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[Clinical and experimental study of clofelin pharmacodynamics].

Hemodynamic mechanisms of clophelin hypotensive effect were studied in 122 patients with arterial hypertension. In most cases, antihypertensive clophelin therapy did not affect the nature or magnitude of orthostatic and stress-induced hemodynamic shifts. The fact that the fall in perfusion BP was not accompanied with a resting, orthostatic or stress-induced impairment of renal function was a particularly valuable aspect of clophelin treatment. Experimental studies demonstrated that clophelin hypotensive effect was partly due to limited Ca2+ entrance through the slow calcium channels in the cel

Role of drugs modifying sympathetic nervous system activity in the treatment of hypertension.

The major sites of action in the nervous system of the various types of drug used in the treatment of hypertension were considered, together with some of their advantages and disadvantages. Consideration was given to the way in which the circulation may be controlled, particularly in hypertension, and the difficulties of using various drugs to analyse controlling mechanisms. The assessment of sympathetic activity and over-activity was also considered, since this remains an area of great difficulty, both in man and in other animals.

Accumulation of 3H-adrenaline by rabbit aorta.

The accumulation of (-)-3H-adrenaline (3H-A) by rabbit isolated aorta was studied. In all experiments, monoamine oxidase and catechol-O-meth … , respectively. The maximal degree of inhibition was almost the same for these drugs, while that of clonidine and corticosterone was 50 and 20%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Tizanidine as an Adjunct to Alpha-Blockers in Adults With Dysfunctional Voiding/Poor Relaxation of the External Sphincter: A Retrospective Review.

BACKGROUND: Skeletal muscle relaxants (SMR), particularly baclofen, have been used in patients with dysfunctional voiding (DV) and poor relaxation of the external sphincter (PRES) with variable efficacy and notable side effects. Tizanidine, a centrally acting α2-adrenergic agonist, may offer comparable benefits with a more favorable tolerability profile. However, data regarding its use in DV remain limited. METHODS: This retrospective analysis included adults diagnosed with DV/PRES between July 2017 and January 2025. Data comprised demographics, lower urinary tract symptoms (LUTS), urodynamic

Fabrication and characterization of matrix type transdermal patches loaded with tizanidine hydrochloride: potential sustained release delivery system.

OBJECTIVE: This study was designed to optimize and develop matrix type transdermal drug delivery system (TDDS) containing tizanidine hydrochloride (TZH) using different polymers by solvent evaporation method. SIGNIFICANCE: A strong need exists for the development of transdermal patch having improved bioavailability at the site of action with fewer side effects at off-target organs. METHODS: The patches were physically characterized by texture analysis (color, flexibility, smoothness, transparency, and homogeneity), in vitro dissolution test and FTIR analysis. Furthermore, functional properti

Oral contraceptives containing ethinyl estradiol and gestodene markedly increase plasma concentrations and effects of tizanidine by inhibiting cytochrome P450 1A2.

BACKGROUND AND OBJECTIVE: Oral contraceptives (OCs) can inhibit drug metabolism, but their effect on various cytochrome P450 (CYP) enzymes and drugs can be different. Our objective was to study the effect of combined OCs, containing ethinyl estradiol (INN, ethinylestradiol) and gestodene, on CYP1A2 activity, as well as their interaction potential with tizanidine. METHODS: In a parallel-group study, 15 healthy women using OCs and 15 healthy women without OCs (control subjects) ingested a single dose of 4 mg tizanidine. Plasma and urine concentrations of tizanidine, as well as several of its me

Newer antidepressants and other nonhormonal agents for the treatment of hot flashes.

The reluctance to use estrogen in breast cancer survivors with hot flashes has extended to its use in healthy women since the 2002 publication of the Women's Health Initiative study. This article reviews the clinical development of nonhormonal agents as alternatives to hormonal therapy for the management of hot flashes.

Interactions between leptin and the human sympathetic nervous system.

Results from animal experimentation suggest a 2-way interaction between leptin and the sympathetic nervous system, with leptin causing sympathetic activation and conversely, with the sympathetic system exercising regulatory feedback inhibition over leptin release. We have now tested this hypothesis in humans. In the absence of results from leptin infusions, to test for sympathetic stimulation of leptin release, we sought a quantitative naturalistic linkage of sympathetic activity with leptin plasma concentration across a broad range of leptin values in men of widely differing adiposity. Renal

The comparative ocular hypotensive effect of apraclonidine with timolol maleate in exfoliation versus primary open-angle glaucoma patients.

PURPOSE: To compare the effect of adding apraclonidine 0.5% to timolol maleate 0.5% in patients with exfoliation versus primary open-angle glaucoma. Since exfoliation glaucoma is known to demonstrate higher pressures than primary open-angle glaucoma on timolol maleate therapy alone, the authors wished to determine whether apraclonidine equalised the intraocular pressure (IOP) between these two glaucomas when added to timolol maleate. METHODS: We age-matched 30 consecutive exfoliation and 30 primary open-angle glaucoma patients who had an IOP > or = 22 mmHg on timolol maleate alone. Patients u…

Novel selective compounds for the investigation of imidazoline receptors.

Over several years our group has sought to synthesize and identify selective ligands for imidazoline (I) receptors, in particular the I2 binding site. As a consequence, [3H]2-(2-benzofuranyl)-2-imidazoline (2BFI) has proved extremely useful for binding and autoradiographic studies. More recently we have synthesized a BU series of compounds and examined these for their affinities for both I1 and I2 binding sites. BU224 (2-(4,5-dihydroimidaz-2-yl)-quinoline) shows high affinity for I2 receptors with a Ki of 2.1 nM. BU226 (2-(4,5-dihydroimidaz-2-yl)-isoquinoline) demonstrated slightly higher affi

Rat pineal alpha 1-adrenoceptor subtypes: studies using radioligand binding and reverse transcription-polymerase chain reaction analysis.

