RESUMEN
OBJECTIVE: The aim of this study is to describe the effectiveness and safety of a magistral formulation of diltiazem 2% rectal gel as a treatment for chronic anal fissure. MATERIAL AND METHODS: A retrospective observational study of all patients that began treatment with diltiazem 2% gel during 2019. The primary endpoint of the study was anal fissure healing. We also looked for differences in effectiveness between those initiating treatment and those who had been previously treated, long-term effectiveness through a 2-year follow-up and frequency of adverse effects. RESULTS: Of the 166 patients included in the study, anal fissure healed in 72.9%. We detected adverse effects in 12 patients, the most common was local irritation. After 2 years of follow-up, 88% of patients did not relapse. CONCLUSION: In this study, use of topical diltiazem 2% has been shown to be effective and safe in the treatment of anal fissure and should be considered as the first line of therapy.
OBJETIVO: El objetivo de este estudio es describir la efectividad y la seguridad de una fórmula magistral de diltiazem 2% gel rectal, como tratamiento de la fisura anal crónica. MATERIAL Y MÉTODOS: Un studio observacional retrospectivo de todos los pacientes que comenzaron a ser tratados con diltiazem 2% gel durante el año 2019. La variable principal del estudio fue la cicatrización de la fisura anal. También se buscaron diferencias de efectividad entre aquellos que iniciaban el tratamiento y los que ya habían sido tratados previamente, efectividad a largo plazo mediante un seguimiento de 2 años y frecuencia de aparición de efectos adversos. RESULTADOS: De los 166 pacientes incluidos en el estudio, el 72,9% cicatrizaron la fisura anal. No detectamos diferencias estadísticamente significativas de efectividad entre los pacientes naive y aquellos que ya habían sido tratados. Detectamos efectos adversos en 12 pacientes, siendo el más frecuente la irritación local. Tras 2 años de seguimiento, el 88% de los pacientes no presentaron ninguna recaída. CONCLUSIÓN: En este estudio, el uso de diltiazem 2% tópico ha mostrado ser efectivo y seguro en el tratamiento de la fisura anal y debería considerarse como primera línea terapéutica.
Asunto(s)
Diltiazem , Fisura Anal , Humanos , Diltiazem/uso terapéutico , Diltiazem/efectos adversos , Fisura Anal/tratamiento farmacológico , Fisura Anal/inducido químicamente , Administración Tópica , Enfermedad Crónica , Cicatrización de Heridas , Resultado del TratamientoRESUMEN
OBJECTIVE: To detect and to compare the apoptotic effects of intraoperatively topically applied diltiazem, papaverine, and nitroprusside. METHODS: Internal thoracic artery segments of ten patients were obtained during coronary bypass grafting surgery. Each internal thoracic artery segment was divided into four pieces and immersed into four different solutions containing separately saline (Group S), diltiazem (Group D), papaverine (Group P), and nitroprusside (Group N). Each segment was examined with both hematoxylin-eosin and the terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling (TUNEL) method in order to determine and quantify apoptosis. RESULTS: Apoptotic cells were counted in 50 microscopic areas of each segment. No significant difference was observed among the four groups according to hematoxylin-eosin staining. However, the TUNEL method revealed a significant increase in mean apoptotic cells in the diltiazem group when compared with the other three groups (Group S=4.25±1.4; Group D=13.31±2.8; Group N=9.48±2.09; Group P=10.75±2.37). The differences between groups were significant (P=0.0001). No difference was observed between the samples of the diabetic and non-diabetic patients in any of the study groups. CONCLUSION: The benefit of topically applied vasodilator drugs must outweigh the potential adverse effects. In terms of apoptosis, diltiazem was found to have the most deleterious effects on internal thoracic artery graft segments. Of the analyzed medical agents, nitroprusside was found to have the least apoptotic activity, followed by papaverine. Diabetes did not have significant effect on the occurrence of apoptosis in left internal thoracic artery grafts.
Asunto(s)
Diltiazem/uso terapéutico , Arterias Mamarias , Nitroprusiato/uso terapéutico , Papaverina/uso terapéutico , Vasodilatadores/uso terapéutico , Diltiazem/farmacología , Humanos , Nitroprusiato/farmacología , Papaverina/farmacología , Vasodilatadores/farmacologíaRESUMEN
Abstract Objective: To detect and to compare the apoptotic effects of intraoperatively topically applied diltiazem, papaverine, and nitroprusside. Methods: Internal thoracic artery segments of ten patients were obtained during coronary bypass grafting surgery. Each internal thoracic artery segment was divided into four pieces and immersed into four different solutions containing separately saline (Group S), diltiazem (Group D), papaverine (Group P), and nitroprusside (Group N). Each segment was examined with both hematoxylin-eosin and the terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling (TUNEL) method in order to determine and quantify apoptosis. Results: Apoptotic cells were counted in 50 microscopic areas of each segment. No significant difference was observed among the four groups according to hematoxylin-eosin staining. However, the TUNEL method revealed a significant increase in mean apoptotic cells in the diltiazem group when compared with the other three groups (Group S=4.25±1.4; Group D=13.31±2.8; Group N=9.48±2.09; Group P=10.75±2.37). The differences between groups were significant (P=0.0001). No difference was observed between the samples of the diabetic and non-diabetic patients in any of the study groups. Conclusion: The benefit of topically applied vasodilator drugs must outweigh the potential adverse effects. In terms of apoptosis, diltiazem was found to have the most deleterious effects on internal thoracic artery graft segments. Of the analyzed medical agents, nitroprusside was found to have the least apoptotic activity, followed by papaverine. Diabetes did not have significant effect on the occurrence of apoptosis in left internal thoracic artery grafts.
