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1.
AAPS PharmSciTech ; 20(8): 322, 2019 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-31650263

RESUMO

The objectives of this work were to prepare a 5 wt% lidocaine-diclofenac ionic liquid drug-loaded gelatin/poly(vinyl alcohol) transdermal patch using a freeze/thaw method and to evaluate its physicochemical properties, in vitro release of lidocaine and diclofenac, and stability test. The lidocaine-diclofenac ionic liquid drug was produced by the ion pair reaction between the hydrochloride salts of lidocaine and the sodium salts of diclofenac. The thermal properties of the final drug product were significantly changed from the primary drugs. The ionic liquid drug could be dissolved in water and mixed in a polymer solution. The resulting transdermal patch was then exposed to 10 cycles of freezing and thawing preparation at - 20°C for 8 h and at 25°C for 4 h, respectively. As a result, it was found that the lidocaine-diclofenac ionic liquid drug-loaded transdermal patch showed good physicochemical properties and could feasibly be used in pharmaceutical applications. The lidocaine-diclofenac ionic liquid drug was not affected by the properties of the transdermal patch due to the lack of chemical interaction between polymer base and drug. The high drug release values of both lidocaine and diclofenac were controlled by the gelatin/poly(vinyl alcohol) transdermal patch. The patch showed good stability over the study period of 3 months when kept at 4°C or under ambient temperature.


Assuntos
Diclofenaco/farmacocinética , Gelatina/farmacocinética , Líquidos Iônicos/farmacocinética , Lidocaína/farmacocinética , Álcool de Polivinil/farmacocinética , Adesivo Transdérmico , Administração Cutânea , Anestésicos Locais/química , Anestésicos Locais/farmacocinética , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacocinética , Preparações de Ação Retardada/química , Preparações de Ação Retardada/farmacocinética , Diclofenaco/química , Combinação de Medicamentos , Liberação Controlada de Fármacos , Congelamento , Gelatina/química , Líquidos Iônicos/química , Lidocaína/química , Álcool de Polivinil/química
2.
Rev. cient. Esc. Univ. Cienc. Salud ; 6(1): 36-46, ene.-jun. 2019. tab
Artigo em Espanhol | LILACS | ID: biblio-1023753

RESUMO

Los anestésicos locales han cambiado de manera destacada la historia y la práctica de la medicina, la evolución en los métodos de desarrollo de anestésicos ha hecho posible el desarrollo de anestésicos convencionales para uso común en procedimientos médicos quirúrgicos locales, hablando en especial de dos anestésicos que se utilizan diariamente en los diferentes niveles de atención de salud mundial, la lidocaína y posteriormente la lidocaína con epinefrina. Es por el uso cotidiano de estos anestésicos que ahora es posible hacer procedimientos menores en los pacientes sin exponer a los mismos al dolor de los procedimientos propiamente dicho o la causa de dolor no procedimental. Se utiliza cada uno de acuerdo al efecto deseado que se requiera en el paciente, teniendo en cuenta las diversas precaucio-nes dada la potencial toxicidad que poseen, así como la técnica que se va a utilizar. En este artículo de revisión bibliográfica, se presentan las generalidades de ambos anestésicos, las indicaciones, precauciones, efectos adversos y comparación de toxici-dad entre ambos anestésicos. Esta revisión bibliográfica se realizó a partir de 36 artícu-los tomando como referencia los siguientes: literatura médica, artículos de revistas cien-tíficas y otras revisiones bibliográficas menores de 5 años de haber sido publica-dos o aquellos con relevancia histórica...(AU)


Assuntos
Humanos , Epinefrina/farmacologia , Anestésicos Locais , Lidocaína/farmacocinética , Revisão
3.
J Pharm Pharmacol ; 71(8): 1282-1290, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31134628

RESUMO

OBJECTIVES: Rectus sheath blocks are an established option for analgesia following abdominal surgery, but pharmacokinetic data are limited. This study sought to characterise the absorption of lidocaine injectate and the pharmacokinetics of lidocaine after rectus sheath injection. METHODS: Bilateral rectus sheath single-injection blocks were given to 10 patients undergoing general or urological surgery. Afterwards, serial lidocaine serum levels and ultrasound measurements of the rectus sheath injectate reservoir were collected. KEY FINDINGS: Injectate within the rectus sheath was visible with ultrasound up to 12 h after injection. However, the rate of drug absorption exceeded that of injectate disappearance. Peak serum concentration occurred within 30 min with average peak concentrations of 1.65 µg/ml. Lidocaine clearance was lower than reported in young healthy subjects. The body mass index positively correlated with lidocaine terminal phase half-life, and clearance negatively correlated with age. CONCLUSIONS: The study provides the first data describing lidocaine pharmacokinetics after rectus sheath injection. Peak serum concentrations transiently achieved systemic levels associated with pain relief after a single bolus injection. The data from this study could be used to develop a regime using single shot rectus sheath blockade with a bolus of lidocaine followed by infusion using bilateral rectus sheath catheters.


