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| Registros recuperados: 26 | |
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| FIGUEIREDO,CLAUDIA P.; FERREIRA,NATALIA C.; PASSOS,GISELLE F.; COSTA,ROBSON DA; NEVES,FERNANDA S.; MACHADO,CLARICE S.C.; MASCARELLO,ALESSANDRA; CHIARADIA-DELATORRE,LOUISE D.; NEUENFELDT,PATRÍCIA D.; NUNES,RICARDO J.; CORDEIRO,YRAIMA. |
| An altered form of the cellular prion protein, the PrPScor PrPRes, is implicated in the occurrence of the still untreatable transmissible spongiform encephalopathies. We have previously synthesized and characterized aromatic compounds that inhibit protease-resistant prion protein (PrPRes) accumulation in scrapie-infected cells. These compounds belong to different chemical classes, including acylhydrazones, chalcones and oxadiazoles. Some of the active compounds were non-toxic to neuroblastoma cells in culture and seem to possess drugable properties, since they are in agreement with the Lipinski´s rule of 5 and present desirable pharmacokinetic profiles as predicted in silico. Before the evaluation of the in vivo efficacy of the aromatic compounds in... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Prion; Acute toxicity; Organic compound; Drug safety; Scrapie; Pharmacokinetics. |
| Ano: 2015 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652015000301421 |
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| MAINARDES,RUBIANA M; PALMIRA D. GREMIÃO,MARIA. |
| The development and validation of a simple and accurate method based on HPLC with ultraviolet detection for the quantification of zidovudine in rat plasma and its application to a pharmacokinetic study following a single intranasal dose zidovudine is described. Zidovudine was extracted from the plasma using a single-step deproteinization. Chromatographic separation of zidovudine from interfering components was achieved with a C-18 reverse phase column, a mobile phase consisting of a mixture of sodium acetate buffer (55mM) with pH adjusted to 7.0 and acetonitrile (91:9 v/v) and UV detection set at 265 nm. The method was linear from 100 to 10000 ng.mL"¹ (r² > 0.9995), and zidovudine had a mean recovery from plasma of 92.8%. The coefficient of variation of... |
| Tipo: Journal article |
Palavras-chave: RP-HPLC; Validation; AZT; Pharmacokinetics; Intranasal delivery. |
| Ano: 2009 |
URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602009000300010 |
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| Olguín,Hugo Juárez; Portugal,Miriam Carrasco; Pérez,Janett Flores; Vieyra,Angélica Camacho; Pérez,Carmen Flores; Rodríguez,Alfonso Alfaro. |
| The study analyzed the effect of mannitol on the pharmacokinetics (PK) of amikacin. Adult Wistar rats were treated as follows: Group 1 (G1) received mannitol for three days, Group 2 (G2) received mannitol plus 10 mg/kg of amikacin simultaneously, and Group 3 only amikacin. The PK study was conducted on the 4th day. For which, blood samples were drawn at fixed times during 24 h and immunoenzymatically analyzed. Results revealed significant differences (p<0.05) between the groups, e.g. Cmax were 62.26 ± 15.75 µg/ml for G1, 72.63 ± 24.80 µg/ml for G2 and 68.61 ± 27.40 µg/ml for G3. The AUC also differed in the three groups, being largest for G2, 222.52 ± 47.30 µg/ml/h, and smallest for G1, 135.59 ± 39.00 µg/ml/h. Alteration of the PK parameters observed... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Pharmacokinetics; Interactions; Amikacin; Mannitol; Antibiotics; Diuretics. |
| Ano: 2009 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-89132009000400006 |
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| Patel,Satish D.; Sadariya,Kamlesh A.; Gothi,Anil K.; Patel,Urvesh D.; Gohil,Pradhuman A.; Jain,Mukul R.; Bhavsar,Shailesh K.; Thaker,Aswin M.. |
| Pharmacokinetics of tolfenamic acid as a single drug (4 mg/kg, intramuscularly) and its co-administration with moxifloxacin (5 mg/kg, intramuscularly) in wistar rats were studied. The plasma drug concentration of tolfenamic acid was assayed by LC-MS/MS. Following intramuscular administration of tolfenamic acid as single drug and in combination with moxifloxacin in male rats, the mean values of observed peak plasma drug concentration (Cmax), area under plasma drug concentration-time curve (AUC(0-¥) ), volume of distribution (Vz), half-life (t½) and clearance (Cl) were 4111.44 ± 493.15 and 3837.69 ± 351.83 ng/ml, 20280.77 ± 3501.67 and 15229.18 ± 678.80 ng.h/ml, 822.17 ± 115.38 and 1249.64 ± 139.52 ml, 2.59 ± 0.16 and 3.27 ± 0.32 hr, and 218.39 ± 25.47 and... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Pharmacokinetics; Tolfenamic acid; Anti inflammatory drug; Rats; Interaction; Moxifloxacin. |