Asunto(s)
Humanos , Papaverina/uso terapéutico , Vasodilatadores/uso terapéutico , Nitroprusiato/uso terapéutico , Diltiazem/uso terapéutico , Arterias Mamarias , Papaverina/farmacología , Vasodilatadores/farmacología , Nitroprusiato/farmacología , Diltiazem/farmacologíaRESUMEN
Anal sphincter spasm contributes to the delay in surgical wound healing after hemorrhoidectomy. A prospective, experimental, randomized, double-blind trial was conducted on two groups of patients that underwent closed hemorrhoidectomy. There were 26 patients in each group. Group A received topical diltiazem in the anal region three times a day. Group B received a placebo. Cicatrization time was documented for 6 weeks through digital photography. Mean healing time for the group treated with diltiazem was 3.19 weeks (22.33±0.884 days) and 3.92 weeks (27.44±1.130 days) for the control group (p=0.012 95% CI). At week three, the wounds in 73.07% of the patients in the diltiazem group had healed, compared with 46.15% of the patients in the control group.
Asunto(s)
Bloqueadores de los Canales de Calcio/uso terapéutico , Diltiazem/uso terapéutico , Hemorreoidectomía/efectos adversos , Complicaciones Posoperatorias/tratamiento farmacológico , Cicatrización de Heridas/efectos de los fármacos , Cicatriz/tratamiento farmacológico , Cicatriz/patología , Método Doble Ciego , Femenino , Humanos , Masculino , Persona de Mediana Edad , Dolor Postoperatorio/tratamiento farmacológico , Estudios Prospectivos , Resultado del TratamientoRESUMEN
A fissura anal é uma laceração do revestimento do canal anal inferior. É uma das patologias benignas anorretais mais comuns e, em muitos casos, resolve-se espontaneamente. Sua prevalência é igual entre os sexos e é mais comum em adultos jovens. A grande maioria das fissuras são primárias e causadas por trauma local, como constipação, diarreia ou sexo anal. Fissuras secundárias são encontradas em pacientes com Doença de Crohn, malignidades (neoplasia epidermoide do canal anal, leucemia), tuberculose ou doenças sexualmente transmissíveis (HIV, sífilis, clamídia). Esta guia apresenta informação que orienta a conduta para casos de fissura anal no contexto da Atenção Primária à Saúde, incluindo: classificação, avaliação clínica, diagnóstico, tratamento clínico, tratamento cirúrgico e encaminhamento para especialista.
Asunto(s)
Humanos , Fisura Anal/diagnóstico , Fisura Anal/terapia , Atención Primaria de Salud , Diltiazem/uso terapéutico , Fisura Anal/cirugía , Esfinterotomía Lateral Interna/instrumentaciónRESUMEN
ABSTRACT A stability indicating HPLC method to determine diltiazem hydrochloride (DTZ) in tablets and compounded capsules was developed and validated according to Brazilian and the International Conference on Harmonization (ICH) guidelines. The separation was carried out on a Purospher Star® C18 (150 x 4.6 mm i.d., 5 µm particle size, Merck Millipore) analytical column. The mobile phase consisted of a 0.05% (v/v) trifluoroacetic acid aqueous solution and a 0.05% trifluoroacetic acid methanolic solution (44:56, v/v). The flow rate was 1.0 mL.min-1 with a run time of 14 minutes. The detection of DTZ and degradation products (DP) was performed at 240 nm, using a diode array detector. The method proved to be linear, precise, accurate, selective, and robust, and was adequate for stability studies and routine quality control analyses of DTZ in tablets and compounded capsules.