Assuntos
Dor Abdominal/tratamento farmacológico , Parede Abdominal/diagnóstico por imagem , Lidocaína/sangue , Reto do Abdome/efeitos dos fármacos , Adulto , Idoso , Idoso de 80 Anos ou mais , Analgesia/métodos , Anestésicos Locais , Índice de Massa Corporal , Feminino , Voluntários Saudáveis , Humanos , Injeções , Lidocaína/farmacocinética , Masculino , Pessoa de Meia-Idade , Bloqueio Nervoso/métodos , Manejo da Dor/métodos
5.
A A Pract ; 13(3): 96-98, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-30920426

RESUMO

Intravenous lidocaine is increasingly being utilized as an opioid-sparing analgesic. A 55-year-old man with well-controlled human immunodeficiency virus on highly active antiretroviral therapy was prescribed a lidocaine infusion at 1 mg/kg/h for postoperative pain. On postoperative day 2, the patient experienced 4 unresponsive episodes with tachycardia, hypertension, and oxygen desaturation. Serum lidocaine level was available 2 days later (high 6.3 µg/mL, therapeutic range 2.5-3.5 µg/mL). There is significant pharmacokinetic interaction between lidocaine and this patient's human immunodeficiency virus medications. This case highlights the need for a readily accessible list of medications that caution against lidocaine. We propose in-house serum lidocaine levels to monitor patients at an increased risk for toxicity.


Assuntos
Anestésicos/efeitos adversos , Lidocaína/efeitos adversos , Dor Pós-Operatória/tratamento farmacológico , Anestésicos/sangue , Anestésicos/farmacocinética , Fármacos Anti-HIV/farmacocinética , Fármacos Anti-HIV/uso terapêutico , Terapia Antirretroviral de Alta Atividade , Infecções por HIV/tratamento farmacológico , Humanos , Infusões Intravenosas , Lidocaína/sangue , Lidocaína/farmacocinética , Masculino , Pessoa de Meia-Idade , Período Perioperatório
6.
Rev. Soc. Esp. Dolor ; 26(1): 14-20, ene.-feb. 2019. tab, graf
Artigo em Espanhol | IBECS | ID: ibc-182831

RESUMO

Introducción: El dolor es un motivo de ausentismo laboral, en especial el dolor irruptivo secundario a canal lumbar estrecho. La dexmedetomidina como analgésico actúa inhibiendo la liberación de sustancia P en la vía nociceptiva y bloquea los receptores de aspartato y glutamato. Por otro lado, la lidocaína también previene y alivia el dolor mediante la interrupción de la neuroconducción, uniéndose a su receptor específico dentro de los canales de sodio. Objetivo: Evaluar la eficacia analgésica de la dexmedetomidina versus lidocaína en perfusión endovenosa como tratamiento del dolor irruptivo secundario a canal lumbar estrecho. Material y métodos: Ensayo clínico controlado, aleatorizado, triple ciego, realizado en la clínica del dolor del HGM, se evaluaron dos grupos de pacientes con diagnóstico de dolor irruptivo secundario a canal lumbar estrecho; un grupo tratado con dexmedetomidina (0,3 mcg/kg) y otro grupo tratado con lidocaína (2 mg/kg) en perfusión endovenosa. Se realizó medición de la intensidad del dolor y el estado de sedación antes de iniciar el tratamiento y posteriormente a los 30, 60 y 120 minutos. También se evaluó la funcionalidad de los pacientes a través del índice de discapacidad de Oswestry antes y a los siete días del tratamiento. Se evaluó de forma secundaria el efecto de los tratamientos sobre los signos vitales. Resultados: No hubo diferencia estadísticamente significativa en la reducción de la intensidad del dolor a los 120 minutos entre los pacientes tratados con dexmedetomidina (EVA 1,29 ± 1,63) comparados con los tratados con lidocaína (EVA 1 ± 1,19, p = 0,594). Se observó que al final de la perfusión de los fármacos, la dexmedetomidina produjo mayor sedación a diferencia de la lidocaína (p = 0,003). Ambos tratamientos mejoran la funcionalidad en todos los pacientes sin haber diferencia estadísticamente significativa entre los tratamientos (p = 0,508) no se observaron efectos depresores sobre los signos vitales. Conclusiones: La dexmedetomidina y la lidocaína son igual de eficaces para el tratamiento del dolor irruptivo, con inicio de acción en los primeros 30 minutos de iniciada la perfusión hasta las siguientes 2 horas. No se observaron eventos adversos medicamentosos a las dosis recomendadas


