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  • isosorbide-5-mononitrate  (2)
  • pharmacodynamics  (2)
  • Coumarin-like action  (1)
  • Nitrate  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Possible coumarin-like mechanism of action for cephalosporins (1984)
    Springer
    Journal of molecular medicine 62 (1984), S. 885-886 
    Details
    ISSN: 1432-1440
    Keywords: Cephalosporins ; Vitamin K1-epoxide ; Coumarin-like action
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary In three patients treated with cephalosporins (one patient with latamoxef, two patients with cefazedone) vitamin K1 was injected to investigate whether this was followed by an increase in vitamin K1 2,3-epoxide plasma concentrations as compared to controls. Such a rise in K1-epoxide concentrations in the plasma can be demonstrated following treatment with coumarins. This reflects an inhibition of the vitamin K1-epoxide reductase in the liver. Coumarins are thought to induce hypoprothrombinaemia by such a mechanism. In all three patients we found a considerable increase in the vitamin K1-epoxide plasma concentrations following injection of 10 mg vitamin K1, whereas in normal subjects only traces of K1-epoxide could be detected (〈0.030 ”g/ml). The K1-epoxide concentrations found in our three patients treated with cephalosporins were 0.12, 0.16 and 0.19 ”g/ml, respectively. This indicates that latamoxef or cefazedone might reduce clotting factor synthesis by a coumarin-like mechanism of action in these patients. Although the effect of cephalosporins in enhancing vitamin K1-epoxide plasma concentrations is less than that of coumarins, it might cause severe hypoprothrombinaemia in the presence of latent vitamin K deficiency.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01712009
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  • 2
    Electronic Resource
    Electronic Resource
    Die Beziehung zwischen Pharmakokinetik und hĂ€modynamischer Toleranz gegenĂŒber isosorbid-5-Mononitrat (1991)
    Springer
    European journal of clinical pharmacology 40 (1991), S. S151 
    Details
    ISSN: 1432-1041
    Keywords: Nitrate ; Pharmakokinetik ; Pharmakodynamik ; Nitrattoleranz ; Isosorbid-5-Mononitrat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Zusammenfassung Gesunde mĂ€nnliche Probanden erhielten Isosorbid-5-Mononitrat in einer Darreichungsform mit verzögerter Freisetzung (IS-5-MN; 60 mg pro Tablette) nach drei unterschiedlichen Dosierungsschemata. Dosierungsschema I bestand aus einer Einzeldosis von tĂ€glich 60 mg ĂŒber eine Dauer von 5 Tagen. Dosierungsschema II begann mit einer Dosis von 60 mg, gefolgt von einer Dosis zu 30 mg 12 Std spĂ€ter und danach alle 8 Std. Die letzte Dosis, gegeben am fĂŒnften Tage, betrug wiederum 60 mg. Bei Dosierungsschema III folgte auf zunĂ€chst 60 mg jeweils 6 Std spĂ€ter eine Gabe von 30 mg. Diese Dosis wurde ĂŒber eine Dauer von 5 Tagen tĂ€glich gegeben. Die peripheren arteriellen und venösen Wirkungen von IS-5-MN wurden wĂ€hrend des ersten und des letzten Dosierungsintervalls anhand von Änderungen der Fingerpulskurve, des systolischen Blutdrucks im Stehen, der Herzfrequenz und der venösen KapazitĂ€t bestimmt. Die Plasmakonzentrationen von IS-5-MN wurden nach Verabreichung der ersten und der letzten Dosis mehrfach gemessen. Bei der nach Dosierungsschema I durchgefĂŒhrten Behandlung blieben alle hĂ€modynamischen Effekte, die durch die erste Dosis hervorgerufen worden waren, wĂ€hrend der gesamten Studiendauer erhalten. Die maximale Plasmakonzentration betrug 400 ng/ml. Die minimalen Plasmaspiegel lagen unterhalb 100 ng/ml. Bei Dosierungsschema II war die hĂ€modynamische Wirksamkeit von IS-5-MN oder sublingual gegebenem Glyzeroltrinitrat am fĂŒnften Behandlungstage vollstĂ€ndig aufgehoben. Die minimalen Plasmakonzentrationen betrugen wĂ€hrend der gesamten Studienperiode ungefĂ€hr 300 ng/ml. Bei Dosierungsschema III wurden am ersten Tage deutliche hĂ€modynamische Effekte gemessen. Jedoch wurde am fĂŒnften Tage eine signifikante AbschwĂ€chung dieser Effekte festgestellt, wobei die minimalen Plasmakonzentrationen zwischen 100 und 230 ng/ml lagen. Das Ausmaß der am fĂŒnften Tage verbliebenen