Asunto(s)
Diltiazem/uso terapéutico , Cromatografía Líquida de Alta Presión/métodos , Estudio de Validación , Comprimidos/farmacología , Cápsulas/farmacologíaRESUMEN
Introducción: en pacientes cardiópatas isquémicos se han diseñado diversas estrategias preventivas farmacológicas para limitar el daño por isquemia- reperfusión, con el fin de optimizar el balance en el consumo miocárdico de oxigeno. Objetivos: determinar qué estrategia cardio-protectora (nitroglicerina o diltiazem) es más efectiva en la revascularización coronaria.Métodos: se realizó un estudio comparativo aleatorio para evaluar el efecto cardio protector de la nitroglicerina y el diltiazem en pacientes intervenidos con el corazón latiendo. Resultados: se estudiaron 175 pacientes; los de nitroglicerina, grupo N=90 pacientes y los de diltiazem, grupo D=85. La isquemia miocárdica sostenida, en el grupo D fue del 20 por ciento vs N con 12 por ciento; p= 0,04. Primó el infra desnivel del ST[a1] . En el grupo N fue 10 % vs grupo D de 39 por ciento; p=0,002. La alteración segmentaria más frecuente fue la hipocinesia en el 36 por ciento de los pacientes. La acinesia fue superior en el grupo D, 9,4 por ciento v/s grupo N 4,4 por ciento; p=0,05. El valor promedio de tensión arterial media intraoperatoria fue en el grupo N=80 mm/Hg vs grupo D= 61,4 mm/Hg; p= 0,003. La frecuencia cardiaca media en el grupo N=63 lpm vs grupo D=50 lpm; p=0,006. La arritmia más frecuente fue la fibrilación auricular 28 por ciento, en el grupo N 34 por ciento vs grupo D 21 por ciento, p=0,037. El valor medio de la troponina Tus a las 24 h, en el grupo D=125 pg/ml, vs grupo N=97,7 pg/ml; p=0,042. Los efectos adversos fueron mínimos. La hipotensión arterial sostenida, en el grupo D fue 30 por ciento vs grupo N 5,5 por ciento; p=0,002. El bloqueo AV[a2] se observó en el grupo N 4 por ciento vs grupo D 15 por ciento; p=0,01. El IMA [a3] perioperatorio fue 2,2 veces más frecuente con diltiazem, que con nitroglicerina.Conclusiones: la infusión perioperatoria de nitroglicerina provee un mejor efecto cardio protector que el diltiazem en la prevención de eventos isquémicos ... (AU)
Introduction: in the cases of ischemic cardiopathy patients, different preventive strategies have been designed to limit the damage for ischemia-reperfusion, in order to optimize the balance in myocardial oxygen consumption. Objectives: To determine what cardio-protective (nitroglycerin or diltiazem) strategy is more effective in coronary revascularization. Methods: A randomized therapeutic trial was conducted to assess the cardio-protective effect of diltiazem and nitroglycerin in patients intervened with heart beating. Results: 175 patients were studied: the nitroglycerin group N=90 patients and the diltiazem group D=85. Sustained myocardial ischemia in group D was 20 percent vs. 12 percent in N; p=0.04. ST infra-imbalance prevailed. It was 10 percent in the N group vs 39 percent in group D; p = 0.002. The most frequent alteration was segmental hypokinesia in 36 percent of the patients. Akinesia was higher in group D, 9.4 percent vs. group N 4.4 percent; p = 0.05. The average value of mean intraoperative blood pressure was 80 mm/Hg in the group N vs.61.4 mm/Hg in group D; p = 0.003. The average heart rate in the group N was 63 bpm vs Group D which was 50 bpm; p = 0.006. The most common arrhythmia was atrial fibrillation 28 percent, in the N group 34 percent vs. group D 21 percent, p = 0.037. The average value of troponin after 24 h was 125 pg/ml in group D vs.97.7 pg/ml in group N; p = 0.042. Adverse effects were minimal. Sustained hypotension in group D was 30 percent vs 5.5 percent in group N; p = 0.002. AV block was observed in the group N 4 percent vs 15 percent in group D; p = 0.01. Perioperative IMA was 2.2 times more frequent with diltiazem than with nitroglycerin. Conclusions: Perioperative infusion of nitroglycerin provides better cardioprotective effect then diltiazem in preventing sustained ischemic events, associated with less release of T troponin and better hemodynamic stability. Diltiazem is associated with a decreased risk of postoperative ...(AU)
Asunto(s)
Humanos , Femenino , Persona de Mediana Edad , Anciano de 80 o más Años , Isquemia Miocárdica/diagnóstico , Isquemia Miocárdica/terapia , Revascularización Miocárdica/efectos adversos , Factores de Riesgo , Diltiazem/uso terapéutico , Nitroglicerina/uso terapéutico , Cardiotónicos/administración & dosificaciónRESUMEN
BACKGROUND: Anal sphincter spasm contributes to the appearance of postoperative pain following hemorrhoidectomy. AIM: To determine the efficacy of topical diltiazem in the control of post-hemorrhoidectomy pain. MATERIAL AND METHODS: A randomized, prospective, experimental, double-blind study was conducted on 2 groups of patients in the postoperative period of closed hemorrhoidectomy. Each group consisted of 17 patients. Group A received topical diltiazem in the anal region 3 times a day and group B received a placebo. Ketorolac was administered to both groups as rescue therapy. RESULTS: In group A, the mean score on the visual analog scale was 2.97±1.18cm at 24h, 1.51±1.18cm at 48h, and 0.84±0.92cm at 72h. In group B, it was 6.82±1.9cm at 24h, 5.3±1.66cm at 48h, and 4.32±2.13cm at 72h (P<.001, 95% CI). The mean number of analgesic doses in group A was 2.41±0.87 at 24h, 1.11±0.85 at 48h, and 0.94±0.96 at 72h. In group B, it was 3.82±0.52 at 24h, 3.64±0.70 at 48h, and 2.88±1.26 at 72h (P<.001, 95% CI). CONCLUSIONS: In this study, topical administration of diltiazem resulted in a statistically significant reduction of postoperative pain in patients that underwent closed hemorrhoidectomy.
