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  • 1
    ISSN: 1432-1041
    Keywords: rifampicin ; cirrhosis ; primary biliary cirrhosis ; enzyme induction ; hepatic drug metabolism ; bile acids
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Six patients with primary biliary cirrhosis (PBC) were treated with a daily oral dose of 600 mg rifampicin for 2 weeks to induce the hepatic metabolism of drugs and bile acids. On rifampicin 5 of 6 patients experienced a pronounced decrease of their pruritus. In all patients the oxidative cytochrome P-450 dependent drug metabolism was induced as shown by an increase of antipyrine-clearance from 36.3±8.8 to 80.6±20.1 ml/min and an enhanced urinary excretion of 6-β-hydroxycortisol from 454±1.99 to 1607±362 µg/24 h. Furthermore, in all 6 patients the serum alkaline phosphatase declined. In the 3 cholestatic patients (bilirubin〉1.0 mg/dl) the serum concentration of total and conjugated bile acids was strikingly reduced. Thus, rifampicin is an inducer of hepatic metabolism in PBC-patients, ameliorates the pruritus and can lower serum concentrations of alkaline phosphatase and bile acids.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 31 (1986), S. 59-62 
    ISSN: 1432-1041
    Keywords: bisoprolol ; cimetidine ; rifampicin ; interaction ; oxidative liver metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 6 healthy volunteers the pharmacokinetics of bisoprolol under steady-state conditions was investigated over three consecutive phases: over 7 days of 10 mg of bisoprolol once daily per os, 7 days of 10 mg of bisoprolol once daily plus 400 mg of cimetidine t.i.d. and 14 days of 10 mg of bisoprolol and 600 mg of rifampicin once daily with adequate intervals free of medication. After therapy with bisoprolol alone peak plasma levels (C max ss ) of the beta-blocker were 55.5±6.4 ng/ml (x±SEM), area under the plasma level-time curve (AUCτ) was 597±70 ng/ml.h, total body clearance (CL) 15.8±1.8 l/h and elimination half-lives (t1/2β) 10.1±1.2 h. Cimetidine did not cause any significant changes in the pharmacokinetics of bisoprolol. Co-administration of rifampicin resulted in a decrease in C max ss (43.0±6.9 ng/ml), AUCτ (397±54 ng/ml·h) and t1/2β (6.2±0.4 h). Accordingly, total body clearance increased to 23.8±2.51/h (p〈0.05). In conclusion bisoprolol showed a statistically significant but probably clinically not important interaction with the enzyme-inducing drug rifampicin, but not with the enzyme inhibitor cimetidine.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 42 (1992), S. 641-644 
    ISSN: 1432-1041
    Keywords: Testosterone ; Enzyme Induction ; antipyrine ; phenobarbital ; rifampicin ; plasma testosterone ; urinary excretion ; FSH ; LH ; 6β-OH cortisol ; 17-OHCS
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of three different enzyme-inducing drugs (antipyrine 1200 mg, phenobarbital 100 mg, rifampicin 600 mg per day for 7 days) on plasma and urinary testosterone concentrations, plasma gonadotropin levels, antipyrine kinetics, and urinary 6β-hydroxycortisol excretion were studied in 18 healthy volunteers. Changes in plasma and urinary testosterone concentrations following exogenous testosterone undecanoate (TU) were also investigated. Although both antipyrine and rifampicin increased antipyrine clearance by about 60%, they produced contrary effects on testosterone: antipyrine lowered the total morning plasma testosterone and plasma testosterone AUC following TU, while rifampicin led to increases of about 20% and 78%, respectively. By contrast, phenobarbital did not significantly alter the endogenous and exogenous plasma testosterone concentrations, but it increased the urinary excretion of testosterone by more than 60%. The other two enzyme inducers did not alter this parameter. Gonadotropin levels remained unchanged. The results indicate that different enzyme-inducing agents exert divergent effects on endogenous and exogenous testosterone concentrations and suggest that the effect of enzyme induction on endogenous testosterone depends on the type of microsomal enzyme-inducing drug used rather than on the extent of the induction achieved.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1573-7241
    Keywords: tertatolol ; ranitidine ; rifampicin ; interaction ; blood pressure
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 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 $$(\bar X \pm SD)$$ 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〈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.
    Type of Medium: Electronic Resource
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