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Drug overview for ANASTROZOLE (anastrozole):
Generic name: ANASTROZOLE (an-AS-troe-zole)
Drug class: Aromatase Inhibitors
Therapeutic class: Antineoplastics
Anastrozole, an aromatase inhibitor, is an antineoplastic agent.
No enhanced Uses information available for this drug.
Generic name: ANASTROZOLE (an-AS-troe-zole)
Drug class: Aromatase Inhibitors
Therapeutic class: Antineoplastics
Anastrozole, an aromatase inhibitor, is an antineoplastic agent.
No enhanced Uses information available for this drug.
DRUG IMAGES
ANASTROZOLE 1 MG TABLET
The following indications for ANASTROZOLE (anastrozole) have been approved by the FDA:
Indications:
Early breast cancer hormone receptor positive and postmenopausal
Hormone receptor positive postmenopausal advanced breast cancer
Metastatic breast carcinoma
Professional Synonyms:
Advanced breast carcinoma
Metastatic breast cancer
Metastatic malignancy of breast
Metastatic malignant neoplasm of breast
Metastatic malignant tumor of breast
Indications:
Early breast cancer hormone receptor positive and postmenopausal
Hormone receptor positive postmenopausal advanced breast cancer
Metastatic breast carcinoma
Professional Synonyms:
Advanced breast carcinoma
Metastatic breast cancer
Metastatic malignancy of breast
Metastatic malignant neoplasm of breast
Metastatic malignant tumor of breast
The following dosing information is available for ANASTROZOLE (anastrozole):
No enhanced Dosing information available for this drug.
Anastrozole is administered orally. Food does not affect the absorption of anastrozole, and the drug may be administered without regard to meals. Commercially available anastrozole tablets should be stored at a controlled room temperature of 20-25degreesC.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| ANASTROZOLE 1 MG TABLET | Maintenance | Adults take 1 tablet (1 mg) by oral route once daily |
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| ANASTROZOLE 1 MG TABLET | Maintenance | Adults take 1 tablet (1 mg) by oral route once daily |
The following drug interaction information is available for ANASTROZOLE (anastrozole):
There are 2 contraindications.
These drug combinations generally should not be dispensed or administered to the same patient. A manufacturer label warning that indicates the contraindication warrants inclusion of a drug combination in this category, regardless of clinical evidence or lack of clinical evidence to support the contraindication.
| Drug Interaction | Drug Names |
|---|---|
| Anastrozole; Letrozole/Tamoxifen SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Tamoxifen may induce the metabolism of anastrozole(1) and letrozole(2) by induction of CYP3A4. CLINICAL EFFECTS: Concurrent use of tamoxifen may result in decreased plasma levels and effectiveness of anastrozole(1,3) and letrozole.(2,3) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The manufacturers of anastrozole(1) and tamoxifen(3) state that these agents should not be coadministered. The manufacturer of letrozole does not recommend concurrent therapy with tamoxifen(4) and the manufacturer of tamoxifen states they should not be used concurrently.(3) Patients may benefit more from sequential therapy, rather than concurrent therapy.(2,5) DISCUSSION: Based on clinical and pharmacokinetic data from the ATAC trial, tamoxifen should not be administered with anastrozole. Concurrent use decreased anastrozole plasma levels by 27%. The combination had no efficacy benefit when compared to tamoxifen administration alone. Tamoxifen pharmacokinetics were not affected.(1,3) A study in 12 subjects examined the concurrent administration of tamoxifen and letrozole for six weeks. Concurrent use decreased the mean concentration of letrozole by 37.6%.(3,4) Although suppression of estradiol, estrone, and estrone sulfate were not effected, the authors speculated that patients may not receive the full benefit of combination therapy.(4) A study in 23 patients found that letrozole had no effect on tamoxifen levels. However, the antitumor effects of combination therapy were less than expected.(6) The therapeutic effect of letrozole is not affected if letrozole is administered immediately after tamoxifen.(5) |