Asunto(s)
Diltiazem/uso terapéutico , Hemorreoidectomía/efectos adversos , Dolor Postoperatorio/tratamiento farmacológico , Vasodilatadores/uso terapéutico , Adulto , Anciano , Canal Anal/fisiopatología , Método Doble Ciego , Femenino , Hemorroides/cirugía , Humanos , Masculino , Persona de Mediana Edad , Dimensión del Dolor/efectos de los fármacos , Estudios Prospectivos , Espasmo/tratamiento farmacológico , Espasmo/etiologíaRESUMEN
La calcinosis cutis es el término empleado para describir una serie de trastornos caracterizados por presentar depósitos de sales de calcio a nivel subcutáneo o de la dermis, ocurriendo tanto en hipercalcemia como en normocalcemia y en ocasiones se asocia a un trastorno subyacente. El pronóstico suele ser benigno y el tratamiento, tanto médico como quirúrgico, presenta resultados variables. Presentamos dos casos de pacientes adultos con diagnóstico de dermatomiositis que desarrollaron extensas zonas de calcificación subcutánea.
Calcinosis cutis is the term used to describe a group of disorders characterized by calcium deposits in the skin, occurring in hypercalcemia or normocalcemia and sometimes associated to an underlying disorder. It has a benign evolution and the treatment, both medical and surgical, present variable outcomes. We report the cases of two adult patients with diagnosis of dermatomyositis that developed extensive areas of calcium deposit.
Asunto(s)
Humanos , Masculino , Femenino , Persona de Mediana Edad , Calcinosis/diagnóstico , Calcinosis/etiología , Dermatomiositis/complicaciones , Enfermedades de la Piel/diagnóstico , Enfermedades de la Piel/etiología , Bloqueadores de los Canales de Calcio/uso terapéutico , Calcinosis/tratamiento farmacológico , Diltiazem/uso terapéutico , Enfermedades de la Piel/tratamiento farmacológicoRESUMEN
BACKGROUND/AIMS: Late efficacy of medical treatment of chronic anal fissure remains controversial due to high recurrence. This study aimed at analyzing safety and efficacy of topical diltiazem and bethanechol regarding healing and symptoms relief, safety, recurrence, and need for surgery. METHODOLOGY: This was a single-center nonrandomized trial. Outcomes of 30 patients with chronic anal fissure treated with 2% diltiazem were compared to 30 patients treated with 0.1% bethanechol, both for eight weeks. Patients were assessed after seven days and eight weeks. RESULTS: In diltiazem group, after seven days, 31% were symptomatic; after bethanechol, 71% (p = 0.06). After seven days, fissure healing occurred in 19% after diltiazem and in 11% after bethanechol. After eight weeks, in both groups, 64% were asymptomatic; after diltiazem, 53% healed; after bethanechol, 50% (p = 0.80). Success was the same for both groups: 63.3%. Groups were similar regarding complications. After diltiazem, 9 (30%) patients were operated on; and 11 (36.7%) after bethanechol (p = 0.60). Recurrence occurred in 4 (13.3%) patients in both groups. Median time to recurrence after diltiazem was 15 (10-24) months and 7.5 (2-15) after bethanechol - p = 0.15. CONCLUSIONS: Both treatments are safe and effective. Diltiazem may be associated to earlier relief and more sustained response.
