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[PMID]:25458200
[Au] Autor:Rogers GB; Bruce KD; Martin ML; Burr LD; Serisier DJ
[Ad] Endereço:Infection and Immunity Theme, South Australia Health and Medical Research Institute, North Terrace, Adelaide, SA, Australia; School of Medicine, Flinders University, Bedford Park, Adelaide, SA, Australia.
[Ti] Título:The effect of long-term macrolide treatment on respiratory microbiota composition in non-cystic fibrosis bronchiectasis: an analysis from the randomised, double-blind, placebo-controlled BLESS trial.
[So] Source:Lancet Respir Med;2(12):988-96, 2014 Dec.
[Is] ISSN:2213-2619
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Long-term macrolide treatment has proven benefit in inflammatory airways diseases, but whether it leads to changes in the composition of respiratory microbiota is unknown. We aimed to assess whether long-term, low-dose erythromycin treatment changes the composition of respiratory microbiota in people with non-cystic fibrosis bronchiectasis. METHODS: Microbiota composition was determined by 16S rRNA gene sequencing of sputum samples from participants in the BLESS trial, a 12-month, double-blind, placebo-controlled trial of twice-daily erythromycin ethylsuccinate (400 mg) in adult patients with non-cystic fibrosis bronchiectasis and at least two infective exacerbations in the preceding year. The primary outcome was within-patient change in respiratory microbiota composition (assessed by Bray-Curtis index) between baseline and week 48, comparing erythromycin with placebo. The BLESS trial is registered with the Australian New Zealand Clinical Trials Registry, number ACTRN12608000460303. FINDINGS: The BLESS trial took place between Oct 15, 2008, and Dec 14, 2011. Paired sputum samples were available from 86 randomly assigned patients, 42 in the placebo group and 44 in the erythromycin group. The change in microbiota composition between baseline and week 48 was significantly greater with erythromycin than with placebo (median Bray-Curtis score 0·52 [IQR 0·14-0·78] vs 0·68 [0·46-0·93]; median difference 0·16, 95% CI 0·01-0·33; p=0·03). In patients with baseline airway infection dominated by Pseudomonas aeruginosa, erythromycin did not change microbiota composition significantly. In those with infection dominated by organisms other than P. aeruginosa, erythromycin caused a significant change in microbiota composition (p=0·03 [by analysis of similarity]), representing a reduced relative abundance of Haemophilus influenzae (35·3% [5·5-91·6] vs 6·7% [0·8-74·8]; median difference 12·6%, 95% CI 0·4-28·3; p=0·04; interaction p=0·02) and an increased relative abundance of P aeruginosa (0·02% [0·00-0·33] vs 0·13% [0·01-39·58]; median difference 6·6%, 95% CI 0·1-37·1; p=0·002; interaction p=0·45). Compared with placebo, erythromycin reduced the rate of pulmonary exacerbations over the 48 weeks of the study in patients with P. aeruginosa-dominated infection (median 1 [IQR 0-3] vs 3 [2-5]; median difference -2, 95% CI -4 to -1; p=0·01), but not in those without P. aeruginosa-dominated infection (1 [0-2] vs 1 [0-3]; median difference 0, -1 to 0; p=0·41; interaction p=0·04). INTERPRETATION: Long-term erythromycin treatment changes the composition of respiratory microbiota in patients with bronchiectasis. In patients without P. aeruginosa airway infection, erythromycin did not significantly reduce exacerbations and promoted displacement of H. influenzae by more macrolide-tolerant pathogens including P. aeruginosa. These findings argue for a cautious approach to chronic macrolide use in patients without P. aeruginosa airway infection. FUNDING: Mater Adult Respiratory Research Trust Fund.
[Mh] Termos MeSH primário: Antibacterianos/administração & dosagem
Bronquiectasia/tratamento farmacológico
Etilsuccinato de Eritromicina/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Bronquiectasia/microbiologia
Método Duplo-Cego
Esquema de Medicação
Feminino
Infecções por Haemophilus/tratamento farmacológico
Haemophilus influenzae
Seres Humanos
Assistência de Longa Duração
Masculino
Microbiota/efeitos dos fármacos
Meia-Idade
Infecções por Pseudomonas/tratamento farmacológico
Pseudomonas aeruginosa
RNA Bacteriano/isolamento & purificação
Sistema Respiratório/microbiologia
Escarro/microbiologia
Adulto Jovem
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (RNA, Bacterial); 1014KSJ86F (Erythromycin Ethylsuccinate)
[Em] Mês de entrada:1511
[Cu] Atualização por classe:141204
[Lr] Data última revisão:
141204
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141203
[St] Status:MEDLINE


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[PMID]:25458199
[Au] Autor:Hurst JR
[Ad] Endereço:UCL Respiratory Medicine, University College London, London NW3 2PF, UK. Electronic address: j.hurst@ucl.ac.uk.
