Highly hydrophilic 1,3-oxazol-5-yl benzenesulfonamide inhibitors of carbonic anhydrase II for reduction of glaucoma-related intraocular pressure
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01.11.2019 |
Kalinin S.
Valtari A.
Ruponen M.
Toropainen E.
Kovalenko A.
Nocentini A.
Gureev M.
Dar'in D.
Urtti A.
Supuran C.
Krasavin M.
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Bioorganic and Medicinal Chemistry |
10.1016/j.bmc.2019.115086 |
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© 2019 Elsevier Ltd Four inhibitors of human carbonic anhydrase II (hCA II) were designed based on the previously reported subnanomolar 1,3-oxazole-based sulfonamide inhibitors of the enzyme to incorporate primary and secondary amine functionality in the carboxamide side chain. The new hydrophilic compounds were found to inhibit the target isoform in sub-nanomolar to low nanomolar range with a good degree of selectivity to several other hCA isoforms. The hydrophilic character of these compounds is advantageous for intraocular residence time but not for corneal permeability which generally requires that a drug be sufficiently lipophilic. Two of the four compounds investigated, however, were found to exert comparable efficacy as 1% eye drops in PBS to that of the clinically used 2% dorzolamide (Trusopt®) eye drops. This indicated that the absorption of the compounds may occur via alternative route across conjunctiva and sclera.
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Population-Based Analysis of Cluster Headache-Associated Genetic Polymorphisms
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01.07.2018 |
Katsarou M.
Papasavva M.
Latsi R.
Toliza I.
Gkaros A.
Papakonstantinou S.
Gatzonis S.
Mitsikostas D.
Kovatsi L.
Isotov B.
Tsatsakis A.
Drakoulis N.
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Journal of Molecular Neuroscience |
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© 2018, Springer Science+Business Media, LLC, part of Springer Nature. Cluster headache is a disorder with increased hereditary risk. Associations between cluster headache and polymorphism rs2653349 of the HCRTR2 gene have been demonstrated. The less common allele (A) seems to reduce disease susceptibility. The polymorphism rs5443 of the GNB3 gene positively influences triptan treatment response. Carriers of the mutated T allele are more likely to respond positively compared to C:C homozygotes, when treated with triptans. DNA was extracted from buccal swabs obtained from 636 non-related Southeastern European Caucasian individuals and was analyzed by real-time PCR. Gene distribution for the rs2653349 was G:G = 79.1%, G:A = 19.2%, and A:A = 1.7%. The frequency of the wild-type G allele was 88.7%. The frequencies for rs5443 were C:C = 44.0%, C:T = 42.6%, and T:T = 13.4%. The frequency of the wild-type C allele was 65.3%. The frequency distribution of rs2653349 in the Southeastern European Caucasian population differs significantly when compared with other European and East Asian populations, and the frequency distribution of rs5443 showed a statistically significant difference between Southeastern European Caucasian and African, South Asian, and East Asian populations. For rs2653349, a marginal statistically significant difference between genders was found (p = 0.080) for A:A versus G:G and G:A genotypes (OR = 2.78), indicating a higher representation of male homozygotes for the protective mutant A:A allele than female. No statistically significant difference was observed between genders for rs5443. Cluster headache pathophysiology and pharmacotherapy response may be affected by genetic factors, indicating the significant role of genotyping in the overall treatment effectiveness of cluster headaches.
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Interchangeability Issues with Glaucoma Medicines Using Latanoprost as an Example
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01.02.2018 |
Bunyatyan N.
Filippova O.
Romanov B.
Prokof’ev A.
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Pharmaceutical Chemistry Journal |
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© 2018, Springer Science+Business Media, LLC, part of Springer Nature. The possible interchangeability of eye drops was analyzed using glaucoma medicines containing latanoprost as examples. It was shown that the reference and generic drugs could be identical with respect to composition of active ingredients when manufactured from the same pharmaceutical substance but could differ in the excipient composition, in particular, have a different buffer and osmolality that could produce differences in their clinical effects. An analysis of the literature showed that the therapeutic efficacy and safety could vary for pharmaceutically equivalent drugs. The lack of therapeutic equivalence on the background of pharmaceutical equivalence could be caused by the use of different packaging and different dosing systems. Therefore, results from clinical trials must be compared to confirm the interchangeability of eye drops.
