RESUMEN
Epilepsy is a common chronic neurological disorder characterized by recurrent unprovoked seizures. There has been a considerable interest in the development of many antiepileptic and anticonvulsant agents for controlling epilepsy with fewer side effects and improvement of quality of life. Since the terms antiepileptics /anticonvulsants are used interchangeably, this article reviews their classification according to the chemical structure into: hydantoins, oxazolidinediones, succinimides, barbiturates, amides, benzodiazepines, valproic acid and its derivatives, GABA-analogues, cycloalkanes, semicarbazones, γ butyrolactones (GBLs), imidaquinazolines and pyrrolidine derivatives as well as miscellaneous compounds. In addition, the review discusses the different mechanisms of action of antiepileptic and anticonvulsant agents.
Asunto(s)
Anticonvulsivantes/química , Anticonvulsivantes/farmacología , Animales , Anticonvulsivantes/uso terapéutico , Humanos , Convulsiones/tratamiento farmacológico , Convulsiones/metabolismoRESUMEN
A series of new 3-mercapto-2-methyl-propanoyl-pyrrolidine derivatives (V, VIa-e) were designed. A new validated ACE inhibitors pharmacophore model (hypothesis) was generated for the first time in this research from the biologically active (frozen) conformation of Lisinopril-Human ACE complex that was downloaded from PDB, using stepwise technique of CATALYST modules. The molecular modeling compare-fit study of the designed molecules (V, VIa-e), with such ACE inhibitors hypothesis was fulfilled, and several compounds showed significant high simulation fit values. The compounds with high fit values were synthesized and biologically evaluated in vivo as hypotensive agents. It appears that the in vivo hypotensive activity of compounds V, VIa, VIb, and VIe was consistent with their molecular modeling results, and compound VIe showed the highest activity in comparison to Captopril.
Asunto(s)
Inhibidores de la Enzima Convertidora de Angiotensina/química , Antihipertensivos/química , Propionatos/química , Pirrolidinas/química , Inhibidores de la Enzima Convertidora de Angiotensina/síntesis química , Inhibidores de la Enzima Convertidora de Angiotensina/farmacología , Animales , Antihipertensivos/síntesis química , Antihipertensivos/farmacología , Catálisis , Gatos , Simulación por Computador , Bases de Datos de Proteínas , Diseño de Fármacos , Modelos Químicos , Modelos Moleculares , Propionatos/síntesis química , Propionatos/farmacología , Pirrolidinas/síntesis química , Pirrolidinas/farmacología , Relación Estructura-ActividadRESUMEN
We have performed immunophenotyping studies on 186 untreated cases of acute lymphoblastic leukemia (ALL) in an Egyptian population, using panels of monoclonal antibodies (mAb) and an avidin-biotin-immunoperoxidase detection system. Sixty-two of these cases were tested with a panel of mAb directed against the T-cell markers CD2, CD4, CD8, B-cell markers CD20, kappa and lambda, the common ALL antigen (common ALLa) and class II HLA antigens. The remaining 124 cases were also tested with additional markers of T- and B-cell precursors, namely CD7 and CD19. The common leukocyte antigen, T200, was used to exclude nonhemopoietic neoplasms. Cases that remained unclassifiable were further tested with a wider panel of T-cell markers, including CD1, CD2, CD3 and CD5. In some cases multiple mAb directed against the same antigens were used. The relative frequencies of common ALL and B ALL were calculated from the total number of cases and were found to be 39.2% and 3.2%, respectively. The proportions of T-cell and null leukemias were calculated from the better characterized subgroup of 124 cases, and were found to be 50% and 4.8%, respectively. In our series, the age distribution of common ALL revealed a peak at 2-5 yr, but this was partially obscured in the entire series by the high proportion of T-cell cases, which had an age peak between 4 and 12 yr of age. Our results demonstrate marked differences in the phenotypic pattern of ALL in Egypt compared to Western Countries, the predominant finding being a relative excess of T-cell ALL and a paucity of common ALL cases. At present it is not clear whether this results from an increased incidence of T-cell ALL or a decreased incidence of common ALL.
Asunto(s)
Leucemia-Linfoma Linfoblástico de Células Precursoras/clasificación , Adolescente , Adulto , Anticuerpos Monoclonales , Antígenos de Diferenciación/análisis , Linfoma de Burkitt/clasificación , Linfoma de Burkitt/epidemiología , Linfoma de Burkitt/inmunología , Niño , Preescolar , Egipto , Femenino , Humanos , Lactante , Leucemia-Linfoma de Células T del Adulto/clasificación , Leucemia-Linfoma de Células T del Adulto/epidemiología , Leucemia-Linfoma de Células T del Adulto/inmunología , Masculino , Persona de Mediana Edad , Fenotipo , Leucemia-Linfoma Linfoblástico de Células Precursoras/epidemiología , Leucemia-Linfoma Linfoblástico de Células Precursoras/inmunología , Factores SexualesRESUMEN
A double-blind study has been performed to search for the possible effect of khellin in psoriasis. 10 patients were treated orally with khellin and subsequently exposed to sunlight for 4 months; a total of 8 cases responded positively with variable degrees of clearance. None of 10 controls had any response. A relapse-free duration of 3 years was recorded for 6 out of the 8 responders. This study would introduce the nonpsoralen compound khellin as a possible agent for the therapy of psoriasis.
