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Influência do nifedipino na disposição cinética dos enantiômeros da venlafaxina e seus metabólitos em voluntários sadios; Influence of nifedipine on the kinetic disposition of venlafaxine enantiomers and its metabolites in healthy volunteers

Tozatto, Eduardo
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Tese de Doutorado Formato: application/pdf
Publicado em 01/06/2012 PT
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37.25%
A venlafaxina é um fármaco usado no tratamento da depressão e dos transtornos de ansiedade generalizada. É disponível na clínica na forma de mistura racêmica dos enantiômeros S-(+) e R-(-) em formulação de liberação controlada. O enantiômero S-(+) inibe a recaptação da serotonina, enquanto o enantiômero R-(-) inibe a recaptação da serotonina e da norepinefrina. A venlafaxina é biotransformada pelo CYP2D6 e CYP2C19 em seu principal metabólito, O-desmetilvenlafaxina, o qual apresenta atividade farmacológica semelhante à venlafaxina. Outros metabólitos da venlafaxina, dependentes do CYP3A4, incluem a N-desmetilvenlafaxina e a N,O-di-desmetilvenlafaxina. A absorção e a distribuição da venlafaxina são moduladas pela ação da glicoproteina-P. O nifedipino, um fármaco da classe dos inibidores dos canais de cálcio, é descrito como inibidor da glicoproteina-P. O presente estudo investiga a influência do nifedipino na disposição cinética e no metabolismo da venlafaxina em voluntários sadios caracterizados como portadores de atividade normal do CYP3A (omeprazol como fármaco marcador) e fenotipados como metabolizadores rápidos do CYP2C19 (omeprazol como fármaco marcador) e do CYP2D6 (metoprolol como fármaco marcador). Os voluntários investigados receberam...

Influência do diabetes mellitus tipo 2 na farmacocinética da nifedipina em gestantes hipertensas; Influence of type 2 diabetes mellitus on pharmacokinetics of nifedipine in hypertensive pregnant women

Filgueira, Gabriela Campos de Oliveira
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 18/11/2014 PT
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37.38%
A nifedipina é uma dihidropiridina, antagonista de canal de cálcio utilizada no tratamento hipertensão arterial na gravidez. O presente estudo visa avaliar a influência do DM2 na farmacocinética da nifedipina em gestantes hipertensas. Foram avaliadas 12 gestantes hipertensas (grupo controle) e 10 gestantes hipertensas portadoras de DM 2 controlado (grupo DM), em uso de nifedipina retard (20 mg, 12/12 horas). A partir da 34ª semana de gestação foram coletadas amostras seriadas de sangue para a análise farmacocinética nos tempos zero, 10, 20, 30, 60, 90, 120, 150, 180, 240, 300, 360, 420, 480, 540, 600, 660 e 720 minutos após a administração do medicamento. Na resolução da gravidez coletou-se sangue materno e fetal para determinar a taxa de transferência placentária da nifedipina. Foram coletadas também alíquotas de sangue do espaço interviloso e de líquido amniótico para a determinação da distribuição do fármaco nestes compartimentos. As concentrações de nifedipina em plasma e líquido amniótico foram analisadas por LC-MS/MS. Os parâmetros farmacocinéticos e de transferência placentária da nifedipina, reportados como mediana foram comparados usando o teste Mann-Whitney, com nível de significância fixado em p<0...

Effects of cyclosporin, phenytoin, and nifedipine on the synthesis and degradation of gingival collagen in tufted capuchin monkeys (Cebus apella): Histochemical and MMP-1 and -2 and collagen I gene expression analyses

