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Modern aspects of domperidone safety
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01.01.2018 |
Kareva E.
Serebrova S.
Drozdov V.
Kurguzova D.
Starodubtsev A.
Vasil N.
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Eksperimental'naya i Klinicheskaya Farmakologiya |
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Ссылка
© 2018 Izdatel'stvo Meditsina. All rights reserved. This review summarizes the state-of-the-art in the problem of assessment of the safety of domperidone - a prokinetic and anti-emetic drug belonging to those most widely used in clinical practice. Special attention is devoted to the potential cardiotoxicity of domperidone, mechanisms of adverse effects development, and risk factors. For reducing the risk of development of dose-dependent side effects, new drugs have been created and used so as to maintain the active agent concentration in the blood plasma within the therapeutic range. Another method of increasing the efficacy and safety of domperidone treatment is based on the potentiation effect. An example is the use of domperidone in a fixed combination with omeprazole (Omez-DSR), in which a the prokinetic is present in a modified release form, which ensures uniform delivery of the acting agent into blood flow (without drug concentration +AJM-peaks+AJQ-related to increased risk of dose-dependent adverse drug reactions.
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The perfusion of cisplatin and cisplatin structural analogues through the isolated rat heart: The effects on coronary flow and cardiodynamic parameters
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01.01.2018 |
Stojic I.
Jakovljevic V.
Zivkovic V.
Srejovic I.
Nikolic T.
Jeremic J.
Jeremic N.
Djuric D.
Radonjic K.
Labudovic-Borovic M.
Bugarcic Z.
Bogojeski J.
Novokmet S.
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General Physiology and Biophysics |
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Ссылка
© 2018, Slovak Academy of Sciences. All rights reserved. The therapeutic use of cisplatin for the treatment of solid tumours is associated with organ toxicity. Amongst those, the cardiotoxicity is an occasional but very serious and severe side effect. To prevent or reduce these negative effects, many cisplatin analogues have been synthesized and evaluated in terms of being a less toxic and more effective agent. In present study, we examined the effects of cisplatin and its three analogues in the isolated rat heart to determine whether changes in the structure of the platinum complexes (changing of carrier ligands – ethylenediamine; 1,2-diaminocyclohexane; 2,2’:6’,2’’-terpyridine) can influence their cardiotoxic effects. The results of our research indicate that the introduction of aromatic rings in the structure of the platinum complexes has a negative influence on the heart function. Conversely, the other two examined complexes had less negative effects on heart function compared to cisplatin. Our findings may be of interest for a possible synthetic strategy of introducing a carrier ligand that will exert a less cardiotoxic effect.
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