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1.
Rev Bras Ginecol Obstet ; 43(5): 414-416, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-34077985

RESUMO

The diagnosis of genital ulcers remains a challenge in clinical practice. Lipschütz ulcer is a non-sexually transmitted rare and, probably, underdiagnosed condition, characterized by the sudden onset of vulvar edema along with painful necrotic ulcerations. Despite its unknown incidence, this seems to be an uncommon entity, with sparse cases reported in the literature. We report the case of an 11-year-old girl who presented at the emergency department with vulvar ulcers. She denied any sexual intercourse. The investigation excluded sexually transmitted infections, so, knowledge of different etiologies of non-venereal ulcers became essential. The differential diagnoses are extensive and include inflammatory processes, drug reactions, trauma, and malignant tumors. Lipschütz ulcer is a diagnosis of exclusion. With the presentation of this case report, the authors aim to describe the etiology, clinical course, and outcomes of this rare disease, to allow differential diagnosis of genital ulceration.


Assuntos
Anti-Infecciosos Locais/uso terapêutico , Dibucaína/uso terapêutico , Úlcera/diagnóstico , Doenças da Vulva/tratamento farmacológico , Administração Tópica , Anti-Infecciosos Locais/administração & dosagem , Criança , Diagnóstico Diferencial , Dibucaína/administração & dosagem , Infecções por Vírus Epstein-Barr , Feminino , Humanos , Doenças Raras , Resultado do Tratamento , Úlcera/tratamento farmacológico , Doenças da Vulva/patologia
2.
Rev. bras. ginecol. obstet ; 43(5): 414-416, May 2021. graf
Artigo em Inglês | LILACS | ID: biblio-1288554

RESUMO

Abstract The diagnosis of genital ulcers remains a challenge in clinical practice. Lipschütz ulcer is a non-sexually transmitted rare and, probably, underdiagnosed condition, characterized by the sudden onset of vulvar edema along with painful necrotic ulcerations. Despite its unknown incidence, this seems to be an uncommon entity, with sparse cases reported in the literature. We report the case of an 11-year-old girl who presented at the emergency department with vulvar ulcers. She denied any sexual intercourse. The investigation excluded sexually transmitted infections, so, knowledge of different etiologies of non-venereal ulcers became essential. The differential diagnoses are extensive and include inflammatory processes, drug reactions, trauma, and malignant tumors. Lipschütz ulcer is a diagnosis of exclusion. With the presentation of this case report, the authors aim to describe the etiology, clinical course, and outcomes of this rare disease, to allow differential diagnosis of genital ulceration.


Assuntos
Humanos , Feminino , Criança , Úlcera/diagnóstico , Doenças da Vulva/tratamento farmacológico , Dibucaína/uso terapêutico , Anti-Infecciosos Locais/uso terapêutico , Úlcera/tratamento farmacológico , Doenças da Vulva/patologia , Administração Tópica , Resultado do Tratamento , Infecções por Vírus Epstein-Barr , Doenças Raras , Diagnóstico Diferencial , Dibucaína/administração & dosagem , Anti-Infecciosos Locais/administração & dosagem
4.
W V Med J ; 112(2): 44-6, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27025119

RESUMO

Prolonged paralysis due to a quantitative or qualitative deficiency of pseudocholinesterase activity is an uncommon but known side effect of succinylcholine. We describe a patient who experienced prolonged paralysis following administration of succinylcholine for general anesthesia and endotracheal intubation for an emergent cesarean section despite laboratory evidence of normal enzyme function. The patient required mechanical ventilation in the intensive care unit for several hours following surgery. The patient was extubated following return of full muscle strength and had a good outcome. The enzyme responsible for the metabolism of succinylcholine, pseudocholinesterase, was determined to be low in quantity in this patient but was functionally normal. This low level, by itself, was unlikely to be solely responsible for the prolonged paralysis. The patient likely had an abnormal pseudocholinesterase enzyme variant that is undetectable by standard laboratory tests.


