Anastrozole is a nonsteroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy for estrogen receptor-positive breast cancer. Anastrozole has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury.
Anastrozole is a nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure. As a third-generation aromatase inhibitor, anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast; aromatase catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis. In estrogen-dependent breast cancers, anastrozole may inhibit tumor growth. (NCI04)
Mechanism of Action
Anastrazole exerts its anti-estrogenic effects via selective and competitive inhibition of the aromatase enzyme found predominantly in the adrenal glands, liver, and fatty tissues. Many breast cancers are hormone receptor-positive, meaning their growth is stimulated and/or maintained by the presence of hormones such as estrogen or progesterone. In postmenopausal women, estrogen is primarily derived from the conversion of adrenally-produced androgens into estrogens by the aromatase enzyme – by competitively inhibiting the biosynthesis of estrogen at these enzymes, anastrozole effectively suppresses circulating estrogen levels and, subsequently, the growth of hormone receptor-positive tumors.
or
Because estrogen acts as a growth factor for hormone-dependent breast cancer cells, anastrozole-induced reduction of serum and tumor concentrations of estrogen inhibits tumor growth and delays disease progression. Anastrozole selectively inhibits the conversion of androgens to estrogens. In postmenopausal women, ovarian secretion of estrogen declines, and the conversion of adrenal androgens (mainly androstenedione and testosterone) to estrone and estradiol in peripheral tissues (adipose, muscle, and liver), catalyzed by the aromatase enzyme, is the principal source of estrogens. Anastrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P-450 unit of the enzyme; suppression of estrogen biosynthesis in all tissues reduces serum concentrations of circulating estrogens, including estrone, estradiol, and estrone sulfate. Anastrozole selectively inhibits the synthesis of estrogens and does not affect the synthesis of adrenal corticosteroids, aldosterone, or thyroid hormone. In animals, anastrozole has not been shown to possess direct progestogenic, androgenic, or estrogenic activity, but alterations in the circulating concentrations of progesterone, androgens, and estrogens have been observed.
Indications
- Anastrozole is indicated as an adjunct therapy in the treatment of hormone receptor-positive early breast cancer in postmenopausal women, and as a first-line treatment for hormone receptor-positive (or hormone receptor-unknown) locally advanced or metastatic breast cancer in postmenopausal women. It may also be used in the treatment of advanced breast cancer in postmenopausal women who experience disease progression despite treatment.
- It may also be used in the treatment of advanced breast cancer in postmenopausal women who experience disease progression despite treatment with tamoxifen.[rx]
- Gynaecomastia, McCune-Albright syndrome, Short stature due to Growth Hormone deficiency, Testotoxicosis
- Anastrozole is a nonsteroidal inhibitor of aromatase that effectively blocks estrogen synthesis in postmenopausal women and is used as therapy of estrogen receptor-positive breast cancer. Anastrozole has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury.
- Breast Cancer
- Breast Cancer, Metastatic
- McCune-Albright Syndrome
- Pubertal Gynecomastia
- Endometrial Cancer
- Advanced Breast Cancer
- Early Breast Cancer
- Invasive Early Breast Cancer
- Locally Advanced Breast Cancer (LABC)
- Metastatic Breast Cancer
Use in Cancer
Anastrozole is approved to treat:
- Breast cancer in postmenopausal women who have any of the following types of breast cancer–
- Early-stage, hormone receptor-positive (HR+) breast cancer. It is used in women who have already received other treatments.
- Locally advanced or metastatic breast cancer that is HR+ or hormone receptor unknown (it is not known whether it is HR+ or hormone receptor-negative). It is used as first-line therapy in these patients.
- Advanced breast cancer that has gotten worse after treatment with tamoxifen citrate.
Anastrozole is also being studied in the treatment of other conditions and types of cancer.