hĂ€modynamischen Wirkung (gemessen als FlĂ€che unter der Fingerpulskurve) zeigte eine negative Korrelation mit der gemessenen minimalen Plasmakonzentration. Die Aufrechterhaltung von Plasmakonzentrationen von IS-5-MN von mindestens 300 ng/ml fĂŒhrt somit zu einer schnellen Entwicklung einer hĂ€modynamischen Nitrat-Toleranz. DemgegenĂŒber wurde keine Toleranz gesehen, wenn die minimalen Plasmakonzentrationen unter 100 ng/ml absinken konnten. Lagen die minimalen Plasmakonzentrationen zwischen 100 und 230 ng/ml, wurde eine signifikante Verminderung der hĂ€modynamischen Effekte festgestellt. In diesem Konzentrationsbereich stieg das Ausmaß der WirkungsabschwĂ€chung mit ansteigender minimaler Plasmakonzentration von IS-5-MN an.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01418412
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and pharmacodynamics of ramipril and piretanide administered alone and in combination (1994)
    Springer
    European journal of clinical pharmacology 46 (1994), S. 545-550 
    Details
    ISSN: 1432-1041
    Keywords: Ramipril ; Piretanide ; pharmacokinetics ; pharmacodynamics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The pharmacokinetics and pharmacodynamics of single oral doses of 5 mg ramipril and 6 mg piretanide administered separately and in combination were determined in a single blind, randomised, 3-period cross-over study in 24 healthy male volunteers. The peak plasma concentrations of ramipril and ramiprilat increased slightly (from 11.9 to 14.8 ng/ml, and from 6.39 to 8.96 ng/ml, respectively) as did the area under the plasma concentration-time curve of ramipril (0–4 h) and ramiprilat (0–24 h) (from 15.8 to 19.8 ng·ml−1·h, and from 63.4 to 74.6 ng·ml−1·h, respectively). The urinary excretion of ramiprilat also rose (from 6.82 to 7.73 % of dose) following simultaneous treatment with piretanide. These effects were probably due to reduced first-pass metabolism of ramipril/ramiprilat to inactive metabolites. The blood pressure lowering effect, the time course of inhibition of ACE activity in plasma and the concentration-response relationship for the inhibition of plasma ACE activity were not affected by piretanide. The peak plasma concentration of piretanide was somewhat reduced (from 285 to 244 ng/ml) following simultaneous treatment with ramipril. No other pharmacokinetic parameter was affected. Piretanide increased urine flow, and sodium, chloride and potassium excretion, especially during the first 2 hours following administration. These pharmacodynamic parameters were not affected by ramipril. Thus, simultaneous administration of single oral doses of ramipril and piretanide caused modest changes in the peak and average plasma concentrations of both drugs, which did not lead to detectable alterations in the pharmacodynamic parameters measured in healthy volunteers.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00196113
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  • 4
    Electronic Resource
    Electronic Resource
    Relationship between pharmacokinetics and hemodynamic tolerance to isosorbide-5-mononitrate (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. S53 
    Details
    ISSN: 1432-1041
    Keywords: nitrates ; pharmacokinetics ; pharmacodynamics ; nitrate tolerance ; isosorbide-5-mononitrate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Healthy male volunteers received three different dose regimens of a controlled-release form of isosorbide-5-mononitrate (IS-5-MN; 60 mg per tablet). Dose regimen I consisted of a single daily dose of 60 mg given for 5 days. Dose regimen 11 was started with a dose of 60 mg, followed by 30 mg 12 h later and thereafter every 8 h. The last dose, on the 5th day was again 60 mg. In dose regimen III60 mg followed by 30 mg 6 h later were administered every day for 5 days. The peripheral arterial and venous effects of IS-5-MN during the first and last dosing interval were followed by changes in the finger pulse curve, standing systolic blood pressure, heart rate, and venous distensibility. Plasma concentrations of IS-5-MN were measured frequently following the first and the last dose. Following dose regimen I all hemodynamic