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[PMID]:26424818
[Au] Autor:Jensen ML; Bendstrup E; Hilberg O
[Ad] Endereço:Department of Pulmonary Medicine, Aarhus University Hospital, Aarhus, Denmark.
[Ti] Título:Granulomatous-lymphocytic interstitial lung disease and recurrent sinopulmonary infections in a patient with Good's syndrome.
[So] Source:BMJ Case Rep;2015, 2015 Sep 30.
[Is] ISSN:1757-790X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Good's syndrome is a rare primary immunodeficiency associated with adult thymoma. Complications are mainly autoimmune manifestations and recurrent infections with encapsulated bacteria. Only one possible case of combined granulomatous-lymphocytic interstitial lung disease (GL-ILD) and Good's syndrome have been described earlier, but the patient died at the time of diagnosis. This is the first case of GL-ILD in Good's syndrome with a successful outcome. We present a case of a 43-year-old man with GL-ILD, who suffered from recurrent infections of Haemophilus influenzae and Pneumocystis jirovecii, with 8-year follow-up. After a thymectomy, he was diagnosed with Good's syndrome and GL-ILD. He was treated with prophylactic pivampicillin, quinolones and cephalosporins for his recurrent P. jirovecii and H. influenzae infections, an approach that proved unsuccessful due to resistance, with relapse after cessation. He was stabilised with oral diaminodiphenyl-sulfone for P. jirovecii and colistimethate-sodium inhalations for H. influenzae, which is a new approach to prophylactic treatment.
[Mh] Termos MeSH primário: Granuloma/microbiologia
Infecções por Haemophilus/patologia
Doenças Pulmonares Intersticiais/microbiologia
[Mh] Termos MeSH secundário: Adulto
Agamaglobulinemia/patologia
Antibacterianos/uso terapêutico
Cefalosporinas/uso terapêutico
Granuloma/patologia
Infecções por Haemophilus/microbiologia
Haemophilus influenzae/isolamento & purificação
Seres Humanos
Síndromes de Imunodeficiência/microbiologia
Síndromes de Imunodeficiência/patologia
Doenças Pulmonares Intersticiais/tratamento farmacológico
Masculino
Neoplasias Epiteliais e Glandulares/patologia
Pivampicilina/uso terapêutico
Infecções por Pneumocystis/microbiologia
Infecções por Pneumocystis/patologia
Pneumocystis carinii/isolamento & purificação
Quinolonas/uso terapêutico
Doenças Raras
Timoma/patologia
Neoplasias do Timo/patologia
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Cephalosporins); 0 (Quinolones); 0HLM346LL7 (Pivampicillin)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:171001
[Lr] Data última revisão:
171001
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151002
[St] Status:MEDLINE


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[PMID]:21144541
[Au] Autor:Winther L; Baptiste KE; Friis C
[Ad] Endereço:Department of Large Animal Sciences, University of Copenhagen, 2630 Taastrup, Denmark. low@dkma.dk
[Ti] Título:Pharmacokinetics in pulmonary epithelial lining fluid and plasma of ampicillin and pivampicillin administered to horses.
[So] Source:Res Vet Sci;92(1):111-5, 2012 Feb.
[Is] ISSN:1532-2661
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Ampicillin concentrations in pulmonary epithelial lining fluid (PELF) and plasma was studied after single intravenous ampicillin administration (15mg/kg) or single intragastric administration of its prodrug, pivampicillin (19.9mg/kg) to horses and discussed in relation to minimum inhibitory concentrations (MIC) of common equine respiratory pathogens. After intravenous administration, elimination of ampicillin was fast and not detectable in plasma after 12h in three out of six horses. Pivampicillin was absorbed well in non-fasted horses with an oral bioavailability of 36%. The degree of penetration of ampicillin into PELF, as described by the AUC(PELF)/AUC(plasma) ratio from 0 to 12h was 0.40 after intravenous administration and 1.00 after pivampicillin administration. In horses, ampicillin administered either intravenously or orally, in the form of pivampicillin, can provide clinically relevant drug concentrations in PELF for at least 12h, when treating susceptible equine respiratory pathogens (e.g. streptococci). Treatment of other bacterial pathogens requires susceptibility testing and possibly more frequent dosing, depending of minimum inhibitory concentrations (MIC) values.
