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  • Antihypertensives  (1)
  • biliary recycling  (1)
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 8 (1975), S. 409-414 
    ISSN: 1432-1041
    Keywords: Antihypertensives ; vasodilator ; PR-G-138-Cl
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary PR-G-138-Cl, a new antihypertensive agent with vasodilating properties, was studied in ten patients with moderate to severe hypertension. The patients were admitted to a metabolic ward and followed on a 2 gm salt diet. Placebo was given daily until blood pressure and weight were stabilized. A dose titration was then started with increasing single daily doses of 3, 5, 8, and 10 mg of PR-G-138-Cl orally. The dose at which the mean arterial pressure was reduced by 15 mm Hg was continued for a total of seven days. PR-G-138-Cl lowered sitting mean arterial pressures significantly in all subjects (133.8±15.1 → 116.0±12.4 mm Hg, p〈0.001). The antihypertensive effect was first noted 30 minutes following drug administration and persisted for as long as six hours with a peak effect at one hour. All patients had a significant increase in sitting pulse rate (80.4±9.11 → 90.0 ±6.91/min, p〈0.002). Blood pressure reduction and increase in pulse rate were dose related. The most common side effects noted were headaches in eight out of ten patients and postural dizziness in seven out of ten patients. There were no signs of fluid retention (weight gain or edema). Electrocardiogram and other laboratory parameters remained essentially unchanged.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 4 (1976), S. 255-280 
    ISSN: 1573-8744
    Keywords: biliary recycling ; bioavailability ; biotransformation ; clearance ; route dependence ; enterohepatic circulation ; indomethacin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract There are no discernible quantitative differences in the biotransformation and the excretion of indomethacin following oral, rectal, and intravenous administration of indomethacin-14 C. Approximately 50% (range 24–115% for n=6) of an intravenous dose undergoes enterohepatic circulation. Thus the bioavailability of indomethacin to the systemic circulation may exceed the administered dose. Relative to the intravenous dose, indomethacin is 80 and 100% bioavailable from suppositories and capsules, respectively. Absorption and/or reabsorption appears to be more rapid and uniform by the rectal route. Recognition of the attributes of biliary recycling also helps to explain the observed variability in apparent plasma half-life, while their neglect requires alternative explanations for anomalies between the disappearance rate from plasma and the corresponding appearance rate in urine.
    Type of Medium: Electronic Resource
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