Contraindications
The following conditions are contraindicated with this drug. Check with your physician if you have any of the following:
- are allergic to anastrozole or any ingredients of the medication
- are breast-feeding
- are pregnant
- high cholesterol
- a low supply of oxygen rich blood to the heart
- decreased calcification or density of bone
- pregnancy
- a patient who is producing milk and breastfeeding
Dosage
Strengths: 1 mg
Breast Cancer
- Initial dose: 1 mg orally taken once a day
- Duration of therapy: Until tumor progression (treatment of advanced breast cancer); unknown (adjuvant treatment of early breast cancer)
Side Effects
The Most Common
- weakness
- headache
- hot flashes
- sweating
- stomach pain
- nausea
- vomiting
- loss of appetite
- constipation
- diarrhea
- heartburn
- weight gain
- joint, bone, or muscle pain
- breast pain
- mood changes
- depression
- difficulty falling asleep or staying asleep
- nervousness
- dizziness
- vaginal bleeding
- vaginal dryness or irritation
- pain, burning, or tingling in the hands or feet
- dry mouth
- hair thinning
More Common
- chest pain
- sore throat, cough, fever, chills, swollen glands, or other signs of infection
- swelling, redness, or warmth in hand or arm
- difficult, painful, or urgent urination
- blurred vision or vision changes
- yellowing of the skin or eyes
- pain in the upper right part of the stomach
- skin lesions, ulcers, or blisters
- rash
- hives
- itching
- shortness of breath
- difficulty swallowing or breathing
- swelling of the eyes, face, lips, tongue, throat, arms, hands, feet, ankles, or lower legs
Rare
- bone fractures
- chest pain
- increased blood pressure
- increased cholesterol levels
- signs of carpal tunnel syndrome (e.g., tingling pain, coldness, and weakness in parts of the hand)
- signs of depression (such as feeling sad, losing interest in things you used to enjoy, weight changes, changes in sleep habits, feelings of guilt or worthlessness, thoughts of suicide)
- tingling or numbness of the skin
- unusual vaginal discharge, itching, or bleeding
- signs of a heart attack (e.g., tightness or feeling of heaviness in your chest or pain radiating to your arms or shoulders, neck, teeth, jaw, abdomen, or back)
- symptoms of liver problems (e.g., abdominal pain, persistent vomiting, feeling unwell, fever, itching, yellowing of the skin and eyes, dark urine)
- signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
- signs of a severe skin reaction such as blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort
Drug Interactions
| DRUG | INTERACTION |
|---|---|
| Abatacept | The metabolism of Anastrozole can be increased when combined with Abatacept. |
| Abiraterone | The metabolism of Anastrozole can be decreased when combined with Abiraterone. |
| Acetyldigitoxin | Acetyldigitoxin may decrease the cardiotoxic activities of Anastrozole. |
| Adalimumab | The metabolism of Anastrozole can be increased when combined with Adalimumab. |
| Almotriptan | The metabolism of Anastrozole can be decreased when combined with Almotriptan. |
| Alpelisib | The metabolism of Anastrozole can be decreased when combined with Alpelisib. |
| Aminophenazone | The metabolism of Aminophenazone can be decreased when combined with Anastrozole. |
| Amiodarone | The metabolism of Amiodarone can be decreased when combined with Anastrozole. |
| Amitriptyline | The metabolism of Anastrozole can be decreased when combined with Amitriptyline. |
| Amodiaquine | The metabolism of Anastrozole can be decreased when combined with Amodiaquine. |
| Amsacrine | The risk or severity of cardiotoxicity can be increased when Amsacrine is combined with Anastrozole. |
| Anakinra | The metabolism of Anastrozole can be increased when combined with Anakinra. |
| Antipyrine | The metabolism of Antipyrine can be decreased when combined with Anastrozole. |
| Apalutamide | The metabolism of Apalutamide can be decreased when combined with Anastrozole. |
| Apixaban | The metabolism of Apixaban can be decreased when combined with Anastrozole. |
| Apomorphine | The metabolism of Anastrozole can be decreased when combined with Apomorphine. |
| Apremilast | The metabolism of Anastrozole can be increased when combined with Apremilast. |
| Arsenic trioxide | The risk or severity of cardiotoxicity can be increased when Arsenic trioxide is combined with Anastrozole. |
| Articaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Articaine. |
| Atazanavir | The metabolism of Anastrozole can be decreased when combined with Atazanavir. |
| Atorvastatin | The metabolism of Anastrozole can be decreased when combined with Atorvastatin. |
| Avatrombopag | The metabolism of Anastrozole can be increased when combined with Avatrombopag. |
| Azelastine | The metabolism of Anastrozole can be decreased when combined with Azelastine. |
| Benzocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Benzocaine. |
| Benzyl alcohol | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Benzyl alcohol. |
| Betamethasone | The metabolism of Anastrozole can be increased when combined with Betamethasone. |
| Bevacizumab | The risk or severity of cardiotoxicity can be increased when Bevacizumab is combined with Anastrozole. |
