Anastrozol

Anastrozol Uses, Dosage, Side Effects, Food Interaction and all others data.

The growth of many cancers of the breast is stimulated or maintained by estrogens. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. The suppression of estrogen biosynthesis in peripheral tissues and in the cancer tissue itself can therefore be achieved by specifically inhibiting the aromatase enzyme.

Anastrozol is a selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.

Anastrozol prevents the conversion of adrenal androgens (e.g. testosterone) to estrogen in peripheral and tumour tissues. As the growth of many breast cancers is stimulated and/or maintained by the presence of estrogen, anastrozole helps to treat these cancers by decreasing the levels of circulating estrogens. Anastrozol has a relatively long duration of action allowing for once daily dosing - serum estradiol is reduced by approximately 70% within 24 hours of beginning therapy with 1mg once daily, and levels remain suppressed for up to 6 days following cessation of therapy.

The incidence of ischemic cardiovascular events was increased during anastrozole therapy and patients with pre-existing ischemic heart disease should consider the risks and benefits of anastrozole before beginning therapy. Anastrozol has also been reported to decrease spine and hip bone mineral density (BMD), so consideration should be given to monitoring of BMD in patients receiving long-term therapy.

Trade Name Anastrozol
Availability Prescription only
Generic Anastrozole
Anastrozole Other Names Anastrozol, Anastrozole
Related Drugs Arimidex, Ibrance, Femara, Aromasin, Faslodex, Verzenio, Afinitor, tamoxifen, Xeloda, Herceptin
Type
Formula C17H19N5
Weight Average: 293.3663
Monoisotopic: 293.164045633
Protein binding

Anastrozole is 40% protein bound in plasma and appears to be independent of plasma concentration.

Groups Approved, Investigational
Therapeutic Class Hormonal Chemotherapy
Manufacturer
Available Country Netherlands
Last Updated: September 19, 2023 at 7:00 am
Anastrozol
Anastrozol

Uses

Adjuvant treatment of post-menopausal women with hormone receptor-positive early breast cancer, and also advanced breast cancer in post-menopausal women. First-line treatment of hormone receptor-positive post-menopausal women who have received 2 to 3 years of adjuvant tamoxifen.

Anastrozol is also used to associated treatment for these conditions: Advanced Breast Cancer, Early Breast Cancer, Locally Advanced Breast Cancer (LABC), Metastatic Breast Cancer, Invasive, early Breast Cancer

How Anastrozol works

Anastrazole exerts its anti-estrogenic effects via selective and competitive inhibition of the aromatase enzyme found predominantly in the adrenal glands, liver, and fatty tissues. Many breast cancers are hormone receptor-positive, meaning their growth is stimulated and/or maintained by the presence of hormones such as estrogen or progesterone. In postmenopausal women, estrogen is primarily derived from the conversion of adrenally-produced androgens into estrogens by the aromatase enzyme - by competitively inhibiting the biosynthesis of estrogen at these enzymes, anastrozole effectively suppresses circulating estrogen levels and, subsequently, the growth of hormone receptor-positive tumours.

Dosage

Anastrozol dosage

Adults and elderly: 1 mg tablet to be taken orally once a day.

Side Effects

More common side effects are: Blurred vision chest pain or discomfort, dizziness, headache nervousness, pounding in the ears, shortness of breath, slow or fast heartbeat, swelling of the feet or lower legs

Toxicity

The reported oral TDLo in a human woman is 1.68 mg/kg given intermittently over the course of 12 weeks. Knowledge of the signs and symptoms of anastrozole overdose is incomplete as there are no documented descriptions of a patient receiving more than 60mg, a dose which was administered to a healthy male volunteer and was well-tolerated. There is no antidote for anastrozole and treatment should be supportive and symptomatic, including close monitoring of patient vital signs. As anastrozole exhibits relatively low protein binding, dialysis may be helpful and should be considered in select cases.

