ABSTRACT
High activity antiretroviral therapy may exacerbate the activity of ergot alkaloids due to an inhibition of cytochrome P450. We report a 57 years old female with AIDS treated with lamivudine, zidovudine, atazanavir, ritonavir and cotrimoxazole presenting with ischemic signs in the four limbs. There was acrocyanosis and weak radial and ulnar pulses. A family member referred that the patient used ergot alkaloids for headaches. An ergotism due to the simultaneous use of ergot alkaloids and antiretroviral therapy was suspected. The latter was discontinued and intravenous nitroglycerin, nifedipine and pentoxifyline were started with good results.
Subject(s)
Humans , Female , Middle Aged , Ergotism/etiology , Antiretroviral Therapy, Highly Active , Ergot Alkaloids/adverse effects , HIV Infections/drug therapy , Ergotism/diagnosis , Ergotism/therapyABSTRACT
The present study deals with the production of ergot alkaloids from Penicillium commune and Penicillium citrinum, using surface culture fermentation process. Impact of various inorganic salts was tested on the production of ergot alkaloids during the optimization studies of fermentation medium such as impact of various concentration levels of succinic acid, ammonium chloride, MgSO[4], FeSO[4], ZnSO[4], pH and the effect of various incubation time periods was also determined on the production of ergot alkaloids from Penicillium commune and Penicillium citrinum. Highest yield of ergot alkaloids was obtained when Penicillium commune and Penicillium citrinum that were grown on optimum levels of ingredients such as 2g succinic acid, 1.5 and 2g NH[4]Cl, 1.5g MgSO[4], 1g FeSO[4], 1 and 1.5g ZnSO[4] after 21 days of incubation time period using pH 5 at 25[degree]C incubation temperature in the fermentation medium. Ergot alkaloids were determined using Spectrophotometry and Thin Layer Chromatography [TLC] techniques
Subject(s)
Ergot Alkaloids , Spectrophotometry , Chromatography, Thin Layer , Fermentation , Culture TechniquesABSTRACT
The present study was designed to isolate and purify chemical constituents from solid culture of endophyte Aspergillus terreus LQ, using silica gel column chromatography, gel filtration with Sephadex LH-20, and HPLC. Fumigaclavine I (1), a new alkaloid, was obtained, along with seven known compounds, including fumigaclavine C (2), rhizoctonic acid (3), monomethylsulochrin (4), chaetominine (5), spirotryprostatin A (6), asperfumoid (7), and lumichrome (8). The structure of compound 1 was elucidated by various spectroscopic analyses (UV, MS, 1D and 2D NMR). The in vitro cytotoxicity of compound 1 was determined by MTT assay in human hepatocarcinoma cell line SMMC-7721, showing weaker cytotoxicity, compared with cisplatin, a clinically used cancer chemotherapeutic agent.
Subject(s)
Humans , Antineoplastic Agents , Chemistry , Aspergillus , Chemistry , Cell Line, Tumor , Cell Survival , Endophytes , Chemistry , Ergot Alkaloids , Chemistry , Magnetic Resonance Spectroscopy , Molecular Structure , Oryza , MicrobiologyABSTRACT
Introdução: As síndromes hemorrágicas estão entre as principais causas obstétricas diretas de mortes maternas. Segundo dados da Organização Mundial de Saúde estima-se uma morte a cada quatro minutos. A hemorragia pós-parto reflete diretamente a qualidade da assistência, sendo uma das causas potencialmente prevenível e tratável. O desenvolvimento de manejos clínicos para seu controle torna-se de extrema importância na redução da mortalidade materna. Objetivo: Definir a melhor estratégia para a prevenção e o tratamento da hemorragia pós-parto, enfatizando o manejo ativo no terceiro estágio do trabalho de parto. Métodos: Foi realizada uma revisão de literatura no banco de dados Medline/PubMed, LILACS/SciELO, Cochrane Library e no site do Royal College of Obstetricians and Gynaecologists em busca das melhores evidências clínicas disponíveis, considerando-se o grau de recomendação. Resultados: Verificou-se que o manejo ativo da terceira fase do trabalho