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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 18 (1980), S. 151-157 
    ISSN: 1432-1041
    Keywords: amitriptyline ; nortriptyline ; tyramine sensitivity ; steady-state ; pharmacodynamic half-life ; pharmacokinetic half-life
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A combined pharmacodynamic and pharmacokinetic approach was made to study the pharmacodynamic half-life (Pd1/2) of amitriptyline (AT). Six depressed patients were treated with 150 mg of amitriptyline as a single oral dose at night for six or more weeks. Decreased tyramine sensitivity (DTS), an index of this drug's pharmacological activity, was determined serially at various intervals after the last dose. Plasma concentrations of AT and nortriptyline (NT) were also estimated at above intervals. It was possible to detect DTS for 228–300 h after the last oral dose and the mean Pd1/2 of this decline of pharmacodynamic effect was observed to be 135 h. However, no measurable amount of AT or NT was present after 84 h and the mean elimination plasma half-life (t1/2) of AT and NT were 37.7 and 38.9 h, respectively. (In this study, pharmacokinetic parameters of NT were directly related with those of AT.) Prolonged pharmacodynamic effect of this drug after discontinuation should be borne in mind in order to avoid drug interactions and autonomic complications, especially after overdosage. Pd1/2, as assessed by DTS, correlated directly with the t1/2 (r=0.91) and inversely with the plasma clearance rate (r=0.60) of NT. DTS test can be used as an alternative technique to assess the biological activity of a drug which inhibits noradrenaline reuptake mechanism and/or blocks α-adrenoceptors at the peripheral neuronal sites, especially, where facilities to measure plasma concentrations of such drugs are limited.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 24 (1983), S. 375-381 
    ISSN: 1432-1041
    Keywords: epilepsy ; carbamazepine ; 10 ; 11-carbamazepine epoxide ; dosage frequency ; serum level
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of dosage frequency of carbamazepine (CBZ) (brand name Tegretol) on pseudosteady state drug serum levels were studied in 14 male (16–18 years) epileptics. They had already been receiving CBZ (mean dose 13.7 mg/kg) for an average period of 2.3 years in combination with other antiepileptic drugs. During this investigation, total daily CBZ dose was kept unaltered, but they received medication in thrice, twice and once daily dosage regimes. Each treatment period lasted for 4 weeks. The profiles of 24 h serum drug levels, as assessed at the end of each treatment period, were observed to be within the therapeutic range during these 3 regimes. However, as expected, there were higher fluctuations of serum CBZ concentrations during once daily medication than during divided dosage regimes. Other concomitant antiepileptic drugs were continued in 2–3 divided daily doses during these 3 treatment periods, and the serum drug levels were measured at 8 h prior to the morning dosing. The concentrations of other drugs remained unchanged apart from a slight decrease in the serum sodium valproate levels during once daily medication. No clinical or electroencephalographic adverse effects were observed and there was no significant change in the fit frequency. In view of this observation, CBZ (Tegretol tablet) is probably effective as a single daily dose, but further long-term controlled clinical trial is necessary.
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  • 3
    ISSN: 1432-1041
    Keywords: benazepril ; benazeprilat ; ACE inhibitor ; pharmacokinetics ; pharmacodynamics ; elderly ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and pharmacodynamics of a single oral dose benazepril·HCl 10 mg have been studied in 15 healthy volunteers aged 65 to 80 y. The kinetics of unchanged benazepril and its active metabolite benazeprilat did not differ significantly in males and females, so the combined kinetic data from all 15 elderly subjects were compared with a historical control group of 19–32 year-old healthy men treated in the same way. The disposition of benazepril was not affected by age. The time to maximum plasma concentration, tmax (0.5 h) and elimination half-life (0.6 h) in the elderly were the same as in young subjects. The kinetics of benazeprilat was slightly changed in the elderly; although its tmax (1.5 h) was not affected, Cmax and the AUC were 20–40% greater. The elimination half-life of benazeprilat during the first 24 h after doing in the elderly was increased by about 20% to 3.2 h. The renal plasma clearance of benazeprilat (18.1 ml·min−1) was about 20% smaller than in the young subjects. An average of 18.5% of the dose was recovered as benazeprilat in the 24 h urine from the elderly subjects, which was similar to the recovery in the young subjects. Both benazepril and benazeprilat were highly bound to serum proteins (96 and 95%, respectively). Mean systolic and diastolic blood pressures in the elderly were reduced by a maximum of 37/16 mm Hg at 6 h, in association with a small rise in pulse rate. Treatment was generally well tolerated. Three of the 15 subjects reported clinical adverse experiences judged to be possibly drug related, namely headache, abdominal pain and cold extremities.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 17 (1980), S. 233-238 
    ISSN: 1432-1041
    Keywords: tyramine ; noradrenaline ; phenylephrine ; pressor response test ; re-uptake ; adrenergic receptor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Tyramine, noradrenaline and phenylephrine pressor response tests were performed in patients suffering from affective disorders during various drug therapies or following electroconvulsive therapies (ECT). Tricyclic and related antidepressive drugs produced decreased tyramine sensitivity and increased noradrenaline sensitivity as expected from their usual characteristic to inhibit the neuronal noradrenaline reuptake mechanism. These drugs also block the post-synaptic adrenergic receptors which was indicated by decreased phenylephrine sensitivity. However, the degree of blockade was variable and some of the newer drugs, in the dosage used, were devoid of these peripheral interactions. No significant change in these pressor response tests were observed in patients who had 3 or more ECT. On the other hand, patients treated with lithium carbonate for 4 or more weeks, had decreased phenylephrine and noradrenaline sensitivities, which were not associated with any change in tyramine sensitivity. It was postulated that lithium not only increased the neuronal amine uptake, but also decreased the sensitivity of the α-adrenergic receptors. Treatment with haloperidol for 48 h decreased 2.5 times tyramine sensitivity, which could be due to postsynaptic receptor blockade or inhibition of amine reuptake process, or both. Since no noradrenaline or phenylephrine sensitivity was determined, it was difficult to be precise. The pressor response tests were shown to be safe, reproducible, and reliable in providing informations regarding peripheral adrenergic interactions. It was suggested that all these 3 pressor response tests should be performed, otherwise incomplete or erroneous conclusions may be drawn.