Kanno, Claudia M.; Oliveira, Jose A.; Garcia, José Fernando; Castro, Alvimar L.; Crivelini, Marcelo M.
Fonte: Amer Acad Periodontology Publicador: Amer Acad Periodontology
Tipo: Artigo de Revista Científica Formato: 114-122
ENG
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Background: The purpose of this experimental study was to evaluate the collagen fiber distribution histologically after phenytoin, cyclosporin, or nifedipine therapy and to correlate it with collagen I and matrix metalloproteinase (MMP)-1 and -2 gene expression levels.Methods: Gingival samples from the canine area were obtained from 12 male monkeys (Cebus apella). The mesial part of each sample was assessed by reverse transcription-polymerase chain reaction, whereas the distal part was processed histologically for picrosirius red and hematoxylin and eosin stainings, as well as for collagen IV immunostaining. One week after the first biopsy, the animals were assigned to three groups that received daily oral dosages of cyclosporin, phenytoin, or nifedipine for 120 days. Additional gingival samples were obtained on days 52 and 120 of treatment from two animals from each group on the opposite sides from the first biopsies.Results: Picrosirius red staining showed a predominance of mature collagen fibers in the control group. Conversely, there was an enlargement of areas occupied by immature collagen fibers in all groups at days 52 and 120, which was not uniform over each section. There was a general trend to lower levels of MMP-1 gene expression on day 52 and increased levels on day 120. Phenytoin led to increased levels of MMP-2 and collagen I gene expression on day 120...

Morphological evaluation of combined effects of cyclosporin and nifedipine on gingival overgrowth in rats

Spolidorio, L. C.; Spolidorio, D. M.; Neves, K. A.; Gonzaga, H. F. S.; Almeida, O. P.
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 192-195
ENG
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It has previously been shown that, while cyclosporin A (CsA) and nifedipine both cause gingival overgrowth in the rat. the combined use of these drugs increases the severity of overgrowth. The aim of this study was to describe the histometry and densities of fibroblasts, collagen fibers and vessels in the gingival tissue of rats that were treated with CsA and nifedipine, either alone or in combination. Rats were treated for 60 days with a daily subcutaneous injection of 10 mg/kg body weight of CsA and/or with 50 mg/kg body weight of nifedipine added to the chow. The results confirmed that CsA causes a more severe overgrowth than nifedipine, and that the combined use of these drugs increases the overgrowth severity. All the rat groups that were studied showed that, as the severity of overgrowth increased, there was a parallel increase in fibroblasts and collagen, and a decrease in vessel content. Therefore, independently of whether the gingival overgrowth was caused by CsA alone, nifedipine alone, or both treatments in combination, the fibroblast and collagen density increased in parallel with the severity of the overgrowth. © Blackwell Munksgaard, 2002.

Combined effects of cyclosporin and nifedipine on gingival overgrowth in rats is not age dependent

Spolidorio, L. C.; Spolidorio, D. M.; Benatti, C.; Sampaio, J. E.; Almeida, O. P.
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 375-379
ENG
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Background: Cyclosporin A and nifedipine cause gingival overgrowth in rat, and the combined use of these drugs increases the overgrowth severity. Objective: The purpose of this study was to compare gingival overgrowth of rats of differents ages treated with cyclosporin A and nifedipine alone or given concurrently. Materials and methods: Rats 15, 30, 60 and 90 d old were treated with 10 mg/kg body weight of cyclosporin A and/or 50 mg/kg body weight of nifedipine in the chow. Results: Young rats showed evident gingival overgrowth with nifedipine, cyclosporin A, and cyclosporin A and nifedipine given concurrently. Adult rats did not show significant gingival alterations when treated with cyclosporin A and nifedipine alone. Nevertheless evident gingival overgrowth with alterations of the epithelium and connective tissue were observed when treated simultaneously with cyclosporin A and nifedipine. Conclusion: These results suggest that the combined effects of cyclosporin A and nifedipine on gingival overgrowth in rat is not age dependent.

Central nifedipine-induced alterations in salivary flow and compounds: Role of nitric oxide

