Sequential, non-arteritic anterior ischemic optic neuropathy in patients taking sildenafil: a report of ten cases

To present a summary of 10 cases of non-arteritic anterior ischemic optic neuropathy [NAION] in patients who received phosphodiesterase type 5 [PDE-5] inhibitors. A case series of 10 patients who, after regular intake of Sildenafil, presented with a first episode of NAION in one eye. NAION was diagnosed based on the following criteria: acute, painless, unilateral loss of vision, fundus features consistent with NAION and exclusion of other possible causes. Despite the initial adverse event [first episode of NAION], all of these patients continued to use the medication and developed a second episode of NAION in the contralateral eye. Only one of the 10 patients presented with bilateral simultaneous NAION. This largest case series published to date, reinforces the general consensus that PDE-5 inhibitors are contraindicated in patients with a history of unilateral NAION.

Central retinal vein occlusion in a patient after being commenced on sildenafil citrate for pulmonary arterial hypertension.

A 75-year-old female was commenced on sildenafil for the treatment of pulmonary arterial hypertension (PAH) secondary to chronic obstructive pulmonary disease (COPD). She reported blurring of vision within 72 hours after starting treatment and was found to have a central retinal vein occlusion (CRVO). Such an occurrence is the second case reported to date, and we review the possible mechanisms and literature on the subject.

Evaluación de la respuesta al sildenafil 50 mg en pacientes con disfunción eréctil sin tratamientos previos en la práctica cotidiana / Evaluation of the response to sildenafil 50 mg in patients with erectil dysfunction without previous treatment during the current practice

Nuestro estudio corrobora la elevada eficacia del Sildenafil para el tratamiento de la Disfunción Sexual Eréctil en el contexto de la práctica diaria de consultorio. El Sildenafil mostró ser un fármaco seguro, aun en pacientes con patologías concomitantes, debiendo pocos pacientes suspender la medicación por efectos secundarios severos. El Sildenafil mejoró no sólo la actividad sexual de los pacientes sino también su calidad de vida.

Uso de levosimendana em diversos quadros de insuficiência cardíaca aguda: [revisão] / Levosimendan use in several scenarios of acute heart failure: [review]

Nos países em que é comercializada, a administração precoce de levosimendana deve ser considerada em pacientes que permanecem sintomáticos e com dispnéia em repouso apesar da terapia inicial, principalmente aqueles com história de insuficiência cardíaca crônica ou em tratamento prolongado com betabloqueadores. Pacientes hipotensos ou com isquemia ativa não são os melhores candidatos para receber infusão de levosimendana e precisam, primeiro, ter esses problemas tratados.

In countries where it is available, early levosimendan infusion can be considered for patients who remain symptomatic with dyspnea at rest despite initial therapy, particularly those with a history of chronic heart failure or chronically treated with beta-blockers. Hypotensive patients or patients with active ischemia are not the best candidates for levosimendan administration and should have these problems addressed first.

Sildenafil citrate and Torsade de pointes

Sildenafil citrate is a drug used in the treatment of erectile dysfunction. It is an inhibitor of the enzyme phosphordiesterase-5; it slows down the breakdown of c-GMP and nitrous oxide. The cardiac effects associated with Sildenafil citrate have been extensively studied in medical literature, especially its potent vasodilatory effect when combined with nitrate-based medications, producing intractable hypotension, but a lesser known and potentially lethal side effect is prolonged cardiac repolarization when used at dosage greater than recommended, leading to QT prolongation that could theoretically lead to dangerous cardiac dysrrhythmias and sudden death in men with coronary artery disease. The authors present the case of a 49-year-old hypertensive Hispanic man who arrived to our emergency department with the chief complaint of acute epigastric pain for 3 hours of evolution after ingestion of Sildenafil citrate 50 milligrams (mg). The patient was found to have an acute ST elevation inferior myocardial infarction (STEMI). Shortly after diagnosis the patient developed a polymorphic ventricular tachycardia (Torsade de pointes) before thrombolytic administration. We present this case followed by a brief discussion, to heighten awareness of the possible association of acute inferior STEMI and the development of Torsade de Pointes after the use of Sildenafil citrate.

Efficacy and safety of sildenafil in Asian males with erectile dysfunction and cardiovascular risk.

