OBJECTIVES: Rutin, quercetin-3-O-rutinoside, a natural flavonol glycoside, has shown various in vitro benefits with potential use treating human diseases, especially cardiovascular system disorders. Antioxidant properties are assumed to underlie the majority of these benefits. Yet rutin pro-oxidant properties have been reported as well. Our research group has recently shown aggravating effects on isoprenaline (ISO)-induced cardiotoxicity in Wistar:Han rats after 24 hours. METHODS: This study was designed to examine in more detail the reasons for the negative effects of rutin (11.5 and 46 mg/kg, i.v.) after administration of ISO (100 mg/kg, s.c.) in rats within 2 hours of continuous experiment and in the H9c2 cardiomyoblast-derived cell line. RESULTS: Like our previous findings, rutin did not (11.5 or 46 mg/kg, i.v.) reduce the ISO-induced mortality within 2 hours although the lower dose significantly reduced cardiac troponin T (cTnT) and partly improved the histological findings. In contrast, the higher dose increased the mortality in comparison with solvent (1.26% w/v sodium bicarbonate). This was not caused by any specific haemodynamic disturbances. It appears to be associated with oxidative stress as rutin enhanced intracellular reactive oxygen species formation in vitro and had the tendency to increase it in vivo. CONCLUSIONS: Rutin, likely due to its pro-oxidative effects, can exacerbate catecholamine cardiotoxicity depending on the dose used.

• MeSH
• Cell Line MeSH
• Dinoprost analogs & derivatives   blood   MeSH
• Electrocardiography MeSH
• Glutathione blood   MeSH
• Injections, Intravenous MeSH
• Isoproterenol adverse effects   MeSH
• Kaplan-Meier Estimate MeSH
• Cardiotoxicity etiology   mortality   MeSH
• Myocardium pathology   MeSH
• Rats, Wistar MeSH
• Reactive Oxygen Species metabolism   MeSH
• Rutin administration & dosage   adverse effects   pharmacokinetics   MeSH
• Heart drug effects   MeSH
• Dose-Response Relationship, Drug MeSH
• Animals MeSH
• Check Tag
• Male MeSH
• Animals MeSH
• Publication type
• Journal Article MeSH

• Keywords
• Wobenzym plus, Phlogenzym,
• MeSH
• Arthralgia * drug therapy   MeSH
• Osteoarthritis, Knee * drug therapy   MeSH
• Bromelains administration & dosage   MeSH
• Diclofenac administration & dosage   MeSH
• Adult MeSH
• Double-Blind Method MeSH
• Enzyme Therapy * MeSH
• Drug Combinations MeSH
• Middle Aged MeSH
• Humans MeSH
• Multicenter Studies as Topic MeSH
• Randomized Controlled Trials as Topic MeSH
• Rutin analogs & derivatives   administration & dosage   MeSH
• Aged, 80 and over MeSH
• Aged MeSH
• Trypsin administration & dosage   MeSH
• Treatment Outcome MeSH
• Check Tag
• Adult MeSH
• Middle Aged MeSH
• Humans MeSH
• Aged, 80 and over MeSH
• Aged MeSH

• Keywords
• 0,33% brimonidin gel, venotonika,
• MeSH
• Medical History Taking MeSH
• Anti-Bacterial Agents administration & dosage   therapeutic use   MeSH
• Antihypertensive Agents administration & dosage   pharmacology   therapeutic use   MeSH
• Adult MeSH
• Erythema * diagnosis   drug therapy   prevention & control   MeSH
• Conjunctivitis diagnosis   drug therapy   MeSH
• Ascorbic Acid administration & dosage   therapeutic use   MeSH
• Middle Aged MeSH
• Humans MeSH
• Rosacea * diagnosis   epidemiology   drug therapy   genetics   complications   prevention & control   psychology   MeSH
• Rutin administration & dosage   therapeutic use   MeSH
• Aged MeSH
• Dry Eye Syndromes diagnosis   drug therapy   complications   MeSH
• Vitamin E administration & dosage   therapeutic use   MeSH
• Treatment Outcome MeSH
• Lubricant Eye Drops administration & dosage   therapeutic use   MeSH
• Check Tag
• Adult MeSH
• Middle Aged MeSH
• Humans MeSH
• Male MeSH
• Aged MeSH
• Female MeSH
• Publication type
• Case Reports MeSH