[Ti] Título:Microbial dysbiosis in bronchiectasis.
[So] Source:Lancet Respir Med;2(12):945-7, 2014 Dec.
[Is] ISSN:2213-2619
[Cp] País de publicação:England
[La] Idioma:eng
[Mh] Termos MeSH primário: Antibacterianos/administração & dosagem
Bronquiectasia/tratamento farmacológico
Etilsuccinato de Eritromicina/administração & dosagem
[Mh] Termos MeSH secundário: Feminino
Seres Humanos
Masculino
[Pt] Tipo de publicação:COMMENT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 1014KSJ86F (Erythromycin Ethylsuccinate)
[Em] Mês de entrada:1511
[Cu] Atualização por classe:141204
[Lr] Data última revisão:
141204
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141203
[St] Status:MEDLINE


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[PMID]:23649599
[Au] Autor:Métivier R; Bourven I; Labanowski J; Guibaud G
[Ad] Endereço:Groupement de Recherche Eau Sol Environnement (EA 4330), Faculté des Sciences et Techniques, Université de Limoges, 123 Av. Albert Thomas, 87 060, Limoges, France.
[Ti] Título:Interaction of erythromycin ethylsuccinate and acetaminophen with protein fraction of extracellular polymeric substances (EPS) from various bacterial aggregates.
[So] Source:Environ Sci Pollut Res Int;20(10):7275-85, 2013 Oct.
[Is] ISSN:1614-7499
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Extracellular polymeric substances (EPS) are, along with microbial cells, the main components of the biological sludges used in wastewater treatment and natural biofilms. EPS play a major role in removing pollutants from water by means of sorption. The ability of soluble EPS (S-EPS) and bound EPS (B-EPS) derived from various bacterial aggregates (flocs, granules, biofilms) to bind at pH 7.0 ± 0.1 to two pharmaceutical substances, acetaminophen (ACE) and erythromycin ethylsuccinate (ERY), has been investigated using the fluorescence quenching method. Two intense fluorescence peaks, A (Ex/Em range, 200-250/275-380 nm) and B (Ex/Em range, 260-320/275-360 nm), corresponding respectively to the aromatic protein region and soluble microbial by-product-like region, were identified in a three-dimensional excitation-emission matrix of EPS samples. The fluorescence peak, which corresponds to humic-like substances, was also identified though at low intensity. The ability of EPS to bind ACE was found to exceed that for ERY. The aromatic protein fraction of EPS displays a slightly higher affinity for drugs than that shown by the soluble microbial by-product-like fraction. The S-EPS and B-EPS present the same affinity for ACE and ERY. The effective quenching constants (log K) derived from the Stern-Volmer Equation equaled at peak A (with S-EPS): 3.7 ± 0.2 to 4.0 ± 0.1 for ACE and 2.1 ± 0.3 to 2.7 ± 0.1 for ERY. With B-EPS, these values were 3.9 ± 0.1 to 4.0 ± 0.1 for ACE and 2.0 ± 0.2 to 2.6 ± 0.1 for ERY. Our results suggest that the weaker EPS affinity for ERY than for ACE serves to partially explain why only about 50-80 % of ERY is removed from wastewater at the treatment plant. Moreover, this work demonstrates that EPS from natural river biofilms are able to bind drugs, which in turn may limit the mobility of drugs in natural waters.
