Influence of 3 calcium channel blockers on gingival overgrowth in a population of severe refractory hypertensive patients.

OBJECTIVE: The aim of the current study was to assess the association between 3 different calcium channel blockers (CCBs) (nifedipine, amlodipine and felodipine) and gingival overgrowth in patients with a diagnosis of severe refractory hypertension. METHODS: One hundred and sixty-two patients with severe refractory hypertension, taking CCBs, were selected. Gingival overgrowth was graded and periodontal measurements were recorded (probing pocket depth, clinical attachment level, plaque index and bleeding on probing). Unconditional multivariable binary logistic regression analyses were performed to assess the association between CCB intake and gingival overgrowth after adjusting for potential confounders. RESULTS: Of the 162 patients, 26 (16.0%) were current smokers and 101 (62.3%) were females. The mean age (SD) was 54.1 (8.5) years and the median age (range) 52.5 (39-78) years. Gingival overgrowth was observed in 55 patients (34.0%). Nifedipine was the most common medication (35.2%; 57 of 162). The results of multiple binary logistic regression showed statistically significant associations between CCB intake (exposure) and gingival overgrowth (outcome) after adjusting for the variables treatment time with antihypertensive and plaque index. Patients with gingival overgrowth were 2.5 (odds ratio = 2.46; 95% confidence interval: 1.04-5.82) and 4.0 (odds ratio = 3.90; 95% confidence interval: 1.47-10.35) times more likely to be taking nifedipine and amlodipine, respectively, than patients without gingival overgrowth. On the other hand, this significant association was not observed for felodipine. CONCLUSION: Nifedipine and amlodipine, but not felodipine, were associated with gingival overgrowth in patients with severe refractory hypertension.

Evaluation of perineal muscle strength in the first trimester of pregnancy / Avaliação da força muscular perineal no primeiro trimestre da gestação / Evaluación de la fuerza muscular perineal en el primer trimestre del embarazo

OBJECTIVES: to analyze the Pelvic Floor Muscle Strength (PFMS) of pregnant women with one or more vaginal or cesarean deliveries; to compare the PFMS of these with pregnant women with the PFMS of primiparous women. METHODS: cross-sectional study with women up to 12 weeks pregnant, performed in Itapecerica da Serra, São Paulo state, from December 2012 to May 2013. The sample consisted of 110 pregnant women with one or more vaginal deliveries or cesarean sections and 110 primigravidae. The PFMS was evaluated by perineometry (Peritron(tm)) and vaginal digital palpation (modified Oxford scale). RESULTS: the average PFMS in pregnant women with a history of vaginal delivery or cesarean section was 33.4 (SD=21.2) cmH2O. From the Oxford scale, 75.4% of the pregnant women with previous vaginal or cesarean deliveries presented grade ≤ 2, and 5.5% grade ≥ 4; among the primiparae, 39.9% presented grade ≤ 2, and 50.9% grade ≥ 4, with a statistically significant difference (p<0.001). From the perineometry, there was no statistically significant difference between the PFMS and age, type of delivery, parity, body mass index, and genitourinary tract symptoms, however, there was a statistically significant difference between the pregnant women with and without a history of episiotomy (p=0.04). In the palpation, none of the variables showed a statistically significant difference. CONCLUSION: pregnancy and childbirth can reduce the PFMS. .

