Indomethacin: Plasma concentrations and protein binding in man

Hvidberg, Eigill F.; Lausen, H. H.; Jansen, Jens Aas

doi:10.1007/bf00562508

Cited by 112 publications

(42 citation statements)

References 5 publications

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“…In one study of arthritic patients, a single dose of 50mg of indomethacin produced a free plasma concentration of the drug of 1 to 8 pM (Emori et al, 1973). In another study, a dose of 25 mg of indomethacin gave plasma concentrations of 1.5 to 8.5 JiM (Hvidberg et al, 1972). In practice, many patients with arthritis have to be given single doses of indomethacin up to 300 mg. From our data, it is clear that concentrations which can be achieved therapeutically can potentiate LPSstimulated release of IL-i-like activity in the mouse peritoneal macrophage.…”

Section: Discussionmentioning

confidence: 99%

The effect of non‐steroidal anti‐inflammatory drugs on the accumulation and release of interleukin‐1‐like activity by peritoneal macrophages from the mouse

Bahl

Dale

Foreman

1994

British J Pharmacology

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1 The non-steroidal anti-inflammatory drugs (NSAIDs) indomethacin, 10 10 nM, all potentiated cell-associated IL-I-like activity in LPS-stimulated macrophages. The drugs had no effect on cell-associated IL-l-like activity by themselves. 6 The 5-lipoxygenase inhibitors BWA4C, 0.01 to 101JM, and L-651,392, 0.01 to 1OJAM, had no effect on LPS-stimulated released or cell-associated IL-i-like activity. Over the same concentration-ranges, neither of the 5-lipoxygenase inhibitors affected released or cell-associated IL-1-like activity in LPSstimulated mouse macrophages in the presence of indomethacin, 1 JM. 7 The synthetic diacylglycerol, DiC8, 10 to 200 JAM, did not itself increase released or cell-associated IL-I-like activity but in the presence of the diacylglycerol kinase inhibitor, R59022, 10 JM, DiC8 increased released and cell-associated IL-i-like activity. The activity of DiC8 on released and cellassociated IL-l-like activity was not increased by indomethacin, 100JM. 8 NSAIDs increase LPS-induced cell-associated IL-i-like activity in mouse macrophages by inhibiting the formation of cyclo-oxygenase products such as PGE2 but at higher concentrations the NSAIDs potentiate LPS-induced release of IL-I-like activity by a mechanism independent of cyclo-oxygenase inhibition. The potentiation of the release of IL-i-like activity appears not to be related to an effect of NSAIDs on either 5-lipoxygenase or diacylglycerol metabolism.

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Section: Discussionmentioning

confidence: 99%

The effect of non‐steroidal anti‐inflammatory drugs on the accumulation and release of interleukin‐1‐like activity by peritoneal macrophages from the mouse

Bahl

Dale

Foreman

1994

British J Pharmacology

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“…The effects of indomethacin and phenylbutazone may have relevance to practice since the levels of drugs in serum were similar to or lower than those measured during therapy for phenylbutazone (Burns et al, 1953) and for indomethacin (Hvidberg, Lausen & Jansen, 1972). Generally, the strongest impairment of performance after phenylbutazone or indomethacin coincided with the highest serum levels of these drugs.…”

Section: Discussionmentioning

confidence: 86%

Acute Effect of Antipyretic Analgesics, Alone or in Combination With Alcohol, on Human Psychomotor Skills Related to Driving

Linnoila

Seppαlä

Mattila

1974

Brit J Clinical Pharma

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1 The effect of acetylsalicylic acid (1 g), indomethacin (50 mg), and phenylbutazone (200 mg) on psychomotor skills was examined double blind on 180 volunteer students. Ninety students received ethyl alcohol (0.5 g/kg) and 90 subjects an equal volume of placebo drink in combination with the drugs. 2 Psychomotor skills were measured with a choice reaction test, two co-ordination tests, and a divided attention test, having correlation with traffic behaviour. The subjects assessed their feelings of performance by means of a rating scale. The tests were done 30, 90 and 150 min after the administration of the agents. 3 Acetylsalicylic acid proved inactive whereas both indomethacin and phenylbutazone impaired eye-hand co-ordination and divided attention. Acetylsalicylic acid did not interact with alcohol to a measurable extent whereas indomethacin in combination with alcohol provedless harmful than without it. The deleterious effects of phenylbutazone and alcohol were additive. 4 An impairment of psychomotor skills related to driving by indomethacin and phenylbutazone should be considered when prescribing these drugs to active out-patients.

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“…As far as protein binding is concerned, indomethacin is highly bound to albumin, with various estimates ranging from 90 to > 99% (17,18). For reasons of standardization and viability ofthe studied tubule, we added 5% fetal calfserum to the bath.…”

Section: Methodsmentioning

confidence: 99%

Indomethacin secretion in the isolated perfused proximal straight rabbit tubule. Evidence for two parallel transport mechanisms.

Zeeuw

Jacobson²,

Brater³

1988

J. Clin. Invest.

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We studied indomethacin as a probe of anion transport across the isolated perfused proximal straight tubule of the rabbit and discovered that a substantial component of transport may occur by anion exchange at the basolateral membrane. Various perturbations involving direct or indirect dissipation of the cellular sodium gradient (ouabain, sodium-or potassium-free solutions, cooling to 18°C) resulted in only a 50% inhibition of indomethacin transport, which raised the question of a co-existent alternative pathway for secretion. Similarly, the anion exchange inhibitor, 4,4'-diisothiocyanostilbene (DIDS), diminished indomethacin secretion by only 50%. Cooling followed by DIDS or the reverse sequence resulted in additive inhibition such that the combination abolished active secretion of indomethacin.We conclude that active secretion of indomethacin by the proximal straight tubule appears to be in part sodium gradient dependent; the remainder may be driven by an anion exchanger on the basolateral membrane.

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Indomethacin: Plasma concentrations and protein binding in man

Cited by 112 publications

References 5 publications

The effect of non‐steroidal anti‐inflammatory drugs on the accumulation and release of interleukin‐1‐like activity by peritoneal macrophages from the mouse

The effect of non‐steroidal anti‐inflammatory drugs on the accumulation and release of interleukin‐1‐like activity by peritoneal macrophages from the mouse

Acute Effect of Antipyretic Analgesics, Alone or in Combination With Alcohol, on Human Psychomotor Skills Related to Driving

Indomethacin secretion in the isolated perfused proximal straight rabbit tubule. Evidence for two parallel transport mechanisms.

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