SOLTAMOX, TAMOXIFEN CITRATE |
| Selected Anti-Aromatase Agents/Estrogens SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Aromatase inhibitors(1-6) and inactivators(7-10) treat breast cancer by inhibiting estrogen synthesis therefore lowering serum estrone and estradiol levels. In postmenopausal women, androgens are metabolized to estrogens via the primary pathway of the aromatase enzyme. CLINICAL EFFECTS: Concurrent administration of estrogen may decrease the effectiveness of aromatase inhibitors.(1-6) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The Canadian,(1) UK,(2) and US(3) manufacturers of anastrozole state that estrogen containing therapies should not be used during anastrozole therapy. The Australian,(7) Canadian,(8) UK,(9) and US(10) manufacturers of exemestane state that exemestane should not be administered with estrogen containing therapies. The Canadian(4) and UK(5) manufacturer of letrozole state that estrogen containing therapies should be avoided during letrozole therapy. DISCUSSION: Many breast cancers have estrogen receptors and their growth can be stimulated by estrogen. Anastrozole is a potent and selective non-steroidal aromatase inhibitor that lowers serum estradiol levels. Concurrent use of estrogen may diminish the effects of anastrozole.(1-3) Exemestane is a steroidal aromatase inactivator that lowers serum estradiol levels. Concurrent use of estrogen may diminish the effects of exemestane.(7-10) |
2-METHOXYESTRADIOL, ACTIVELLA, AFIRMELLE, ALTAVERA, ALYACEN, AMETHIA, AMETHYST, ANGELIQ, ANNOVERA, APRI, ARANELLE, ASHLYNA, AUBRA, AUBRA EQ, AUROVELA, AUROVELA 24 FE, AUROVELA FE, AVIANE, AYUNA, AZURETTE, BALCOLTRA, BALZIVA, BEYAZ, BIJUVA, BLISOVI 24 FE, BLISOVI FE, BRIELLYN, CAMRESE, CAMRESE LO, CAZIANT, CHARLOTTE 24 FE, CHATEAL EQ, CLIMARA, CLIMARA PRO, COMBIPATCH, COVARYX, COVARYX H.S., CRYSELLE, CYRED, CYRED EQ, DASETTA, DAYSEE, DELESTROGEN, DEPO-ESTRADIOL, DESOGESTR-ETH ESTRAD ETH ESTRA, DIETHYLSTILBESTROL, DIVIGEL, DOLISHALE, DOTTI, DROSPIRENONE-ETH ESTRA-LEVOMEF, DROSPIRENONE-ETHINYL ESTRADIOL, DUAVEE, EEMT, EEMT H.S., ELESTRIN, ELINEST, ELURYNG, ENILLORING, ENPRESSE, ENSKYCE, ESTARYLLA, ESTRACE, ESTRADIOL, ESTRADIOL (ONCE WEEKLY), ESTRADIOL (TWICE WEEKLY), ESTRADIOL BENZOATE, ESTRADIOL CYPIONATE, ESTRADIOL HEMIHYDRATE, ESTRADIOL HEMIHYDRATE MICRO, ESTRADIOL MICRONIZED, ESTRADIOL VALERATE, ESTRADIOL-NORETHINDRONE ACETAT, ESTRATEST F.S., ESTRATEST H.S., ESTRING, ESTRIOL, ESTRIOL MICRONIZED, ESTROGEL, ESTROGEN-METHYLTESTOSTERONE, ESTRONE, ETHINYL ESTRADIOL, ETHYNODIOL-ETHINYL ESTRADIOL, ETONOGESTREL-ETHINYL ESTRADIOL, EVAMIST, FALMINA, FEMLYV, FEMRING, FINZALA, FYAVOLV, GEMMILY, HAILEY, HAILEY 24 FE, HAILEY FE, HALOETTE, ICLEVIA, IMVEXXY, ISIBLOOM, JAIMIESS, JASMIEL, JINTELI, JOLESSA, JOYEAUX, JULEBER, JUNEL, JUNEL FE, JUNEL FE 24, KAITLIB FE, KALLIGA, KARIVA, KELNOR 1-35, KELNOR 1-50, KURVELO, LARIN, LARIN 24 FE, LARIN FE, LAYOLIS FE, LEENA, LESSINA, LEVONEST, LEVONORG-ETH ESTRAD ETH ESTRAD, LEVONORG-ETH ESTRAD-FE BISGLYC, LEVONORGESTREL-ETH ESTRADIOL, LEVORA-28, LO LOESTRIN FE, LO-ZUMANDIMINE, LOESTRIN, LOESTRIN FE, LOJAIMIESS, LORYNA, LOW-OGESTREL, LUTERA, LYLLANA, MARLISSA, MENEST, MENOSTAR, MERZEE, MIBELAS 24 FE, MICROGESTIN, MICROGESTIN FE, MILI, MIMVEY, MINIVELLE, MINZOYA, MONO-LINYAH, MYFEMBREE, NATAZIA, NECON, NEXTSTELLIS, NIKKI, NORELGESTROMIN-ETH ESTRADIOL, NORETHIN-ETH ESTRA-FERROUS FUM, NORETHINDRON-ETHINYL ESTRADIOL, NORETHINDRONE-E.ESTRADIOL-IRON, NORGESTIMATE-ETHINYL ESTRADIOL, NORTREL, NUVARING, NYLIA, OCELLA, ORIAHNN, ORTHO TRI-CYCLEN, ORTHO-NOVUM, PHILITH, PIMTREA, PORTIA, PREMARIN, PREMPHASE, PREMPRO, RECLIPSEN, RIVELSA, SAFYRAL, SETLAKIN, SIMLIYA, SIMPESSE, SPRINTEC, SRONYX, SYEDA, TARINA 24 FE, TARINA FE, TARINA FE 1-20 EQ, TAYTULLA, TILIA FE, TRI-ESTARYLLA, TRI-LEGEST FE, TRI-LINYAH, TRI-LO-ESTARYLLA, TRI-LO-MARZIA, TRI-LO-MILI, TRI-LO-SPRINTEC, TRI-MILI, TRI-SPRINTEC, TRI-VYLIBRA, TRI-VYLIBRA LO, TRIVORA-28, TURQOZ, TWIRLA, TYBLUME, VAGIFEM, VELIVET, VESTURA, VIENVA, VIORELE, VIVELLE-DOT, VOLNEA, VYFEMLA, VYLIBRA, WERA, WYMZYA FE, XULANE, YASMIN 28, YAZ, YUVAFEM, ZAFEMY, ZARAH, ZOVIA 1-35, ZUMANDIMINE |
There are 2 severe interactions.
