Gastroduodenal toxicity of low-dose acetylsalicylic acid: a comparison with non-steroidal anti-inflammatory drugs

Yeomans, Neville D; Hawkey, Christopher J.; Brailsford, Wayne; Næsdal, J

doi:10.1185/03007990903212682

Cited by 32 publications

(21 citation statements)

References 111 publications

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“…Gastrointestinal (GI) erosions and bleeding are two of the most common toxic side-effects associated with the administration of NSAIDs. These effects have been observed even with small prophylactic doses of aspirin (81 mg/d) 10 . Approximately 50% of patients taking NSAIDs on a long-term basis may develop mucosal damage in the small intestine 11 .…”

Section: Introductionmentioning

confidence: 98%

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NSAIDs do not require the presence of a carboxylic acid to exert their anti-inflammatory effect – why do we keep using it?

Ullah

Huang²,

Sanaee

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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The carboxylic acid group (-COOH) present in classical NSAIDs is partly responsible for the gastric toxicity associated with the administration of these drugs. This concept has been extensively proven using NSAID prodrugs. However, the screening of NSAIDs with no carboxylic acid at all has been neglected. The goal of this work was to determine if new NSAID derivatives devoid of acidic moieties would retain the anti-inflammatory activity of the parent compound, without causing gastric toxicity. To test this concept, we replaced the carboxylic acid group in ibuprofen, flurbiprofen, and naproxen with three ammonium moieties. We tested the resulting water-soluble NSAID derivatives for anti-inflammatory and ulcerogenic activity in vitro and in vivo. In this regard, we observed that all non-acidic NSAIDs exerted a potent antiinflammatory activity, suggesting that the acid group in commercial 2-phenylpropionic acid NSAIDs not be an essential requirement for anti-inflammatory activity. These data provide complementary evidence supporting the discontinuation of ulcerogenic acidic NSAIDs.

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Section: Introductionmentioning

confidence: 98%

“…Finally, we evaporated the solvent under vacuum, and we purified the corresponding amines by flash chromatography. All products (10)(11)(12) were used immediately after purification to obtain the corresponding ammonium salts (13-15) described below.…”

Section: Ch)mentioning

confidence: 99%

NSAIDs do not require the presence of a carboxylic acid to exert their anti-inflammatory effect – why do we keep using it?

Ullah

Huang²,

Sanaee

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Aspirin also raises the risk of hemorrhagic stroke and other major bleeding (Baigent et al, 2009), significant gastro duodenal damage even in the low doses used for cardiovascular protection (Yeomans et al, 2009). Avoid use in severe liver disease (Lacy et al, 2011), because liver toxicity is reported by aspirin (Bjorkman, 1998) days or weeks are required to develop hepatotoxicity (Zimmerman, 1981).…”

Section: Introductionmentioning

confidence: 99%

Aspirin Associated Liver Toxicity – The Optimal Dose of Aspirin in Liver Insufficiency

Rafeeq¹,

Najam²,

Hussain³

2016

IJSRK

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Abstract. Acetylsalicylic acid (Aspirin) belongs to nonsteroidal anti-inflammatory drugs (NSAIDs). Numerous studies have proven that aspirin reduces the signs and symptoms of inflammation and exhibited a broad range of pharmacological activities, including analgesic, antipyretic and antiplatelet properties. Previous studies suggested that beside the pharmacological activities aspirin was also associated with the side effects and toxicity of various doses and in various formulations. The present study is performed to explore the effects of aspirin in various doses (75mg (EC), 100mg, 150 (EC)mg and 300mg) in different preparation (enteric coated (EC), non-enteric coated) on liver enzymes (Serum glutamic oxaloacetate transaminase (SGOT) and Serum glutamic pyruvic transaminase (SGPT)) followed by daily administration for 10 days and for 30 days. We found that the SGOT level was increased by all doses of aspirin after 30 days of treatment, this effect was most significant at 75mg (EC) and 100mg dose, whereas at 150mg (EC) and 300mg was not very significant. The level of SGPT was decreased by all doses regardless of duration of treatment, only 75mg (EC) dose increased its level after 30 days of treatment, suggesting 75mg (EC) aspirin could be hepatotoxic due to lessen of anti-oxidant effects, furthermore suggests that patients with hepatic insufficiency should not receive 75mg (EC) dose of aspirin.

