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  • enzyme induction  (2)
  • propranolol  (2)
  • 1
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 13 (1978), S. 13-16 
    ISSN: 1432-1041
    Schlagwort(e): Pharmacokinetics ; beta-blocking drugs ; pindolol ; propranolol ; multiple doses ; steady state concentration
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of pindolol were studied in six healthy individuals following a single 10 mg dose (SD) and multiple (5 mg tid over 6 days) doses (MD). The plasma elimination half-life was identical after SD (4.7±0,8 h) and MD (4.1±1.1 h). Steady state plasma concentrations were reached after 36 h and remained stable thereafter. The variation in steady state concentrations was small in each individual and also between individuals. The steady state concentration of pindolol can be predicted from the pharmacokinetic data obtained after a single dose. The results of the present study suggest that the disposition of pindolol is linear over the concentration range studied.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 22 (1982), S. 85-90 
    ISSN: 1432-1041
    Schlagwort(e): lignocaine ; verapamil ; propranolol ; bioavailability ; predictions ; first pass effect ; oral clearance
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary For drugs with a high hepatic clearance, bioavailability is low due to the so-called “first pass effect”. Prediction of the bioavailability for these drugs has been only lossely tested. It is proposed that by plotting the reciprocal of bioavailability versus the oral clearance, a straight line with intercept of unity and slope of reciprocal of hepatic blood flow should ensue. For lignocaine and verapamil, this relationship was found to be strong and gave good predictability, whereas for propranolol this relationship was weak and gave poor predictability. The proposed method may be of value in determining whether the low bioavailability of a drug is due to hepatic first pass metabolism.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 3
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 19 (1981), S. 343-347 
    ISSN: 1432-1041
    Schlagwort(e): cimetidine ; phenobarbital ; gastro-intestinal absorption ; bioavailability ; renal clearance ; non-renal clearance ; enzyme induction
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of orally administered cimetidine was studied in 8 healthy subjects before and after 3 weeks of treatment with phenobarbital 100 mg daily, and in a separate study 4 subjects received cimetidine intravenously before and after the administration of phenobarbital. There was no change in the volume of distribution, but total plasma clearance was increased by a mean of 18%, mainly due to a 37% increase in nonrenal clearance. Renal clearance and half-life were not significantly altered. The area under the plasma concentration-time curve after oral administration was significantly (P≪0.05) reduced by a mean of 15% after phenobarbital treatment. The amount of cimetidine excreted in urine and its sulphoxide metabolite were significantly (P〈0.05) reduced, on average by 34% and 26%, respectively by phenobarbital treatment. The data indicate that an apparent 20% reduction in the absorption of cimetidine was due to induction of gastrointestinal metabolism of cimetidine, with some contribution also from hepatic metabolism. Reduced absorption per se could not be totally excluded. Although the magnitude of the change was small, the finding of an 11% decrease in the time to achieve an effective plasma level of cimetidine after phenobarbital treatment may contribute to the ineffectiveness of cimetidine in certain patients.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 4
    Digitale Medien
    Digitale Medien
    Springer
    Journal of molecular medicine 51 (1973), S. 1081-1090 
    ISSN: 1432-1440
    Schlagwort(e): Anticoagulants ; coumarins ; drug interaction ; protein binding ; enzyme induction ; enzyme inhibition ; Antikoagulantien ; Cumarine ; Arneimittelwechselwirkung ; Interaktion ; Eiweißbindung ; Enzyminduktion ; Enzymhemmung
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Beschreibung / Inhaltsverzeichnis: Zusammenfassung Eine große Zahl von Medikamenten tritt bei gleichzeitiger Gabe in Interaktion mit Cumarinderivaten. Wesentliche Mechanismen sind dabei Resorptionshemmung, Verdrängung aus der Plasmaeiweißbindung, Hemmung oder Induktion des metabolisierenden Enzymsystems sowie Beeinflussung von Synthese oder Abbau der Vitamin Kabhängigen Gerinnungsfaktoren. Auch die Cumarine selbst sind in der Lage, die Metabolisierung anderer Pharmaka hemmend zu beeinflussen. Es ergibt sich die Notwendigkeit, neu einzuführende Medikamente auf die Interaktion mit Cumarinen zu testen. Eine sorgfältige Überwachung des Patienten ist bei Beginn oder Beendigung jeder Therapie mit einem in Kombination mit Cumarinen eingesetzten Pharmakon angezeigt.
    Notizen: Summary Many drugs are known to modify the pharmacological action of coumarin anticoagulants when administered simultaneously. Mechanisms of interaction may consist in inhibition of absorption, displacement from protein binding sites, inhibition or induction of drug metabolizing enzymes in liver microsomes, and effect on synthesis and metabolization of the vitamin K-dependent clotting factors. Coumarins also may inhibit the metabolic degradation of other drugs. It is therefore necessary to test new compounds for a possible interaction with coumarin agents. Patients treated with coumarin anticoagulants should be controled carefully for changes in the hypoprothrombinaemic action when additional drugs are given or when these are discontinued.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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