[Mh] Termos MeSH primário: Ampicilina/farmacocinética
Antibacterianos/farmacocinética
Cavalos/metabolismo
Pivampicilina/farmacocinética
[Mh] Termos MeSH secundário: Administração Oral
Ampicilina/administração & dosagem
Ampicilina/sangue
Animais
Antibacterianos/administração & dosagem
Antibacterianos/sangue
Disponibilidade Biológica
Líquido da Lavagem Broncoalveolar/química
Cromatografia Líquida de Alta Pressão/veterinária
Feminino
Cavalos/sangue
Injeções Intravenosas/veterinária
Pivampicilina/administração & dosagem
Pivampicilina/sangue
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0HLM346LL7 (Pivampicillin); 7C782967RD (Ampicillin)
[Em] Mês de entrada:1208
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:101215
[St] Status:MEDLINE
[do] DOI:10.1016/j.rvsc.2010.11.001


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[PMID]:19623605
[Au] Autor:Mizuma T
[Ad] Endereço:Department of Drug Absorption and Pharmacokinetics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, Tokyo, Japan. mizuma@ps.toyaku.ac.jp
[Ti] Título:Kinetic assessment of luminal degradation of orally effective prodrugs for rational drug development.
[So] Source:J Pharm Sci;99(2):1078-86, 2010 Feb.
[Is] ISSN:1520-6017
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Although prodrugging (prodrug derivatization) is a powerful technique for improving the pharmacokinetic characteristics of drugs, the intestinal pharmacokinetics of prodrugs has yet to be elucidated fully. A previous article reported the kinetic requirement of prodrugs to overcome membrane barriers. In the present article, the luminal degradation of prodrugs was kinetically assessed to understand crucial factors in the intestinal absorption of prodrugs and to show a rational development procedure. A kinetic model equation involving luminal degradation clearance (CL(deg)) was derived, and CL(deg) was estimated according to the equation with in vitro and in vivo reported data of two kinds of ampicillin prodrugs (lenampicillin and pivampicillin) and one acyclovir prodrug (valacyclovir). For lenampicillin ((2,2-dimethyl-1-oxopropoxy)methyl ester derivative), CL(deg) was approximately 1.7 times as large as absorption clearance (CL(abs)), whereas for pivampicillin ((5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester derivative), CL(deg) was approximately one tenth of CL(abs). For valacyclovir (acyclovir prodrug), CL(deg) was negligible. These results indicate that not only membrane permeability but also luminal stability should be assessed for the rational development of orally effective prodrugs, and that luminal stabilization can improve the intestinal absorption of prodrugs. A procedure was proposed to develop orally effective prodrugs considered for luminal degradation as well as membrane permeability.
[Mh] Termos MeSH primário: Desenho de Drogas
Absorção Intestinal
Pró-Fármacos/farmacocinética
[Mh] Termos MeSH secundário: Aciclovir/análogos & derivados
Aciclovir/farmacocinética
Administração Oral
Algoritmos
Ampicilina/análogos & derivados
Ampicilina/farmacocinética
Antibacterianos/farmacocinética
Antivirais/farmacocinética
Modelos Estatísticos
Permeabilidade
Pivampicilina/farmacocinética
Pró-Fármacos/administração & dosagem
Valina/análogos & derivados
Valina/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antiviral Agents); 0 (Prodrugs); 0HLM346LL7 (Pivampicillin); 7C782967RD (Ampicillin); 8M568DM08K (lenampicillin); HG18B9YRS7 (Valine); MZ1IW7Q79D (valacyclovir); X4HES1O11F (Acyclovir)
[Em] Mês de entrada:1003
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090723
[St] Status:MEDLINE
[do] DOI:10.1002/jps.21867


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[PMID]:19155372
[Au] Autor:Korbila IP; Manta KG; Siempos II; Dimopoulos G; Falagas ME
[Ad] Endereço:Alfa Institute of Biomedical Sciences in Athens, Greece.