Saad, Wilson Abrão; Guarda, Ismael Francisco Motta Siqueira; Camargo, Luiz Antonio de Arruda; Santos, Talmir Augusto Faria Brizola dos; Simões, Sylvio; Saad, William Abrão
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 596-603
ENG
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The aim of this study was to examine the role of nifedipine and Nitric Oxide (NO) on salivary flow and compounds (salivary amylase, saliva total proteins, saliva calcium, sodium and potassium). Male Holtzman rats weighting 200-250 g were anesthetized with zoletil 50 mg kg -1 (tiletamine chloridrate 125.0 mg and zolazepan chloridrate 125.0 mg) into quadriceps muscle and stainless steel cannulas were implanted into their lateral ventricle of the brain (LV). Animals in divided group were injected with nifedipine (50 μg μL -1) alone and in combination with 7-nitroindazol (7-NIT) (40 μg μL -1), neuronal NO Sinthase Inhibitor (nNOSI) and Sodium Nitroprussate (SNP) (30 μg μL -1) NO donor agent. As a secretory stimuli, pilocarpine dissolved in isotonic was administered intraperitoneally (ip) at a dosage of 10 mg kg -1 body weight. Saliva was collected for 7 min with four cotton balls weighing approximately 20 mg each, two of which were placed on either side of the oral cavity, with the other two placed under the tongue. Nifedipine treatment induced a reduction in saliva secretion rate and concentration of amylase, total protein and calcium without changes in sodium and potassium concentration in comparison with controls. Co-treatment of animals with nifedipine and SNP retained flow rate and concentration of amylase...

Anticonvulsant and antiarrhythmic effects of nifedipine in rats prone to audiogenic seizures

Damasceno,D.D.; Ferreira,A.J.; Doretto,M.C.; Almeida,A.P.
Fonte: Associação Brasileira de Divulgação Científica Publicador: Associação Brasileira de Divulgação Científica
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/11/2012 EN
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Calcium ion participates in the regulation of neural transmission and the presynaptic release of neurotransmitters. It is also involved in epileptic events, cardiac arrhythmias and abnormal conduction of stimuli. The purpose of the present study was to evaluate the effects of nifedipine, a calcium channel blocker, on epileptic seizures and on reperfusion arrhythmias in rats prone to audiogenic epileptic seizures (Wistar audiogenic rats, WAR) and in normal Wistar rats (N = 6/group). The seizure severity index was applied after an intraperitoneal injection of 20 or 40 mg/kg nifedipine (N20 and N40 groups, respectively). The Langendorff technique was used to analyze cardiac function, as well as the incidence and severity of the reperfusion arrhythmias after ligature and release of the left coronary artery in rats treated or not with nifedipine. We found that nifedipine treatment decreased seizure severity (0.94 ± 0.02 for WAR; 0.70 ± 0.10 for WAR + N20; 0.47 ± 0.08 for WAR + N40) and increased the latent period (13 ± 2 s for WAR; 35 ± 10 s for WAR + N20; 48 ± 7 s for WAR + N40) for the development of seizures in WAR. Furthermore, the incidence and severity of the reperfusion arrhythmias were lower in WAR and normal Wistar rats injected with nifedipine. In WAR...

Nifedipine-induced histological changes in the parotid glands of hypertensive rats

Seferos,Nikos; Daskala,Ioanna; Kotsiou,Antonia; Tsamouri,Madeleine; Tesseromatis,Christine
Fonte: Sociedade Brasileira de Pesquisa Odontológica - SBPqO Publicador: Sociedade Brasileira de Pesquisa Odontológica - SBPqO
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2014 EN
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Nifedipine is a widely used anti-anginal and anti-hypertensive agent. It is associated with significant gingival changes attributed more to collagen hyperplasia than to enhancement of protein synthesis. We investigated the influence of nifedipine on morphological changes in the parotid glands of rats in a model of hypertension. Twenty-eight male Wistar rats (8–10 weeks; 200 ± 15 g) were divided into four groups (A–D). Hypertension was induced by surgical means in groups C and D. Animals in groups B and D were treated with nifedipine (0.85 mg/kg) via a gastroesophageal catheter the day after surgery (experimental day-1) for 2 weeks. A significant difference was observed between the control group and nifedipine group and between the control group and hypertension group with regard to the weight of the parotid gland and its surface area. Histological findings demonstrated changes in the parotid glands of hypertensive animals with mild vessel dilatation and infiltration of inflammatory cells. These histological findings seemed to be due more to changes in venous function than to alterations in gland architecture.