[Mh] Termos MeSH primário: Acetaminofen/química
Etilsuccinato de Eritromicina/química
Polissacarídeos Bacterianos/química
Esgotos/química
Poluentes Químicos da Água/química
[Mh] Termos MeSH secundário: Biofilmes/crescimento & desenvolvimento
Concentração de Íons de Hidrogênio
Polímeros/química
Espectrometria de Fluorescência/métodos
Eliminação de Resíduos Líquidos/métodos
Águas Residuais/química
Águas Residuais/microbiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Polymers); 0 (Polysaccharides, Bacterial); 0 (Sewage); 0 (Waste Water); 0 (Water Pollutants, Chemical); 1014KSJ86F (Erythromycin Ethylsuccinate); 362O9ITL9D (Acetaminophen)
[Em] Mês de entrada:1401
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130508
[St] Status:MEDLINE
[do] DOI:10.1007/s11356-013-1738-2


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[PMID]:22512082
[Au] Autor:Cho YA; Lee W; Choi JS
[Ad] Endereço:School of Medicine, Research Institute of Life Science, Gyeongsang National University, Jinju, Republic of Korea.
[Ti] Título:Effects of curcumin on the pharmacokinetics of tamoxifen and its active metabolite, 4-hydroxytamoxifen, in rats: possible role of CYP3A4 and P-glycoprotein inhibition by curcumin.
[So] Source:Pharmazie;67(2):124-30, 2012 Feb.
[Is] ISSN:0031-7144
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The effects of curcumin, a natural anti-cancer compound, on the bioavailability and pharmacokinetics of tamoxifen and its metabolite, 4-hydroxytamoxifen, were investigated in rats. Tamoxifen and curcumin interact with cytochrom P450 (CYP) enzymes and P-glycoprotein, and the increase in the use of health supplements may result in curcumin being taken concomitantly with tamoxifen as a combination therapy to treat or prevent cancer. A single dose of tamoxifen was administered orally (9 mg x kg(-1)) with or without curcumin (0.5, 2.5 and 10 mg x kg(-1)) and intravenously (2mg x kg(-1)) with or without curcumin (2.5 and 10 mg x kg(-1)) to rats. The effects of curcumin on P-glycoprotein (P-gp) and CYP3A4 activity were also evaluated. Curcumin inhibited CYP3A4 activity with 50% inhibition concentration (IC50) values of 2.7 microM. In addition, curcumin significantly (P < 0.01 at 10 microM) enhanced the cellular accumulation of rhodamine-123 in MCF-7/ADR cells overexpressing P-gp in a concentration-dependent manner. This result suggested that curcumin significantly inhibited P-gp activity. Compared to the oral control group (given tamoxifen alone), the area under the plasma concentration-time curve (AUC(0-infinity)) and the peak plasma concentration (C(max)) of tamoxifen were significantly (P < 0.05 for 2.5 mg x kg(-1); P < 0.01 for 10 mg x kg(-1)) increased by 33.1-64.0% and 38.9-70.6%, respectively, by curcumin. Consequently, the absolute bioavailability of tamoxifen in the presence of curcumin (2.5 and 10 mg x kg(-1)) was 27.2-33.5%, which was significantly enhanced (P < 0.05 for 2.5 mg x kg(-1); P < 0.01 for 10 mg x kg(-1)) compared to that in the oral control group (20.4%). Moreover, the relative bioavailability of tamoxifen was 1.12- to 1.64-fold greater than that in the control group. Furthermore, concurrent use of curcumin significantly decreased (P < 0.05 for 10 mg x kg(-1)) the metabolite-parent AUC ratio (MR), implying that curcumin may inhibit the CYP-mediated metabolism of tamoxifen to its active metabolite, 4-hydroxytamoxifen. The enhanced bioavailability of tamoxifen by curcumin may be mainly due to inhibition of the CYP3A4-mediated metabolism of tamoxifen in the small intestine and/or in the liver and to inhibition of the P-gp efflux transporter in the small intestine rather than to reduction of renal elimination of tamoxifen, suggesting that curcumin may reduce the first-pass metabolism of tamoxifen in the small intestine and/or in the liver by inhibition of P-gp or CYP3A4 subfamily.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/antagonistas & inibidores
Antineoplásicos Hormonais/farmacocinética
Curcumina/farmacologia
Inibidores das Enzimas do Citocromo P-450
Tamoxifeno/análogos & derivados