de parto é de fundamental importância para a prevenção da hemorragia pós-parto. O uso de uterotônicos, sendo a ocitocina o fármaco de primeira linha para este fim, a tração controlada de cordão umbilical com massagem uterina são a base deste tratamento. O tratamento cirúrgico também pode ser necessário e deve ter uma indicação precisa e de acordo com a experiência do cirurgião. Conclusão: Uma boa assistência a gestantes durante o trabalho de parto, principalmente uma conduta ativa no terceiro estágio, interfere de forma positiva para a prevenção de hemorragias maternas graves, contribuindo para o controle e diminuição da mortalidade materna.(AU)
Introduction: The haemorrhagic syndromes are the main causes of direct obstetric maternal deaths. According to data from the World Health Organization estimated one death every four minutes. Postpartum haemorrhage directly reflects the quality of care, being a potentially preventable and treatable causes. The development of clinical managements to their control it becomes of extremely important for reduction maternal mortality. Objective: The aim of this work was to search in literature the most important strategy to prevent and the treat the postpartum haemorrhage, emphaesing the active management in the third stage of labour. Methods: A revision of literature in the Medline/ PubMed, LILACS/ SciELO, Cochrane Library and in the site of the Royal College of Obstetricians and Gynaecologists data base was carried through, in search of the best clinical evidences available, take into account also the degree of recommendation. Results: It was founded that the active management of third stage of labour is fundamental for prevention of postpartum hemorrhage. The oxytocin was first line drug for this effect, the control umbilical lace traction with uterine massage is the base of this treatment. The surgery can be necessary and must have a straight indication and the experience of surgeon has a lot of importance. Conclusion: A good care for pregnant women during the labour, mainly in the active third stage of labour interferes in a positive way to prevent severe mothers' haemorrhages, and contributes to the reduction of maternal mortality.(AU)
Subject(s)
Humans , Female , Pregnancy , Labor, Obstetric , Postpartum Hemorrhage/prevention & control , Oxytocin/therapeutic use , Prostaglandins/therapeutic use , Clinical Protocols , Ergot Alkaloids/therapeutic use , Clinical Audit , Postpartum Hemorrhage/surgery , Postpartum Hemorrhage/drug therapyABSTRACT
Diidroergocristina (DHEC) é um fármaco semi-sintético, derivada do alcalóide do Ergot, principalmente utilizada para enxaqueca e estudada em distúrbios cognitivos relacionados ao envelhecimento. No presente estudo, o seu principal metabólito 8-hidroxidiidroergocristina (8'-OH-DHEC) foi produzido através de incubação de preparações enzimáticas de fígado de boi usando o Mesilato de Diidroergocristina como substrato. Foi feita uma avaliação de qual o melhor método de preparação enzimática a ser utilizado para produção do padrão do metabólito ativo em grande escala através da comparação de atividade enzimática entre microssomos e S12, ambos extraídos de heptócitos de fígado bovino. A purificação desse metabólito foi feita através da utilização de uma coluna cromatográfica clássica com sílica gel e cromatografia líquida de fase reversa. Sua identificação foi baseada em mensuração de sua massa molecular por espectro de fragmentação de massa e Ressonância Magnética (NMR - 1H/13C). Através da produção dessa substância in vitro, um método rápido, sensível e robusto de determinação da DHEC e seu principal metabólito foi desenvolvido e validado em LC-MS/MS a partir de análise de plasma humano. Bromocriptina foi utilizado com padrão interno e os limites de quantificação da DHEC e 8-OH-DHEC foram 10 pg/ml e 20 pg/ml, respectivamente. Os parâmetros farmacocinéticos foram investigados em 12 voluntários masculinos através da administração de uma dose única oral de 18mg...