Solubility enhancement, physicochemical characterization and formulation of fast-dissolving tablet of nifedipine-betacyclodextrin complexes

Jagdale,Swati Changdeo; Jadhav,Vinayak Narhari; Chabukswar,Aniruddha Rajaram; Kuchekar,Bhanudas Shankar
Fonte: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas Publicador: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/03/2012 EN
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The main objective of the study was to enhance the dissolution of nifedipine, a poorly water soluble drug by betacyclodextrin complexation and to study the effect of the preparation method on the in vitro dissolution profile. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of nifedipine with β-cyclodextrin was 1:1. Binary complex was prepared by different methods and was further characterized using XRD, DSC and FT-IR. A saturation solubility study was carried out to evaluate the increase in solubility of nifedipine. The optimized complex was formulated into fast-dissolving tablets by using the superdisintegrants Doshion P544, pregelatinized starch, crospovidone, sodium starch glycolate and croscarmellose sodium by direct compression. Tablets were evaluated for friability, hardness, weight variation, disintegration and in vitro dissolution. Tablets showed an enhanced dissolution rate compared to pure nifedipine.

Hemodynamic and metabolic effects after nifedipine and ritodrine tocolysis

Papatsonis, D.; van Geijn, H.; Bleker, O.; Ader, H.; Dekker, G.
Fonte: Elsevier Sci Ireland Ltd Publicador: Elsevier Sci Ireland Ltd
Tipo: Artigo de Revista Científica
Publicado em //2003 EN
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Objectives: The purpose of this study is to compare the hemodynamic and metabolic changes after ritodrine and nifedipine tocolysis. Methods: For an open randomized study, patients with preterm labor (N=185) were allocated to groups to receive ritodrine intravenously (N=90) or nifedipine orally (N=95). Results: The mean diastolic blood pressure was significantly lower in the ritodrine group 24 h (65±12 vs. 70±8, P=0.001) and 48 h (65±12 vs. 71±8, P=0.004) after starting tocolysis compared with the nifedipine group. Mean maternal heart rate was significantly higher in the ritodrine group 24 h (105±17 vs. 86±13, P<0.0001) and 48 h (100±21 vs. 85±12, P<0.0001) after starting tocolysis compared with the nifedipine group. Mean fasting glucose levels were higher (6.68±2.53 vs. 4.93±1.23, P=0.0016), while mean potassium levels were lower (3.52±0.84 vs. 3.81±0.45, P=0.04) in the ritodrine group 48 h after starting tocolysis compared with the nifedipine group. Conclusions: Use of nifedipine for preterm labor is associated with a lower incidence of adverse hemodynamic and metabolic changes compared with ritodrine after 24 and 48 h of tocolysis. In our opinion nifedipine is the preferred drug of choice for the treatment of preterm labor.; D. N. M. Papatsonis...

Crossover comparison of nifedipine OROS(R) and felodipine extended release with blind 24 H ambulatory blood pressure assessments

Taverner, D.; Marley, J.; Tonkin, A.
Fonte: BLACKWELL SCIENCE ASIA Publicador: BLACKWELL SCIENCE ASIA
Tipo: Artigo de Revista Científica
Publicado em //1999 EN
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1. The aim of the present study was to compare the efficacy of nifedipine Oros and felodipine extended release (ER) in controlling 24 h ambulatory blood pressures (ABP) in hypertensive patients. 2. The study was a randomized cross-over design with a 2 week open placebo run-in phase and two observer-blind treatment periods. 3. Subjects were males and females, aged between 18 and 65 years, suffering from mild to moderate essential hypertension with a sitting mean diastolic blood pressure (DBP) within the range of 95-114 mmHg. Twenty-three subjects were randomized to treatment; 15 patients completed the study. 4. Treatment intervention was 2 weeks of placebo followed by either 30 mg nifedipine OROS once daily or 5 mg felodipine ER once daily for 6 weeks, which was titrated up to 60 mg nifedipine OROS daily or 10 mg felodipine ER daily after 2 weeks of treatment on the lower doses if the DBP was > 90 mmHg. The main outcome measure was 24 h ABP after 6 weeks of active treatment, evaluated by an independent observer blinded as to treatment allocation. 5. Compared with placebo, mean (+/- SD) 24 h DBP was reduced by 6.2 +/- 6.8 and 5.2 +/- 5.1 mmHg after nifedipine and felodipine, respectively. The 24 h mean systolic blood pressure (SBP) fell by 11.8 +/- 10.9 and 10.1 +/- 8.2 mmHg for nifedipine and felodipine...