These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.
| Drug Interaction | Drug Names |
|---|---|
| Deferiprone/Selected Myelosuppressive Agents SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Concurrent use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis may increase the frequency or risk for severe toxicity.(1) CLINICAL EFFECTS: Concurrent use of deferiprone and myelosuppressive agents may result in severe neutropenia or agranulocytosis, which may be fatal. PREDISPOSING FACTORS: Agranulocytosis may be less common in patients receiving deferiprone for thalassemia, and more common in patients treated for other systemic iron overload conditions (e.g. myelodysplastic syndromes, sickle cell disease).(2,3) Inadequate monitoring appears to increase the risk for severe outcomes. Manufacturer post market surveillance found that in all fatal cases of agranulocytosis reported between 1999 and 2005, data on weekly white blood count (WBC) monitoring was missing. In three fatal cases, deferiprone was continued for two to seven days after the detection of neutropenia or agranulocytosis.(2) PATIENT MANAGEMENT: If possible, discontinue one of the drugs associated with risk for neutropenia or agranulocytosis. If alternative therapy is not available, documentation and adherence to the deferiprone monitoring protocol is essential. Baseline absolute neutrophil count (ANC) must be at least 1,500/uL prior to starting deferiprone. Monitor ANC weekly during therapy. If infection develops, interrupt deferiprone therapy and monitor ANC more frequently. If ANC is less than 1,500/uL but greater than 500/uL, discontinue deferiprone and any other drugs possibly associated with neutropenia. Initiate ANC and platelet counts daily until recovery (i.e. ANC at least 1,500/uL). If ANC is less than 500/uL, discontinue deferiprone, evaluate patient and hospitalize if appropriate. Do not resume deferiprone unless potential benefits outweigh potential risks.(1) DISCUSSION: Drugs linked to this monograph have an FDA Boxed Warning for risk of neutropenia, agranulocytosis, or pancytopenia, or have > 5% risk for neutropenia and/or warnings describing risk for myelosuppression in manufacturer prescribing information.(1-25) In pooled clinical studies submitted to the FDA, 6.1% of deferiprone patients met criteria for neutropenia and 1.7% of patients developed agranulocytosis.(1) The time to onset of agranulocytosis was highly variable with a range of 65 days to 9.2 years (median, 161 days).(3) |
DEFERIPRONE, DEFERIPRONE (3 TIMES A DAY), FERRIPROX, FERRIPROX (2 TIMES A DAY), FERRIPROX (3 TIMES A DAY) |
| Clozapine/Selected Myelosuppressive Agents SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Clozapine and other myelosuppressive agents may be associated with neutropenia or agranulocytosis.(2) CLINICAL EFFECTS: Moderate neutropenia, even if due to combination therapy, may require abrupt discontinuation of clozapine resulting in decompensation of the patient's psychiatric disorder (e.g. schizophrenia). The disease treated by the myelosuppressive agent may be compromised if myelosuppression requires dose reduction, delay, or discontinuation of the myelosuppressive agent. Undetected severe neutropenia or agranulocytosis may be fatal. PREDISPOSING FACTORS: Low white blood counts prior to initiation of the myelosuppressive agent may increase risk for clinically significant neutropenia. PATIENT MANAGEMENT: If a patient stabilized on clozapine therapy requires treatment with a myelosuppressive agent, the clozapine prescriber should consult with prescriber of the myelosuppressive agent (e.g. oncologist) to discuss treatment and monitoring options.(2) More frequent ANC monitoring or treatment alternatives secondary to neutropenic episodes may need to be considered. Clozapine is only available through a restricted distribution system which requires documentation of the absolute neutrophil count (ANC) prior to dispensing.(1-2) For most clozapine patients, clozapine treatment must be interrupted for a suspected clozapine-induced ANC < 1000 cells/microliter. For patients with benign ethnic neutropenia (BEN), treatment must be interrupted for suspected clozapine-induced neutropenia < 500 cells/microliter.(2) DISCUSSION: Clozapine is only available through a restricted distribution system which requires documentation of the ANC prior to dispensing.(1) Agents linked to this interaction generally have > 5% risk for neutropenia and/or warnings describing risk for myelosuppression in manufacturer prescribing information.(3-26) |
CLOZAPINE, CLOZAPINE ODT, CLOZARIL, VERSACLOZ |
There are 0 moderate interactions.