Introduction: The pain is a reason for absenteeism labour, especially breakthrough pain secondary to narrow lumbar canal. Dexmedetomidine is an analgesic, act by inhibiting the release of substance P in the nociceptive pathway and blocks the aspartate and glutamate receptors. On the other hand, lidocaine also prevents and relieves pain by interrupting neuroconduction, binding to its specific receptor within the sodium channels. Objective: To evaluate the analgesic efficacy of dexmedetomidine versus lidocaine in intravenous perfusion as a treatment for breakthrough pain secondary to narrow lumbar canal. Material and methods: Controlled clinical trial, randomized, triple-blind, performed at the HGM pain clinic, two groups of patients with diagnosis of breakthrough pain secondary to narrow lumbar canal were evaluated; group one was treated with dexmedetomidine (0.3 mcg/kg) and the other group was treated with lidocaine (2 mg/kg) in intravenous infusion. Measurement of pain intensity and sedation status was made before starting the treatment and after 30, 60 and 120 minutes. The functionality of the patients was also assessed through the Oswestry disability index before and seven days after treatment. Secondarily evaluated the effect of treatments on vital signs. Results: There was not any statistically significant difference in the reduction of pain intensity at 120 minutes between patients treated with dexmedetomidine (EVA 1.29 ± 1.63) compared with those who were treated with lidocaine (EVA 1 ± 1.19, p = 0.594), it was observed that at the end of drugs perfusion, dexmedetomidine produced greater sedation, unlike lidocaine (p = 0.003), both treatments improved functionality in all patients without having a statistically significant difference between treatments (p = 0.508), they were not observed depressant effects on vital signs. Conclusions: Dexmedetomidine and lidocaine are just as equally effective for the treatment of breakthrough pain, with onset of action in the first 30 minutes after the infusion started until the next 2 hours, no adverse drug events were observed at the recommended doses


Assuntos
Humanos , Masculino , Feminino , Adulto , Pessoa de Meia-Idade , Idoso , Idoso de 80 Anos ou mais , Dexmedetomidina/farmacocinética , Lidocaína/farmacocinética , Dor Irruptiva/tratamento farmacológico , Dor Lombar/tratamento farmacológico , Manejo da Dor/métodos , Administração Intravenosa/métodos , Constrição Patológica/tratamento farmacológico , Resultado do Tratamento
7.
Oral Maxillofac Surg ; 22(4): 457-461, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30327982

RESUMO

PURPOSE: To determine the quantity of dexamethasone plasma concentration achieved following intrapterygomandibular space injection of dexamethasone when co-administered with inferior alveolar nerve block correlating with the clinical effects in the postoperative phase. OBJECTIVE: A preliminary prospective study to evaluate the dexamethasone plasma concentration achieved following intrapterygomandibular space injection of dexamethasone with 2% lignocaine inferior alveolar nerve block to achieve hemi-mandibular anesthesia for minor oral surgical procedures and derive clinical correlations. BACKGROUND: Dexamethasone is a glucocorticoid, chiefly used for the management of postsurgical sequelae like trismus and swelling in maxillofacial surgical practice. Conventionally, parenteral dexamethasone is administered via intravenous or intramuscular route. Intrapterygomandibular space injection is a novel route of steroid delivery described in literature. For minor oral surgical procedures in maxillofacial surgical practice requiring inferior alveolar nerve block, dexamethasone can be administered along with local anesthetic through a single injection as a mixture (twin mix). METHODS: Prospective double-blind randomized clinical trial was designed to evaluative plasma concentration of dexamethasone achieved following injection of a freshly prepared mixture of 1.8 ml of 2% lignocaine with adrenaline (1:200000) and 1 ml (4 mg) dexamethasone [2.8 ml solution of twin mix] in the pterygomandibular space. The 30 candidates included for the trial were randomly split into three study groups (ten each)-(1) control group (C); (2) intramuscular group (IM); (3) intraspace group (IS). RESULTS: The mean plasma dexamethasone concentration at 30 min postinjection in group IM was 226.41 ± 48.67 ng/ml and for IS group it was 209.67 ± 88.13 ng/ml. Post hoc (Bonferroni-Holm test) intergroup comparison for plasma dexamethasone concentration (IM and IS) was found statistically insignificant (P = 0.605). CONCLUSION: Intraspace route of drug administration can be utilized to deliver dexamethasonized local anesthetics safely with predictable clinical effects in the patients requiring mandibular minor oral surgery under local anesthesia.


Assuntos
Adjuvantes Anestésicos/administração & dosagem , Anestésicos Locais/administração & dosagem , Dexametasona/administração & dosagem , Lidocaína/administração & dosagem , Nervo Mandibular , Bloqueio Nervoso/métodos , Adjuvantes Anestésicos/sangue , Adjuvantes Anestésicos/farmacocinética , Adulto , Anestésicos Locais/sangue , Anestésicos Locais/farmacocinética , Dexametasona/sangue , Dexametasona/farmacocinética , Método Duplo-Cego , Feminino , Humanos , Injeções , Lidocaína/sangue , Lidocaína/farmacocinética , Masculino , Mandíbula , Músculos Pterigoides
8.
Curr Drug Deliv ; 15(10): 1411-1416, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30207229

RESUMO

BACKGROUND: Effective postoperative pain control is essential for the recovery of surgical patients. However, long-term analgesia can seldom be achieved with the existing medications. The injectable implants prepared by biodegradable polyesters can be conveniently used during the surgery and slowly release analgesics near the operative incision for a long period. METHOD: In this study, we prepared lidocaine hydrochloride (Lido-HCl)-loaded injectable poly(lacticco- glycolic acid) (PLGA) implants for prolonged analgesia. The optimized formulation of this injectable implant sustained drug release for up to 5 days, with a cumulative release of 85.8%±1.9% in the in vitro release experiment. RESULTS: The in vivo release of the implants in rats showed good consistency with the in vitro release. The pharmacokinetics of Lido-HCl implants in the thigh muscle of rats was evaluated, and the AUC0-120 h of the Lido-HCl implant was 11.4 times that of Lido-HCl solution, indicating a good sustained release function of the implant. The pharmacodynamics of Lido-HCl implants was measured by the hot plate test. The Lido-HCl solution blocked the sciatic nerve of rats for less than 4 h, while the Lido-HCl implant efficiently blocked the nerve for approximately 120 h. CONCLUSION: These results demonstrated that the PLGA-based injectable implant is a suitable carrier for postoperative pain control.


