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  • pharmacokinetics  (44)
  • 1985-1989  (44)
  • 1955-1959
  • 1986  (44)
  • 1
    Electronic Resource
    Electronic Resource
    Isosorbide dinitrate in plasma and dialysate during haemodialysis (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 187-190 
    Details
    ISSN: 1432-1041
    Keywords: isosorbide dinitrate ; haemodialysis ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 10 patients with end stage renal disease on regular haemodialysis the plasma concentrations and dialyzer clearance of isosorbide dinitrate (ISDN) were determined after an oral dose of a retarded release formulation of 60 mg ISDN. The maximal plasma concentration of ISDN 2–7 h after oral administration was higher (14 ng/ml) than has been reported in healthy volunteers. The haemodialyzer clearance of ISDN was 92.4 ml/min at a blood flow of 200 ml/min and dialysate flow of 500 ml/min. During a 5-h haemodialysis an average of 0.3 mg ISDN was removed from the patient's circulation, representing about 0.5% of the administered dose and about 3% of the available drug in the circulation. No influence of haemodialysis on the plasma level of ISDN was found.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614300
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  • 2
    Electronic Resource
    Electronic Resource
    The pharmacokinetics ofα-human atrial natriuretic polypeptide in healthy subjects (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 101-103 
    Details
    ISSN: 1432-1041
    Keywords: atrial natriuretic polypeptide ; α-hANP ; pharmacokinetics ; radioimmunassay
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have analysed the pharmacokinetics ofα-human atrial natriuretic polypeptide (α-hANP) in healthy subjects, using a two-compartment open model following bolus intravenous injection. The plasma half-times for the fast and slow components were 1.7±0.07 min and 13.3±1.69 min respectively. V1 (the volume of the central compartment), Vz (volume of distribution) and Vss (volume of distribution at steady-state) were 5370±855 ml (89.5±14.3 ml·kg−1), 32000±4620 ml (533±77.0 ml·kg−1), and 11900±1530 ml (198±25.5 ml·kg−1) respectively. The mean plasma clearance was 1520±121 ml·min−1 (25.4±2.0 ml·min−1·kg−1.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870995
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  • 3
    Electronic Resource
    Electronic Resource
    The effects of domperidone on the absorption of levodopa in normal subjects (1986)
    Springer
    European journal of clinical pharmacology 29 (1986), S. 721-723 
    Details
    ISSN: 1432-1041
    Keywords: domperidone ; levodopa ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of simultaneous oral administration of 20, 40, or 80 mg domperidone on the pharmacokinetics of an oral 500 mg dose of levodopa was studied in eight normal women. No significant differences in maximum plasma levodopa concentration, the time of its attainment, or the area under the plasma levodopa concentration versus time profile occurred. Domperidone significantly reduced the incidence of adverse gastrointestinal effects due to levodopa administration.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00615966
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  • 4
    Electronic Resource
    Electronic Resource
    Cefodizime penetration into skin suction blister fluid following a single intravenous dose (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 295-298 
    Details
    ISSN: 1432-1041
    Keywords: cefodizime ; skin suction blister fluid ; pharmacokinetics ; protein binding ; healthy subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Cefodizime pharmacokinetics was investigated, evaluating drug concentrations in serum, skin suction blister fluid (SBF), saliva and urine in six healthy male subjects who were administered a 1-g dose intravenously. Serum levels in five subjects can be described according to a two-compartment open model; terminal half-life is 181±14 min. Volume of distribution (Vdβ) amounts to 15.3±1.61, serum clearance to 59±6 ml/min, renal clearance to 33±3 ml/min. Of the administered dose, 54% is renally excreted unchanged within 27 h. Unbound drug fraction in serum is 19.0% and in SBF 38.4%. Thus renal clearance of free cefodizime amounts to 172 ml/min, Vdss to 68.91 (free drug). Whereas cefodizime has not been detected in saliva samples, SBF concentration 3–9 h post administration parallel serum levels, amounting to 40% of the respective serum concentration. At 9 h, unbound cefodizime concentrations in SBF amount to 1.4±0.4 µg/ml, this value being well above the MIC90% values of many clinically relevant bacteria.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541531