Assuntos
Anestésicos Locais , Cesárea , Dibucaína , Emergências , Fármacos Neuromusculares Despolarizantes/efeitos adversos , Complicações do Trabalho de Parto/induzido quimicamente , Paralisia/induzido quimicamente , Succinilcolina/efeitos adversos , Adulto , Anestesia Geral/efeitos adversos , Anestésicos Locais/administração & dosagem , Butirilcolinesterase/sangue , Butirilcolinesterase/deficiência , Dibucaína/administração & dosagem , Feminino , Humanos , Unidades de Terapia Intensiva , Intubação Intratraqueal/efeitos adversos , Fármacos Neuromusculares Despolarizantes/administração & dosagem , Gravidez , Respiração Artificial , Succinilcolina/administração & dosagem , Fatores de Tempo , Resultado do Tratamento
5.
J Anesth ; 29(5): 763-8, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26302690

RESUMO

In many anesthesia textbooks written in English, lidocaine, tetracaine, bupivacaine, ropivacaine, and chloroprocaine are listed as useful local anesthetics for spinal anesthesia. In contrast, T-cain is not included in these lists, even though it has been reported to be suitable for spinal anesthesia in Japan. T-cain was developed as a local anesthetic in the early 1940s by Teikoku Kagaku Sangyo Inc. in Itami, Japan, by replacing a methyl group on tetracaine (Pantocaine(®)) with an ethyl group. T-cain was clinically approved for topical use in Japan in November 1949, and a mixture of dibucaine and T-cain (Neo-Percamin S(®)) was approved for spinal use in May 1950. Simply because of a lack of foreign marketing strategy, T-cain has never attracted global attention as a local anesthetic. However, in Japan, T-cain has been used topically or intrathecally (as Neo-Percamin S(®)) for more than 60 years. Other than the side effects generally known for all local anesthetics, serious side effects have not been reported for T-cain. In fact, several articles have reported that T-cain decreases the neurotoxicity of dibucaine. In this historical review, the characteristics of T-cain and its rise to become a major spinal anesthetic in Japan are discussed.


Assuntos
Anestesia Local/métodos , Raquianestesia/métodos , Anestésicos Locais/administração & dosagem , Administração Tópica , Anestésicos Locais/química , Dibucaína/administração & dosagem , Dibucaína/química , Humanos , Japão , Síndromes Neurotóxicas/prevenção & controle , Tetracaína/química
6.
Rev Col Bras Cir ; 41(2): 92-8, 2014.
Artigo em Inglês, Português | MEDLINE | ID: mdl-24918721

RESUMO

OBJECTIVE: To evaluate the effects of topical policresulen and cinchocaine in the postoperative pain behavior of open hemorrhoidectomy. METHODS: We conducted a prospective, double-blinded, controlled study. The control group received the usual guidelines with oral medications. The topical treatment group received, in addition, the application of the ointment and was comprised of two subgroups (policresulen + cinchocaine, and placebo). Pain intensity was recorded with the visual analogue scale. RESULTS: 43 patients were operated on: control group - n = 13, one excluded; placebo - n = 15; and policresulen + cinchocaine - n = 15. The mean age was 45.98 years and 37.2% were men. The average pain intensity was 4.09 (immediate postoperative), 3.22 (hospital discharge), 5.73 (day 1) , 5.77 (day 2), 5.74 (day 3), 5.65 (day 7), 5.11 (day 10), 2.75 (day 15) and 7.70 (first bowel movement), with no difference between groups in all periods. CONCLUSION: This study showed no reduction in pain after hemorrhoidectomy with the use of topical policresulen and cinchocaine.


Assuntos
Analgesia/métodos , Anestésicos Locais/administração & dosagem , Anti-Infecciosos/administração & dosagem , Cresóis/administração & dosagem , Dibucaína/administração & dosagem , Formaldeído/administração & dosagem , Hemorroidectomia , Dor Pós-Operatória/prevenção & controle , Administração Tópica , Método Duplo-Cego , Combinação de Medicamentos , Quimioterapia Combinada , Feminino , Humanos , Estudos Longitudinais , Masculino , Pessoa de Meia-Idade , Medição da Dor , Estudos Prospectivos
7.
Rev. Col. Bras. Cir ; 41(2): 92-98, Mar-Apr/2014. tab, graf
Artigo em Inglês | LILACS | ID: lil-711825

