The antithrombotic profile of aspirin. Aspirin resistance, or simply failure?

Altman, Raúl; Luciardi, Héctor; Muntaner, Juan; Herrera, Ramón N.

doi:10.1186/1477-9560-2-1

Cited by 97 publications

(41 citation statements)

References 89 publications

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“…However, some of them were associated with cardiovascular thrombotic events. 2 Since COX inhibition blocks one pathway of arachidonic acid metabolism, administration of COX inhibitors leads to induction of the second pathway resulting to overproduction of leucotrienes (LTs) 3 and lipoxines (LXs) via the action of LOX. LTs were found to have pro-inflammatory action.…”

Section: Introductionmentioning

confidence: 99%

“…Thus, many researchers focused on the development of dual acting COX/LOX inhibitors. 1,2,5 It has been stated that a balanced modulation of several targets can provide superior therapeutic effects and a favorable side effect profile compared to the action of a selective ligand, particularly in cases of complex diseases. 6 Licofelone, a COX-2/5-LOX inhibitor, has been evaluated in a phase III clinical trial.…”

Section: Introductionmentioning

confidence: 99%

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N-substituted [phenyl-pyrazolo]-oxazin-2-thiones as COX-LOX inhibitors: influence of the replacement of the oxo -group with thioxo- group on the COX inhibition activity of N-substituted pyrazolo-oxazin-2-ones

Geronikaki¹,

Bennamane²,

Nedjar-Kolli³

et al. 2010

Arkivoc

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Targeting to the synthesis of potent dual acting COX/LOX inhibitors as future anti-inflammatory drugs, we attempted a modification of the compounds based on docking analysis results. A substitution of the oxygen of the oxo-group of the oxazin-2-one ring by sulphur resulted in a four to over ten fold improvement of COX and LOX inhibitory action. N-phenyl derivatives exhibited the best biological properties with the 4-methoxy-phenyl derivative showing the best COX-1 and LOX inhibitory action and the 4-Br-phenyl derivative exhibiting the best COX-2 inhibitory action combined with good COX-1 and LOX inhibitory capacity.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

N-substituted [phenyl-pyrazolo]-oxazin-2-thiones as COX-LOX inhibitors: influence of the replacement of the oxo -group with thioxo- group on the COX inhibition activity of N-substituted pyrazolo-oxazin-2-ones

Geronikaki¹,

Bennamane²,

Nedjar-Kolli³

et al. 2010

Arkivoc

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“…One more large study -SELECT (Safety and Efficacy Large-scale Evaluation of COX-inhibiting Therapies) compared the gastrointestinal safety of meloxicam and pyroxecam [48]. The combined analysis of the results of some studies with participation of more than 5600 patients has confirmed that meloxicam is characterized by significantly less marked gastrointestinal toxicity compared to naproxen, diclofenac and piroxicam [16,48].…”

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confidence: 99%

The place of meloxicam in the series of modern non-steroidal anti-inflammatory drugs