Nifedipine pharmacokinetics and plasma levels in the management of preterm labor

Papatsonis, D.; Bos, J.; van Geijn, H.; Lok, C.; Dekker, G.
Fonte: Lippincott Williams & Wilkins Publicador: Lippincott Williams & Wilkins
Tipo: Artigo de Revista Científica
Publicado em //2007 EN
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The aim of this study was to determine if the dose regimen of nifedipine used for tocolysis was effective to achieve uterine quietness, and at which plasma concentration levels this tocolysis was achieved to optimize our dose regimen of nifedipine. In women with preterm labor, nifedipine was administered orally to achieve uterine quietness to prevent preterm birth. Patients (n = 5) were administered 10 mg nifedipine capsules (Adalat capsules, Bayer AG) orally every 15 minutes up to 40 mg in the first hour, and were subsequently given 1 tablet of 20 mg nifedipine slow release (Adalat retard, Bayer AG) t = 90 min. Plasma levels of nifedipine were measured at regular intervals during the first 4 hours after starting tocolysis. In all 5 patients tocolysis was achieved with nifedipine. Peak plasma concentration of nifedipine was 127.2 +/- 44 ng/mL at 1.2 +/- 0.1 hours. Mean plasma concentrations of nifedipine was 67.4 +/- 28.4 ng/mL. In all patients, tocolysis was achieved during the 4 hours of blood sampling. There were no adverse hemodynamic side effects seen before and after starting tocolysis with nifedipine. Initial dose regimen of 4 times 10 mg nifedipine capsule orally in the first hour, followed by 20 mg slow release nifedipine at t = 90 min is effective in achieving tocolysis in women with preterm labor. In steady state...

Nifedipine as a uterine relaxant for external cephalic version: a randomized controlled trial

Kok, M.; Bais, J.; van Lith, J.; Papatsonis, D.; Kleiverda, G.; Hanny, D.; Doornbos, J.; Mol, B.; van der Post, J.
Fonte: Lippincott Williams & Wilkins Publicador: Lippincott Williams & Wilkins
Tipo: Artigo de Revista Científica
Publicado em //2008 EN
Relevância na Pesquisa
37.2%
OBJECTIVE: To estimate the effectiveness of nifedipine as a uterine relaxant during external cephalic version to correct breech presentation. METHODS: In this randomized, double-blind, placebo-controlled trial, women with a singleton fetus in breech presentation and a gestational age of 36 weeks or more were eligible for enrollment. Participating women received two doses of either nifedipine 10 mg or placebo, 30 and 15 minutes before the external cephalic version attempt. The primary outcome was a cephalic-presenting fetus immediately after the procedure. Secondary outcome measures were cephalic presentation at delivery, mode of delivery, and adverse events. A sample size of 292 was calculated to provide 80% power to detect a 17% improvement of the external cephalic version success rate, assuming a placebo group rate of 40% and alpha of .05. RESULTS: Outcome data for 310 of 320 randomly assigned participants revealed no significant difference in external cephalic version success rates between treatment (42%) and control group (37%) (relative risk 1.1, 95%; 95% confidence interval 0.85–1.5). The cesarean delivery rate was 51% in the treatment group and 46% in the control group (relative risk 1.1, 95% confidence interval 0.88–1.4). CONCLUSION: Nifedipine did not significantly improve the success of external cephalic version. Future use of nifedipine to improve the outcome of external cephalic version should be limited to large clinical trials.; Marjolein Kok...