Asunto(s)
Betanecol/uso terapéutico , Diltiazem/uso terapéutico , Fisura Anal/tratamiento farmacológico , Agonistas Muscarínicos/uso terapéutico , Vasodilatadores/uso terapéutico , Administración Tópica , Adulto , Anciano , Enfermedad Crónica , Estudios de Cohortes , Femenino , Fisura Anal/patología , Fisura Anal/cirugía , Humanos , Masculino , Persona de Mediana Edad , Factores de Tiempo , Resultado del Tratamiento , Cicatrización de Heridas , Adulto JovenRESUMEN
The lack of dystrophin in mdx mice and in Duchenne muscular dystrophy causes sarcolemmal breakdown and increased calcium influx followed by myonecrosis. We examined whether the calcium channel blockers diltiazem and verapamil protect dystrophic muscles from degeneration. Mdx mice received daily intraperitoneal injections of diltiazem or verapamil for 18 days, followed by removal of the sternomastoid, diaphragm, tibialis anterior, and cardiac muscles. Control mdx mice were injected with saline. Both drugs significantly decreased blood creatine kinase levels. Total calcium content was significantly higher in mdx muscles than in control C57Bl/10. Verapamil and diltiazem reduced total calcium content only in diaphragm and cardiac muscle. Histological analysis showed that diltiazem significantly attenuated myonecrosis in diaphragm. Immunoblots showed a significant increase of calsequestrin and beta-dystroglycan levels in some diltiazem- and verapamil-treated muscles. Possible interactions of these drugs with the sarcoplasmic reticulum and sarcolemma may also contribute to the improvement of the dystrophic phenotype.
Asunto(s)
Bloqueadores de los Canales de Calcio/uso terapéutico , Diltiazem/uso terapéutico , Distrofia Muscular Animal/patología , Distrofia Muscular Animal/prevención & control , Sarcolema/efectos de los fármacos , Verapamilo/uso terapéutico , Animales , Calcio/metabolismo , Calsecuestrina/metabolismo , Creatina Quinasa/sangre , Modelos Animales de Enfermedad , Distroglicanos/metabolismo , Femenino , Masculino , Ratones , Ratones Endogámicos C57BL , Ratones Endogámicos mdx , Fibras Musculares Esqueléticas/efectos de los fármacos , Fibras Musculares Esqueléticas/metabolismo , Fibras Musculares Esqueléticas/ultraestructura , Sarcolema/metabolismoRESUMEN
OBJECTIVES: The aim of this work was to evaluate the pharmacokinetic-pharmacodynamic properties of diltiazem in an experimental model of high-renin hypertension, such as the aortic coarctated (ACo) rat, to further characterize the responsiveness of this model to calcium channel blockers. METHODS: A 'shunt' microdialysis probe was inserted in a carotid artery of anaesthetized ACo and control sham-operated (SO) rats for simultaneous determination of diltiazem plasma concentrations and their effects on mean arterial pressure and heart rate after the intravenous application of 3 and 6 mg/kg of the drug. Correlation between plasma levels and cardiovascular effects was established by fitting the data to a modified Emax model. KEY FINDINGS: Volume of distribution was greater in ACo than in SO rats. Diltiazem plasma clearance (Cl) was significantly greater in ACo rats than in normotensive SO rats after administration of diltiazem (6 mg/kg). Moreover, Cl increased with dose in ACo but not in SO rats. No differences were observed in the maximal bradycardic effect comparing both experimental groups, and sensitivity (S0) to diltiazem chronotropic effect was similar comparing SO and ACo rats. Differences were not found in the maximal response of the hypotensive effect comparing SO and ACo rats, but the S0 to diltiazem hypotensive effect was greater in ACo rats than in SO rats. CONCLUSIONS: ACo induced profound changes in diltiazem pharmacokinetic behaviour. In addition, our results suggested an increased sensitivity to diltiazem blood pressure lowering effect in experimental renovascular hypertension with high-renin levels.
Asunto(s)
Antihipertensivos/uso terapéutico , Presión Sanguínea/efectos de los fármacos , Diltiazem/uso terapéutico , Hipertensión/tratamiento farmacológico , Algoritmos , Animales , Antihipertensivos/sangre , Antihipertensivos/farmacocinética , Área Bajo la Curva , Bloqueadores de los Canales de Calcio/administración & dosificación , Bloqueadores de los Canales de Calcio/farmacocinética , Bloqueadores de los Canales de Calcio/uso terapéutico , Cromatografía Líquida de Alta Presión , Diltiazem/sangre , Diltiazem/farmacocinética , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Frecuencia Cardíaca/efectos de los fármacos , Hipertensión/sangre , Hipertensión/fisiopatología , Inyecciones Intravenosas , Masculino , Microdiálisis , Ratas , Ratas Sprague-Dawley , Renina/sangre , Resultado del TratamientoRESUMEN
We report the case of a 42-year-old man with no risk factors for coronary artery disease admitted with atypical chest pain. The electrocardiogram performed after intravenous injection of nitrate revealed ST-segment elevation in leads V1 to V4. The coronary angiography showed myocardial bridges in the three coronary arteries, besides an unusual length of the left anterior descending artery (80 mm). The patient progressed well following the discontinuation of nitrate use and introduction of beta-blockers and calcium channel antagonists.
