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Percent Inhibition (percent + inhibition)

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Medical Sciences	100%

Selected Abstracts

Activated protein C resistance determined with a thrombin generation-based test is associated with thrombotic events in patients with lupus anticoagulants

JOURNAL OF THROMBOSIS AND HAEMOSTASIS, Issue 11 2007
S. LIESTØL
Summary.,Background:,Several studies suggest that antiphospholipid antibodies interfere with the activity of activated protein C (APC). This acquired form of APC resistance has been proposed as a possible pathogenic mechanism underlying hypercoagulability associated with the antiphospholipid syndrome (APS).Objectives:,We wanted to investigate the inhibitory effect of recombinant APC (rAPC) on ex vivo thrombin generation in plasma and the modification of this effect by the presence of lupus anticoagulants (LA).Patients/Methods:,We analyzed plasmas from 81 patients with LA (52 patients fulfilling the criteria for the APS) and 91 controls. Percent inhibition of the endogenous thrombin potential (ETP) as a parameter of APC sensitivity was determined in plasmas using a thrombin generation-based APC resistance test probed with rAPC. All results were normalized using pooled normal plasma (PNP) as a reference.Results:,Normalized percent inhibition of ETP by APC was lower in patients with LA [61.4%, 95% confidence interval (CI) 45.8,74.5%] compared to controls (107.8%, 95% CI: 107.1,109.3%). In patients with LA and APS, median inhibition was lower than in patients with LA without APS (44.6%, 95% CI: 30.1,55.7% vs. 78.8%, 95% CI: 73.9,95.8%). This difference also persisted when patients on warfarin therapy were excluded from the APS subgroup.Conclusions:,APC resistance can be demonstrated with a thrombin generation-based test in a majority of patients with the LA laboratory phenotype. A history of thrombotic events in patients with LA is associated with a stronger resistance to the anticoagulant effect of APC. [source]

The effect of 5-aminosalicylic acid,containing drugs on sulfide production by sulfate-reducing and amino acid,fermenting bacteria

INFLAMMATORY BOWEL DISEASES, Issue 1 2003
Laurie M. Edmond
Abstract The toxic, bacterial metabolite sulfide is implicated in ulcerative colitis. Ulcerative colitis patients taking 5-aminosalicylic acid,containing drugs have lower fecal sulfide levels than those not taking these drugs. The effects of sulfasalazine, balsalazide, olsalazine, and 5-aminosalicylic acid on sulfide production were studied in a three-stage chemostat pulsed on days 1 to 3 with 5 g sulfasalazine (40 mM) and in pure cultures of amino acid,fermenting and sulfate-reducing bacteria. By the third day of sulfasalazine addition to the chemostat, sulfide concentrations in vessels 1 through 3 had dropped from 1.73, 1.78, and 1.43 mM to 0.01, 0.15, and 0.9 mM, respectively. In pure cultures, 50% inhibition of sulfide production from amino acids occurred at 2.5 ± 0.05 mM for sulfasalazine, 5 ± 0.2 mM for olsalazine, 6 ± 1 mM for balsalazide, and more than 20 mM for 5-aminosalicylic acid. Fifty percent inhibition of sulfide production from sulfate occurred at 0.25 ± 0.05 mM for sulfasalazine, 0.7 ± 0.2 mM for balsalazide, and 9.0 ± 1.0 mM for 5-aminosalicylic acid. The order of effectiveness of equimolar concentrations of drugs (most effective first) in this assay was sulfasalazine, then olsalazine (though given clinically at half the dose of other 5-aminosalicylic acid prodrugs) and balsalazide, and lastly 5-aminosalicylic acid. Inhibition of sulfide production by 5-aminosalicylic acid,containing drugs may contribute to their therapeutic effect in ulcerative colitis. [source]

Activated protein C resistance determined with a thrombin generation-based test is associated with thrombotic events in patients with lupus anticoagulants

Inhibitory effect of anticholinergics on the contraction of isolated caprine urinary bladder detrusor muscle

AUTONOMIC & AUTACOID PHARMACOLOGY, Issue 3 2010
N. George
Summary 1. This study investigated whether four anticholinergics which are not clinically used for relaxing the urinary bladder detrusor muscle inhibit the contraction of isolated caprine (goat) detrusor muscle: cyclopentolate (100 nm), homatropine (5 ,m), ipratropium (500 nm) and valethamate (1 ,m). 2. The effects of these anticholinergics were compared with tolterodine (3 ,m), an anticholinergic clinically used for relaxing the detrusor muscle. The inhibitory effect of each of these five anticholinergics was studied on six strips of caprine detrusor muscle made to contract with 100 ,m acetylcholine (ACh) by determining the percent inhibition of height of contraction and the area under the contractile curve (AUC). 3. It was found that all five anticholinergics inhibited the ACh-induced contraction of the caprine detrusor and that this inhibition was reversed by raising the concentration of ACh. Hence, these four anticholinergics, like tolterodine, may be useful in managing clinical conditions that require relaxation of the detrusor muscle. [source]