Arimidex, 1 mg, film-coated tablets, 28 pcs.

pharmachologic effect

The medicine has an antitumor effect. It is based on the ability of anastrozole to suppress the synthesis of female sex hormones, primarily estradiol.

Reducing estradiol has a therapeutic effect in patients with breast cancer. At a daily dose of 1 mg causes a reduction of 80%.

In daily doses of up to 10 mg, it does not affect the secretion of cortisol and aldosterone. This means that the use of Arimidex does not require additional administration of corticosteroids.

The drug does not have progestogenic, androgenic and estrogenic activity.

Release form and composition

Arimidex is available as a round, white, biconvex tablet with an engraving on both sides (“A” on one side and “Adx” and “1” as a fraction on the other).

One tablet contains 1 mg of anastrozole (active component) and excipients (povidone, lactose monohydrate, magnesium stearate, carbosimethylene starch and purified water). The Arimidex shell contains hypromellose, macrogol 300, titanium dioxide and purified water.

The tablets are packaged in blisters of 14 pieces. There are two blisters in one cardboard box.

Pharmacodynamics of the drug

During the postmenopausal period, androstenedione is the main source of female sex hormones. In peripheral tissues, it goes through a series of biochemical reactions, turning directly into estrone and then into estradiol. These transformations occur with the direct participation of the aromatase enzyme, which blocks the active substance of the drug Arimidex.

Reducing aromatase activity significantly reduces the amount of estradiol produced in peripheral tissues (primarily adipose tissue). This has a positive effect on the course of hormone-positive breast cancer.

Arimidex oral tablets

Instructions for medical use of the drug

Description of pharmacological action

Highly selectively inhibits aromatase, an enzyme that converts androstenedione in peripheral tissues into estrone and then into estradiol in postmenopausal women. Reducing circulating estradiol levels in breast cancer patients has a therapeutic effect. In postmenopausal women, Arimidex at a daily dose of 1 mg causes a decrease in estradiol levels by 80%. Arimidex does not have progestogenic, androgenic and estrogenic activity. Arimidex in daily doses of up to 10 mg has no effect on the secretion of cortisol and aldosterone; therefore, corticosteroid replacement is not required when using Arimidex.

Indications for use

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

Release form

film-coated tablets 1 mg; blister 14, cardboard pack 2;

Pharmacokinetics

Absorption of anastrozole is rapid, Cmax in plasma is achieved within 2 hours after oral administration (on an empty stomach). Food slightly reduces the rate of absorption, but not its extent, and does not lead to a clinically significant effect on the steady-state plasma concentration of the drug with a single daily dose of Arimidex. After 7 days of taking the drug, approximately 90–95% of the steady-state concentration of anastrozole in plasma is achieved. 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 and has not been studied in children. Binding to blood plasma proteins is 40%. Anastrozole is excreted slowly, T1/2 - 40–50 hours. It is 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 is metabolized by N-dealkylation, hydroxylation and glucuronidation. Metabolites are excreted primarily in the urine. Triazole, the main metabolite detected in plasma, does not inhibit aromatase. The clearance of anastrozole after oral administration in patients with liver cirrhosis or impaired renal function does not change.

Use during pregnancy

Contraindicated. Breastfeeding should be stopped during treatment.

Contraindications for use

- hypersensitivity to anastrozole or other components of the drug; - in premenopausal women; - severe renal failure (creatinine Cl less than 20 ml/min); - moderate or severe liver failure (safety and effectiveness have not been established); - concomitant therapy with tamoxifen; - pregnancy; - period of breastfeeding; - children's age (safety and effectiveness in children have not been established).