Assuntos
Anestésicos Locais/uso terapêutico , Implantes de Medicamento/uso terapêutico , Lidocaína/uso terapêutico , Dor Pós-Operatória/tratamento farmacológico , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/uso terapêutico , Anestésicos Locais/administração & dosagem , Anestésicos Locais/farmacocinética , Animais , Implantes de Medicamento/administração & dosagem , Implantes de Medicamento/farmacocinética , Injeções Intramusculares , Lidocaína/administração & dosagem , Lidocaína/farmacocinética , Masculino , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/administração & dosagem , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/farmacocinética , Ratos , Ratos Sprague-Dawley
9.
Drugs ; 78(12): 1229-1246, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30117019

RESUMO

Lidocaine is an amide local anaesthetic initially used intravenously as an antiarrhythmic agent. At some point it was proposed that intravenous lidocaine (IVL) had an analgesic effect that could be potentially beneficial in perioperative settings. Since these preliminary reports, a large body of evidence confirmed that IVL had anti-inflammatory and opiate-sparing effects, a combination of characteristics leading to an array of effects such as a decrease in postoperative pain and opiate consumption, and a reduction in the duration of digestive ileus. Additional studies demonstrated IVL to possess antithrombotic, antimicrobial and antitumoral effects. Beneficial effects of IVL have been characterized in abdominal surgery but remain controversial in other types of surgeries. Because the quality of evidence was limited, due to inconsistency, imprecision and study quality, recent conclusions from meta-analysis pooling together all types of surgery stated the uncertainty about IVL benefits. Additional indications such as the prevention of propofol-induced injection pain, prevention of hyperalgesia, protection against bronchial reactivity by bronchotracheal relaxation during surgery, and the increase in depth of general anaesthesia have since emerged. IVL is rapidly distributed in the body and metabolized by the liver. With the commonly recommended doses, lidocaine's therapeutic index remains very high and the plasma concentrations stay largely below the cardiotoxic and neurotoxic threshold levels, a notion that may be used by clinicians to draw conclusions on the benefit-risk profile of IVL in comparison to other analgesic strategies. The purpose of this review is to address the pharmacokinetic and pharmacodynamic properties of lidocaine in healthy and pathological conditions.


Assuntos
Analgésicos/uso terapêutico , Anestésicos Locais/uso terapêutico , Lidocaína/uso terapêutico , Dor Pós-Operatória/tratamento farmacológico , Administração Intravenosa , Analgésicos/farmacocinética , Analgésicos/farmacologia , Analgésicos Opioides/uso terapêutico , Anestésicos Locais/farmacocinética , Anestésicos Locais/farmacologia , Animais , Humanos , Hiperalgesia/prevenção & controle , Lidocaína/farmacocinética , Lidocaína/farmacologia , Período Perioperatório , Resultado do Tratamento
10.
J Vet Pharmacol Ther ; 41(6): 825-837, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30028024

RESUMO

Intravenous (iv), subcutaneous (sq), and topical (tp) lidocaine was administered to six horses in a cross-over, randomized design study. Samples were collected for up to 72 hr. Compartmental models were used to investigate the pharmacokinetics of (LD) and its metabolites 3-hydroxylidocaine (3-OH), 4-hydroxylidocaine (4-OH), and monoethylglycinexylidide (MEGX). Metabolites 3-OH and 4-OH were present in conjugated forms, whereas LD and metabolite MEXG were present primarily in the un-conjugated form. Plasma concentrations of LD after iv administration (100 mg) were described by three-compartment model with an additional three compartments to describe the elimination of metabolites. Median (range) elimination micro-constants (Ke ) for LD, 3-OH, 4-OH, and MEXG were 4.12 (2.62-6.23), 1.25 (1.10-2.15), 1.79 (1.22-2.39), and 1.69 (1.03-1.99)/hr, respectively. Median (range) values of alpha (t½α ), beta (t½ß ), and gamma (t½Î³ ) half-lives were 0.08 (0.07-0.13), 0.57 (0.15-1.25), and 4.11 (0.52-7.36) hr. Plasma concentrations of LD after sq (200 mg) administration were described by absorption and two-compartment elimination model. The median (range) of the LD absorption half-life (t½ab ) was 0.47 (0.29-0.61) hr. The Ke for LD, 3-OH, 4-OH, and MEXG was 3.91 (1.48-9.25), 1.00 (0.78-1.08), 1.76 (0.96-2.11), and 1.13 (0.69-1.33)/hr. The median (range) of t½α and t½ß was 0.15 (0.06-0.27) and 3.04 (2.53-6.39) hr. Plasma concentrations of LD after tp (400 mg) application were described by one-compartment model with a t½ab of 8.49 (5.16-11.80) hr. The Ke for LD, 3-OH, and MEXG was 0.24 (0.10-0.81), 0.41 (0.08-0.93), and 0.38 (0.26-1.14)/hr.