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  • 5
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of ergotamine in healthy volunteers following oral and rectal dosing (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 331-334 
    Details
    ISSN: 1432-1041
    Keywords: ergotamine ; pharmacokinetics ; volunteers ; mass spectrometry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Twenty-four healthy volunteers participated in a study on the disposition of ergotamine following oral and rectal administration. Plasma samples were collected surrounding each dose of medication and a new mass spectrometry method was used for quantitation of the samples. A mean peak plasma concentration of 454 pg/ml was measured an average of 50 min following a 2 mg rectal dose. In contrast, the 2 mg oral dose produced a mean peak plasma concentration of 21 pg/ml an average of 69 min following the dose. Area under the concentration time curve indicated a relative bioavailability of 5% for the oral dosage form. Conflicting data on ergotamine disposition highlight the factors which may be responsible for determining bioavailability and pharmacologic activities of the compound.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541538
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  • 6
    Electronic Resource
    Electronic Resource
    Lack of effect of cimetidine on pharmacodynamics and kinetics of single oral doses of R- and S-acenocoumarol (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 619-623 
    Details
    ISSN: 1432-1041
    Keywords: acenocoumarol ; cimetidine interaction ; stereoselectivity ; healthy subjects ; pharmacokinetics ; anticoagulant effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics and dynamics of single doses (5 mg p.o.) of the optical isomers of acenocoumarol (R-AC and S-AC) were followed in healthy subjects and the effect on them of cimetidine 800 mg/day was also investigated. The AC enantiomers differed greatly in their pharmacokinetics. The mean residence time (MRT) of R-AC was about 10 times longer than that of S-AC, 15 h vs 1.2 h. There was no difference in the volume of distribution. Depression of blood clotting activity (Thrombotest) was observed only after administration of R-AC. The inactivity of S-AC as a vitamin K antagonist must be ascribed to its short MRT. Cimetidine did not affect the acute oral kinetics of R- and S-AC, nor did it affect the anticlotting activity of R-AC. The urinary excretion pattern of the 6- and 7-hydroxylated AC metabolites was not altered during cimetidine treatment. Although the present studies showed no effect of cimetidine on the pharmacokinetics and dynamics of acenocoumarol, the findings of Serlin et al. [3] suggest that cimetidine should not be administered during acenocoumarol therapy.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542424
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  • 7
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of single and multiple doses of flusoxolol (Ro 31-1411) in healthy subjects (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 113-115 
    Details
    ISSN: 1432-1041
    Keywords: flusoxolol ; multiple-dose ; pharmacokinetics ; Ro 31-1118 ; optical isomer
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Flusoxolol (Ro 31-1411) is the pharmacologically active optical isomer of Ro 31-1118, a potent cardioselective β-adrenoceptor antagonist with partial agonist activity. It was given to 6 healthy volunteers in a single dose, 40 mg, and then in multiple doses, 40 mg daily for 8 days. Plasma concentration data were best described by a linear two-compartment pharmacokinetic model with first order absorption, and the results confirmed linear kinetics. Pharmacokinetic data for flusoxolol were comparable to those for the racemate Ro 31-1118.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870998
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  • 8
    Electronic Resource
    Electronic Resource
    Antiemetic effect and pharmacokinetics of high dose metoclopramide in cancer patients treated with cisplatin-containing chemotherapy regimens (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 33-40 
    Details
    ISSN: 1432-1041
