.1111/bjd.14848


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[PMID]:27145989
[Au] Autor:Liu D; Peng J; Liu S; Zhou M; Zhang J; Li A
[Ad] Endereço:Education Ministry Key Laboratory on Luminescence and Real-Time Analysis, Chemistry and Chemical Engineering, Southwest University, Chongqing, People's Republic of China.
[Ti] Título:Resonance Rayleigh scattering technique as a detection method for the RP-HPLC determination of local anaesthetics in human urine.
[So] Source:Luminescence;32(1):4-10, 2017 Feb.
[Is] ISSN:1522-7243
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A highly selective and sensitive method of reversed phase high-performance liquid chromatography (RP-HPLC) coupled with resonance Rayleigh scattering (RRS) was developed for the determination of procaine, bupivacaine and tetracaine. Separation of three local anaesthetics was achieved at 35 °C on a C column. The mobile phase was 30: 70 (v/v) acetonitrile/triethylamine-phosphoric acid buffer (pH 2.9) at flow rate of 0.3 mL/min. The RRS detection was conducted by taking advantage of the strong RRS enhancement of the local anaesthetics with erythrosine reaction in an acidic medium. Under optimum conditions, the limit of detection (S/N = 3) values were in the range of 2.4-11.2 ng/mL. Recoveries from spiked human urine samples were 95.8%-104.5%. The proposed method applied to the determination of local anaesthetics in human urine achieved satisfactory results. In addition, the mechanism of the reaction is fully discussed. Copyright © 2016 John Wiley & Sons, Ltd.
[Mh] Termos MeSH primário: Anestésicos Locais/urina
Bupivacaína/urina
Procaína/urina
Tetracaína/urina
[Mh] Termos MeSH secundário: Cromatografia Líquida de Alta Pressão
Seres Humanos
Espalhamento de Radiação
Espectrometria de Fluorescência
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anesthetics, Local); 0619F35CGV (Tetracaine); 4Z8Y51M438 (Procaine); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170421
[Lr] Data última revisão:
170421
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160506
[St] Status:MEDLINE
[do] DOI:10.1002/bio.3140



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