• MeSH
• Adjuvants, Immunologic administration & dosage   therapeutic use   MeSH
• Anti-Inflammatory Agents, Non-Steroidal MeSH
• Osteoarthritis, Knee * drug therapy   classification   physiopathology   MeSH
• Adult MeSH
• Double-Blind Method MeSH
• Hydrolases administration & dosage   therapeutic use   MeSH
• Clinical Trials as Topic MeSH
• Knee Joint drug effects   MeSH
• Middle Aged MeSH
• Humans MeSH
• Randomized Controlled Trials as Topic MeSH
• Rutin administration & dosage   therapeutic use   MeSH
• Aged, 80 and over MeSH
• Aged MeSH
• Severity of Illness Index MeSH
• Treatment Outcome MeSH
• Check Tag
• Adult MeSH
• Middle Aged MeSH
• Humans MeSH
• Aged, 80 and over MeSH
• Aged MeSH

• Keywords
• Phlogenzym, Wobenzym,
• MeSH
• Osteoarthritis, Knee * drug therapy   MeSH
• Bromelains administration & dosage   MeSH
• Diclofenac administration & dosage   MeSH
• Adult MeSH
• Enzyme Therapy * MeSH
• Drug Combinations MeSH
• Middle Aged MeSH
• Humans MeSH
• Multicenter Studies as Topic MeSH
• Randomized Controlled Trials as Topic MeSH
• Rutin analogs & derivatives   administration & dosage   MeSH
• Aged MeSH
• Trypsin administration & dosage   MeSH
• Treatment Outcome MeSH
• Check Tag
• Adult MeSH
• Middle Aged MeSH
• Humans MeSH
• Aged MeSH
• Publication type
• Newspaper Article MeSH

Autoři ve svém příspěvku popisují případ neočekávaného pooperačního krvácení po estetické rhinoplastice v důsledku předem nezjištěné asymptomatické hemofilie.

Authors report a case of unexpected postoperative bleeding after an aesthetic rhinoplasty that was due to previously undiagnosed asymptomatic haemophilia

• Keywords
• Ascorutin,
• MeSH
• Adult MeSH
• Epistaxis * etiology   drug therapy   complications   MeSH
• Drug Combinations MeSH
• Hemophilia A * diagnosis   drug therapy   complications   MeSH
• Ascorbic Acid administration & dosage   MeSH
• Humans MeSH
• Postoperative Complications MeSH
• Rhinoplasty * adverse effects   MeSH
• Rutin administration & dosage   MeSH
• Check Tag
• Adult MeSH
• Humans MeSH
• Female MeSH
• Publication type
• Case Reports MeSH

Preparation of coated pellets intended for rutin colon delivery, their evaluation in vitro and in vivo in experimental colitis in rats was the purpose of this study. Pellets were obtained using extrusion/spheronization and coated with three types of coatings (caffeic acid/hypromellose/alginic acid; sodium alginate/hypromellose/zinc acetate; sodium alginate/chitosan). Dissolution using buffers of pH values, β-glucosidase and times corresponding to gastrointestinal tract (GIT) was provided. Pellets coated with alginate/chitosan showed low rutin dissolution (12-14%) in upper GIT conditions and fast release (87-89%) under colon conditions; that is a good presumption of intended rutin release. After colitis induction and development, the rats were treated with pellets and rutin solution administered orally, solution also rectally. Colon/body weight ratio, myeloperoxidase activity and histological evaluation were performed. Rutin was able to promote colonic healing at the dose of 10mg/kg: colon/body weight ratio decreased and myeloperoxidase activity was significantly suppressed. Pellets coated with alginate/chitosan applied orally and rutin solution administered rectally showed the best efficacy. The combination of rutin as natural product, mucoadhesive chitosan degraded in the colon and sodium alginate as the main coating substance in the form of pellets create a promising preparation for therapy of this severe illness.