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 33 (1987), S. 505-509 
    ISSN: 1432-1041
    Keywords: lofepramine ; amitryptyline ; anticholinergic effect ; adverse effects ; psychometric tests
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a double-blind five-way cross-over study, six drug free healthy elderly subjects received single oral doses of lofepramine (70 mg, 105 mg and 140 mg), amitriptyline (50 mg) and matched placebo tablets. A dose related increase in plasma drug levels and pharmacological effects of lofepramine was observed. Lofepramine (140 mg) improved psychomotor performance (choice reaction time and letter cancellation), but no such change was seen with lower dose regimes or placebo. No significant differences between lofepramine and placebo were observed in other parameters measured. Amitriptyline, as expected, reduced salivary volume, produced drowsiness and impaired psychomotor performance. These changes correlated with plasma amitriptyline levels. The incidence of subjective side-effects with amitryptyline was also higher than that of lofepramine or placebo. In the dosage used, lofepramine exhibited no deleterious effect on the peripheral cholinergic system or psychomotor performance. This drug therefore is likely to be a relatively safe antidepressant for the elderly, but further investigations during long-term medication are required to verify these observations.
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  • 6
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Chemical Physics Letters 187 (1991), S. 637-641 
    ISSN: 0009-2614
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Naturwissenschaften 51 (1964), S. 364-365 
    ISSN: 1432-1904
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology , Natural Sciences in General
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Journal of thermal analysis and calorimetry 36 (1990), S. 869-880 
    ISSN: 1572-8943
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Mittels DTA/TG/DTG, XRD sowie IR wurde die thermische Zersetzung von Bis-hydrazinocarboxylat-eisen(II)-dihydrazinat untersucht. Die thermische Zersetzung verläuft in sechs Schritten und endet bei genügend niedriger temperatur mit der Bildung vonγ-Fe2O3. Durch Auswertung der Untersuchungsdaten konnten die einzelnen Zwischenprodukte, darunter eine neuartige Verbindung FeO2.2CO, identifiziert werden.
    Notes: Abstract Low temperature (T〈200°C) thermal decomposition in air of bishydrazinocarboxylate iron(II) dihydrazinate [Fe(II)(N2H3COO)2(N2H4)2] is known to produceγ-Fe2O3 in ultrafine form [1–4]. This decomposition process is known to be exothermal and autocatalytic but details regarding the stepwise mechanism of decomposition is yet unknown although a few attempts have been made with limited success [1, 5]. In our present work, we have combined the results from (i) thermal analysis of complex precursor and (ii) characterization of products isolated at intermediate and final stages of decomposition in order to explain the stepwise mechanism of decomposition of Fe(N2H3COO)2(N2H4)2 in air.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Mycopathologia 79 (1982), S. 79-85 
    ISSN: 1573-0832
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract A total of 21 cases of granuloma caused by Aspergillus species were encountered during the period 1972–79. The organs involved were nasal and paranasal sinuses, brain, orbit, subcutaneous tissue of cheek, lungs and endocardial valve in the decreasing order of their frequency. Aspergillus flavus was the main etiological agent. Immunodiffusion tests with various Aspergillus species as antigen showed a positivity of 17 out of 18 (94.4 per cent) cases. The role of precipitins in diagnosis and prognosis of the disease has been discussed.
    Type of Medium: Electronic Resource
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  • 10
    Publication Date: 1987-01-01
    Print ISSN: 0031-6970
    Electronic ISSN: 1432-1041
    Topics: Chemistry and Pharmacology , Medicine
    Published by Springer
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