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“…As úlceras gástricas são caracterizadas por danos na mucosa e estão predominantemente relacionadas à infecção por Helicobacter pylori, utilização de ácido acetilsalicílico (Yeomans et al, 2009), fármacos anti-inflamatórios não esteroidais (AINES), tabagismo e ao consumo de álcool (Soberg et al, 2010). Estas lesões resultam basicamente de um desequilíbrio entre mecanismos de defesa (secreção de muco, regeneração celular e agentes protetores endógenos) e fatores agressivos (secreção de ácido e pepsina) (Maity et al, 2003).…”

Section: Introductionunclassified

Atividade antiulcerogênica do extrato aquoso de Salvia officinalis L. (Lamiaceae)

Junior

Picolli

Morais

et al. 2015

Rev. bras. plantas med.

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RESUMO:As úlceras pépticas são decorrentes de um desequilíbrio entre os agentes agressores endógenos, exógenos e agentes protetores. Neste estudo avaliou-se a atividade antiulcerogênica in vivo para o extrato aquoso de Salvia officinalis (EAS). Após os tratamentos (n = 6; v.o) com o controle (C) água; pantoprazol (30 mg/kg) e EAS (100, 250 e 400 mg/kg, respectivamente) os ratos receberam uma solução de HCl 0,3 M em etanol 60% (v.o) e realizaram-se avaliações morfológicas dos estômagos por meio de uma tabela de escores de lesão (ANOVA; one way e Tukey). EAS (400 mg/kg) apresentou atividade antiulcerogênica (31,47%) semelhante ao pantoprazol (33,83%) em comparação (p<0,0001) com o grupo C. A análise fitoquímica por cromatografia líquida de alta eficiência revelou uma elevada concentração de ácido rosmarínico (3,53%) para EAS. Os flavonoides (0,25%) e os fenóis totais (309,0 EAG) foram quantificados por espectrofotometria de UV/Vis. EAS e ácido rosmarínico apresentaram elevadas atividades antioxidantes por DPPH (Concentração Efetiva 50%-CE 50 9,2 e 0,7 mg/mL, respectivamente) justificando pelo menos em parte, o efeito antiulcerogênico do extrato. Palavras-chave:Salvia officinalis, antiulcerogênica, polifenóis, antioxidante. ABSTRACT: Antiulcerogenic activity of aqueous extract of Salvia officinalis L. (Lamiaceae).Peptic ulcers are caused by an unbalance among endogenous, exogenous damaging agents and protective agents. In this study we evaluated the in vivo antiulcerogenic activity for the aqueous extract of Salvia officinalis (EAS). After treatments (n = 6; v.o) with control (C) water; pantoprazole (30 mg/kg) and EAS (100, 250 and 400 mg/kg, respectively) the rats received a 0.3 M HCl solution in ethanol 60% (v.o) and it were performed morphological evaluations of the stomachs through the use of a table of injury scores (ANOVA, one way and Tukey). The EAS (400 mg/kg) showed an antiulcerogenic activity (32.53%). Similar to the pantoprazole (29.91%), in comparison with (p<0.0001) the group C. The phytochemical analysis through high performance liquid chromatography revealed high acid rosmarinic (3.53%) for the EAS. The flavonoids (0.25%) and the total phenolics (GAE 309.0) were quantified by spectrophotometry UV/Vis. The EAS and the rosmarinic acid exhibited elevated antioxidant activities by DPPH (Effective Concentration 50% -EC 50 9.2 and 0.7 mg/mL, respectively,) at least partially explaining the antiulcerogenic effect of the extract.

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Gastroduodenal toxicity of low-dose acetylsalicylic acid: a comparison with non-steroidal anti-inflammatory drugs

Cited by 32 publications

References 111 publications

NSAIDs do not require the presence of a carboxylic acid to exert their anti-inflammatory effect – why do we keep using it?

NSAIDs do not require the presence of a carboxylic acid to exert their anti-inflammatory effect – why do we keep using it?

Aspirin Associated Liver Toxicity – The Optimal Dose of Aspirin in Liver Insufficiency

Atividade antiulcerogênica do extrato aquoso de Salvia officinalis L. (Lamiaceae)

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