Troxerutin
Sources réglementaires consultées
Indications approuvées
- Traitement des symptômes liés à l'insuffisance veineuse légère chez l'adulte.
Contre-indications
Absolues
- Hypersensibilité à la troxérutine ou à l'un des excipients.
Mises en garde cliniques
- Mise en garde majeure · Ne pas utiliser pour un œdème des membres inférieurs dû à une maladie cardiaque, rénale ou hépatique, car l'efficacité n'a pas été démontrée dans ces indications. — https://cima.aemps.es/cima/dochtml/ft/74423/FT_74423.html
- Effets indésirables rares : troubles gastro-intestinaux, flatulences, diarrhée, douleur abdominale, gêne gastrique, dyspepsie, éruption, prurit et urticaire. Très rares : vertiges, céphalées, bouffées vasomotrices, fatigue, hypersensibilité et réactions anaphylactoïdes. — https://cima.aemps.es/cima/dochtml/ft/74423/FT_74423.html
Effets indésirables
Rares mais graves
Très rares : réactions anaphylactoïdes
Grossesse et allaitement
L'utilisation peut être envisagée si nécessaire, mais ne pas utiliser pendant les 3 premiers mois de grossesse. L'utilisation pendant l'allaitement n'est pas recommandée faute de données suffisantes.
Bibliographie récente (PubMed)
Hypertension, or high blood pressure (BP), is a complex disease influenced by various risk factors. It is characterized by persistent elevation of BP levels, typically exceeding 140/90 mmHg. Endothelial dysfunction and reduced nitric oxide (NO) bioavailability play crucial roles in hypertension development. L-NG-nitro arginine methyl ester (L-NAME), an analog of L-arginine, inhibits endothelial NO synthase (eNOS) enzymes, leading to decreased NO production and increased BP. Animal models exposed to L-NAME manifest hypertension, making it a useful design for studying the hypertension condition. Natural products have gained interest as alternative approaches for managing hypertension. Flavonoids, abundant in fruits, vegetables, and other plant sources, have potential cardiovascular benefits, including antihypertensive effects. Flavonoids have been extensively studied in cell cultures, animal models, and, to lesser extent, in human trials to evaluate their effectiveness against L-NAME-induced hypertension. This comprehensive review summarizes the antihypertensive activity of specific flavonoids, including quercetin, luteolin, rutin, troxerutin, apigenin, and chrysin, in L-NAME-induced hypertension models. Flavonoids possess antioxidant properties that mitigate oxidative stress, a major contributor to endothelial dysfunction and hypertension. They enhance endothelial function by promoting NO bioavailability, vasodilation, and the preservation of vascular homeostasis. Flavonoids also modulate vasoactive factors involved in BP regulation, such as angiotensin-converting enzyme (ACE) and endothelin-1. Moreover, they exhibit anti-inflammatory effects, attenuating inflammation-mediated hypertension. This review provides compelling evidence for the antihypertensive potential of flavonoids against L-NAME-induced hypertension. Their multifaceted mechanisms of action suggest their ability to target multiple pathways involved in hypertension development. Nonetheless, the reviewed
Transient receptor potential vanilloid 1 (TRPV1) is associated with skin sensitivity and mainly activated by capsaicin and heat. Interestingly, troxerutin can inhibit TRPV1 activation. However, its efficacy in reducing skin sensitivity remains undetermined. We evaluated the efficacy of troxerutin in alleviating skin sensitivity using clinical tests and in vitro experiments. For the in vitro experiment, HaCaT keratinocytes were pretreated with different concentrations of troxerutin, followed by incubation with 50 μM capsaicin for 1, 24, or 48 h. The gene and protein expressions of four inflammatory cytokines involved in skin irritation were determined. Among 35 Korean women with sensitive skin recruited for the clinical trial, 13 were involved in assessing the immediate soothing effects of 0.1% and 0.0095% troxerutin following capsaicin irritation, whereas 22 participated in evaluating the preventive soothing effect of 10% and 1% troxerutin over 4 weeks against capsaicin- and heat-induced irritation. We evaluated the soothing rate using skin redness, visual analog scale, and high temperature sensitive index as evaluation indices. Troxerutin inhibited the mRNA and protein expressions of cytokines in capsaicin-treated keratinocytes. In the clinical study, 0.1% and 0.0095% troxerutin promptly alleviated capsaicin-induced skin redness, whereas 10% troxerutin notably decreased both the visual analog scale and high temperature sensitive index for capsaicin- and heat-related irritation. However, 1% troxerutin was only effective in reducing the visual analog scale in response to capsaicin irritation. Troxerutin can inhibit TRPV1 activation in clinical and in vitro tests.