Side effects

Determination of the frequency of adverse reactions: very often (>10%); often (from 1 to 10%); rarely (from 0.1 to 1%); very rarely ( From the vascular system: very often - flushing of the face. From the musculoskeletal system: often - arthralgia. From the reproductive system: often - vaginal dryness; rarely - vaginal bleeding (mainly during the first weeks after withdrawal or changing previous hormonal therapy to Arimidex). From the skin and skin appendages: often - thinning hair, skin rash; very rarely - erythema multiforme (Stevens-Johnson syndrome). From the digestive system: often - nausea, diarrhea; rarely - anorexia , vomiting, increased activity of gamma-glutamine transferase and alkaline phosphatase. From the nervous system: often - headache; carpal tunnel syndrome (mainly observed in patients with risk factors for this disease); rarely - drowsiness. From the metabolic side: rarely - hypercholesterolemia. Taking the drug may cause a decrease in bone mineral density due to a decrease in circulating estradiol levels, thereby increasing the risk of osteoporosis and bone fractures. Other: often - asthenia; very rarely - allergic reactions, including angioedema, urticaria and anaphylactic shock.

Directions for use and doses

Inside. Swallow the tablet whole with water; at the same time. Adults (including the elderly) - 1 mg 1 time per day (long term). If signs of disease progression appear, the drug should be discontinued. As adjuvant therapy, the recommended duration of treatment is 5 years. In patients with mild to moderate renal impairment, as well as mild liver dysfunction, no dose adjustment is required.

Overdose

Isolated clinical cases of drug overdose have been described. A single dose of Arimidex that could lead to life-threatening symptoms has not been established. There is no specific antidote. Treatment: symptomatic therapy. Vomiting can be induced if the patient is conscious. Dialysis is possible. General supportive therapy, patient monitoring and monitoring of vital organs and systems are recommended.

Interactions with other drugs

Drug interaction studies with antipyrine and cimetidine indicate that coadministration of Arimidex with other drugs is unlikely to result in clinically significant drug interactions mediated by cytochrome P450. There are no clinically significant drug interactions 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 anticancer drugs. Preparations containing estrogens reduce the pharmacological effect of Arimidex, and therefore they should not be prescribed simultaneously with Arimidex. Tamoxifen should not be prescribed simultaneously with Arimidex, as it may weaken the pharmacological effect of the latter.

Special instructions for use

Safety and effectiveness in children have not been established. In women with estrogen receptor-negative tumors, the effectiveness of Arimidex has not been demonstrated unless there has been a previous positive clinical response to tamoxifen. If there is doubt about the patient's hormonal status, menopause should be confirmed by determining sex hormones in the blood serum. There is no data on the use of Arimidex in patients with severe liver dysfunction or in patients with severe renal impairment (Cl creatinine). In case of persistent uterine bleeding while taking Arimidex, consultation and observation of a gynecologist is necessary. Preparations containing estrogens should not be prescribed simultaneously with Arimidex , since these drugs will neutralize its pharmacological effect. By reducing the level of circulating estradiol, Arimidex can cause a decrease in bone mineral density. In patients suffering from osteoporosis or at risk of developing osteoporosis, bone mineral density should be assessed by densitometry (for example, DEXA- scanning) at the beginning of treatment and over time. If necessary, treatment or prevention of osteoporosis should be started under the close supervision of a physician. There is no data on the simultaneous use of anastrozole and LHRH analogue drugs (luteinizing hormone releasing hormone). It is not known whether anastrozole improves treatment results when combined use with chemotherapy. 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. Some side effects of Arimidex, such as asthenia and drowsiness, may negatively affect the ability to perform potentially hazardous activities that require increased concentration and speed of psychomotor reactions. In this regard, it is recommended to exercise caution when operating vehicles and machinery when these symptoms appear.

Storage conditions

At a temperature not exceeding 30 °C. Keep out of the reach of children.

Best before date

60 months

ATX classification:

L Antineoplastic drugs and immunomodulators

L02 Antitumor hormonal drugs

L02B Hormone antagonists and their analogues

L02BG Enzyme inhibitors

L02BG03 Anastrozole

Indications for use

Arimidex tablets are used to treat breast cancer. Indications for the use of this drug are:

• As an adjuvant (additional) in the treatment of early hormone-positive cancer affecting the mammary gland in postmenopausal women.
• Treatment of advanced breast cancer in postmenopausal women.
• As an additional treatment for early hormone-positive breast cancer in postmenopausal women as a replacement for Tamoxifen (in situations where treatment with the drug lasted 2–3 years).