OBJETIVOS: analisar a força muscular do assoalho pélvico de gestantes com um ou mais partos normais ou cesarianas; comparar a a força muscular do assoalho pélvico dessas gestantes com a de primigestas. MÉTODO: estudo transversal com gestantes até 12 semanas de gravidez, realizado em Itapecerica da Serra, SP, de dezembro de 2012 a maio de 2013. A amostra foi composta por 110 gestantes, com um ou mais partos normais ou cesarianas e 110 primigestas. A força muscular do assoalho pélvico foi avaliada pela perineometria e palpação digital vaginal (Escala de Oxford modificada). RESULTADOS: a média da força muscular do assoalho pélvico em gestantes com antecedentes de parto normal ou cesariana foi 33,4 (desvio-padrão=21,2) cmH2O. Pela escala de Oxford, 75,4% das gestantes com partos ou cesarianas anteriores apresentaram grau ≤2 e 5,5%, grau ≥4; entre as primigestas, 39,9% apresentaram grau ≤2 e 50,9%, grau ≥4, com diferença estatisticamente significante (p<0,001). Pela perineometria, não houve diferença estatisticamente significante entre a força muscular do assoalho pélvico e idade, tipo de parto, paridade, índice de massa corpórea e sintomas do trato geniturinário, mas houve entre as gestantes com e sem antecedente de episiotomia (p=0,04). Na palpação, nenhuma das variáveis mostrou diferença estatisticamente significante. CONCLUSÃO: a gravidez e o parto podem reduzir a força muscular do assoalho pélvico. .

OBJETIVOS: analizar la Fuerza Muscular del Suelo Pélvico (FMSP) de embarazadas con uno o más partos normales o cesáreas; comparar la FMSP de estas embarazadas con la FMSP de primigestas. MÉTODO: estudio transversal con embarazadas hasta 12 semanas de embarazo, realizado en Itapecerica de la Serra, SP, de diciembre de 2012 a mayo de 2013. La muestra fue de 110 embarazadas con uno o más partos normales o cesáreas y 110 primigestas. La FMSP fue evaluada por la perineometría (Peritron(tm)) y palpación digital vaginal (escala de Oxford modificada). RESULTADOS: el promedio de la FMSP en embarazadas con antecedentes de parto normal o cesárea fue 33,4 (de=21,2) cmH2O. Por la escala de Oxford, 75,4% de las embarazadas con partos o cesáreas anteriores presentaron grado ≤ 2 y 5,5%, grado ≥ 4; entre las primigestas, 39,9% presentaron grado ≤ 2 y 50,9%, grado ≥ 4, con diferencia estadísticamente significativa (p<0,001). Por la perineometría, no hubo diferencia estadísticamente significativa entre la FMSP y edad, tipo de parto, número de partos anteriores, índice de masa corporal y síntomas del tracto genitourinario, pero hubo entre las embarazadas con y sin antecedente de episiotomía (p=0,04). En la palpación, ninguna de las variables mostró diferencia estadísticamente significativa. CONCLUSIÓN: el embarazo y el parto pueden reducir la FMSP. .

Design and optimization of self-microemulsifying drug delivery system (SMEDDS) of felodipine for chronotherapeutic application

The objective of this research work was to design, develop and optimize the self micro-emulsifying drug delivery system (SMEDDS) of Felodipine (FL) filled in hard gelatine capsule coated with polymer in order to achieve rapid drug release after a desired time lag in the management of hypertension. Microemulsion is composed of a FL, Lauroglycol FCC, Transcutol P and Cremophor EL. The optimum surfactant to co-surfactant ratio was found to be 2:1. The resultant microemulsions have a particle size in the range of 65-85 nm and zeta potential value of -13.71 mV. FL release was adequately adjusted by using pH independent polymer i.e. ethyl cellulose along with dibutyl phthalate as plasticizer. Influence of formulation variables like viscosity of polymer, type of plasticizer and percent coating weight gain was investigated to characterize the time lag. The developed formulation of FL SMEDDS capsules coated with ethyl cellulose showed time lag of 5-7 h which is desirable for chronotherapeutic application.

O objetivo desse trabalho de pesquisa foi planejar, desenvolver e otimizar sistema de liberação de fármaco auto-microemulsificante(SMEDDS) de felodipino (FL) em cápsulas de gelatina dura revestidas com polímero, a fim de obter liberação rápida após tempo desejado no manejo da hipertensão. A microemulsão é composta de FL, lauroglilcol FCC, Transcutol P e Cremophor EL. A proporção ótima de tensoativo e de co-tensoativo foi de 2:1. As microemulsões resultantes têm tamanho de partícula na faixa de 65-85 nm com potencial zeta de -13,71 mV. A liberação de FL foi ajustada adequadamente, utilizando-se polímero independente de pH, como etilcelulose com ftalato de dibutila como plastificante. A influência das variáveis da formulação, como viscosidade do polímero, tipo de plastificante e ganho percentual de peso do revestimento foi investigada para caracterizar o intervalo de tempo de liberação. A formulação de cápsulas de FL SMEDDS revestidas com etilcelulose mostrou intervalo de tempo de liberação de 5 a 7 horas, o que é desejável para uma aplicação cronoterapêutica.