1. The pharmacological characteristics of alpha 1-adrenoceptor binding sites in rat pineal gland membranes, detected by use of a selective alpha 1-adrenoceptor antagonist ([125I]-iodo-2-[beta-(4-hydroxyphenyl) ethylaminomethyl]tetralone, [125I]-HEAT), were investigated with the alkylating agent, chloroethylclonidine (CEC), and in competition experiments with a number of adrenoceptor agonists and antagonists. 2. Chloroethylclonidine (CEC) treatment (10 microM, 10 min) of rat pineal membranes inactivated approximately 70% of specific [125I]-HEAT binding sites. Higher concentrations of CEC (up to…

Can opiate addicts tell us about their relapse risk? Subjective predictors of clinical prognosis.

Given the high relapse rate of opiate addicts following detoxification, it is pertinent to identify whether any subjective variables mediate outcome, since these may then be targets of treatment. The present study assessed personality, cue-elicited craving, outcome expectancies for drug use, and self-efficacy for resisting drug use, in 43 opiate addicts receiving inpatient detoxification in either a specialist drug-dependence unit or a behavioral/general psychiatric ward, within the context of a randomised, controlled-treatment trial. Subjects were followed-up at between 1 and 3 months and aga

Local regulation of transmitter release from rodent sympathetic nerve terminals?

1. Electrophysiological techniques were used to observe the release of transmitter from single release sites in the sympathetic neuro-effector junction of the rodent vas deferens. Transmitter release produces transient peaks in the rate of depolarization of the smooth muscle cells, known as 'discrete events'. 2. The amplitude distributions of stimulus-evoked discrete events in both mouse and guinea-pig vas are multi-modal. In the mouse, the distribution fits a Poisson with a 'quantal content' of about two. There are too many zeros in the amplitude distributions of guinea-pig discrete events to

Pentoxifylline for diabetic kidney disease.

BACKGROUND: Diabetic kidney disease (DKD) is associated with increased morbidity and mortality, mostly relating to cardiovascular complicati … MD 1.37 mm Hg, 95% CI -0.23 to 2.98) between pentoxifylline and the active comparator (captopril or clonidine/methyldopa) for patients with type 1 and type 2 DKD. CrCl was significantly increased when pentoxifylline was compared to clonidine/methyldopa (MD 10.90 mL/min, 95% CI -1.40 to 20.40) but not with captopril (MD 3.26 mL/min, 95% CI -1.05 to 7.59). No …

Сексуальные отношения с лицами, страдающими расстройством бдительности: обзор.

Целью этого обзора повествования является проведение синтетического обзора современных знаний о взаимосвязи между расстройством гиперактивности (АДХД) и сексуальным функционированием взрослых с уделением особого внимания нейробиологическим механизмам, коморбидным расстройствам и воздействию фармакотерапии. Шесть независимых исследователей провели всеобъемлющий обзор литературы с использованием баз данных PubMed, Scopus и Google Scientist, охватывающих публикации, имеющиеся по состоянию на май 2024 года. Были включены первоначальные исследовательские документы, обзоры и метаанализы на английско

Совпадение в аннотации оригинала
This narrative review aimed to provide a synthetic overview of current knowledge on the relationship between attention-deficit hyperactivity … imulant drugs (e.g., methylphenidate and lisdexamfetamine) and nonstimulants (e.g., atomoxetine and clonidine) demonstrate both beneficial and adverse impacts on sexual functioning, although empirical data are limited. ADHD shows a significant correlation with the occurrence of a wide spectrum of sexual disorders, which requires consideration in diagnostics …

Not first-line antihypertensive agents, but still effective-The efficacy and safety of imidazoline receptor agonists: A network meta-analysis.

Cardiovascular disorders are the leading cause of death in the world. Many organ diseases (kidney, heart, and brain) are substantially more … azoline receptor agonists. After 8 weeks of treatment, the appearance of dry mouth was highest with clonidine (OR: 9.27 95% CI: 4.70-18.29) and lowest with rilmenidine (OR: 6.46 95% CI: 0.85-49.13) compared to placebo. Somnolence was less frequent with moxonidine compared to rilmenidine (OR: 0.63 95% CI: 0.17-2.31). Imidazoline receptor agonists were nearly …

Leptin Does Not Influence TSH Levels in Obese Short Children.

INTRODUCTION: Growth hormone (GH) and thyroid hormones are important for children growing. In some obese children a slightly elevated TSH co … han 10 mIU/L), with a similar frequency across subgroups. The higher the leptin, the lower maxGH in clonidine stimulation test was recorded. CONCLUSIONS: It seems that in obese children with idiopathic short stature leptin does not increase TSH secretion. This may be related to a disruption of the effect of leptin on TSH production and could indicate wide …

Target-Controlled Inhalational Anesthesia-Isoflurane Consumption with Adequacy of Anesthesia Monitoring in Conventional and Multimodal Analgesia - A Comparative Study.

BACKGROUND: In a time of increased concern over the environmental impact of chlorofluorocarbons, there is an impetus to minimize inhalationa … d 2% xyloadrenaline infiltration at entry ports. MMA group in addition received paracetamol 1 g and clonidine 0.75 μg.kg- 1. Intraoperatively, patients were on EtCA with AoA monitoring. STATISTICAL ANALYSIS: Mean differences in isoflurane consumption between the two groups were compared using an independent t-test. Postextubation adverse effects of analges …