Assuntos
Anestésicos Locais/farmacocinética , Cavalos/metabolismo , Lidocaína/análogos & derivados , Lidocaína/farmacocinética , Anestésicos Locais/administração & dosagem , Animais , Área Sob a Curva , Estudos Cross-Over , Vias de Administração de Medicamentos , Feminino , Meia-Vida , Cavalos/sangue , Lidocaína/administração & dosagem , Lidocaína/farmacologia , Masculino , Distribuição Aleatória
11.
Rev Esp Anestesiol Reanim ; 65(10): 589-592, 2018 Dec.
Artigo em Inglês, Espanhol | MEDLINE | ID: mdl-30001858

RESUMO

Erector spinae plane block (ESPB) as postoperative analgesia method has been successfully carried out in several surgical interventions. Postoperative pain treatment for cesarean section is considered one of the important challenges for anesthesiologists due to the risk of chronic pain development and even pospartum depression. Regional anesthesia techniques were effectively used to prevent the pain together with multimodal analgesia regimes in cesarean section. Formerly, successful erector spinae plane block was documented as postoperative analgesia treatment for cesarean section; however, no motor weakness was recorded as a side effect. In this case report, we present an unexpected motor weakness as a side effect of the erector spinae plane block after cesarean delivery operation in a 29 year old patient. To our knowledge, this is the first report of motor weakness related to the ESPB.


Assuntos
Analgesia Obstétrica/efeitos adversos , Transtornos Neurológicos da Marcha/etiologia , Debilidade Muscular/etiologia , Bloqueio Nervoso/efeitos adversos , Músculos Paraespinais/efeitos dos fármacos , Adulto , Bupivacaína/efeitos adversos , Bupivacaína/farmacocinética , Cesárea/efeitos adversos , Difusão , Feminino , Humanos , Leiomioma/cirurgia , Lidocaína/efeitos adversos , Lidocaína/farmacocinética , Plexo Lombossacral/efeitos dos fármacos , Plexo Lombossacral/fisiopatologia , Bloqueio Nervoso/métodos , Dor Pós-Operatória/prevenção & controle , Músculos Paraespinais/inervação , Músculos Paraespinais/fisiopatologia , Gravidez , Complicações Neoplásicas na Gravidez/cirurgia , Ultrassonografia de Intervenção , Neoplasias Uterinas/cirurgia
12.
Int J Dermatol ; 57(11): 1335-1343, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29978889

RESUMO

BACKGROUND: Lidocaine Hydrochloride (HCL) is one of the commonest topical local anesthetic drugs. The permeation of the lidocaine can be enhanced by iontophoresis (IOP). The purpose of this study was to evaluate the permeability of 2.5 and 5% lidocaine permeation in ex vivo human skin using different IOP waveform. METHODS: Continuous and modulated IOP at the current density of 0.5 mA/cm2 were applied across human skin (n = 3) in donor chamber of vertical diffusion cell at 2.5 and 5% lidocaine concentration. High Performance Liquid Chromatography was used to determine lidocaine concentration. RESULTS: Findings revealed that lidocaine concentration increased effectively in a time-dependent manner in both modulated and continuous IOP at 2.5 and 5% lidocaine concentration. Compared to the passive group, the flux of lidocaine with modulated and continuous IOP were higher of about six and ten-fold, respectively. However, no significant difference was observed between continuous and modulated IOP groups at both lidocaine concentrations. At 2.5% lidocaine concentration, the permeation time taken by modulated and continuous IOP to attain therapeutic levels of 142 and 164 µg/cm2 , respectively, was approximately 10 minutes. At 5% lidocaine, the therapeutic permeation of 129 and 147 µg/cm2 , respectively, was achieved at approximately 5 minutes after applying iontophoresis waveform. CONCLUSION: Study shows that modulated IOP can be a promising alternative method in clinical settings aside from continuous IOP. Based on the clinical requirements, IOP can be used at 2.5 and 5% lidocaine concentration depending on need of relatively short or very short onset action.


