Studies on the disposition of antipyrine, aminopyrine, and phenacetin using plasma, saliva, and urine

Abstract

In normal male subjects, the half-lives of antipyrine, aminopyrine, or phenacetin were not significantly different from the half-lives of each drug in saliva. Apparent volumes of distribution (aVd) in plasma and saliva differed by the extent to which each drug has been reported to bind to plasma proteins. Thus, the aVd of antipyrine in plasma and saliva was similar; there were significant differences in aVd for aminopyrine; even greater differences were observed for penacetin. The expression (see article) equals the fraction of the drug bound to plasma proteins. Rates of appearance in the urine of metabolites of antipyrine and aminopyrine were measured. General equations were used to show the relationship between half-life for elimination of the parent drug from the body and rate of excretion of metabolites. There were significant correlations between the half-life for elimination of antipyrine from the body and the half-life for production of 4-OH antipyrine (r equal 0.90), as well as between the plasma half-life of aminopyrine and the half-life of 4-aminoantipyrine (r equal 0.95). No significant correlation was observed in the same individual between the plasma half-lives of antipyrine and phenacetin (r equal 0.05, p greater than 0.05), of aminopyrine and phenacetin (r equal 0.11, p greater than 0.05), or of antipyrine and aminopyrine (r equal 0.50, p greater than 0.05).

D‐glucaric acid excretion in critical care patients‐comparison with 6 beta‐hydroxycortisol excretion and serum gamma‐glutamyltranspeptidase activity and relation to multiple drug therapy.

“…For evaluation of enzyme induction, a number of tests are available (Park, 1982), mainly the administration of marker drugs like antipyrine (Vesell et al, 1975), hexobarbitone (Breimer et al, 1978), or aminopyrine (Hildebrandt et al, 1975) and the analysis of their pharmacokinetics. The usefulness of this approach, however, is limited should these test compounds compete with therapeutically given drugs (Vesell, 1979).…”

A comparative study of antipyrine and lignocaine disposition in normal subjects and in patients treated with enzyme‐inducing drugs.

“…Drugs which have been used to this purpose include antipyrine (Stevenson, 1977;Sotaniemi, Pelkonen, Ahokas, Pirttiaho & Ahlqvist, 1978;Vesell, 1979), aminopyrine (Vesell, Passananti, Glenwright & Dvorchik, 1975), phenylbutazone (O'Malley, Crooks, Duke & Stevenson, 1971), hexobarbitone (Breimer, Zilly & Richter, 1977), warfarin (Orme, Breckenridge & Brooks, 1972) and tolbutamide (Pond, Birkett & Wade, 1977). Since these agents are invariably characterized by a low hepatic extraction ratio and by non-saturable, flow-independent, restrictive elimination, it is generally preferable that estimated values of systemic blood clearance for these drugs be calculated from blood concentration data following intravenous administration (Wilkinson & Shand, 1975).…”

Comparative Study on Salivary Distribution of Fluoroquinolones in Rats.

“…About 100 ml of the blood was collected in a heparinized microtube at 3, 10, 30 min and the midpoints (5,20,45,75,105,135, 165 min) of the above time periods for saliva collection. The plasma was immediately obtained by centrifugation.…”