Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole

Abstract The antihistamine and anticholinergic properties of mequitazine have been investigated and compared with those of clemizole. Both mequitazine and clemizole antagonized the effect of histamine in guinea-pig ileum competitively, the pA2 values calculated by Schild plot were 9.95 ± 0.44 for mequitazine and 10.54 ± 0.44 for clemizole. Mequitazine at 10−7 M produced a parallel shift of the dose-response curve to acetylcholine in the rat duodenum, clemizole and the lower doses of mequitazine failed to modify the effect of acetylcholine. The potency of mequitazine and clemizole as H1-histamine blockers is similar, but only mequitazine at highest concentration used showed anticholinergic a…

Effect of histamine and histamine analogues on human isolated myometrial strips.

1. The effect of histamine and histamine H1- and H2-receptor agonists on isolated myometrium strips of premenopausal women has been examined. The effect of acetylcholine was also determined. 2. Histamine, 2-pyridylethylamine, 4-methylhistamine and acetylcholine, but not dimaprit, produced a concentration-related contractile response in human isolated myometrial strips. Histamine also produced a further contraction in human isolated myometrial strips precontracted with KCl (55 mM). 3. The contractile response to histamine was antagonized by the histamine H1-receptor antagonist, clemizole (0.1 microM) but was potentiated by the histamine H2-receptor antagonist, ranitidine (10 microM). Clemizo…

Weight Gain Associated with Cinnarizine

OBJECTIVE: To report four cases of cinnarizine-induced weight gain. DATA SOURCES: Case reports from a local obesity center and review articles. DATA EXTRACTION: Data were abstracted from spontaneous comments made by patients to one of the authors, who was a doctor at the clinic, and reviewed by the remaining authors. DATA SYNTHESIS: We reviewed the cases of four women, aged 50–57 years without endocrine or metabolic pathologies, that showed weight gain associated with the intake of cinnarizine for one to two years. No other drugs usually were administered during the period in which the women gained weight, although in two cases cinnarizine was associated with dihydroergocristine in the same…

Nuevos lenguajes informáticos en la difusion de información sobre medicamentos

¿Se ha modificado el uso de antitérmicos tras la introducción de ibuprofeno a diferentes concentraciones?

Resumen: Introducción: Se analiza la utilización de antitérmicos en pediatría extrahospitalaria en España después de la aparición de medicamentos con 40 mg/ml de ibuprofeno. Pacientes y métodos: Estudio transversal, observacional y descriptivo en pacientes menores de 14 años con síndrome febril ya tratado, atendidos en Urgencias del Servicio de Pediatría del Consorcio Hospital General Universitario de Valencia entre noviembre del 2012 y enero del 2013. Resultados: De 217 niños, 144 estaban tratados con paracetamol o ibuprofeno, 69 recibían ambos fármacos, y uno paracetamol y metamizol. Hubo un 58,7% de exposiciones a paracetamol y un 40,9% a ibuprofeno. En el 63,2% de los casos el uso de an…

Ranitidine-Induced Confusion with Concomitant Morphine

Characteristics of histamine tachyphylaxis in rat uterine smooth muscle.

Objective and design: To study both the desensitisation induced by short-term exposure to histamine and the mechanism responsible in the isolated rat uterus.¶Material: Precontracted isolated uterus (37 mM KCl) from oestrogenised Wistar rats were used.¶Treatment: Repetitive responses to histamine (10–6, 10–5, 10–4, 10–3 M), dimaprit and clonidine (10–4 M) were tested at 15, 30, 45 and 105 min., with their modifications by (5 mg/ kg, 24 h before sacrifice) reserpine, 10–7 M propranolol, 10–8 M atropine, and 10–6 M indomethacin. Dose-response curves for adrenaline were carried out as standard protocol.¶Methods: In vitro techniques (de Jalon's solution, 31°C, carbogen, isotonic registration, re…

The effects of histamine on the isolated mouse uterus

1. A study is made of the contractile and relaxant effects, and mechanism of action, of histamine on isolated uterus from mice treated with diethylstilboestrol, employing acetylcholine and adrenaline as contractile and relaxant standard agents. 2. Concentration-response curves for histamine agonists were obtained in the absence and presence of selective histaminergic blocking drugs (clemizole, ranitidine and thioperamide) and indomethacin. A number of experiments were carried out in uterus from reserpinised mice. Concentration-response curves for acetylcholine and adrenaline were also obtained in the absence and presence of their selective antagonist (atropine and propranolol). 3. In isolat…