RESUMO

OBJECTIVE: To evaluate the effects of topical policresulen and cinchocaine in the postoperative pain behavior of open hemorrhoidectomy. METHODS: We conducted a prospective, double-blinded, controlled study. The control group received the usual guidelines with oral medications. The topical treatment group received, in addition, the application of the ointment and was comprised of two subgroups (policresulen + cinchocaine, and placebo). Pain intensity was recorded with the visual analogue scale. RESULTS: 43 patients were operated on: control group - n = 13, one excluded; placebo - n = 15; and policresulen + cinchocaine - n = 15. The mean age was 45.98 years and 37.2% were men. The average pain intensity was 4.09 (immediate postoperative), 3.22 (hospital discharge), 5.73 (day 1) , 5.77 (day 2), 5.74 (day 3), 5.65 (day 7), 5.11 (day 10), 2.75 (day 15) and 7.70 (first bowel movement), with no difference between groups in all periods. CONCLUSION: This study showed no reduction in pain after hemorrhoidectomy with the use of topical policresulen and cinchocaine. .


OBJETIVO: avaliar a ação do policresuleno e cinchocaína tópicos no comportamento da dor no pós-operatório de hemorroidectomias abertas. MÉTODOS: estudo prospectivo, duplo cego e controlado. O grupo controle recebeu as orientações usuais com medicações de uso oral. O grupo de tratamento tópico recebeu, adicionalmente, a aplicação de pomada e foi composto de dois subgrupos (policresuleno + cinchocaína; e placebo). A intensidade da dor foi registrada a partir da escala visual analógica. RESULTADOS: foram operados 43 pacientes: grupo controle (n=13; um excluído), placebo (n=15) e policresuleno + cinchocaína (n=15). A média de idade foi 45,98 anos e 37,2% foram homens. A média da intensidade da dor foi 4,09 (PO imediato), 3,22 (alta hospitalar), 5,73 (dia 1), 5,77 (dia 2), 5,74 (dia 3), 5,65 (dia 7), 5,11 (dia 10), 2,75 (dia 15) e 7,70 (primeira evacuação), sem diferença entre os grupos em todos os períodos estudados. CONCLUSÃO: este estudo não demonstrou redução da dor após hemorroidectomias como o uso do tratamento tópico. .


Assuntos
Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Analgesia/métodos , Anestésicos Locais/administração & dosagem , Anti-Infecciosos/administração & dosagem , Cresóis/administração & dosagem , Dibucaína/administração & dosagem , Formaldeído/administração & dosagem , Hemorroidectomia , Dor Pós-Operatória/prevenção & controle , Administração Tópica , Método Duplo-Cego , Combinação de Medicamentos , Quimioterapia Combinada , Estudos Longitudinais , Medição da Dor , Estudos Prospectivos
8.
Gan To Kagaku Ryoho ; 39(4): 605-11, 2012 Apr.
Artigo em Japonês | MEDLINE | ID: mdl-22504686

RESUMO

Our first report mentioned the analysis results of the safety and efficacy of trigger point (TP) therapy by Neovitacain® injection (NV) in the daily clinical treatment of myofascial pain in cancer patients. This time, we report additional considerations regarding the following points; (1) Injection sites: they were concentrated on both sides of the spine, indicating that TPs could be easily formed on the points and near them to support the body's weight when patients were supine. (2) Correlation between VAS and FS: VAS and FS were positively correlated in every measurement period. (3) Patient satisfaction: many patients made several comments expressing feelings of satisfaction from this treatment. The comments were considered to reflect the patients' candid feelings. Therefore, all comments were classified according to the degree of patients' feeling of satisfaction. It may be possible to obtain much higher patient satisfaction by hearing out the voice of the patients. Judging from this study, TP therapy by NV for myofascial pain in cancer patients relieved the total pain of cancer patients. TP therapy has potential for obtaining high patient satisfaction.


