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ARIMIDEX (anastrozole) tablets for oral administration contain 1 mg of anastrozole, a non-steroidal aromatase inhibitor. It is chemically described as 1,3-Benzenediacetonitrile, a, a, a’, a’-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl). Its molecular formula is C17H19N5 and its structural formula is:
ARIMIDEX® (anastrozole) Structural Formula Illustration
Anastrozole is an off-white powder with a molecular weight of 293.4. Anastrozole has moderate aqueous solubility (0.5 mg/mL at 25°C); solubility is independent of pH in the physiological range. Anastrozole is freely soluble in methanol, acetone, ethanol, and tetrahydrofuran, and very soluble in acetonitrile.
Arimidex (anastrozole) is a non-steroidal aromatase inhibitor used to treat breast cancer in postmenopausal women. It is often given to women whose cancer has progressed even after taking tamoxifen (Nolvadex, Soltamox). Arimidex is available in generic form. Common side effects of Arimidex include constipation, diarrhea, nausea, vomiting, upset stomach, loss of appetite, body aches and pains (back pain, bone pain, joint pain or stiffness), breast swelling/tenderness/pain, headache, dry mouth, scratchy or sore throat, increased cough, dizziness, trouble sleeping (insomnia), tiredness/weakness, flushing and sweating (hot flashes/hot flushes), vaginal bleeding, hair thinning, weight changes, depression, mood changes, problems with your fingers while gripping, or numbness, tingling, cold feeling, or weakness in your hand or wrist.
Important Safety Information About ARIMIDEX
Prescription ARIMIDEX is only for postmenopausal women. ARIMIDEX should not be taken if you are pregnant because it may harm your unborn child. Do not take ARIMIDEX if you are allergic to any of its ingredients
Based on information from a study in patients with early breast cancer, women with a history of blockages in heart arteries (ischemic heart disease) who take ARIMIDEX may have a slight increase in this type of heart disease compared to similar patients who take tamoxifen
ARIMIDEX can cause bone softening/weakening (osteoporosis) increasing the chance of fractures. In a clinical study in early breast cancer, there were more fractures (including fractures of the spine, hip, and wrist) with ARIMIDEX (10%) than with tamoxifen (7%)
In a clinical study in early breast cancer, some patients taking ARIMIDEX had an increase in cholesterol. Skin reactions, allergic reactions, and changes in blood tests of liver function have also been reported.
Arimidex is not a steroid. It is a tablet form anti-aromitase that is used by many body builders to help prevent bloating (edema) and Gynecomastia (bitch tit) associated with the use of testosterone and androgens. It can be used in place of Nolvadex, Clomid, etc. Bodybuilders are using around .25mg to 1mg per day or .5mg to 1mg every other day and are having good success with it. The FDA approved uses are for the treatment of breast cancer in post-menopausal women with disease progression following tamoxifen therapy. Hypersensitivity to anastrozole are reasons not to use this drug. If you have these problems please inform your doctor. Common side effects are: shortness of breath, dizziness, diarrhea, vomiting, headache, hat flashes, weakness, cough, dry mouth, skin rash, sweating, abdominal pain and bone pain. Some less common symptoms are vaginal bleeding, weight gain, tiredness, chills, fever, breast pain, and itching. In case of an overdose, it is recommended to contact your poison control center. Anastrozole (Arimidex) is the aromatase inhibitor of choice. The drug is appropriately used when using substantial amounts of aromatizing steroids, or when one is prone to gynecomastia and using moderate amounts of such steroids. Arimidex does not have the side effects of aminoglutethimide (Cytadren) and can achieve a high degree of estrogen blockade, much moreso than Cytadren. It is possible to reduce estrogen too much with Arimidex, and for this reason blood tests, or less preferably salivary tests, should be taken after the first week of use to determine if the dosing is correct. As an aromatase inhibitor, Arimidex’s mechanism of action — blocking conversion of aromatizable steroids to estrogen — is in contrast to the mechanism of action of anti-estrogens such as clomiphene (Clomid) or tamoxifen (Nolvadex), which block estrogen receptors in some tissues, and activate estrogen receptors in others. During a cycle, if using Arimidex, there is generally no need to use Clomid as well, but (as mentioned in the section on Clomid) there may still be benefits to doing so.With moderate doses of testosterone 0,5mg/day is usually sufficient and in some cases may be too much.
In the early breast cancer clinical trial, the most common side effects seen with ARIMIDEX include hot flashes, joint symptoms (including arthritis and arthralgia), weakness, mood changes, pain, back pain, sore throat, nausea and vomiting, rash, depression, high blood pressure, osteoporosis, fractures, swelling of arms/legs, insomnia, and headache
In advanced breast cancer trials, the most common side effects seen with ARIMIDEX versus tamoxifen include hot flashes, nausea, decreased energy and weakness, pain, back pain, headache, bone pain, increased cough, shortness of breath, sore throat, and swelling of arms and legs. Joint pain/stiffness has been reported in association with the use of ARIMIDEX
ARIMIDEX should not be taken with tamoxifen or estrogen-containing therapies.