P100 ‘Arimidex’ (anastrozole): Lack of interactions with tamoxifen, antipyrine, cimetidine and warfarin

Dowsett, Mitch; Yates, R A; Wong, Y.W. James

doi:10.1016/s0959-8049(97)89317-3

Cited by 9 publications

(2 citation statements)

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“…Co-administration of anastrozole with a variety of compounds, for example antipyrine, cimetidine and warfarin, indicate that anastrozole is unlikely to result in clinically significant drug interactions mediated by cytochrome P-450 (Dowsett et al, 1998). Nonetheless, in vivo pharmacokinetic interactions are not always predictable.…”

Section: Discussionmentioning

confidence: 99%

The effect of anastrozole on the pharmacokinetics of tamoxifen in post-menopausal women with early breast cancer

et al. 1998

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Summary Thirty-four post-menopausal women with early breast cancer who had received 20 mg tamoxifen once daily as adjuvant therapy for at least 10 weeks participated in a randomized, double-blind, parallel-group, multicentre trial. The primary aim of the trial was to determine the effect of anastrozole upon tamoxifen pharmacokinetics, with secondary aims of assessing the tolerability of the two drugs in combination and whether or not tamoxifen had any effect upon the oestradiol suppression seen with anastrozole. Patients were randomized to receive either 1 mg anastrozole (16 patients) or matching placebo (18 patients) once daily on a double-blind basis for 28 days. No significant difference (P = 0.919) was observed in serum tamoxifen concentrations between the anastrozole and placebo groups during the trial. The serum concentration of oestradiol was significantly suppressed (P < 0.0001) in patients co-administered anastrozole compared with placebo in the presence of tamoxifen, confirming that anastrozole remained an effective suppressant of oestradiol in the presence of tamoxifen. The combination of tamoxifen and anastrozole was well tolerated, with very little difference in side-effects reported between anastrozole and placebo. In conclusion, the results of this study confirm that anastrozole does not affect the pharmacokinetics of tamoxifen when the two drugs are given in combination to post-menopausal women with early breast cancer. In addition, the oestradiol suppressant effects of anastrozole appear unaffected by tamoxifen.

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Section: Discussionmentioning

confidence: 99%

The effect of anastrozole on the pharmacokinetics of tamoxifen in post-menopausal women with early breast cancer

et al. 1998

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“…In addition to the lack of interaction with tamoxifen, further pharmacokinetic studies have shown that anastrozole does not affect, and in turn is not itself affected by, a number of drugs that may impact upon liver metabolism. For instance, anastrozole did not affect the pharmacokinetics of antipyrine or warfarin, both of which are metabolised by the liver, and anastrozole itself was not affected when co-administered with cimetidine, a nonspecific inhibitor of liver cytochrome P450 (Dowsett et al 1998). For a drug such as anastrozole, which will, in the first instance, be given for up to 5 years to postmenopausal patients, in whom concomitant drug treatment is not uncommon, lack of interaction with other drugs is an important property.…”

Section: The Atac Trialmentioning

confidence: 98%

Use of aromatase inhibitors in the adjuvant treatment of breast cancer.

Baum

1999

Endocrine-Related Cancer

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The value of endocrine treatment of early breast cancer has been illustrated by the antioestrogen, tamoxifen, which has now been available for nearly 30 years. However, if the recognised side effects and pharmacological properties of tamoxifen are taken into consideration, it is possible that other endocrine treatments that are now available can provide equal or superior efficacy, along with improved tolerability. One such group of agents is the aromatase inhibitors specifically the new-generation triazole aromatase inhibitors, such as anastrozole and letrozole, which have both shown tolerability and efficacy advantages over standard treatments in postmenopausal women with advanced breast cancer. There are convincing reasons why the new generation of aromatase inhibitors have advantages over tamoxifen. For instance, from their agonist properties, the effects on the endometrium and tumour stimulation seen with tamoxifen would not be expected, nor would the visual disturbances that have been associated with the triphenylethylene compounds, including tamoxifen. A number of aromatase inhibitors, for instance, anastrozole, letrozole and exemestane, are currently being investigated for treatment of early breast cancer. The results of the trials of aromatase inhibitors and tamoxifen will, in the next few years, define whether or not the new-generation aromatase inhibi- Endocrine-Related Cancer (1999) 6 231-234 tors have a role to play in the treatment of postmenopausal women with early breast cancer.

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Clinical studies with anastrozole

Howell¹,

Wakeling²

2006

Aromatase Inhibitors

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P100 ‘Arimidex’ (anastrozole): Lack of interactions with tamoxifen, antipyrine, cimetidine and warfarin

Cited by 9 publications

References 0 publications

The effect of anastrozole on the pharmacokinetics of tamoxifen in post-menopausal women with early breast cancer

The effect of anastrozole on the pharmacokinetics of tamoxifen in post-menopausal women with early breast cancer

Use of aromatase inhibitors in the adjuvant treatment of breast cancer.

Clinical studies with anastrozole

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