Benzodiazepine antagonism by harmane and other β-carbolines in vitro and in vivo

Rommelspacher, Hans; Nanz, Christel; Borbe, Harald O.; Fehske, Klaus J.; Müller, Wernér E.G.; Wollert, U.

doi:10.1016/0014-2999(81)90173-4

Cited by 124 publications

(20 citation statements)

References 21 publications

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“…A hypothesis about dependence supposes that the stimulating action of a drug elicit$ dependence. With respect to harman, activating effects are weil known (Naranjo 1979;Rommelspacher et al 1981;Saano and Airaksinen 1982). Whether or not the increase of harman is more pronounced in high-risk patients than in other patients or in healthy volunteers remains to be clarified.…”

Section: Results and Diseussionmentioning

confidence: 96%

Increased Formation of β-carbolines in Alcoholic Patients following Ingestion of Ethanol

Rommelspacher¹,

Schmidt²

1985

Pharmacopsychiatry

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Section: Results and Diseussionmentioning

confidence: 96%

Increased Formation of β-carbolines in Alcoholic Patients following Ingestion of Ethanol

Rommelspacher¹,

Schmidt²

1985

Pharmacopsychiatry

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“…8-Carbolines have been purported to act as inverse agonists with regard to BZP receptors (12) since it has been evidenced to bind to these receptors (9,11), to reverse BZP action (9-11, 16, 17) and to be antagonized by a BZP antagonist, Ro 15 1788 (18,19). Therefore, l3-carbolines and BZP are expected to have a certain common feature from the structural point of view on the binding to the BZP receptor.…”

Section: Discussionmentioning

confidence: 99%

“…l3-Carbolines such as (3-CCE and 8-CCM are well known to reverse the benzodiazepine action in the central nervous system (9)(10)(11). Recently, Hunkeler et al (12) claimed that (3-carbolines act on the BZP receptor as inverse agonists in the central nervous system.…”

mentioning

confidence: 99%

β-Carbolines Selectively Antagonize the Cholecystokinin Action in Isolated Guinea-Pig Gallbladder Muscle

Kubota

Itonaga

1986

Japanese Journal of Pharmacology

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Abstract-Two(3-carbolines, methyl (3-carboline-3-carboxylate (8-CCM) and ethyl , caused the parallel shift of the dose response curve for cholecystokinin (CCK) in isolated guinea-pig gallbladder muscle. The Schild plot regarding the parallel shift in the dose-response curves had a regression line with a slope of 1.03 and a pA2 value of 5.17 for l3-CCE, while the method of van Rossum gave a pA2 value of 5.24 for (3-CCE and 5.53 for 3-CCM. Both the (3-carbolines protected CCK receptors in the gallbladder muscle from alkylation by dibenamine, but 9-CCM did not protect acetylcholine receptors from dibenamine alkylation.These results suggest that 9-CCM and 3-CCE, so-called inverse agonists of benzodiazepines (BZP), antagonize the CCK action in the gallbladder muscle in a competitive manner, and the antagonism takes place at CCK receptor sites.No spare receptors for CCK were found in the guinea-pig gallbladder muscle.

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“…Las crisis comiciales se producen en una fase temprana del SAA y son debidas a un aumento de la actividad de los receptores NMDA -que incrementan su número ante exposición crónica al etanol (35) -al desaparecer, por una parte, el efecto bloqueante del alcohol sobre los canales de cationes asociados a dichos receptores y, por otra parte, por estar deprimido el sistema gabérgi-co, responsable del efecto inhibidor a través de la apertura de canales de aniones (36) . Otros dos mecanismos que favorecen el desencadenamiento de crisis comiciales son la hipomagnesemia (37) así como el aumento de β-carbolinas durante el síndrome de abstinencia (38) . El cortejo de síntomas vegetativos que acompañan al SAA (temblor fino, taquicardia, hipertensión, diaforesis, midriasis, hiperreflexia, etc.)…”

Section: Modelo Biológico De La Dependencia Y Del Sín-drome De Abstinunclassified

Estrategias en el tratamiento de desintoxicación alcohólica

Stauber¹

2003

Adicciones

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Antecedentes: El alcoholismo es uno de los problemas más graves con los que se enfrentan los sistemas de salud, tanto por el alto grado de morbilidad como por el índice de discapacidad y por las complicaciones médicas y psicosociales. La fase de desintoxicación supone la piedra angular en el tratamiento del paciente alcohólico.Métodos: Partimos de una revisión bibliográfica crítica del TDA y de una discusión teórica de las dimensiones que ha de atender un tratamiento eficaz.Resultados: Proponemos una secuencia de fases con características propias ( proceso diagnóstico y primeras medidas, decisiones médicas y psicoterápicas, coordinación multiprofesional del tratamiento, planificación del alta y seguimiento) y discutimos un conjunto de técnicas adaptadas a cada fase del tratamiento (arsenal farmacológico, estandarización de la exploración, trabajo de motivación, prevención secundaria). Proponemos un protocolo de tratamiento escalonado para los diferentes cuadros en orden a su gravedad; éste incluye fármacos eficaces (clometiazol, diazepam, tiapride, clonidina, carbamacepina, haloperidol, disulfiram, acamprosato y naltrexona) así como técnicas psicoterápicas (terapia grupal de confrontación constructiva, análisis de los mecanismos de defensa patológicos, self-management guiado por una reorientación de valores y por técnicas de modificación de conducta).Conclusión: El TDA tiene una dimensión fundamentalmente médica pero su éxito depende de un plan terapéutico multidimensional, pluriprofesional y personalizado que incluya un trabajo de motivación a la abstinencia así como una profilaxis de recaída. SUMMARYBackground: Due to high morbidity as well as severe medical and psychosocial consequences, alcoholism is one of our society's most serious health and social problems. Inpatient detoxification is probably the decisive phase in the whole treatment strategy. Method:We review the related literature and discuss the relevant dimensions of alcohol-withdrawal syndrome treatment strategies.Results: Our discussion is based on an incremental treatment program with specified characteristics at each stage. The stages include: diagnostic process, first measures after admission, medical and psychotherapeutic issues, treatment coordination, and finally, discharge and follow-up planning. We advocate appropriate measures at each stage (pharmacology, examination guide, motivation program, relapse prevention). After reviewing the most prevalent pharmaceutical treatments for alcohol withdrawal, we outline recommended treatments according to the degree of withdrawal, from mild symptoms to delirium tremens. Some drugs were effective, such as: clomethiazole, haloperidol, carbamazepine, tiapride, diazepam, clonidine, disulfiram, acamprosate and naltrexone. There were also effective psychotherapeutic approaches (group psychotherapy with confrontation techniques, defence-mechanism analysis, selfmanagement led by value reorientation and behaviour therapy). Conclusion:The treatment of alcohol-withdrawal syndrome entails a substantial medical ...

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Benzodiazepine antagonism by harmane and other β-carbolines in vitro and in vivo

Cited by 124 publications

References 21 publications

Increased Formation of β-carbolines in Alcoholic Patients following Ingestion of Ethanol

Increased Formation of β-carbolines in Alcoholic Patients following Ingestion of Ethanol

β-Carbolines Selectively Antagonize the Cholecystokinin Action in Isolated Guinea-Pig Gallbladder Muscle

Estrategias en el tratamiento de desintoxicación alcohólica

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