| Ano: 2011 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-89132011000400013 |
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| Romanelli,Roberta Maia de Castro; Anchieta,Lêni Márcia; Fernandes,Juliana Chaves Abreu; Lima,Mariana Antunes Faria; Souza,Taís Marina de; Rosado,Viviane; Clemente,Wanessa Trindade; Camargos,Paulo Augusto Moreira. |
| Abstract Coagulase-negative Staphylococcus has been identified as the main nosocomial agent of neonatal late-onset sepsis. However, based on the pharmacokinetics and erratic distribution of vancomycin, recommended empirical dose is not ideal, due to the inappropriate serum levels that have been measured in neonates. The aim of this study was to evaluate serum levels of vancomycin used in newborns and compare the prediction of adequate serum levels based on doses calculated according to mg/kg/day and m2/day. This is an observational reprospective cohort at a referral neonatal unit, from 2011 to 2013. Newborns treated with vancomycin for the first episode of late-onset sepsis were included. Total dose in mg/kg/day, dose/m2/day, age, weight, body surface and... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Vancomycin; Drug dosage calculations; Pharmacokinetics; Infant; Newborn; Sepsis. |
| Ano: 2016 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1413-86702016000500451 |
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| Silva,Dáfne Cardoso Bourguignon da; Seixas,Gláucia Toribio Finoti; Araujo,Orlei Ribeiro de; Arduini,Rodrigo Genaro; Carlesse,Fabianne Altruda de Moraes Costa; Petrilli,Antonio Sergio. |
| BACKGROUND: Usual treatment regimens with vancomycin often fail to provide adequate serum levels in patients with severe infections. METHODS: Retrospective analysis of vancomycin trough serum measurements. The following parameters were calculated by Bayesian analysis: vancomycin clearance, distribution volume, and peak estimated concentrations. The area under the concentration curve (AUC) (total daily dose/24 h clearance of vancomycin) was used to determine the effectiveness of treatment through the ratio of AUC/minimum inhibitory concentration (MIC) above 400, using MIC = 1 µg/mL, based on isolates of Staphylococci in cultures. RESULTS: Sixty-one vancomycin trough measurements were analyzed in 31 patients. AUC/MIC > 400 was obtained in 34 out of 61... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Immunosuppression; Drug resistance; Microbial; Staphylococcus; Anti-bacterial agents; Pharmacokinetics. |
| Ano: 2012 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1413-86702012000400009 |
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| Brantley,Richard K.; Williams,K. Robert; Silva,Terezinha M.J.; Sistrom,Maria; Thielman,Nathan M.; Ward,Honorine; Lima,Aldo A. M.; Guerrant,Richard L.. |
| Advanced HIV infection is frequently complicated by diarrhea, disruption of bowel structure and function, and malnutrition. Resulting malabsorption of or pharmacokinetic changes in antiretroviral agents might lead to subtherapeutic drug dosing and treatment failure in individual patients, and could require dose adjustment and/or dietary supplements during periods of diarrheal illness. We determined the plasma levels of antiretroviral medications in patients that had already been started on medication by their physicians in an urban infectious diseases hospital in northeast Brazil. We also obtained blood samples from patients hospitalized for diarrhea or AIDS-associated wasting, and we found reduced stavudine and didanosine levels in comparison with... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: HIV; Malabsorption; DdI; D4T; Pharmacokinetics. |
| Ano: 2003 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1413-86702003000100003 |
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| Conte,F.P.; Fidalgo-Neto,A.A.; Manhães-Rocha,D.A.; Paumgartten,F.J.R.; De-Oliveira,A.C.A.X.. |
| The effects of schistosomiasis on microsomal enzymes were studied on post-infection day 90 when accumulated damage and fibrosis are most intense but granulomatous reaction around the eggs harbored in the liver is smaller than during the earlier phases. Swiss Webster (SW) and DBA/2 mice of either sex (N = 12 per sex per group) were infected with 100 Schistosoma mansoni cercariae on postnatal day 10 and killed on post-infection day 90. Cytochrome P-450 (CYP) concentration and alkoxyresorufin-O-dealkylases (EROD, MROD, BROD, and PROD), p-nitrophenol-hydroxylase (PNPH), coumarin-7-hydroxylase (COH), and UDP-glucuronosyltransferase (UGT) activities were measured in hepatic microsomes. Age-matched mice of the same sex and strain were used as controls. In S.... |
| Tipo: Info:eu-repo/semantics/other |