2016

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The article describes the pharmacological characteristics of the first selective COX-2 inhibitormeloxicam, aspects of its mechanism of action, peculiarities of pharmacodynamics and indications, as well as the advantages of the drug compared to the classic and highly selective NSAIDs in termsNon-steroidal anti-inflammatory drugs (NSAIDs) take one of the most important places in clinical practice. The broad spectrum of NSAIDs is stipulated by the unique combination of pharmacological properties, which allow considering them one of the most widely used group of drugs [3]. NSAIDs have been successfully used in the therapy of most rheumatologic diseases. Due to their high clinical efficiency, impact on the main manifestations of the inflammatory process (pain, edema, fever), rapid clinical effect, the absence of reduction of the therapeutic efficiency during prolonged treatment they are used in cases of both inflammatory diseases − rheumatoid arthritis (RA), seronegative spondylarthrosis and in degenerative cases such as osteoarthritis (OA), osteochondrosis, diseases of paraarticular tissues [12,17].However, in spite of the obvious clinical efficiency, the use of NSAIDs has its limitations. The problem matter of the modern rheumatology is development of gastropathies against the background of the therapy by the drugs of this NSAID group; these gastropathies have a negative effect for adherence of patients to the therapy, and make them refuse from further therapy [46]. In some cases NSAID gastropathies may have real hazard for the life of patients [61]. For example, in the USA the death rate caused by the NSAID induced lesions of the gastrointestinal tract equals the death rate caused by the AIDS, and it is higher than the death rate caused by melanoma, bronchial asthma, carcinoma of the uterine cervix or lymphogranulomatosis [10]. In individuals, who take NSAIDs constantly, the frequency of erosive and ulcer changes is compared to the frequency of such pathology development in patients of the gastroenterological profile [69]. It is also generally known that different classes of NSAIDs are hepatotoxic, nephrotoxic and cardiotoxic in different degrees [4].Though the experience of the NSAID application has more than 100 years, the most important aspects of the mechanism of action of using these drugs were found out only in the 70-th of the last century [6]. It has been determined that the most important link of the mechanism of the NSAID action is their ability to inhibit the activity of cycloxygenase (COG) enzyme and thereby to reduce the synthesis of prostaglandins (PG) and other mediators of inflammation. According to the modern conception, COG is a multienzyme complex, including dioxygenase, isomerase, reductase and other components. COG is a hemoprotein located within the endoplasmic reticulum near the sites of arachidonic acid release from membranous phospholipids under the influence of phospholipase enzyme A2. In the presence of molecular oxygen and a number of co-factors COG catalyzes two key reactions in transf...

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“…Acetylsalicylic acid irreversibly inhibits platelet function for the duration of the life of the platelets which is known to be 10 days [12], so the 7 days might have been too short. The begin of symptoms on day 3 which is day 10 after acetylsalicylic acid has been stopped suggests no influence on this bleeding.…”

mentioning

confidence: 99%

“…The observations may indicate a competitive interaction between the two drugs. In vivo experiments showed that intravenously administered metamizol was an effective antiplatelet drug and can be considered as a therapeutic alternative, when acetylsalicylic acid cannot be used in oral form [12] [16].…”

mentioning

confidence: 99%

Can High Dose Metamizol Medication Contribute to Postsurgical Hemorrhage:A Case Report

Wildpaner¹,

Flueckiger²,

Schmid³

et al. 2015

OJMN

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The use of metamizol significantly increased in the last decade, especially in non US countries [1]. Although metamizol is known to be a non selective COX inhibitor and therefore has platelet inhibiting potential, it is widely used in pain management in postsurgical setting. Methods: We present a case of bleeding after microsurgical decompression of a narrow lumbar spinal canal. Our patient developed a bleeding complication 3 days after the surgery. The bleeding spontaneously resolved after stopping the application of metamizol. Metamizol is a non selective COX inhibitor and is used as standard analgetic drug after surgery in our department, whereas other COX inhibitors are not. We made an intensive literature research to evaluate the prohaemorrhagic potential of metamizol. Metamizol has proven dose dependent platelet inhibiting effect. Conclusions: This is a quite ordinary case and there is no proof of metamizol being responsible for the bleeding in this case, it still poses questions at our daily routine and the question about a dose dependent clinically relevant prohaemorrhagic effect of metamizol remains unanswered. A proper study is needed.

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The antithrombotic profile of aspirin. Aspirin resistance, or simply failure?

Cited by 97 publications

References 89 publications

N-substituted [phenyl-pyrazolo]-oxazin-2-thiones as COX-LOX inhibitors: influence of the replacement of the oxo -group with thioxo- group on the COX inhibition activity of N-substituted pyrazolo-oxazin-2-ones

N-substituted [phenyl-pyrazolo]-oxazin-2-thiones as COX-LOX inhibitors: influence of the replacement of the oxo -group with thioxo- group on the COX inhibition activity of N-substituted pyrazolo-oxazin-2-ones

The place of meloxicam in the series of modern non-steroidal anti-inflammatory drugs

Can High Dose Metamizol Medication Contribute to Postsurgical Hemorrhage:A Case Report

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