[Mh] Termos MeSH secundário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Administração Oral
Animais
Antineoplásicos Hormonais/sangue
Área Sob a Curva
Disponibilidade Biológica
Linhagem Celular Tumoral
Cromatografia Líquida de Alta Pressão
Citocromo P-450 CYP3A
Sistema Enzimático do Citocromo P-450/metabolismo
Etilsuccinato de Eritromicina
Corantes Fluorescentes
Seres Humanos
Indicadores e Reagentes
Injeções Intravenosas
Masculino
Ratos
Ratos Sprague-Dawley
Rodamina 123
Tamoxifeno/sangue
Tamoxifeno/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Antineoplastic Agents, Hormonal); 0 (Cytochrome P-450 Enzyme Inhibitors); 0 (Fluorescent Dyes); 0 (Indicators and Reagents); 094ZI81Y45 (Tamoxifen); 1014KSJ86F (Erythromycin Ethylsuccinate); 17197F0KYM (afimoxifene); 1N3CZ14C5O (Rhodamine 123); 9035-51-2 (Cytochrome P-450 Enzyme System); EC 1.14.14.1 (Cyp3a2 protein, rat); EC 1.14.14.1 (Cytochrome P-450 CYP3A); IT942ZTH98 (Curcumin)
[Em] Mês de entrada:1205
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120420
[St] Status:MEDLINE


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[PMID]:20235137
[Au] Autor:Liu YM; Shi YM; Liu ZL; Peng LF
[Ad] Endereço:College of Chemistry and Chemical Engineering, Xinyang Normal University, Xinyang, PR China. liuym9518@sina.com
[Ti] Título:Sensitive determination of tilmicosin, erythromycin ethylsuccinate and clindamycin by CE with electrochemiluminescence detection using azithromycin as internal standard and its applications.
[So] Source:J Sep Sci;33(9):1305-11, 2010 May.
[Is] ISSN:1615-9314
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A sensitive approach for the simultaneous determination of tilmicosin, erythromycin ethylsuccinate and clindamycin was developed by CE coupled with electrochemiluminescence detection with ionic liquid. The parameters for CE, electrochemiluminescence detection and the effect of ionic liquid were investigated systematically. The three analytes were well separated and detected within 8 min. The limits of detection (S/N=3) of tilmicosin, erythromycin ethylsuccinate and clindamycin are 3.4x10(-9), 2.3x10(-8) and 1.3x10(-8) mol/L, respectively. The precisions (RSD%) of the peak area and the migration time are from 0.8 to 1.5% and from 0.2 to 0.5% within a day and from 1.8 to 2.7% and from 0.6 to 0.8% in 3 days, respectively. The limits of quantitation (S/N=10) of tilmicosin, erythromycin ethylsuccinate and clindamycin are 3.2x10(-8), 2.9x10(-7) and 9.1x10(-8) mol/L in human urines and 5.5x10(-8), 3.2x10(-7) and 2.1x10(-7) mol/L in milk samples, respectively. The recoveries of three analytes at different concentration levels in urine, milk and drugs are between 90.0 and 104.7%. The proposed method was successfully applied to the determination of three analytes in human urine, milk and drugs.
[Mh] Termos MeSH primário: Antibacterianos/análise
Azitromicina/análise
Clindamicina/análise
Eletroforese Capilar/métodos
Etilsuccinato de Eritromicina/análise
Tilosina/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Antibacterianos/urina
Tampões (Química)
Clindamicina/urina
Etilsuccinato de Eritromicina/urina
Feminino
Seres Humanos
Concentração de Íons de Hidrogênio
Limite de Detecção
Luminescência
Leite/química
Padrões de Referência
Tilosina/análise
Tilosina/urina
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Buffers); 1014KSJ86F (Erythromycin Ethylsuccinate); 3U02EL437C (Clindamycin); 83905-01-5 (Azithromycin); XL4103X2E3 (tilmicosin); YEF4JXN031 (Tylosin)
[Em] Mês de entrada:1007
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100318
[St] Status:MEDLINE
[do] DOI:10.1002/jssc.200900843


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[PMID]:19924535
[Au] Autor:Moshiree B; McDonald R; Hou W; Toskes PP
[Ad] Endereço:Division of Gastroenterology, Hepatology and Nutrition, University of Florida, Gainesville, FL 32610, USA. moshib@medicine.ufl.edu
[Ti] Título:Comparison of the effect of azithromycin versus erythromycin on antroduodenal pressure profiles of patients with chronic functional gastrointestinal pain and gastroparesis.
[So] Source:Dig Dis Sci;55(3):675-83, 2010 Mar.