| Bexarotene | The metabolism of Anastrozole can be decreased when combined with Bexarotene. |
| Bezafibrate | The metabolism of Anastrozole can be decreased when combined with Bezafibrate. |
| Bimekizumab | The metabolism of Anastrozole can be increased when combined with Bimekizumab. |
| Bleomycin | The risk or severity of cardiotoxicity can be increased when Bleomycin is combined with Anastrozole. |
| Bortezomib | The risk or severity of cardiotoxicity can be increased when Bortezomib is combined with Anastrozole. |
| Bosutinib | The metabolism of Anastrozole can be decreased when combined with Bosutinib. |
| Brigatinib | The metabolism of Brigatinib can be decreased when combined with Anastrozole. |
| Bupivacaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Bupivacaine. |
| Buprenorphine | The metabolism of Anastrozole can be decreased when combined with Buprenorphine. |
| Busulfan | The risk or severity of cardiotoxicity can be increased when Busulfan is combined with Anastrozole. |
| Butacaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Butacaine. |
| Butamben | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Butamben. |
| Cabazitaxel | The metabolism of Cabazitaxel can be decreased when combined with Anastrozole. |
| Cabozantinib | The metabolism of Anastrozole can be decreased when combined with Cabozantinib. |
| Canakinumab | The metabolism of Anastrozole can be increased when combined with Canakinumab. |
| Candesartan cilexetil | The metabolism of Anastrozole can be decreased when combined with Candesartan cilexetil. |
| Cannabidiol | The metabolism of Anastrozole can be decreased when combined with Cannabidiol. |
| Capecitabine | The risk or severity of cardiotoxicity can be increased when Capecitabine is combined with Anastrozole. |
| Capsaicin | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Capsaicin. |
| Carmustine | The risk or severity of cardiotoxicity can be increased when Carmustine is combined with Anastrozole. |
| Celecoxib | The metabolism of Anastrozole can be decreased when combined with Celecoxib. |
| Cenobamate | The metabolism of Anastrozole can be increased when combined with Cenobamate. |
| Cerivastatin | The metabolism of Anastrozole can be decreased when combined with Cerivastatin. |
| Certolizumab pegol | The metabolism of Anastrozole can be increased when combined with Certolizumab pegol. |
| Chloroprocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Chloroprocaine. |
| Chloroquine | The metabolism of Anastrozole can be decreased when combined with Chloroquine. |
| Cimetidine | The metabolism of Anastrozole can be decreased when combined with Cimetidine. |
| Cinchocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Cinchocaine. |
| Cisapride | The metabolism of Anastrozole can be decreased when combined with Cisapride. |
| Cisplatin | The risk or severity of cardiotoxicity can be increased when Cisplatin is combined with Anastrozole. |
| Cladribine | The risk or severity of cardiotoxicity can be increased when Cladribine is combined with Anastrozole. |
| Clopidogrel | The metabolism of Anastrozole can be decreased when combined with Clopidogrel. |
| Cocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Cocaine. |
| Conjugated estrogens | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Conjugated estrogens. |
| Cyclophosphamide | The risk or severity of cardiotoxicity can be increased when Cyclophosphamide is combined with Anastrozole. |
| Dabrafenib | The serum concentration of Anastrozole can be decreased when it is combined with Dabrafenib. |
| Dapsone | The metabolism of Anastrozole can be decreased when combined with Dapsone. |
| Darbepoetin alfa | The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Anastrozole. |
| Dasabuvir | The metabolism of Dasabuvir can be decreased when combined with Anastrozole. |
| Daunorubicin | The risk or severity of cardiotoxicity can be increased when Daunorubicin is combined with Anastrozole. |
| Deferasirox | The metabolism of Anastrozole can be decreased when combined with Deferasirox. |
| Deslanoside | Deslanoside may decrease the cardiotoxic activities of Anastrozole. |
| Dexamethasone | The metabolism of Anastrozole can be increased when combined with Dexamethasone. |
| Dexibuprofen | The metabolism of Dexibuprofen can be decreased when combined with Anastrozole. |
| Diclofenac | The metabolism of Anastrozole can be decreased when combined with Diclofenac. |
| Dienestrol | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Dienestrol. |
| Diethylstilbestrol | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Diethylstilbestrol. |
| Digitoxin | Digitoxin may decrease the cardiotoxic activities of Anastrozole. |
| Digoxin | Digoxin may decrease the cardiotoxic activities of Anastrozole. |
| Diltiazem | The metabolism of Anastrozole can be decreased when combined with Diltiazem. |
| Diphenhydramine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Diphenhydramine. |
| Docetaxel | The risk or severity of cardiotoxicity can be increased when Anastrozole is combined with Docetaxel. |