[Ti] Título:Penicillins vs trimethoprim-based regimens for acute bacterial exacerbations of chronic bronchitis: meta-analysis of randomized controlled trials.
[So] Source:Can Fam Physician;55(1):60-7, 2009 Jan.
[Is] ISSN:1715-5258
[Cp] País de publicação:Canada
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To compare the effectiveness and toxicity of semisynthetic penicillins (SSPs) (amoxicillin, ampicillin, pivampicillin) and trimethoprim-based regimens (trimethoprim, trimethoprim-sulfamethoxazole, trimethoprim-sulfadiazine) in treating acute bacterial exacerbations of chronic bronchitis (ABECB). DATA SOURCES: We searched MEDLINE, EMBASE, Current Contents, and the Cochrane Central Register of Controlled Trials to identify and extract data from relevant randomized controlled trials (RCTs). STUDY SELECTION: Only RCTs comparing penicillins with trimethoprim-based regimens for the treatment of patients with ABECB that reported data on effectiveness, toxicity, or mortality were considered eligible for this meta-analysis. SYNTHESIS: Out of 134 RCTs identified in the search, 5 RCTs involving 287 patients were included in the analysis. There were no differences between patients with ABECB treated with SSPs and those treated with trimethoprim, alone or in combination with a sulfonamide, in treatment success (intention-to-treat patients: n = 262, odds ratio [OR] 1.68, 95% confidence interval [CI] 0.91-3.09; clinically evaluable patients: n = 246, OR 1.59, 95% CI 0.79-3.20) or number of drug-related adverse events in general (n = 186 patients, OR 0.37, 95% CI 0.11-1.24), frequency of diarrhea or skin rashes, or number of withdrawals due to adverse events (n = 179 patients, OR 0.27, 95% CI 0.07-1.03). CONCLUSION: Based on limited evidence leading to wide CIs of the estimated treatment effects, SSPs and trimethoprim-based regimens seem to be equivalent in terms of effectiveness and toxicity for ABECB.
[Mh] Termos MeSH primário: Amoxicilina/uso terapêutico
Anti-Infecciosos/uso terapêutico
Bronquite Crônica/tratamento farmacológico
Pivampicilina/uso terapêutico
Combinação Trimetoprima e Sulfametoxazol/uso terapêutico
[Mh] Termos MeSH secundário: Doença Aguda
Quimioterapia Combinada
Seres Humanos
Guias de Prática Clínica como Assunto
Ensaios Clínicos Controlados Aleatórios como Assunto
Resultado do Tratamento
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0HLM346LL7 (Pivampicillin); 804826J2HU (Amoxicillin); 8064-90-2 (Trimethoprim, Sulfamethoxazole Drug Combination)
[Em] Mês de entrada:0904
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090122
[St] Status:MEDLINE


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[PMID]:17603179
[Au] Autor:Oda M; Fujimoto K; Kobayashi M; Saitoh H
[Ad] Endereço:Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Hokkaido, Japan.
[Ti] Título:Bacampicillin uptake is shared with thiamine in Caco-2 cells.
[So] Source:Biol Pharm Bull;30(7):1344-9, 2007 Jul.
[Is] ISSN:0918-6158
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Bacampicillin was developed as a prodrug to improve the intestinal absorption of its metabolite ampicillin. This study was undertaken to characterize bacampicillin transport in Caco-2 cells. The uptake of bacampicillin in Caco-2 cells was significantly greater than those of ampicillin and pivampicillin. An Eadie-Hofstee plot obtained from 5-min uptake of 0.2-5 mM bacampicillin was linear, indicating the presence of a saturable transport system for bacampicillin with K(m) and V(max) of 3.6 mM and 23.9 nmol/mg protein/min, respectively. Hydrophilic organic cations such as choline, cimetidine, guanidine, nicotinamide, 1-methylnicotiamide, and tetraethylammonium failed to modulate bacampicillin uptake in Caco-2 cells whereas diphenhydramine, procainamide, and thiamine significantly depressed it. Moreover, when thiamine was preloaded in Caco-2 cells, bacampicillin uptake was significantly increased, indicating that this cationic vitamin was capable of trans-stimulating bacampicillin transport across the apical membrane of Caco-2 cells. However, trans-stimulated bacampicillin uptake was not observed in the presence of diphenhydramine. Bacampicillin uptake increased with elevation of the medium pH, and the known modulators of thiamine transport such as amiloride and oxythiamine significantly inhibited bacampicillin uptake. Thiamine also significantly decreased the apical-to-basolateral transport of bacampicillin across Caco-2 cell monolayers. However, thiamine did not exert any modulating effect on pivampicillin uptake and its apical-to-basolateral permeation in Caco-2 cells. These results suggest that bacampicillin is transported in Caco-2 cells, sharing a carrier-mediated system with thiamine.