Enhancement of felodipine dissolution rate through its incorporation into Eudragit® E-PHB polymeric microparticles: in vitro characterization and investigation of absorption in rats.

In this study, felodipine was incorporated into microparticles prepared with Eudragit® E and it blended with poly(3-hydroxybutyrate) (PHB) using the emulsion-solvent evaporation technique, with the aim of improving the dissolution rate of the drug. The formulation prepared with Eudragit® E showed irregular and fragmented microparticles, with a loading efficiency (LE) of 82.6%. When the microparticles were prepared with a blend of Eudragit® E and PHB, they had a spherical form with a LE of 103.9%. X-ray diffraction and differential thermal analysis indicated a reduction in the crystallinity of felodipine after its incorporation into the microparticles, which caused a significant increase in the felodipine dissolution rate. An investigation into the absorption in rats was carried out using high-performance liquid chromatography analysis of the blood collected 20 and 60 min after the animals were administered felodipine [30 mg/Kg, orally (p.o.)] or felodipine microparticles (30 mg/Kg, p.o.). Animals that were given felodipine showed mean plasmatic levels of 0.0125 (±0.00156) and 0.0240 (±0.0069) µg mL(-1) after 20 and 60 min, respectively, whereas animals that received microparticles containing felodipine showed respective mean plasmatic levels of 0.0651 (±0.0120) and 0.0369 (±0.0145) µg mL(-1) . Our data suggest that the incorporation into microparticles significantly enhanced the release of felodipine, improving its absorption in rats.

Effect of felodipine on myocardial and renal injury induced by aldosterone-high salt hypertension in uninephrectomized rats.

It has been recently shown that calcium channel blockers might have a protective effect on cardiac fibrogenesis induced by aldosterone. The objective of this study was to evaluate the protective effect of felodipine, a dihydropyridine calcium channel blocker, against heart and kidney damage caused by aldosterone-high sodium intake in uninephrectomized rats. Wistar rats were divided into three groups: CNEP (uninephrectomized + 1% NaCl in the drinking water, N = 9); ALDO (same as CNEP group plus continuous infusion of 0.75 microg/h aldosterone, N = 12); ALDOF (same as ALDO group plus 30 mg*kg(-1)*day(-1) felodipine in the drinking water, N = 10). All results were compared with those of age-matched, untreated rats (CTL group, N = 10). After 6 weeks, tail cuff blood pressure was recorded and the rats were killed for histological analysis. Blood pressure (mmHg) was significantly elevated (P < 0.05) in ALDO (180 +/- 20) and ALDOF (168 +/- 13) compared to CTL (123 +/- 12) and CNEP (134 +/- 13). Heart damage (lesion scores - median and interquartile range) was 7.0 (5.5-8.0) in ALDO and was fully prevented in ALDOF (1.5; 1.0-2.0). Also, left ventricular collagen volume fraction (%) in ALDOF (2.9 +/- 0.5) was similar to CTL (2.9 +/- 0.5) and CNEP (3.4 +/- 0.4) and decreased compared to ALDO (5.1 +/- 1.6). Felodipine partially prevented kidney injury since the damage score for ALDOF (2.0; 2.0-3.0) was significantly decreased compared to ALDO (7.5; 4.0-10.5), although higher than CTL (null score). Felodipine has a protective effect on the myocardium and kidney as evidenced by decreased perivascular inflammation, myocardial necrosis and fibrosis.

