Rapid onset of an increase in caffeine residence time in young women due to oral contraceptive steroids

Rietveld, E.C.; Broekman, Mark; Houben, J. J. G.; Eskes, T.K.A.B.; Rossum, J. M. van

doi:10.1007/bf00548769

Cited by 49 publications

(35 citation statements)

References 12 publications

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“…In another study, Rietfeld et al [4] investigated the influence of different oral contraceptives on caffeine clearance in women and noted that the extent of clearance reduction was independent of the kind of progestogen administered; however, there seemed to be an increasing effect with prolonged oral contraceptive treatment. A similar trend was observed in the present study, where a more marked reduction of caffeine clearance was observed after 3 weeks of treatment compared with our previous investigations, where the oral contraceptives were only administered for a period of 2 weeks [11,14].…”

Section: Discussionmentioning

confidence: 99%

“…Both in animal experiments and in clinical studies, the hepatic clearance of marker drugs, such as theophylline, caffeine, aminopyrine and antipyrine, has been found to be impaired during concomitant treatment with contraceptive steroids, compared with untreated controls [3][4][5][6]. Since these marker compounds are almost completely metabolized prior to their elimination from the body, a reduced clearance can be interpreted as an impairment of hepatic cytochrome P-450-dependent enzymes by the contraceptive steroids.…”

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confidence: 99%

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Influence of ethinylestradiol-containing combination oral contraceptives with gestodene or levonorgestrel on caffeine elimination

Balogh

Klinger

Henschel

et al. 1995

Eur J Clin Pharmacol

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In a controlled clinical trial, the elimination of caffeine was examined in 20 healthy women prior to and during one cycle of treatment with either of two oral contraceptive formulations, one containing 0.075 mg gestodene and 0.03 mg ethinylestradiol and one containing 0.125 mg levonorgestrel and 0.03 mg ethinylestradiol. In addition, caffeine clearance was determined 1 month after the last intake of the oral contraceptives. Compared with pretreatment values, the clearance of caffeine was reduced by about 54% and 55% after one treatment cycle with gestodene- and the levonorgestrel-containing oral contraceptive, respectively. Other pharmacokinetic parameters of caffeine, such as tmax and Cmax, were not affected. Clearance values returned to pretreatment values 1 month after the last administration of the oral contraceptives. There was no difference in the reduction of caffeine clearance between contraceptive formulations. A small, but significant difference in the AUC(0-24 h) values of ethinylestradiol was noted between both preparations. There was no correlation between the AUC(model) values of caffeine and the AUC(0-24 h) values of ethinylestradiol. In the present study, a somewhat more pronounced effect on the elimination of caffeine was observed than in previous investigations, where several contraceptive steroids were administered only for a period of 2 weeks.

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

Influence of ethinylestradiol-containing combination oral contraceptives with gestodene or levonorgestrel on caffeine elimination

Balogh

Klinger

Henschel

et al. 1995

Eur J Clin Pharmacol

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“…The use of oral contraceptive steroids has been shown to lead to a doubling of the elimination half-life of caffeine, normally ranging from 3-5 h but increasing to 6-10 h during use of OCS [4][5][6][7]. Caffeine elimination is also significantly slower during the second and third trimesters of pregnancy [8], with the elimination half-life rising to almost three-times the normal value in the weeks prior to parturition.…”

Section: Abstract: Caffeine Menstrual Cycle; Pharmacokinetics Femalesmentioning

confidence: 99%

Menstrual cycle effects on caffeine elimination in the human female

Lane

Steege

Rupp

et al. 1992

Eur J Clin Pharmacol

145

103

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Increases in the levels of sex steroids due to pregnancy or oral contraceptive steroid use are known to decrease significantly the rate at which caffeine is eliminated from the body. An investigation has now been made into whether the changes in sex steroid levels that occur during normal menstrual cycling also affect the rate of caffeine elimination, especially whether hormonal shifts in the luteal phase are associated with slower elimination of caffeine. Repeated 24-hour caffeine elimination studies were conducted during the follicular and luteal phases of the menstrual cycle in 10 healthy women. Comparisons of the follicular and luteal phases revealed that systemic clearance of caffeine was slower in the luteal phase, although the t1/2 did not differ. The slowing effect was related to the proximity to onset of menstruation and to levels of progesterone. The evidence suggests that caffeine elimination may be slowed in the late luteal phase, prior to the onset of menstruation. Such a reduction would lead to increased accumulation of caffeine with repeated self-administration during the day, but the effect may be too small to be of clinical significance in the majority of women.

