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  • healthy volunteers  (11)
  • Lepidoptera  (5)
  • 42.65
  • Springer  (17)
  • 2005-2009
  • 1980-1984  (17)
  • 1965-1969
  • 1984  (17)
Collection
Publisher
  • Springer  (17)
Years
  • 2005-2009
  • 1980-1984  (17)
  • 1965-1969
Year
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 27 (1984), S. 447-452 
    ISSN: 1432-1041
    Keywords: alaproclate ; antipyrine clearance ; serotonin reuptake inhibitor ; healthy volunteers ; antipyrine metabolism ; metabolite clearance ; alaproclate kinetics ; inhibition of drug metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Alaproclate, a selective serotonin reuptake inhibitor, presently undergoing clinical trial for the treatment of major depressive disorders, has been shown to inhibit hexobarbital metabolism in mice. In the present study the influence of oral alaproclate on the total plasma clearance of antipyrine and on the formation of its metabolites was investigated in 10 healthy volunteers. The peak level of alaproclate was reached after about 1.5 h, and after a distribution phase, its plasma elimination half-life was between 3.0 and 3.5 h. Antipyrine tests were performed before treatment, during the first four doses and after the seventh dose of alaproclate 200 mg/day. During treatment, total plasma antipyrine clearance and the clearance for production of all antipyrine metabolites were reduced by 30%, indicating non-selective inhibition of oxidative drug-metabolizing enzyme activity in man by alaproclate. After the last dose of alaproclate, antipyrine plasma clearance and the clearance to its metabolites returned to control values. In order to allow more detailed evaluation of the results, the time course of the clearances for production of metabolites was investigated. This revealed that the extent of inhibition of metabolite formation by alaproclate was dependent on the plasma alaproclate level, indicating a rapidly reversible inhibition.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Noctuidae ; Oncocnemis chandleri ; Oncocnemis cibalis ; Oncocnemis mackiei ; (5E7Z)-5 ; 7-dodecadienyl acetate ; (Z)-7-dodecenyl acetate ; sex attractant
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Oncocnemis chandleri, O. cibalis, andO. mackiei were attracted to chemically baited traps in the field. In all three cases, (5E,7Z)-dodecadienyl acetate was a key component for attraction. Attraction ofO. chandleri to traps baited with the (5E,7Z)-dodecadienyl acetate was inhibited by addition of (Z)-7-dodecenyl acetate.O. cibalis required both (5E,7Z)-dodecadienyl acetate and (Z)-7-dodecenyl acetate for attraction. Electroantennogram responses for the three species are also reported.
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  • 3
    ISSN: 1432-0649
    Keywords: 42.60 ; 42.65
    Source: Springer Online Journal Archives 1860-2000
    Topics: Physics
    Notes: Abstract We report the observation of coherent uv emission at 330.2±0.5 nm when sodium vapor in a heatpipe is irradiated with a pulsed visible dye laser with output wavelength in the 570–595 nm region. It is found that intense uv emission can be produced from Na atoms as well as from Na2 molecules. The excitation functions and their dependence on vapor density and laser power density are presented and the mechanisms for producing the emission are discussed.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 26 (1984), S. 635-637 
    ISSN: 1432-1041
    Keywords: theophylline ; inhalation ; saliva-serum distribution ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Six healthy volunteers received an iv infusion of 317 mg lysine theophylline (equivalent to 197 mg anhydrous theophylline) in order to calculate theophylline clearance by standard methods. They subsequently received a 20 minute inhalation of nebulised lysine theophylline. Serum and salivary theophylline concentrations were measured and all saliva was collected for the first hour. From these concentrations estimates were made of the distribution of theophylline into the blood and saliva with 40% to 94% identified in the blood. Very high salivary concentrations were reached during the inhalation phase with saliva: serum concentration ratios of between 60 and 1600.
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  • 5
    ISSN: 1432-1041
    Keywords: spironolactone ; canrenone ; metabolites ; pharmacokinetics ; single/multiple oral doses ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of canrenone and ‘total metabolites’ after base hydrolysis was studied in eight young volunteers following single and multiple dose oral administration of spironolactone. The plasma levels of canrenone and ‘total metabolites’ were fitted to a two-compartment open model with a first-order absorption process. From our eight normal subjects studied, the harmonic mean of the distributive half-life (t1/2α) of canrenone was found to be 1.66 h, and the harmonic mean of the terminal elimination half-life (t1/2β) to be 22.6 h. Harmonic means of the distributive and elimination half-lives of ‘total metabolites’ after base hydrolysis were 2.48 h and 28.8 h respectively. The accumulation ratio of canrenone was 2.53, whereas that of ‘total metabolites’ was 1.89. Despite the fact that spironolactone has been shown to induce hepatic metabolism of other drugs, no evidence of autoinduction was noted in the present study, as plasma levels of canrenone and ‘total metabolites’ were found to obey a linear two-compartment model with reproducible absorption and disposition after single and multiple doses.
