Absorption, distribution and toxicity of ibuprofen

Adams, S. S.; Bough, R.G.; Cliffe, E. E.; Lessel, B.; Mills, R. F. N.

doi:10.1016/0041-008x(69)90032-5

Cited by 159 publications

(54 citation statements)

References 13 publications

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“…The tolerability profile of racemic ibuprofen is well established and extensively documented in the literature. [18][19][20][21][22] Maximum consumption of 6 tablets/d of 200 mg ibuprofen arginate (corresponding to the maximum recommended OTC daily dosage) would result in total daily dosages of L-arginine equivalent to 16 mg/kg. This corresponds to a daily intake of 1100 mg L-arginine, which is considered to be unlikely to present any significant risk for serious AEs, considering that the recommended dietary allowance of arginine is 4.7 to 5.4 g. L-Arginine is commercially available as a dietary supplement and has been administered in 400-to 500-mg doses IV with relatively little toxicity.…”

Section: Discussionmentioning

confidence: 99%

Analgesia with ibuprofen arginate versus conventional ibuprofen for patients with dysmenorrhea: a crossover trial

Mehlisch¹,

Ardia

Pallotta³

2003

Current Therapeutic Research

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Background: Dysmenorrhea produces painful abdominal cramps that can disrupt the personal lives and productivity of women.Objective: The aim of this study was to compare the analgesic efficacy, including onset and duration of pain relief, peak effect, and total effect, and tolerability of ibuprofen arginate with those of conventional ibuprofen in patients with moderate to severe pain associated with primary dysmenorrhea.Methods: Patients were administered a single dose of ibuprofen arginate (200 or 400 mg), conventional ibuprofen (200 or 400 mg), or placebo during each of 5 menstrual cycles in a single-center, double-blind, randomized, doubledummy, 5-cycle, crossover study. Patients recorded their pain intensity and pain relief at regularly scheduled intervals (10,20, 30, 40, 50, 60, and 90 minutes and 2, 3, 4, 5, and 6 hours) after taking the study medication, and all study observations were recorded in a patient diary. Pain intensity was rated using the following 4-point categoric rating scale: 0 ϭ none, 1 ϭ mild, 2 ϭ moderate, and 3 ϭ severe. Pain relief was rated on a 5-point scale as 0 ϭ none, 1 ϭ a little, 2 ϭ some, 3 ϭ a lot, and 4 ϭ complete relief. Tolerability of ibuprofen arginate was based on a comparison of the incidence of spontaneously reported adverse events in each of the treatment groups.Results: One hundred four patients entered the study. Of these, 81.7% were white; the mean (SD) age was 27.5 (5.0) years. A total of 65.4% of patients reported moderate pain from dysmenorrhea, and the remaining 34.6% reported severe pain; 20.2% of patients did not complete the study. The median time to achieve meaningful pain relief was ϳ30 minutes faster with ibuprofen arginate 400 mg than with either dose of conventional ibuprofen. Tolerability was similar across all treatments.Conclusions: In this study population of patients experiencing acute pain as a result of primary dysmenorrhea, ibuprofen arginate was associated with 327CURRENT THERAPEUTIC RESEARCH effective, tolerable analgesia and a more rapid onset of action than conventional ibuprofen. The faster onset of analgesia may have a role in clinical practice in treating women with dysmenorrhea. A faster onset of action may be important to women whose personal relationships, productivity, or ability to sleep is being adversely affected by pain. (Curr Ther Res Clin Exp. 2003;64:327-337)

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Section: Discussionmentioning

confidence: 99%

Analgesia with ibuprofen arginate versus conventional ibuprofen for patients with dysmenorrhea: a crossover trial

Mehlisch¹,

Ardia

Pallotta³

2003

Current Therapeutic Research

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“…It is well-recognized that this species is particularly sensitive to the ulcerogenic activity of anti-inflammatory compounds (5), including ibuprofen (1). Single oral doses above 125 mg/kg and repeated oral doses of 8 and 16 mg/kg for 30 days were accompanied by ulcers or erosions in the gastric antrum or pylorus.…”

