Interaction of bisoprolol with cimetidine and rifampicin

Kirch, Wilhelm; Röse, I; Klingmann, Ingrid; Pabst, J.; Ohnhaus, E. E.

doi:10.1007/bf00870987

Cited by 41 publications

(28 citation statements)

References 12 publications

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“…Investigations with bisoprolol in healthy volunteers have shown that about 50% of the drug is excreted unchanged by the kidneys and 50% is subjected to oxidative biotransformation (Kirch et al 1986;Leopold et al 1982Leopold et al , 1986. These findings have been confirmed by the results in the healthy subjects in this study.…”

Section: Discussionsupporting

confidence: 89%

“…The data collected did not permit the calculation of the individual bioavailability fractions and the mean value of f was used. This procedure was assumed to be acceptable on the grounds that bisoprolol is a substance which is readily absorbed (> 90%), is subject to only a small first-pass effect (~ 10%), is not influenced by genetic oxidation polymorphism and which is insensitive to liver enzyme inhibition (Kirch et al 1986;Leopold et al 1986). Possible changes in bioavailability of bisoprolol caused by kidney or liver diseases should only be of minor degree.…”

Section: Glossary Of Phannacokinetic Symbolsmentioning

confidence: 99%

“…About 30% of bisoprolol in the plasma is bound to proteins and the plasma elimination half-life is 10 to 12 hours. 50% of the substance is excreted unmetabolised via the kidneys, while 50% is metabolised in the liver and predominantly eliminated via the kidneys in the form of pharmacologically inactive polar metabolites (Kirch et al 1986;Leopold et al 1982Leopold et al , 1986.…”

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confidence: 99%

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Pharmacokinetics of Bisoprolol During Repeated Oral Administration to Healthy Volunteers and Patients with Kidney or Liver Disease

Kirch¹,

Röse²,

Demers

et al. 1987

Clinical Pharmacokinetics

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The pharmacokinetics of bisoprolol were investigated following oral administration of 10mg once daily for 7 days in 8 healthy subjects, in 14 patients with different degrees of renal impairment and in 18 patients with liver disease. In healthy subjects peak and trough steady-state concentrations of 52 micrograms/L and 11 micrograms/L, respectively, an elimination half-life of 10.0 hours and total body clearance of 14.2 L/h were observed. 5.21 mg/24 hours of unchanged bisoprolol were recovered following urinary excretion during the dosage interval. In 11 patients with renal impairment (mean CLCR = 28 +/- 5 ml/min/1.72m2) half-life was prolonged to 18.5 hours, and peak and trough concentrations were 74 and 32 micrograms/L, respectively. Correspondingly, urinary excretion decreased to 3.35 mg/24 hours and total body clearance to 7.8 L/h. In uraemic patients (CLCR less than 5 ml/min/1.73m2) the total clearance of bisoprolol was 5.0 L/h and the elimination half-life was 24.2 hours. In patients with liver cirrhosis half-life increased to 13.5 hours, steady-state peak and trough concentrations increased to 62 and 22 micrograms/L, respectively, and total body clearance decreased to 10.8 L/h. The present study indicates that in patients with impairment of kidney or liver function accumulation of bisoprolol above a factor of 2 did not occur. However, in the terminal stages of insufficiency of kidney or liver function bisoprolol dosage should not exceed 10mg.

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Section: Discussionsupporting

confidence: 89%

Section: Glossary Of Phannacokinetic Symbolsmentioning

confidence: 99%

mentioning

confidence: 99%

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Pharmacokinetics of Bisoprolol During Repeated Oral Administration to Healthy Volunteers and Patients with Kidney or Liver Disease

Kirch¹,

Röse²,

Demers

et al. 1987

Clinical Pharmacokinetics

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“…After a therapy-fl'ee interval of 2 weeks, the crossover to the corresponding treatment phase, administering 600 mg rifampicin once daily or 150 mg vanitidine twice daily to the same patients orally for 7 days, was performed. In earlier studies it had been ascertained that 7 days of rifampicin therapy is sufficiently long enough to achieve the maxinmm enzyme-inducing effect of rifampicin [11]. Circadian blood pressure and heart rate were automatieally measured in all patients using the portable Pressurometer III (del Mar Avionics, Irving, CA, USA), which determined these values every half hour for 24 hours.…”

Section: Methodsmentioning

confidence: 99%

Interaction of tertatolol with rifampicin and ranitidine pharmacokinetics and antihypertensive activity

