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November 25, 2025
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Brand Name :
Arimidex
(United States) [Available]Synonyms :
anastrozole
Class :
Antineoplastic agents & Aromatase inhibitors
Brand Name :
Arimidex
(United States) [Available]Synonyms :
anastrozole
Class :
Antineoplastic agents & Aromatase inhibitors
Dosage Forms & Strengths
Tablet, Oral:
1 mg
For postmenopausal patients:
1
mg
Orally
once a day
until tumor progression
1
mg
Orally
once a day
depending upon symptoms
1
mg
Orally
once a day
depending upon symptoms
1
mg
Orally
once a day
until disease progression
may enhance the serum concentration of each other when combined
may enhance the serum concentration of each other when combined
may enhance the serum concentration of each other when combined
may enhance the serum concentration of each other when combined
may enhance the serum concentration of each other when combined
anastrozole: they may diminish the serum concentration of hormonal contraceptives
anastrozole: they may diminish the serum concentration of hormonal contraceptives
anastrozole: they may diminish the serum concentration of hormonal contraceptives
anastrozole: they may diminish the serum concentration of hormonal contraceptives
anastrozole: they may diminish the serum concentration of hormonal contraceptives
may reduce the therapeutic effect of gallium
may enhance the serum concentration when combined with fenfluramine
may have a decreased diagnostic effect when combined with cosyntropin
may enhance the serum concentration
may increase the serum concentration of Rasagiline
may enhance the concentration of serum when combined with theophylline derivatives
may decrease the diagnostic effect when combined with Piflufolastat F18
pirfenidone: they may enhance the serum concentration of CYP1A2 Inhibitors
pomalidomide: they may enhance the serum concentration of CYP1A2 Inhibitors
propranolol: they may enhance the serum concentration of CYP1A2 Inhibitors
may decrease the diagnostic effect when combined with metyrapone
cyproterone and ethinyl estradiol
may decrease the diagnostic effect of each other when combined
may decrease the therapeutic effect when combined with growth hormone analogs
may decrease the therapeutic effect when combined with growth hormone analogs
may decrease the therapeutic effect when combined with growth hormone analogs
may decrease the therapeutic effect when combined with growth hormone analogs
the therapeutic effect of anastrozole may be reduced by the use of estrogen derivatives
the therapeutic effect of anastrozole may be reduced by the use of estrogen derivatives
bazedoxifene/conjugated estrogens
the therapeutic effect of anastrozole may be reduced by the use of estrogen derivatives
the therapeutic effect of anastrozole may be reduced by the use of estrogen derivatives
the therapeutic effect of anastrozole may be reduced by the use of estrogen derivatives
The Therapeutic efficacy of anastrozole might be reduced by the presence of Estrogen Derivatives
The Therapeutic efficacy of anastrozole might be reduced by the presence of Estrogen Derivatives
tamoxifen decreases the concentration of anastrozole in serum
relugolix/estradiol/norethindrone
may diminish the effects of each other by pharmacodynamic antagonism
they increase the concentration of alosetron in the serum
the therapeutic effect of anastrozole may be reduced by the use of estrogen derivatives
dehydroepiandrosterone may increase the adverse/toxic effects of estrogen derivatives
the therapeutic effect of exemestane may be reduced by the use of estrogen derivatives
the therapeutic effect of hemin may be reduced by the use of estrogen derivatives
may enhance the serum concentration when combined
estrogens esterified/methyltestosterone
may decrease the therapeutic effect of estrogen derivatives
may diminish the concentration of serum when combined with CYP1A2 substrates
agomelatine: they may enhance the serum concentration of CYP1A2 Inhibitors
duloxetine: they may enhance the serum concentration of CYP1A2 Inhibitors
melatonin: they may enhance the serum concentration of CYP1A2 Inhibitors
mexiletine: they may enhance the serum concentration of CYP1A2 Inhibitors
ramelteon: they may enhance the serum concentration of CYP1A2 Inhibitors
tasimelteon: they may enhance the serum concentration of CYP1A2 Inhibitors
etonogestrel/ethinyl estradiol
may diminish the therapeutic effect of estrogen derivatives
may have an increased thrombogenic effect when combined with c1 inhibitors
synthetic conjugated estrogens, b
the activity of anastrozole may be decreased due to pharmacodynamic antagonism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
may increase the level by affecting hepatic enzyme CYP3A4 metabolism
Aromatase inhibitors may enhance the serum concentration of levomethadone
Aromatase inhibitors may enhance the serum concentration of methadone
Anastrozole may enhance the serum concentration of nintedanib
May reduce the serum concentration of anastrozole
may decrease the levels of serum concentration of hormonal contraceptives
may decrease the levels of serum concentration of hormonal contraceptives
may decrease the levels of serum concentration of hormonal contraceptives
may decrease the levels of serum concentration of hormonal contraceptives
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
they decrease the effect of thyroid products
they decrease the effect of thyroid products
they decrease the effect of thyroid products
they decrease the effect of thyroid products
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
It may enhance the effects when combined with tasimelteon by affecting CYP3A4 metabolism
may diminish the therapeutic effect
may diminish the therapeutic effect
