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  • 1
    Electronic Resource
    Electronic Resource
    Lipoxygenase inhibitory activity of U-66,858 and its deacetylated metabolite U-68,244 in human whole blood (1994)
    Springer
    Inflammation research 41 (1994), S. 32-36 
    Details
    ISSN: 1420-908X
    Keywords: Leukotriene B4 ; 5-Lipoxygenase inhibitor ; Calcium ionophore ; Whole blood
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The inhibitory effects of the semi-quinone U-66,858 and its metabolite U-68,244 on the ionophore-induced formation of leukotriene B4 (LTB4) were examined in human whole blood (WB). Preincubation of U-66,858 and U-68,244 for 1 min prior to challenge of blood with calcium ionophore A23187 resulted in IC50 values of 1080±644 and 820±442 nmol/L, respectively (NS). After 60 min preincubation, values were 250±85 and 270±79 nmol/L (NS). The activity of the lipoxygenase inhibitor AA-861 in this system was similar to that of U-66,858, while vitamin K and the sulphate conjugate of U-66,858 showed significant inhibition of LTB4 release only at micromolar concentrations. U-66,858 exhibited significant inhibition of thromboxane A2 release (p〈0.02) in a comparative study with the known cyclooxygenase (CO) inhibitor flurbiprofen. The metabolism of U-66,858 in contact with WB at 37°C was monitored for 70 min using [14C]-labelled drug and reverse-phase HPLC, the majority of recovered radioactivity no longer in the form of U-66,858 being accounted for by U-68,244 and polar conjugates of U-66,858. Thus, U-66,858 is a potent inhibitor of LTB4 production in human whole blood and undergoes deacetylation to an initial metabolite with similar pharmacological potency. However, other metabolites of U-66,858 such as the sulphate conjugate, are relatively weak inhibitors of 5-lipoxygenase (5-LO) under similar conditions.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01986390
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  • 2
    Electronic Resource
    Electronic Resource
    The measurement of plasma digoxin concentration: A comparison of two methods (1972)
    Springer
    European journal of clinical pharmacology 5 (1972), S. 22-27 
    Details
    ISSN: 1432-1041
    Keywords: Plasma digoxin concentration ; radioimmunoassay ; 86Rb uptake method
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary No significant differences were found between plasma digoxin concentrations in samples assayed by both radioimmunoassay and86Rb uptake. The mean plasma digoxin concentration in 27 patients on a stable maintenance dose of digoxin was 1.1±0.6 ng/ml, while that in a group of 12 patients with clinical evidence of full or overdigitalization was 2.2±0.6 ng/ml, which was significantly greater (p〈0.05).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00560891
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and pharmacodynamics of procyclidine in man (1985)
    Springer
    European journal of clinical pharmacology 28 (1985), S. 73-78 
    Details
    ISSN: 1432-1041
    Keywords: procyclidine ; Kemadrin ; pharmacokinetics ; pharmacodynamics ; humans
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and pharmacodynamics of procyclidine (10 mg) after oral and intravenous administration were studied in six healthy volunteers. Treatment order was randomised and the study was placebo-controlled and conducted blind. After oral dosing the mean peak plasma concentration was 116 ng/ml and mean bioavailability was 75%. After both oral and intravenous dosing the mean values for the volume of distribution, total body clearance and plasma elimination half-life of procyclidine were in the order of 1 l/kg, 68 ml/min and 12 h respectively. Autonomic effects were maximal within 0.5 h of intravenous administration and at about 1–2 h after oral dosing. Significant effects on pupil diameter, visual near point, salivary secretion and heart rate occurred after intravenous treatment and similar but less marked effects occurred after the oral dose. Significant autonomic effects were still detectable 12 h after both forms of treatment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635711
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  • 4
    Electronic Resource
    Electronic Resource
    Alcohol and bupropion pharmacokinetics in healthy male volunteers (1984)
    Springer
    European journal of clinical pharmacology 26 (1984), S. 627-630 
    Details
    ISSN: 1432-1041