Asunto(s)
Anomalías de los Vasos Coronarios/diagnóstico , Antagonistas Adrenérgicos beta/uso terapéutico , Adulto , Aspirina/uso terapéutico , Bloqueadores de los Canales de Calcio/uso terapéutico , Angiografía Coronaria , Anomalías de los Vasos Coronarios/tratamiento farmacológico , Diltiazem/uso terapéutico , Electrocardiografía , Humanos , Masculino , Metoprolol/uso terapéuticoRESUMEN
Homem de 42 anos, sem fatores de risco para doença arterial coronariana, internado com precordialgia atípica. Eletrocardiograma após a introdução de nitrato endovenoso evidenciou supradesnivelamento do segmento ST de V1 a V4. Cineangiocoronariografia demonstrou ponte miocárdica nas três artérias coronárias além de extensão incomum na descendente anterior (80 mm). A evolução foi satisfatória com a suspensão do nitrato e instituição de betabloqueador e antagonista de canais de cálcio.
We report the case of a 42-year-old man with no risk factors for coronary artery disease admitted with atypical chest pain. The electrocardiogram performed after intravenous injection of nitrate revealed ST-segment elevation in leads V1 to V4. The coronary angiography showed myocardial bridges in the three coronary arteries, besides an unusual length of the left anterior descending artery (80 mm). The patient progressed well following the discontinuation of nitrate use and introduction of beta-blockers and calcium channel antagonists.
Asunto(s)
Adulto , Humanos , Masculino , Anomalías de los Vasos Coronarios/diagnóstico , Antagonistas Adrenérgicos beta/uso terapéutico , Aspirina/uso terapéutico , Angiografía Coronaria , Bloqueadores de los Canales de Calcio/uso terapéutico , Anomalías de los Vasos Coronarios/tratamiento farmacológico , Diltiazem/uso terapéutico , Electrocardiografía , Metoprolol/uso terapéuticoRESUMEN
Cytochrome-P450 enzymes metabolize cyclosporine both in the liver and in the intestinal wall. Diltiazem, by competitive inhibition of these enzymes, may increase the absorption and the bioavailability of cyclosporine. Some evidence points to a higher activity of some specific enzymes in women, such as CYP3A, that may influence differences in cyclosporine pharmacokinetics. We examined possible gender-associated differences in pharmacokinetic profiles of cyclosporine in 19 stable renal transplant recipients cotreated with diltiazem. Ten women and nine men, chronically using diltiazem associated with cyclosporine, azathioprine, and prednisone were randomly assigned to an 8-week period of continued controlled treatment with diltiazem (10 patients) or a wash-out period discontinuing diltiazem (nine patients). At the end of this period, the time-concentration curves of cyclosporine in the first 4 hours were performed after a single dose of cyclosporine. Thereafter, a cross-over between groups was performed, and time-concentration curves repeated. A specific RIA was used to measure cyclosporine concentrations. Comparisons between male and female patients in doses of cyclosporine and other pharmacokinetics parameters (C(0), C(2), AUC(0-4)), with or without diltiazem, did not show any difference related to gender. The association of diltiazem allowed a similar degree of reduction in Neoral dosage in male and female patients (21%). No changes in serum creatinine, blood urea nitrogen, potassium, uric acid, or blood pressure, or other adverse event were observed during the study. In these groups of patients, gender was not an important factor to be considered when diltiazem is added to cyclosporine therapy.
Asunto(s)
Ciclosporina/farmacocinética , Ciclosporina/uso terapéutico , Diltiazem/uso terapéutico , Trasplante de Riñón/inmunología , Área Bajo la Curva , Bloqueadores de los Canales de Calcio/uso terapéutico , Ciclosporina/sangre , Interacciones Farmacológicas , Femenino , Humanos , Inmunosupresores/sangre , Inmunosupresores/farmacocinética , Inmunosupresores/uso terapéutico , Trasplante de Riñón/fisiología , Masculino , Caracteres SexualesRESUMEN
BACKGROUND: The area-under-the-curve (AUC) of cyclosporine (CsA) reflects exposure to the drug, but this monitoring strategy is time-consuming and not cost-effective. Recently, it has been suggested that the concentration at 2 hours after dosing (C2) shows the best correlation with AUC. The C2 has been replacing the trough measurement (C0) to monitor CsA therapy, but in patients receiving diltiazem there is not much information about this issue. We investigated the correlations between C2 and C0 with absorption AUC over the first 4 hours (AUC(0-4)) in renal stable transplant patients receiving CsA therapy with or without diltiazem. PATIENTS AND METHODS: Ten patients (five men) of ages 23 to 68 years and 6 to 84 months after transplantation, were randomly assigned to an 8-week initial period of either diltiazem washout or controlled treatment with diltiazem. Time-concentration curves of cyclosporine were performed at the end of this period using a specific RIA measurement of blood samples. Thereafter, a crossover of the groups was performed and after another 8 weeks, a second curve was obtained. Drugs that change the pharmacokinetics of cyclosporine or diltiazem were not allowed. RESULTS: The cyclosporine daily dose was lower with diltiazem (173 +/- 4 mg vs 213 +/- 4 mg, P = .002), but despite a dose reduction of only 19% +/- 1.5%, there was a trend to a larger AUC/dose (28 +/- 5 ng x h/mL x mg vs 17 +/- 2 ng x h/mL x mg, P = .1) and a trend to an increased C2 when treatment included diltiazem (1035 +/- 156 ng/mL vs 652 +/- 126 ng/mL, P = NS). Moreover, we confirmed that C2 showed the best correlation with AUC(0-4), (r = 0.7, P = .04), a correlation that improved with diltiazem (r = 0.9, P < .002). CONCLUSION: C2 is the point that correlates best with AUC(0-4) with or without diltiazem. C2 in the presence of diltiazem was associated with a stronger, more significant correlation with AUC(0-4).