Assuntos
Dibucaína/uso terapêutico , Síndromes da Dor Miofascial/tratamento farmacológico , Neoplasias/complicações , Piridoxina/uso terapêutico , Salicilato de Sódio/uso terapêutico , Pontos-Gatilho/anatomia & histologia , Dibucaína/administração & dosagem , Humanos , Injeções , Síndromes da Dor Miofascial/etiologia , Piridoxina/administração & dosagem , Salicilato de Sódio/administração & dosagem , Inquéritos e Questionários
9.
J Clin Pediatr Dent ; 37(1): 15-8, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23342561

RESUMO

UNLABELLED: Topical anesthesia is widely advocated in pediatric dentistry practice to reduce pain and anxiety produced by administration of local anesthesia. There are different combinations of topical anesthetic agents that are marketed worldwide. However, sparse literature reports exist regarding clinical efficacy of these agents. AIM: To compare the clinical effectiveness of two strawberry flavored topical anesthetics viz. Precaine (8% Lidocaine + 0.8% Dibucaine) and Precaine B (20% Benzocaine) in children before intra oral local anesthetic injections and for extraction of mobile primary teeth. STUDY DESIGN: This triple blind clinical study included sixty children divided equally under three techniques--palatal injections, inferior alveolar nerve block and extraction of mobile primary teeth. Both the products were used alternately using split mouth design in two visits and the child's pain response was assessed using VAS and SEM pain scale. The scores obtained were subjected to statistical analysis. RESULTS: Precaine has shown lower mean scores in all the techniques under both the pain scales, but were statistically insignificant. Gender wise comparison has also shown lower mean scores for Precaine for both males and females, however these were statistically insignificant. On visit wise comparison, Precaine B reported significant lower scores (p < 0.05) in visit 2 compared to visit 1 for inferior alveolar nerve block and extraction of mobile primary teeth under SEM pain scale. CONCLUSION: Precaine (8% Lidocaine + 0.8% Dibucaine) can be used as effectively as Precaine B (20% Benzocaine).


Assuntos
Anestesia Dentária/métodos , Anestesia Local/métodos , Anestésicos Locais/administração & dosagem , Dor/prevenção & controle , Anestésicos Combinados/administração & dosagem , Benzocaína/administração & dosagem , Criança , Dibucaína/administração & dosagem , Feminino , Aromatizantes/administração & dosagem , Humanos , Injeções/efeitos adversos , Injeções/instrumentação , Lidocaína/administração & dosagem , Masculino , Nervo Mandibular , Agulhas/efeitos adversos , Bloqueio Nervoso/métodos , Medição da Dor , Palato , Extração Dentária , Mobilidade Dentária/cirurgia , Dente Decíduo/cirurgia , Resultado do Tratamento
10.
Eur J Radiol ; 81(7): 1652-6, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21459531

RESUMO

In computed tomography (CT) angiogram or some dedicated CT studies of the abdomen, the use of positive enteric contrast should be avoided as its presence could decrease the sensitivity of the test. There are, however, cases of CT scans with unexpected hyperdense intraluminal contents detected due to the use of certain oral or rectal medications. Reports on medications as causes of intraluminal hyperdensities are sparse in the English literature. We have studied several commonly used medications and revealed that many drugs appear hyperdense in CT scans. The presence of unexpected intraluminal hyperdensities can potentially cause erroneous interpretation of images and in some cases decrease the sensitivity of the test. The hyperdense bowel contents may be mistaken as acute hemorrhage in CT angiogram for detection of GI bleeding. Active GI bleeding, presented as intraluminal extravasation of contrast material, can also be obscured. Certain intra-abdominal pathologies could be masked, for example, in plain CT scan for detection of urinary tract stones or in contrast CT study for suspected bowel ischaemia. It is important for radiologists and clinicians to be aware of this situation in order to prevent misinterpretation of images and to select the most appropriate imaging modality when such unexpected intraluminal hyperdensities are encountered.


