Arimidex (Anastrozole 1mg)
Drug profile of Arimidex
Arimidex is classified as an Aromatase inhibitor. Arimidex is non-steroidal prohibitor of estrogen synthesis
Arimidex is belongs to third generation of Aromatase inhibitor, which specifically binds to and feasibly prohibits the Aromatase, a CYP 450 enzyme occurred in many tissues along with ovary, liver, & breast
Arimidex is used in the treatment of estrogen receptor positive breast cancer
Arimidex indicated for
Arimidex is indicated for treatment of breast cancer in postmenopausal women.
Pharmacological action of Arimidex
Anastrozole selectively prohibits aromatase. The main source of circulating estrogen (primarily estradiol) is changes of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues. Hence, aromatase prevention causes to a reduce in serum and tumor concentration of estrogen, leading to a reduced tumor mass or delayed progression of tumor development in some women. Anastrozole has no detectable effect on combination of adrenal corticosteroids, aldosterone, and thyroid hormone.
The absorption of Arimidex tablets after administration occurs very quickly,
The maximum plasma concentration time occurs in a period of 2 hours.
Drug gets bound to the human plasma protein is Only 40% .
The metabolism of Arimidex arises by;
Hydroxylation, Glucuronidation & N-Dealkylation
These three metabolites are recovered in urine.
Nearly 85% of drug is eliminated through hepatic metabolism.
Eliminated 10% in urine
The half-life period of Arimidex is 50 hours.
Dosage regimens and administration of Arimidex
The recommended dose of Arimidex is one tablet 1mg should be taken orally as a single dose.
In metastatic breast cancer condition, the dose should be resumed until disease advancement.
In ATAC (Arimidex, tamoxifen, alone or in combination treatment), the dose of Arimidex should be followed for 5 years.
The drug Arimidex can be taken with or without food.
In specific populations:
In renal & hepatic damaged patients
For mild & moderate renal impaired patients, dosage adjustment is not allowed.
In severe condition, the usage of Arimidex should be in caution.
For mild or moderate hepatic impaired patients, dosage adjustment should not be suggested
In severe condition, use with caution.
The maximum dose of Arimidex is 10mg should be given to post-menopausal women with metastatic breast cancer. No special antidote is preferred, therapy should be symptomatic. Signs and symptoms associated to the over dosage of Arimidex should be monitored. Provide general supportive measures to the patients who are suffered with over dosage of Arimidex.
Common side effects
If an adverse effect persists, discontinue the therapy.
For adjuvant therapy;
Like that, some variations like;
Flu like syndrome
Ischemic cardiac disease
Venous thromboembolic events
Deep venous thromboembolic events
Ischemic Cerebrovascular event
Drug- drug interaction
- Combination of tamoxifen with Arimidex causes depletion in plasma concentration of Arimidex by 27%. This co administration did not affect the pharmacokinetic of tamoxifen ad its metabolites. Based on ATAC trials, this combination should be discontinued.
- Concomitant use of Arimidex with warfarin, causes increasing in bleeding effects. To avoid this problem patient must be examine with prothrombin time and INR value.
- Interaction of Arimidex with cytochrome 450 enzymes, causes prevention of CYP450
- Arimidex tablets should not be used in combination with drugs containing estrogens, leads to reduce the pharmacological actions.
Arimidex tablets are contraindicated to following conditions
pregnancy and premenopausal women, it may cause fetal harm.
Hypersensitivity reactions may occur;
Ischemic cardiovascular events
The drug will lead to high incidence of ischemic cardiovascular events in women with preexisting ischemic heart disease; use only if benefits greatly outweigh risks.
During Arimidex therapy, patient may suffer with diminishing the lumbar spine & total hip bone mineral density levels.
This condition is occurring at high range in tamoxifen therapy, to reduce this adverse patient may frequently examined with bone mineral density.
Increase serum cholesterol resulted; check closely; use with caution in patients with hyperlipidemias; check and regulate cholesterol levels with current guidelines for patients with LDL elevations.
Allow no clinical advantages to premenopausal women with breast cancer
Pregnancy and lactation
Pregnancy category of Arimidex X
Arimidex tablets are not used in pregnancy and lactating period because it may cause fetal death.
Storage and handling
Arimidex tablets stored between 20oC to 25oC (68oF to 77oF).
Protect the container away from heat, moisture & light.
If patients missed a dose, then have the dose before next dose reaches or the missed dose should be skipped and follow the regular dosing schedule.
If missed dose happens, must consult with practiced medical oncologist and follow the instructions.
- Trade name Arimidex
- Substance Anastrozole 1mg
- Manufacturer AstraZeneca
- Packaging 28 tablets
- Country of origin India