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Comparison of Pharmacokinetics, Bioequivalence, and Safety of Femorix<sup>®</sup>(Valenta Pharm Company, Russia) and Aubagio<sup>®</sup>(Sanofi Winthrop Industrie, France) Film-Coated Tablets (14 mg)
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01.02.2018 |
Reikhart D.
Arnautov V.
Belostotskii A.
Globenko A.
Lopukhov I.
Torshina E.
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Pharmaceutical Chemistry Journal |
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© 2018, Springer Science+Business Media, LLC, part of Springer Nature. The pharmacokinetics, bioequivalence, and safety of Femorix®(Valenta Pharm Co., Russia) and Aubagio®(SanofiWinthrop Industrie, France) film-coated tablets (14 mg) were compared in a double-blind randomized investigation in parallel groups of healthy volunteers. The bioavailabilities of Femorix®film-coated tablets (14 mg, Valenta Pharm Co., Russia) were 96.18% [87.92 – 105.22%] for ln(Cmax) and 96.24% [88.67 – 104.44%] for ln(AUC0–72) of those for Aubagio®film-coated tablets (14 mg, Sanofi Winthrop Industrie, France), which fell in the commonly accepted range (80 – 125%) for proving the bioequivalence of the tested products.
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The work of the american medical detachment as а part of the Russian army on the Caucasian front during World War I
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01.01.2018 |
Chizh I.
Karpenko I.
Sergeeva M.
Fedoseikin I.
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History of Medicine |
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© Ivan M. Chizh, Igor V. Karpenko, Maria S. Sergeeva, Ilya V. Fedoseikin. The article covers a little-known episode from World War I, concerning the work of one of the foreign detachments (hospitals) in the Russian Tsarist army. The large-scale sanitary losses and epidemics of infectious diseases, which accompanied the war, required special efforts from the medical service of the Russian army. The Russian Red Cross Society (RRCS), which had monopoly rights to organize medical care during the war, did not cope with the problems that arose. In connection with this, the international community, primarily the medical personnel of neutral and allied states, in particular, England and America, played a big role in the provision of medical care to the wounded Russian army. The activities of foreign doctors, nurses and hospitals were carried out under the auspices of the RRCS in the framework of the humanitarian assistance that allies provided to Russia during World War I. Based on archival documents and materials from RRCS periodicals for 1914–1917, the activities of the medical unit of the North American United States in the Caucasian theater of military operations and the American hospital organized by it on the territory of Persia (the town of Khoy) are investigated. The materials under review single out a number of problems in the provision of medical assistance to the troops of the Caucasian Front, requiring special urgency and unprecedented work from the American specialists in Khoy. Throughout the period under review, anti-epidemic, clinical, evacuation and charitable activities predominated the detachment’s work. Doctors and nurses of the detachment risked their lives in performing their duties during typhus epidemics. It is noted that in addition to American doctors and nurses, Russian doctors and nurses worked at the hospital.
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Optical coherence tomography for examination of glaucoma surgery site
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01.01.2018 |
Avetisov S.
Petrov S.
Volzhanin A.
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Vestnik oftalmologii |
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The article reviews the results of using optical coherence tomography (OCT) - a non-invasive non-contact examination method for obtaining a tomographic slice image of the site of glaucoma surgery. The method helped reveal the functional relationships between the newly created outflow pathways and various parameters of the filtering bleb such as its linear dimensions, wall structure, presence of microcysts, position of drainage, etc. Due to its high resolution and noninvasiveness, OCT can be reliably used to examine the structure of aqueous outflow pathways in different postoperative periods with accuracy close to morphometric. The amount of data that had been obtained with the method has allowed the creation of new classifications and clarification of OCT-relevant prognostic signs for glaucoma surgery site.
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Influence of cataract phacoemulsification on eye hydrodynamics in patients with prior trabeculectomy
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01.01.2018 |
Avetisov S.