Assuntos
Erros de Diagnóstico , Radiografia Abdominal , Tomografia Computadorizada por Raios X , Hidróxido de Alumínio/administração & dosagem , Amiodarona/administração & dosagem , Combinação Amoxicilina e Clavulanato de Potássio/administração & dosagem , Angiografia , Anti-Inflamatórios/administração & dosagem , Carbonato de Cálcio/administração & dosagem , Meios de Contraste/administração & dosagem , Cresóis/administração & dosagem , Dibucaína/administração & dosagem , Combinação de Medicamentos , Glicerol/administração & dosagem , Humanos , Iodetos/administração & dosagem , Compostos de Ferro/administração & dosagem , Imagens de Fantasmas , Poliestirenos/administração & dosagem , Cloreto de Potássio/administração & dosagem
11.
Arch Pharm Res ; 33(8): 1277-83, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20803132

RESUMO

In relieving local pains, dibucaine, one of ester type local anesthetics, has been used. In case of their application such as ointments and creams, it is difficult to expect their effects for a required period of time, because they are easily removed by wetting, movement and contacting. To develop suitable bioadhesive gels, the bioadhesive force of hydroxypropyl cellulose (HPC) was tested using auto-peeling tester. The effect of drug concentration on drug release was studied from the prepared 2% HPC-HF gels using synthetic cellulose membrane at 37 +/- 0.5 degrees C. We investigated the enhancing effects on drug permeation into skins, using some kind of enhancers such as the glycols, the non-ionic surfactants, the fatty acids, and the propylene glycol derivatives. Anesthetic effects of dibucaine gels containing polyoxyethylene 2-oleyl ether were measured by tail flick analgesic meter. The bioadhesive force of various types of HPC such as GF, MF, and HF, was 0.0131, 0.0501, and 0.1346 N, at 2% HPC concentration, respectively. The HPC-HF gels showed the highest bioadhesive force. As the concentration of HPC-HF increased, the drug release increased. As the temperature increased, the drug release increased. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest enhancing effects. According to the rat tail flick test, 1% drug gels containing polyoxyethylene 2-oleyl ether showed the prolonged local anesthetic effects. In conclusion, the dibucaine gel containing penetration enhancer and vasoconstrictor showing enhanced local anesthetic action could be developed by using the bioadhesive polymer, HPC.


Assuntos
Anestésicos Locais/farmacologia , Dibucaína/farmacologia , Dor/tratamento farmacológico , Absorção Cutânea , Adesividade , Administração Cutânea , Anestésicos Locais/administração & dosagem , Anestésicos Locais/farmacocinética , Animais , Celulose/análogos & derivados , Celulose/química , Dibucaína/administração & dosagem , Dibucaína/farmacocinética , Relação Dose-Resposta a Droga , Excipientes/química , Géis , Masculino , Medição da Dor , Ratos , Ratos Sprague-Dawley , Temperatura
12.
J Med Toxicol ; 6(1): 44-9, 2010 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-20224995

RESUMO

INTRODUCTION: Dibucaine is a potent, long-lasting local anesthetic (LA). Topical dibucaine ointments are marketed directly to consumers in the USA without prescription. Dibucaine ointment is intended to treat discomfort associated with sunburn, eczema, minor rashes, minor scratches, insect bites, and poison ivy and is used alone or in combination with other active ingredients to treat pain associated with hemorrhoids or other anorectal disorders. Oral dibucaine toxicosis has been reported in children and includes gastrointestinal upset and neurologic and cardiovascular dysfunction. CASE REPORT: An 18-month-old, female, Parson Russell terrier ingested approximately 23 g of 1% dibucaine ointment (approximately 38 mg/kg dibucaine) recommended to the owner for the treatment of hemorrhoids. Onset and resolution of clinical signs were relatively rapid, 5 min and 60 min, respectively. Clinical signs included vomiting, ptyalism, whole-body muscle fasciculations, disorientation, and severe ataxia. DISCUSSION: Oral dibucaine toxicosis in dogs is similar to oral dibucaine toxicosis in children. Dibucaine ointment poses a real and potentially serious toxicological risk to pets and thus should be stored in a safe location.