    Keywords: bupropion ; ethanol ; pharmacokinetic interaction ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A study was performed to determine whether there is a pharmacokinetic interaction between alcohol and the novel antidepressant bupropion. In the first part 8 healthy male volunteers received single doses of 100 mg bupropion hydrochloride orally on 2 occasions accompanied by either ethanol in orange or plain orange drink according to a balanced cross over design. Plasma bupropion concentrations were determined by radioimmunoassay and kinetics analysed with the aid of NONLIN. Blood alcohol levels were assessed by breathalyser. The disposition of bupropion was adequately described by a 2 compartment model and kinetic parameters were not significantly altered by the presence of alcohol. In the second part of the study the same subjects received 40 ml ethanol in orange drink 3.5 h after ingestion of 100 mg bupropion or dummy tablet in a double blind cross over fashion. Bupropion did not affect alcohol kinetics. In contrast to many other psychotropic drugs there is no evidence for a kinetic interaction between bupropion and alcohol.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00543497
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  • 5
    Electronic Resource
    Electronic Resource
    Tolerance and pharmacokinetics of A515U, an acyclovir analogue, in healthy volunteers (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 471-475 
    Details
    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.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00549597
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  • 6
    Electronic Resource
    Electronic Resource
    The disposition of bupropion and its metabolites in healthy male volunteers after single and multiple doses (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 97-103 
    Details
    ISSN: 1432-1041
    Keywords: bupropion ; metabolites ; pharmacokinetics ; single and multiple dose ; side-effects ; enzyme induction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of bupropion and 3 of its basic metabolites were determined in 8 young, healthy, male volunteers after single and multiple oral doses of bupropion. Plasma profiles were obtained: 1) after a single 100 mg oral dose of bupropion hydrochloride, 2) following administration of 100 mg 8-hourly for 14 days and 3) again after a single 100 mg dose 14 days later. Plasma concentrations of the parent drug and metabolites were determined by high-performance liquid chromatography. Saliva secretion and pupil diameters were measured, subjective assessments of sleep made using visual analogue scales and side effects, blood counts and biochemistry were monitored. After the first dose mean elimination half lives (t1/2) of bupropion, and metabolites I and II were 8, 19 and 19 h respectively. On repeated administration there was little accumulation of the parent drug and no evidence for induction of its own metabolism. Accumulation of I was consistent with its rate of elimination after single doses while that of II was greater than predicted with prolongation of t1/2 to 35 h. Metabolite III was barely detectable after single doses but its accumulation on multiple dosing was consistent with its long half life (35 h) determined on occasion 2. Saliva secretion was significantly reduced during the multiple dosing period but there were no complaints of dry mouth. Subjective assessments of sleep were not significantly altered though one subject reported vivid dreams. There were no other adverse reactions.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00547376
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  • 7
    Electronic Resource
    Electronic Resource
    Determination of cyclizine and norcyclizine in plasma and urine using gas-liquid chromatography with nitrogen selective detection
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 222 (1981), S. 135-140 
    Details
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/S0378-4347(00)81043-9
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  • 8
    Electronic Resource
    Electronic Resource
    Sensitive assay for pseudoephedrine and its metabolite, norpseudoephedrine in plasma and urine using gas-liquid chromatography with electron-capture detection
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 222 (1981), S. 297-302 
    Details
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/S0378-4347(00)81064-6
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  • 9
    Electronic Resource
    Electronic Resource
    Simple high-performance liquid chromatographic method for the analysis of 9-(2-hydroxyethoxymethyl)guanine (acyclovir) in human plasma and urine
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 224 (1981), S. 51-58 
    Details
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/S0378-4347(00)80137-1
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  • 10
    Electronic Resource
    Electronic Resource
    Specific and sensitive method for the determination of aspirin and salicylic acid in plasma using reversed-phase high-performance liquid chromatography
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 181 (1980), S. 473-477 
    Details
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/S0378-4347(00)81152-4
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