In Vitro Investigation of Binding Interactions between Albumin–Gliclazide Model and Typical Hypotensive Drugs

Type 2 diabetes management usually requires polytherapy, which increases the risk of drug-to-drug interactions. Among the multiple diabetes comorbidities, hypertension is the most prevalent. This study aimed to investigate the binding interactions between the model protein, bovine albumin, and the hypoglycemic agent gliclazide (GLICL) in the presence of typical hypotensive drugs: quinapril hydrochloride (QUI), valsartan (VAL), furosemide (FUR), amlodipine besylate (AML), and atenolol (ATN). Spectroscopic techniques (fluorescence quenching, circular dichroism) and thermodynamic experiments were employed. The binding of the gliclazide to the albumin molecule was affected by the presence of an additional drug ligand, which was reflected by the reduced binding constant of the BSA–DRUG–GLICL system. This may indicate a possible GLICL displacement and its enhanced pharmacological effect, as manifested in clinical practice. The analysis of the thermodynamic parameters indicated the spontaneity of the reaction and emphasized the role of hydrogen bonding and van der Waals forces in these interactions. The secondary structure of the BSA remained almost unaffected.

XEN 63 gel stent device in glaucoma surgery: A 5-years follow-up prospective study

Purpose: To evaluate the efficacy and safety of the XEN63 Gel Stent in patients with open-angle glaucoma (OAG). Methods: Prospective, nonrandomized, open-label, not-controlled, and single center study conducted on OAG patients who underwent glaucoma surgery with the XEN63 gel stent. The main outcome measure was intraocular pressure (IOP). Secondary end-points were number of topical ocular hypotensive drugs, percentage of patients achieving an IOP reduction ⩾20%, and treatment-related adverse events. Results: Eleven eyes from 11 patients were treated with XEN 63. Mean (95% confidence interval, CI) age was 78.8 (73.7–85.9). Two eyes (18.2%) underwent XEN alone, while nine eyes (81.8%) underwent combined XEN + cataract extraction (phacoemulsification). The median (95% CI) IOP reduction was 17.7% (−13.3% to 34.9%). At the end of the study 9 (81.8%) eyes had an IOP ⩽ 18 mm Hg, six of them without treatment. Six (54.6%) eyes obtained an IOP reduction ⩾20%. Compared to baseline, there was a significant reduction in the number of ocular hypotensive drugs ( p = 0.0039). There were no treatment-related serious adverse events. Early postoperative complications included diplopia (1), blood in endothelium (2), ocular hypertension (1), corneal edema (1), folds in Descemet’s membrane (1), and contact between the implant and the iris (1). All the adverse events were successfully solved without sequalae. One eye required bleb needling. Conclusion: The XEN63 implant significantly reduced both IOP and the amount of ocular hypotensive medications while maintaining a good safety profile.

The profile of drug treatment in subjects aged over 50 years with hypertension in an urban russian population

Objective To analyze a profile of hypotensive drug therapy in patients with arterial hypertension (АH) aged 55–84 in a sample of urban population at a current period of time (2015–2017).Materials and Methods AH is a leader among risk factors of cardiovascular diseases (CVD) due to its high prevalence and serious prognosis. Despite the availability of effective hypotensive drugs and guidelines on AH treatment, 50% of patients do not achieve blood pressure (BP) goals. Knowledge about drug correction of AH in the Russian population is limited to clinical studies. Taking into account changing approaches in management of patients with AH, the population-based evaluation of hypotensive treatment if relevant. A random population sample of males and females aged 55-84 (n=3.898) was evaluated in Novosibirsk in 2015-2017 (international project, Health, Alcohol and Psychosocial Factors in Eastern Europe (HAPIEE)). AH was diagnosed in presence of systolic BP ≥140 mm Hg or diastolic BP ≥90 mm Hg and/or treatment with hypotensive drugs within the recent two weeks. Regular intake of medication for 12 months was evaluated with coding according to the Anatomic Therapeutic Chemical Classification System (АТХ / АТС).Results In the population sample aged 55–84, AH prevalence was 80.9 %, and 21.1 % of persons with AH did not receive drug therapy. Hypotensive medicines included (total/as a part of combination therapy) angiotensin-converting enzyme (ACE) inhibitors (42.3 % / 25.3 %), angiotensin II receptor blockers (ARBs) (30.3 % / 18.9 %), diuretics (22.6 % / 20.4 %), calcium channel blockers (20.2 % / 16.1 %), and beta-blockers (34.7 % / 27.6 %). 45.7 % of people with AH received a combination therapy. Effective BP control was achieved in 23.4 % of AH patients and in 29.6 % of patients receiving a hypotensive therapy. In the group of ineffective BP control, the proportion of females was lower, AH duration was longer, and blood glucose was higher than in the group of effective control.Conclusion In the sample of urban population aged 55–84 in 2015–2017, each fourth participant with AH and each third participant using hypotensive drugs achieved effective BP control. The therapy profile in AH patients included recommended drug classes. However, combination therapy was used insufficiently (50% of AH patients). By frequency of use, ACE inhibitors were on the first place, beta-blockers were on the second place, ARBs were on the third place, diuretics were on the fourth place, and calcium channel blockers were on the fifth place, which differed from the guidelines (the difference from the recommended priority ranking is that the drugs taking the first places in the guidelines were in fact on the 3rd and 4th places in their actual frequency of use). 20% of persons with AH did not receive hypotensive therapy, which significantly contributed to the insufficient BP control in the population.