OBJECTIVE: Assess the effectiveness of sildenafil in Asian males with erectile dysfunction (ED) and one or more of the co-morbidities, mild-to-moderate hypertension, dyslipidemia, and diabetes. MATERIAL AND METHOD: A six-week, double-blind, randomized, placebo-controlled, multicenter study was carried out in Thailand, Malaysia and Singapore. One hundred and fifty five male subjects were randomized (2:1) to sildenafil (n = 104) or placebo (n = 51). Sildenafil was started at 50 mg and increased (100 mg) or decreased (25 mg) at week 2 if necessary. RESULTS: On the primary efficacy endpoint, sildenafil-treated subjects had significantly better scores on the International Index of Erectile Function (IIEF) questions 3 and 4 than placebo (p < 0.001, both questions). When accumulated into IIEF domains, all five domains were significant in favor of sildenafil. In addition, sildenafil-treated subjects were more satisfied with treatment and had a higher intercourse success rate. The majority of adverse events were mild in severity; the most commonly reported treatment-related events were dizziness (7.7%) and tinnitus (2.9%). CONCLUSION: Sildenafil (25, 50, and 100 mg) was found to be an effective, safe, and well-tolerated treatment for ED in the present study population of Thai, Malaysian, and Singaporean males who also had increased cardiovascular risk

Sildenafil masticable, análisis prospectivo de nueva presentación farmacológica / Cheweable sildenafil: prospective analysis of a new presentation

La disfunción eréctil es una patología de alta frecuencia, especialmente en población masculina de mayor edad. La erección está dada fundamentalmente por la activación del sistema parasimpático, por acción del óxido nítrico y aumento de GMP cíclico; es así como fármacos como Sildenafil que disminuyen la eliminación de GMP cíclico al inhibir la actividad de la 5 fosfodiesterasa, potencian la mantención de dicha erección. Recientemente se lanzó al mercado la presentación masticable de este fármaco, lo que eliminaría el primer paso hepático de la presentación oral clásica. En este estudio, se analizaron 20 pacientes con disfunción eréctil sin comorbilidad asociada, los que consumieron la forma masticable; con el objetivo de evaluar eficacia clínica y efectos adversos. Los resultados obtenidos muestran que existe un alto grado de satisfacción de usuario en cuanto a forma de presentación, tiempo de administración y eficacia, y que los efectos adversos no difieren a los de la presentación tradicional. Se propone realizar estudios prospectivos comparativos de ambas presentaciones y otros inhibidores de la 5 fosfodiesterasa, para confirmar estos resultados preliminares.

Erectil dysfunction is a very frequent pathology in the elderly male. Erections are activated mainly by the parasympathic system, caused by nitric oxide and the increase of cyclic cGMP; it is because of this that drugs like Sildenafil improve partial erections by inhibiting the enzyme that facilitates the reduction of cyclic guanosine monophosphate (cGMP). Recently a chewable new form of this drug entered the market,it is deemed to avoid hepatic transformation of the drug. In this study we analyzed 20 patients witherectile dysfunction without other associated comorbidities that were treated with this drug. Results showed that patients were highly satisfied with the form of presentation, the dosage regimen, and efficacy. Side effects are no different from the other and more traditional version. We will conduct prospective comparative studies of both versions of the drugs and other inhibitors of the cGMP specific phosphodiesterase type 5,to confirm these preliminary results.

Effect of sildenafil citrate on the cardiovascular system

Sildenafil citrate is a drug commonly used to manage erectile dysfunction. It is designated chemically as 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H -pyrazolo[4,3-d]pyrimidin-5-yl)-4 ethoxyphenyl] sulfonyl]-4-methylpiperazine citrate (C22H30N6O4 S). It is a highly selective inhibitor of cyclic guanine monophosphate-specific phosphodiesterase type 5. In late March through mid-November 1998, the US Food and Drug Administration (FDA) published a report on 130 confirmed deaths among men (mean age, 64 years) who received prescriptions for sildenafil citrate, a period during which >6 million outpatient prescriptions (representing about 50 million tablets) were dispensed. The US FDA recently reported that significant cardiovascular events, including sudden cardiac death, have occurred in men with erectile dysfunction who were taking sildenafil citrate. These reports have raised concerns that sildenafil citrate may increase the risk of cardiovascular events, particularly fatal arrhythmias, in patients with cardiovascular disease. In the past few years, the cardiac electrophysiological effects of sildenafil citrate have been investigated extensively in both animal and clinical studies. According to extensive data available to date, sildenafil citrate has been shown to pose minimal cardiovascular risks to healthy people taking this drug. Some precautions are needed for patients with cardiovascular diseases. However, the only absolute contraindication for sildenafil citrate is the concurrent use of nitrates. This article is intended to review sildenafil citrate's cardiovascular effects, as well as current debates about its arrhythmogenic effects.