Effect of felodipine on myocardial and renal injury induced by aldosterone-high salt hypertension in uninephrectomized rats

It has been recently shown that calcium channel blockers might have a protective effect on cardiac fibrogenesis induced by aldosterone. The objective of this study was to evaluate the protective effect of felodipine, a dihydropyridine calcium channel blocker, against heart and kidney damage caused by aldosterone-high sodium intake in uninephrectomized rats. Wistar rats were divided into three groups: CNEP (uninephrectomized + 1 percent NaCl in the drinking water, N = 9); ALDO (same as CNEP group plus continuous infusion of 0.75 µg/h aldosterone, N = 12); ALDOF (same as ALDO group plus 30 mg·kg-1·day-1 felodipine in the drinking water, N = 10). All results were compared with those of age-matched, untreated rats (CTL group, N = 10). After 6 weeks, tail cuff blood pressure was recorded and the rats were killed for histological analysis. Blood pressure (mmHg) was significantly elevated (P < 0.05) in ALDO (180 ± 20) and ALDOF (168 ± 13) compared to CTL (123 ± 12) and CNEP (134 ± 13). Heart damage (lesion scores - median and interquartile range) was 7.0 (5.5-8.0) in ALDO and was fully prevented in ALDOF (1.5; 1.0-2.0). Also, left ventricular collagen volume fraction ( percent) in ALDOF (2.9 ± 0.5) was similar to CTL (2.9 ± 0.5) and CNEP (3.4 ± 0.4) and decreased compared to ALDO (5.1 ± 1.6). Felodipine partially prevented kidney injury since the damage score for ALDOF (2.0; 2.0-3.0) was significantly decreased compared to ALDO (7.5; 4.0-10.5), although higher than CTL (null score). Felodipine has a protective effect on the myocardium and kidney as evidenced by decreased perivascular inflammation, myocardial necrosis and fibrosis.

Photophysics and photochemical studies of 1,4-dihydropyridine derivatives.

The absorption and fluorescence properties of nifedipine (NPDHP), felodipine (CPDHP) and a series of structurally related 1,4-dihydropyridines were studied in aqueous solution and organic solvents of different properties. The absorption and fluorescence spectra were found to depend on the chemical nature of the substituents at the position 4 of the 1,4-dihydropyridine ring (DHP) and on solvent properties. In aqueous solution, the fluorescence spectra of 4-phenyl substituted compounds are blue-shifted with respect to the alkyl substituted compounds. The more fluorescent compound is CPDHP. Nifedipine is not fluorescent. All compounds, with the exception of CPDHP, present monoexponential fluorescence decay with very short lifetime (0.2-0.4 ns). CPDHP showed a biexponential emission decay with a long-lived component of 1.7 ns; this behavior is explained in terms of different conformers because of the hindered rotation of the phenyl group by the ortho-substitution. Analysis of the solvent effect on the maximum of the absorption spectrum by using the linear solvent-energy relation solvato-chromic equation indicates the redshifts are influenced by the polarizability, hydrogen bonding ability and the hydrogen bond acceptance of the solvent. Whereas, the fluorescence characteristics (spectra, quantum yields and lifetimes) are sensitive to the polarizabilty and hydrogen bond ability of the solvents. Photo-decomposition of nifedipine is dependent on the solvent properties. Faster decomposition rates were obtained in nonprotic solvents. The 4-carboxylic derivative goes to decarboxylation. Under similar conditions, the other DHP compounds did not show appreciable photodecomposition.

Felodipine quantification in human plasma by high-performance liquid chromatography coupled to tandem mass spectrometry.

A rapid, sensitive, robust and specific method was developed for the determination and quantitation of felodipine, in human blood plasma by liquid chromatography coupled with tandem mass spectrometry using nimodipine as internal standard. Felodipine was extracted from 0.5 mL human plasma by use of a liquid/liquid procedure using diethyl ether/hexane (80/20, v/v) as eluent. The method included a chromatographic run of 5 min using a C(18) analytical column (100 mm x 4.6 mm i.d.) and the calibration curve was linear over the range from 0.02 to 10 ng mL(-1) (r(2) > 0.994). The between-run precision, determined as relative standard deviation of replicate quality controls, was 5.7% (0.06 ng mL(-1)), 7.1% (0.6 ng mL(-1)) and 6.8% (7.5 ng mL(-1)). The between-run accuracy was +/- 0.0, 2.1 and 3.1% for the above-mentioned concentrations, respectively.