[Mh] Termos MeSH primário: Ampicilina/análogos & derivados
Antibacterianos/farmacocinética
Tiamina/metabolismo
[Mh] Termos MeSH secundário: Ampicilina/farmacocinética
Transporte Biológico/efeitos dos fármacos
Células CACO-2
Difenidramina/farmacologia
Seres Humanos
Concentração de Íons de Hidrogênio
Proteínas de Membrana Transportadoras/fisiologia
Transportador 1 de Peptídeos
Pivampicilina/farmacocinética
Simportadores/fisiologia
Tiamina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Membrane Transport Proteins); 0 (Peptide Transporter 1); 0 (SLC15A1 protein, human); 0 (SLC19A2 protein, human); 0 (Symporters); 0HLM346LL7 (Pivampicillin); 7C782967RD (Ampicillin); 8GM2J22278 (bacampicillin); 8GTS82S83M (Diphenhydramine); X66NSO3N35 (Thiamine)
[Em] Mês de entrada:0708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070703
[St] Status:MEDLINE


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[PMID]:15793098
[Au] Autor:Chanteux H; Van Bambeke F; Mingeot-Leclercq MP; Tulkens PM
[Ad] Endereço:Unité de pharmacologie cellulaire et moléculaire, Université catholique de Louvain 73-70, Avenue E. Mounier, 73, B-1200 Brussels, Belgium.
[Ti] Título:Accumulation and oriented transport of ampicillin in Caco-2 cells from its pivaloyloxymethylester prodrug, pivampicillin.
[So] Source:Antimicrob Agents Chemother;49(4):1279-88, 2005 Apr.
[Is] ISSN:0066-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Pivampicillin (PIVA), an acyloxymethylester of ampicillin, is thought to enhance the oral bioavailability of ampicillin because of its greater lipophilicity compared to that of ampicillin. The fate of PIVA in intestinal cells and the exact location of its conversion into ampicillin have, however, never been unambiguously established. Polarized Caco-2 cells have been used to examine the handling of PIVA and the release of ampicillin from PIVA by the intestinal epithelium. Experiments were limited to 3 h. Cells incubated with PIVA (apical pole) showed a fast accumulation of ampicillin and transport toward the basolateral medium, whereas PIVA itself was only poorly accumulated and transported. Cells incubated with free ampicillin accumulated and transported only minimal amounts of this drug. Release of ampicillin from cells incubated with PIVA was unaffected by PEPT1 and OCTN2 inhibitors but was sharply decreased after ATP depletion or addition of bis(4-nitrophenyl)-phosphate (BNPP; an esterase inhibitor). PIVA incubated with Caco-2 lysates released free ampicillin, and this release was inhibited by BNPP. Efflux studies showed that the ampicillin that accumulated in cells after incubation with PIVA was preferentially transported out of the cells through the basolateral pole. This efflux was decreased by multidrug resistance-associated protein (MRP) inhibitors (probenecid, MK-571) and by ATP depletion. A phthalimidomethylester of ampicillin that resists cellular esterases failed to cause any significant release (cell lysate) or transport (polarized Caco-2 cells) of ampicillin. These results show that when PIVA is given to Caco-2 cells from their apical pole, ampicillin is released intracellularly and that ampicillin is thereafter preferentially effluxed into the basolateral medium through an MRP-like transporter.
