Clinical Pharmacology of Predisintegrated Ibuprofen 800 mg Tablets: An Endoscopic and Pharmacokinetic Study

Friedman, H.; Seckman, C. E.; Lanza, Frank L.; Royer, George; Perry, Kimberly T.; Francom, Steven F.

doi:10.1002/j.1552-4604.1990.tb03439.x

Cited by 13 publications

(3 citation statements)

References 7 publications

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“…A number of studies have reported that prescription dosage level ibuprofen produces time and dose-dependent blood loss (assessed using the radiochromium blood loss technique) from the GI tract of volunteers or patients (Warrington et al 1982;Aabakken et al 1989;Hunt et al 2000) and mild-moderate endoscopic changes in fasted human volunteers (Lanza et al 1979(Lanza et al , 1981(Lanza et al , 1987Friedman et al 1990;Bergmann et al 1992;Roth et al 1993;Müller et al 1995;Gallego-Sandin et al 2004) or those with rheumatic diseases (Teixeira et al 1997). The extent of the loss of blood maybe overestimated using the radiochromium technique as a consequence of biliary excretion of the radiolabelled chromium (Schneider et al 1984;Rainsford 2004a).…”

Section: Gastro-intestinal (Gi) Toxicitymentioning

confidence: 97%

Ibuprofen: pharmacology, efficacy and safety

2009

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This assessment of the safety and benefits of ibuprofen can be summarized thus: (1) Ibuprofen at OTC doses has low possibilities of serious GI events, and little prospect of developing renal and associated CV events. Ibuprofen OTC does not represent a risk for developing liver injury especially the irreversible liver damage observed with paracetamol and the occasional liver reactions from aspirin. (2) The pharmacokinetic properties of ibuprofen, especially the short plasma half-life of elimination, lack of development of pathologically related metabolites (e.g. covalent modification of liver proteins by the quinine-imine metabolite of paracetamol or irreversible acetylation of biomolecules by aspirin) are support for the view that these pharmacokinetic and notably metabolic effects of ibuprofen favour its low toxic potential. (3) The multiple actions of ibuprofen in controlling inflammation combine with moderate inhibition of COX-1 and COX-2 and low residence time of the drug in the body may account for the low GI, CV and renal risks from ibuprofen, especially at OTC doses.

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Section: Gastro-intestinal (Gi) Toxicitymentioning

confidence: 97%

Ibuprofen: pharmacology, efficacy and safety

2009

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“…No clinically significant gastrointestinal bleeds were observed. Two studies each observed that one aspirin-treated subject had occult blood in stools [13, 14]. …”

Section: Resultsmentioning

confidence: 99%

Gastrointestinal Adverse Effects of Short-Term Aspirin Use: A Meta-Analysis of Published Randomized Controlled Trials

Baron

Senn²,

Voelker

et al. 2013

Drugs R D

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Background and ObjectivesAspirin is widely used for short-term treatment of pain, fever or colds, but there are only limited data regarding the safety of this use. To summarize the available data on this topic, we conducted a meta-analysis of the published clinical trial literature regarding the gastrointestinal adverse effects of short-term use of aspirin in comparison with placebo and other medications commonly used for the same purpose.Data Sources and MethodsAn extensive literature search identified 119,310 articles regarding possible adverse effects of aspirin, among which 23,131 appeared to possibly include relevant data. An automated text-mining procedure was used to score the references for potential relevance for the meta-analysis. The 3,983 highest-scoring articles were reviewed individually to identify those with data that could be included in this analysis. Ultimately, 78 relevant articles were identified that contained gastrointestinal adverse event data from clinical trials of aspirin versus placebo or an active comparator. Odds ratios (ORs) computed using a Mantel–Haenszel estimator were used to summarize the comparative effects on dyspepsia, nausea/vomiting, and abdominal pain, considered separately and also aggregated as ‘minor gastrointestinal events’. Gastrointestinal bleeds, ulcers, and perforations were also investigated.ResultsData were obtained regarding 19,829 subjects (34 % treated with aspirin, 17 % placebo, and 49 % an active comparator). About half of the aspirin subjects took a single dose. Aspirin was associated with a higher risk of minor gastrointestinal events than placebo or active comparators: the summary ORs were 1.46 (95 % confidence interval [CI] 1.15–1.86) and 1.81 (95 % CI 1.61–2.04), respectively. Ulcers, perforation, and serious bleeding were not seen after use of aspirin or any of the other interventions.ConclusionsDuring short-term use, aspirin is associated with a higher frequency of gastrointestinal complaints than other medications commonly used for treatment of pain, colds, and fever. Serious adverse events were not observed with aspirin or any of the comparators.Electronic supplementary materialThe online version of this article (doi:10.1007/s40268-013-0011-y) contains supplementary material, which is available to authorized users.

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“…The fibre optic endoscope has permitted repeated studies of the acute and medium-term damage that occurs in individuals ingesting NSAIDs [46][47][48][49][50][51][52][53][54][55][56]. Early studies were simply concerned to document an effect, and later there was interest in the extent to which the degree of damage varied between individual NSAIDs.…”

Section: Studies Of Gastrointestinal Toxicity With Nsaidsmentioning

confidence: 99%

Current Problems with Non-Specific COX Inhibitors

McGettigan¹,

Henry

2000

CPD

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Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used and effective treatments for pain and inflammation. They have a substantial toxicity profile with side effects mainly affecting the gastrointestinal tract, heart and kidneys. Although they comprise a chemically diverse group of drugs, NSAIDs are unified by a common mode of action the ability to inhibit the enzyme cyclo-oxygenase (COX). This also accounts for much of their toxicity. The enzyme exists in at least 2 isoforms. COX-1 generates prostaglandins with physiological functions, COX-2 is induced by inflammation and its physiologic functions are unclear at present. Conventional NSAIDs, like diclofenac, ibuprofen, and naproxen, are non-selective COX inhibitors, blocking the production of both physiologic and inflammatory prostaglandins. In this chapter, we describe the main predictable gastrointestinal, cardiac and renal toxicities that can be explained by such blockade and review the supporting clinical and epidemiological evidence. In the gastrointestinal tract, the side effects associated with conventional NSAIDs are both local and systemic, and include ulceration, bleeding, perforation, and obstruction. The upper gastrointestinal tract is more commonly affected than the lower. The cardiac and renal side effects are most likely to occur in patients with existing heart or kidney disease, where prostaglandins play an essential role in maintaining the vasoconstrictor/dilator balance necessary for homeostasis. The patients at highest risk of toxicity are the elderly, those with a prior history of ulceration or bleeding, and those with a history of cardiac disease. Among such patients, the decision to prescribe NSAIDs requires careful consideration of the potential benefits and harms.

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Clinical Pharmacology of Predisintegrated Ibuprofen 800 mg Tablets: An Endoscopic and Pharmacokinetic Study

Cited by 13 publications

References 7 publications

Ibuprofen: pharmacology, efficacy and safety

Ibuprofen: pharmacology, efficacy and safety

Gastrointestinal Adverse Effects of Short-Term Aspirin Use: A Meta-Analysis of Published Randomized Controlled Trials

Current Problems with Non-Specific COX Inhibitors

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