RESUMO
Flavonoids are oral venoactive drugs frequently prescribed to relieve the symptoms of chronic venous disorders (CVD). Among venoactive drugs, diosmin is a naturally occurring flavonoid glycoside that can be isolated from various plant sources; it can also be obtained after conversion of hesperidin extracted from citrus rinds. Micronized purified flavonoid fraction (MPFF) is a preparation that contains mainly diosmin and a small fraction of hesperidin. We performed a state-of-the-art literature review to collect and analyze well-conducted randomized clinical studies comparing diosmin - also called non-micronized or hemisynthetic diosmin - 600 mg a day and MPFF, 1000 mg a day. Three clinical studies met the criteria and were included for this literature review. These clinical studies showed a significant decrease of CVD symptom intensity (up to approximately 50%) and global patient satisfaction after one-to-six-month treatment with diosmin or MPFF, without statistical differences between these two forms of diosmin. Both treatments were well tolerated with few mild adverse drug reactions reported. Overall, based on this literature review, there is no clinical benefit to increase the dose of diosmin beyond 600 mg per day, to use the micronized form, or to add hesperidin, since clinical efficacy on venous symptomatology is achieved with 600 mg per day of pure non-micronized diosmin. This challenges the status of diosmin - 600 mg a day - in guidelines for the management of CVD, which is currently categorized 2C (weak recommendations for use and poor quality of evidence), while the most widely used and assessed preparation MPFF is rated 1B (strong recommendation for use and moderate quality of evidence).
Assuntos
Diosmina/uso terapêutico , Flavonoides/uso terapêutico , Hesperidina/uso terapêutico , Insuficiência Venosa/tratamento farmacológico , Doença Crônica , Diosmina/efeitos adversos , Flavonoides/efeitos adversos , Hesperidina/efeitos adversos , Humanos , Ensaios Clínicos Controlados Aleatórios como Assunto , Resultado do Tratamento , Doenças Vasculares , Insuficiência Venosa/diagnósticoRESUMO
BACKGROUND: Phlebotonics have beneficial effects on some symptoms related to chronic venous disease (CVD) of the lower limbs. The most commonly used one is diosmin, available in a pure semisynthetic form or as a micronized purified flavonoid fraction. Patients and Methods. The primary objective of this single-blind, randomized, parallel-group, prospective study was to assess the clinical noninferiority of nonmicronized diosmin 600 mg once daily (D-group) compared to micronized diosmin 900 mg plus hesperidin 100 mg once daily (D/H-group) over a 6-month treatment period. Adult patients with a symptomatic CVD of the lower limbs (C0-C3 grade; 20-60 mm on a 100 mm visual analog scale (VAS)) were included. The primary endpoint was the change (from baseline to last postbaseline value) of the intensity of the lower-limb symptoms on VAS. RESULTS: 114 patients (mean age, 44.4 years; women, 90.4%) were randomized in the per-protocol analysis (D-group, n = 57; D/H-group, n = 57; D/H-group, p < 0.0001) in the D-group and -22.8 mm (p < 0.0001) in the D-group and -22.8 mm (p < 0.0001) in the D-group and -22.8 mm (. CONCLUSION: Nonmicronized diosmin 600 mg was proven to have a noninferior efficacy compared to micronized diosmin 900 mg plus hesperidin 100 mg, associated with greater ease in swallowing the tablet.
