A stable isotope method for the quantification ofN-acetyl-5-aminosalicylic acid in plasma and urine

Fischer, Christine; Meese, Claus O.; Klotz, Ulrich

doi:10.1002/bms.1200111009

Cited by 10 publications

(2 citation statements)

References 19 publications

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“…In brief, 200 to 500 ,ul plasma were spiked with an internal standard (5-propionyl-aminosalicylic acid) (Fischer et al, 1984), acidified with 100 ,ul phosphoric acid (1M), vortexed and extracted into 2 ml diethylether.…”

Section: Salicylate Plasma Concentrationsmentioning

confidence: 99%

Effects of salicylic and acetylsalicylic acid alone and in combination on platelet aggregation and prostanoid synthesis in man.

Rosenkranz¹,

Fischer²,

Meese³

et al. 1986

Brit J Clinical Pharma

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The present study was designed to investigate the effects of salicylate on the antiplatelet action of acetylsalicylic acid as well as on in vivo prostanoid formation and platelet function in healthy volunteers. In the first study six female volunteers received 350 mg acetylsalicylic acid intravenously, with and without previous oral administration of sodium salicylate (1200 mg daily for 3 days). Urinary prostanoid excretion as well as platelet aggregation and thromboxane formation were measured before and during salicylate and after acetylsalicylic acid. In the second study seven female volunteers received sodium salicylate (52.6 mg kg‐1) or acetylsalicylic acid (60.7 mg kg‐1) for 8 days in a randomized cross‐over protocol. Urinary prostanoid excretion, platelet aggregation and thromboxane formation as well as salicylate plasma concentrations were determined before, during and after administration of each drug. Sodium salicylate did not impair the complete suppression of arachidonic acid‐induced platelet thromboxane formation and aggregation obtained by the single intravenous dose of acetylsalicylic acid in the first study. Sodium salicylate in the second study did not affect urinary excretion of prostaglandin E2, its major urinary metabolite (7 alpha‐hydroxy‐5,11‐ diketo‐tetranor‐prostane‐1,16‐dioic acid), and 2,3‐dinor‐6‐keto‐ prostaglandin F1 alpha, the main urinary metabolite of epoprostenol (prostacyclin, PGI2). In contrast, acetylsalicylic acid significantly decreased excretion rates of these prostanoids by 64, 59 and 61%, respectively. In both studies platelet aggregation and thromboxane formation induced by collagen, thrombin or arachidonic acid were not significantly affected by salicylate administration, whereas acetylsalicylic acid inhibited platelet aggregation induced by all three agents as well as thrombin‐ and arachidonic acid induced thromboxane formation.(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Salicylate Plasma Concentrationsmentioning

confidence: 99%

Effects of salicylic and acetylsalicylic acid alone and in combination on platelet aggregation and prostanoid synthesis in man.

Rosenkranz¹,

Fischer²,

Meese³

et al. 1986

Brit J Clinical Pharma

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“…and GCIMS have been described in detail elsewhere (Fischer et al, 1981(Fischer et al, , 1984. The disposition and excretion of d3-ac-5-AS was studied in two healthy male volunteers with normal kidney and liver function following a single rectal dose of 500 mg in the form of two suppositories.…”

Section: Introduction Methodsmentioning

confidence: 99%

Is N‐acetylation of 5‐aminosalicylic acid reversible in man?

Meese¹,

Fischer²,

Klotz³

1984

Brit J Clinical Pharma

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In two healthy male subjects the disposition of deuterated N‐(2H3) acetyl‐5‐aminosalicylic acid (d3‐ac‐5‐AS) was investigated after a single rectal dose of 500 mg d3‐ac‐5‐AS. Urine and plasma were analysed by h.p.l.c. and gas chromatography mass‐spectrometry. Peak concentrations of around 0.5 microgram/ml occurred within 6 h and plasma concentrations declined thereafter with a half‐life (t1/2) of about 6 h which was confirmed by urinary excretion data. Renal clearance of d3‐ac‐5‐AS ranged between 200 and 300 ml/min and only 4.4‐ 11.2% of the dose could be recovered in the 48 h urine. Since no undeuterated ac‐5‐AS could be detected in any of the plasma and urine samples an irreversible acetylation of 5‐AS is assumed in man.

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Drug Biotransformation: Mechanistic Studies With Stable Isotopes

Baillie

Rettenmeier

1986

The Journal of Clinical Pharma

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A stable isotope method for the quantification ofN-acetyl-5-aminosalicylic acid in plasma and urine

Cited by 10 publications

References 19 publications

Effects of salicylic and acetylsalicylic acid alone and in combination on platelet aggregation and prostanoid synthesis in man.

Effects of salicylic and acetylsalicylic acid alone and in combination on platelet aggregation and prostanoid synthesis in man.

Is N‐acetylation of 5‐aminosalicylic acid reversible in man?

Drug Biotransformation: Mechanistic Studies With Stable Isotopes

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