Assuntos
Anestésicos Locais/intoxicação , Dibucaína/intoxicação , Doenças do Cão/induzido quimicamente , Acidentes , Administração Oral , Anestésicos Locais/administração & dosagem , Animais , Antídotos/uso terapêutico , Ataxia/induzido quimicamente , Ataxia/veterinária , Carvão Vegetal/uso terapêutico , Confusão/induzido quimicamente , Dibucaína/administração & dosagem , Doenças do Cão/diagnóstico , Doenças do Cão/terapia , Cães , Feminino , Intoxicação/veterinária , Sialorreia/induzido quimicamente , Sialorreia/veterinária , Espasmo/induzido quimicamente , Espasmo/veterinária , Resultado do Tratamento , Vômito/induzido quimicamente , Vômito/veterinária
14.
Eur J Pharmacol ; 611(1-3): 92-9, 2009 Jun 02.
Artigo em Inglês | MEDLINE | ID: mdl-19344707

RESUMO

In patients with atopic dermatitis, alcoholic beverages can sometimes trigger or enhance itching. We have previously reported that HR-1 hairless mice fed a commercial special diet, HR-AD, but not a normal diet, develop atopic dermatitis-like skin inflammation with prolonged spontaneous scratching, and that skin barrier dysfunction is involved in the basal scratching. In the present study, the effects of ethanol on itch-related scratching were examined in this mouse model. When ethanol (30%, 10 ml/kg) was given orally to HR-AD-fed mice, scratching with long duration was further markedly increased, while oral ethanol administration had little effect on the scratching response in normal diet-fed mice. The scratching response after oral ethanol administration in HR-AD-fed mice (ethanol-induced scratching) was attenuated by antagonism of the mu-opioid receptor or local skin anesthesia, as in human itching. Ethanol-induced scratching was also suppressed by improvement of skin barrier function by an application of petrolatum ointment, while ethanol administration itself did not affect the function. This suggests that ethanol indirectly aggravates the basal scratching. Although antagonism of the transient receptor potential vanilloid-1 did not affect ethanol-induced scratching, blockade of ethanol actions in the central nervous system (CNS), including gamma-aminobutyric acid type A receptor antagonism and N-methyl-d-aspartate receptor activation, inhibited it. Taken together, the present study demonstrates that orally administered ethanol markedly aggravates itch-related scratching in HR-AD-fed mice developing atopic dermatitis, and suggests that the CNS depressant actions of ethanol play an important role in the aggravation.


Assuntos
Dermatite Atópica/fisiopatologia , Etanol/farmacologia , Prurido/induzido quimicamente , Prurido/fisiopatologia , Administração Oral , Animais , Capsaicina/administração & dosagem , Capsaicina/análogos & derivados , Capsaicina/farmacologia , Dermatite Atópica/complicações , Dermatite Atópica/patologia , Dibucaína/administração & dosagem , Dibucaína/farmacologia , Etanol/administração & dosagem , Feminino , Camundongos , Camundongos Pelados , N-Metilaspartato/administração & dosagem , N-Metilaspartato/farmacologia , Naltrexona/administração & dosagem , Naltrexona/farmacologia , Vaselina/administração & dosagem , Vaselina/farmacologia , Prurido/complicações , Temperatura Cutânea/efeitos dos fármacos
15.
Drug Deliv ; 15(5): 323-30, 2008 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-18763163

RESUMO

The skin permeation enhancement of many kinds of drugs and cosmetic substances by microemulsions has been widely known; however, the correlations between microemulsion microstructures and the efficiency of skin permeation are not fully elucidated. Therefore, the aim of our study was to investigate the influence of microemulsion types on in vitro skin permeation of model hydrophobic drugs and their hydrophilic salts. The microemulsion systems were composed of isopropyl palmitate (IPP), water, a 2:1 w/w mixture of Aerosol OT (AOT) and 1-butanol, and a model drug. The concentrations of surfactant mixture and model drug were maintained at 45% and 1% w/w, respectively. The concentrations of IPP and water were 15% and 39% w/w, respectively, for oil-in-water (o/w) type and vice versa for water-in-oil (w/o) type. The samples were prepared by simple mixing and characterized by visual appearance, pH, refractive index, electrical conductivity, viscosity, and determination of the state of water and IPP in the formulations using differential scanning calorimetry. Transdermal flux of lidocaine, tetracaine, dibucaine, and their respective hydrochloride salts from the drug-loaded AOT-based microemulsions through heat-separated human epidermis was investigated in vitro using modified Franz diffusion cells. The o/w microemulsions resulted in the highest fluxes of the model drugs in base form as compared with the other formulations within the same group of drugs. Moreover, the skin permeation of drug from microemulsions depended on drug molecular structure and interaction between drug and surfactant.


