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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 24 (1983), S. 349-352 
    ISSN: 1432-1041
    Keywords: diltiazem ; pharmacokinetics ; intravenous dose ; oral dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetic profile of diltiazem, a novel calcium antagonist, was studied in 12 volunteers following oral (60 mg) and intravenous (15 mg) administration. After i.v. administration biphasic elimination was observed, with a distribution half-life of 0.3±0.2 h and an elimination half-life of 3.1±1.0 h; the apparent volume of distribution was 5.3±1.71/kg and the total clearance was 1.28±0.48 l/kg/h. After the oral dose the elimination phase had a half-life of 3.2±1.3 h. The absolute bioavailability of diltiazem ranged from 24 to 74% (mean 42±18%). The interindividual variation may be explained by a variable first pass effect.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 37 (1989), S. 245-248 
    ISSN: 1432-1041
    Keywords: breast milk ; zolpidem ; pharmacokinetics ; imidazopyridine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Five, lactating, healthy white women were treated with a single 20 mg tablet of zolpidem 3–4 days after the delivery of a full term baby. The drug was administered at 20.00 h, 30 min after dinner, and milk samples were collected before and 3, 13 and 16 h. Venous blood 5 ml was taken before and 1.5, 3, 13, 16 h after zolpidem administration. The apparent elimination half life, estimated from plasma zolpidem concentrations was 2.6 h. The amount of zolpidem excreted in the milk at 3 h ranged between 0.76 and 3.88 µg, which represented 0.004 to 0.019% of the administered dose; no detectable (below 0.5 ng/ml) zolpidem was found in the milk at subsequent sampling times. The ratio of the zolpidem concentrations in breast milk and plasma at 3 h was 0.13. The apparent breast milk clearance of zolpidem, calculated from the ratio of the total amount of zolpidem excreted in milk to its AUC in plasma was 1.48 ml/h. The results show that the excretion of zolpidem in human milk is very low (below 0.02%) and that most of it takes place during the first 3 h following drug intake.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 0306-042X
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Betaxolol, a beta selective adrenoceptor antagonist recently approved for the treatment of hypertension, was determined by monitoring in chemical ionization mode with ammonia the [MH]+ ions of the trimethylsilyl derivatives of the drug and of its internal standard ((2H5)betaxolol). Its pharmacokinetic profile obtained following administration of a 20 mg oral dose was characterized by a half-life of 22 h and a bioavailability of 85%. The main acid metabolite formed by elimination of the isopropylamino group may also be determined as the methyl TMS derivative but methylation with BF3-methanol should be used with caution since it may induce the opening of the cyclopropyl group. The routine electron capture determination procedure was compared to this mass spectrometric method and an excellent correlation was found (r = 0.9974). Both procedures have the same sensitivity (1 ng ml-1). Finally it was observed that under electron impact mode betaxolol trimethylsilyl side chain rearranged to lose TMS—O—CH=CH2; this elimination was confirmed by deuterium labelling studies.
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
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