| Domperidone | The metabolism of Anastrozole can be decreased when combined with Domperidone. |
| Doxorubicin | The risk or severity of cardiotoxicity can be increased when Doxorubicin is combined with Anastrozole. |
| Dyclonine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Dyclonine. |
| Efavirenz | The metabolism of Anastrozole can be decreased when combined with Efavirenz. |
| Elagolix | The metabolism of Elagolix can be decreased when combined with Anastrozole. |
| Eltrombopag | The metabolism of Anastrozole can be decreased when combined with Eltrombopag. |
| Emapalumab | The metabolism of Anastrozole can be increased when combined with Emapalumab. |
| Enasidenib | The metabolism of Enasidenib can be decreased when combined with Anastrozole. |
| Enzalutamide | The metabolism of Anastrozole can be decreased when combined with Enzalutamide. |
| Epirubicin | The risk or severity of cardiotoxicity can be increased when Epirubicin is combined with Anastrozole. |
| Erlotinib | The metabolism of Erlotinib can be decreased when combined with Anastrozole. |
| Erythropoietin | The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Anastrozole. |
| Esterified estrogens | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Esterified estrogens. |
| Estetrol | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estetrol. |
| Estradiol | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estradiol. |
| Estradiol acetate | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estradiol acetate. |
| Estradiol benzoate | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estradiol benzoate. |
| Estradiol cypionate | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estradiol cypionate. |
| Estradiol dienanthate | The metabolism of Estradiol dienanthate can be decreased when combined with Anastrozole. |
| Estradiol valerate | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estradiol valerate. |
| Estriol | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estriol. |
| Estrone | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estrone. |
| Estrone sulfate | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Estrone sulfate. |
| Eszopiclone | The metabolism of Anastrozole can be decreased when combined with Eszopiclone. |
| Etanercept | The metabolism of Anastrozole can be increased when combined with Etanercept. |
| Ethinylestradiol | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Ethinylestradiol. |
| Ethyl chloride | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Ethyl chloride. |
| Etidocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Etidocaine. |
| Etoposide | The risk or severity of cardiotoxicity can be increased when Etoposide is combined with Anastrozole. |
| Favipiravir | The metabolism of Anastrozole can be decreased when combined with Favipiravir. |
| Felodipine | The metabolism of Anastrozole can be decreased when combined with Felodipine. |
| Fenofibrate | The metabolism of Anastrozole can be decreased when combined with Fenofibrate. |
| Finerenone | The metabolism of Finerenone can be decreased when combined with Anastrozole. |
| Fludarabine | The risk or severity of cardiotoxicity can be increased when Fludarabine is combined with Anastrozole. |
| Fluorouracil | The metabolism of Fluorouracil can be decreased when combined with Anastrozole. |
| Fluticasone | The metabolism of Anastrozole can be decreased when combined with Fluticasone. |
| Fluticasone furoate | The metabolism of Anastrozole can be decreased when combined with Fluticasone furoate. |
| Fluticasone propionate | The metabolism of Anastrozole can be decreased when combined with Fluticasone propionate. |
| Fluvastatin | The metabolism of Anastrozole can be decreased when combined with Fluvastatin. |
| Fosphenytoin | The metabolism of Fosphenytoin can be decreased when combined with Anastrozole. |
| Gemfibrozil | The metabolism of Anastrozole can be decreased when combined with Gemfibrozil. |
| Glasdegib | The metabolism of Glasdegib can be decreased when combined with Anastrozole. |
| Golimumab | The metabolism of Anastrozole can be increased when combined with Golimumab. |
| Halofantrine | The metabolism of Halofantrine can be decreased when combined with Anastrozole. |
| Hydrocortisone | The metabolism of Anastrozole can be increased when combined with Hydrocortisone. |
| Hydroxychloroquine | The metabolism of Hydroxychloroquine can be decreased when combined with Anastrozole. |
| Ibuprofen | The metabolism of Anastrozole can be decreased when combined with Ibuprofen. |
| Idarubicin | The risk or severity of cardiotoxicity can be increased when Idarubicin is combined with Anastrozole. |
| Ifosfamide | The risk or severity of cardiotoxicity can be increased when Ifosfamide is combined with Anastrozole. |
| Imatinib | The risk or severity of cardiotoxicity can be increased when Imatinib is combined with Anastrozole. |
| Infliximab | The metabolism of Anastrozole can be increased when combined with Infliximab. |
| Irbesartan | The metabolism of Anastrozole can be decreased when combined with Irbesartan. |
| Isavuconazole | The metabolism of Anastrozole can be decreased when combined with Isavuconazole. |