The following contraindication information is available for ANASTROZOLE (anastrozole):
Drug contraindication overview.
* Known hypersensitivity to anastrozole or any ingredient in the formulation.
* Known hypersensitivity to anastrozole or any ingredient in the formulation.
There are 1 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Lactation |
There are 2 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Myocardial ischemia |
| Pregnancy |
There are 2 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Hypercholesterolemia |
| Osteopenia |
The following adverse reaction information is available for ANASTROZOLE (anastrozole):
Adverse reaction overview.
In the early breast cancer study (ATAC), the most common adverse effects (occurring in 10% or more of patients) included hot flashes, asthenia, arthritis, pain, arthralgia, pharyngitis, hypertension, depression, nausea, vomiting, rash, osteoporosis, fractures, back pain, insomnia, headache, peripheral edema, and lymphedema. In advanced breast cancer studies, the most common adverse effects (occurring in 10% or more of patients) included hot flashes, nausea, asthenia, pain, headache, back pain, bone pain, increased cough, dyspnea, pharyngitis, and peripheral edema.
In the early breast cancer study (ATAC), the most common adverse effects (occurring in 10% or more of patients) included hot flashes, asthenia, arthritis, pain, arthralgia, pharyngitis, hypertension, depression, nausea, vomiting, rash, osteoporosis, fractures, back pain, insomnia, headache, peripheral edema, and lymphedema. In advanced breast cancer studies, the most common adverse effects (occurring in 10% or more of patients) included hot flashes, nausea, asthenia, pain, headache, back pain, bone pain, increased cough, dyspnea, pharyngitis, and peripheral edema.
There are 22 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Chest pain Dyspnea Fracture Hypertension |
Anemia Angina Cataracts Leukopenia Thromboembolic disorder Thrombophlebitis Tumor flare reaction |
| Rare/Very Rare |
|---|
|
Anaphylaxis Angioedema Erythema multiforme Hepatitis Hyperbilirubinemia Jaundice Myocardial ischemia Stevens-johnson syndrome Tendon rupture Tenosynovitis Urticaria |
There are 51 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Abdominal pain with cramps Arthralgia Arthritis Back pain Bone pain Cough Depression Diarrhea Dizziness Drug-induced hot flash Flushing Gastrointestinal irritation General weakness Headache disorder Insomnia Lymphedema Nausea Osteoporosis Pain Paresthesia Peripheral edema Pharyngitis Skin rash Vomiting Xerostomia |
Abnormal vaginal bleeding Alopecia Carpal tunnel syndrome Constipation Dyspepsia Flu-like symptoms Hyperhidrosis Mastalgia Mood changes Myalgia Pelvic pain Pruritus of skin Rhinitis Sinusitis Urinary tract infection Vaginal discharge Vaginal dryness Vulvovaginitis Weight gain |
| Rare/Very Rare |
|---|
|
Abnormal hepatic function tests Acute cognitive impairment Drowsy Hypercalcemia Hypercholesterolemia Tendonitis Trigger finger |
The following precautions are available for ANASTROZOLE (anastrozole):
Efficacy of anastrozole for the treatment of pubertal gynecomastia+ in adolescent males and for the treatment of progressive precocious puberty associated with McCune-Albright syndrome+ in girls has not been established. Results of a randomized, double-blind, placebo-controlled trial in 80 adolescent males 11-18 years of age with pubertal gynecomastia failed to establish efficacy of anastrozole (1 mg daily for 6 months) in reducing gynecomastia or relieving breast pain. Serum estradiol concentrations were reduced by 15.4
or 4.5% in patients receiving anastrozole or placebo, respectively. Patients receiving anastrozole were more likely to experience treatment-related adverse effects (16.3 versus 8.1%), and the difference was related mainly to higher rates of acne and headache in those receiving anastrozole.