Effect of maintenance tocolysis with nifedipine in threatened preterm labor on perinatal outcomes: a randomized controlled trial

Roos, C.; Spaanderman, M.; Schuit, E.; Bloemenkamp, K.; Bolte, A.; Cornette, J.; Duvekot, J.; van Eyck, J.; Franssen, M.; de Groot, C.; Kok, J.; Kwee, A.; Merien, A.; Bijivank, B.; Opmeer, B.; Oudijk, M.; van Pampus, M.; Papatsonis, D.; Porath, M.; Scheep
Fonte: American Medical Association Publicador: American Medical Association
Tipo: Artigo de Revista Científica
Publicado em //2013 EN
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IMPORTANCE In threatened preterm labor, maintenance tocolysis with nifedipine, after an initial course of tocolysis and corticosteroids for 48 hours, may improve perinatal outcome. OBJECTIVE To determine whether maintenance tocolysis with nifedipine will reduce adverse perinatal outcomes due to premature birth. DESIGN, SETTING, AND PARTICIPANTS APOSTEL-II (Assessment of Perinatal Outcome with Sustained Tocolysis in Early Labor) is a double-blind, placebo-controlled trial performed in 11 perinatal units including all tertiary centers in the Netherlands. From June 2008 to February 2010, women with threatened preterm labor between 26 weeks (plus 0 days) and 32 weeks (plus 2 days) gestation, who had not delivered after 48 hours of tocolysis and a completed course of corticosteroids, were enrolled. Surviving infants were followed up until 6 months after birth (ended August 2010). INTERVENTION Randomization assigned 406 women to maintenance tocolysis with nifedipine orally (80 mg/d; n = 201) or placebo (n = 205) for 12 days. Assigned treatment was masked from investigators, participants, clinicians, and research nurses. MAIN OUTCOME MEASURES Primary outcome was a composite of adverse perinatal outcomes (perinatal death, chronic lung disease...

Pharmacokinetics of nifedipine slow-release during sustained tocolysis

ter Laak, M.A.; Roos, C.; Touw, D.J.; van Hattum, P.R.; Kwee, A.; Lotgering, F.K.; Mol, B.W.; van Pampus, M.G.; Porath, M.M.; Spaanderman, M.E.; van der Post, J.A.; Papatsonis, D.N.; van 't Veer, N.E.
Fonte: Dustri-Verlag Publicador: Dustri-Verlag
Tipo: Artigo de Revista Científica
Publicado em //2015 EN
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OBJECTIVE: The pharmacokinetics of nifedipine as a tocolytic agent has not been studied in great detail in pregnant women and has instead focused on immediate release tablets and gastrointestinal therapeutic system (GITS) tablets. The aim of this study was to determine nifedipine slow-release half-life and distribution volume in pregnant women and to compare these with pharmacokinetic parameters of nifedipine in non-pregnant subjects described in the literature. MATERIALS: This is a study parallel to a trial studying women with threatened preterm labor between 26 + 0 and 32 + 2 weeks after initial tocolysis and a completed course of corticosteroids, who were randomly allocated to maintenance nifedipine (slow-release tablets 20 mg 4 times daily) or placebo. Exclusion criteria for the pharmacokinetic study were contra-indications for nifedipine, impaired liver function, and concomitant intake of inhibitors or inducers of the cytochrome P450 3A4 isoenzyme. Blood samples for measuring nifedipine plasma concentrations were drawn at t = 0, t = 12 hours, t = 24 hours, t = 48 hours, t = 72 hours, t = 7 days, and t = 9 days. METHODS: Pharmacokinetic parameters were estimated using iterative two-stage Bayesian population pharmacokinetic analysis by MWPharm© software. The study was designed to establish a correlation between body weight and nifedipine plasma level. RESULTS: The pharmacokinetic parameters of nifedipine slow-release tablets were determined from the data of 8 pregnant women. Nifedipine slow-release had a half-life of 2 - 5 hours...