Farmacologia de la solifenacina

Departamento de Farmacologia. Facultad de Medicina y Odontologia. Universidad de Valencia. Valencia. Espana.Resumen.- Los antimuscarinicos son los farmacos de primera eleccion para el tratamiento del sindrome de vejiga hiperactiva y su relacion beneficio/riesgo depen-de en gran medida de la selectividad por los distintos subtipos de receptores muscarinicos. Solifenacina es el antimuscarinico que muestra mayor selectividad por los receptores M3 vesicales, lo que puede traducirse en una menor incidencia de reacciones adversas relacionadas con otros subtipos de receptor. Las vias metabolicas de los antimuscarinicos pueden influir en la eficacia y en la aparicion de interacciones. Solifenacina es …

Has the use of antipyretics been modified after the introduction of different concentrations of ibuprofen into the market?

Introduction: Due to the emergence of new pharmaceutical presentations of ibuprofen (40 mg/mL), an analysis was made on the use of antipyretics in paediatric outpatients in Spain. Patients and methods: A cross-sectional, observational, descriptive study was carried out on a sample of children under 14 years old with treated febrile syndrome, seen in the Emergency Room of the Hospital General Universitario de Valencia from November 2012 to January 2013. Results: Of the 217 children included, 144 were treated with paracetamol or ibuprofen, 69 received both drugs, and one received paracetamol and metamizol. There were 58.7% of exposures to paracetamol and 40.9% to ibuprofen. The parents decide…

Efecto del fosinopril sobre los niveles plasmáticos de fibrinógeno en hipertensos esenciales

Objetivo Valorar si fosinopril es capaz de reducir las cifras de fibrinogeno en pacientes con hipertension arterial esencial (HTA) y valorar la influencia de otros factores de riesgo cardiovascular. Metodos Hipertensos esenciales (PAD: 90-114; PAS: 140-180 mmHg) de cualquier sexo y edad superior a 30 anos sin contraindicaciones para el uso de fosinopril. Tres visitas con registro de presion arterial (PA) y fibrinogeno por nefelometria (basal, 3 meses, 6 meses). Tratamiento con fosinopril 20 mg/dia. Resultados Setenta y cinco pacientes (54,7 % mujeres); edad media: 59,8±10,4 anos; peso: 73,9±10,9 kg; IMC: 28,0 ± 3,8 kg/m2. Fosinopril disminuye significativamente la PA y el fibrinogeno plasma…

Vitamin K, and Anaphylactic Shock

Relevancia clínica de la selectividad de los inhibidores del cotransportador sodio-glucosa tipo 2

Selectivity is the property of a drug to preferentially bind to a biological structure. Most drugs can bind and stimulate or inhibit more than one system. Therefore, it is important that they are selective for the intended site and that the doses used do not have effects on other sites, which could provoke adverse reactions. Selectivity is assessed through in vitro experiments on organs or isolated cells. If the aim is to compare drugs, the experiment should be conducted in the same tissue and with the same design. Even so, the results cannot be directly extrapolated to clinical practice due to the influence of pharmacokinetic properties, which allow an adequate dose of the drug to reach th…

Relaxant effect of dopamine on the isolated rat uterus.

The effect of dopamine was studied on the isolated uterus of diethylstilboestrol-treated rats. Dopamine, at concentrations (10(7)-10(-4) M) produced a concentration-dependent relaxation in the K+-depolarized rat uterus. On a molar basis, dopamine was about 500 times less potent than adrenaline in relaxing the uterus, the maximum degree of relaxation obtained with both drugs was the same. Pretreatment of the rats with reserpine (5 mg/kg) did not produce any modification of the dose-response curve to dopamine. Similarly, cocaine (3 x 10(-6) M) failed to modify the relaxant effect of dopamine. The dopamine induced relaxation was inhibited by propranolol (10(-9)-10(-7) M) in a dose-dependent ma…

Mejores medicamentos para los niños: La iniciativa pediátrica europea cumple 5 años

h ( q d s s p r d Como consecuencia del «desastre de la talidomida», se hizo patente la necesidad de disponer de informacion sobre los efectos de los medicamentos en los ninos, pero transcurrieron casi 30 anos desde que en 1968 H. Shirkey calificara a los pacientes pediatricos como huerfanos terapeuticos hasta que los Estados iniciaron acciones efectivas para promover la investigacion de medicamentos pediatricos. El primer documento en Estados Unidos (Best Pharmaceuticals for Children Act) se aprobo en 1997 y el reglamento europeo 1901/2006 sobre uso de medicamentos en pediatria en diciembre del 2006. El reglamento entro en vigor en enero de 2007, pero algunos articulos se aplicaron mas tar…

Influence of hormonal treatment on the response of the rat isolated uterus to histamine and histamine receptor agonists.