АНАЛИЗ ПРИМЕНЕНИЯ ГИПОТЕНЗИВНЫХ СРЕДСТВ ПО ДАННЫМ АНКЕТИРОВАНИЯ ПОСЕТИТЕЛЕЙ АПТЕК В г. ГРОДНО

The aim of the study is to assess the structure of use of hypotensive drugs and adherence to the antihypertensive therapy among pharmacy visitors in Grodno. Material and methods. We conducted questionnaire survey among 109 pharmacy visitors who bought antihypertensive drugs.Results. ACE inhibitors is the most widely used group of antihypertensive drugs among the pharmacy visitors in Grodno. 44% of them took one drug. The most of the pharmacy visitors used hypotensive drugs regularly; however, 19,3% respondents were non-adherent, mostly from the middle-aged group (45-59 years). Conclusion. The structure of use of antihypertensive drugs among the pharmacy visitors in Grodno complies to the international guidelines for the management of arterial hypertension. However, there are some disadvantages: 1) relatively large number of respondents use only one antihypertensive drug; 2) some respondents, especially among middle-aged persons, take antihypertensive drugs not regularly.

A milk-derived pentapeptide reduces blood pressure in advanced hypertension in a CCK system-dependent manner

Orally administered KFWGK exhibits potent and long-lasting antihypertensive effects in SHR with advanced hypertension, at which known hypotensive drugs are sometimes less effective. The minimum effective dose of KFWGK was 5 μg kg−1.

Cardiotropic action of combined use of celecoxib and amlodipine in rats sicked on adjuvant arthritis coupled with arterial hypertension

Drug therapy of rheumatoid arthritis combined with arterial hypertension is among actual medical objectives. The complexity of pharmacological treatment of comorbid state is due to not only pathological process severity, insufficient efficacy and side effects of disease modifying and symptomatic drugs but also property of nonsteroidal anti-inflammatory drugs (NSAIDs) to aggravate already existed arterial hypertension in patients with rheumatoid arthritis or to increase pressure. Many hypotensive drugs loose or don’t manifest their activity when used in combination with NSAIDs. High risk of cardio toxicity is registered for one of NSAIDs group – coxibs. The cardio safety of combined use of coxibs and hypotensive drugs on the ground of comorbid pathology is studied not enough. These aspects had predefined the aim of this study – to investigate cardiotropic effects of celecoxib when administered in combinations with amlodipine on the ground of experimental rheumatoid arthritis coupled with arterial hypertension. Arterial hypertension was modeled in rats by method of salt load. On the basis of arterial hypertension rheumatoid arthritis was caused by full Freund adjuvant injection. Arterial blood pressure and heart rate registered on sphygmomanometer. It was found that comorbid state is followed by arterial hypertension and tachyarrhythmia. Celecoxib does not facilitate hypertension enhancing but leads to increasing heart rate. Amlodipine manifests specific pharmacological activity as hypotensive drug. The results obtained predefined opportunity of combined use of celecoxib with amlodipine on the ground of rheumatoid arthritis coupled with arterial hypertension.