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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 9 (1981), S. 419-429 
    ISSN: 1573-8744
    Keywords: propranolol ; pharmacokinetics ; male volunteers ; oral and intravenous doses
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics of propranolol after the administration of 40, 80, and 120 mg p.o. and 10 mg i.v. was studied in nine healthy male volunteers. Propranolol was analyzed after extraction and derivatization by gas-liquid chromatography. A multiexponential curve-stripping program was used for the pharmacokinetic analysis. The volume of distribution was about 6 liters · kg −1 ,bioavailability around 25%, with a mean terminal half-life of 6hr. There was no evidence of either dose dependent disposition kinetics or an oral threshold dose. A slight increase in urine volume was observed after propranolol administration.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 9 (1981), S. 431-441 
    ISSN: 1573-8744
    Keywords: bendroflumethiazide ; pharmacokinetics ; male volunteers ; sodium and potassium excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics of bendroflumethiazide after oral administration of 1.25, 2.5, and 5.0 mg were studied in nine healthy male volunteers. Bendroflumethiazide was analyzed by GLC after extractive alkylation. After the lowest dose, the plasma concentration could be followed to 14 hr, and the data were adequately fitted by a one-compartment model; the half-life was 3.1 hr. After the 2.5 and 5.0 mg doses, the plasma concentration was followed for 24 hr, and the data were fitted by a two-compartment model with half-lives of 8.9 hr. The urinary sodium concentration was doubled after bendroflumethiazide intake, but the urinary potassium concentration remained almost constant. The renal clearance of bendroflumethiazide was around 30 ml · min −1 .
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1573-904X
    Keywords: aerosol ; terbutaline sulphate ; gamma scintigraphy ; charcoal-block ; lung deposition
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A comparison has been made of pulmonary deposition of terbutaline sulphate from a pressurized metered dose inhaler (pMDI), measured in 8 healthy male subjects by gamma scintigraphy and by a pharmacokinetic (charcoal-block) method, involving drug recovery in urine. Measurements were carried out with a pMDI at slow (27 1/min) and fast (151 1/min) inhaled flows and with Nebuhaler® large volume spacer device (average inhaled flow 171/min). Overall, the two methods did not differ significantly in their estimates of whole lung deposition, although values obtained by gamma scintigraphy exceeded those from the charcoal-block method for the pMDI with fast inhalation. The regional distribution of drug within the lungs and deposition in the oropharynx could be assessed by gamma scintigraphy, but not by the charcoal-block method. It is concluded that either method may be used to assess whole lung deposition of terbutaline sulphate from pMDIs, both with and without a spacer, although each method has its own inherent advantages and disadvantages.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 79 (1983), S. 142-147 
    ISSN: 1432-2072
    Keywords: Prolactin ; CFFF ; Arousal ; Pharmaco-kinetics ; Melperone
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The pharmacokinetics of melperone and the relationship between plasma concentration and the effect on arousal and prolactin secretion after single oral doses (10, 25, 50 and 100 mg) was studied in normal subjects. Dose-dependent kinetics were indicated by the fact that higher plasma concentrations than expected were demonstrated after the 100-mg dose. Melperone decreased arousal and increased prolactin secretion in a dose-dependent manner. The level of arousal was correlated to melperone plasma concentration over the entire dose range. Prolactin secretion was also correlated to melperone plasma concentration, provided the relationship was studied separately for the individual melperone doses. Thus at higher doses, higher plasma concentrations are needed to elicit the same prolactin outflow. The possibility that reduced arousal reactions might contribute in the antipsychotic action of neuroleptic drugs was discussed.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1432-2072
    Keywords: Melperone ; CFFF ; Plasma concentration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The relationship between plasma concentration and effect on arousal was studied in normal subjects after single oral and parenteral doses of melperone. A strong correlation between plasma concentration and effect was found when the effector compartment and central compartment were in equilibrium. The relationship was independent of the route of administration.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Chirality 1 (1989), S. 174-177 
    ISSN: 0899-0042
    Keywords: pharmacokinetics ; terbutaline ; enantiomers ; human ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Terbutaline is a β2-agonist and administered as the racemic mixture. The pharmacokinetics of the separate enantiomers differ with respect to degree of absorption and clearance. In the present study, repeated doses of racemic terbutaline were given to six healthy volunteers. Plasma was analyzed for the concentrations of the two enantiomers. The observed plasma concentrations at steady state differed from those predicted from the values observed after single dose administration of the separate enantiomers. The difference between the observed and predicted values can be tentatively explained by a combined influence of (-)-terbutaline on the absorption of (+)-terbutaline and the influence of (+)-terbutaline on the elimination of (-)-terbutaline. The results have implications for the interpretation of effect/concentration studies with terbutaline, but do not affect the doses used in clinical practice.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 7 (1990), S. 1068-1070 
    ISSN: 1573-904X
    Keywords: terbutaline sulfate ; lung deposition ; bioavailability ; metered dose inhaler ; stable isotope
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Terbutaline sulfate (4 × 0.250 mg) was given to 11 healthy volunteers by inhalation from a metered dose inhaler (MDI), with and without oral administration of a charcoal slurry. Before the inhalations, the adsorbing capacity of the charcoal slurry was tested. Deuterated terbutaline, 0.125 mg, was given intravenously at the same time as the test doses. The charcoal slurry adsorbed 97% of an oral dose. The oral contribution to the overall systemic bioavailability after inhalation, when charcoal was coadministered, could thus be neglected. After inhalation of terbutaline, 9.1% of the dose was deposited in the lungs and an additional 6.7% was systemically available via the oral route. The method presented measures the absolute pulmonary bioavailability after inhalation from a MDI. Since a deuterated analogue is given intravenously together with the inhalations, fewer subjects are needed to obtain reliable data.
    Type of Medium: Electronic Resource
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