The response of the isolated uterus to histamine and histamine agonists was investigated in progesterone- and oestrogen-treated rats. The uterine inhibitory responses to histamine and 4-methylhistamine (a histamine H2 receptor agonist) were similar in KCl-contracted uteri from progesterone- and oestrogen-treated rats. The histamine H1 receptor agonist, 2-pyridyl-ethylamine, produced a relaxant response only in progesterone dominant uterus. This was inhibited by the histamine H1 receptor antagonist. In the rat isolated uterus which was not preconstricted by KCl, neither histamine, 4-methylhistamine, nor 2-pyridyl-ethylamine produced any effect in the presence or absence of ranitidine. Raniti…

Medicines of high health and economic impact: The required balance between innovation and sustainability

Urinary albumin excretion and glomerular filtration rate across the spectrum of glucose abnormalities in essential hypertension.

The objective of this study was to assess the relationship between urinary albumin excretion (UAE) and GF across the spectrum of the glucose metabolism abnormalities in a large population of patients with hypertension. The Microaluminuria en Pacientes con Glucemia Basal Alterada (MAGAL) is a multicenter, cross-sectional study that was carried out by 1723 primary care physicians. A total of 6227 patients with essential hypertension (in three groups: [1] normal fasting glucose100 mg/dl, [2] impaired fasting glucoseor =100 to 126 mg/dl, and [3] type 2 diabetes) were analyzed in this substudy. GFR was estimated by using the Modification of Diet in Renal Disease (MDRD) abbreviated equation. A si…

[Adverse reactions to human papillomavirus vaccine in the Valencian Community (2007-2011)].

Introduction: In 2009, two cases of seizures in adolescents following quadrivalent human papillomavirus vaccine (qHPV) administration generated important media attention, and adversely affected public trust in this vaccine. Our objectives were to describe suspected adverse reactions (SARs) reported to the Pharmacovigilance Centre in the Valencian Community (PCVC) after administration of HPV vaccine, and to compare reporting rates of syncope and seizures following this vaccine with those of other vaccines administered to girls aged 13–15 years. Materials and methods: Descriptive study of SARs reported following administration of this vaccine to the PCVC between 2007 and 2011. Results: The cl…

Medicamentos de alto impacto sanitario y económico: el necesario equilibrio entre innovación y sostenibilidad

Effect of histamine on the longitudinal and circular muscle of the oestrogen dominated rat uterus.

The response of the longitudinal and circular myometrial strips to histamine was studied in oestrogen-treated rats. Histamine produced a dose-related inhibitory response in KCl-contracted longitudinal and circular uterine strips. Histamine was equipotent in producing the relaxant response but the maximal effect achieved in the longitudinal muscle was higher than the circular one. Ranitidine antagonized the histamine-induced relaxation with a similar dose ratio in both longitudinal and circular strips. Clemizole and reserpine treatment did not produce any modification of the dose-response curve to histamine. In the longitudinal and circular strips which were not preconstricted by KCl, neithe…

Fluticasone in mild to moderate atopic dermatitis relapse: A randomized controlled trial

Background: The long-term efficacy of corticosteroids to prevent atopic dermatitis (AD) relapses has partially been addressed in children. This study compared an intermittent dosing regimen of fluticasone propionate (FP) cream 0.05% with its vehicle base in reducing the risk of relapse in children with stabilized AD. Methods A randomized controlled, multicentric, double-blind trial was conducted. Children (2-10 years) with mild/moderate AD (exclusion criteria: > 30% affected body surface area and/or head) were enrolled into an Open-label Stabilization Phase (OSP) of up to 2 weeks on twice daily FP. Those who achieved treatment success entered the Double-blind Maintenance Phase (DMP). They w…

El diseño y las conclusiones del estudio ALLHAT

Adverse reactions to human papillomavirus vaccine in the Valencian Community (2007-2011)

Resumen: Introducción: En 2009, 2 casos de convulsiones en adolescentes tras la administración de la vacuna tetravalente frente al virus del papiloma humano (VPH) generaron impacto mediático y afectaron negativamente la confianza del público en esta vacuna.Nuestros objetivos fueron describir las sospechas de reacciones adversas (SRA) notificadas al Centro Autonómico de Farmacovigilancia de la Comunidad Valenciana (CAFCV) tras la administración de la vacuna frente al VPH y comparar la tasa de notificación de síncope y convulsiones de esta vacuna con la de otras vacunas administradas en adolescentes. Material y métodos: Estudio descriptivo de las notificaciones de SRA relacionadas con esta va…

The KARTAN study: a postmarketing assessment of Irbesartan in patients with hypertension.

