RESUMEN
The aim of our study was to examine the use of pharmacological therapy and to evaluate the economical aspects of treating hypertension (HT) in elderly patients in Poland. Two hundred and sixty eight elderly persons (147 females, 121 males; mean age: 72.2 +/- 6.0 years) were selected from Polish population by stratified and cluster random sampling with quotas. BP measurement was performed 3 times every 2 minutes at respondents home. In the questionnaire, awareness of HT was assessed. Prevalence of hypertension among subjects aged 65 years and over by JNC VI criteria (SAP > or = 140 mm Hg, DAP > or = 90 mm Hg or hypotensive therapy) was 74%. Awareness of HT was equal to 61%. Eleven percent of all hypertensives were well controlled. Among hypertensives, 71% took prescribed antihypertensive drugs on a regular basis. Patients with HT were taking the following antihypertensive drugs: diuretics 16%, diuretics and reserpine 20%, beta-blockers 19%, ACE inhibitors 53%, calcium antagonists 30%, and other 3%. Newer drugs were prescribed in 7%, and multi-source (generic) products in 93%. The average cost of treatment with one drug was 147 PLN (37.5 USD) per year (newer drugs: 413 PLN; multi-source product 126 PLN). Assuming those data and number of elderly people in Poland (4.335 mln), we estimated that 3.208 mln of subjects have had hypertension according to JNC VI criteria. Only 1.957 mln of patients with HT have been detected and only 0.353 mln of hypertensives have been well controlled. The approximate global cost of antihypertensive drugs per year in elderly patients in Poland has been equal to 285 mln PLN (72.8 mln USD). In hypothetical situation with optimal (100%) detection and control of HT the global cost by the actual rate of regularity in taking drugs would increase to 569 mln PLN (145.3 mln USD). The prevalence of HT in elderly people in Poland is very high. In elderly hypertensives ACE inhibitors are used most often. More than 90% of prescribed drugs are multi-source products. An optimal improvement of HT detection and control would cause a two-fold augmentation of the costs of pharmacological therapy.
Asunto(s)
Antihipertensivos/uso terapéutico , Hipertensión/tratamiento farmacológico , Hipotensión/tratamiento farmacológico , Hipotensión/economía , Anciano , Antihipertensivos/economía , Economía Farmacéutica , Humanos , Hipertensión/epidemiología , Persona de Mediana Edad , Polonia/epidemiología , PrevalenciaRESUMEN
A series of twelve 2-methylbenzimidazole derivatives was prepared and their effect on the contraction of isolated rat tail artery, on beating rate and amplitude of isolated rat heart atria, on human blood platelet aggregation, and on blood pressure in urethane-anesthetized normotensive rats were tested. Numerical measures of pharmacodynamic activity were quantitatively related to the changes in chemical structure of the agents. Conclusions are drawn about the mechanism of pharmacodynamic action of 2-methylbenzimidazole derivatives, which is not executed directly through the adrenergic system. The further direction of synthesis is established basing on the results obtained.
Asunto(s)
Antihipertensivos/farmacología , Bencimidazoles/farmacología , Hemodinámica/efectos de los fármacos , Animales , Presión Sanguínea/efectos de los fármacos , Fenómenos Químicos , Química Física , Humanos , Técnicas In Vitro , Masculino , Agregación Plaquetaria/efectos de los fármacos , Ratas , Ratas Endogámicas , Relación Estructura-ActividadAsunto(s)
Adamantano/análogos & derivados , Antituberculosos/síntesis química , Bencimidazoles/síntesis química , Fármacos Cardiovasculares/síntesis química , Imidazoles/síntesis química , Adamantano/síntesis química , Adamantano/farmacología , Animales , Bencimidazoles/farmacología , Hemodinámica/efectos de los fármacos , Imidazoles/farmacología , Técnicas In Vitro , Masculino , Músculo Liso Vascular/efectos de los fármacos , Mycobacterium tuberculosis/efectos de los fármacos , Ratas , Ratas EndogámicasRESUMEN
The effects of newly synthetized pyrazinimidazolines on the contraction of isolated rat tail artery and on the chronotropic action of rat atria as well as the effects on blood pressure in anaesthetized rats were determined. The structure-activity relationships were studied, including standard imidazoline drugs. Starting from practically inactive derivatives the step-by-step structural modifications have been made resulting in markedly active chemical congeners, which were designed, synthetized and tested pharmacologically.
Asunto(s)
Hemodinámica/efectos de los fármacos , Imidazoles/farmacología , Receptores Adrenérgicos alfa/fisiología , Animales , Arterias/fisiología , Función Atrial , Presión Sanguínea/efectos de los fármacos , Fenómenos Químicos , Química , Frecuencia Cardíaca/efectos de los fármacos , Masculino , Ratas , Ratas Endogámicas , Receptores Adrenérgicos alfa/efectos de los fármacos , Relación Estructura-Actividad , Cola (estructura animal) , Vasoconstricción/efectos de los fármacosRESUMEN
Condensation reactions of 3-(1H-benzimidazole-2)propanoic acid (procodazol) with aromatic aldehydes were carried out resulting in lactam and acid derivatives. Basing on the spectral studies (MS, NMR) it was found that in the reaction the hydrogen atoms of the 3-methylene group of procodazol take part. 3-[2'-Acetoxyphenyl)methylene]-2,3-dihydro-1 H-pyrrole[1,2-a]benzimidazol-1-one (3c) was found to possess some analgetic properties.
Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Bencimidazoles/síntesis química , Animales , Bencimidazoles/farmacología , Fenómenos Químicos , Química , Ratas , Ratas Endogámicas , Tiempo de Reacción/efectos de los fármacos , Espectrofotometría UltravioletaRESUMEN
A group of new pyrazinylimidazolines was prepared and their effect on the contraction of isolated rat tail artery as well as their effect on blood pressure in urethane anesthetized normotensive rats were tested. The biological responses were compared to those elicited by standard imidazoline drugs and structure-activity relationships were analysed. The new chemical derivatives were subsequently synthetized and tested pharmacologically. Basing on the experimental results obtained and comparing these to the reported data on arylimidazolines the following suggestions have been put forward concerning the further modifications of alpha-adrenergically active pyrazinylimidazolines: 1) a distance of about 5 A should separate imidazoline nitrogen and pyrazine nucleus, 2) bond refractivity of the separating bridge should be above 5.33, 3) hydrophobicity of substituents in pyrazine ring must be possibly high.