may diminish the therapeutic effect
may diminish the therapeutic effect
It may diminish the effects when combined with estradiol valerate by pharmacodynamic antagonism
may enhance the concentration of serum when combined with corticosteroids
May have an increased the thrombogenic effect when combined with anthrax immune globulin
May have an increased the thrombogenic effect when combined with anthrax immune globulin
May have an increased the thrombogenic effect when combined with anthrax immune globulin
May have an increased the thrombogenic effect when combined with anthrax immune globulin
May have an increased the thrombogenic effect when combined with anthrax immune globulin
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
Combining tegafur with anastrozole can reduce tegafur’s metabolism
human rabies immune globulin (HRIG)
may have an increased thrombogenic effect when combined with anthrax immune globulin
When anastrozole is used together with capsaicin, this leads to enhanced risk or seriousness of methemoglobinemia
may have an increased hypoglycemic effect when combined with hypoglycemic agents
may have an increased hypoglycemic effect when combined with hypoglycemic agents
may have an increased hypoglycemic effect when combined with hypoglycemic agents
may have an increased hypoglycemic effect when combined with hypoglycemic agents
may have an increased hypoglycemic effect when combined with hypoglycemic agents
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the serum concentration when combined with propranolol
may enhance the serum concentration when combined with propranolol
may enhance the serum concentration when combined with propranolol
may enhance the serum concentration when combined with propranolol
may enhance the serum concentration when combined with propranolol
may decrease the level of serum concentration of pretomanid
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may increase the levels of serum concentration of estrogen derivatives
may diminish the serum concentration of Lidocaine
may increase the levels of serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
It may enhance the thrombogenic activities when combined with sotrovimab
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
estrogen Derivatives may lower the effectiveness of chenodiol
estrogen derivatives can enhance the hepatotoxic effect of dantrolene
clozapine: they may enhance the serum concentration of CYP1A2 Inhibitors
It may increase the thrombogenic effect when combined with C1 inhibitors
may enhance the concentration of serum when combined with asenapine
anagrelide: they may enhance serum concentrations of CYP1A2 Inhibitors
bromazepam: they may enhance the serum concentration of CYP1A2 Inhibitors
clomipramine: they may enhance the serum concentration of CYP1A2 Inhibitors
levobupivacaine: they may enhance the serum concentration of CYP1A2 Inhibitors
lidocaine: they may enhance the serum concentration of CYP1A2 Inhibitors
olanzapine: they may enhance the serum concentration of CYP1A2 Inhibitors
pentoxifylline: they may enhance the serum concentration of CYP1A2 Inhibitors
ramosetron: they may enhance the serum concentration of CYP1A2 Inhibitors
riluzole: they may enhance the serum concentration of CYP1A2 Inhibitors
ropinirole: they may enhance the serum concentration of CYP1A2 Inhibitors
ropivacaine: they may enhance the serum concentration of CYP1A2 Inhibitors
The combination of estrogen derivatives with ajmaline could potentially amplify its harmful and toxic effects
methadone concentration serum may be enhanced by aromatase inhibitors
The therapeutic efficacy of guanethidine may be reduced by estrogen derivative
The concentration serum of melatonin may be intensified by estrogen derivative
may decrease the serum concentration when combined with CYP1A2 substrates
may decrease the serum concentration when combined with CYP1A2 substrates
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may enhance the risk of adverse effects when combined with CYP1A2 inhibitors
It may enhance the risk of adverse effects when combined with CYP1A2 inhibitors
It may enhance the risk of adverse effects when combined with CYP1A2 inhibitors
It may enhance the risk of adverse effects when combined with Hormone antagonists
the rate of metabolism of anastrozole may be reduced
the risk of methemoglobinemia may be increased
may have an increased fluid-retaining effect when combined with androgens
may have an increased fluid-retaining effect when combined with androgens
may have an increased fluid-retaining effect when combined with androgens
may have an increased fluid-retaining effect when combined with androgens
the activity of estrogen pills may be reduced with agnus-castus
it may increase the levels of serum concentration
it may increase the levels of serum concentration
it may increase the levels of serum concentration
it may increase the levels of serum concentration
it may increase the levels of serum concentration
anastrozole can enhance the potency or impact of intranasal dihydroergotamine by modulating the metabolism of the hepatic/intestinal enzyme CYP3A4
anastrozole can impact the hepatic/intestinal enzyme CYP3A4 metabolism, leading to an elevation in the level or potency of intranasal midazolam
Androgen Deprivation Therapy Agents decrease the effect of diagnosis of flotufolastat F18
could lead to a reduction in the concentration serum of Hormonal Contraceptives
Action:
Anastrozole is a non-steroidal aromatase inhibitor. It works by inhibiting the enzyme aromatase, which is responsible for converting androgens (like testosterone) into estrogens (specifically estradiol) in peripheral tissues. By blocking this conversion, anastrozole significantly reduces circulating estrogen levels in the body.