An important purpose of postmarketing surveillance of drugs is to better characterize the safety profile of drug therapy in the clinical setting. Another goal is to confirm the effectiveness of these drugs in patients who are candidates for antihypertensive therapy and who may have been excluded from Phase III studies. Irbesartan is a long-acting angiotensin II-receptor blocker specific for the angiotensin 1-receptor subtype that, in clinical trials in patients with hypertension, reduces blood pressure.The KARTAN (this word was derived from the first and last syllables of Karvea [trademark of Bristol-Myers Squibb Group, Madrid, Spain] and irbesartan) study was designed to confirm and extend…

Pharmacological investigation into the effects of histamine and histamine analogues on guinea-pig and rat colon in vitro.

The effects of histamine and specific histamine agonists has been examined on isolated longitudinal colon strips of guinea-pig and rat. Histamine and 2-pyridyl-ethylamine but not 4 methylhistamine produced a concentration-related contractile response in the guinea-pig colon. The H1-antagonist clemizole antagonized competitively the effect of histamine but the H2-antagonist ranitidine did not modify the dose-response curve to histamine in the guinea-pig colon. Atropine, hexamethonium, prazosin and propranolol failed to modify the contractile response to histamine. Tone induced with KCl in guinea-pig isolated colon was not modified by histamine agonists even in tissues pretreated with clemizo…

Are the Adverse Drug Reactions of Amoxycillin and Amoxycillin-Clavulanic Acid Similar?

UNLABELLED In an attempt to assess the relative toxicity of amoxycillin and amoxycillin-clavulanic acid, we compared the adverse drug reactions reports collected using the spontaneous reporting system of a Regional Drug Surveillance Centre of Spain for both drugs between November 1986 and December 1992. During the 7-year period 1986-92, the 247 reports of amoxycillin-clavulanic acid represent twice the number of reports of amoxycillin alone, and the number of reports related with sales received concerning the association were higher than those concerning amoxycillin alone. The adverse effects classified as severe were quantitatively and qualitatively similar for both drugs and gastrointesti…

La actividad de la renina plasmática. Papel de la inhibición directa de la renina

Resumen La renina es la enzima encargada de transformar el angiotensinogeno en angiotensina I, primer paso en la activacion del sistema renina-angiotensina (SRA). La actividad de la renina plasmatica (ARP) mide la capacidad de la renina para producir angiotensina I a partir de angiotensinogeno, se expresa como concentracion de angiotensina I generada por unidad de tiempo (ng/ml/h) y se utiliza para valorar el grado de activacion del SRA. Hay relacion entre valores de ARP y enfermedad cardiovascular. Se ha descrito que valores de ARP alta se asocian con mayor incidencia de infarto agudo de miocardio, perdida de funcion renal, peor pronostico de la insuficiencia cardiaca y aumento de la morta…

Fármacos antihipertensivos en Atención Primaria

a hipertension arterial es un factor de riesgocardiovascular de elevada prevalencia quepuede afectar a alrededor de 8 millones deespanoles. Esta bien demostrado que inclusopequenas elevaciones de las cifras tensionalespor encima de lo que se considera normoten-sion (<140/90 mmHg) pueden incrementar deforma notable el riesgo de enfermedad corona-ria, accidente cerebrovascular (ACV), insuficien-cia cardiaca o insuficiencia renal, y que el trata-miento farmacologico de la hipertension reducela morbilidad y mortalidad cardiovascular.El diagnostico y seguimiento de los pacienteshipertensos se hace mayoritariamente en asis-tencia extrahospitalaria, y por ello la mayor par-te de las decisiones ter…

Papel actual de los diuréticos en el tratamiento de la hipertensión arterial

El grupo de los diureticos incluye las tiazidas y farmacos tiazida-like, los diureticos de asa y los ahorradores de potasio. Las tiazidas son los farmacos mas recomendados para el tratamiento inicial de la hiperpresion arterial esencial por razones economicas, su bajo coste, pero tambien por su eficacia y tolerabilidad tanto en monoterapia como en combinacion con otros antihipertensivos. El uso de tiazidas puede reducir la incidencia de ictus y de enfermedad coronaria como han demostrado numerosos ensayos clinicos, desde la decada de los sesenta hasta los mas recientes, como el ALLHAT. Hidroclorotiazida en dosis de 12,5-25 mg una vez al dia reduce la presion arterial en alrededor de la mita…

