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  • Industrial Chemistry
  • Seismology
  • man
  • Springer  (4)
  • 2005-2009
  • 1975-1979
  • 1970-1974  (4)
  • 1971  (4)
Collection
Publisher
Years
  • 2005-2009
  • 1975-1979
  • 1970-1974  (4)
Year
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 3 (1971), S. 106-112 
    ISSN: 1432-1041
    Keywords: Probenecid ; probenecid acyl glucuronide ; sulfinpyrazone ; renal ; man ; metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The metabolism of probenecid has been investigated in both normal and gouty subjects. To carry out these studies, specific spectrophotometric methods were developed for the measurement of a major metabolite of probenecid, the acyl glucuronide. This conjugate was isolated in semi-pure state and its identity as a mono acyl glucuronide established. Our experiments indicate that about 25% of probenecid is converted to its acyl glucuronide and that only a small amount of the drug is excreted unchanged. About 80% of orally administered14C probenecid could be accounted for in urine, and about half of this was found to consist of metabolites more polar than the parent drug. The renal clearance of probenecid acyl glucuronide was shown to be about 1/3 that of creatinine clearance, whereas the clearance of probenecid was lower. The present findings in man and those of other workers in animals, raise the important question of the possible contribution of these metabolites to the overall pharmacological effects resulting from the administration of probenecid.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: Psychoactive drugs (or psychopharmaca) ; long-term treatment ; haemodynamics ; plasma-noradrenaline ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Haemodynamic effects in patients treated with imipramine and haloperidol were studied at rest and during exercise and were related to the arterial plasma levels of noradrenaline. The results were compared with earlier observations on untreated and chlorpromazine-treated patients studied by the same techniques. After imipramine in a daily dose of 150–350 mg, there was a tendency for the heart rate to increase but no other particular haemodynamic effects were observed. During imipramine treatment noradrenaline levels were not increased compared to the controls, at a work load of less than 900 kpm/min, after which there appeared to be some increase. After haloperidol in a dose of 12–22 mg per day no changes were observed in the circulation or plasma noradrenaline levels. More marked effects on the circulation and plasma noradrenaline levels were found in patients treated with very large doses of chlorpromazine (1800–3600 mg daily). They showed a lower cardiac output, stroke volume and systolic and mean arterial blood pressure during exercise than the other groups. In the chlorpromazine-treated group the heart rate was higher both at rest and during mild exercise. The plasma noradrenaline levels were higher at rest and at all work loads than in the other patients. It may be concluded that the haemodynamic effects of chlorpromazine and its effects on the plasma noradrenaline levels are primarily due to its peripheral α-adrenergic receptor blocking effect, which induces a compensatory increase in sympathetic nerve impulse flow. However, an increased overflow of noradrenaline from the nerve terminals per nerve impulse due to drug effects at the nerve terminal-effector cell level might also contribute to the high plasma levels of noradrenaline found after chlorpromazine treatment.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 3 (1971), S. 113-118 
    ISSN: 1432-1041
    Keywords: Enzyme-induction ; man ; phenacetin ; phenazone
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary After the oral administration to volunteers of phenacetin (15 mg/kg) the highest concentration in blood was reached 2 h later. The decline appeared to follow first order kinetics with an apparent biological half-life (t′/2) of 0.8 h. The highest concentration in blood of the unconjugated metabolite, paracetamol, was twice that of phenacetin. About 70 per cent of a dose of phenacetin was excreted as conjugated paracetamol in the urine, and 70 per cent of this compound was eliminated during the first 12 h period. — After daily administration of 1.4, 2.5 and 3.6 mg/kg of Phenobarbital, each dose sequentially for 1 week, the apparent biological half-life of phenacetin and the elimination rates of its metabolites, unconjugated and conjugated paracetamol, remained unchanged. The elimination rate of phenazone (16 mg/kg) was increased by 40 per cent in the same subjects after treatment with phenobarbital. — The blood concentration of phenacetin varied more than 20 times between individuals, although no individual variation was found for the blood levels of unconjugated paracetamol.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 3 (1971), S. 144-147 
    ISSN: 1432-1041
    Keywords: Adrenaline ; alprenolol ; blood coagulation ; fibrinolysis ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of intravenous infusions of adrenaline alone, and after alprenolol (Aptin®) pre-treatment, on whole blood clotting time, factor VIII, fibrinolysis, partial thromboplastin time (PTT), platelet count and fibrinogen have been studied in four healthy, fasting male subjects by double-blind technique using saline infusions as control. The adrenaline infusion caused increases in factor VIII levels, fibrinolysis and platelet counts and a decrease in whole blood clotting time. Alprenolol inhibited the effects of adrenaline on factor VIII and fibrinolysis in all subjects, and the effects on whole blood clotting time in all but one subject. The adrenaline-induced rise in platelet count was not significantly influenced by alprenolol pre-treatment. No effects were seen of the alprenolol infusion itself.
    Type of Medium: Electronic Resource
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