    Keywords: metoclopramide ; high dose ; antiemetic efficacy ; cancer patients ; pharmacokinetics ; cisplatin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Fifteen cancer patients receiving cisplatin-containing chemotherapy participated in two antiemetic studies. In Study 1 they received standard antiemetics in low doses on demand, and in Study 2 the same patients participated in an open randomized cross-over study between metoclopramide 1 and 2 mg/kg i.v.×5. Serum metoclopramide was determined by HPLC. Self-reporting of nausea using a visual analogue scale (VAS) was compared with observer rated scores. Tolerability and volume vomited were assessed by nurse observers. The biological half-life of metoclopramide was 9.9 h, the volume of distribution was 9.9 l/kg and the clearance was 0.68 l/h/kg. The pharmacokinetics of high dose metoclopramide was linear in the range 0.15–2 mg/kg×5, with very little accumulation. Compared to standard antiemetics, both high dose regimens of metoclopramide had a significant effect on nausea, but no effect on the volume vomited. Self reports of nausea were significantly correlated with observer rated values. Tolerance of high dose metoclopramide was good except in 3 patients who left the study because of restlessness and trismus. It is concluded that high dose metoclopramide probably can be administered for several consecutive days without appreciable accumulation of the drug. Self-reporting of nausea by patients on VAS is a simple and feasible method of evaluation. The finding that metoclopramide affects nausea but not vomiting supports the hypothesis that nausea and vomiting should be evaluated separately in assessing antiemetic efficacy.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00870982
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  • 9
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of diclofenac sodium after intramuscular administration in combination with triamcinolone acetate (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 363-365 
    Details
    ISSN: 1432-1041
    Keywords: diclofenac sodium ; triamcinolone acetate ; pharmacokinetics ; drug interactions ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Seventy-five mg diclofenac sodium were given intramuscularly to 15 subjects alone and in combination with 40 mg triamicinolone acetate. Plasma levels of diclofenac were measured and pharmacokinetic parameters were calculated. The results indicate no statistically significant differences for most of the parameters. The maximum plasma concentrations (Cpmax) was increased by about 20% in combination with the glucocorticoid, whereas terminal elimination rate did not change significantly.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981139
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  • 10
    Electronic Resource
    Electronic Resource
    Comparative pharmacokinetics and cardiovascular effects of tiapamil in healthy volunteers and patients with hepatic cirrhosis (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 397-404 
    Details
    ISSN: 1432-1041
    Keywords: tiapamil ; desmethyltiapamil ; pharmacokinetics ; cardiovascular effects ; cirrhotic patients ; plasma protein binding ; impaired hepatic elimination ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Tiapamil 70 mg was administered i.v. to 8 healthy male volunteers and 8 patients (7 males, 1 female) with biopsy proven hepatic cirrhosis. Two of the patients also received 600 mg p.o. Serial plasma and urine samples were collected and the parent drug in plasma and urine and desmethyl-tiapamil in urine were assayed by a specific HPLC method. The plasma and urine data for the parent drug after i.v. and p.o. dosing were simultaneously fitted to linear p.o. and i.v. two compartment models with exit from and input into the central compartment. Absorption was assumed to be a first order process. In the volunteers the mean pharmacokinetic parameters were: 101 l for the steady-state volume of distribution, 750 ml·min−1 for nonrenal clearance, 195 ml·min−1 for renal clearance and 1.7 h for the half-life of the terminal disposition phase. The urinary recoveries of the parent drug and desmethyltiapamil averaged 21.4 and 0.8% of the dose, respectively. In the patients the steady-state volume of distribution, the amount of unchanged drug in urine and the half-life of the terminal disposition phase were significantly increased (171 l, 29.0% of the dose, 3.5 h, respectively). Decreased plasma protein binding in the patients accounted for the larger steady-state volume of distribution. The nonrenal clearance of 519 ml·min−1, tended to be smaller in the patients than in the volunteers. Together with the increased urinary recovery of tiapamil in the patients this indicates a moderately impaired elimination capacity in the cirrhotics. The renal clearance was similar in the patients (213 ml·min−1) and the volunteers. The absolute oral bioavailability of tiapamil was 55 and 49% in 2 patients. No effects of tiapamil on heart rate or supine blood pressure were detected, either in volunteers or in patients. Negative dromotropic effects were found in 2 volunteers and 2 patients after i.v. dosing.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613513
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