A prospective study of adverse drug reactions in hospitalized children

Aims There are few publications of adverse drug reactions (ADRs) among paediatric patients, though ADR incidence is usually stated to be higher during the first year of life and in male patients. We have carried out a prospective study to assess the extent, pattern and profile risk for ADRs in hospitalized patients between 1 and 24 months of age. Methods An intensive events monitoring scheme was used. A total of 512 successive admissions to two medical paediatric wards (47 beds) were analysed. The hospital records were screened daily during two periods (summer, 105 days and winter, 99 days), and adverse clinical events observed were recorded. Results A total of 282 events were detected; of …

Analgesic use for postoperative pain: differences arise when comparing departments of surgery

Purpose The goal of the study is to analyse whether the analgesic therapy of postoperative pain during the first 2 days after surgery differs among the different surgical departments. Methods Patients were randomly chosen from among all those who underwent elective surgery. Characteristics of analgesic treatment (drug, dosage, schedule) and pain intensity were determined at the postoperative anaesthetic care unit and in the first and second postoperative days on the ward. All comparisons were carried out by surgical departments. Results Six hundred and twenty-three patients from six surgical departments were studied. Analgesic treatment orders varied greatly among the different departments,…

Weight Gain Induced by Long-Term Propranolol Treatment

Isolated human chorionic vascular reactivity: Technical considerations for fresh preparations

1. 1. Sixty chorionic vascular rings from normal term placentas were immersed in an organ bath for isometric tension recording to study (A) the contractile response to 120 mM of potassium chloride (KCI) after adjustment and equilibration to 1–5 g of passive tension; and (B) the concentration-response curve to KCI after adjustment and equilibration to the optimal passive tension. 2. 2. Adjustment to 4 g of passive tension elicited the maximal (P<0.007) and the latest (P<0.006) KCl-induced contraction among arterial rings. Venous rings showed the greatest contraction when adjusted to 3 g, but the differences were not significant except when compared to 1 g of passive tension (P<0.03). 3. 3. T…

Antihistamínico-H1 camuflado y accidente de tráfico

Riesgo de interacciones farmacológicas por la coadministración de estatinas con fármacos metabolizados por la isoenzima 3A4 del citocromo P450: estudio epidemiológico, transversal y multicéntrico

Resumen Fundamento y objetivo Las estatinas son farmacos seguros, pero con un elevado riesgo de interacciones farmacologicas. El objetivo del estudio fue evaluar la prevalencia de interacciones potenciales en la isoenzima 3A4 del citocromo P450 (CYP3A4), en una amplia muestra de pacientes tratados con estatinas, y determinar los factores asociados, tanto del paciente como del medico prescriptor. Pacientes y metodo Estudio observacional, transversal, de base poblacional. Fueron seleccionados 7.880 sujetos en tratamiento con estatinas. Se recogieron datos referentes a los pacientes y a los 1.681 medicos participantes. Resultados Un 59% de los pacientes recibia estatinas metabolizadas por el C…

Effects of dopamine in isolated rat colon strips.

The aim of the present work is to investigate the effects of dopamine on isolated rat colon strips, and whether dopamine receptors are involved in these effects. Experiments on spontaneous motility and under potassium contraction were performed with dopamine and isoprenaline, both in the absence and presence of antagonists (distal colon strips, isotonic recording, Tyrode solution, 31 °C, 1 g of resting tension). At higher concentration (10–4mol/L), dopamine abolished spontaneous motility of the rat colon and this effect was not modified by antagonists. In isolated rat colon strips that were depolarized with potassium, dopamine produced concentration-dependent relaxation, without significant…

Interacciones farmacológicas de los fármacos antihipertensivos

A drug interaction is the quantitative or qualitative modification of the effect of a drug by the simultaneous or successive administration of a different one. Hypertensive patients, mainly the more elderly ones, frequently present concomitant diseases that require the administration of several medicines which facilitates the appearance of interactions. The lack of effectiveness of the antihypertensive treatment is a relatively frequent fact that sometimes is due to interactions of antihypertensive drugs with other treatments. It is difficult to determine the incidence of interactions, but it is related to the number of drugs administered simultaneously. Between 37 and 60% of hospital-admis…

Spanish Society of Hypertension position statement on the 2017 ACC/AHA hypertension guidelines