| Istradefylline | The metabolism of Istradefylline can be decreased when combined with Anastrozole. |
| Ketamine | The metabolism of Ketamine can be decreased when combined with Anastrozole. |
| Ketoconazole | The metabolism of Anastrozole can be decreased when combined with Ketoconazole. |
| Ketoprofen | The metabolism of Anastrozole can be decreased when combined with Ketoprofen. |
| Ketorolac | The metabolism of Anastrozole can be decreased when combined with Ketorolac. |
| Lansoprazole | The metabolism of Anastrozole can be decreased when combined with Lansoprazole. |
| Lapatinib | The metabolism of Lapatinib can be decreased when combined with Anastrozole. |
| Letermovir | The metabolism of Anastrozole can be decreased when combined with Letermovir. |
| Levobupivacaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Levobupivacaine. |
| Levoketoconazole | The metabolism of Anastrozole can be decreased when combined with Levoketoconazole. |
| Levomilnacipran | The metabolism of Levomilnacipran can be decreased when combined with Anastrozole. |
| Levothyroxine | The metabolism of Anastrozole can be decreased when combined with Levothyroxine. |
| Lidocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Lidocaine. |
| Linzagolix | The serum concentration of Anastrozole can be increased when it is combined with Linzagolix. |
| Liotrix | The metabolism of Anastrozole can be decreased when combined with Liotrix. |
| Loperamide | The metabolism of Anastrozole can be decreased when combined with Loperamide. |
| Loratadine | The metabolism of Anastrozole can be decreased when combined with Loratadine. |
| Losartan | The metabolism of Anastrozole can be decreased when combined with Losartan. |
| Lovastatin | The metabolism of Anastrozole can be decreased when combined with Lovastatin. |
| Lumacaftor | The metabolism of Anastrozole can be decreased when combined with Lumacaftor. |
| Magnesium | The serum concentration of Magnesium can be decreased when it is combined with Anastrozole. |
| Mechlorethamine | The risk or severity of cardiotoxicity can be increased when Mechlorethamine is combined with Anastrozole. |
| Medroxyprogesterone acetate | The metabolism of Anastrozole can be decreased when combined with Medroxyprogesterone acetate. |
| Meloxicam | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Meloxicam. |
| Mephenytoin | The metabolism of Anastrozole can be decreased when combined with Mephenytoin. |
| Mepivacaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Mepivacaine. |
| Mestranol | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Mestranol. |
| Methadone | The serum concentration of Methadone can be increased when it is combined with Anastrozole. |
| Methotrexate | The risk or severity of cardiotoxicity can be increased when Methotrexate is combined with Anastrozole. |
| Methoxy polyethylene glycol- | The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Anastrozole. |
| Methylene blue | The metabolism of Anastrozole can be decreased when combined with Methylene blue. |
| Metronidazole | The metabolism of Anastrozole can be decreased when combined with Metronidazole. |
| Miconazole | The metabolism of Anastrozole can be decreased when combined with Miconazole. |
| Mifepristone | The serum concentration of Anastrozole can be increased when it is combined with Mifepristone. |
| Mitapivat | The metabolism of Anastrozole can be increased when combined with Mitapivat. |
| Mitomycin | The risk or severity of cardiotoxicity can be increased when Mitomycin is combined with Anastrozole. |
| Mitoxantrone | The risk or severity of cardiotoxicity can be increased when Mitoxantrone is combined with Anastrozole. |
| Mometasone furoate | The metabolism of Anastrozole can be decreased when combined with Mometasone furoate. |
| Montelukast | The metabolism of Anastrozole can be decreased when combined with Montelukast. |
| Morphine | The metabolism of Anastrozole can be decreased when combined with Morphine. |
| Mycophenolate mofetil | The metabolism of Anastrozole can be decreased when combined with Mycophenolate mofetil. |
| Naproxen | The metabolism of Anastrozole can be decreased when combined with Naproxen. |
| Nicardipine | The metabolism of Anastrozole can be decreased when combined with Nicardipine. |
| Nilutamide | The metabolism of Anastrozole can be decreased when combined with Nilutamide. |
| Nilvadipine | The metabolism of Anastrozole can be decreased when combined with Nilvadipine. |
| Olodaterol | The metabolism of Olodaterol can be decreased when combined with Anastrozole. |
| Ombitasvir | The metabolism of Ombitasvir can be decreased when combined with Anastrozole. |
| Omeprazole | The metabolism of Anastrozole can be decreased when combined with Omeprazole. |
| Ouabain | Ouabain may decrease the cardiotoxic activities of Anastrozole. |
| Oxetacaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Oxetacaine. |
| Oxybuprocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Oxybuprocaine. |
| Oxybutynin | The metabolism of Anastrozole can be decreased when combined with Oxybutynin. |
| Ozanimod | The metabolism of Ozanimod can be decreased when combined with Anastrozole. |