[Is] ISSN:1573-2568
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Current pharmacologic treatments for gastroparesis have been disappointing due to the limited options available. Erythromycin ethylsuccinate is a potent prokinetic agent that stimulates gastric emptying. Recently, erythromycin has been linked to the occurrences of sudden cardiac death due to QT prolongation. Azithromycin is similar to erythromycin in structure but does not have significant drug-drug interactions as seen with erythromycin. PURPOSE: This study aims to determine whether azithromycin stimulates antral activity in patients with chronic gastrointestinal pain and refractory gastroparesis. METHODS: Small bowel manometric data on 30 patients undergoing clinical evaluation for chronic digestive problems or documented refractory gastroparesis were reviewed. Antral activity was measured after infusion of erythromycin 250 mg intravenous and azithromycin (500 or 250 mg intravenous) given at different intervals during the small bowel manometry. The parameters measured included the total duration of effect, mean amplitude of antral contractions, duration of the highest antral contraction phase, number of cycles per minute, and the motility index. RESULTS: Comparison of erythromycin and azithromycin at similar doses showed a similar positive effect on antral activity. However, comparison of erythromycin and azithromycin at the higher dose of 500 mg showed that the mean amplitude, duration of antral activity, and motility index were significantly increased with azithromycin (P < 0.05). CONCLUSIONS: Azithromycin stimulates antral activity similar to erythromycin and moreover has a longer duration of effect. However, unlike erythromycin, azithromycin does not have significant drug-drug interactions and maybe a potential new medication for the treatment of gastroparesis and gastrointestinal dysmotility.
[Mh] Termos MeSH primário: Dor Abdominal/tratamento farmacológico
Antibacterianos/uso terapêutico
Azitromicina/uso terapêutico
Etilsuccinato de Eritromicina/uso terapêutico
Fármacos Gastrointestinais/uso terapêutico
Gastroparesia/tratamento farmacológico
Antro Pilórico/efeitos dos fármacos
[Mh] Termos MeSH secundário: Dor Abdominal/fisiopatologia
Adulto
Idoso
Antibacterianos/farmacologia
Azitromicina/farmacologia
Doença Crônica
Etilsuccinato de Eritromicina/farmacologia
Feminino
Fármacos Gastrointestinais/farmacologia
Motilidade Gastrointestinal/fisiologia
Gastroparesia/fisiopatologia
Seres Humanos
Masculino
Manometria
Meia-Idade
Antro Pilórico/fisiopatologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Gastrointestinal Agents); 1014KSJ86F (Erythromycin Ethylsuccinate); 83905-01-5 (Azithromycin)
[Em] Mês de entrada:1003
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:091120
[St] Status:MEDLINE
[do] DOI:10.1007/s10620-009-1038-3


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[PMID]:20037552
[Au] Autor:Bogomil'skii MR; Dreval' AA; D'iakonova IN; Rakhmanova IV; Tikhomirov AM; Iarygin VN
[Ti] Título:[Specific ototoxic effects of monomycin in immature animals].
[So] Source:Vestn Otorinolaringol;(5):26-9, 2009.
[Is] ISSN:0042-4668
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Dynamics of the hearing function was evaluated using immature animals based on the SSCP data. Morphological characteristics of the cochlear auditory ganglion were studied after administration of therapeutic doses of the ototoxic antibiotic monomycin. Untreated animals served as controls. The results of morphofunctional investigations were evaluated in comparison with the similar data obtained in adult cats after injection of the same doses of monomycin.
[Mh] Termos MeSH primário: Antibacterianos/toxicidade
Etilsuccinato de Eritromicina/toxicidade
Perda Auditiva Neurossensorial/induzido quimicamente
Gânglio Espiral da Cóclea/ultraestrutura
[Mh] Termos MeSH secundário: Animais
Gatos
Potenciais Evocados Auditivos do Tronco Encefálico/efeitos dos fármacos
Seguimentos
Perda Auditiva Neurossensorial/patologia
Perda Auditiva Neurossensorial/fisiopatologia
Microscopia Eletrônica
Gânglio Espiral da Cóclea/efeitos dos fármacos
Gânglio Espiral da Cóclea/fisiopatologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 1014KSJ86F (Erythromycin Ethylsuccinate)
[Em] Mês de entrada:1002
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:091229
[St] Status:MEDLINE


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[PMID]:20209795
[Au] Autor:Stan CD; Stefanache A; Tântaru G; Poiata A; Dumitrache M; Diaconu DE; Profire L
[Ad] Endereço:Disciplina de Industria Medicamentului si Biotehnologii Farmaceutice, Facultatea de Farmacie, Universitatea de Medicina si Farmacie Gr.T. Popa Iasi.