Palavras-chave: Schistosoma mansoni; Pharmacokinetics; Cytochrome P-450; Monooxygenases; Granuloma; Liver microsomes. |
| Ano: 2007 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2007000500008 |
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| Schettini,D.A.; Costa Val,A.P.; Souza,L.F.; Demicheli,C.; Rocha,O.G.F.; Melo,M.N.; Michalick,M.S.M.; Frézard,F.. |
| The aim of the present study was to evaluate the impact of a multiple dose regimen of a liposomal formulation of meglumine antimoniate (LMA) on the pharmacokinetics of antimony in the bone marrow of dogs with visceral leishmaniasis and on the ability of LMA to eliminate parasites from this tissue. Dogs naturally infected with Leishmania chagasi received 4 intravenous doses of either LMA (6.5 mg antimony/kg body weight, N = 9), or empty liposomes (at the same lipid dose as LMA, N = 9) at 4-day intervals. A third group of animals was untreated (N = 8). Before each administration and at different times after treatment, bone marrow was obtained and analyzed for antimony level (LMA group) by electrothermal atomic absorption spectrometry, and for the presence of... |
| Tipo: Info:eu-repo/semantics/other |
Palavras-chave: Liposome; Meglumine antimoniate; Pharmacokinetics; Leishmaniasis; Dogs; Bone marrow. |
| Ano: 2005 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2005001200017 |
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| Suarez-Kurtz,G.; Ribeiro,F.M.; Estrela,R.C.E.; Vicente,F.L.; Struchiner,C.J.. |
| Bioanalytical data from a bioequivalence study were used to develop limited-sampling strategy (LSS) models for estimating the area under the plasma concentration versus time curve (AUC) and the peak plasma concentration (Cmax) of 4-methylaminoantipyrine (MAA), an active metabolite of dipyrone. Twelve healthy adult male volunteers received single 600 mg oral doses of dipyrone in two formulations at a 7-day interval in a randomized, crossover protocol. Plasma concentrations of MAA (N = 336), measured by HPLC, were used to develop LSS models. Linear regression analysis and a "jack-knife" validation procedure revealed that the AUC0-<FONT FACE=Symbol>¥</FONT> and the Cmax of MAA can be accurately predicted (R²>0.95, bias <1.5%, precision... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Dipyrone; 4-methylaminoantipyrine; Limited-sampling models; Pharmacokinetics; Bioequivalence. |
| Ano: 2001 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2001001100017 |
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| Velasque,L.S.; Estrela,R.C.E.; Suarez-Kurtz,G.; Struchiner,C.J.. |
| Didanosine (ddI) is a component of highly active antiretroviral therapy drug combinations, used especially in resource-limited settings and in zidovudine-resistant patients. The population pharmacokinetics of ddI was evaluated in 48 healthy volunteers enrolled in two bioequivalence studies. These data, along with a set of co-variates, were the subject of a nonlinear mixed-effect modeling analysis using the NONMEM program. A two-compartment model with first order absorption (ADVAN3 TRANS3) was fitted to the serum ddI concentration data. Final pharmacokinetic parameters, expressed as functions of the co-variates gender and creatinine clearance (CL CR), were: oral clearance (CL = 55.1 + 240 x CL CR + 16.6 L/h for males and CL = 55.1 + 240 x CL CR for... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Didanosine; Pharmacokinetics; NONMEM. |
| Ano: 2007 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2007000100013 |
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| Carmona,M.J.C.; Malbouisson,L.M.S.; Pereira,V.A.; Bertoline,M.A.; Omosako,C.E.K.; Le Bihan,K.B.; Auler Jr.,J.O.C.; Santos,S.R.C.J.. |
| The pharmacokinetics of propranolol may be altered by hypothermic cardiopulmonary bypass (CPB), resulting in unpredictable postoperative hemodynamic responses to usual doses. The objective of the present study was to investigate the pharmacokinetics of propranolol in patients undergoing coronary artery bypass grafting (CABG) by CPB under moderate hypothermia. We evaluated 11 patients, 4 women and 7 men (mean age 57 ± 8 years, mean weight 75.4 ± 11.9 kg and mean body surface area 1.83 ± 0.19 m²), receiving propranolol before surgery (80-240 mg a day) and postoperatively (10 mg a day). Plasma propranolol levels were measured before and after CPB by high-performance liquid chromatography. Pharmacokinetic Solutions 2.0 software was used to estimate the... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Propranolol; Pharmacokinetics; Cardiopulmonary bypass. |
| Ano: 2005 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2005000500008 |