[Mh] Termos MeSH primário: Ampicilina/farmacocinética
Antibacterianos/farmacocinética
Polaridade Celular
Colo/metabolismo
Pivampicilina/farmacocinética
Pró-Fármacos/farmacocinética
[Mh] Termos MeSH secundário: Transporte Biológico
Células CACO-2
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Prodrugs); 0HLM346LL7 (Pivampicillin); 7C782967RD (Ampicillin)
[Em] Mês de entrada:0505
[Cu] Atualização por classe:140608
[Lr] Data última revisão:
140608
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:050329
[St] Status:MEDLINE


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[PMID]:12972457
[Au] Autor:Chanteux H; Mingeot-Leclercq MP; Sonveaux E; Van Bambeke F; Tulkens PM
[Ad] Endereço:Unité de Pharmacologie Cellulaire et Moléculaire, UCL 73-70, avenue E Mounier 73, B-1200 Brussels, Belgium. hugues.chanteux@facm.ucl.ac.be
[Ti] Título:Intracellular accumulation and activity of ampicillin used as free drug and as its phthalimidomethyl or pivaloyloxymethyl ester (pivampicillin) against Listeria monocytogenes in J774 macrophages.
[So] Source:J Antimicrob Chemother;52(4):610-5, 2003 Oct.
[Is] ISSN:0305-7453
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AIMS: To determine the intracellular accumulation in a macrophage cell line of ampicillin and ampicillin esters, and to measure their activity against intracellular Listeria monocytogenes. METHODS: Quantitative evaluation of the activity of ampicillin, phthalimidomethylampicillin (PIMA) or pivaloyloxymethylampicillin (PIVA) against intracellular L. monocytogenes, and direct measurement of cellular ampicillin concentration in J774 macrophages. RESULTS: Ampicillin, PIMA and PIVA caused a 0.5 log decrease in cell-associated cfu within 5 h when used at an extracellular concentration of 3.6 microM [10 x MIC of ampicillin (1.25 mg/L); 1.83 mg/L for PIMA and 1.67 mg/L for PIVA]. Addition of beta-lactamase in the extracellular milieu abolished the activity of ampicillin and of PIMA but not that of PIVA. At low extracellular concentrations [0.5 x MIC ampicillin (62.5 microg/L); equimolar concentrations for PIMA (91.5 microg/L) and PIVA (83.5 microg/L)], ampicillin and PIMA lost all activity (compared with controls), but PIVA remained as active as at the higher concentration. Incubation of cells with PIVA at the low concentration (83.5 microg/L) for 20 h caused a 2 log reduction of cfu if the medium was changed every 5 h (to compensate for the degradation of extracellular PIVA). Incubation of cells with PIVA allowed for a marked (four- to 25-fold) cell accumulation of ampicillin, whereas no ampicillin accumulation was seen for cells incubated with ampicillin or with PIMA. CONCLUSIONS: This is the first demonstration that PIVA (a prodrug of ampicillin) can be used to promote ampicillin cellular accumulation and, thereby to increase ampicillin intracellular activity. PIVA could be useful for control of the intracellular multiplication of L. monocytogenes.
[Mh] Termos MeSH primário: Ampicilina/metabolismo
Líquido Intracelular/metabolismo
Listeria monocytogenes/metabolismo
Macrófagos/metabolismo
Ftalimidas/metabolismo
Pivampicilina/metabolismo
[Mh] Termos MeSH secundário: Ampicilina/análogos & derivados
Ampicilina/farmacologia
Animais
Linhagem Celular Tumoral
Líquido Intracelular/efeitos dos fármacos
Listeria monocytogenes/efeitos dos fármacos
Macrófagos/efeitos dos fármacos
Camundongos
Ftalimidas/farmacologia
Pivampicilina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Phthalimides); 0 (phthalimidomethylampicillin); 0HLM346LL7 (Pivampicillin); 7C782967RD (Ampicillin)
[Em] Mês de entrada:0407
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:030916
[St] Status:MEDLINE


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[PMID]:12739771
[Au] Autor:Chanteux H; Paternotte I; Mingeot-Leclercq MP; Brasseur R; Sonveaux E; Tulkens PM
[Ad] Endereço:Unité de pharmacologie cellulaire et moléculaire, Université Catholique de Louvain, 73-70, avenue E. Mounier, 73, B-1200 Brussels, Belgium. hugues.chanteux@facm.ucl.ac.be
[Ti] Título:Cell handling, membrane-binding properties, and membrane-penetration modeling approaches of pivampicillin and phthalimidomethylampicillin, two basic esters of ampicillin, in comparison with chloroquine and azithromycin.
