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Anastrozole

 
Drug Info: Anastrozole
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Brand names: Arimidex®

Chemical formula:



Anastrozole tablets

What are anastrozole tablets?

ANASTROZOLE (Arimidex®) blocks the production of the hormone estrogen. Some types of breast cancer depend on estrogen to grow, and anastrozole can stop tumor growth by blocking estrogen production. Anastrozole is for the treatment of breast cancer in postmenopausal women only. Generic anastrozole tablets are not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• liver disease
• an unusual or allergic reaction to anastrozole, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take anastrozole tablets by mouth at the same time each day with or without food. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Do not take your medicine more often than directed. Do not stop taking except on your prescriber's advice.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses. If you vomit after taking a dose, call your prescriber or health care professional for advice.

What drug(s) may interact with anastrozole?

• androstenedione
• any medicine containing estrogens (This may include some herbal products and some birth control pills)
• DHEA

Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking anastrozole?

Visit your prescriber or health care professional for regular checks on your progress. Let your prescriber or health care professional know about any unusual vaginal bleeding.

Do not treat yourself for diarrhea, nausea, vomiting or other side effects. Ask your prescriber or health care professional for advice.

What side effects may I notice from taking anastrozole?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• any new or unusual symptoms
• difficulty breathing
• chest pain
• leg pain or swelling
• vaginal bleeding
• vomiting

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• back or bone pain
• cough, or throat infection
• diarrhea or constipation
• dizziness
• headache
• hot flashes
• loss of appetite
• nausea
• stomach pain
• sweating
• weakness and tiredness
• weight gain

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store between 20 and 25 degrees C (68 and 77 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia: Anastrozole
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Home > Library > Miscellaneous > Wikipedia
Anastrozole
Systematic (IUPAC) name
2-[3-(1-cyano-1-methyl-ethyl)- 5-(1H-1,2,4-triazol-1-ylmethyl)phenyl]- 2-methyl- propanenitrile
Identifiers
CAS number 120511-73-1
ATC code L02BG03
PubChem 2187
DrugBank APRD00016
ChemSpider 2102
Chemical data
Formula C17H19N5 
Mol. mass 293.366 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 83-85%
Protein binding 40%
Metabolism 85% hepatic
Half life 72 hours
Excretion 11% renal
Therapeutic considerations
Pregnancy cat.

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Legal status

Rx only (U.S.)
Routes oral
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Anastrozole (INN, trade name Arimidex, AstraZeneca) is a drug used to treat breast cancer after surgery and for metastases in post-menopausal women.

Anastrozole is an aromatase inhibitor, which means that it interrupts a critical step in the body's synthesis of estrogen. Some breast cancer cells require estrogen to grow, and eliminating estrogen suppresses their growth.

Annual sales approx $2.2bn. Patent expires 2010 in the US[1]; however, the generic form is available in some other markets.

Contents

Clinical trials

The ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial represents a long-term follow-up study of 9366 women with localized breast cancer who received either anastrozole, tamoxifen, or both.[2] After more than 5 years the group that received anastrozole had significantly better clinical results than the tamoxifen group. The trial suggested that anastrozole is the preferred medical therapy for postmenopausal women with localized breast cancer that is estrogen receptor (ER) positive.

Another study found that the risk of recurrence was reduced 40% (with some risk of bone fracture) and that ER negative patients also benefited from switching to Arimidex.[3]

Mechanism of Action

Anastrozole inhibits the enzyme aromatase, which is responsible for converting androgens to estrogens. Anastrozole binds reversibly to the aromatase enzyme through competitive inhibition.

Elevated levels of estrogens may increase the severity of breast cancer, as sex hormones can cause hyperplasia and differentiation at estrogen receptor sites.

Side effects

Bone weakness : Women who switched to Arimidex (after two years on tamoxifen) reported twice as many fractures as those who continued to take tamoxifen (2.1% compared to 1%).[3]

Bisphosphonates are sometimes prescribed to prevent the osteoporosis induced by aromatase inhibitors but have another serious side effect, osteonecrosis of the jaws. Since statins have a bone strengthening effect [4], combining a statin with an aromatase inhibitor may avoid both fractures and possible cardiovascular risks [5] without jaw osteonecrosis.[6] In one study of women with breast cancer taking anastrozole, statin use was associated with a 38% reduced fracture risk, or approximately the equivalent of 10 mg Fosamax daily.[7]

Usage for men

While officially indicated for women, this drug has proven effective in the off-label use of reducing estrogens (in particular and more importantly, estradiol) in men. Excess estradiol in men can cause benign prostatic hyperplasia, gynecomastia, and symptoms of hypogonadism. Some athletes and body builders will also use anastrozole as a part of their steroid cycle to reduce and prevent symptoms of excess estrogens; in particular, gynecomastia and water retention.

Study data currently suggests that dosages of 0.5 mg to 1 mg a day reduce serum estradiol by about 50% in men, which differs from the typical reduction in postmenopausal women. However the reduction may be different for men with grossly elevated estradiol (clinical data is currently lacking).

Usage for children

This drug is frequently used in the treatment of children with growth disorder to stop or slow the onset of puberty. The cause of the growth disorder is through hormones which may trigger the early onset of puberty. At the onset of puberty the bone growth plates begin to close. This can occur in children as young as 5 years old, so for children severely behind in growth, the opportunity for increased growth is diminished. Arimidex is shown to slow or stop this process.

References

  1. ^ Details for Anastrozole
  2. ^ Howell A, Cuzick J, Baum M, et al. (2005). "Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial after completion of 5 years' adjuvant treatment for breast cancer". Lancet 365 (9453): 60–2. doi:10.1016/S0140-6736(04)17666-6. PMID 15639680. 
  3. ^ a b http://www.breastcancer.org/treatment/hormonal/new_research/20051003.jsp Review of: Arimidex After Two Years of Tamoxifen Reduces Recurrence in Post-Menopausal Women. R. Jakesz et al., The Lancet, August 6, 2005
  4. ^ Rejnmark L, Vestergaard P, Mosekilde L. Statin but not nonstatin lipid-lowering drugs decrease fracture risk: a nationwide case-control study. Calcif Tissue Int 2006; 79:27–36 [1]
  5. ^ Ewer MS, Glück S. A woman's heart: the impact of adjuvant endocrine therapy on cardiovascular health. Cancer. 2009 May 1;115(9):1813-26.
  6. ^ Lehrer, S. Statin use to prevent aromatase inhibitor-induced fracture and cardiovascular complications. Med Hypotheses. 2007;68(6)1417. Epub 2006 Dec 29.
  7. ^ R. Eastell. Risk factors for fracture: 5-year results of the 'arimidex' (anastrozole), tamoxifen, alone or in combination (ATAC) trial. 33rd European Calcified Tissue Symposium 2006. abstract OC008. Calcif Tissue Int (2006) 78(Suppl 1):S27.

External links

v • d • e
Sex hormones and related agents (primarily G03, also L02, H01C) – human endogenous in SMALL CAPS
#WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III

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