• MeSH
• Alginates chemistry   MeSH
• Anti-Inflammatory Agents administration & dosage   chemistry   pharmacology   MeSH
• Administration, Oral MeSH
• Time Factors MeSH
• Chitosan chemistry   MeSH
• Chemistry, Pharmaceutical MeSH
• Technology, Pharmaceutical methods   MeSH
• Gastrointestinal Agents administration & dosage   chemistry   pharmacology   MeSH
• Drug Implants MeSH
• Colitis chemically induced   drug therapy   pathology   MeSH
• Colon drug effects   pathology   MeSH
• Hydrogen-Ion Concentration MeSH
• Rats MeSH
• Glucuronic Acid chemistry   MeSH
• Trinitrobenzenesulfonic Acid MeSH
• Hexuronic Acids chemistry   MeSH
• Caffeic Acids chemistry   MeSH
• Methylcellulose analogs & derivatives   chemistry   MeSH
• Disease Models, Animal MeSH
• Zinc Acetate chemistry   MeSH
• Rats, Wistar MeSH
• Drug Compounding MeSH
• Buffers MeSH
• Solubility MeSH
• Rutin administration & dosage   chemistry   pharmacology   MeSH
• Drug Stability MeSH
• Animals MeSH
• Check Tag
• Rats MeSH
• Male MeSH
• Animals MeSH
• Publication type
• Journal Article MeSH
• Research Support, Non-U.S. Gov't MeSH

Pelety s obsahem rutinu připravené metodou extruze/sferonizace se potáhly obalem složeným z natrium-alginátu a chitosanu. U pelet se před obalením zhodnotily důležité jakostní parametry a po obalení disoluční profil léčiva v disolučních prostředích o pH odpovídajícím podmínkám v gastrointestinálním traktu. Vzorky obalených pelet se založily do boxů určených pro testování stability při různých podmínkách, tj. 25 °C a 60 % relativní vlhkosti (RH); 30 °C a 65 % RH a 40 °C a 75 % RH. Po 1, 3, 6, 9 a 12 měsících (nebo po 1, 3 a 6 měsících) se disoluce léčiva opakovala a porovnala s počátečními profily pomocí faktorů podobnosti. Všechny hodnoty faktorů podobnosti vyšší než 50 naznačují výbornou stabilitu obalu tvořeného natrium-alginátem a chitosanem.

Pellets containing rutin prepared by the extrusion/spheronization method were coated with sodium alginate-chitosan film. Important quality parameters in the pellets before coating were determined, and after coating the dissolution profiles of the drug were evaluated in dissolution media of the pH corresponding to the conditions in the gastrointestinal tract. Samples of coated pellets were located in the boxes for stability testing under different conditions, i.e. 25 °C and 60% of relative humidity (RH); 30 °C and 65% RH and 40 °C and 75% RH. After 1, 3, 6, 9 and 12 months (or 1, 3 and 6 months), the dissolution test was repeated and compared with the original profiles using similarity factors. All similarity factor values above 50 indicate excellent stability of alginate-chitosan films.

• Keywords
• transport léčiv do kolonu,
• MeSH
• Alginates MeSH
• Chitosan MeSH
• Dosage Forms MeSH
• Drug Delivery Systems methods   MeSH
• Humans MeSH
• Surface Properties MeSH
• Rutin administration & dosage   MeSH
• Drug Stability MeSH
• Intestine, Large MeSH
• Check Tag
• Humans MeSH
• Publication type
• Review MeSH

Farmakoterapie nespecifických střevních zánětů je zdlouhavá, často celoživotní, doprovázená nežádoucími účinky, které jsou důsledkem vysokých dávek podávaných léčiv a jejich systémové absorpce v tenkém střevě. Vývoj lékové mikroformy, která by specifickydoručila léčivo do místa jeho lokálního působení, by přispěl k vyšší efektivitě terapie, snížení vedlejších účinků a zvýšení compliance pacientů. Výhodou lékové mikroformy založené na chitosanu je mimo transportu léčiva do nemocného místa (úloha obalu)také možnost vazby léčivých částic na střevní mucin a tím prodloužené působení léčivé látky v požadovaném místě. Jako léčivé látky se vybraly standardní kyselina 5-aminosalicylová a rutin s antioxidačními účinky. Součástí projektu je i vývoj nové disoluční metody pro hodnocení uvolňování léčiva z chitosanových mikropelet.; Pharmacotherapy of inflammatory bowel disease is long-term, often lifelong, accompanied with side-effects, which are a consequence of high doses of administered drugs and their systemic absorption in small intestine. Development of drug microform, that would deliver its drug into the specific site of its local action, would contribute to the increased effectivity of the therapy, reduction of unwanted effects and improvement of patient compliance. Besides the drug transport into the diseased site, the drug microform based on chitosan is advantageous also because of the possibility to be binded to the intestinal mucine and thus prolong the drug action in the demanded place. Standard drug 5-aminosalicylic acid and rutin with antioxidative effects were chosen as the model drugs. Project is also concentrated on the development of a new dissolution method for drug release evaluation from chitosan micropellets.