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 27 (1984), S. 471-475 
    ISSN: 1432-1041
    Keywords: acyclovir ; A515U ; 6-deoxyacyclovir ; pharmacokinetics ; prodrug ; antiviral chemotherapy ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A515U (6-deoxyacyclovir) is an analogue of acyclovir devoid of antiviral activity in vitro but which is well absorbed and undergoes conversion to acyclovir after oral administration to rats. The tolerance and pharmacokinetics of various doses of A515U have been studied in 8 healthy volunteers. Single oral doses of 25, 50, 100, 200 and 400 mg A515U and 400 mg acyclovir for comparison were administered to the volunteers at weekly intervals. Concentrations of the parent drug and acyclovir were determined in plasma and urine. The prodrug was well tolerated and did not cause adverse reactions or changes in haematological or biochemical variables. It was well absorbed and conversion to acyclovir was rapid and extensive at all doses. Plasma concentrations of acyclovir achieved with 50 mg A515U orally were comparable to and less variable than those produced by 400 mg acyclovir. A515U was rapidly cleared with a short plasma elimination half life of approximately 0.5 h. The attainment of high plasma concentrations of acyclovir by oral administration of a prodrug may represent an important advance in antiviral chemotherapy.
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  • 7
    ISSN: 1432-1041
    Keywords: benzodiazepine antagonist ; visual function ; intrinsic effect ; Ro 15-1788 ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Ro 15-1788 is a specific benzodiazepine antagonist, which has also been shown to have some agonist properties. Since benzodiazepine receptors are involved in the physiological mechanisms of vision, a possible intrinsic effect of Ro 15-1788 was sought in 6 healthy volunteers by study of psychophysical flicker thresholds, including critical fusion frequency and low frequency modulation threshold, and pattern reversal visual evoked response, using double blind cross-over methodology. In each session 2 tablets of Ro 15-1788 30 mg were administered. Using a two factorial univariate analysis of variancé, no change was detected in any of the parameters studied.
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  • 8
    ISSN: 1432-1041
    Keywords: zetidoline ; prolactin ; aldosterone ; dopamine ; healthy volunteers ; pharmacodynamic effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The neuroendocrinological effects of acute oral administration of 20 mg zetidoline, a new antipsychotic drug with antidopaminergic properties, were evaluated in 8 healthy volunteers, by a double-blind, crossover comparison with placebo. Zetidoline significantly increased serum prolactin (p〈0.01 at 1–3 h; p〈0.05 at 4–6 h). No significant change was observed in blood levels of aldosterone, renin, cortisol, growth hormone and electrolytes, or in blood pressure and heart rate. The data suggest that the drug increases prolactin through blockade of dopaminergic receptors. The lack of change in the aldosterone levels may be evidence against the hypothesis of dopaminergic control of aldosterone secretion.
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 27 (1984), S. 191-196 
    ISSN: 1432-1041
    Keywords: pizotifen 5-hydroxyindoleacetic acid ; homovanillic acid ; urinary excretion ; healthy volunteers ; migraine prevention
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A single dose of 0.5 mg pizotifen or a placebo was administered to 10 healthy male volunteers in a double blind cross-over trial. 5-hydroxyindoleacetic acid (5-HIAA) and homovanillic acid (HVA) in hourly urine samples were determined by liquid chromatography with amperometric detection. The 5-HIAA levels were strongly correlated with the HVA levels in control samples (r=0.95, p〈0.001). Pizotifen produced a significant increase in the urinary 5-HIAA/HVA ratio over the 3 hours following absorption of the drug (+0.21, +0.18, +0.19, p〈0.05). The increase demonstrates an interaction between pizotifen and 5-HT metabolism, which may be involved in its antimigraine effect.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 27 (1984), S. 453-458 
    ISSN: 1432-1041
    Keywords: dipyrone ; metabolism ; metabolite pharmacokinetics ; acetylation polymorphism ; healthy volunteers ; dapsone phenotyping
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of the dipyrone metabolites 4-methylaminoantipyrine (MAA), 4-aminoantipyrine (AA), 4-formylaminoantipyrine (FAA) and 4-acetylaminoantipyrine (AAA) were evaluated following the administration of a single oral 1.0 g dose of dipyrone to 23 healthy volunteers. Twelve were slow and 11 were rapid acetylators as previously determined by dapsone phenotyping. For MAA and FAA the mean peak plasma concentrations were 10.5±2.8 µg/ml and 2.1±0.8 µg/ml and the half-lives were 3.3±1.0 and 10.1±1.8 h, respectively. No significant difference was found between rapid and slow acetylators in MAA and FAA kinetics. For AA, the mean peak plasma concentrations were 2.7±0.6 and 1.6±0.7 µg/ml (p〈0.01), the peak times 6.7±2.1 and 3.1±1.1 h (p〈0.01) and the half-lives were 5.5±1.0 and 3.8±1.2 h in slow and rapid acetylators, respectively. For AAA, the mean peak plasma concentrations were 1.6±0.4 and 4.4±1.1 µg/ml (p〈0.01) and the peak time 16.1±5.1 and 10.0±2.6 h (p〈0.01) in slow and rapid acetylators, respectively. There was no difference in the elimination half-life between the two groups (10.6±2.2 h). Thus, it has been demonstrated that the AAA/AA ratio is an indicator of the acetylation phenotype, as it is closely correlated with that determined by dapsone (r=0.895, p〈0.0005).
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