Assuntos
Anestésicos Locais/farmacocinética , Ácido Dioctil Sulfossuccínico/química , Tensoativos/química , 1-Butanol/química , Administração Cutânea , Anestésicos Locais/administração & dosagem , Varredura Diferencial de Calorimetria , Cromatografia Líquida de Alta Pressão , Dibucaína/administração & dosagem , Dibucaína/farmacocinética , Portadores de Fármacos , Condutividade Elétrica , Emulsões , Epiderme/metabolismo , Humanos , Concentração de Íons de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Técnicas In Vitro , Lidocaína/administração & dosagem , Lidocaína/farmacocinética , Palmitatos/química , Permeabilidade , Refratometria , Absorção Cutânea , Tetracaína/administração & dosagem , Tetracaína/farmacocinética , Viscosidade
16.
J Pharm Pharmacol ; 59(10): 1447-50, 2007 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-17910822

RESUMO

A novel type of lipid vesicles, propylene glycol-embodying liposomes or PG-liposomes, composed of phospholipid, propylene glycol and water, is introduced. The new lipid vesicles were developed and investigated as carriers for skin delivery of the model drug, cinchocaine base. PG-liposomes showed high entrapment efficiency and were stable for at least one month of storage at 5 +/- 1 degree C. Preliminary in-vivo skin deposition studies, carried out using albino rabbit dorsal skin, showed that PG-liposomes were superior to traditional liposomes, deformable liposomes and ethosomes, suggesting that PG-liposomes, introduced in the current work, are promising carriers for skin delivery of drugs.


Assuntos
Anestésicos Locais/farmacocinética , Dibucaína/farmacocinética , Portadores de Fármacos/química , Propilenoglicol/química , Administração Cutânea , Animais , Dibucaína/administração & dosagem , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Lipossomos , Fosfatidilcolinas/química , Coelhos , Pele/metabolismo , Absorção Cutânea , Água/química
17.
Acta Pharm ; 56(3): 311-24, 2006 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-19831280

RESUMO

A method for determining the rate of hydrophilic and hydrophobic drugs release from different types of liposomal dispersions and gels using a dialysis method is described. Dibucaine base and 5-fluorouracil were used as model drugs for a hydrophobic and a hydrophilic drug, respectively. A dialysis technique was employed. Release rates were affected by the rate of rotation of the paddles of the tablet dissolution tester, temperature, and the volume of release medium. The method was used to evaluate the in vitro drug release from hydrophilic and hydrophobic drugs from liposomal dispersions and gels. The in vitro release study of dibucaine base showed no burst effect, while the in vitro release study of 5-fluorouracil showed a clear burst effect with an initial fast release phase followed by a sustained release phase.


Assuntos
Diálise/métodos , Dibucaína/administração & dosagem , Fluoruracila/administração & dosagem , Química Farmacêutica , Preparações de Ação Retardada , Dibucaína/química , Fluoruracila/química , Géis , Interações Hidrofóbicas e Hidrofílicas , Lipossomos , Solubilidade , Temperatura
18.
Acta Pol Pharm ; 62(5): 369-79, 2005.
Artigo em Inglês | MEDLINE | ID: mdl-16459486

RESUMO

Formulation of local anesthetics in liposomal topical drug delivery system could provide a sustained and localized anesthesia. The aim of this study was to develop a liposomal dibucaine base (DB) local anesthetic delivery system. DB-loaded multilamellar vesicles (MLVs) were prepared through varying lipid composition, induced charge and pH of the hydration medium. Liposomes were characterized for morphology, size, entrapment efficiency (EE), in vitro drug release and stability including leakage stability. The percentage of drug entrapped in liposomes was found to be hydration medium pH dependent and charge dependent and more pronounced for negatively charged liposomes prepared using hydration medium of pH 9. In vitro release studies of liposomes have shown a sustained release of entrapped dibucaine compared to control solution. Results revealed that adjusting the various formulation variables of dibucaine base MLVs could yield stable and effective topical liposomal local anesthetic formulations.