Erichev V.
Petrov S.
Volzhanin A.
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Vestnik Oftalmologii |
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© 2018, Media Sfera. All rights reserved. At present, phacoemulsification and trabeculectomy are the most widespread surgery methods in cataract and glaucoma treatment, generally recognized as the gold standard. Among elderly patients, comorbid glaucoma and cataract are extremely prevalent, so the order of the two surgeries and the time interval between them are pivotal choices when planning treatment strategy. The reason for it is that almost any eye surgery is considered a risk factor for long-term trabeculectomy effectiveness. In attempts to solve this problem, numerous studies have been conducted on the impact of cataract surgery on filtration bleb scarring. The problem of determining the time interval between surgeries, as well as other treatment nuances, remains relevant despite the long history of research and publications. Some results are cited as general recommendations on treatment tactics (increasing the time interval between operations, using antimetabolite and anti-inflammatory therapy, minimizing intraoperative traumatism). However, currently there are no specific recommendations for one of the most important factors - the time interval between cataract extraction and trabeculectomy.
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Effects of artificial tears on ocular surface in glaucomatous patients with long-term instillation of preserved antiglaucoma eye drops
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01.01.2018 |
Makashova N.
Vasilieva A.
Kolosova O.
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Vestnik Oftalmologii |
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© 2018 Media Sfera. All rights reserved. Purpose. To study the effects of long-term instillation of 0.18% sodium hyaluronate artificial tears VISMED multi on ocular surface in glaucomatous patients with long-term instillation of preserved anti-glaucoma drops. Material and methods. The study included 79 patients (40 female and 39 male; 79 eyes in total) with primary open-angle glaucoma (POAG) divided into 3 groups according to disease stage: mild or early (stage I) glaucoma - 15 patients (15 eyes), moderate (stage II) glaucoma - 30 patients (30 eyes), advanced or severe (stage III) glaucoma - 34 patients (34 eyes). Conjunctival and corneal changes were assessed with Norn's test, Schirmer I test and corneal fluorescein staining test. All patients completed Ocular Surface Disease Index (OSDI) questionnaire. Corneal compensated intraocular pressure (IOPcc) was measured using Ocular Response Analyzer (ORA) (Reichert Optics Inc., USA). In addition to hypotensive therapy, all patients received instillations of 0.18% sodium hyaluronate (VISMED multi) three times every day. After 14 days, all examinations were repeated. Results. The condition of eye surface in patients with moderate and advanced (stage II and III) glaucoma depends on the degree of IOPcc compensation. As glaucoma increases in severity, the pathological changes in the ocular surface progress. Instillations of 0.18% sodium hyaluronate solution lead to significant improvement of the test results in all groups, and in early glaucoma patients it restores all objective indicators to normal values. Conclusion. Treatment with 0.18% sodium hyaluronate solution (VISMED multi) leads to statistically significant (p<0.05) improvement of ocular surface condition in glaucoma patients with long-term instillation of preserved antiglaucoma eye drops.
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Specific features of collagen implant biodegradation after glaucoma surgery in rabbit eye (experimental study)
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01.01.2018 |
Mamikonyan V.
Fisenko N.
Demura T.
Kogan E.
Kazaryan E.
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Eksperimental'naya i Klinicheskaya Farmakologiya |
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© 2018 Izdatel'stvo Meditsina. All rights reserved. The healing process in the adult rabbit conjunctiva and sclera tissues after translimbal microdrainage with the use of either biodegradable antiglaucomatous drainage (BDAD) or iGen was studied. Wound areas showed similar acute inflammatory response to the implantation of both matrixes on the 7th day. Complete lysis degradation of iGen and BDAD was observed on 30th day and 60th day, respectively. Within 60 - 90 days after BDAD implantation, the wound areas of conjunctiva and sclera showed intensive angiogenesis and poor extracellular matrix scarring. In contrast, on the 90th day after iGen implantation, a decrease in angiogenesis and intensive extracellular matrix scar formation were observed. As a result of scarring the thin-walled vessels were compressed, which led to the reduction of aqueous humor outflow.
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