ESTUDO COMPARATIVO DUPLO-CEGO DA EFICACIA E SEGURANCA DO CILAZAPRIL COMPARADAS A NIFEDIPINE 'RETARD' NO TRATAMENTO DA HIPERTENSAO ARTERIAL LEVE E MODERADA

Velasco-Cornejo, I. F.; Mion, D.; Cuadrado Martin, L.; Tinucci, T.; Sampaio, M.; Pascoal, I. J.; Athanazio-Heliodoro, R. C.; Marcondes, M.; Franco, Roberto Jorge da Silva
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 159-164
POR
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Purpose: To evaluate the antihypertensive efficacy and safety of cilazapril compared to nifedipine retard in mild to moderate hypertension. Methods: Forty randomized out-patients with mild moderate hypertension, diastolic pressure (DP) between 95 and 115 mmg/Hg, with placebo for 15 days were randomized and allocated for treatment, double-blind, once daily with cilazapril 2.5 mg (n = 20) or nifedipine retard 20 mg (20 = n) for four weeks. The non-responders (DP > 90 mmHg) had the dosage increased twice, b.i.d., while responders were maintained up to 10 weeks. Clinical visits were performed before, at baseline and every two weeks and the laboratory test was performed after placebo run-in, 4th and 10th weeks of treatment. Results: The blood pressure (BP) were similar between groups at the end of the placebo (cilazapril 151 ± 14/103 ± 5 - nifedipine 157 ± 17/108 ± 7 mmHg, p > 0.05). DP decreased already at second weeks (cilazapril 95 ± 9 - nifedipine 96 ± 11 mmHg, p < 0.05, compared to week 0) in both groups at the end of study with no differences inter groups. BP normalization was obtained in 58% of the patients with cilazapril and in 61% in the nifedipine group. Adverse biochemical effects were not observed in any group. Six (16%) patients of the cilazapril and 15 (39%) of nifedipine related collateral events...

Epidemiological analysis of nifedipine and phenytoin-induced gingival overgrowth in users of the Primary Health Care System

Fonseca,Luciara Viana Leão; Martelli Júnior,Hercílio; Gonçalves,Patrícia Furtado; Carvalho,Fillipe Mateus Castro de; Coletta,Ricardo Della; Bonan,Paulo Rogério Ferreti
Fonte: Pontifícia Universidade Católica do Rio Grande do Sul Publicador: Pontifícia Universidade Católica do Rio Grande do Sul
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2010 EN
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PURPOSES: The aim of this study was to evaluate the prevalence of drug-induced gingival overgrowth (DIGO) in Brazilian users of nifedipine and/or phenytoin and to determine the presence of predisposing/modifying factors. METHODS: Demographic, pharmacological, and periodontal data were obtained from 100 users of the Brazilian Primary Health Care System in Diamantina, Jequitinhonha Valley, Minas Gerais state, Brazil, who were taking nifedipine and/or phenytoin. Clinical evaluations including gingival overgrowth analysis were carried out by a single calibrated examiner. Bivariate analysis (Chi-square test or Student's t-test) were used to identify demographic, periodontal and drug-related significant factors associated with gingival overgrowth severity. Multivariate analysis (Poisson regression) was used to assess confounding factors. RESULTS: The prevalence of DIGO was high (86%), but its severity was predominately mild. The prevalence of DIGO was significantly higher in phenytoin users than in nifedipine users (p=0.01). There was no association between DIGO and demographic, pharmacological or periodontal variables. CONCLUSION: The high occurrence of DIGO among users of nifedipine and phenytoin emphasizes the importance of the dentist as part of the public health team to provide the prevention...

Nifedipina promove diminuição da qualidade óssea em ratas com osteopenia; Nifedipine decreases bone quality in female rats with osteopenia

Bertoncello, Dernival; Silva, Andrezza Ferreira da; Borges, Juliana Almeida de Souza
Fonte: Universidade de São Paulo. Faculdade de Medicina Publicador: Universidade de São Paulo. Faculdade de Medicina
Tipo: info:eu-repo/semantics/article; info:eu-repo/semantics/publishedVersion; ; ; ; ; ; Formato: application/pdf
Publicado em 01/10/2008 POR
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37.2%
O objetivo do trabalho foi avaliar, por parâmetros biomecânicos e físicos, a qualidade óssea dos fêmures de ratas ovariectomizadas tratadas com nifedipina. Foram utilizadas 28 ratas Wistar, de 4 meses de idade, divididas nos grupos: intactas (Int); ovariectomizadas tratadas com salina (Ovx+Sal); ovariectomizadas tratadas com nifedipina (Ovx+Nfd), intactas tratadas com nifedipina (Int+Nfd). O tratamento durou oito semanas, seis dias por semana, com administração de nifedipina ou salina, por gavage, na dose de 10 mg e 0,1g/100g PC respectivamente. Tendo-se retirado o fêmur direito de cada animal, verificou-se a carga máxima suportada, a densidade mineral e a qualidade óssea. Os resultados foram analisados estatisticamente, com nível de significância fixado em p; The aim of this study was to assess, by biomechanical and physical parameters, the bone quality of femurs from ovariectomized female rats treated with nifedipine. Twenty eight Wistar female rats, 4 months old, were divided into four groups: intact (Int); intact treated with nifedipine (Int+Nfd); ovariectomized treated with saline (Ovx+Sal); ovariectomized treated with nifedipine (Ovx+Nfd). Treatment was carried out for eight weeks, six days per week, with administration of 10 mg of nifedipine or 0.1/100g BW of saline...

