Tetracaine stimulates insulin secretion through the mobilization of Ca2+ from thapsigargin- and IP3-insensitive Ca2+ reservoir in pancreatic beta-cells

The effect of tetracaine on Ca-45 efflux, cytoplasmic Ca2+ concentration [Ca2+](i), and insulin secretion in isolated pancreatic islets and beta-cells was studied. In the absence of external Ca2+, tetracaine (0.1-2.0 mM) increased the Ca-45 efflux from isolated islets in a dose-dependant manner. Tetracaine did not affect the increase in Ca-45 efflux caused by 50 mM K+ or by the association of carbachol (0.2 mM) and 50 mM K+. Tetracaine permanently increased the [Ca2+](i) in isolated beta-cells in Ca2+-free medium enriched with 2.8 mM glucose and 25 mu M D-600 (methoxiverapamil). This effect was also observed in the presence of 10 mM caffeine or 1 mu M thapsigargin. In the presence of 16.7 mM glucose, tetracaine transiently increased the insulin secretion from islets perfused in the absence and presence of external Ca2+. These data indicate that tetracaine mobilises Ca2+ from a thapsigargin-insensitive store and stimulates insulin secretion in the absence of extracellular Ca2+. The increase in Ca-45 efflux caused by high concentrations of K+ and by carbachol indicates that tetracaine did not interfere with a cation or inositol triphosphate sensitive Ca2+ pool in beta-cells.

Cauda equina syndrome after spinal tetracaine: Electromyographic evaluation-20 years follow-up

CAUDA equina syndrome (CES) has long been recognized as a rare complication of spinal anesthesia.(1) CES has been described after administration of spinal anesthetics with lidocaine(2) and bupivacaine.(3) In 1991,(4) CES was reported after continuous spinal anesthesia with 1% tetracaine. In 1980, at our university hospital, six adult female patients underwent perineal gynecologic surgery using a spinal anesthetic of 2 ml tetracaine, 1.2%, in 10% glucose. The concentration of the injected tetracaine was unknown by the anesthetists. In all cases, lumbar puncture was performed at the L3-L4 interspace with a disposable spinal needle while the patients were in the sitting position. CES was first diagnosed 72 h or later postoperatively; previous diagnosis was not possible because patients had an indwelling urethral catheter. The diagnosis of CES was confirmed in all patients. During the past year, after institutional approval and informed consent, clinical, magnetic resonance imaging, electromyographic examinations, and conduction studies were performed in three of the above patients. Examinations were not possible on the other three patients because one had recently died, another could not be located, and the third refused to participate. T1 and T2 magnetic resonance image readings were obtained with Gadolinium contrast from a 0.5 Tesla General Electric apparatus (General Electric, Tokyo, Japan). Bilateral sensory and motor conduction studies of the sciatic nerve branches were obtained using a two-channel Nihon-Kohden Neuropack 2 (Nihom-Kohden Corporation, Tokyo, Japan). Electromyography was performed in accordance with conventional techniques.(5,6)

Anestesia subaracnóidea em crianças

JUSTIFICATIVA E OBJETIVOS: Tem aumentado muito o emprego da anestesia subaracnóidea em crianças, principalmente neonatos com risco de desenvolver apnéia neonatal. O objetivo deste trabalho foi rever as diferenças anatômicas, fisiológicas e farmacológicas desta técnica em crianças. CONTEÚDO: A anestesia subaracnóidea em crianças, apesar de ter sido técnica empregada desde o início do século XX, teve sua popularidade diminuída com o advento dos anestésicos inalatórios e bloqueadores neuromusculares, para ser novamente resgatada em 1979. As características favoráveis desta técnica em pediatria são relativas à estabilidade cardiovascular, em crianças de até 8 anos de idade, à analgesia satisfatória e ao relaxamento muscular. Os anestésicos mais utilizados em crianças são a tetracaína e a bupivacaína, cujas doses são ajustadas tomando-se por base o peso corporal. Esta técnica é limitada pela duração relativamente curta, devendo ser utilizada para procedimentos cirúrgicos que não ultrapassem 90 minutos e também pela analgesia não abranger o pós-operatório. As complicações são as mesmas encontradas no paciente adulto, incluindo cefaléia por punção dural e irritação radicular transitória. As indicações são várias: cirurgias de abdômen inferior, genitália, membros inferiores, região perineal e, em alguns casos, até em cirurgias torácicas. Seu emprego tem particular interesse nos recém-nascidos prematuros, pelo risco de apresentarem a apnéia da prematuridade. CONCLUSÕES: A anestesia subaracnóidea em crianças é técnica relativamente segura, com poucas complicações e pode ser considerada como opção para anestesia geral, principalmente nos recém-nascidos prematuros com risco de apresentarem complicações respiratórias no pós-operatório.

EFEITO DE SURFACTANTES NA ESTABILIDADE DE COMPOSTOS DE USO TERAPEUTICO

A critical revision of literature as regards to the drug stability in the presence of surfactants were realized. The functional groups envolved in the drug decomposition were used to the development of the discussion. The analysis indicated that the detergent effect can be used to control the rates and mechanisms of drug decomposition and to obtain specific information about the drug reactivity in the environment of pharmacological action.

Análise retrospectiva da toxicidade de gotas otológicas, medicamentos tópicos nasais e orofaríngeos registrada na Grande São Paulo.

BACKGROUND: Retrospective analysis of human toxicity files involving topical medicines for treatment of upper airways diseases (eardrops, topical nasal medicines, lozenges, drops and sprays for oropharyngeal affections). METHODS: Thirty-four brands of eardrops, 48 of topical nasal medicines and 22 of tablets, lozenges and sprays for oropharyngeal affections were selected, from a total of 104 products available in Brazil. We analyzed the registries in the electronic database from the Poison Control Centre of São Paulo (CCI-Jabaquara), Brazil, for the period from January 1996 through December 2000. The cases related to selected pharmaceuticals were collected. RESULTS: 10,823 cases of human toxicity caused by medicines were voluntarily reported to CCI-Jabaquara. Topical medicines for treatment of upper airways diseases accounted for 291 cases (2.68%), from which 240 (82.5%) represented poisoning; 12 (4.1%) involved ear drops, 268 (92%), topical nasal medicines and 11 (3.9%), topical medicines for oropharyngeal affections. Among topical nasal medicines, vasoconstrictors predominated (233 cases), and among medicines for oropharyngeal affections, it was tetracaine (four cases). Considering age distribution, toxicity predominated significantly in children aged from 1 to 4 years (p=0.0003). The main causes of toxicity were: accidental intake of medicines (43%) and error in drug administration (14.8%). Hypereflexia and vomiting were the most frequent symptoms related to toxicity. CONCLUSIONS: There was significant incidence of systemic toxicity due to eardrops, topical nasal and oropharyngeal medicines in children 1 to 4 years-old, whose main cause was accidental intake of these medicines.