The American College of Cardiology (ACC) and the American Heart Association (AHA) have recently published their guidelines for the prevention, detection, evaluation, and management of hypertension in adults. The most controversial issue is the classification threshold at 130/80 mmHg, which will allow a large number of patients to be diagnosed as hypertensive who were previously considered normotensive. Blood pressure (BP) is considered normal (&lt;120 mmHg systolic and &lt;80 mmHg diastolic), elevated (120-129 and &lt;80 mmHg), stage 1 (130-139 or 80-89 mmHg), and stage 2 (≥140 or ≥90 mmHg). Out-of-office BP measurements are recommended to confirm the diagnosis of hypertension and for titra…

The Effects of Epinine on Arterial Blood Pressure and Regional Vascular Resistances in Anesthetized Rats

1. We carried out experiments in anesthetized rats to study the hemodynamic effects of intravenous injections of epinine. 2. Epinine (1-320 micrograms/kg) produced a biphasic effect on mean arterial blood pressure (n = 30). At doses lower than 40 micrograms/kg, arterial blood pressure decreased (by as much as 21.5 +/- 3.4%), though at higher doses it increased dose dependently (by as much as 73.2 +/- 14.5%). Epinine also produced bradicardia in a dose-dependent manner (by as much as 26.4 +/- 4.9%). Sulpiride (100 micrograms/kg) suppressed the hypotensive effect of epinine but did not change the hypertensive effect. In the presence of prazosin (1,000 micrograms/kg), arterial blood pressure r…

The lack of the effect of DA-1 and DA-2 dopamine agonists on the isolated guinea-pig atria.

1 The effects of dopamine and both DA-1 and DA-2 dopamine receptor agonists have been studied on the contractile force of electrically driven guinea-pig left atria and frequency of spontaneously beating right atria. 2 Pretreatment of animals with reserpine caused a parallel rightward shift of the concentration-response curve to dopamine of either preparation. 3 Propranolol, but not domperidone, shifted to the right the dose-response curve for the positive inotropic and chronotropic effects of dopamine. 4 Neither apomorphine, fenoldopam, bromocriptine nor piribedil had effects on the frequency and contractile force of the isolated guinea-pig atria. 5 These results suggest that DA-1 and DA-2 …

Histamine inhibits spontaneous activity of the uterus of the progesterone-treated rat

A prospective study of adverse drug reactions as a cause of admission to a paediatric hospital

1A total of 512 consecutive paediatric hospital admissions of children 2 years old or less were evaluated to assess the extent and pattern of admission caused by suspected adverse drug reactions (ADRs). The proportion of suspected ADRs related to hospital admissions was 4.3%. 2The organ-systems most commonly implicated were the central nervous system (40.5%), digestive system (16.7%), and skin and appendages (14.3%). Together, they accounted for 71.5% of admissions attributed to ADRs. The most common clinical manifestations inducing admission were convulsions (4 cases), dizziness (4), vomiting (3), and tremor, fever, itching and apnoea (2 cases each). 3The four classes of drugs most frequen…

Response to dopamine agonists of the rat isolated uterus.

1. Quinpirole did not produce any effect in isolated uterus from oestrogenized rats even when it is contracted by KCl (37 mM). 2. Fenoldopam produced a relaxant effect on rat isolated uterus contracted by KCl which was not significantly modified by SCH 23390. 3. Reserpine decreased the effect of the lowest doses of fenoldopam. In reserpinized rats, propranolol (10(-9), 10(-8), 10(-7) M) antagonized the effect of the lowest doses of fenoldopam and neither SCH 23390, sulpiride nor ranitidine modified the effect of fenoldopam. 4. The results confirm our previous finding that DA1-receptors are not functional in our preparation. The effect of fenoldopam was partially due to a catecholamine-relea…

Olmesartán: evidencia y práctica clínica

Resumen Olmesartan medoxomilo es un antagonista no peptidico del receptor AT1 de la angiotensina con afinidad superior a la de otros farmacos del grupo. Ha demostrado en numerosos ensayos clinicos su eficacia antihipertensiva y su buena tolerabilidad. Se ha comparado en ensayos clinicos con otros farmacos del grupo (azilsartan, candesartan, irbesartan, losartan y valsartan). En general, el efecto de olmesartan administrado por via oral, una sola vez al dia a dosis de entre 20 y 40 mg, ha sido superior en cuanto a la reduccion de cifras tensionales, se ha iniciado antes y ha persistido durante 24 h. Varios metaanalisis han confirmado estas ventajas de olmesartan. Hay algunos estudios que dem…