Características del uso de Sildenafil en una muestra de pacientes a nivel de farmacias comunitarias de Concepción, Chile / Features of subjects purchasing Sildenafil at community pharmacies in Concepción, Chile

Background: Erectile dysfunction is a public health problem. Millions of men worldwide experience this condition, affecting their quality of life. Sildenafil, a phosphodiesterase type 5 inhibitor, is the treatment of choice for erectile dysfunction. Aim: To study the characteristics of Sildenafil use among costumers of community pharmacies in Concepcion Chile. Material and methods: A structured interview about Sildenafil use was applied to subjects purchasing the drug in community pharmacies and that consented to participate. Results: One hundred thirty eight males were studied. Forty six percent of patients were fifty years old or older. Most (47.1%) used Sildenafil for one year or more and 60.5% had no adverse events. Among those experiencing side effects, headache was experienced by 38.9%, flushing by 16.6% and gastrointestinal effects by 16.7%. Ninety percent of patients had a good evaluation of the drug in terms of benefits and tolerance. Thirty two percent of the subjects, had diseases associated to erectile dysfunction. Among these, 45% had diabetes mellitus, 29.5% had hypertension, and 18.2% had prostatic diseases. In 54% of cases, the drug was prescribed by a physician. Twenty two percent of patients experienced changes in the effect of the drug when it was simultaneously used with other drugs or meals. Thirty four percent of patients used other drugs. Among these, 43.3% were using antihypertensives, and 26.7% were using antidiabetic drugs. Conclusions: Considering the elevated age and the number of associated disease of patients using Sildenafil, the use of the drug under medical prescription must be emphasized to avoid untoward effects.

Eficacia y tolerabilidad sostenida en el tiempo después de 2 años de tratamiento con vardenafil 10 mg y 20 mg en hombres chilenos con disfunción eréctil / Efficacy and tolerance on the long term 2 years with doses of 10 and 20 mgs. per day of vardenafil in chilean patient with erectile dysfunction

Vardenafil es un inhibidor de la 5 fosfodiesterasa que mejora la calidad de la erección. Los estudios publicados demuestran su eficacia y seguridad en grandes series de pacientes. El objetivo de este estudio fue comparar la eficacia y tolerabilidad de Vardenafil a largo plazo (2 años) de dos dosis diferentes de la droga. Se analizan los resultados obtenidos en un grupo de pacientes chilenos que participan en un estudio multicéntrico internacional, randomizado, doble ciego, para evaluar la eficacia y tolerancia de Vardenafil 10 mg y 20 mg, a 2 años plazo. Los pacientes fueron sometidos a estrictos criterios de inclusión y exclusión y completaron el cuestionario validado Índice Internacional de la Función Eréctil (IIEF) en cada visita y un cuestionario de Perfil de Encuentros Sexuales (SEP) incluido en un diario que se llenó después de cada intento sexual. La eficacia primaria se midió con el escore de dominio de la función eréctil del IIEF (preguntas 1, 2, 3, 4, 5 y 15) y con el diario del paciente SEP. La seguridad y tolerabilidad se evaluó en cada visita por medio del registro de los eventos adversos (cualquier situación médica relacionada ono con la droga) ocurridos entre visitas. Treinta y cinco pacientes randomizados completan el período de 2 años (18 del grupo de 10 mg, con un promedio de edad de 55 años y 17 del grupo de 20 mg, con 58,8 años de edad promedio). El tratamiento con Vardenafil 10 mg o 20 mg produjo una mejoría en el escore de dominio de la función eréctil del IIEF. La mejoría se obtuvo desde la primera evaluación a las 4 semanas y se mantuvo hasta el final del estudio.En el grupo de Vardenafil 10 mg, el escore mejoró de 11,9 ±4,54 en la primera visita (semana 0) a 28,1 ±1,92 en la última visita (semana 104). En el grupo de Vardenafil 20 mg, el escore subió de 10,7 ± 4,18 en la primera visita a 26,2 ± 5,06 al final del estudio. Se produjeron eventos adversos en el 78 por ciento del grupo 10 mg y 88 por ciento del grupo de 20 mg. El evento adverso más frecuente fue cefalea en el 22 por ciento y 18 por ciento de cada grupo, respectivamente. Los eventos adversos serios no se relacionaron con la droga. Podemos concluir que Vardenafil, en dosis de 10 mg y 20 mg, es eficaz y seguro a largo plazo en el tratamiento de la disfunción eréctil.