Assuntos
Anestésicos Locais/administração & dosagem , Dibucaína/administração & dosagem , Anestésicos Locais/química , Química Farmacêutica , Dibucaína/química , Composição de Medicamentos , Estabilidade de Medicamentos , Lipossomos , Membranas Artificiais
19.
Indian J Gastroenterol ; 23(3): 91-3, 2004.
Artigo em Inglês | MEDLINE | ID: mdl-15250565

RESUMO

OBJECTIVE: To compare symptomatic relief, healing, and changes in maximal anal resting pressure with the use of topical formulations in patients with chronic anal fissure. METHODS: Sixty-four consecutive patients with chronic anal fissure were randomized into 4 groups that received, in a double-blind manner, a topical ointment that contained 0.2% nitroglycerine (GTN), 5% xylocaine, Proctosedyl (hydrocortisone acetate, heparin, framycetin sulfate, esculoside, ethoform, butoform) or petroleum jelly (Vaseline), to be applied twice daily. Patients were reviewed at 2-week intervals for 6 weeks. Anal manometry was done before, and 20 minutes after, the first application of the ointment. RESULTS: There was significant (p < 0.0001) reduction in mean anal resting pressure after application of GTN, but not any other ointment. Of 16 patients receiving GTN, complete pain relief occurred in 6 and 15 patients after 2 and 4 weeks of treatment, respectively; this was more frequent than in the other 3 groups. At 6 weeks also, complete pain relief occurred more often with GTN than with Vaseline or xylocaine. After 4 weeks of treatment, 3 patients on GTN had complete healing of fissure as compared to one each in the xylocaine and Proctosedyl groups and none in the Vaseline group. At 6 weeks, healing of fissure had occurred in 15 of 16 patients receiving GTN as compared to 4 receiving Vaseline, 11 receiving xylocaine, and 12 on Proctosedyl. CONCLUSIONS: Topical nitroglycerine produces 'chemical sphincterotomy' with reduction in mean anal resting pressure. Pain relief and healing of fissure occurred earlier with GTN than with other treatments. GTN should be considered as the treatment of choice for the non-surgical management of patients with chronic anal fissure.


Assuntos
Dibucaína/administração & dosagem , Esculina/administração & dosagem , Fissura Anal/tratamento farmacológico , Framicetina/administração & dosagem , Hidrocortisona/administração & dosagem , Lidocaína/administração & dosagem , Fármacos Neuromusculares/administração & dosagem , Nitroglicerina/administração & dosagem , Administração Tópica , Adulto , Doença Crônica , Método Duplo-Cego , Combinação de Medicamentos , Feminino , Humanos , Masculino , Resultado do Tratamento
20.
Masui ; 53(4): 396-8, 2004 Apr.
Artigo em Japonês | MEDLINE | ID: mdl-15160665

RESUMO

We report three cases of cauda equina syndrome following spinal anesthesia with dibucaine. In two cases, the lumbar puncture was repeated and additional doses of dibucaine were administered to obtain adequate sensory blockade. In the last case, spinal anesthesia worked well with single injection of dibucaine. In all cases patients complained of varying degrees of bladder and bowel dysfunction, perineal sensory loss and lower extremity motor weakness on the next day, and the diagnosis of cauda equina syndrome was made. With only one case, the symptom disappeared four months later, but the rest of the patients suffered from sensory disturbance and defecation for more than four months after the surgery. One possible cause is a direct neurotoxic effect of high concentration dibucaine due to its maldistribution within the subarachnoid space. We have to consider the neurotoxicity and dose of the local anesthetic for obtaining a safer method and for preventing this complication.


Assuntos
Anestésicos Locais/efeitos adversos , Dibucaína/efeitos adversos , Polirradiculopatia/induzido quimicamente , Adulto , Raquianestesia , Anestésicos Locais/administração & dosagem , Dibucaína/administração & dosagem , Feminino , Humanos , Injeções Espinhais , Pessoa de Meia-Idade
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