Anastrazole is sold under the brand name Arimidex which evacuate its activity by prohibiting Aromatase enzyme Arimidex is belongs to non-steroidal Aromatase inhibitor. Arimidex which indicated to diminshes the estrogen formation by preventing Aromatase, an enzyme responsible for transformation of androgen into estrogen Arimidex tablet is a prescription drug which is used under the supervission of medical oncologist
First line therapy:
Arimidex is used for the treatment of first line therapy in post menopausal women who are acquire positive receptor or hormone receptor locally progressive or metastatic breast carcinoma
Second line therapy:
Arimidex is used for the treatment of second line therapy in patients possess advanced breast cancer, in post menopausal women with cancer development consequently tamoxifen therapy. The drug also used for the treatment of Patients with hormone receptor negative disorder or patient who are not reacting to tamoxifen treatment periodically reacted to Arimidex tablets.
The normal dose of Arimidex tablet is given 1mg should be administered as a single dose by taken with or without food In renal impairment patients or for elderly patients no dose adjustments required in mild to moderate hepatic impairment condition no dose adjustment takes place . Arimidex should be maintained until disease improvement In the condition of metastatic breast cancer, Arimidex should be followed for five years in ATAC trials
The time to maximum plasma concentration reaches within 2 hours. Arimidex tablet administrating with food will reduce the rate but not all the time of anastrazole absorption
The bounding of human plasma protein is Arimidex is occurred at 40%
Arimidex tablet metabolism is arising through;
N-Dealkylation, hydroxylation and Glucuronidation
The metabolites of anastrazole are;
• A glucoronide conjugate of hydroxyl anastrazole
• A glucoronide conjugate of anastrazole
• Triazole-major circulating metabolite which has poor pharmacological activity
Anastrazole eliminated in feces and urine of Nearly 85% In Renal metabolism: 10% total clearance half life period of Arimidex tablet is 50 hours
Mechanism of action :
Anastrazole essentially inhibits Aromatase, that is an enzyme included in converting of circulating estrogen to estrone through adrenally advanced androstenedione by Aromatase in peripheral tissues Hence the prevention of Aromatase leads to reduce in serum and tumor aggregation of estrogen, successive to reduce malignant lump or passive improvement of cancer development.
If not concomitant use in Estrogen therapy with Arimidex tablet which may cause depletion of its pharmacological activity Warfarin interaction with anastrazole, it did not alter the anti-coagulant effect While concomitant use of tamoxifen with Arimidex leads to reduce the serum concentration of anastrazole by 27% it concluded as CYP-450 prohibition , the drug Anastrazole will chance the effect of other drugs
Blood related effects:
Lymph edema, anemia
Metabolism: Peripheral edema, weight gain, hypercholesterolemia
Musculoskeletal: Arthritis, arthralgia, osteoporosis, fracture, bone pain, arthrosis, joint pain, Myalgia
Nervous: Depression, insomnia, dizziness, anxiety, paresthesia
Respiratory:Pharyngitis, cough increased, dyspnea, sinusitis, bronchitis
Skin: Rashes, sweating.
Whole body: headache , pain, back pain, , abdominal pain, infection, injury, flu like syndrome, chest pain, Asthenia, neoplasm, cyst
Cardiovascular: Vasodilatation, hypertension
Digestive: Nausea, constipation, diarrhea, dyspepsia, GI disorders
Eye: Cataract specified
Urogenital: vaginitis , vulvovaginitis , Leucorrhea, urinary tract infection, breast pain, breast neoplasm, , vaginal hemorrhage,
Arimidex tablets may arises the plasma cholesterol range corresponds to the patient getting tamoxifen
In ischemic cardiovascular action:
There is a chance of high proportion of ischemic cardiovascular effects while administrating Arimidex tablets. Arimidex treatment getting patients may have chance to produce diminish in total hip bone mineral density and lumbar spine density.
Pregnancy category of anastrazole: X For pregnant women or women who are become pregnant and breast feeding mothers, Arimidex tablets should not be recommended If administrating the Arimidex tablets in pregnancy condition, it may affect to fetal harm even to death
stored at between 20oC to 25oC (68oF to 77oF) controlled room temperature Protect the carton away from heat, moisture, and light
If patient who are missed to take the dose of Arimidex, should consult doctor as soon as possible. Arimidex is a single dose therapy
Or the missed dose should be skipped and follow the next dosing schedule Do not take double time a day
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