Evaluation of Committee on Safety of Medicines yellow card reports on oral contraceptive‐drug interactions with anticonvulsants and antibiotics.

Back, DJ; Grimmer, S. F. M.; Orme, ML; Proudlove, Christine; Rd, Mann; Breckenridge, AM

doi:10.1111/j.1365-2125.1988.tb03341.x

Cited by 98 publications

(26 citation statements)

References 20 publications

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“…There is considerable confusion in the marketplace as to which antibiotics may decrease the effectiveness of oral contraceptives. Back et al (1988) reported epidemiological data showing that 63 women had become pregnant in a 17-year period in Great Britain while taking OCs, and 70% of them became pregnant while taking either penicillins or tetracyclines plus OCs. Subsequently, similar reports were described from New Zealand (Sparrow, 1989) and Holland (Kovacs et al, 1989).…”

Section: Downloaded Frommentioning

confidence: 99%

A Comprehensive in Vitro and in Silico Analysis of Antibiotics That Activate Pregnane X Receptor and Induce CYP3A4 in Liver and Intestine

Yasuda

Ranade²,

Venkataramanan³

et al. 2008

Drug Metab Dispos

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ABSTRACT:We have investigated several in silico and in vitro methods to improve our ability to predict potential drug interactions of antibiotics. Our focus was to identify those antibiotics that activate pregnane X receptor (PXR) and induce CYP3A4 in human hepatocytes and intestinal cells. Human PXR activation was screened using reporter assays in HepG2 cells, kinetic measurements of PXR activation were made in DPX-2 cells, and induction of CYP3A4 expression and activity was verified by quantitative polymerase chain reaction, immunoblotting, and testosterone 6␤-hydroxylation in primary human hepatocytes and LS180 cells. We found that in HepG2 cells CYP3A4 transcription was activated strongly (>10-fold) by rifampin and troleandomycin; moderately (>7-fold) by dicloxacillin, tetracycline, clindamycin, griseofulvin, and (>4-fold) erythromycin; and weakly (>2.4-fold) by nafcillin, cefaclor, sulfisoxazole, and (>2-fold) cefadroxil and penicillin V. Similar although not identical results were obtained in DPX-2 cells. CYP3A4 mRNA and protein expression were induced by these antibiotics to differing extents in both liver and intestinal cells. CYP3A4 activity was significantly increased by rifampin (9.7-fold), nafcillin and dicloxacillin (5.9-fold), and weakly induced (2-fold) by tetracycline, sufisoxazole, troleandomycin, and clindamycin. Multiple pharmacophore models and docking indicated a good fit for dicloxacillin and nafcillin in PXR. These results suggest that in vitro and in silico methods can help to prioritize and identify antibiotics that are most likely to reduce exposures of medications (such as oral contraceptive agents) which interact with enzymes and transporters regulated by PXR. In summary, nafcillin, dicloxacillin, cephradine, tetracycline, sulfixoxazole, erythromycin, clindamycin, and griseofulvin exhibit a clear propensity to induce CYP3A4 and warrant further clinical investigation.

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Section: Downloaded Frommentioning

confidence: 99%

A Comprehensive in Vitro and in Silico Analysis of Antibiotics That Activate Pregnane X Receptor and Induce CYP3A4 in Liver and Intestine

Yasuda

Ranade²,

Venkataramanan³

et al. 2008

Drug Metab Dispos

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“…Thus, ofloxacin does not seem to interact with steroid metabolism in the same way as some other antibiotics [7][8][9][10][11][12]. Signs of ovarian activity in terms of high E2 levels up to 600 pmol/L in combination with ovarian follicles >~ 15 mm without any rise in P4 levels above 3 nmol/L were seen in four subjects.…”

Section: Discussionmentioning

confidence: 96%

Risk for ovulation in women taking a low-dose oral contraceptive (Microgynon) when receiving antibacterial treatment with a fluoroquinolone (ofloxacin)

Csemiczky

Alvendal

1996

Adv Contracept

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The possibility of escape ovulation in women using a fluoroquinolone ofloxacin for antibacterial treatment at a dose of 200 mg twice daily for 7 days when taking a combined oral contraceptive (Microgynon, 150 micrograms levonorgestrel and 30 micrograms ethinyl estradiol) was studied in 20 women. By using a placebo-controlled, randomized, cross-over design 6 contraceptive pill cycles were followed. Follicle-stimulating hormone and estradiol concentrations were measured on tablet days 5-8, 19-21; progesterone was assayed on days 19-21 during treatment with ofloxacin or placebo. Ultrasonographical investigations for measurements of the number and diameter of ovarian follicles were performed on one of days 5-10, 11-17, 18-24, 25-28. No indications of ovulation during ofloxacin medication were detected. It is concluded that alternative contraceptive precautions should not be needed when ofloxacin is prescribed for patients taking oral contraceptives.

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“…The influence of antibiotics on the risk of pregnancy for individual women is unclear, even from data reported to the CSM. 95 All trials investigating the use of antibiotics in women using hormonal contraception are limited by their sample size, short duration, inconsistent assessment of ovulation, and failure to eliminate bias. These limitations were highlighted in a systematic review on antibiotics and hormonal contraception.…”

Section: Other Drugsmentioning

confidence: 99%

FFPRHC Guidance (April 2005) Drug interactions with hormonal contraception

2005

j fam plann reprod health care

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This Guidance provides information for clinicians and women using hormonal contraception applicable when concurrent medications are prescribed. A key to the grades of recommendations, based on levels of evidence, is given at the end of this document. Details of the methods used by the Clinical Effectiveness Unit (CEU) in developing this Guidance and evidence tables summarising the research basis of the recommendations are available on the Faculty website (www.ffprhc.org.uk). Abbreviations (in alphabetical order) used include:

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Evaluation of Committee on Safety of Medicines yellow card reports on oral contraceptive‐drug interactions with anticonvulsants and antibiotics.

Cited by 98 publications

References 20 publications

A Comprehensive in Vitro and in Silico Analysis of Antibiotics That Activate Pregnane X Receptor and Induce CYP3A4 in Liver and Intestine

A Comprehensive in Vitro and in Silico Analysis of Antibiotics That Activate Pregnane X Receptor and Induce CYP3A4 in Liver and Intestine

Risk for ovulation in women taking a low-dose oral contraceptive (Microgynon) when receiving antibacterial treatment with a fluoroquinolone (ofloxacin)

FFPRHC Guidance (April 2005) Drug interactions with hormonal contraception

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