Oxidation of Hantzsch 1,4-dihydropyridines of pharmacological significance by electrogenerated superoxide.

PURPOSE: To study the reaction of a series of Hantzsch dihydropyridines with pharmacological significance such as, nifedipine, nitrendipine, nisoldipine, nimodipine, isradipine and felodipine, with electrogenerated superoxide in order to identify products and postulate a mechanism. METHODS: The final pyridine derivatives were separated and identified by gas chromatography/mass spectrometry (GC-MS). The intermediates, anion dihydropyridine and the HO2*/HO2- species, were observed from voltammetric studies and controlled potential electrolysis was used to electrogenerate O2*-. RESULTS: The current work reveals that electrogenerated superoxide can quantitatively oxidize Hantzsch dihydropyridines to produce the corresponding aromatized pyridine derivatives. CONCLUSIONS: Our results indicate that the aromatization of Hantzsch dihydropyridines by superoxide is initiated by proton transfer from the N1-position on the 1,4-dihydropyridine ring to give the corresponding anion dihydropyridine, which readily undergoes further homogeneous oxidations to provide the final aromatized products. The oxidation of the anionic species of the dihydropyridine is more easily oxidized than the parent compound.

Reduction in diastolic blood pressure and cardiovascular mortality in nondiabetic hypertensive patients. A reanalysis of the HOT study.

OBJECTIVE: To use published Hypertension Optimal Treatment (HOT) Study data to evaluate changes in cardiovascular mortality in nondiabetic hypertensive patients according to the degree of reduction in their diastolic blood pressure. METHODS: In the HOT Study, 18,700 patients from various centers were allocated at random to groups having different objectives of for diastolic blood pressure:

Reduçäo da pressäo arterial diastólica e mortalidade cardiovascular em hipertensos näo diabéticos. Uma reanálise do Hot-Study / Reduction in diastolic blood pressure and cardiovascular mortality in nondiabetic hypertensive patients. A reanalysis of the HOT study

OBJECTIVE: To use published Hypertension Optimal Treatment (HOT) Study data to evaluate changes in cardiovascular mortality in nondiabetic hypertensive patients according to the degree of reduction in their diastolic blood pressure. METHODS: In the HOT Study, 18,700 patients from various centers were allocated at random to groups having different objectives of for diastolic blood pressure: <=90 (n=6264); <=85 (n=6264); <=80mmHg (n=6262). Felodipine was the basic drug used. Other antihypertensive drugs were administered in a sequential manner, aiming at the objectives of diastolic blood pressure reduction. RESULTS: The group of nondiabetic hypertensive subjects with diastolic pressure<=80mmHg had a cardiovascular mortality ratio of 4.1/1000 patients/year, 35.5 percent higher than the group with diastolic pressure <=90mmHg (cardiovascular mortality ratio, 3.1/1000 patients/year). In contrast, diabetic patients allocated to the diastolic pressure objective group of <=80mmHg had a 66.7 percent reduction in cardiovascular mortality (3.7/1000 patients/year) when compared with the diastolic pressure group of <=90mmHg (cardiovascular mortality ratio, 11.1/1000 patients/year). CONCLUSION: The results indicate that in hypertensive diabetic patients reduction in diastolic blood pressure to levels <=80mmHg decreases the risk of fatal cardiovascular events. It remains necessary to define the level of diastolic blood pressure <=90mmHg at which maximal reduction in cardiovascular mortality is obtained for nondiabetics

Effects of 3-chloro-phenyl-1,4-dihydropyridine derivatives on Trypanosome cruzi epimastigotes.

A series of 3-chloro-phenyl-1,4-dihydropyridine derivatives produced different degrees of inhibition of parasite growth and respiration on clone Brener, LQ and Tulahuen strains of Trypanosome cruzi epimastigotes. Respiratory chain inhibition appears to be a posible determinant of the trypanosomicidal activity of this compounds. No difference in the action of these derivatives was found among the different parasite strains. For comparative purposes, the inhibitory effects of felodipine and nicardipine are also reported. A good correlation between toxic effects and the easiness of oxidation of the dihydripyridine ring was found. The presence of a fused ring on the dihydropyridine moiety significantly diminished the inhibitory effects.