One patient discontinued anastrozole therapy because of testicular enlargement. Results of a noncomparative open-label trial of anastrozole (1 mg daily for 12 months) in 28 girls (2 to less than 10 years of age) with McCune-Albright syndrome and progressive precocious puberty showed no reduction from baseline in the frequency of vaginal bleeding days or in the rate of increase in bone age and no clinically important changes in Tanner staging, mean ovarian or uterine volume, or mean predicted adult height. A small reduction in growth rate was observed; however, because the study was uncontrolled, it is unclear whether this effect was related to anastrozole or to other confounding factors (e.g., variations in endogenous estrogen levels commonly observed in patients with McCune-Albright syndrome).
Adverse effects (i.e., nausea, acne, extremity pain, increased aminotransferase concentrations, allergic dermatitis) were reported in 18% of patients. Pharmacokinetics of anastrozole were similar in adolescent males with pubertal gynecomastia and in girls with McCune-Albright syndrome, and the elimination half-life in these pediatric populations (about 47 hours) was similar to that observed in postmenopausal women with breast cancer.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
or 4.5% in patients receiving anastrozole or placebo, respectively. Patients receiving anastrozole were more likely to experience treatment-related adverse effects (16.3 versus 8.1%), and the difference was related mainly to higher rates of acne and headache in those receiving anastrozole.
One patient discontinued anastrozole therapy because of testicular enlargement. Results of a noncomparative open-label trial of anastrozole (1 mg daily for 12 months) in 28 girls (2 to less than 10 years of age) with McCune-Albright syndrome and progressive precocious puberty showed no reduction from baseline in the frequency of vaginal bleeding days or in the rate of increase in bone age and no clinically important changes in Tanner staging, mean ovarian or uterine volume, or mean predicted adult height. A small reduction in growth rate was observed; however, because the study was uncontrolled, it is unclear whether this effect was related to anastrozole or to other confounding factors (e.g., variations in endogenous estrogen levels commonly observed in patients with McCune-Albright syndrome).
Adverse effects (i.e., nausea, acne, extremity pain, increased aminotransferase concentrations, allergic dermatitis) were reported in 18% of patients. Pharmacokinetics of anastrozole were similar in adolescent males with pubertal gynecomastia and in girls with McCune-Albright syndrome, and the elimination half-life in these pediatric populations (about 47 hours) was similar to that observed in postmenopausal women with breast cancer.
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Anastrozole may cause fetal harm; the drug has been shown to be embryotoxic, fetotoxic, and abortifacient in animals. The manufacturer states that a pregnancy test should be performed prior to initiation of anastrozole therapy in females of reproductive potential and that such women should be advised to use effective contraceptive methods while receiving the drug and for at least 3 weeks after discontinuance of therapy. If the drug is administered during pregnancy or if the patient becomes pregnant while receiving the drug, the patient should be informed of the potential hazard to the fetus and the potential risk for loss of the pregnancy.
Adequate, well-controlled studies of anastrozole in pregnant women have not been conducted. Anastrozole has been shown to cross the placenta in rats and rabbits receiving oral doses of 0.1 mg/kg (approximately 1 and 1.9 times the recommended human dose, respectively, on a mg/m2 basis).
Increased pregnancy loss (increased preimplantation and/or postimplantation loss, increased resorption, and decreased numbers of live fetuses) was demonstrated in rats and rabbits receiving anastrozole dosages equal to or exceeding 0.1 and 0.02 mg/kg daily, respectively (about one and one-third times the recommended human dosage, respectively, on a mg/m2 basis), during the period of organogenesis; in rats, this effect was dose-related.
In rats receiving dosages equal to or exceeding 0.1 mg/kg daily, placental weights were increased. In rats, anastrozole dosages of 1 mg/kg daily (which produced steady-state peak plasma anastrozole concentrations and AUC0-24h values that were 19 and 9 times higher, respectively, than those observed in healthy postmenopausal women receiving the recommended dose) resulted in fetotoxicity, including delayed fetal development (i.e., incomplete ossification and depressed fetal body weights).
In rats, no evidence of teratogenicity was observed at dosages of up to 1 mg/kg daily. In rabbits, anastrozole dosages equal to or exceeding 1 mg/kg daily (about 16 times the recommended human dosage on a mg/m2 basis) caused pregnancy failure. No evidence of teratogenicity was observed in rabbits receiving anastrozole 0.2 mg/kg daily (about 3 times the recommended human dosage on a mg/m2 basis).
Adequate, well-controlled studies of anastrozole in pregnant women have not been conducted. Anastrozole has been shown to cross the placenta in rats and rabbits receiving oral doses of 0.1 mg/kg (approximately 1 and 1.9 times the recommended human dose, respectively, on a mg/m2 basis).