Kirch

Milferstädt

Halabi

et al. 1990

Cardiovasc Drug Ther

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The interaction of the new beta-receptor antagonist tertatolol with rifampicin and ranitidine was investigated in ten patients with arterial hypertension (WHO stages I-II). They were treated orally with a single dose of tertatolol 5 mg alone and, after randomized allocation, with ranitidine 150 mg twice daily or rifampicin 600 mg once daily for 1 week each (tertatolol 5 mg was concurrently administered on the seventh day of the treatment phases). Following each therapeutic phase, circadian blood pressure values as well as kinetic parameters were obtained. On treatment with tertatolol alone, maximum plasma concentrations were 123.7 +/- 32.4 ng/ml (mean +/- SD) and were reached after 1.95 +/- 1.77 hours. The tertatolol elimination half-life was 9.0 +/- 7.1 hours. Coadministration of ranitidine did not significantly alter the kinetic parameters and antihypertensive effect of tertatolol. Rifampicin, however, decreased the maximum plasma levels of tertatolol to 80.6 +/- 18.5 ng/ml and markedly shortened the elimination half-life to 3.4 +/- 2.6 hours (p less than 0.01 compared with tertatolol alone). Urinary excretion of parent tertatolol and unchanged 4-hydroxy tertatolol was decreased under rifampicin, and a tendency to a reduction in the effect of tertatolol on circadian blood pressure values was observed. Twenty-four hours after administration, the heart rate in those patients on tertatolol alone (68 +/- 6 beats/min) was lower than in those on tertatolol plus rifampicin (74 +/- 7 beats/min). In conclusion, a pronounced pharmacokinetic interaction, with a limited consequence in terms of pharmacodynamic effects, was found in the present study when tertatolol was administered with rifampicin, but not with ranitidine.

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“…Only PRO in high dose showed a marked membrane activity [72]. After oral treatment, ATE significantly reduced blood pressure and heart rate in hypertensive patients but failed to inhibit 5-HT-induced platelet aggregation and 5-HT uptake by thrombocytes [116].…”

Section: Bab Drugs and Platelet 5-htmentioning

confidence: 98%

Antiplatelet and Antileukocyte Effects of Cardiovascular,Immunomodulatory and Chemotherapeutic Drugs

Nosáľ¹

2006

CHAMC

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In vitro and ex vivo interactions of betaadrenoceptor blocking drugs, antihistamines and chloroquine with blood platelets and polymorphonuclear leukocytes resulted in different alterations of regulatory functions of these blood cells. Inhibition of platelet aggregation, arachidonate regulatory pathway, 5-hydroxytryptamine transportation, removal of platelet membrane receptors, inhibition of second messenger pathways at subcellular level and suppression of phagocytosis are indicative of nonreceptor rather than specific receptor interactions. Binding of drugs with biomembranes is reversible depending on the ionic charge of the molecule and hydrophobicity of the bilayer, partition coefficient, pH and pKa of the amphiphilic molecules and other physico-chemical properties of amphiphilic drugs. Alterations in the drug molecule structure alters the drug-phospholipid binding profile. Any change in the metabolism of membrane phospholipids directly or indirectly influences one or more of the important components of the phospholipid-signalling pathway. In addition to changes in phospholipase A, C and D activities, protein kinase C, calmodulin-phosphodiesterase, Ca2+,Mg2+-ATPase, Na+,K+-ATPase and other messengers were found to be changed in cells and tissue after cationic amphiphilic drug (CAD) administration. Although not much has been understood of the mechanism by which some CAD affect immune functions, there are good reasons to suggest that these effects might occur. CADs share sufficient similarities in their structure even though they come from diverse pharmacological classes. CADs affect ion transport, immune functions, tumour growth, serotonin metabolism and several other functions in the body. Extensive therapeutic use and associated side effects have generated a great deal of interest in understanding the nonreceptor interactions with CADs.

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Interaction of bisoprolol with cimetidine and rifampicin

Cited by 41 publications

References 12 publications

Pharmacokinetics of Bisoprolol During Repeated Oral Administration to Healthy Volunteers and Patients with Kidney or Liver Disease

Pharmacokinetics of Bisoprolol During Repeated Oral Administration to Healthy Volunteers and Patients with Kidney or Liver Disease

Interaction of tertatolol with rifampicin and ranitidine pharmacokinetics and antihypertensive activity

Antiplatelet and Antileukocyte Effects of Cardiovascular,Immunomodulatory and Chemotherapeutic Drugs

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