Can grapefruit juice influence ethinylestradiol bioavailability?

Contraception

Volumn 53, Issue 1, 1996, Pages 41-47

  Weber, A ^a   Jager R ^a   Borner A ^a   Klinger, G ^a   Vollanth, R ^a   Matthey, K ^b   Balogh, A ^a,b  

^a BAYER PHARMA AG   (Germany)

^b FRIEDRICH SCHILLER UNIVERSITY JENA   (Germany)

Author keywords

17 ethinylestradiol; cytochrome P450; flavonoids; food drug interactions; grapefruit juice; naringenin; pharmacokinetics

Indexed keywords

CYTOCHROME P450; ETHINYLESTRADIOL;

ADULT; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG DEGRADATION; DRUG FORMULATION; FEMALE; FOOD DRUG INTERACTION; FRUIT JUICE; HUMAN; HUMAN EXPERIMENT; NORMAL HUMAN; ORAL CONTRACEPTION; ORAL DRUG ADMINISTRATION; RANDOMIZED CONTROLLED TRIAL; TEA;

EID: 0342655944     PISSN: 00107824     EISSN: None     Source Type: Journal    
DOI: 10.1016/0010-7824(95)00252-9     Document Type: Article

References (45)

1. Bolt HM, Bolt M, Kappus H. Interaction of rifampicin treatment with pharmacokinetics and metabolism of ethinylestradiol in man. Acta Endocrinol 1977;85:189-97.
2. Reimers D, Nocke-Fink L, Breuer H. Rifampicin and the "pill" do not go well together. Am Med Assoc 1974; 277:608-11.
3. Rogers SM, Back DJ, Stevenson PJ, Grimmer SFM, Orme ML'E. Paracetamol interaction with oral contraceptive steroids: increased plasma concentration of ethinylestradiol. Br J Clin Pharmacol 1987;23:721-5.
4. Back DJ, Breckenridge AM, Maclver M, Orme ML'E, Purba HS, Rowe PH. Interaction of ethinylestradiol with ascorbic acid in man. J Br Med 1981;282:1516.
5. Bolt HM, Kappus H, Bolt M. Effect of rimpacin treatment on the metabolism of oestradiol and 17α-ethinylestradiol by human liver microsomes. Eur J Clin Pharmacol 1975;8:301-7.
6. Guengerich FP. Inhibition of oral contraceptive steroid-metabolizing enzymes by steroids and drugs. Am J Obstet Gynaecol 1990;63:2159-63.
7. Back DJ, Bates M, Bowden A, Breckenridge AM, Hall MJ. The interaction of phenobarbital and other anticonvulsants with oral contraceptive steroid therapy. Contraception 1980;30:495-503.
8. Reimers D, Jezek A. Rifampicin und andere Antituberkulostatika bei gleichzeitiger oraler Kontrazeption. Prax Pneumo 1971;25:255-62.
9. Donley TG, Smith RF, Roy B. Reduced oral contraceptive effectiveness with concurrent antibiotic use: a protocol for prescribing antibiotics to women in childbearing age. Compendium Continuing Education Dentistry 1990;11:392-6.
10. JC. Petrie, Ed. Nervous system, endocrine system and infusion therapy. Amsterdam: 1994 (Back DJ, Breckenridge AM, Orme MLE. Clinically important adverse drug interactions 1984;2:305-7).
11. JC. Petrie, Ed. Nervous system, endocrine system and infusion therapy. Amsterdam: 1994 (Back DJ, Breckenridge AM, Orme MLE. Clinically important adverse drug interactions 1984;2:305-7).
12. Ahluwalia BS, Curry CL, Crocker CL, Verma PS. Evidence of higher ethynylestradiol blood levels in human hypertensive oral contraceptive users. Fertil Steril 1977;28:627-30.
13. Stadel BV. Oral contraception and cardiovascular disease. New Eng J Med 1981;305:612-8.
14. Back DJ, Breckenridge AM, Crawford FE. An investigation of the pharmacokinetics of ethinylestradiol in women using radioimmunoassay. Contraception 1979; 20:263-273.
15. Back DJ, Breckenridge AM, Maclver M, Orme ML'E, Purba HS. The gut wall metabolism of ethinylestradiol and its contribution to the pre-systemic metabolism of ethinylestradiol in human. Br J Clin Pharmacol 1982; 13:325-30.
16. Back DJ, Bates M, Breckenridge AM, Ellis A, Hall JM, MacIver M, Orme ML'E, Rowe PH. The in vitro metabolism of ethinylestradiol, mestranol and levonorgestrel by human jejunal mucosa. Br J Clin Pharmacol 1981;11:275-8.
17. Back DJ, Madden S, Orme M L'E. Gastrointestinal metabolism of contraceptive steroids. Am J Obstet Gynecol 1990;163:2138-45.
18. 14C] 17α-ethinylestradiol-3 methyl ether (mestranol) by women. Steroids 1975;25:343-54.
19. Bolt WH, Kappus H, Bolt HM. Ring A-oxidation of 17-ethinylestradiol in man. Acta Endocrinol 1977;85:189-97.
20. Bolt HM, Kappus H, Remmer H. Studies on the metabolism of ethinylestradiol in vitro and in vivo: the significance of 2-hydroxylation and the formation of polar products. Xenobiotica 1973;3:733-85.
21. Fuhr U, Klittich K, Staib AH. Inhibitory effect of grapefruit juice and its bitter principal, naringenin, on CYP2A2-dependent metabolism of caffeine in man. Br J Clin Pharmacol 1993;35:431-6.