Diferencias y similitudes entre diuréticos

Resumen Los diureticos tiazidicos son los farmacos mas recomendados para el tratamiento inicial de la hipertension arterial, por su bajo coste, pero tambien por su eficacia y tolerabilidad tanto en monoterapia como en combinacion. Aunque el farmaco mas utilizado es la hidroclorotiazida existen argumentos a favor de su sustitucion por clortalidona. El uso de tiazidas reduce la incidencia de ictus y de enfermedad coronaria, como han demostrado numerosos ensayos clinicos. La combinacion de tiazidas con otros antihipertensivos aumenta su eficacia. El efecto adverso mas comun es la hipopotasemia, por lo que deben vigilarse los valores plasmaticos de potasio. Dado que muchos pacientes no alcanzan…

Interacciones medicamentosas. Nuevos aspectos

Se denomina interaccion farmacologica a la modificacion cuantitativa o cualitativa del efecto de un farmaco causada por la administracion simultanea o sucesiva de otro. La polimedicacion facilita la aparicion de interacciones cuyo resultado puede ser una reaccion adversa o la perdida de efecto terapeutico. La incidencia es dificil de determinar, pero se relaciona fundamentalmente con el numero de farmacos administrados conjuntamente al mismo paciente. Aunque es imposible recordar todas las interacciones de interes clinico, conocer su existencia y mecanismos de produccion ayuda a identificarlas y prevenirlas. Las que con mayor frecuencia causan problemas son las de tipo farmacocinetico, sobr…

Adverse drug reactions in children reported by means of the yellow card in Spain.

Abstract Objective: To analyze the case reports concerning children (14 years or younger) in the Spanish Pharmacovigilance System over a 10-year period (1982–1991). Findings: The study of 1419 reports of adverse drug reaction (9.8% of all those received) showed the most commonly involved organs and systems to be the skin, digestive tract, and nervous system (62.8%). The most commonly involved pharmacological groups were antibiotics, respiratory medications, and vaccines (69%). The absolute number of reports is higher in children between 1 and 4 years of age (37.9%). There were more reports among males than in females. Less than 5% of the reports notified directly life-threatening or fatal r…

¿Son los niños hipertensos españoles huérfanos terapéuticos?

Introducción: Según las guías, la hipertensión en los niños debe tratarse con los mismos fármacos usados en adultos ajustando las dosis al tamaño corporal. El término huérfano terapéutico se refiere a la falta de información sobre el uso de medicamentos en niños. El objetivo es investigar si el Vademécum Internacional (V-I) contiene información para el uso correcto de antihipertensivos en niños. Material y método: Revisión en el V-I de la posología pediátrica de antihipertensivos. Si existen varias especialidades para un fármaco se selecciona el del logotipo del Ministerio de Sanidad y Consumo más reciente. Si en una monografía no hay información, se revisan las de otras especialidades del …

Reactivity of isolated human chorionic vessels: analysis of some influencing variables

The aim of the study was to determine whether 24 h of cold storage of samples, mode of delivery, and gestational age influenced in vitro human chorionic vascular reactivity (35 arteries and 34 veins). The following groups were compared: (i) fresh versus 24-h cold-stored (4 °C in Krebs–Henseleit solution) chorionic vascular rings from normal term placentas, (ii) fresh chorionic vascular rings from normal term placentas obtained after vaginal delivery versus those obtained after elective caesarean section, and (iii) fresh chorionic vascular rings from normal term placentas versus those obtained from preterm deliveries. Isometric recording of the concentration–response curve to KCl (5–120 mM)…

Hipertensión al día en 6 preguntas. Curso precongreso SEH-LELHA Valencia 2016. Presentación

Studies of the spontaneous motility and the effect of histamine on isolated myometrial strips of the nonpregnant human uterus: the influence of various uterine abnormalities.

We investigated the spontaneous uterine activity of isolated corpus uteri myometrial strips from 30 patients with nonpathologic myometrium, 26 patients with uterine myoma, 23 patients with uterine adenomyosis, and three patients with uterine malignancy. We also investigated the influence of these conditions on the response of the uterus to histamine. The results show the same qualitative cyclic changes of the spontaneous motility of isolated myometrial strips throughout the menstrual cycle in all the abnormalities studied. These changes are characterized by a low amplitude and high frequency of spontaneous contractions in the proliferative phase and lower frequency with higher amplitude of …