This action is particularly important in postmenopausal women with hormone receptor-positive breast cancer, where estrogen promotes the growth of cancer cells. By lowering estrogen levels, anastrozole helps to slow or stop the growth of estrogen-dependent tumors.
Spectrum:
Anastrozole has a narrow but targeted spectrum, acting specifically by reducing estrogen production to treat certain types of breast cancer driven by hormonal activity.
Frequency defined:
>10%:
Edema (25%)
Hypertension (9%)
Hot flash (15%)
Constipation (23%)
Dyspepsia (6%)
Urinary tract infection (12%)
Bruise
Increased serum alanine aminotransferase
Fatigue
Insomnia
Arthralgia
Joint swelling
1%-10%
Cardiac arrhythmia
Cardiac failure
Nocturia
Headache
Bone fracture
Fever
<1%:
Adrenocortical insufficiency
None
Contraindication:
Anastrozole may cause fetal harm or pregnancy loss and is therefore contraindicated in women who are pregnant or may become pregnant.
Hypersensitivity
Caution:
Elevations in serum cholesterol have been observed with anastrozole use; therefore, lipid levels should be monitored regularly, particularly in patients with a history of hyperlipidemia.
If LDL cholesterol is elevated, management should follow established clinical guidelines.
Anastrozole has not demonstrated clinical effectiveness in premenopausal women with breast cancer.
Additionally, there is an increased risk of ischemic cardiovascular events in individuals with a prior history of ischemic heart disease, warranting careful assessment and monitoring in this population.
Pregnancy consideration: based on animal studies, it may cause harm to patients who can become pregnant.
Lactation: excretion of anastrozole in breast milk is not known.
Pregnancy category:
Anastrozole is a non-steroidal aromatase inhibitor that works by selectively inhibiting the aromatase enzyme, which converts androgens into estrogens in peripheral tissues. By blocking estrogen synthesis, anastrozole reduces circulating estrogen levels, which is crucial in treating hormone receptor-positive breast cancer in postmenopausal women.
Pharmacokinetics:
Absorption
Anastrozole is absorbed orally, reaching peak plasma concentrations approximately 2 hours after dosing on an empty stomach and around 5 hours when taken with food. The onset of action shows a 70% reduction in estrogen levels within 24 hours, increasing to 80% within two weeks. Steady-state concentrations are typically achieved within 7 days.
Distribution
About 40% of the drug binds to plasma proteins.
Metabolism
It undergoes hepatic metabolism primarily through N-dealkylation, hydroxylation, and glucuronidation, with around 85% being metabolized. Its primary metabolite, triazole, is inactive.
Excretion and elimination
The drug has a half-life of approximately 50 hours, is dialyzable, and is eliminated mainly via the urine (10%).
Anastrozole is administered orally, typically with or without food. It should be taken at the same time each day to maintain consistent blood levels. The tablet should be swallowed whole with water and not crushed or chewed.
Patient information leaflet
Generic Name: anastrozole
Pronounced: An-AS-troe-zole
Why do we use anastrozole?
Anastrozole is primarily used to treat hormone receptor-positive breast cancer in postmenopausal women. It is indicated as adjuvant therapy for early-stage breast cancer, first-line treatment for advanced or metastatic disease, and as extended therapy following tamoxifen. It helps reduce estrogen levels, thereby slowing the growth of estrogen-dependent tumors. Off-label, it may also be used for breast cancer prevention in high-risk women, gynecomastia in men, and ovulation induction in infertility, although these uses require specialist supervision. It is not effective in premenopausal women unless combined with ovarian suppression.
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