[So] Source:Pharm Res;20(4):624-31, 2003 Apr.
[Is] ISSN:0724-8741
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: The purpose of this work was to examine and understand the cellular pharmacokinetics of two basic esters of ampicillin, pivaloyloxymethyl (PIVA) and phthalimidomethyl (PIMA), in comparison with lysosomotropic drugs (chloroquine, azithromycin). METHODS: Cell culture studies (J774 macrophages) were undertaken to study uptake and release kinetics and to assess the influence of concentration, pH, proton ionophore (monensin), and MRP and P-gp inhibitors (probenecid, gemfibrozil, cyclosporin A, GF 120918). Equilibrium dialysis with liposomes were performed to directly asses the extent of drug binding to bilayers. Conformational analysis modeling of the drug penetration in bilayers was conducted to rationalize the experimental observations. RESULTS: PIVA and PIMA showed properties in almost complete contrast with those of chloroquine and azithromycin, i.e., fast apparent accumulation and fast release at 4 degrees C as well as at 37 degrees C, saturation of uptake (apparent Kd 40 microM), no influence of monensin, MRP, or P-gp inhibitors; tight binding to liposomes (Kd approx. 40 microM); and sharp increase in calculated free energy when forced in the hydrophobic domain. CONCLUSIONS: Although they are weak organic bases, PIVA and PIMA show none of the properties of lysosomotropic agents. We hypothesize that they remain locked onto the pericellular membrane and may never penetrate cells as such in significant amounts.
[Mh] Termos MeSH primário: Ampicilina/análogos & derivados
Ampicilina/farmacocinética
Azitromicina/farmacocinética
Membrana Celular/efeitos dos fármacos
Membrana Celular/metabolismo
Cloroquina/farmacocinética
Ftalimidas/farmacocinética
Pivampicilina/farmacocinética
[Mh] Termos MeSH secundário: Técnicas de Cultura de Células
Lisossomos/efeitos dos fármacos
Lisossomos/metabolismo
Macrófagos/efeitos dos fármacos
Macrófagos/metabolismo
Modelos Biológicos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Phthalimides); 0 (phthalimidomethylampicillin); 0HLM346LL7 (Pivampicillin); 7C782967RD (Ampicillin); 83905-01-5 (Azithromycin); 886U3H6UFF (Chloroquine)
[Em] Mês de entrada:0401
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:030513
[St] Status:MEDLINE


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[PMID]:10983860
[Au] Autor:Schouenborg P; Gerdes N; Rasmussen H; Wickers-Nielsen N; Mathiassen E
[Ad] Endereço:Department of Microbiology, Vejle Hospital, Denmark.
[Ti] Título:Azithromycin versus pivampicillin in the treatment of acute exacerbations of chronic bronchitis: a single-blind, double-dummy, multicentre study.
[So] Source:J Int Med Res;28(3):101-10, 2000 May-Jun.
[Is] ISSN:0300-0605
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This single-blind, double-dummy, multicentre study compared oral azithromycin, administered as tablets, 500 mg once daily for 3 days, versus oral pivampicillin, 700 mg twice daily for 10 days, in adults with acute exacerbations of chronic bronchitis (not needing parenteral antibiotic therapy, hospitalization or oxygen support). Clinical success (cure + improvement) rates were similar for both groups at the end of treatment (day 10; azithromycin, 124 of 133 [93%]; pivampicillin, 79 of 92 [86%]) and at follow-up (day 52; 98 of 126 [78%] versus 66 of 81 [81%]). The treatments produced similar levels of pathogen eradication at the end of treatment (49 of 54 [91%] versus 32 of 37 [86%]). Azithromycin-treated patients had significantly reduced chest discomfort at the end of treatment, and a trend towards improved lung function. The two groups were similar with respect to improvements in other clinical symptoms and patient well-being, and to the incidences of adverse events and treatment discontinuations. This oral azithromycin regime is an effective treatment for acute exacerbations of chronic bronchitis, similar in efficacy to the longer pivampicillin regime and may offer superior patient compliance.