Nuevos estudios multicéntricos en hipertensión arterial / New multicentric studies in arterial hypertension

Prospective, randomized and long term multicentric studies, published since 1988, on the effects of pharmacological or non pharmacological treatment of hypertension are analyzed. Former studies, performed between 1967 and 1987, are devoted, in chronological order, to special populations or to forms of hypertension not sufficiently studied previously (elders and isolated systolic hypertension), using classical pharmacological treatments such as diuretics and beta blockers. Their results confirm the reduction in mortality obtained using such therapies. Ensuing studies, focused on the analysis of new drugs such as calcium antagonists and angiotensin converting enzyme inhibitors, also demonstrated a reduction in cardiovascular risk, even in severely damaged populations. Thereafter, meta analysis of new pharmacological treatments and of non pharmacological therapies such as sodium restriction, weight reduction, avoidance of alcohol intake, calcium and potassium supplementation have appeared. These studies have emphasized the importance of prevention through changes in lifestyles. Their positive, although modest results, encourage the assessment of long term preventive and therapeutic measures in hypertension

Hypertension optimal treatment (HOT) study

O "Hypertension Optimal Treatment (HOT) Study" é um grande "trial" multicêntrico, randomizado, prospectivo (com desenho PROBE), envolvendo cerca de 19.000 pacientes hipertensos leves a moderados, em 26 países, que objetiva estabelecer o nível ótimo da pressão arterial, comparando morbidade e mortalidade cardiovasculares em três grupos-alvo de pressão diastólica (80, 85 e 90 mmHg). As drogas de escolha foram felodipina, um inibidor da ECA, betabloqueador e hidroclorotiazida, sendo também observada a eficácia do ácido acetilsalicílico sobre morbidade e mortalidade cardiovasculares "versus" placebo. Os dados obtidos em um ano de Estudo HOT indicam que o tratamento com felodipina isoladamente ou em combinação com outras drogas é muito eficaz e bem tolerado.

Felodipina versus nifedipina en el tratamiento de la crisis hipertensiva / Felodipine vs nifedipine in treatment of hypertensive crisis

Comparar la eficacia de la felodipina un calcio antagonista en el tratamiento de la crisis hipertensiva con una terapia de referencia, la nifedipina. Cincuenta y cuatro pacientes con edades comprendidas entre 30 y 80 años de edad que consultaron a la sala de emergencia con cifras tensionales diastólicas mayores de 110 mmHg a los cuales se les administro por método ciego simple una tableta de felodipina masticada o el contenido de una cápsula de nifedipina sublingual. Tanto felodipina como nifedipina fueron efectivos para disminuir las cifras tensionales, no se observaron diferencias significativas entre los medicamentos para este parámetro. La felodipina es al menos tan efectiva como la nifedipina para el tratamiento de las crisis hipertensivas, ambos son bien tolerados

Estudo multicêntrico comparativo entre felodipina e captopril como monoterapia em pacientes com hipertensäo leve e moderada / Comparative multicenter study between felodipine and captopril as monotherapy in hypertensive patients

Comparamos a eficácia antihipertensiva e a tolerabilidade da Felodipina com o Captopril. Estudamos pacientes que após quatro semanas de placebo (PAD entre 95 e 110mmHg), receberam por quatro semanas de maneira duplo cega Felodipina 5mg/dia (n=43) ou Captopril 50mg/dia (n=39). Nos dois grupos houve queda progressiva da pressäo (diferenças significativas em relaçäo ao placebo). Näo houve diferenças entre as duas drogas quanto a pressäo e a freqüência cardíaca. Os efeitos adversos foram discretos. Concluimos que Felodipina (5mg/dia) e Captopril (50mg/dia) säo regimes terapêuticos igualmente eficazes como monoterapia no controle da hipertensäo leve/moderada, tendo poucos efeitos colaterais e com a vantagem da Felodipina poder ser administrada em dose única diária.