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Diltiazem/farmacocinética , Trasplante de Riñón/inmunología , Vasodilatadores/farmacocinética , Adulto , Anciano , Área Bajo la Curva , Ciclosporina/sangre , Ciclosporina/farmacocinética , Ciclosporina/uso terapéutico , Diltiazem/sangre , Diltiazem/uso terapéutico , Monitoreo de Drogas/métodos , Humanos , Inmunosupresores/farmacocinética , Inmunosupresores/uso terapéutico , Persona de Mediana Edad , Vasodilatadores/uso terapéuticoRESUMEN
La fisura anal es una lesión que aparece en la porción epidérmica del canal anal, con sintomatología muy florida de dolor y sangrado defecatorio. Existen dos formas típicas, la primaria o idiopática, relacionada con la isquemia relativa del anodermo debida al incremento del tono basal esfintérico interno, y la secundaria a patologías infecciosas o del tubo digestivo. Objetivo y diseño: En los últimos años surgió el concepto de esfinterotomía química. El motivo de este trabajo es la comparación entre estas técnicas incruentas y la esfinterotomía quirúrgica, evaluando en forma prospectiva randomizada los pacientes tratados con diltiazem al 2 por ciento en vaselina sólida, trinitrato de glicerilo aplicados tópicamente y la esfinterotomía lateral interna.Material y Métodos: Durante el período comprendido entre el 31 de diciembre de 2002 y el 31 de diciembre de 2004 se trataron 174 pacientes; 56 con diltiazem al 2 por ciento, 60 con trinitrato de glicerilo y 58 por medio de esfinterotomía lateral interna 10 abierta y 48 cerrada, (Nottaras). La ubicación de la fisura fue en el 76.8 por ciento o 134 pacientes en hora VI, y en el 23.2 por ciento o 40 en hora XII. La distribución según sexo fue 96 (55.3 por ciento) varones y 78 ( 44.7 por ciento) mujeres. Resultados: Luego de una media de seguimiento de 87 días (7 a 330 días), en el grupo tratado con diltiazem, 33 pacientes presentaron la desaparición de los síntomas en la primer semana, con una curación y epitelización, sin recidiva, en 38 pacientes a las 6 semanas. 7 pacientes evolucionaron mal y necesitaron cirugía, y 9 no se presentaron al control y seguimiento.En el grupo tratado con trinitrato de glicerilo, 36 pacientes tuvieron una buena evolución, 5 necesitaron cirugía, 10 no volvieron a control y 9 suspendieron el tratamiento por reacciones adversas. El grupo de 58 pacientes tratado quirúrgicamente evolucionó favorablemente excepto 2 de ellos que necesitaron una anoplastía con deslizamiento de colgajo. Conclu...
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Humanos , Masculino , Adolescente , Adulto , Femenino , Niño , Persona de Mediana Edad , Anciano de 80 o más Años , Canal Anal , Canal Anal/irrigación sanguínea , Fisura Anal/cirugía , Fisura Anal/clasificación , Fisura Anal/tratamiento farmacológico , Fisura Anal/terapia , Administración Tópica , Diltiazem/administración & dosificación , Diltiazem/uso terapéutico , Estudios de Seguimiento , Nitroglicerina/administración & dosificación , Nitroglicerina/uso terapéutico , Procedimientos Quirúrgicos del Sistema Digestivo/métodos , Resultado del Tratamiento , Toxinas Botulínicas/administración & dosificación , Toxinas Botulínicas/uso terapéuticoRESUMEN
En este estudio se evaluó la eficacia del atenolol y diltiazen en pacientes digitalizados que acudieron a la consulta de cardiología del Hospital Universitario "Antonio María Pineda" con fibrilación auricular crónica y respuesta ventricular rápida en el lapso comprendido Agosto 2000 - Agosto 2001. Se realizó un estudio clínico controlado doble ciego y se constituyeron dos grupos en forma aleatoria de diez pacientes cada uno. Los criterios de inclusión fueron: diferentes sexos, edad entre 40-80 años, EKG con fibrilación auricular crónica con respuesta ventricular rápida y valores normales de urea creatinina, enzimas hepáticas, pruebas de funcionalismo tiroideo, digoxinemia y electrolitos séricos (Na, K, Ca, Mg). Las dosis de atenolol y diltiazem fueron de 50 mg al día y 60 más dos veces al día respectivamente. En el grupo de pacientes que recibió diltiazem se observó que la reducción de la frecuencia cardíaca mínima y máxima, así como el aumento de la fracción de eyección del ventrículo izquierdo fueron estadísticamente significativas con el valor de P= 0.005; P= 0,001 y P= 0.014 respectivamente. En el grupo de pacientes que recibió atenolol se observó que sólo el descenso de la frecuencia cardíaca máxima fue estadísticamente significativo (P= 0.029). Queda demostrado que la combinación diltiazem-digoxina en nuestro grupo de pacientes es más eficaz que atenolol-digoxina en controlar la FA crónica con respuesta ventricular rápida, así como mejorar la fracción de eyección determinada por ecocardiografía.