| Paclitaxel | The metabolism of Paclitaxel can be decreased when combined with Anastrozole. |
| Paramethadione | The metabolism of Anastrozole can be decreased when combined with Paramethadione. |
| Pazopanib | The metabolism of Pazopanib can be decreased when combined with Anastrozole. |
| Peginesatide | The risk or severity of Thrombosis can be increased when Peginesatide is combined with Anastrozole. |
| Peginterferon alfa-2a | The risk or severity of cardiotoxicity can be increased when Peginterferon alfa-2a is combined with Anastrozole. |
| Pentostatin | The risk or severity of cardiotoxicity can be increased when Pentostatin is combined with Anastrozole. |
| Pertuzumab | The risk or severity of cardiotoxicity can be increased when Anastrozole is combined with Pertuzumab. |
| Phenobarbital | The metabolism of Anastrozole can be increased when combined with Phenobarbital. |
| Phenol | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Phenol. |
| Phenprocoumon | The metabolism of Phenprocoumon can be decreased when combined with Anastrozole. |
| Phenytoin | The metabolism of Phenytoin can be decreased when combined with Anastrozole. |
| Pioglitazone | The metabolism of Anastrozole can be decreased when combined with Pioglitazone. |
| Piroxicam | The metabolism of Anastrozole can be decreased when combined with Piroxicam. |
| Pitavastatin | The metabolism of Pitavastatin can be decreased when combined with Anastrozole. |
| Polyestradiol phosphate | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Polyestradiol phosphate. |
| Ponatinib | The metabolism of Ponatinib can be decreased when combined with Anastrozole. |
| Pralsetinib | The metabolism of Anastrozole can be decreased when combined with Pralsetinib. |
| Pramocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Pramocaine. |
| Prednisolone phosphate | The metabolism of Anastrozole can be increased when combined with Prednisolone phosphate. |
| Prilocaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Prilocaine. |
| Probenecid | The metabolism of Anastrozole can be increased when combined with Probenecid. |
| Procaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Procaine. |
| Proparacaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Proparacaine. |
| Propofol | The metabolism of Anastrozole can be decreased when combined with Propofol. |
| Propoxycaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Propoxycaine. |
| Pyrimethamine | The metabolism of Anastrozole can be decreased when combined with Pyrimethamine. |
| Quinestrol | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Quinestrol. |
| Quinidine | The metabolism of Anastrozole can be decreased when combined with Quinidine. |
| Quinine | The metabolism of Anastrozole can be decreased when combined with Quinine. |
| Raloxifene | The metabolism of Anastrozole can be decreased when combined with Raloxifene. |
| Repaglinide | The metabolism of Anastrozole can be decreased when combined with Repaglinide. |
| Rifabutin | The metabolism of Anastrozole can be increased when combined with Rifabutin. |
| Rifampicin | The metabolism of Anastrozole can be increased when combined with Rifampicin. |
| Rifamycin | The metabolism of Anastrozole can be decreased when combined with Rifamycin. |
| Rifapentine | The metabolism of Anastrozole can be increased when combined with Rifapentine. |
| Rilonacept | The metabolism of Anastrozole can be increased when combined with Rilonacept. |
| Rilpivirine | The metabolism of Anastrozole can be decreased when combined with Rilpivirine. |
| Riociguat | The metabolism of Riociguat can be decreased when combined with Anastrozole. |
| Ritonavir | The metabolism of Anastrozole can be decreased when combined with Ritonavir. |
| Rofecoxib | The metabolism of Anastrozole can be decreased when combined with Rofecoxib. |
| Ropivacaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Ropivacaine. |
| Rosiglitazone | The metabolism of Anastrozole can be decreased when combined with Rosiglitazone. |
| Roxadustat | The metabolism of Roxadustat can be decreased when combined with Anastrozole. |
| Salmeterol | The metabolism of Anastrozole can be decreased when combined with Salmeterol. |
| Saquinavir | The metabolism of Anastrozole can be decreased when combined with Saquinavir. |
| Secobarbital | The metabolism of Anastrozole can be increased when combined with Secobarbital. |
| Secukinumab | The metabolism of Anastrozole can be increased when combined with Secukinumab. |
| Selegiline | The metabolism of Anastrozole can be decreased when combined with Selegiline. |
| Selexipag | The metabolism of Selexipag can be decreased when combined with Anastrozole. |
| Selpercatinib | The serum concentration of Anastrozole can be increased when it is combined with Selpercatinib. |
| Selumetinib | The metabolism of Selumetinib can be decreased when combined with Anastrozole. |
| Siltuximab | The metabolism of Anastrozole can be increased when combined with Siltuximab. |
| Simvastatin | The metabolism of Anastrozole can be decreased when combined with Simvastatin. |
| Sitagliptin | The metabolism of Sitagliptin can be decreased when combined with Anastrozole. |