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| Andrade,E.L.; Bento,A.F.; Cavalli,J.; Oliveira,S.K.; Schwanke,R.C.; Siqueira,J.M.; Freitas,C.S.; Marcon,R.; Calixto,J.B.. |
| The process of drug development involves non-clinical and clinical studies. Non-clinical studies are conducted using different protocols including animal studies, which mostly follow the Good Laboratory Practice (GLP) regulations. During the early pre-clinical development process, also known as Go/No-Go decision, a drug candidate needs to pass through several steps, such as determination of drug availability (studies on pharmacokinetics), absorption, distribution, metabolism and elimination (ADME) and preliminary studies that aim to investigate the candidate safety including genotoxicity, mutagenicity, safety pharmacology and general toxicology. These preliminary studies generally do not need to comply with GLP regulations. These studies aim at... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Non-clinical studies; GLP studies; Safety; Pharmacokinetics; Toxicology. |
| Ano: 2016 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2016001200301 |
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| Park,S.I.; Felipe,C.R.; Machado,P.G.; Garcia,R.; Skerjanec,A.; Schmouder,R.; Tedesco-Silva Jr.,H.; Medina-Pestana,J.O.. |
| FTY720 is a new and effective immunosuppressive agent, which produces peripheral blood lymphopenia through a lymphocyte homing effect. We investigated the relationship between the dose of FTY720 or blood concentration (pharmacokinetics, PK) and peripheral lymphopenia (pharmacodynamics, PD) in 23 kidney transplant recipients randomized to receive FTY720 (0.25-2.5 mg/day) or mofetil mycophenolate (2 mg/day) in combination with cyclosporine and steroids. FTY720 dose, blood concentrations and lymphocyte counts were determined weekly before and 4 to 12 weeks after transplantation. The effect of PD was calculated as the absolute lymphocyte count or its reductions. PK/PD modeling was used to find the best-fit model. Mean FTY720 concentrations were 0.36 ± 0.05... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: FTY720; Lymphopenia; Pharmacokinetics; Pharmacodynamics; Immunosuppression; Renal transplants. |
| Ano: 2005 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2005000500005 |
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| Mansur,A.P.; Avakian,S.D.; Paula,R.S.; Donzella,H.; Santos,S.R.C.J.; Ramires,J.A.F.. |
| The bioavailability of propranolol depends on the degree of liver metabolism. Orally but not intravenously administered propranolol is heavily metabolized. In the present study we assessed the pharmacokinetics and pharmacodynamics of sublingual propranolol. Fourteen severely hypertensive patients (diastolic blood pressure (DBP) <FONT FACE="Symbol">³</font>115 mmHg), aged 40 to 66 years, were randomly chosen to receive a single dose of 40 mg propranolol hydrochloride by sublingual or peroral administration. Systolic (SBP) and diastolic (DBP) blood pressures, heart rate (HR) for pharmacodynamics and blood samples for noncompartmental pharmacokinetics were obtained at baseline and at 10, 20, 30, 60 and 120 min after the single dose. Significant... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Propranolol; Pharmacokinetics; Pharmacodynamics; Arterial hypertension; Sublingual vs peroral administration. |
| Ano: 1998 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X1998000500014 |
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| Nunan,E.A.; Arya,V.; Hochhaus,G.; Cardoso,V.N.; Moraes-Santos,T.. |
| The pharmacokinetics of scorpion venom and its toxins has been investigated in experimental models using adult animals, although, severe scorpion accidents are associated more frequently with children. We compared the effect of age on the pharmacokinetics of tityustoxin, one of the most active principles of Tityus serrulatus venom, in young male/female rats (21-22 days old, N = 5-8) and in adult male rats (150-160 days old, N = 5-8). Tityustoxin (6 µg) labeled with 99mTechnetium was administered subcutaneously to young and adult rats. The plasma concentration vs time data were subjected to non-compartmental pharmacokinetic analysis to obtain estimates of various pharmacokinetic parameters such as total body clearance (CL/F), distribution volume (Vd/F),... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Scorpion venom; Tityustoxin; Pharmacokinetics; Age; Bootstrapping resampling; Non-compartmental analysis. |
| Ano: 2004 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2004000300016 |
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| Registros recuperados: 26 | |
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