• MeSH
• Chitosan MeSH
• Flavonoids administration & dosage   therapeutic use   MeSH
• Inflammatory Bowel Diseases drug therapy   MeSH
• Salicylic Acid administration & dosage   therapeutic use   MeSH
• Drug Delivery Systems MeSH
• Polymers MeSH
• Rutin administration & dosage   therapeutic use   MeSH

• Conspectus
• Farmacie. Farmakologie
• NML Fields
• gastroenterologie
• farmakoterapie
• farmacie a farmakologie
• NML Publication type
• závěrečné zprávy o řešení grantu IGA MZ ČR

Chronická žilní choroba je onemocnění chronické, progresivní, s poměrně nízkou mortalitou, ale vysokou morbiditou, která je spojena s vysokými léčebnými náklady. Výskyt chronické žilní choroby (CVD) v populaci souvisí se stylem života moderní společnosti a narůstá u obou pohlaví téměř lineárně s věkem. Příčina vzniku CVD je multifaktoriální a představuje kombinaci vnitřních a vnějších vlivů. Vlastní příčinou CVD je reflux, obstrukce nebo obojí v povrchových žilách, v hlubokém žilním systému a v perforátorech. Dochází ke vzniku žilní hypertenze s odezvou v makrocirkulaci, mikrocirkulaci a v lymfatických cévách. Klinické projevy jsou rozmanité. Léčbu CVD lze rozdělit na konzervativní a chirurgickou. Konzervativní léčba varixů spočívá v režimových a dietních opatřeních, elevaci a kompresi dolních končetin a ve farmakoterapii. Podávání venoaktivních látek je indikováno u symptomatických pacientů s chronickým žilním onemocněním. K odstranění žilního refluxu v pokročilejších stadiích CVD je nutno přistoupit k chirurgickému řešení.

with relatively low mortality but high morbidity which is associated with high health care costs. The occurrence of chronic venous disease (CVD) in population seems to be related to the life style of modern society and it increases almost linearly with age in both sexes. The origin of CVD appears to be multifactorial and embodies a combination of intrinsic and extrinsic factors. The principal cause of CVD is a reflux, obstruction or both in superficial veins, in perforators and in deep venous system. Venous hypertension ensues with its impact on macrocirculation, microcirculation and on lymphatic veins. Clinical symptoms vary. The treatment of CVD involves both medical and surgical approaches. Conservative approach includes life style and dietary arrangements, elevation and compression of lower extremities and pharmacotherapy. Venoactive substances are indicated in symptomatic patients with chronic venous disease. Venous reflux in advanced stages of CVD can only be managed surgically.

• Keywords
• kompresivní léčba, chirurgická léčba,
• MeSH
• Arterial Occlusive Diseases drug therapy   complications   therapy   MeSH
• Chronic Disease MeSH
• Diet, Atherogenic MeSH
• Diosmin pharmacology   therapeutic use   MeSH
• Drug Therapy MeSH
• Ginkgo biloba MeSH
• Hesperidin pharmacology   therapeutic use   MeSH
• Stockings, Compression utilization   MeSH
• Humans MeSH
• Vascular Diseases drug therapy   complications   therapy   MeSH
• Peripheral Vascular Diseases drug therapy   complications   therapy   MeSH
• Rutin administration & dosage   adverse effects   therapeutic use   MeSH
• Sclerotherapy methods   utilization   MeSH
• Varicose Veins drug therapy   complications   therapy   MeSH
• Leg Ulcer drug therapy   complications   therapy   MeSH
• Vascular Surgical Procedures methods   utilization   MeSH
• Check Tag
• Humans MeSH