| Sorafenib | The metabolism of Sorafenib can be decreased when combined with Anastrozole. |
| Spironolactone | The metabolism of Anastrozole can be decreased when combined with Spironolactone. |
| Stiripentol | The metabolism of Anastrozole can be decreased when combined with Stiripentol. |
| Sulfadiazine | The metabolism of Anastrozole can be decreased when combined with Sulfadiazine. |
| Sulfaphenazole | The metabolism of Anastrozole can be decreased when combined with Sulfaphenazole. |
| Synthetic Conjugated Estrogens, A | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Synthetic Conjugated Estrogens, A. |
| Synthetic Conjugated Estrogens, B | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Synthetic Conjugated Estrogens, B. |
| Tamoxifen | The serum concentration of Anastrozole can be decreased when it is combined with Tamoxifen. |
| Tazarotene | The metabolism of Anastrozole can be decreased when combined with Tazarotene. |
| Tecovirimat | The metabolism of Anastrozole can be increased when combined with Tecovirimat. |
| Tegafur | The metabolism of Tegafur can be decreased when combined with Anastrozole. |
| Tegaserod | The metabolism of Anastrozole can be decreased when combined with Tegaserod. |
| Teniposide | The risk or severity of cardiotoxicity can be increased when Teniposide is combined with Anastrozole. |
| Terbinafine | The metabolism of Anastrozole can be decreased when combined with Terbinafine. |
| Terfenadine | The metabolism of Anastrozole can be decreased when combined with Terfenadine. |
| Teriflunomide | The metabolism of Anastrozole can be decreased when combined with Teriflunomide. |
| Testosterone cypionate | The metabolism of Testosterone cypionate can be decreased when combined with Anastrozole. |
| Testosterone enanthate | The metabolism of Testosterone enanthate can be decreased when combined with Anastrozole. |
| Tetracaine | The risk or severity of methemoglobinemia can be increased when Anastrozole is combined with Tetracaine. |
| Thalidomide | The risk or severity of cardiotoxicity can be increased when Thalidomide is combined with Anastrozole. |
| Theophylline | The metabolism of Anastrozole can be decreased when combined with Theophylline. |
| Tibolone | The therapeutic efficacy of Anastrozole can be decreased when used in combination with Tibolone. |
| Ticlopidine | The metabolism of Anastrozole can be decreased when combined with Ticlopidine. |
| Tocilizumab | The metabolism of Anastrozole can be increased when combined with Tocilizumab. |
| Tolbutamide | The metabolism of Anastrozole can be decreased when combined with Tolbutamide. |
| Torasemide | The metabolism of Anastrozole can be decreased when combined with Torasemide. |
| Trametinib | The metabolism of Anastrozole can be decreased when combined with Trametinib. |
| Trastuzumab | The risk or severity of cardiotoxicity can be increased when Trastuzumab is combined with Anastrozole. |
| Treprostinil | The metabolism of Anastrozole can be decreased when combined with Treprostinil. |
| Tretinoin | The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Anastrozole. |
| Triclabendazole | The metabolism of Anastrozole can be decreased when combined with Triclabendazole. |
| Trimethadione | The metabolism of Anastrozole can be decreased when combined with Trimethadione. |
| Trimethoprim | The metabolism of Anastrozole can be decreased when combined with Trimethoprim. |
| Troglitazone | The metabolism of Anastrozole can be decreased when combined with Troglitazone. |
| Tucatinib | The metabolism of Tucatinib can be decreased when combined with Anastrozole. |
| Velpatasvir | The metabolism of Velpatasvir can be decreased when combined with Anastrozole. |
| Vemurafenib | The metabolism of Anastrozole can be decreased when combined with Vemurafenib. |
| Verapamil | The metabolism of Anastrozole can be decreased when combined with Verapamil. |
| Vinblastine | The risk or severity of cardiotoxicity can be increased when Vinblastine is combined with Anastrozole. |
| Vincristine | The risk or severity of cardiotoxicity can be increased when Vincristine is combined with Anastrozole. |
| Vindesine | The risk or severity of cardiotoxicity can be increased when Vindesine is combined with Anastrozole. |
| Vinorelbine | The risk or severity of cardiotoxicity can be increased when Vinorelbine is combined with Anastrozole. |
| Vortioxetine | The metabolism of Vortioxetine can be decreased when combined with Anastrozole. |
| Voxilaprevir | The metabolism of Voxilaprevir can be decreased when combined with Anastrozole. |
| Zidovudine | The metabolism of Anastrozole can be decreased when combined with Zidovudine. |
| Zopiclone | The metabolism of Anastrozole can be decreased when combined with Zopiclone |
Pregnancy and Lactation
FDA Pregnancy Category D
Pregnancy
Although anastrozole has not been studied with pregnant women (it is intended for use only by women who have passed menopause), it is suspected that it could cause serious problems, possibly including miscarriage. Therefore, it should not be used during pregnancy. Tell your doctor immediately if you become pregnant.