[Ti] Título:[Erythromycin ethylsuccinate obtaining possibilities].
[Ti] Título:Posibilitati de obtinere a etil-succinatului de eritromicina..
[So] Source:Rev Med Chir Soc Med Nat Iasi;112(4):1104-9, 2008 Oct-Dec.
[Is] ISSN:0048-7848
[Cp] País de publicação:Romania
[La] Idioma:rum
[Ab] Resumo:UNLABELLED: In this study we tried to improve the erythromycin ethylsuccinate obtaining, having in view to separate the erythromycin ester by crystallization in water. MATERIAL AND METHODS: The erythromycin acylation and the erythromycin ethylsuccinate crystallization were realized, following the next steps: 1. the acylation of the erythromycin with a methylene chloride solution of monoethylsuccinyl chloride, at 25-28 degrees C for 3 hours in the presence of NaHCO3; 2. the transfer of the erythromycin ethylsuccinate from methylene chloride solution in acetone solution by distillation of mixture methylene chloride: acetone 1:1 at 25-28 degrees C; 3. erythromycin ethylsuccinate separation by crystallization in water at pH = 8-8.5 and 5 degrees C for 90 minutes. The quality control for the erythromycin ester was performed according to the Xth edition of Romanian Pharmacopoeia standards using national standard for erythromycin ethylsuccinate and national standard for erythromycin with an activity of 1: 937 U and 2.02% humidity. The Micrococcus luteus ATCC 9341 was used as a test microorganism and a thin layer cromatography was performed for qualitative control. RESULTS: 13.1 g of erythromycin ethylsuccinate were obtained with an output of the process of 82.02%. Using water for the separation of erythromycin ethylsuccinate the output of the process is greater (82.02%) than in case of using petroleum ether (74.14%) or hexane (80.25%). The thin layer cromatography revealed an Rf = 0.56 and the microbiological activity of the erythromycin ethylsuccinate was 98.7% compared with the standard. CONCLUSIONS: Using water instead of hexane or petroleum ether is gainful for the separation of erythromycin ethylsuccinate from the reaction medium. The obtained erythromycin ethylsuccinate corresponds to the Xth edition of Romanian Pharmacopoeia standards. So, the raw materials consumption is decreased, the costs are cut down, the obtained product purity is high and the output of the process is greater.
[Mh] Termos MeSH primário: Antibacterianos/síntese química
Antibacterianos/farmacologia
Etilsuccinato de Eritromicina/síntese química
Etilsuccinato de Eritromicina/farmacologia
Micrococcus luteus/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antibacterianos/economia
Cromatografia em Camada Delgada
Cristalização/economia
Etilsuccinato de Eritromicina/economia
Seres Humanos
Água
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 059QF0KO0R (Water); 1014KSJ86F (Erythromycin Ethylsuccinate)
[Em] Mês de entrada:1005
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100310
[St] Status:MEDLINE


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[PMID]:19000270
[Au] Autor:Albarellos GA; Kreil VE; Ambros LA; Waxman S; Montoya L; Tarragona L; Quaine PC; Hallu RE; Rebuelto M
[Ad] Endereço:Cátedra de Farmacología, Facultad de Ciencias Veterinarias, Universidad de Buenos Aires, Buenos Aires, Argentina. albarell@fvet.uba.ar
[Ti] Título:Pharmacokinetics of erythromycin after the administration of intravenous and various oral dosage forms to dogs.
[So] Source:J Vet Pharmacol Ther;31(6):496-500, 2008 Dec.