effects produced by the first dose were maintained during the study. The maximal plasma concentrations were about 400 ng/ml and the trough value, lower than 100 ng/ml. Following dose regimen II the hemodynamic effects of IS-5-MN and sublingual glyceroltrinitrate were completely abolished on the 5th day. Trough plasma concentrations were approximately 300 ng/ml during the entire study period. Following dose regimen III pronounced hemodynamic effects were seen on the 1st day. However, a significant attenuation of the hemodynamic effects was measured on the 5th day, when trough plasma concentrations were between 100 and 230 ng/ml. There was a significant negative correlation between the magnitude of hemodynamic effect remaining on the 5th day (measured by the area under the finger pulse curve) and the trough plasma concentration. Thus, the maintenance of minimum plasma concentrations of IS-5MN of 300 ng/ml or higher produces a rapid development of hemodynamic nitrate tolerance, whereas no tolerance was found when the plasma concentrations were allowed to decline below 100 ng/ml before the next dose was given. A significant attenuation of hemodynamic effects was found when minimum plasma concentrations were between 100 and 230 ng/ml. The degree of attenuation in this concentration range increased with increasing trough plasma concentrations.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01417565
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  • 5
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and haemodynamic effects of ISDN following different dosage forms and routes of administration (1994)
    Springer
    European journal of clinical pharmacology 46 (1994), S. 319-324 
    Details
    ISSN: 1432-1041
    Keywords: Isosorbide dinitrate ; route of administration ; isosorbide-5-mononitrate ; finger pulse wave ; pharmacokinetics ; haemodynamic effects ; plasma nitrates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The pharmacokinetics and haemodynamic effects of isosorbide dinitrate (ISDN) have been investigated following administration of single doses as a sublingual (SL) spray (2.5 mg), sublingual tablet (5 mg) and peroral tablet (10 mg) in a randomised, placebo-controlled double-blind cross-over trial in 16 healthy volunteers. After the sublingual spray Cmax was higher (39.0 ng·ml-1) and tmax was shorter (3.9 min) than after the sublingual (22.8 ng·ml-1 and 13.8 min) and peroral (16.9 ng·ml-1 and 25.6 min) tablets. The AUC of ISDN did not differ following any of the three formulations (1031; 879; 997 ng·ml-1·min, for the spray, SL tablet and PO-tablet, respectively). Mononitrate metabolites of ISDN (IS-2-MN and IS-5-MN) and total nitrates in plasma increased in proportion to the administered dose. This indicates that the fraction of the dose absorbed was the same for all the formulations but that the extent of first-pass metabolism increased in the order sublingual spray 〈 sublingual tablet 〈 peroral tablet. Thus, compared to the spray, the relative bioavailability of ISDN was 48% and 28% from the sublingual and peroral tablets, respectively. The haemodynamic effects were quantified using the a/b ratio of the finger pulse wave and the systolic blood pressure and heart rate under orthostatic conditions. For the a/b ratio of the finger pulse, the maximal effect was higher (emax=130%) and the time to emax (temax) shorter (16.6 min) after the spray than the sublingual tablet (84.4% and 25.5 min) or peroral tablet (90.2 and 31.3 min). The onset of effect was within 3, 5 and 7.5 min after the spray, sublingual and peroral tablets, respectively. A larger change in the orthostatically-induced decrease in systolic blood pressure and increase in heart rate was obtained following peroral than sublingual administration despite the similar plasma concentrations of ISDN. This probably reflects the larger amount of pharmacodynamically active mononitrate metabolites formed after oral dosing. The integrated effect following administration of 2.5 mg ISDN as spray was similar to that of a sublingual tablet of 5 mg.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00194399
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