Increased pregnancy loss (increased preimplantation and/or postimplantation loss, increased resorption, and decreased numbers of live fetuses) was demonstrated in rats and rabbits receiving anastrozole dosages equal to or exceeding 0.1 and 0.02 mg/kg daily, respectively (about one and one-third times the recommended human dosage, respectively, on a mg/m2 basis), during the period of organogenesis; in rats, this effect was dose-related.
In rats receiving dosages equal to or exceeding 0.1 mg/kg daily, placental weights were increased. In rats, anastrozole dosages of 1 mg/kg daily (which produced steady-state peak plasma anastrozole concentrations and AUC0-24h values that were 19 and 9 times higher, respectively, than those observed in healthy postmenopausal women receiving the recommended dose) resulted in fetotoxicity, including delayed fetal development (i.e., incomplete ossification and depressed fetal body weights).
In rats, no evidence of teratogenicity was observed at dosages of up to 1 mg/kg daily. In rabbits, anastrozole dosages equal to or exceeding 1 mg/kg daily (about 16 times the recommended human dosage on a mg/m2 basis) caused pregnancy failure. No evidence of teratogenicity was observed in rabbits receiving anastrozole 0.2 mg/kg daily (about 3 times the recommended human dosage on a mg/m2 basis).
It is not known whether anastrozole or its metabolites are distributed into human milk or if the drug has any effect on nursing infants or on milk production. Because many drugs are distributed into milk and because tumorigenic effects of anastrozole have been observed in animals and anastrozole has the potential to cause serious adverse reactions in nursing infants, women should be advised to discontinue breast-feeding during anastrozole therapy and for 2 weeks after discontinuance of the drug.
Among patients receiving anastrozole as adjuvant therapy for early-stage breast cancer in the ATAC trial, 45% were 65 years of age or older. Subgroup analysis showed that anastrozole did not provide the same benefit for disease-free survival in women 65 years of age or older (hazard ratio of 0.93 with a 95% confidence interval of 0.8-1.08) that it provided in postmenopausal women younger than 65 years of age (hazard ratio of 0.79 with a 95% confidence interval of 0.67-0.94). Among patients receiving anastrozole as first-line or second-line therapy in clinical trials, about 50% were 65 years of age or older. No difference in efficacy was observed for geriatric patients (65 years or older) compared with younger patients receiving anastrozole as second-line therapy for advanced breast cancer; moderately greater efficacy was observed for geriatric patients (65 years or older) receiving either anastrozole or tamoxifen as first-line therapy for advanced breast cancer.
The following prioritized warning is available for ANASTROZOLE (anastrozole):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for ANASTROZOLE (anastrozole)'s list of indications:
| Early breast cancer HR positive and postmenopausal | |
| C50.11 | Malignant neoplasm of central portion of breast, female |
| C50.111 | Malignant neoplasm of central portion of right female breast |
| C50.112 | Malignant neoplasm of central portion of left female breast |
| C50.119 | Malignant neoplasm of central portion of unspecified female breast |
| C50.21 | Malignant neoplasm of upper-inner quadrant of breast, female |
| C50.211 | Malignant neoplasm of upper-inner quadrant of right female breast |
| C50.212 | Malignant neoplasm of upper-inner quadrant of left female breast |
| C50.219 | Malignant neoplasm of upper-inner quadrant of unspecified female breast |
| C50.31 | Malignant neoplasm of lower-inner quadrant of breast, female |
| C50.311 | Malignant neoplasm of lower-inner quadrant of right female breast |
| C50.312 | Malignant neoplasm of lower-inner quadrant of left female breast |
| C50.319 | Malignant neoplasm of lower-inner quadrant of unspecified female breast |
| C50.41 | Malignant neoplasm of upper-outer quadrant of breast, female |
| C50.411 | Malignant neoplasm of upper-outer quadrant of right female breast |
| C50.412 | Malignant neoplasm of upper-outer quadrant of left female breast |
| C50.419 | Malignant neoplasm of upper-outer quadrant of unspecified female breast |
| C50.51 | Malignant neoplasm of lower-outer quadrant of breast, female |
| C50.511 | Malignant neoplasm of lower-outer quadrant of right female breast |
| C50.512 | Malignant neoplasm of lower-outer quadrant of left female breast |
| C50.519 | Malignant neoplasm of lower-outer quadrant of unspecified female breast |
