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  • Acetanilide  (2)
  • D-glucaric acid  (1)
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 7 (1974), S. 387-391 
    ISSN: 1432-1041
    Keywords: Acetanilide ; diphenylhydantoin ; D-glucaric acid ; induction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of a single-dose acetanilide (AA) test, and the urinary D-glucaric acid output (UDGAO) were studied in healthy drug free volunteer subjects before and at the end of a fourteen-day period of medication with 5 mg diphenylhydantoin sodium (DPH) per kg metabolically active mass, thrice daily. The steady state plasma concentration (SSPC) of DPH was also determined. The SSPC of DPH was found to vary from 3.4 to 19.6 µg per ml. The mean UDGAO values increased significantly during DPH medication from 9.5 µmol per g creatinine to 29.5 (p〈0.002). The half-life of plasma AA concentration decreased significantly during DPH medication from a mean of 4.2 h to a mean of 2.8 (p〈0.001). However, the plasma clearance of AA did not change significantly during DPH medication. The increase of UDGAO whilst on treatment with DPH correlated positively with the SSPC of DPH. The evidence from this study suggests that measurement of UDGAO, which is a measure of the activity of the glucuronic pathway does not necessarily indicate the state of induction of oxidizing enzymes in the hepatic endoplasmic reticulum.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 7 (1974), S. 461-466 
    ISSN: 1432-1041
    Keywords: Acetanilide ; oxidation ; diphenylhydantoin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Acetanilide and diphenylhydantoin have a similar first stage biotransformation in that both are oxidized in the para position of the benzene ring incorporated in each of the two molecules. The elimination of acetanilide from the plasma was studied in thirty healthy volunteer subjects following a single oral dose of 50 mg per kg metabolically active mass (MAM = weight to the power of 0.7). Plasma clearance values varied from 12.4 to 25.11 per hour. A dose of 5 mg diphenylhydantoin sodium (DPH) per kg MAM was then given thrice daily for 13 days to the same volunteers. The steady state plasma concentrations of DPH varied from 3.4 to 19.6 µg per ml. Statistically significant correlation was demonstrated between plasma acetanilide clearance and DPH clearance (r=+0.4984). This finding suggests either a common enzyme acceptor or a common rate-limiting step in the metabolism of the two drugs. It is possible that the pharmacokinetics of other widely used drugs known to be oxidized, especially phenylbutazone, may also be correlated with the kinetics of acetanilide and of DPH. If this were so, then certain individuals might be at a relatively high risk (due to drug accumulation) of developing adverse effects from drugs metabolized mainly by oxidation, and certain other individuals who metabolize these compounds at a fast rate are likely not to derive therapeutic benefit. A single dose study with simple measurement of acetanilide pharmacokinetics could be used to identify these groups.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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