[Mh] Termos MeSH primário: Antibacterianos/uso terapêutico
Azitromicina/uso terapêutico
Bronquite/tratamento farmacológico
Penicilinas/uso terapêutico
Pivampicilina/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Antibacterianos/administração & dosagem
Antibacterianos/efeitos adversos
Azitromicina/administração & dosagem
Azitromicina/efeitos adversos
Bronquite/microbiologia
Bronquite/fisiopatologia
Doença Crônica
Segurança de Produtos ao Consumidor
Tolerância a Medicamentos
Feminino
Seres Humanos
Masculino
Penicilinas/administração & dosagem
Penicilinas/efeitos adversos
Pivampicilina/administração & dosagem
Pivampicilina/efeitos adversos
Método Simples-Cego
Resultado do Tratamento
[Pt] Tipo de publicação:CLINICAL TRIAL; COMPARATIVE STUDY; JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Penicillins); 0HLM346LL7 (Pivampicillin); 83905-01-5 (Azithromycin)
[Em] Mês de entrada:0102
[Cu] Atualização por classe:170214
[Lr] Data última revisão:
170214
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:000913
[St] Status:MEDLINE


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[PMID]:10830765
[Au] Autor:Larsen H; Nielsen GL; Sørensen HT; Møller M; Olsen J; Schønheyder HC
[Ad] Endereço:Department of Gynaecology and Obstetrics, Aalborg Hospital, Denmark.
[Ti] Título:A follow-up study of birth outcome in users of pivampicillin during pregnancy.
[So] Source:Acta Obstet Gynecol Scand;79(5):379-83, 2000 May.
[Is] ISSN:0001-6349
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Pivampicillin is a prodrug which is widely used in Scandinavian countries for oral antibiotic therapy. The pivaloyl moiety has a carnitine depleting effect, which has caused doubts about the safety of administering pivampicillin during pregnancy. The aim of the study was to evaluate the risk of congenital malformations in general, preterm delivery and low birth weight in users of pivampicillin. METHODS: Seven hundred and ninety-one women who had redeemed a prescription of pivampicillin during their first pregnancy from 1 January 1991 to 31 December 1996 were identified in the North Jutland Pharmaco-Epidemiological Prescription Database. By linkage to the Danish Medical Birth Registry and Regional Hospital Discharge Registry we compared their birth outcomes (malformations, preterm delivery and low birth weight) with the outcomes in 7472 reference pregnancies on which the mother had not redeemed any prescription at all during pregnancy. RESULTS: The prevalence of malformations was 5.5% (11 cases) in offspring of 199 women who had used pivampicillin during the first trimester, and 5.6% (420 cases) in offspring of controls (OR: 0.95, 95% CI: 0.51-1.76). Furthermore, we did not find any significant risk of preterm delivery (OR: 0.75, 95% CI: 0.54-1.05) or low birth weight (OR: 0.93, 95% CI: 0.55-1.57). CONCLUSION: This study showed no increased risk of congenital malformations, preterm delivery or low birth weight in offspring of women who had redeemed a prescription for pivampicillin during pregnancy.
[Mh] Termos MeSH primário: Anormalidades Induzidas por Medicamentos/epidemiologia
Penicilinas/efeitos adversos
Pivampicilina/efeitos adversos
Resultado da Gravidez
Pró-Fármacos/efeitos adversos
[Mh] Termos MeSH secundário: Adolescente
Adulto
Dinamarca/epidemiologia
Feminino
Seguimentos
Seres Humanos
Recém-Nascido de Baixo Peso
Recém-Nascido
Recém-Nascido Prematuro
Modelos Lineares
Análise Multivariada
Trabalho de Parto Prematuro/induzido quimicamente
Penicilinas/uso terapêutico
Pivampicilina/uso terapêutico
Gravidez
Prevalência
Pró-Fármacos/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Penicillins); 0 (Prodrugs); 0HLM346LL7 (Pivampicillin)
[Em] Mês de entrada:0006
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:000601
[St] Status:MEDLINE



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