Assuntos
Anestésicos Locais/farmacocinética , Iontoforese/métodos , Lidocaína/farmacocinética , Pele/metabolismo , Anestésicos Locais/administração & dosagem , Humanos , Lidocaína/administração & dosagem , Permeabilidade , Fatores de Tempo
13.
Biomed Chromatogr ; 32(10): e4322, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29934999

RESUMO

A sensitive HPLC-MS/MS method was established for the quantification of ceftriaxone sodium (CFT) and lidocaine HCl (LDC) in human plasma utilizing cefixime (CFX) and tadalafil (TDA) as internal standards. The analytes were extracted from human plasma by protein precipitation using acetonitrile. Chromatographic separation was performed on Kinetex C18 (50.0 × 4.6 mm, 5 µm particle size) column with methanol-0.01 M ammonium acetate pH 6.4 (70: 30, v/v) as mobile phase. Multiple reaction monitoring involving the transitions 555.10 → 396.20, 235.20 → 86.00, 454.20 → 284.80 and 390.20 → 268.20 was utilized to quantify CFT, LDC, CFX and TDA, respectively, using a triple quadrupole mass spectrometer which was operated in positive ion mode. The method revealed linearity in the concentration range of 3.0-300.0 µg/mL for CFT and 3.0-300.0 ng/mL for LDC. The validation of the method was achieved in accordance to the US Food and Drug Administration guidelines. A pharmacokinetic study was performed on healthy Egyptian volunteers after intramuscular injection of sterile ceftriaxone sodium (1 g CFT dissolved in 3.5 mL of 1% LDC) after approval from the ethics committee. The pharmacokinetic parameters were: Cmax 141.15 ± 39.84 (µg/mL) and 55.02 ± 9.36 (ng/mL); tmax (h) 2.50 ± 0.50 and 1.5 ± 0.50; t½ (h) 7.30 ± 2.98 and 4.23 ± 1.96; and Kel (h-1 ) 0.10 ± 0.04 and 0.20 ± 0.13 for CFT and LDC, respectively.


Assuntos
Ceftriaxona/sangue , Ceftriaxona/farmacocinética , Cromatografia Líquida de Alta Pressão/métodos , Lidocaína/sangue , Lidocaína/farmacocinética , Espectrometria de Massas em Tandem/métodos , Ceftriaxona/administração & dosagem , Ceftriaxona/química , Estabilidade de Medicamentos , Humanos , Injeções Intramusculares , Lidocaína/administração & dosagem , Lidocaína/química , Modelos Lineares , Reprodutibilidade dos Testes , Sensibilidade e Especificidade
14.
Eur J Clin Pharmacol ; 74(10): 1309-1315, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29909577

RESUMO

PURPOSE: Tumescent lidocaine anesthesia (TLA) is an opportunity to perform mastectomy for breast cancer without general anesthesia in elderly women. Few reports are available on the pharmacokinetics of lidocaine in a context of TLA during a unilateral mastectomy. The aim of this study was to describe lidocaine pharmacokinetics in elderly women undergoing breast cancer surgery after TLA and to explore the risk of the toxicity of this technique. METHODS: A prospective study was conducted to examine the pharmacokinetics of lidocaine in women undergoing TLA. TLA consists of an intradermal lidocaine instillation (20 mL, 1% [200 mg]) followed by a tumescent lidocaine infiltration (100 mL of 1% lidocaine [1000 mg] and 0.5 mg epinephrine to 1 L Ringer's lactate) via an infusion pump. A population pharmacokinetic (popPK) analysis was performed using the nonlinear mixed effects model (NONMEM). RESULTS: The analysis included 116 observations from 17 women with a median (range) age of 83.4 (60.5-90.0). The median tumescent lidocaine dose was 800 mg (range 375-1000 mg) infused over 48.0 ± 11.0 min. A one-compartment disposition model with first order absorption, two input compartments, and a central elimination best described the pharmacokinetics of lidocaine. The estimates (between subject variability; relative standard error, %) of apparent volume, apparent clearance, tumescent absorption rate, and instillation absorption rate were 195.0 (46.3; 14.5%) L, 24.7 (48.9; 13.3%) L h-1, 0.28 (39.6; 13.8%) h-1, and 2.56 (135.3; 44.9%) h-1, respectively. CONCLUSIONS: This is the first popPK model developed to describe kinetic profiles of TLA. These findings confirm the slow diffusion of lidocaine from the tumescent deposit.


Assuntos
Anestésicos Locais/administração & dosagem , Lidocaína/administração & dosagem , Mastectomia/métodos , Modelos Biológicos , Idoso , Idoso de 80 Anos ou mais , Anestésicos Locais/farmacocinética , Neoplasias da Mama/cirurgia , Epinefrina/administração & dosagem , Feminino , Humanos , Bombas de Infusão , Lidocaína/farmacocinética , Pessoa de Meia-Idade , Dinâmica não Linear , Estudos Prospectivos
15.
J Chromatogr B Analyt Technol Biomed Life Sci ; 1087-1088: 158-172, 2018 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-29747144

RESUMO

Sensitive LC-MS/MS methods were developed to measure lidocaine and its metabolite 2,6-dimethylaniline (2,6-DMA) with application to transdermal studies. The methods for lidocaine in minipig plasma, tissue biopsies, and dermal tapes utilized mixed mode/SCX solid phase extraction, with lower quantitation limits of 25 pg/mL in plasma, 15 ng/g tissue, and 5 ng/tape. 2,6-DMA was measured in plasma and skin tissue homogenates by ultrafiltration and (for tissue) by further derivatization with 4-methoxybenzoyl chloride to form the corresponding benzamide derivative, which extended the lower limit of quantitation to 200 pg/mL. The methods allowed local measurement of lidocaine in stratum corneum, punch biopsies, and plasma and of 2,6-DMA in plasma and biopsies obtained from minipigs dosed with experimental transdermal formulations. Quantitation limits were approximately 7-fold lower than previously reported for lidocaine and 3-fold lower for 2,6-DMA.