[Felodipine in the treatment of essential arterial hypertension in elderly patients]. / Felodipino en el tratamiento de la hipertensión arterial esencial de adultos mayores.

BACKGROUND: Felodipine is a calcium channel inhibitor with high vascular selectivity. AIM: To study the effectiveness of felodipine in the treatment of essential hypertension in subjects older than 64 years old. PATIENTS AND OUTCOME: Fifty subjects were studied. After a washout period of four weeks, subjects received a placebo for two weeks followed by the active drug given in an initial dose of 5 mg/day, adjusted to 10 and 20 mg every 21 days if normal blood pressure levels were not attained. RESULTS: Compared to the placebo period, Felodipine treatment reduced blood pressure from 173 +/- 7.5/102 +/- 3.3 mm Hg to 158 +/- 6.3/91 +/- 4.2 mm Hg. There was no orthostatic reduction of blood pressure, and 87% of subjects attained systolic and diastolic pressure levels below 140 and 90 mm Hg respectively. Adverse reactions (edema, cephalea and flushing) were reported by 38% of subjects and in three, the drug was discontinued. There were no changes in laboratory parameters during the treatment period. Quality of life improved during treatment in the items of concentration, health status perception, mood, physical condition, depression, effects of hypertension on life events and initiative. CONCLUSIONS: Felodipine is effective in the treatment of elders with essential hypertension.

Acción antihipertensiva de felodipina: efectos en reposo, ejercicio y durante la actividad diaria / Antihypertensive action of felodipine: effects during rest, exertion and everyday activity

Se estudió la acción antihipertensiva de la felodipina, antagonista del transporte transmembranal del calcio de segunda generación, en un grupo de 20 pacientes portadores de hipertensión arterial primaria de grado leve y moderado. El estudio comprendió el control clínico periódico, la detección de efectos colaterales, y las variaciones de presión arterial, frecuencia cardíaca y, en las situaciones indicadas, parámetros derivados (producto presión por frecuencia, cargas sistólicas y diastólicas, curva circadiana), comparando contra placebo. Felodipina se administró en dosis de 2.5 a 5 mg cada 12 horas por un período de 8 a 12 semanas. La acción antihipertensiva se estudió en diferentes situaciones: reposo, posición sentada y de pie, actividad diaria, sueño y esfuerzo físico calibrado, por medio del control en consultorio, monitoreo de presión en las 24 hs. y prueba presora ergométrica. Felodipina redujo en forma significativa los valores tensionales, normalizándose en 85 por ciento de los pacientes, sin modificar la frecuencia cardíaca. Efectos colaterales (edema maleolar) aparecieron en 5 pacientes (25 por ciento), siendo de intensidad leve(AU)

Felodipino en el tratamiento de la hipertensión arterial esencial de adultos mayores / Felodipine in the treatment of essential arterial hypertension in elders

Felodipine is a calcium channel inhibitor with high vascular selectivity. To studu the effectiveness of felodipine in the treatment of essential hypertension in subjects older than 64 years old, 50 subjects were studied. After a washout period of 4 weeks, subjects received a placebo for 2 weeks followed by the active drug given in an initial dose of 5 mg/day, adjusted to 10 and 20 mg every 21 days if normal blood pressure levels were not attained. Compared to the placebo period, Felodipine treatment reduced blood pressure from 173ñ7.5/102ñ3.3 mm Hg to 158ñ6.3/91ñ4.4 mm Hg. There was no orthostatic reduction of blood pressure and 87 percent of subjects attained systolic and diastolic pressure levels below 140 and 90 mm Hg respectively. Adverse reactions (edema, cephalea and flushing) were reported by 38 percent of subjects and in 3, the drug was discontinued. There were no changes in laboratory parameters during the treatment period. Quality life improved during treatment in the items of concentration, health status perception, mood, physical condition, depression, effects of hypertension on life evets and initiative. Felodipine is effective in the treatment of elders with essential hypertension