Breast-feeding
It is not known whether anastrozole passes into breast milk. Because of the risks associated with this drug, women using this medication should not breastfeed. This medication is not intended for use by children.
Bone mineral density: Long-term use of anastrozole may decrease the density of bones, thereby increasing the risk of osteoporosis. Your doctor will order bone mineral density tests periodically while you are taking anastrozole.
Cholesterol: Anastrozole can cause increases in cholesterol and other lipids in the blood. If you are at an increased risk of developing high cholesterol, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Drowsiness/dizziness: Anastrozole may cause dizziness or drowsiness. If you experience either or both of these side effects, you should not drive, use machinery, or perform any other activities that require alertness.
Heart disease: This medication may increase the risk of heart attack or increased blood pressure. If you are at risk for heart disease or high blood pressure, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. If you experience signs of a heart attack, such as tightness or heaviness in your chest, sudden chest pain spreading to your arms or shoulders, sweating, nausea, or anxiety, seek medical help immediately.
Kidney function: If you have reduced kidney function, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Liver function: If you have liver disease or reduced liver function, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Pre-menopausal women: You should not use this medication if you have not yet started menopause.
What special precautions should I follow?
Before taking anastrozole,
- tell your doctor and pharmacist if you are allergic to anastrozole, or any other medications, or any of the ingredients in anastrozole. Ask your pharmacist for a list of the ingredients.
- tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: medications that contain estrogen such as hormone replacement therapy (HRT) and hormonal contraceptives (birth control pills, patches, rings, and injections); raloxifene (Evista); and tamoxifen (Nolvadex). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
- tell your doctor if you have or have ever had high cholesterol, osteoporosis (a condition in which the bones are fragile and break easily), or liver, or heart disease.
- you should know that anastrozole should only be taken by women who have undergone menopause and cannot become pregnant. However, if you are pregnant or breastfeeding, you should tell your doctor before you begin taking this medication. Anastrozole may harm the fetus.
When To Contact Your Doctor or Health Care Provider:
Contact your health care provider immediately, day or night, and go to the nearest emergency room, if you should experience any of the following symptoms:
- New or worsening chest pain
- Shortness of breath
- Swelling of the face, lips, tongue, and/or throat
- Difficulty swallowing and/or breathing.
- Vaginal bleeding (similar to a period)
- Tickling, Tingling, or Numbness of your skin
- Nausea (interfering with the ability to eat and unrelieved with prescribed medication)
- Vomiting (vomiting more than 4-5 times in a 24-hour period)
- Yellowing of your skin or the whites of your eyes
- Pain on the right side of your stomach-area
Always inform your healthcare provider if you experience any unusual symptoms.
- Before starting anastrozole treatment, make sure you tell your doctor about any other medications you are taking (including over-the-counter drugs, vitamins, or herbal remedies)
- Anastrozole interacts with certain medications. Make sure you tell your doctor if you are taking these medications:
- Tamoxifen
- Estrogen
- Warfarin
- Estrogen/estradiol-containing medications (commonly used for menopause and birth control)
- Before starting anastrozole treatment, make sure you tell your doctor about health conditions you have including heart conditions, osteoporosis, and abnormal cholesterol. Anastrozole may cause an increased risk for heart disease. Talk with your healthcare provider to weigh the benefit and risks.
- Inform your healthcare professional if you have not had menopause yet (premenopausal).
- Inform your healthcare professional if you are pregnant or may be pregnant prior to starting this treatment. Anastrozole is pregnancy category X (anastrozole may be hazardous to the fetus. Anastrozole is contraindicated in women who are pregnant or may become pregnant).
- Anastrozole may enter breast milk. It is unclear what effect this may have on babies. Tell your doctor if you are breastfeeding or plan to breastfeed.
Self-Care Tips:
- If you experience hot flashes, wearing light clothing, staying in a cool environment, and putting cool clothes on your head may reduce symptoms. Consult your healthcare provider if these worsen, or become intolerable.
- Acetaminophen or ibuprofen may help relieve discomfort from generalized aches and pains. However, be sure to talk with your doctor before taking it.
- Anastrozole causes little nausea. However, to reduce nausea, take anti-nausea medications as prescribed by your doctor before taking them.
- Good health practices such as getting plenty of rest and eating a healthy diet along with regular exercise are recommended
- If you experience symptoms or side effects, be sure to discuss them with your healthcare team. They can prescribe medications and/or offer other suggestions that are effective in managing such problems.
References