| C50.61 | Malignant neoplasm of axillary tail of breast, female |
| C50.611 | Malignant neoplasm of axillary tail of right female breast |
| C50.612 | Malignant neoplasm of axillary tail of left female breast |
| C50.619 | Malignant neoplasm of axillary tail of unspecified female breast |
| C50.81 | Malignant neoplasm of overlapping sites of breast, female |
| C50.811 | Malignant neoplasm of overlapping sites of right female breast |
| C50.812 | Malignant neoplasm of overlapping sites of left female breast |
| C50.819 | Malignant neoplasm of overlapping sites of unspecified female breast |
| C50.91 | Malignant neoplasm of breast of unspecified site, female |
| C50.911 | Malignant neoplasm of unspecified site of right female breast |
| C50.912 | Malignant neoplasm of unspecified site of left female breast |
| C50.919 | Malignant neoplasm of unspecified site of unspecified female breast |
| Z17.0 | Estrogen receptor positive status [Er+] |
| Z19.1 | Hormone sensitive malignancy status |
| Hormone receptor + postmenopausal advanced breast cancer | |
| C50.11 | Malignant neoplasm of central portion of breast, female |
| C50.111 | Malignant neoplasm of central portion of right female breast |
| C50.112 | Malignant neoplasm of central portion of left female breast |
| C50.119 | Malignant neoplasm of central portion of unspecified female breast |
| C50.21 | Malignant neoplasm of upper-inner quadrant of breast, female |
| C50.211 | Malignant neoplasm of upper-inner quadrant of right female breast |
| C50.212 | Malignant neoplasm of upper-inner quadrant of left female breast |
| C50.219 | Malignant neoplasm of upper-inner quadrant of unspecified female breast |
| C50.31 | Malignant neoplasm of lower-inner quadrant of breast, female |
| C50.311 | Malignant neoplasm of lower-inner quadrant of right female breast |
| C50.312 | Malignant neoplasm of lower-inner quadrant of left female breast |
| C50.319 | Malignant neoplasm of lower-inner quadrant of unspecified female breast |
| C50.41 | Malignant neoplasm of upper-outer quadrant of breast, female |
| C50.411 | Malignant neoplasm of upper-outer quadrant of right female breast |
| C50.412 | Malignant neoplasm of upper-outer quadrant of left female breast |
| C50.419 | Malignant neoplasm of upper-outer quadrant of unspecified female breast |
| C50.51 | Malignant neoplasm of lower-outer quadrant of breast, female |
| C50.511 | Malignant neoplasm of lower-outer quadrant of right female breast |
| C50.512 | Malignant neoplasm of lower-outer quadrant of left female breast |
| C50.519 | Malignant neoplasm of lower-outer quadrant of unspecified female breast |
| C50.61 | Malignant neoplasm of axillary tail of breast, female |
| C50.611 | Malignant neoplasm of axillary tail of right female breast |
| C50.612 | Malignant neoplasm of axillary tail of left female breast |
| C50.619 | Malignant neoplasm of axillary tail of unspecified female breast |
| C50.81 | Malignant neoplasm of overlapping sites of breast, female |
| C50.811 | Malignant neoplasm of overlapping sites of right female breast |
| C50.812 | Malignant neoplasm of overlapping sites of left female breast |
| C50.819 | Malignant neoplasm of overlapping sites of unspecified female breast |
| C50.91 | Malignant neoplasm of breast of unspecified site, female |
| C50.911 | Malignant neoplasm of unspecified site of right female breast |
| C50.912 | Malignant neoplasm of unspecified site of left female breast |
| C50.919 | Malignant neoplasm of unspecified site of unspecified female breast |
| Z17.0 | Estrogen receptor positive status [Er+] |
| Z19.1 | Hormone sensitive malignancy status |
| Metastatic breast carcinoma | |
| C50 | Malignant neoplasm of breast |
| C50.1 | Malignant neoplasm of central portion of breast |
| C50.11 | Malignant neoplasm of central portion of breast, female |
| C50.111 | Malignant neoplasm of central portion of right female breast |
| C50.112 | Malignant neoplasm of central portion of left female breast |
| C50.119 | Malignant neoplasm of central portion of unspecified female breast |
| C50.12 | Malignant neoplasm of central portion of breast, male |
| C50.121 | Malignant neoplasm of central portion of right male breast |
| C50.122 | Malignant neoplasm of central portion of left male breast |
| C50.129 | Malignant neoplasm of central portion of unspecified male breast |
| C50.2 | Malignant neoplasm of upper-inner quadrant of breast |
| C50.21 | Malignant neoplasm of upper-inner quadrant of breast, female |
| C50.211 | Malignant neoplasm of upper-inner quadrant of right female breast |
