Arimidex 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.

Absorption

The absorption of Arimidex tablets after administration occurs very quickly,

The maximum plasma concentration time occurs in a period of 2 hours.

Distribution

Drug gets bound to the human plasma protein is Only 40%  .

Metabolism

The metabolism of Arimidex arises by;

Hydroxylation, Glucuronidation & N-Dealkylation

These three metabolites are recovered in urine.

Excretion

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.

Over dosage

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.

Side effects

Common side effects

Depression

Nausea

Vomiting

Rash

Osteoporosis

Fractures

Back pain

Insomnia

Pain

Arthralgia

Hypertension

Headache

Bone pain

Hot flushes

Asthenia

Arthritis

Peripheral edema

Cough

Dyspnea

Pharyngitis

Lymphoedema

If an adverse effect persists, discontinue the therapy.

For adjuvant therapy;

Like that, some variations like;

Accidental injury

Flu like syndrome

Chest pain

Neoplasm

Cyst

Vaginal hemorrhage

Vaginitis

Ischemic cardiac disease

Venous thromboembolic events

Deep venous thromboembolic events

Ischemic Cerebrovascular event

Vasodilatations

GI disorders

Hypercholesteremia

Leucorrhea

UTI

Breast pain

Vulvovaginitis

Infection

Endometrial cancer

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.

Contraindications

Arimidex tablets are contraindicated to following conditions

 pregnancy and premenopausal women, it may cause fetal harm.

Hypersensitivity reactions may occur;

Precautions

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.

Bone effects

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.

Cholesterol

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 20^oC to 25^oC (68^oF to 77^oF).

Protect the container away from heat, moisture & light.

Missed dose

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.