Dihydroergocristine (DHEC) is a semi-synthetic drug mainly used for migraine and studied in age-related cognitive impairment. In this study, its major metabolite 8´-hydroxy-dihydroergocristine (8´-OH-DHEC) was produced in incubates of a bovine liver preparation using dihydroergocristine mesylate (DHECM) as substrate. An evaluation of the best enzymatic preparation method was done in order to verify the adequate process for massive production of the metabolite. A comparison between microssomes and S12 was performed, where both preparations were extracted from bovine hepatocytes. Purification was achieved by flash silica gel column and reverse phase liquid chromatographies, and identification was based on accurate molecular mass measurements, mass fragmentation spectra and NMR (1H/13C) chemical shifts. By using the substance produced in vitro, a fast, sensitive, specific and robust LC/MS/MS method for the simultaneous determination of DHEC and its major metabolite in human plasma was...
Subject(s)
Ergot Alkaloids/pharmacokinetics , Dihydroergocristine , In Vitro Techniques , Spectrometry, Mass, Electrospray Ionization , Chromatography, Liquid/methods , Spectrometry, Mass, Electrospray Ionization/methodsABSTRACT
Cases of acute myocardial infarction (AMI) that occurs during pregnancy or postpartum are rarely reported. Ergot derivatives were known to induce spasmodic contraction of coronary arteries. Administration of ergot derivatives can cause AMI even in normal healthy people. Several cases are also reported that ergot derivatives may trigger severe AMI in postpartum period. Here, we report a case of a forty-year-old pregnant woman who was succeeded to be pregnant by artificial fertilization died after treatment with ergot derivatives. Examinations of autopsy have revealed AMI with severe coronary atherosclerosis. This case is the first report which shows aggravation of preexistent severe coronary atherosclerosis after postpartum infusion of ergot derivatives.
Subject(s)
Female , Humans , Pregnancy , Autopsy , Coronary Artery Disease , Coronary Vessels , Ergot Alkaloids , Fertilization , Myocardial Infarction , Postpartum Period , Pregnant WomenABSTRACT
Cases of acute myocardial infarction (AMI) that occur during pregnancy or postpartum are rarely reported. Ergot derivatives are known to induce the spasmodic contraction of coronary arteries. Administration of ergot derivatives can cause AMI, even in normal healthy people. In several reported cases, ergot derivatives triggered severe AMI during the postpartum period. Here, we report the case of a forty-year-old woman who was successfully impregnated by artificial fertilization and died after treatment with ergot derivatives. The autopsy revealed AMI with severe coronary atherosclerosis. This is the first case that reports aggravation of pre-existent severe coronary atherosclerosis after postpartum infusion of ergot derivtives.
Subject(s)
Pregnancy , Humans , Female , Adult , Postpartum Period , Myocardial Infarction/chemically induced , Maternal Age , Ergot Alkaloids/adverse effects , Coronary Artery Disease/chemically inducedABSTRACT
Los autores informan sobre 7 casos clínicos de ergotismo gangrenoso (6 mujeres y 1 hombre) provocado por la ingestión inmoderada de ergotamina ministrada para aliviar las crisis de migraña. En todos los enfermos estaban presentes síntomas y signos clínicos, ecográficos y angiográficos de constricción arterial severa y ninguno sufrió alucinaciones. El ergotismo fue tratado con la suspensión de la ergotamina, la ministración de vasodilatadores y la simpatectomía. Después del tratamiento, la mejoría de los 7 pacientes fue evidente por la desaparición de los síntomas y signos de isquemia distal y aumento significativo (P < 0.05) del índice pletismográfico de perfusión sanguínea, medido por medio de la ecografía Doppler. Estos cambios fueron observados aún en un paciente que perdió 2 dedos del pie derecho, secundariamente al ergotismo gangrenoso. Si bien, ninguno de los enfermos manifestó alucinaciones, los autores hacen referencia al primer uso del cornezuelo de centeno, reconocido históricamente, en las ceremonias mágico religiosas de Eleusis de la Grecia clásica; así, como al caso de brujería de Salem, Nueva Inglaterra, en 1692. La migraña no puede ser considerada banal; frecuentemente, causa desesperación del enfermo, que se intoxica con la ergotamina, cuando es sólo este medicamento el recomendado por su médico tratante. En consecuencia, el médico especialista, familiar, general o rural, debe conocer perfectamente la terapia profiláctica de las crisis de migraña con medicamentos vasodilatadores y así, reducir la posibilidad de ergotismo.