| C50.212 | Malignant neoplasm of upper-inner quadrant of left female breast |
| C50.219 | Malignant neoplasm of upper-inner quadrant of unspecified female breast |
| C50.22 | Malignant neoplasm of upper-inner quadrant of breast, male |
| C50.221 | Malignant neoplasm of upper-inner quadrant of right male breast |
| C50.222 | Malignant neoplasm of upper-inner quadrant of left male breast |
| C50.229 | Malignant neoplasm of upper-inner quadrant of unspecified male breast |
| C50.3 | Malignant neoplasm of lower-inner quadrant of breast |
| C50.31 | Malignant neoplasm of lower-inner quadrant of breast, female |
| C50.311 | Malignant neoplasm of lower-inner quadrant of right female breast |
| C50.312 | Malignant neoplasm of lower-inner quadrant of left female breast |
| C50.319 | Malignant neoplasm of lower-inner quadrant of unspecified female breast |
| C50.32 | Malignant neoplasm of lower-inner quadrant of breast, male |
| C50.321 | Malignant neoplasm of lower-inner quadrant of right male breast |
| C50.322 | Malignant neoplasm of lower-inner quadrant of left male breast |
| C50.329 | Malignant neoplasm of lower-inner quadrant of unspecified male breast |
| C50.4 | Malignant neoplasm of upper-outer quadrant of breast |
| C50.41 | Malignant neoplasm of upper-outer quadrant of breast, female |
| C50.411 | Malignant neoplasm of upper-outer quadrant of right female breast |
| C50.412 | Malignant neoplasm of upper-outer quadrant of left female breast |
| C50.419 | Malignant neoplasm of upper-outer quadrant of unspecified female breast |
| C50.42 | Malignant neoplasm of upper-outer quadrant of breast, male |
| C50.421 | Malignant neoplasm of upper-outer quadrant of right male breast |
| C50.422 | Malignant neoplasm of upper-outer quadrant of left male breast |
| C50.429 | Malignant neoplasm of upper-outer quadrant of unspecified male breast |
| C50.5 | Malignant neoplasm of lower-outer quadrant of breast |
| C50.51 | Malignant neoplasm of lower-outer quadrant of breast, female |
| C50.511 | Malignant neoplasm of lower-outer quadrant of right female breast |
| C50.512 | Malignant neoplasm of lower-outer quadrant of left female breast |
| C50.519 | Malignant neoplasm of lower-outer quadrant of unspecified female breast |
| C50.52 | Malignant neoplasm of lower-outer quadrant of breast, male |
| C50.521 | Malignant neoplasm of lower-outer quadrant of right male breast |
| C50.522 | Malignant neoplasm of lower-outer quadrant of left male breast |
| C50.529 | Malignant neoplasm of lower-outer quadrant of unspecified male breast |
| C50.6 | Malignant neoplasm of axillary tail of breast |
| C50.61 | Malignant neoplasm of axillary tail of breast, female |
| C50.611 | Malignant neoplasm of axillary tail of right female breast |
| C50.612 | Malignant neoplasm of axillary tail of left female breast |
| C50.619 | Malignant neoplasm of axillary tail of unspecified female breast |
| C50.62 | Malignant neoplasm of axillary tail of breast, male |
| C50.621 | Malignant neoplasm of axillary tail of right male breast |
| C50.622 | Malignant neoplasm of axillary tail of left male breast |
| C50.629 | Malignant neoplasm of axillary tail of unspecified male breast |
| C50.8 | Malignant neoplasm of overlapping sites of breast |
| C50.81 | Malignant neoplasm of overlapping sites of breast, female |
| C50.811 | Malignant neoplasm of overlapping sites of right female breast |
| C50.812 | Malignant neoplasm of overlapping sites of left female breast |
| C50.819 | Malignant neoplasm of overlapping sites of unspecified female breast |
| C50.82 | Malignant neoplasm of overlapping sites of breast, male |
| C50.821 | Malignant neoplasm of overlapping sites of right male breast |
| C50.822 | Malignant neoplasm of overlapping sites of left male breast |
| C50.829 | Malignant neoplasm of overlapping sites of unspecified male breast |
| C50.9 | Malignant neoplasm of breast of unspecified site |
| C50.91 | Malignant neoplasm of breast of unspecified site, female |
| C50.911 | Malignant neoplasm of unspecified site of right female breast |
| C50.912 | Malignant neoplasm of unspecified site of left female breast |
| C50.919 | Malignant neoplasm of unspecified site of unspecified female breast |
| C50.92 | Malignant neoplasm of breast of unspecified site, male |
| C50.921 | Malignant neoplasm of unspecified site of right male breast |
| C50.922 | Malignant neoplasm of unspecified site of left male breast |
| C50.929 | Malignant neoplasm of unspecified site of unspecified male breast |
Formulary Reference Tool