RESUMO
JUSTIFICATIVA E OBJETIVOS: Os anti-inflamatórios não esteroides (AINES) apresentam atividade farmacológica de inibição das isoenzimas ciclo-oxigenase-1 (COX-1) e ciclo-oxigenase-2 (COX-2) em graus diversos, cujos perfis de segurança variam individualmente.A eficácia é semelhante, porém os possíveis eventos adversos são relevantes nas decisões do tratamento prescrito. O diclofenaco está disponível internacionalmente há mais de 40 anos, tendo seu perfil farmacológico e de segurança documentados em diversos estudos básicos e clínicos. O objetivo desta revisão da literatura foi de apresentar aspectos da dor e do uso de diclofenaco na prática clínica, incluindo as indicações as questões de segurança e a eficácia do medicamento. CONTEÚDO: Esta revisão da literatura apresentará a farmacologia básica do diclofenaco, bem como evidências terapêuticas com o uso deste fármaco em diversas condições dolorosas e suas implicações na prática clínica. CONCLUSÃO: O diclofenaco tem demonstrado eficácia clínica no tratamento de diversas condições dolorosas, entre estas lombalgias, artrites, dores pós-traumáticas e pós-cirúrgicas, dismenorreias,bem como cólica renal e biliar. Vale ressaltar que, na avaliação de um paciente apresentando dor e ao decidir um plano de tratamento e na prescrição de qualquer medicamento, cabe ao médico avaliar cuidadosamente o paciente para determinar o melhor curso de ação no individuo, levando-se em consideração o histórico médico do paciente, comorbidades e uso de medicamentos concomitantes, a fim de proporcionar a melhor alternativa terapêutica, com redução máxima da dor e inflamação e a restauração da funcionalidade de forma mais segura.
BACKGROUND AND OBJECTIVES: The nonsteroidal antiinflammatory-drugs (NSAIDs) exhibit pharmacological activity inhibiting the isoenzymes cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) in varying degrees, and their safety profiles vary individually. Their efficacy is similar, but the possible adverse effects are relevant in deciding treatment prescriptions. Diclofenac has been available internationally for over 40 years, and its pharmacological and safety profile has been documented in numerous preclinical and clinical studies. The objective of this literature review was to present aspects of pain and the use of diclofenac in clinical practice, including indications, safety issues, and efficacy of the drug. CONTENTS: This literature review will present the basic pharmacology of diclofenac, as well as evidence for the therapeutic use of this drug in several painful conditions and the implications for clinical practice. CONCLUSION: Diclofenac has shown clinical efficacy in the treatment of a variety of painful conditions, including lumbagos,arthritis, post-traumatic and post-surgical pain, dysmenorrhea,as well as renal and biliary colic. It is important to note that in the evaluation of a patient presenting pain and when deciding a treatment plan and the prescription of any medication, it is upto the physician to carefully assess the patient to determine the best course of action in that individual, taking into account thepatients' medical history, co-morbidities, and use of concomitant medications, in order to provide the best therapeutic alternative,with a maximum reduction of pain and inflammation and restoration of functionality in the safest possible way.
Assuntos
Humanos , Anti-Inflamatórios não Esteroides , Diclofenaco/farmacologia , Diclofenaco/uso terapêutico , EficáciaRESUMO
Chronic Venous Disorder (CVD) is a term used to represent all abnormal clinical changes that result from venous disease of the lower extremities, and that have a chronic pattern. This disease has a documented socioeconomic impact, involving a significant part of the western populations, and consuming 2-3% or more of societies? health budgets. This review of the literature focuses on diosmin, a benzopyrone phlebotonic, specifically mechanisms of action as well as preclinical and clinical evidence.
Assuntos
Humanos , Diosmina , Insuficiência VenosaRESUMO
Neste trabalho, estudam-se as comunicaçöes arteriovenosas em 27 membros inferiores com insuficiência arterial, divididos em dois grupos: no primeiro estäo incluidos 12 membros nos quais os pacientes referem dor tipo claudicaçäo intermitente e, no segundo, 15 que apresentam isquemia de repouso. O método empregado é o de injeçäo venosa e arterial, consecutivas, de doses semelhantes de macroagregado de soro-albumina humana marcado com tecnécio -99m, seguidas respectivamente de varreduras de corpo inteiro em um contador de corpo total. O acrécimo da atividade pulmonar após a injeçäo arterial (percentagem de comunicaçöes arteriovenosas) foi calculado. No grupo de extremidades onde havia somente isquemia muscular ao esforço, a fraçäo do fluxo sanguíneo do membro que atravessou as comunicaçöes arteriovenosas foi, em média, inferior a 3%, resultado superponível ao observado em membros com circulaçäo normal. No grupo de extremidades com isquemia de respouso a percentagem dessas comunicaçöes foi significativamente superior, atingindo, em média, níveis acima de 8%