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“…No association between coffee and breast volumes was observed in women with the CYP1A2*1F A/A genotype or in women who currently used hormonal contraception. As hormonal contraceptives lower the CYP1A2 enzyme activity (Rietveld et al, 1984), the latter observation was expected.…”

Section: Discussionmentioning

confidence: 76%

“…We stratified the women according to the use of hormonal contraceptives as this changes endogenous hormone levels (Jernström and Olsson, 1994;Jernström et al, , 2005, influences breast volumes in nulliparous women and reduces the CYP1A2 enzyme activity (Rietveld et al, 1984).…”

Section: Resultsmentioning

confidence: 99%

Coffee intake and CYP1A2*1F genotype predict breast volume in young women: implications for breast cancer

et al. 2008

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As breast volume may be associated with heart cancer risk, we studied the relationship between breast volume, CYP1A2*1F and coffee intake. Among healthy premenopausal non-hormone users, 3 þ cups per day was associated with lower volume only in C-allele carriers (P interaction ¼ 0.02), which is consistent with reports that coffee protects only C-allele carriers against breast cancer. A recent study reported that coffee reduced the risk of breast cancer in BRCA1 carriers with the CYP1A2*1F C-allele but not in those with the CYP1A2*1F A/A genotype (Kotsopoulos et al, 2007). Another study found significantly lower coffee consumption in sporadic breast cancer cases with at least one C-allele compared with the A/A genotype (Bågeman et al, 2008) in spite of the fact that coffee consumption is similar across CYP1A2*1F genotypes in the general population (Cornelis et al, 2006). Some studies (Vatten et al, 1990;Baker et al, 2006;Nkondjock et al, 2006;Ganmaa et al, 2008), but not all (Rosenberg et al, 1985;Vatten et al, 1990;McLaughlin et al, 1992;Stensvold and Jacobsen, 1994;Michels et al, 2002), have reported that moderate-to-high coffee consumption protects against breast cancer, though a mechanism is unknown. None of these studies took CYP1A2*1F into account.Coffee is metabolised by the CYP1A2 enzyme, which also plays a key role in oestrogen metabolism (Le Marchand et al, 1997;Lee et al, 2003). Coffee contains not only caffeine but also phytooestrogens that can interact with and even block the oestrogen receptor (Magee and Rowland, 2004). Women with high coffee intake and the highly inducible CYP1A2*1F A/A genotype (Sachse et al, 1999) have a high 2-hydroxyoestrone (2-OHE1) to 16a-OHE1 ratio (Jernström et al, 2003;Bradlow et al, 2006;Klug et al, 2006). 2-Hydroxyoestrone is a weak oestrogen (Schneider et al, 1984), whereas 16a-OHE1 is procarcinogenic (Telang et al, 1992). In line with this, we found that breast volume in breast cancer patients was significantly higher in women with a lower 2-OHE to 16a-OHE1 ratio . Coffee also affects testosterone and SHBG levels (Ferrini and Barrett-Connor, 1996;Nagata et al, 1998). Although hormonal regulation of breast tissue has been extensively studied, little is known about hormones, genes, diet influence, density, size and diseases of the breast.Mammographic density is a strong risk factor for breast cancer (Boyd et al, 2005), the risk increasing with larger percentage density. The non-inducible CYP1A2*1F C-allele was associated with the percent density in normal-weight postmenopausal women not using hormone therapy (Takata et al, 2007). CYP1A2 enzyme activity has also been associated with density (Hong et al, 2004), and coffee induces CYP1A2 enzyme activity (Djordjevic et al, 2007). There is no direct correlation between breast density and size after adjustment for waist-to-hip ratio and BMI (Beijerinck et al, 1995). However, a larger breast size has been associated with increased breast cancer risk (Kato et al, 1995), especially in lean women (Kusano et al, 2006) or in women wi...

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Rapid onset of an increase in caffeine residence time in young women due to oral contraceptive steroids

Cited by 49 publications

References 12 publications

Influence of ethinylestradiol-containing combination oral contraceptives with gestodene or levonorgestrel on caffeine elimination

Influence of ethinylestradiol-containing combination oral contraceptives with gestodene or levonorgestrel on caffeine elimination

Menstrual cycle effects on caffeine elimination in the human female

Coffee intake and CYP1A2*1F genotype predict breast volume in young women: implications for breast cancer

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