Precaution

There are no data to support the safe use of anastrozole in patients with moderate or severe hepatic impairment, or patients with severe impairment of renal function (creatinine clearance less than 20 mL/min). Women with osteoporosis or at risk of osteoporosis should have their bone mineral density at regular intervals monitored.

There are no data available for the use of anastrozole with LHRH analogues. This product contains lactose. Patients with rare hereditary problems of galactose intolerance, the lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Interaction

Antipyrine and cemetidine clinical interaction studies indicate that the co administration of anastrozole with other drugs is unlikely to result in clinically significant drug interactions mediated by cytochrome P450. Tamoxifen should not be co-administered with anastrozole as this may reduce its pharmacological action.

Food Interaction

  • Take with or without food. Co-administration with food reduces the rate, but not the overall extent, of absorption.

Anastrozol Cholesterol interaction

[Moderate] During a clinical trial, more patients receiving anastrozole were reported to have elevated serum cholesterol compared to patients receiving tamoxifen (9% versus 3.5%, respectively).

Caution should be taken when this agent is prescribed to these patients.

Volume of Distribution

The volume of distribution of anastrozole into brain tissue in mice is 3.19 mL/g. Distribution into the CNS is limited due to the activity of P-gp efflux pumps at the blood brain barrier, of which anastrozole is a substrate.

Elimination Route

Anastrozol is rapidly absorbed and Tmax is typically reached within 2 hours of dosing under fasted conditions. Coadministration with food reduces the rate but not the overall extent of absorption - mean Cmax decreased by 16% and the median Tmax was extended to 5 hours when anastrozole was administered 30 minutes after ingestion of food, though this relatively minor alteration in absorption kinetics is not expected to result in clinically significant effects.

Half Life

The elimination half-life of anastrozole is approximately 50 hours.

Clearance

Anastrozol's clearance is mainly via hepatic metabolism and can therefore be altered in patients with hepatic impairment - patients with stable hepatic cirrhosis exhibit an apparent oral clearance approximately 30% lower compared with patients with normal liver function. Conversely, renal impairment has a negligible effect on total drug clearance as the renal route is a relatively minor clearance pathway for anastrozole. In volunteers with severe renal impairment, renal clearance was reduced by 50% while total clearance was only reduced by approximately 10%.

Elimination Route

Hepatic metabolism accounts for approximately 85% of anastrozole elimination. Approximately 10% of the administered dosage is eliminated unchanged in the urine.

Pregnancy & Breastfeeding use

Anastrozol is contraindicated in pregnant and lactating women.

Contraindication

Patients with severe renal impairment (Creatinine clearance less than 20 mL/min), patients with moderate to severe hepatic disease and known hypersensitivity to anastrozole or to any of the excipients. Oestrozen-containing therapies should not be co-administered with anastrazole as they would negate its pharmacological action.

Special Warning

Renal impairment: No dose change is recommended in patients with mild or moderate renal impairment.

Hepatic impairment: No dose change is recommended in patients with mild hepatic impairment. For early disease, the recommended duration of treatment should be 5 years.

Acute Overdose

Clinical trials have been conducted with Anastrozol tablets, up to 60 mg in a single dose given to healthy male volunteers and up to 10 mg daily given to postmenopausal women with advanced breast cancer; these dosages were tolerated. A single dose of Anastrozol tablets that results in life-threatening symptoms has not been established. There is no specific antidote to overdosage and treatment must be symptomatic.

In the management of an overdose, consider that multiple agents may have been taken. Vomiting may be induced if the patient is alert. Dialysis may be helpful because Anastrozol tablet is not highly protein bound. General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated.

Storage Condition

Product should be stored within 30°C

Innovators Monograph

You find simplified version here Anastrozol

Anastrozol contains Anastrozole see full prescribing information from innovator Anastrozol Monograph, Anastrozol MSDS, Anastrozol FDA label

FAQ

What is Anastrozol used for?

Anastrozol is a medication used in addition to other treatments for breast cancer. Specifically it is used for hormone receptor-positive breast cancer. It has also been used to prevent breast cancer in those at high risk.