[Is] ISSN:1365-2885
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to describe and compare the pharmacokinetic properties of different formulations of erythromycin in dogs. Erythromycin was administered as lactobionate (10 mg/kg, IV), estolate tablets (25 mg/kg p.o.) and ethylsuccinate tablets or suspension (20 mg/kg p.o.). After intravenous (i.v.) administration, the principal pharmacokinetic parameters were (mean +/- SD): AUC((0-infinity)) 4.20 +/- 1.66 microg x h/mL; C(max) 6.64 +/- 1.38 microg/mL; V(z) 4.80 +/- 0.91 L/kg; Cl(t) 2.64 +/- 0.84 L/h.kg; t((1/2)lambda) 1.35 +/- 0.40 h and MRT 1.50 +/- 0.47 h. After the administration of estolate tablets and ethylsuccinate suspension, the principal pharmacokinetic parameters were (mean +/- SD): C(max), 0.30 +/- 0.17 and 0.17 +/- 0.09 microg/mL; t(max), 1.75 +/- 0.76 and 0.69 +/- 0.30 h; t((1/2)lambda), 2.92 +/- 0.79 and 1.53 +/- 1.28 h and MRT, 5.10 +/- 1.12 and 2.56 +/- 1.77 h, respectively. The administration of erythromycin ethylsuccinate tablets did not produce measurable serum concentrations. Only the i.v. administration rendered serum concentrations above MIC(90) = 0.5 microg/mL for 2 h. However, these results should be cautiously interpreted as tissue erythromycin concentrations have not been measured in this study and, it is recognized that they can reach much higher concentrations than in blood, correlating better with clinical efficacy.
[Mh] Termos MeSH primário: Antibacterianos/administração & dosagem
Antibacterianos/farmacocinética
Estolato de Eritromicina/administração & dosagem
Estolato de Eritromicina/farmacocinética
Etilsuccinato de Eritromicina/farmacocinética
[Mh] Termos MeSH secundário: Administração Oral
Animais
Antibacterianos/sangue
Área Sob a Curva
Estudos Cross-Over
Cães
Formas de Dosagem
Estolato de Eritromicina/sangue
Etilsuccinato de Eritromicina/administração & dosagem
Etilsuccinato de Eritromicina/sangue
Feminino
Meia-Vida
Injeções Intravenosas
Modelos Lineares
Masculino
Taxa de Depuração Metabólica
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Dosage Forms); 1014KSJ86F (Erythromycin Ethylsuccinate); XRJ2P631HP (Erythromycin Estolate)
[Em] Mês de entrada:0902
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:081113
[St] Status:MEDLINE
[do] DOI:10.1111/j.1365-2885.2008.00982.x


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[PMID]:18574125
[Au] Autor:Veraldi S; Lunardon L; Persico MC; Francia C; Bottini S
[Ad] Endereço:Institute of Dermatological Sciences, University of Milan, IRCCS Foundation, Ospedale Maggiore Policlinico, Mangiagalli e Regina Elena, Milan, Italy. stefano.veraldi@unimi.it
[Ti] Título:Multiple aphthoid syphilitic chancres of the oral cavity.
[So] Source:Int J STD AIDS;19(7):486-7, 2008 Jul.
[Is] ISSN:0956-4624
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We describe the case of a 31-year-old man who was affected by three asymptomatic, aphthoid, syphilitic chancres of the oral cavity. These lesions were accompanied by right latero-cervical and chin lymphadenopathy. The infection was previously diagnosed as aphthous stomatitis. The search for Treponema pallidum by means of darkfield microscope examination was positive. The patient was successfully treated with oral erythromycin ethylsuccinate. To our knowledge, this is the first case of multiple aphthoid syphilitic chancres of the oral cavity reported in the literature. We suggest that all patients with a recent history of painless ulcers in the oral cavity, accompanied by regional lymphadenopathy in which the clinical diagnosis has not been confirmed, should undergo a darkfield microscope examination.
[Mh] Termos MeSH primário: Cancro
Boca
Treponema pallidum/isolamento & purificação
[Mh] Termos MeSH secundário: Adulto
Antibacterianos/uso terapêutico
Cancro/diagnóstico
Cancro/tratamento farmacológico
Cancro/microbiologia
Cancro/patologia
Etilsuccinato de Eritromicina/uso terapêutico
Seres Humanos
Masculino
Boca/microbiologia
Boca/patologia
Úlceras Orais/diagnóstico
Úlceras Orais/microbiologia
Úlceras Orais/patologia
Estomatite Aftosa/diagnóstico
Estomatite Aftosa/microbiologia
Estomatite Aftosa/patologia
Treponema pallidum/efeitos dos fármacos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 1014KSJ86F (Erythromycin Ethylsuccinate)
[Em] Mês de entrada:0809
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM; X
[Da] Data de entrada para processamento:080625
[St] Status:MEDLINE
[do] DOI:10.1258/ijsa.2007.007262



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