Clinical disorders associated with chronic pelvic pain (CPP) cause demonstrable emotional and physical dysfunction as well as increased health care utilization. Interventions that have been studied for the treatment of CPP often provide inadequate relief and/or intolerable adverse effects. The common practice of combining multiple CPP treatments needs more supportive evidence, and emerging combination trials have been evaluated in this systematic review. We searched MEDLINE and EMBASE and CENTRAL databases for CPP combination trials. This review included double-blind randomized controlled trials comparing combinations of 2 or more agents to at least 1 monotherapy in adults with CPP. The primary outcome was reduction in pain intensity or pain relief, and secondary outcomes included adverse events, quality of life, and other symptoms. Risk of bias was assessed. Nine studies (1,299 participants) were included and involved various different treatments including ciprofloxacin, tamsulosin, pentosan polysulfate, hyaluronic acid, chondroitin, hydroxyzine, troxerutin, carbazochrome, linzagolix, and allopurinol. Studies were heterogenous according to several features including studied treatments, dose and route of administration, and underlying condition such that no studies could be combined for meta-analysis. None of the included studies reported a significant difference in reducing pain intensity for combination therapy vs monotherapy. If future proof-of-concept studies demonstrate that a given combination is superior to all monotherapy components, subsequent large, double-blind randomized, controlled clinical trials of such combinations for CPP are required to better elucidate the role of combination therapy in clinical settings.
Ginkor Fort® (Tonipharm, Recordati Group; GB-T-H combined treatment) comprises ginkgo biloba extract, troxerutin and heptaminol chlorhydrate. It is a venotonic and vasculoprotective agent that strengthens veins, increases vessel resistance, and reduces permeability. Thanks to these synergistic actions, it is indicated for the treatment of signs and symptoms of venous insufficiency (VI) and signs related to the hemorrhoidal crisis. This review recapitulates the rationale for using venotonics to manage VI and discusses available evidence on the use of GB-T-H combined treatment to manage VI and hemorrhoidal crisis. Papers were retrieved by a PubMed search using different keywords. No language or publication date restrictions were used. Documents from the Authors' literature collection were also considered. Papers were selected for inclusion according to their relevance to the topic. Preclinical and clinical studies showed that the GB-T-H combined treatment acts on both the acute phase symptoms and the pathogenetic mechanisms of the VI, through the prevention of the hypoxia-induced activation of endothelial cells, the reduction of the capillary tone and the hemostatic activity. This leads to the long-term slowing of the disease progression, suggesting that the GB-T-H combined treatment can manage the acute clinical manifestations and as a prevention measure with prolonged use in both VI and hemorrhoidal crises. In the available study, the GB-T-H combined treatment showed excellent tolerability. Available literature evidence and extensive clinical experience support the use of the GB-T-H combined treatment as an effective and safe option for treating and preventing the clinical manifestation of VI and hemorrhoidal crisis.
- Application of Drug Repurposing Approach for Therapeutic Intervention of Inflammatory Bowel Disease.
Inflammatory bowel disease (IBD), represented by Crohn's disease (CD) and ulcerative colitis (UC), is a chronic inflammatory disorder of the gastrointestinal tract (GIT) characterized by chronic relapsing intestinal inflammation, abdominal pain, cramping, loss of appetite, fatigue, diarrhoea, and weight loss. Although the etiology of IBD remains unclear, it is believed to be an interaction between genes, and environmental factors, such as an imbalance of the intestinal microbiota, changing food habits, an ultra-hygiene environment, and an inappropriate immune system. The development of novel effective therapies is stymied by a lack of understanding of the aetiology of IBD. The current therapy involves the use of aminosalicylates, immunosuppressants, and corticosteroids that can effectively manage symptoms, induce and sustain remission, prevent complications, modify the course of the disease, provide diverse treatment options, showcase advancements in biologic therapies, and enhance the overall quality of life. However, the efficacy of current therapy is overshadowed by a plethora of adverse effects, such as loss of weight, mood swings, skin issues, loss of bone density, higher vulnerability to infections, and elevated blood pressure. Biologicals, like anti-tumour necrosis factor agents, can stimulate an autoimmune response in certain individuals that may diminish the effectiveness of the medication over time, necessitating a switch to alternative treatments. The response of IBD patients to current drug therapy is quite varied, which can lead to disease flares that underlines the urgent need to explore alternative treatment option to address the unmet need of developing new treatment strategies for IBD with high efficacy and fewer adverse effects. Drug repurposing is a novel strategy where existing drugs that have already been validated safe in patients for the management of certain diseases are redeployed to treat other, unindicated diseases. The present narrative r