22. Merkel U, Sigusch H, Hoffmann A. Grapefruit juice inhibits 7-hydroxylation of coumarin in healthy volunteers. Eur J Clin Pharmacol 1994;46:175-7.
23. Bailey DG, Spence JD, Munoz C, Arnold MO. Interaction of citrus juice with felodipine and nifedipine. The Lancet 1991;337:268-9.
24. Bailey DG, Arnold JMO, Strong HA, Munoz C, Spence JD. Effect of grapefruit juice and naringin on nisoldipine pharmacokinetics. Clin Pharmacol Ther 1993;54:589-94.
25. Soons PA, Vogels BAPM, Roosemalen MCM, Schoemaker HC, Uchida E, Edgar B, Lundahl J, Cohen AF, Breimer DD. Grapefruit juice and cimetidine inhibit stereoselective metabolism of nitrendipine in humans. Clin Pharmacol Ther 1991;50:394-403.
26. Bailey DG, Arnold JMO, Munoz C, Spence JD. Grapefruit juice - felodipine interaction: mechanism, predictability and effect of naringin. Clin Pharmacol Ther 1993;53:637-42.
27. Schubert W, Cullberg G, Edgar B, Hedner T. Inhibition of 17β-estradiol metabolism by grapefruit juice in ovariectomized women. Maturitas 1995;20:155-63.
28. Guengerich FP. Inhibition of oral contraceptive steroidmetabolizing enzymes by steroids and drugs. Am J Obstet Gynecol 1990;163:2159-63.
29. Guengerich FP. Oxidation of 17α-ethinylestradiol by human liver cytochrome P-450. Mol Pharmacol 1988; 33:500-8.
30. Watkins PB, Wrighton SA, Schuetz EG, Molowa DT, Guzelian PS. Identification of glucocorticoid-inducible cytochrome P-450 in the intestinal mucosa of rats and man. Clin Invest 1987;80:1029-36.
31. Ducharme MP, Provenzano R, Dehoorne-Smith M, Edwards DJ. Trough concentration of cyclosporine in blood following administration with grapefruit juice. Br J Clin Pharmacol 1993;36:457-9.
32. Pierpoint WS. Flavonoids in the human diet. In: Cody V, Middleton E Jr, Harborne JB, eds. Plant flavonoids in biology and medicine: Biochemical, pharmacological and structure-activity relationships. Alan R Liss Inc, 1986;125-40.
33. Fotherby K. Intrasubject variability in the pharmacokinetics of ethinylestradiol. Steroid Biochem Mol Biol 1991;38:733-6.
34. Kuhnz W, Louton T, Back DJ, Michaelis K. Radioimmunological analysis of ethinylestradiol in human serum - Validation of the method and comparison with a gas chromatographic-mass spectrometric assay. Arzneimittel-Forschung/Drug Research 199;43:16.
35. Kanarkowski R, Tornatore KM, D'Ambrosio R, Gardner MJ, Jusko WJ. Pharmacokinetics of single and multiple doses of ethinylestradiol and levonorgestrel in relation to smoking. Clin Pharmacol Ther 1988;43:23-31.
36. Goldzieher JW, Dozier TS, de la Pena A. Plasma levels and pharmacokinetics of ethinyl estrogens in various populations. Contraception 1980;21:1-16.
37. Bocker R, Kleingeist B, Eichhorn M, Lepper H. In vitro interaction of contraceptive steroids with human liver cytochrome P-450 enzymes. Adv Contracept 1991;7: 140-8.
38. Ball SE, Forrester M, Wolf CR, Back DJ. Differences in the cytochrome P-450 isoenzymes involved in the 2-hydroxylation of oestradiol and 17-ethinylestradiol. Biochem J 1990;267:221-6.
39. Miniscalco A, Lundahl J, Regardh CG, Edgar B, Eriksson UG. Inhibition of dihydropyridine metabolism in rat and human liver microsomes by flavonoids found in grapefruit juice. Pharmacol Exp Therap 1992;261:1195-9.
40. Kuhnz W, Louton T, Humpel M, Back DJ, Zamah NM. Influence of high doses of vitamin C on the bioavailability and the serum protein binding of levonorgestrel in women using a combination oral contraceptive. Contraception 1995;51:111-6
41. Orme ML'E, Back DJ, Breckenridge AM. Clinical pharmacokinetics of oral contraceptive steroids. Clin Pharmacokinet 1983;8:95-136.
42. Fotherby K, Akpoviroro J. Pharmacokinetics of ethinylestradiol in women from different populations. Contraception 1981;23:487-96.
43. Guengerich FP. Polymorphins of cytochrome P-450 in humans. Trends Pharmacol Sci 1989;10:107-9.
44. Lown KS, Kolars JC, Thummel KE, Barnett JE, Kunze KL, Wrighton SA, Watkins PB. Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel - Lack of prediction by the erythromycin breath test. Drug Metab Dispos 1994;22:947-55.
45. Stadel BV, Sternthal PM, Schlesselman JJ, Douglas MB, Hall WD, Kaul L, Ahluwalia B. Variation of ethinylestradiol blood levels among healthy women using oral contraceptives. Fertil Steril 1980;33:257-60