• Corpus ID: 13926853

Studies on Drug Interactions between CYP 3 A 4 Inhibitors and Glucocorticoids by

@inproceedings{Varis2000StudiesOD,
  title={Studies on Drug Interactions between CYP 3 A 4 Inhibitors and Glucocorticoids by},
  author={Tiina Varis},
  year={2000}
}
............................................................................................................................8 INTRODUCTION ...................................................................................................................9 REVIEW OF THE LITERATURE......................................................................................10 1. Drug metabolism.............................................................................................................10… 
ethesis.helsinki.fi

References

SHOWING 1-10 OF 232 REFERENCES

The effects of diltiazem on hepatic drug metabolizing enzymes in man using antipyrine, trimethadione and debrisoquine as model substrates.

Six healthy male subjects were given single oral doses of antipyrine, trimethadione and debrisoquine before and during diltiazem treatment (30 mg three times daily orally for 8 days), which selectively inhibits cytochrome P-450 isoenzymes.

Comparative effects of the antimycotic drugs ketoconazole, fluconazole, itraconazole and terbinafine on the metabolism of cyclosporin by human liver microsomes.

  • D. BackJ. Tjia
  • Biology, Medicine
    British journal of clinical pharmacology
  • 1991
Ketoconazole is confirmed as being a potent inhibitor of cyclosporin metabolism and this has clinical relevance, and inhibition by fluconazole was much less than that by itraconazole at equimolar concentrations, it should be noted that in patients plasma concentrations of flu Conazole are much greater than those of itraconsazole.

Metabolic interactions between mibefradil and HMG-CoA reductase inhibitors: an in vitro investigation with human liver preparations.

Mibefradil is a potent mechanism-based inhibitor of CYP3A4/5, and it is anticipated that clinically significant drug-drug interactions will likely ensue when mibef Radil is coadministered with agents which are cleared primarily by CYP 3A-mediated pathways.

Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A.

It is shown that the mouse mdr1a and the human MDR1 P-glycoprotein actively transport ivermectin, dexamethasone, digoxin, and cyclosporin A and, to a lesser extent, morphine across a polarized kidney epithelial cell layer in vitro.

Oxidation of the antihistaminic drug terfenadine in human liver microsomes. Role of cytochrome P-450 3A(4) in N-dealkylation and C-hydroxylation.

Evidence is provided that P- 450 3A4 (and possibly other P-450 3A enzymes) play a major role in the oxidation of (both enantiomers of) terfenadine to both of its major oxidation products.

Effects of the Antifungal Agents on Oxidative Drug Metabolism

The interactions of ketoconazole with cyclosporin and tacrolimus have been applied for therapeutic purposes to allow a lower dosage and cost of the immunosuppressant and a reduced risk of fungal infections.

Protein binding of itraconazole and fluconazole in patients with cancer.

Both antifungal drugs show different protein binding behaviour in cancer patients, and a weak association between the binding of these drugs and serum protein levels has been observed.

Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.

The extent and the severity of the observed drug interactions in humans suggest that inhibition of additional systems important to drug disposition, such as the drug transporter P-glycoprotein (P-gp), may also have contributed to the severe drug-drug interactions of mibefradil.

Modulation and prevention of multidrug resistance by inhibitors of P-glycoprotein

Findings suggest that MDR modulation may delay the emergence of clinical drug resistance and support the concept of prevention of drug resistance in the earlier stages of disease.

The role of human cytochrome P450 enzymes in the metabolism of anticancer agents: implications for drug interactions.

Although cyclosporin and calcium channel blockers may influence the pharmacokinetics of certain anticancer agents by inhibiting their CYP3A mediated metabolism, it is more likely that these P-glycoprotein inhibitors inhibit P- glycoprotein mediated drug elimination.
...