Solubility enhancement, physicochemical characterization and formulation of fast-dissolving tablet of nifedipine-betacyclodextrin complexes

Jagdale, Swati Changdeo; Jadhav, Vinayak Narhari; Chabukswar, Aniruddha Rajaram; Kuchekar, Bhanudas Shankar
Fonte: Universidade de São Paulo. Faculdade de Ciências Farmacêuticas Publicador: Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
Tipo: info:eu-repo/semantics/article; info:eu-repo/semantics/publishedVersion; ; ; ; ; ; Formato: application/pdf
Publicado em 01/03/2012 ENG
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The main objective of the study was to enhance the dissolution of nifedipine, a poorly water soluble drug by betacyclodextrin complexation and to study the effect of the preparation method on the in vitro dissolution profile. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of nifedipine with β-cyclodextrin was 1:1. Binary complex was prepared by different methods and was further characterized using XRD, DSC and FT-IR. A saturation solubility study was carried out to evaluate the increase in solubility of nifedipine. The optimized complex was formulated into fast-dissolving tablets by using the superdisintegrants Doshion P544, pregelatinized starch, crospovidone, sodium starch glycolate and croscarmellose sodium by direct compression. Tablets were evaluated for friability, hardness, weight variation, disintegration and in vitro dissolution. Tablets showed an enhanced dissolution rate compared to pure nifedipine.; Este estudo teve por objetivo principal incrementar a dissolução do nifedipino, fármaco pouco solúvel em água, por meio de sua complexação com β-ciclodextrina e estudar o efeito do método de preparação sobre o perfil de dissolução in vitro. A razão estequiométrica...

The NIFTY study: a multicentre randomised double-blind placebo-controlled trial of nifedipine maintenance tocolysis in fetal fibronectin-positive women in threatened preterm labour

Parry, E.; Roos, C.; Stone, P.; Hayward, L.; Mol, B.W.; McCowen, L.
Fonte: Wiley Publicador: Wiley
Tipo: Artigo de Revista Científica
Publicado em //2014 EN
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OBJECTIVE: In an unselected group of women with signs of preterm labour, maintenance tocolysis is not effective in the prevention of preterm birth and does not improve neonatal outcome. Among women with signs of preterm labour, those who are fetal fibronectin positive have an increased risk of preterm birth. We investigated whether maintenance tocolysis with nifedipine would delay delivery and improve neonatal outcome in women with threatened preterm labour and a positive fetal fibronectin status. STUDY DESIGN: Women with a singleton pregnancy in threatened preterm labour (24(+0) to 33(+6)  weeks) with a positive fetal fibronectin test were randomised to nifedipine or placebo. Study medication was continued until 36 completed weeks' gestation. The primary endpoint was prolongation of pregnancy of seven days. Secondary endpoints were gestational age at delivery and length of NICU admission. RESULTS: Of the 60 participants, 29 received nifedipine and 31 placebo. Prolongation of pregnancy by >7 days occurred in 22/29 (76%) in the nifedipine group and 25/31 (81%) in the placebo group (relative risks, RR 0.94 [0.72-1.2]). Gestational age at delivery was 36.1 ± 5.1 weeks for nifedipine and 36.8 ± 3.6 weeks for placebo (P = 0.027). Length of NICU admission [median (interquartile ranges...