Arimidex, 1 mg, 28 pcs

AstraZeneca, Great Britain

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$37
Arimidex, 1 mg, 28 pcs
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Product Overview

Composition

Active substances:

anastrozole 1 mg.

Excipients:

lactose monohydrate,

povidone

sodium carboxymethylene starch,

magnesium stearate,

purified water.

Shell composition:

macrogol 300, hypromellose, titanium dioxide, purified water.

pharmachologic effect

Arimidex is a highly selective non-steroidal aromatase inhibitor, an enzyme with which in postmenopausal women, androstenedione in peripheral tissues is converted to estrone and then to estradiol. Reducing the level of circulating estradiol in patients with breast cancer has a therapeutic effect. In postmenopausal women, a daily dose of 1 mg causes a decrease in estradiol by 80%.
 
The drug does not have progestogen, androgenic and estrogenic activity. The drug in daily doses up to. 10 mg has no effect on the secretion of cortisol and aldosterone, therefore, when using the drug, corticosteroid replacement is not required. Effect on bone mineral density.
 
It is shown that in patients with hormone-positive early breast cancer in postmenopausal women who are taking the drug, changes in the skeletal system can be prevented in accordance with the standards established for the treatment of patients with a certain risk of fractures.
 
Thus, the advantage of the drug in combination with bisphosphonates (as compared to therapy with Arimidex alone) in patients with medium and high risk of fractures was demonstrated after 12 months in terms of mineral bone density, structural change in 'bone tissue' and markers of bone resorption. Moreover, in the low-risk group, there was no change in the indicator of mineral bone density during therapy with one, with the drug and with the supportive treatment with vitamin D and calcium. Lipids.
 
During drug therapy, including when taken in combination with bisphosphonates; no changes in plasma lipid levels were detected.
 
Pharmacokinetics
 
Anastrozole absorption is fast, the maximum concentration in plasma is reached within 2 hours after ingestion (on an empty stomach). Food slightly reduces the rate of absorption, but not its degree and does not lead to a clinically significant effect on the equilibrium concentration of the drug in plasma with a single dose of the drug.
 
After a 7-day administration of the drug, approximately 90-95% of the equilibrium plasma concentration of anastrozole is reached. There is no information on the dependence of the pharmacokinetic parameters of anastrozole on time or dose. The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women. Communication with blood plasma proteins - 40%.
 
Anastrozole is excreted slowly, the half-life from plasma is 40-50 hours. Extensively metabolized in postmenopausal women. Less than 10% of the dose is excreted unchanged in the urine within 72 hours after taking the drug. Anastrozole metabolism is carried out by N-dealkylation, hydroxylation and glucuronidation.
 
Metabolites are excreted mainly in urine. Triazole, a major plasma metabolite, does not inhibit aromatase. The clearance of anastrozole after oral administration with cirrhosis of the liver or impaired renal function does not change.

Indications

  • Adjuvant therapy for early hormone-positive breast cancer in postmenopausal women;
  • treatment of advanced breast cancer in postmenopausal women;
  • adjuvant therapy of early hormone-positive breast cancer in postmenopausal women after tamoxifen therapy for 2-3 years.

Pregnancy and lactation

The drug is contraindicated in pregnancy and lactation (breastfeeding).

Contraindications

Hypersensitivity to anastrozole or other components of the drug.
 
Pregnancy and lactation. In premenopausal women.
 
Severe renal failure (creatinine clearance less than 20 ml / min)
 
Moderate or severe liver failure (safety and efficacy not established).
 
Concomitant therapy with tamoxifen or drugs containing estrogens.
 
Children's age (safety and efficacy in children not established).

Side effects

From the reproductive system: often - dryness of the vaginal mucosa; vaginal bleeding (mainly during the first weeks after cancellation or change of previous hormone therapy to Arimidex®).
 
On the part of the skin and skin appendages: very often - a skin rash; often - thinning of the hair (alopecia), allergic reactions; infrequently - urticaria; rarely - erythema multiforme, anaphylactoid reaction, skin vasculitis (including isolated cases of purpura (Shenlein-Genoch syndrome)); very rarely - Stevens-Johnson syndrome, angioedema.
 