Assuntos
Compostos de Anilina/sangue , Cromatografia Líquida de Alta Pressão/métodos , Lidocaína/sangue , Pele/química , Espectrometria de Massas em Tandem/métodos , Adesivos , Administração Cutânea , Compostos de Anilina/administração & dosagem , Compostos de Anilina/análise , Compostos de Anilina/farmacocinética , Animais , Feminino , Lidocaína/administração & dosagem , Lidocaína/análise , Lidocaína/farmacocinética , Modelos Lineares , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Pele/metabolismo , Suínos
16.
J Pharm Biomed Anal ; 154: 1-6, 2018 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-29524770

RESUMO

The application of local anesthetics, usually administered by subcutaneous injection, is common in the course of diagnostic, therapeutic, and cosmetic dermatology procedures. The effective dermal delivery of lidocaine could offer a solution to many adverse effects caused by needle insertion, such as pain, local reactions or toxicity, and additionally, it avoids the disruption of anatomical landmarks. Therefore, novel dermal formulations of local anesthetics are needed to overcome the barrier function of the skin and provide sufficient and prolonged anesthesia. In our study, we aimed to investigate and compare the penetration profiles of four different lidocaine containing formulations (hydrogel, oleogel, lyotropic liquid crystal and nanostructured lipid carrier) by Raman microscopic mapping of the drug. The application of Raman spectroscopy provided information about the spatial distribution of lidocaine in the skin ex vivo. The penetration of lidocaine from lyotropic liquid crystal and nanostructured carrier reached deeper skin layers and a higher amount of the drug was diffused into the skin, compared with hydrogel and oleogel. This study confirmed that nanostructured carriers can improve skin penetration properties of lidocaine and proved the applicability of Raman spectroscopy in the research of dermatological preparations ex vivo as a nondestructive, relatively easy and fast technique.


Assuntos
Anestésicos Locais/administração & dosagem , Portadores de Fármacos/farmacocinética , Lidocaína/administração & dosagem , Absorção Cutânea/efeitos dos fármacos , Pele/metabolismo , Administração Cutânea , Anestésicos Locais/farmacocinética , Química Farmacêutica/métodos , Portadores de Fármacos/química , Estudos de Viabilidade , Feminino , Humanos , Hidrogéis/química , Hidrogéis/farmacocinética , Lidocaína/farmacocinética , Lipídeos/química , Lipídeos/farmacocinética , Nanopartículas/química , Compostos Orgânicos/química , Compostos Orgânicos/farmacocinética , Permeabilidade , Análise Espectral Raman
17.
Headache ; 58(5): 783-789, 2018 05.
Artigo em Inglês | MEDLINE | ID: mdl-29536530

RESUMO

BACKGROUND: Lidocaine, an amide anesthetic, has been used in the treatment of a wide variety of pain disorders for over 75 years. In addition to pain control, lidocaine is an anti-arrhythmic agent and has anti-inflammatory properties. Lidocaine's unique properties, including nonlinear pharmacokinetics, have limited its modern-day use. OBJECTIVE: The purpose of this review is to offer a better understanding of the properties of this unique treatment, which we hope will allow more practitioners to offer this to their patients. METHODS: An analysis of the history, pharmacokinetics, and relevant uses of lidocaine in headache medicine based on a synthesis of the medical literature and clinical experience. RESULTS: Lidocaine is an amide anesthetic that inhibits voltage gated sodium channels, and lidocaine metabolism occurs exclusively in the liver. One lidocaine metabolite has its own unique properties and may be an active form of the drug. CONCLUSION: Open label and retrospective studies have investigated the use of lidocaine in many headache disorders, primarily via injection or infusion. Further research into the active metabolite of lidocaine may allow for its use as a novel nonopiate treatment of chronic pain.


Assuntos
Anestésicos/farmacologia , Transtornos da Cefaleia/tratamento farmacológico , Lidocaína/farmacologia , Anestésicos/administração & dosagem , Anestésicos/metabolismo , Anestésicos/farmacocinética , Humanos , Lidocaína/administração & dosagem , Lidocaína/metabolismo , Lidocaína/farmacocinética
18.
J Oral Maxillofac Surg ; 76(2): 315.e1-315.e7, 2018 02.
Artigo em Inglês | MEDLINE | ID: mdl-29102601

