Drug/drug interaction of common NSAIDs with antiplatelet effect of aspirin in human platelets

Saxena, Aaruni; Balaramnavar, Vishal M.; Hohlfeld, Thomas; Saxena, Anil Kumar

doi:10.1016/j.ejphar.2013.09.032

Cited by 70 publications

(59 citation statements)

References 37 publications

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“…Supported by molecular docking simulations, this work reveals that none of the derivatives were able to bind residues from the COX-1 catalytic site. Although interactions with both ARG120 and TYR355 were observed, the literature reports that such interactions are only significant for molecules capable of occupying the hydrophobic cavity of COX-1, ultimately blocking ARA interaction with TYR385 tyrosyl radical 59 a feature that is absent for all ligandenzyme complexes with the molecules presented herein, as they are not capable of docking to the vicinity of the active site.…”

Section: Discussionmentioning

confidence: 84%

Antiplatelet pyrazolopyridines derivatives: pharmacological, biochemical and toxicological characterization

Saito

Lourenço

Dias

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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Platelet aggregation is one of the main events involved in vascular thrombus formation. Recently, N 0 -substituted-phenylmethylene-3-methyl-1,6-diphenyl-1H-pyrazolo [3,4-b]pyridine-4-carbohydrazides were described as antiplatelet derivatives. In this work, we explore the properties of these antiplatelet agents through a series of pharmacological, biochemical and toxicological studies. The antiplatelet activity of each derivative was confirmed as 3a, 3b and 3 h significantly inhibited human platelet aggregation induced by arachidonic acid, with no detectable effect on clotting factors or healthy erythrocytes. Importantly, mice treated with derivative 3a showed a higher survival rate at an in vivo model of pulmonary thromboembolism with a lower bleeding risk in comparison to aspirin. The in silico studies pointed a series of structural parameters related to thromboxane synthase (TXS) inhibition by 3a, which was confirmed by tracking plasma levels of PGE 2 and TXB 2 through an in vitro enzyme immunoassay. Derivative 3a showed selective TXS inhibition allied with low bleeding risk and increased animal survival, revealing the derivative as a promising candidate for treatment of cardiovascular diseases.

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Section: Discussionmentioning

confidence: 84%

Antiplatelet pyrazolopyridines derivatives: pharmacological, biochemical and toxicological characterization

Saito

Lourenço

Dias

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Egészséges önkéntesekben vizsgál-va például az ibuprofennel ellentétben a diclofenac és az acetaminophen nem befolyásolta számottevően az ASA thrombocytaaggregációt gátló hatását [10]. Egy közel-múltban publikált vizsgálatban [11] pedig in vitro kö-…”

Section: Az Nsaid-ok éS Az Aszpirin Együttes Használataunclassified

“…Az ASA thrombocytaaggregáció-mértékének változása különböző NSAID-készítmények mellett Az ábra elemei engedéllyel átvéve Saxena és mtsai közleményéből [11]. A fehér oszlopok a kontroll (NSAID nélkül) észlelt aggregációt mutatják, a fekete vonal a fehér oszlop mellett az aggregáció mértékét 30 μmol/l ASA jelenlétében reprezentálja (teljes thrombocytaaggregáció-gátlás).…”

Section: áBraunclassified

Cardiovascular side effects of non-steroidal anti-inflammatory drugs in the light of recent recommendations.Diclofenac is not more dangerous

et al. 2015

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A nem szteroid gyulladásgátló készítmények jótékony hatásaik mellett számos, az alkalmazott gyógyszer típusától és dózisától is függő mellékhatással rendelkeznek. A leggyakoribb gastrointestinalis mellékhatások a terápia megkezdését követően már rövid időn belül jelentkezhetnek, de más nem kívánt hatások, mint a cardiovascularis események kockázatának fokozódása (amelyek a gastrointestinalis mellékhatásokhoz képest lényegesen ritkábbak) is előfordul-hatnak a gyógyszerek alkalmazásának megkezdését követően, latenciaperiódus nélkül. Fontos megemlíteni, hogy fájdalomcsillapítás céljából nem szteroid gyulladásgátló kezelést leggyakrabban az idősebb, cardiovascularis szempontból fokozott kockázatú populáción alkalmazzák hosszabb ideig, ahol más gyógyszerek -például a kis dózisú acetilszalicilsav -kölcsönhatásba léphetnek az alkalmazott fájdalomcsillapító készítményekkel; ebben a tekintetben a diclofenac alkalmazása kevesebb kockázatot rejthet magában. Összefoglaló közleményükben a szerzők a nem szteroid gyulladásgátlók cardiovascularis mellékhatásainak előfordulását, azok kialakulását befolyásoló tényezőket és terápiás konzekvenciáit, valamint e készítmények acetilszalicilsavval történő interakcióit elemzik. Orv. Hetil., 2015, 156(13), 516-520. Kulcsszavak: nem szteroid gyulladásgátló, acetilszalicilsav, cardiovascularis mellékhatás, diclofenac Cardiovascular side effects of non-steroidal anti-infl ammatory drugs in the light of recent recommendations Diclofenac is not more dangerousAmong their benefi cial effects, non-steroidal anti-infl ammatory drugs may also exert several side effects which depend on the dosage and the type of these medications. The most frequent gastrointestinal side effects usually develop shortly after the beginning of their administration, but others such as cardiovascular interactions (which are present much less frequently than gastrointestinal side effects) can also occur after the beginning of drug administration without a latency period. For a long-term treatment, non-steroidal anti-infl ammatory drugs are most frequently used in the elderly population where patients typically have high cardiovascular risk and take other medicines, e.g. low dose acetylsalicylic acid that can interact with non-steroidal anti-infl ammatory drugs; in this aspect diclofenac may cause less side effects. In this review, the authors briefl y review cardiovascular side effects of non-steroidal anti-infl ammatory drugs, the processes which potentially infl uence them, therapeutic consequences and their interaction with acetylsalicylic acid.

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“…Therefore aspirin may fail to exert its irreversible antiplatelet effects for the life span of the affected platelet. [7,8] In this study we aimed to investigate (i) aspirin antiplatelet effects and (ii) neurological outcome in stroke patients with aspirin and dipyrone comedication. We hypothesized, that impaired pharmacodynamic Vascular Pharmacology xxx (2016) xxx-xxx response to aspirin in dipyrone treated patients is associated with impaired clinical outcome.…”

Section: Introductionmentioning

confidence: 99%

Dipyrone comedication in aspirin treated stroke patients impairs outcome

Dannenberg

Erschoff

Gliem

et al. 2016

Vascular Pharmacology

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Drug/drug interaction of common NSAIDs with antiplatelet effect of aspirin in human platelets

Cited by 70 publications

References 37 publications

Antiplatelet pyrazolopyridines derivatives: pharmacological, biochemical and toxicological characterization

Antiplatelet pyrazolopyridines derivatives: pharmacological, biochemical and toxicological characterization

Cardiovascular side effects of non-steroidal anti-inflammatory drugs in the light of recent recommendations.Diclofenac is not more dangerous

Dipyrone comedication in aspirin treated stroke patients impairs outcome

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