Section: Discussionmentioning

confidence: 99%

The Propionic Acids. Gastrointestinal Toxicity in Various Species

et al. 1988

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A s s~~c rThe propionic acids represent the largest chemical class of nonsteroidal anti-inflammatory agents (NSAID). Several of them are widely used, both in the United States and internationally. This paper discusses observations made on fenoprofen, flurbiprofen, ibuprofen and naproxen. Of these compounds, three are racemates; the fourth, naproxen, is an enantiomer. As a group, the propionic acids, along with most members of the other classes of NSAID, produce gastrointestinal damage in most species. These lesions vary from erythema, hemorrhage and erosion to ulceration and peritonitis. As might be expected, the degree of gastrointestinal intolerance depends on many factors: the individual compound, the dose-level, the duration of the period of drug administration, and the pharmacokinetics and metabolism in a given species. For example, in our experience the rat is less tolerant of NSAID than is the monkey, and the dog is less tolerant than the rat. Gastrointestinal lesions have been seen following both parenteral and oral administration; these findings suggest that factors other than local irritation play a role in the development of lesions. Most NSAID inhibit prostaglandin cyclo-oxygenase activity, which results in a prostaglandin deficiency at the tissue level. The administration of relevant exogenous prostaglandins, such as 16,16-dimethyl PGE,, has been shown to inhibit the gastrointestinal toxicity accompanying the administration of several NSAID, including some of the propionic acids.

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“…inoculated with Diclo (14.8 mg/kg, five times less than LD50 and 7.4 mg/kg, 10 times less than LD50 respectively (EC-SDS diclofenac, 2014)); group4 and group5 i.p. injected with Ibu (120 mg/kg, five times less than LD50 and 60 mg/kg, 10 times less than LD50 correspondingly (Adams, Bough, Cliffe, Lessel, & Mills, 1969)); and group6 and group7 i.p. injected with Para (73.4 mg/kg, five times less than LD50 and 36.7 mg/kg, 10 times less than LD50 separately (EC-SDS Acetaminophen, 2015)) daily for a period of 1 month.…”

Section: Experimental Designmentioning

confidence: 99%

Adverse effects induced by diclofenac, ibuprofen, and paracetamol toxicity on immunological and biochemical parameters in Swiss albino mice

Gomaa

2018

JoBAZ

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Background: Nonsteroidal anti-inflammatory drugs (NSAIDs) are generally used to reduce pain in different diseases acting as anti-inflammatory, antipyretic, and analgesic. Paracetamol is a nonprescription drug extremely used for antipyresis and analgesia. In spite of their beneficial effects, NSAIDs have been notified to be linked with some adverse effects. The present study was conducted to elucidate the comparative biochemical and immunological changes in mice treated with diclofenac (Diclo), ibuprofen (Ibu), or paracetamol (Para). Methods: Swiss albino mice were divided uniformly into seven different groups. Mice were intraperitoneally (i.p.) administered with Diclo (7.4 and 14.8 mg/kg), Ibu (60 and 120 mg/kg), and Para (36.7 and 73.4 mg/kg) daily for 1 month against saline-treated mice served as control. Blood samples were collected, and the assessments of some biochemical and immunological markers were measured.

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Absorption, distribution and toxicity of ibuprofen

Cited by 159 publications

References 13 publications

Analgesia with ibuprofen arginate versus conventional ibuprofen for patients with dysmenorrhea: a crossover trial

Analgesia with ibuprofen arginate versus conventional ibuprofen for patients with dysmenorrhea: a crossover trial

The Propionic Acids. Gastrointestinal Toxicity in Various Species

Adverse effects induced by diclofenac, ibuprofen, and paracetamol toxicity on immunological and biochemical parameters in Swiss albino mice

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