RESUMO

PURPOSE: Palatal local anesthetic injection is a painful procedure. Previous studies have reported successful extraction of maxillary teeth using only buccal infiltration of 4% articaine without palatal anesthesia. The aim of the present study was to determine levels of 4% articaine solution in palatal bone and mucosal tissues after buccal injection and compare those levels with 2% lidocaine solution in New Zealand white rabbits. MATERIALS AND METHODS: Eight rabbits received 2 different injections of 0.6 mL of 4% articaine with 1:100,000 epinephrine and 0.6 mL of 2% lidocaine with 1:100,000 epinephrine buccal to the right and left maxillary first molar, respectively, in a split-mouth study design using quantitative syringes. All injections were administered using the buccal infiltration technique without any palatal injection. Ten minutes later, palatal bone and mucosa specimens were collected for analysis. Levels of the 2 local anesthetic agents were measured in palatal tissues using high-performance liquid chromatography (HPLC). RESULTS: HPLC analysis showed markedly higher 4% articaine solution values (0.319 ± 0.037) in palatal mucosal tissues compared with palatal mucosal concentrations of 2% lidocaine solution (0.0839 ± 0.017). In palatal bone, the mean concentration of 2% lidocaine solution was markedly lower than the mean concentration of 4% articaine solution (0.085 ± 0.012 vs 0.155 ± 0.012, respectively). There was no relevant difference between levels of 2% lidocaine in the palatal bone and mucosal tissues. However, the mean concentration of 4% articaine in the palatal mucosa was markedly higher than its concentration in palatal bone. CONCLUSIONS: The buccal vestibule-palatal diffusion of 4% articaine solution with 1:100,000 epinephrine is greater than 2% lidocaine solution with 1:100,000 epinephrine in a rabbit model.


Assuntos
Anestesia Local/métodos , Anestésicos Locais/farmacocinética , Carticaína/farmacocinética , Lidocaína/farmacocinética , Palato Duro/metabolismo , Administração Bucal , Anestésicos Locais/administração & dosagem , Animais , Carticaína/administração & dosagem , Cromatografia Líquida de Alta Pressão , Lidocaína/administração & dosagem , Masculino , Coelhos
19.
Pharm Dev Technol ; 23(5): 520-529, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29067849

RESUMO

Mucoadhesive formulations have a wide scope of application for both systemic and local treatment of various diseases. In the case of recurrent aphthous stomatitis, to ensure effective therapy, the concentration of corticosteroids, and/or anesthetics at the mouth ulcer side should be maintained with minimal systemic absorption. Therefore, the aim of the study was to investigate cellulose-based formulations, in achieving suitable hardness, mucoadhesiveness, and sustained release of the active ingredients directed towards the mucosa for an extended period of time (∼4 h). This was examined by creating polymer reinforced cellulose composites which consisted of porous cellulose discs (CD) and different polymer components namely polyethylene glycol 6000 (PEG6000), polyethylene glycol 400 (PEG400), and ethyl cellulose. Empty CDs were formed by dropping dissolved cellulose into coagulation medium. The empty porous CDs were immersed into different drug loading solutions which were prepared by dissolving three different concentrations of triamcinolone acetonide and lidocaine hydrochloride in five different ratios of PEG 6000:PEG 400:ethanol (w:w:w %) solutions. All formulations were investigated regarding drug content, release, hardness, and mucoadhesive properties. The results indicate that the non-dispersing buccal discs had sufficient hardness, drug content and in vitro release properties, but further studies are needed to achieve proper mucoadhesiveness.


Assuntos
Celulose/química , Preparações de Ação Retardada/química , Polietilenoglicóis/química , Adesividade , Administração Bucal , Anestésicos Locais/administração & dosagem , Anestésicos Locais/farmacocinética , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/farmacocinética , Celulose/análogos & derivados , Sistemas de Liberação de Medicamentos , Lidocaína/administração & dosagem , Lidocaína/farmacocinética , Mucosa Bucal/metabolismo , Porosidade , Suínos , Triancinolona Acetonida/administração & dosagem , Triancinolona Acetonida/farmacocinética
20.
J Microencapsul ; 34(8): 722-731, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29105520

RESUMO

Anal fissure is common and painful disease of anorectum. In this study, microparticles containing nifedipine and lidocaine HCl were prepared by spray drying and applied to bio-degradable and bio-stable tampons. Characterization of microparticles was determined by visual analyses, mass yield, particle size measurement, encapsulation efficiency, drug loading and in vitro drug release. Mass yield was between 5.5 and 45.9%. The particle size was between 15.1 and 26.8 µm. Encapsulation efficiency were 96.142 ± 5.931 and 85.571 ± 3.301; drug loading were 65.261 ± 3.914% and 37.844 ± 4.339% of L2 and N1, respectively. Well-separated, mainly spherical microparticles with suitable properties were obtained. Optimum microparticles were applied to tampons. Physical properties and visual characteristics of tampons were investigated before and after binder application. In vitro drug release from tampons were also examined. According to the results, textile-based carrier systems loaded microparticles containing nifedipine and lidocaine HCl will be an effective and promising alternative for current anal fissure treatment.


Assuntos
Anestésicos Locais/administração & dosagem , Sistemas de Liberação de Medicamentos/métodos , Fissura Anal/tratamento farmacológico , Lidocaína/administração & dosagem , Nifedipino/administração & dosagem , Tampões Cirúrgicos , Vasodilatadores/administração & dosagem , Alginatos/química , Anestésicos Locais/farmacocinética , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Humanos , Lidocaína/farmacocinética , Nifedipino/farmacocinética , Têxteis/análise , Vasodilatadores/farmacocinética
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