Asunto(s)
Khellin/administración & dosificación , Psoriasis/tratamiento farmacológico , Adolescente , Adulto , Método Doble Ciego , Femenino , Helioterapia , Humanos , Masculino , Persona de Mediana EdadAsunto(s)
Analgésicos/síntesis química , Ciclohexilaminas/síntesis química , Antagonistas de los Receptores Histamínicos H1/síntesis química , Analgésicos/farmacología , Animales , Ciclohexilaminas/farmacología , Cobayas , Antagonistas de los Receptores Histamínicos H1/farmacología , Ratones , Relación Estructura-ActividadRESUMEN
An anticipated effect of khellin, related to its chemical structure, in the photochemotherapy of amelanosis has been investigated. In a double-blind clinical study, khellin has been orally administered to 30 vitiligo patients for 4 months with subsequent exposure to natural sunlight. At the end of the trial period, 5 patients out of 30 (16.6%) repigmented 90-100%; 7 cases (23.3%) repigmented 50-60% of the vitiliginous areas treated; 11 (36.6%) repigmented 25% or less, and 7 subjects (23.3%) showed negative response. 30 control subjects failed to repigment at all. The achieved repigmentation was stable after drug cessation for a period of 1 year. These data add a previously unreported effect for the non-psoralen compound, khellin, in the therapy of vitiligo.
Asunto(s)
Khellin/uso terapéutico , Fotoquimioterapia/métodos , Vitíligo/tratamiento farmacológico , Adolescente , Adulto , Niño , Ensayos Clínicos como Asunto , Método Doble Ciego , Femenino , Humanos , Khellin/farmacología , Masculino , Persona de Mediana Edad , Pigmentación de la Piel/efectos de los fármacos , Luz SolarRESUMEN
Amikacin was used in the treatment of severe urinary tract infections in twenty-five seriously ill patients. In twenty-four of the patients, cystitis or pyelonephritis complicated carcinoma of the bladder. Structural changes in the urinary tract, resulting from schistosomiasis, presented additional obstacles to treatment in many of the patients. The most commonly isolated pathogens were Escherichia coli and Pseudomonas. Most patients received 500 mg of amikacin every twelve hours. Three patients experienced adverse renal reactions which showed subsequent improvement. Amikacin effected twenty-one (84%) complete cures and four (16%) clinical cures in the twenty-five patients. This represents 100% clinical success in this study.
Asunto(s)
Amicacina/uso terapéutico , Cistitis/tratamiento farmacológico , Kanamicina/análogos & derivados , Pielonefritis/tratamiento farmacológico , Neoplasias de la Vejiga Urinaria/complicaciones , Adulto , Anciano , Amicacina/efectos adversos , Cistitis/complicaciones , Infecciones por Escherichia coli/tratamiento farmacológico , Femenino , Humanos , Masculino , Persona de Mediana Edad , Infecciones por Pseudomonas/tratamiento farmacológico , Pielonefritis/complicacionesRESUMEN
"Twenty cases of Down's syndrome and 25 age-matched normal controls were subjected to hematologic study including Hb, R.B.Cs, W.B.Cs., HbF., bone marrow, protein electrophoresis and chromosomal study. Peripheral blood and bone marrow showed noticeable increase in granulocytes, increase in staff, and decrease in lymphocytes in mongols as compared to the controls. HbF was lower than normal in 18 cases. The other two showed abnormally high HbF. Protein electrophoretic study showed normal pattern except one case in which a remarkable decrease in the Beta and Gamma Fraction was noticed".
Asunto(s)
Síndrome de Down/diagnóstico , Electroforesis de las Proteínas Sanguíneas , Preescolar , Cromosomas Humanos 21-22 e Y , Síndrome de Down/sangre , Síndrome de Down/genética , Pruebas Hematológicas , Humanos , Lactante , TrisomíaRESUMEN
A new drug, NSC-140117, was used in the management of 15 patients who had late bronchogenic carcinoma and were unable to receive surgical or radiotherapeutic treatment. Good responses in the form of 90% shrinkage in the size of the lesionswere encountered in nine patients (60%). Response is still being maintained from 6 months to 1.5 years after the start of therapy. No toxic effects, including hematopoietic toxicity, were encountered.