Management of erectile dysfunction in patients with ischemic heart disease by intracavernous injection of vasoactive drugs because of failure, complications or contraindication of sildenafil

The aim of the present study was to evaluate the effectiveness of intracavemous injection [ICI] of vasoactive drugs combination in patients with ischemic heart disease [IHD] and erectile dysfunction [ED] who were not proper cadidatefor treatment with sildenafil citrate. The study population included 122 selected patients with IHD and ED in whom sildenafil was not an option because of its failure, side effects, or presence of contraindication for its use. The ICI program consisted of two combinations of vasoactive drugs. The first combination [A] included a mixture of papaverine, phen-tolamine, and verapamil The second combination [B] included a mixture of the former 3 drugs plus prostaglandin El. Patients who failed to respond with the first combination were switched to the second combination. A positive response was defined as an erection sufficient for vaginal penetration and maintained till ejaculation. A positive response was achieved with combination [A] in 67 [54.9%] of the 122 patients and with combination [B] in 24 [43.6%] of the remaining 55 patients. The total success rate was [74.6%]. Patients with positive response [91 pts.] were followed-up for one year with 80 [87.9%] patients reported successjid coitus during this period. The remaining 11 patients [12.1%] dropped out of the program, 2 [2.2%] because of treatment failure, and 9 [9.9%] because of marital and health reasons. Adverse effects of ICI therapy included prolonged erection in 10 [11%], painful erection in 9 [9.9%], subcutaneous hematoma in 7 [7.7%], and plaque formation in 3 [3.3%]. We conclude that ICI ofvasoactive drugs is a good alternative for the treatment of ED in patients with IHD in whom stidenafil is not anoption

Influência da cafeína no comportamento da pressäo arterial e da agregaçäo plaquetária / Influence of caffeine on blood pressure and platelet aggregation

OBJECTIVE: Studies have demonstrated that methylxanthines, such as caffeine, are A1 and A2 adenosine receptor antagonists found in the brain, heart, lungs, peripheral vessels, and platelets. Considering the high consumption of products with caffeine in their composition, in Brazil and throughout the rest of the world, the authors proposed to observe the effects of this substance on blood pressure and platelet aggregation. METHODS: Thirteen young adults, ranging from 21 to 27 years of age, participated in this study. Each individual took 750mg/day of caffeine (250mg tid), over a period of seven days. The effects on blood pressure were analyzed through the pressor test with handgrip, and platelet aggregation was analyzed using adenosine diphosphate, collagen, and adrenaline. RESULTS: Diastolic pressure showed a significant increase 24 hours after the first intake (p<0.05). This effect, however, disappeared in the subsequent days. The platelet aggregation tests did not reveal statistically significant alterations, at any time during the study. CONCLUSION: The data suggest that caffeine increases diastolic blood pressure at the beginning of caffeine intake. This hypertensive effect disappears with chronic use. The absence of alterations in platelet aggregation indicates the need for larger randomized studies.

Influence of adenosine agonists and antiepileptic drugs on theophylline-induced seizures in rats.

Seizures is a major toxicity of theophylline. The mechanism of theophylline-induced seizures is not known, but antagonism at adenosine receptors may be a possibility. The effect of pretreatment with different doses of adenosine (100, 500 and 1000 mg/kg, i.p.), and the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA), 1, 5 and 10 mg/kg, i.p., was studied against seizures induced by theophylline in rats. Both these drugs, at all dose levels tested, failed to protect theophylline seizures. Thus adenosinergic system is unlikely to be involved in mediating the convulsant action of theophylline. On the other hand, the conventional antiepileptic drugs, i.e. diazepam (4 mg/kg), sodium valproate (300 mg/kg) and phenobarbitone (50 mg/kg), but not carbamazepine, afforded some protection. The modification of course of seizures, by the antiepileptic drugs suggests the involvement of some other alternate mechanism in theophylline-induced seizures.