Study on the histamine-like activity of guanfacine

Abstract The effects of guanfacine have been studied on guinea-pig isolated atria and diethylstilboestrol-treated rat isolated uterus to determine whether it possesses histamine-like activity. Guanfacine produced a concentration-dependent negative chronotropic effect which was not modified by ranitidine (0.1 μM). In rat isolated uterus contracted by KCl, clonidine (5–5000 μM) produced concentration-dependent relaxation which was blocked by ranitidine (0.1 μM), but guanfacine only produced relaxation at high concentrations (100–1000 μM), and this was not affected by ranitidine (0.1 μM). It is concluded that guanfacine, unlike clonidine, does not produce effects due to activation of H2-recept…

Explorando el contexto del tratamiento antihipertensivo en Atención Primaria. Estudio SIMPLITENS

Resumen A pesar de la existencia de diferentes guias sobre el manejo de la hipertension arterial y de los numerosos farmacos antihipertensivos disponibles, el grado de control de la hipertension dista de ser optimo, siendo muchas las razones que pueden explicar esta circunstancia. El objetivo del estudio SIMPLITENS fue describir la situacion del tratamiento antihipertensivo en Atencion Primaria en Espana con los objetivos secundarios de hacer un retrato de la actitud terapeutica de los medicos, identificar el papel de factores circunstanciales (administracion, guias) sobre las decisiones terapeuticas y validar un modelo de simplificacion del tratamiento. Se utilizo el metodo Delphi para inv…

Management of high blood pressure in children and adolescents: recommendations of the European Society of Hypertension.

Hypertension in children and adolescents has been gaining ground in cardiovascular medicine, mainly due to the advances made in several areas of pathophysiological and clinical research. These guidelines arose from the consensus reached by specialists in the detection and control of hypertension in children and adolescents. Furthermore, these guidelines are a compendium of scientific data and the extensive clinical experience it contains represents the most complete information that doctors, nurses and families should take into account when making decisions. These guidelines, which stress the importance of hypertension in children and adolescents, and its contribution to the current epidemi…

Manejo de la hipertensión arterial en niños y adolescentes: recomendaciones de la Sociedad Europea de Hipertensión

Resumen: La hipertensión en niños y adolescentes ha ido ganando terreno en la medicina cardiovascular, gracias a los avances producidos en distintas áreas de la investigación fisiopatológica y clínica. Estas guías nacen del consenso al que han llegado los especialistas en la detección y control de la hipertensión en niños y adolescentes. Por otra parte, dichas guías son un compendio de los datos científicos y la extensa experiencia clínica con la que se cuenta, y constituyen la información clínica más completa que los médicos, enfermeras y familiares deberían tener en cuenta a la hora de tomar decisiones. Estas guías, que hacen hincapié en la importancia de la hipertensión en niños y adoles…

Number of drugs used in secondary cardiovascular prevention and late survival in the population of Valencia Community, Spain.

Abstract Background Drug treatment for secondary prevention of cardiovascular disease is recommended by guidelines, but it is not always followed in real life. This study wanted to assess the size of this gap and its impact on mortality in subjects after a cardiovascular event (MACE). Methods Patients with any of MACE in the period from January 1st 2011 to December 31st 2013, and more than one year of follow-up were selected from population of the Valencian Community. Drugs for secondary prevention were antiplatelets, renin-angiotensin system blockers and statins. Assessment of treatment was performed one year after the initial event. Mortality risk was assessed using Cox by the number of d…

Effect of verapamil and diltiazem on isolated gastro-oesophageal sphincter of the rat

Abstract The effect of verapamil and diltiazem on the contraction induced by agonists on the rat lower oesophageal sphincter in-vitro has been studied. Both calcium entry blockers inhibited the contractile response to acetylcholine, carbachol and KCl. The potency of the inhibitory action was diltiazem &amp;gt; verapamil. The results give substance to the use of calcium entry blockers in the treatment of oesophageal spasm.

Medicamentos utilizados en pediatría extrahospitalaria: ¿disponemos de información suficiente?

Objetivo: Analizar los medicamentos que reciben los pacientes pediátricos en el ámbito extrahospitalario y la información disponible sobre los mismos. Pacientes y métodos: Estudio transversal, observacional y descriptivo realizado en una muestra de pacientes menores de 14 años atendidos en urgencias del Servicio de Pediatría del Consorcio Hospital General Universitario de Valencia entre junio 2005 y agosto 2006. Se cuantifican y clasifican los medicamentos utilizados antes de acudir a urgencias y se analiza la información sobre su uso que contiene el Vademécum Internacional Medicom y la ficha técnica. Resultados: Se recogió información sobre 462 niños con media de edad de 5,2 años (interval…