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Olomouc, Czech Republic

The medicinal product Relvar Ellipta is a new dry powder inhaler containing a new fixed combination of the inhaled corticosteroid fluticasone furoate (FF) and the selective ultra-long-Acting, 2-Adrenergic agonist vilanterol. The article summarizes the most interesting data from the preclinical development and phase I clinical evaluation of both molecules. Among the modern inhaled corticosteroids, FF has the highest affinity towards the glucocorticoid receptor. In preclinical testing in vitro and in vivo, the glucocorticoid activity of FF was stronger and it had longer duration than that of fluticasone propionate. The inhaled particles of FF dissolve very slowly bringing two major advantages. First, the pulmonary residence time is two-fold longer than that of fluticasone propionate making a once-daily inhalation possible and, second, the slower rate of absorption results in very low concentrations of FF in the blood. The safety profile of FF is further supported with the high velocity of hepatic elimination, biotransformation to inactive metabolites, negligible oral bioavailability and extensive binding to plasma proteins. Preclinical and clinical evaluation of vilanterol was able to document its improved pharmacodynamic characteristics in comparison to salmeterol. Namely, the intrinsic activity of vilanterol is higher and its effect has a more rapid onset and a longer duration. Both the extraordinary 2-selectivity and appropriate pharmacokinetic characteristics (fast hepatic elimination, conversion to inactive metabolites, short half-life, minimal oral bioavailability) are responsible for a favorable safety profile of vilanterol. The duration of action over 24 h following inhalation is ascribed to the high-Afinity binding of vilanterol to specific binding sites on the 2-receptor which enables its retention nearby and a repeated interaction with the receptors active site. Source


Bultas J.,Ustav farmakologie
Casopis Lekaru Ceskych | Year: 2015

Mountaineering brings many health risks, one of which is mountain sickness. Its mildest form - acute mountain sickness - is mainly characterized by subjective symptoms (headache, loss of appetite, insomnia, weakness, nausea and rarely also vomiting). Advanced and life-threatening forms are characterized by tissue edema - cerebral or pulmonary high altitude edema. The common denominator of these acute forms is the low oxygen tension leading to hypoxemia and tissue ischemia. Sum of maladaptive or adaptive processes can modify the clinical picture. Underlying mechanisms of the chronic forms of pulmonary disease are the adaptation processes - pulmonary hypertension and polycythemia leading to heart failure. The only causal therapeutic intervention is to restore adequate oxygen tension, descend to lower altitudes or oxygen therapy. Pharmacotherapy has only a supportive effect. The prophylaxis includes stimulation of the respiratory center by carbonic anhydrase inhibitors (acetazolamide) antiedematous treatment with glucocorticoids (dexamethasone), increase lymphatic drainage of the lungs and brain by β2-agonists (salmeterol) or mitigation of pulmonary hypertension by calcium channel blockers or phosphodiesterase-5 inhibitors (sildenafil or tadalafil). Source


Sliva J.,Ustav farmakologie | Svacina S.,III. Interni Klinika
Interni Medicina pro Praxi | Year: 2016

The progress in the treatment of diabetes mellitus during last decade has been unprecedented, especially in the field of new oral antidiabetics. A high evidence of their effectiveness is needed for their successful clinical use as well as the evidence of their safety. In accordance to regulations of EMA and FDA, their cardiovascular safety has to be newly proven. Hence, the article summarizes most recent information from this topic, which was extensively discussed during last calendar year. Source


Bencova A.,Klinika Pneumologie a Ftizeologie | Antosova M.,Ustav farmakologie | Kocan I.,Klinika Pneumologie a Ftizeologie | Rozborilova E.,Klinika Pneumologie a Ftizeologie
Studia Pneumologica et Phthiseologica | Year: 2014

The prevalence of chronic obstructive pulmonary disease (COPD) has been increasing both globally and in our country. It represents a serious problem because of its rising prevalence, morbidity, mortality and treatment costs. COPD is multi-component disease associated with several extrapulmonary manifestations which create conditions for development of comorbidities. Methods: A retrospective single-center study analyzing comorbidities in COPD patients hospitalized at the Clinic of Pneumology and Phthisiology, Jessenius Faculty of Medicine and University Hospital in Martin between 2007 and 2011. The data were sorted according to the involvement of organ systems and GOLD classification. The results were compared with similar studies performed worldwide. Results: The group comprised 994 patients. The most significant differences between genders were observed in musculoskeletal diseases, followed by mental disorders and gastrointestinal diseases, with female and male preponderance, respectively. The results and distribution of individual stages and comorbidities were expressed as absolute numbers and percentages and statistically analyzed. All results are shown in tables and graphs. Conclusion: The analysis showed that the most frequent comorbidity in COPD patients was cardiac diseases, with a prevalence twice that elsewhere in the world. Source


Methotrexate (MTX) is a conventional immunosuppressive drug of first choice in oral therapy of moderate-to-severe plaque psoriasis. Its use is comfortable and cost effective. The therapy improves the skin status according to the PASI score (psoriasis area and severity index) by 50% or more in up to 75% of patients. However, a high inter-individual variability in pharmacokinetics is one of the major factors responsible for either insufficient efficacy of the therapy or its premature discontinuation due to adverse effects of MTX. The review article critically evaluates the possible benefits of therapeutic drug monitoring (TDM) of MTX as a tool for personalized pharmacotherapy of psoriasis. Prospective clinical studies unraveled a relationship between the pharmacokinetics and the therapeutic effect of MTX. Recommendations on how to perform TDM were worked out and verified, which helped to improve the outcomes of the initial treatment phase (remission induction). Besides the individualization of MTX dosing, supplementation with folic acid was individually tailored only to patients with a proven folate deficit. © 2015, Ambit Media a.s. All rights reserved. Source

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