How safe is Anastrozol?

Anastrozol may cause or worsen osteoporosis. It can decrease the density of your bones and increase the chance of broken bones and fractures. Talk to your doctor about the risks of taking this medication and to find out what you can do to decrease these risks.

How does Anastrozol work?

Anastrozol works by lowering the levels of oestrogen hormones in your body.

What are the common side effects of Anastrozol?

Common side effects of Anastrozol are include:

  • weakness
  • headache
  • hot flashes
  • sweating
  • stomach pain
  • nausea
  • vomiting
  • loss of appetite
  • constipation
  • diarrhea
  • heartburn
  • weight gain
  • joint, bone, or muscle pain
  • breast pain
  • mood changes
  • depression
  • difficulty falling asleep or staying asleep
  • nervousness
  • dizziness
  • vaginal bleeding
  • vaginal dryness or irritation
  • pain, burning, or tingling in the hands or feet
  • dry mouth
  • hair thinning

Is Anastrozol safe during pregnancy?

Anastrozol is used mainly in women after menopause. If you have not gone through menopause, this medication must not be used during pregnancy. It may harm an unborn baby.

Is Anastrozol safe during breastfeeding?

Anastrozol is not recommended when pregnant or breastfeeding, because it interferes with hormone levels in you and your baby.

Can I drink alcohol with Anastrozol?

It's best to avoid or limit alcohol intake when using breast cancer medications like Anastrozol. Alcohol can raise your risk of experiencing side effects from Anastrozol, such as hot flashes or joint pain.

Can I drive after taking Anastrozol?

Do not drive, ride a bike or operate machinery if you feel very tired while taking Anastrozol.

What time of day is best to take Anastrozol?

You may take Anastrozol at whatever time of day you find easiest to remember, but try to take your doses at the same time each day.

Who should not take Anastrozol?

You should not use Anastrozol if you are allergic to it, or if you have not yet completed menopause.
Anastrozol is not approved for use in men or children. You should not take Anastrozol if you also take tamoxifen.

Can I take Anastrozol on an empty stomach?

It is usually taken once a day with or without food.

How often can I take Anastrozol ?

Anastrozol is taken as a tablet once a day. It's best to take it at the same time every day.

How long does Anastrozol take to work?

Anastrozol works quickly to lower estrogen and some side effects start within 24 hours of starting.

How long does Anastrozol stay in your system?

The half life of Anastrozol is 30 to 60 hours. Generally it takes four to five half-lives for a drug to be eliminated from the body, so in the case of Anastrozol this would be 150 to 300 hours, or six to 12 days.

How many years should Anastrozol be taken?

This will depend on your individual circumstances, but Anastrozol is usually taken for five to ten years.

What happens if I miss a dose?

Take the Anastrozol as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

Is Anastrozol toxic?

This Anastrozol can cause liver toxicity, which your doctor will monitor for using blood tests called liver function tests.

Can Anastrozol affect my eyesight?

Based on analysis of OCT retinal thickness data, it is likely that Anastrozol increases the tractional force between the vitreous and retina.

Does Anastrozol affect the heart?

The aromatase inhibitor Anastrozol has been linked to heart attacks and other cardiovascular events.

Does Anastrozol damage the liver?

Liver injury attributed to Anastrozol is usually mild and self-limited, typically a transient, asymptomatic elevation in serum enzymes.

Can Anastrozol affect my kidneys?

Renal dysfunction was considered to be a rare complication of Anastrozol. Patients who are prescribed Anastrozol should be watched carefully for the development of renal dysfunction.

What happens if I overdose of Anastrozol?

Anastrozol may cause your cholesterol levels to rise. Higher cholesterol levels put you at increased risk of heart disease.

How does Anastrozol make me feel?

Anastrozol can sometimes cause headaches, nausea and vomiting.

Can Anastrozol cause memory loss?

A pattern of decline in working memory and concentration with initial exposure to Anastrozol was observed.

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*** Taking medicines without doctor's advice can cause long-term problems.
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