From the digestive system: very often - nausea; often - diarrhea, vomiting.
 
From the hepatobiliary system: often - increased activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; infrequently - increased activity of gamma-glutamyl transferase and bilirubin concentration, hepatitis.
 
From the nervous system: very often - headache; often - drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease).
 
From the side of metabolism: often - anorexia, hypercholesterolemia. Taking the drug can cause a decrease in bone mineral density due to a decrease in the concentration of circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures.
 
From the vascular system: very often - hot flashes.
 
From the musculoskeletal system: very often - arthralgia / stiffness of joints, arthritis; often - bone pain; infrequently - trigger finger.
 
Other: very often - asthenia of mild or moderate severity.

Interaction

Clinical studies on drug interactions with antipyrine and cimetidine indicate that co-administration of Arimidex with other drugs is unlikely to lead to a clinically significant interaction due to cytochrome P450.

There is no clinically significant drug interaction when taking Arimidex simultaneously with other commonly prescribed drugs.

At the moment, there is no information on the use of Arimidex in combination with other antitumor drugs.

Drugs containing estrogens should not be prescribed simultaneously with Arimidex, because they reduce the pharmacological effect of the latter.

Tamoxifen should not be prescribed simultaneously with Arimidex, since it can weaken the pharmacological effect of the latter.

How to take, course of administration and dosage

For adults, including elderly patients, the drug is prescribed 1 mg orally 1 time / day, for a long time. If signs of disease progression appear, the drug should be discontinued. As adjuvant therapy, the recommended treatment duration is 5 years.

Patients with mild to moderate impaired renal function do not require dose adjustment.

Patients with mild hepatic impairment do not require dose adjustment.

The tablet should be swallowed whole and washed down with water. It is recommended to take the drug at the same time of day.

Overdose

Isolated clinical cases of accidental overdose of the drug are described.
 
A single dose of the drug, which could lead to life-threatening symptoms, has not been established.
 
There is no specific antidote; in case of an overdose, treatment should be symptomatic.
 
You can induce vomiting if the patient is conscious. Dialysis may be performed.
 
General supportive therapy, patient monitoring, and monitoring the function of vital organs and systems are recommended.

Special instructions

In women with an estrogen receptor-negative tumor, the efficacy of Arimidex has not been demonstrated, unless there has been a previous positive clinical response to tamoxifen.

In case of doubt about the hormonal status of the patient, menopause should be confirmed by the determination of sex hormones in the blood serum.

There is no data on the safety of Arimidex in patients with severe hepatic impairment or in patients with severe renal failure (CC less than 20 ml / min).

In the case of persistent uterine bleeding while taking Arimidex, consultation and observation by a gynecologist is necessary.

Drugs containing estrogen should not be prescribed at the same time as Arimidex.

By decreasing the level of circulating estradiol, Arimidex can cause a decrease in bone mineral density.

In patients with osteoporosis or at risk of developing osteoporosis, bone mineral density should be evaluated by densiometry (e.g., DEXA scanning) at the beginning of treatment and in dynamics. If necessary, treatment or prevention of osteoporosis should be initiated under the close supervision of a physician.

There is no data on the simultaneous use of anastrozole and GnRH analogues.

It is not known whether anastrozole improves treatment outcomes when used together with chemotherapy.

Safety data for long-term treatment with anastrozole has not yet been obtained.

When using Arimidex more often than with tamoxifen therapy, ischemic diseases were observed, but no statistical significance was noted.

The effectiveness and safety of Arimidex and tamoxifen when used simultaneously, regardless of the status of hormonal receptors, are comparable to those when using tamoxifen alone. The exact mechanism of this phenomenon is not yet known.

Pediatric Use

Safety and efficacy of the drug in children have not been established.

Influence on the ability to drive vehicles and other mechanisms requiring increased concentration of attention

Some side effects of Arimidex, such as asthenia and drowsiness, can adversely affect the ability to perform work that requires an increased concentration of attention and speed of psychomotor reactions. In this regard, it is recommended that when these symptoms appear, caution is required when driving or moving machinery.

Release form

Coated tablets

Storage conditions

At a temperature not exceeding 30 ° C

Shelf life

5 years

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