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Humanos , Masculino , Femenino , Persona de Mediana Edad , Fibrilación Atrial , Atenolol/uso terapéutico , Digoxina , Diltiazem/uso terapéutico , Cardiología , VenezuelaRESUMEN
OBJECTIVE: To evaluate the impact of the use, prior to the procedure, of injectable diltiazem to prevent complications. METHODS: Between September 2000 and July 2001, 50 patients underwent transradial coronary angiography and were randomized to receive placebo (GI) or diltiazem (GII) through a catheter inserted into the radial artery. All patients received isosorbide mononitrate. Ultrasound analyses of the radial artery were performed before examination, 30 minutes afterwards, and 7 days afterwards to evaluate the flow, the diameter, and the artery output. RESULTS: The radial artery diameter of GI was 2.4d +/- 0.5 mm before the procedure and 2.3 +/- 0.5 mm after 30 minutes (NS), whereas in GII the diameter was 2.2 +/- 0.3 mm before the examination and +/- 2.5 0.4 mm 30 minutes after it (P<0.001). Radial artery output in group 1 was 7.3 +/- 5.l2 mL/min before the examination and 6.1 +/- 3.5 mL/min 30 minutes after the examination (NS), and GII had an increase of 5.9 +/- 2.5 mL/min before examination to 9.05 +/- 7.78 mL/min after the examination (P=0.04). Complications (spasm, occlusion, and partial obstruction) occurred in 4 patients (17.4%) in GI and did not occur in GII (P=0.04). CONCLUSION: The study suggests a decrease in vascular complications through the transradial access for coronary angiography with the use of diltiazem as an antispasmodic drug, resulting in the significant increase in the diameter of the radial artery and radial artery output.
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Enfermedades Cardiovasculares/prevención & control , Angiografía Coronaria/efectos adversos , Diltiazem/uso terapéutico , Parasimpatolíticos/uso terapéutico , Arteria Radial/efectos de los fármacos , Angiografía Coronaria/métodos , Diuréticos Osmóticos/farmacología , Método Doble Ciego , Quimioterapia Combinada , Femenino , Humanos , Isosorbida/farmacología , Masculino , Persona de Mediana Edad , Arteria Radial/anatomía & histología , Arteria Radial/fisiologíaRESUMEN
OBJECTIVE: Antihypertensive therapy with thiazides decreases coronary events in elderly patients. However, the influence of diuretics on myocardial ischemia has not been fully investigated. The aim of this study was to compare the effect of chlorthalidone and diltiazem on myocardial ischemia. METHODS: Following a randomized, double-blind, crossover protocol, we studied 15 elderly hypertensive patients aged 73.6+/-4.6 years with myocardial ischemia. All patients had angiographically documented coronary artery disease. We measured patients using 48- hour ambulatory electrocardiogram monitoring and exercise testing. After a 2-week period using placebo, patients received chlorthalidone or diltiazem for 4 weeks. RESULTS: Both treatments lowered systolic and diastolic blood pressures. The number of ischemic episodes on ambulatory electrocardiogram recordings was reduced with the use of chlorthalidone (2.5+/-3.8) and diltiazem (3.2+/-4.2) when compared with placebo (7.9+/-8.8; p<0.05). The total duration of ischemic episodes was reduced in both treatments when compared with placebo (chlorthalidone: 19.2+/-31.9min; diltiazem: 19.3+/-29.6min; placebo: 46.1+/-55.3min; p<0.05). CONCLUSION: In elderly hypertensive patients with coronary artery disease, chlorthalidone reduced myocardial ischemia similarly to diltiazem. This result is consistent with epidemiological studies and suggests that reduction of arterial blood pressure with thiazide therapy plays an important role in decreasing myocardial ischemia.