Also, at their own risk, Arimidex, like Tamoxifen, is used by bodybuilders during (as well as after) a course of anabolic steroids.

Analogues substitutes

There are a number of analogues of substitutes for the drug Arimidex, which can be found in pharmacies at a more affordable price:

• Acastrol;
• Anaster;
• Aromasin;
• Letrozole;
• Mammozol;
• Texlo;
• Femara.

Photo gallery of analogues:

Femara

Akastrol

Anastera Aromasin Letrozole

They have the same group, pharmacological action and indications for use, but before replacing Arimidex, it is better to get a doctor’s advice.

Contraindications

Arimidex should not be used in the following situations:

• If you are hypersensitive to anastrozole or other substances contained in Arimidex tablets.
• During premenopause.
• In case of severe renal failure, with a glomerular filtration rate of less than 20 ml/min.
• In case of severe as well as moderate liver failure, since there are no studies in favor of the safety of the drug.
• If you are treated with medications containing female sex hormones.
• During pregnancy and breastfeeding.
• In childhood.

Arimidex is prescribed with caution for: osteoporosis, coronary heart disease, lactase deficiency, hypercholesterolemia, liver dysfunction, glucose-galactose malabsorption.

Method of use and dosage of Arimidex

The tablets are intended for oral use. They are swallowed whole, without chewing, and washed down with water. It is recommended to take Arimidex at the same time every day.

Adult patients are prescribed one tablet (1 mg) once a day. If the disease progresses, then use of Arimidex should be discontinued. The recommended duration of treatment with the drug (as an auxiliary drug therapy) is 5 years.

Patients with mild liver dysfunction do not require dose adjustment. Patients with moderate to mild renal failure also do not require dose adjustment.

Side effects

Like any other antitumor drug, the drug has side effects, including:

• Feeling of blood rushing to the skin of the face.
• Pain and a feeling of stiffness in the joints, arthritis often develops, and there are complaints of pain in the bones.
• Vaginal dryness is considered one of the most common adverse effects. Vaginal bleeding is also common, especially in the first weeks after discontinuation or after replacing the previous drug with Arimidex tablets.
• Rash, thinning and hair loss, allergic reactions: from skin rashes to angioedema and Stevens-Johnson syndrome (which, however, is extremely rare).
• From the digestive system: nausea is the most common concern, vomiting and diarrhea are somewhat less common.
• From the liver and gallbladder: increased activity of liver enzymes in the blood plasma, increased bilirubin levels, drug-induced hepatitis.
• Headache, carpal tunnel syndrome (especially in patients with a predisposition to this pathology), drowsiness, asthenia.
• Increased cholesterol levels in the blood plasma, anorexia, decreased bone mineralization, which increases the risk of fractures.

Side effects and consequences

More than 80% of patients taking Arimidex are susceptible to adverse reactions, which are divided into rare, common, very common, infrequent and very rare.

So we are talking about such manifestations:

• arthritis and joint pain;
• vaginal bleeding, discharge or dryness of the vaginal mucosa;
• skin rashes and scabies;
• hives;
• vomiting, nausea and diarrhea;
• hepatitis;
• migraines, fatigue and weakness;
• anorexia, metabolic disorder;

This is not the entire list of side effects from taking Arimidex tablets, since it all depends on the dosage, the body’s reaction and the age of the patient.

You should inform your doctor about the appearance of symptoms, especially if they do not go away for more than five days. Then the course can be changed, canceled, and the drug Arimidex can be replaced with another.

Compatibility with other drugs

The interaction of Arimidex and other drugs has not been studied enough. It is known for sure that drugs containing female sex hormones reduce the effectiveness of this antitumor drug, and therefore should not be prescribed along with it. The simultaneous use of Arimidex and Tamoxifen is also not recommended, since the latter can weaken the pharmacological effect of anastrozole.

Drug interaction studies with antipyrine and cimetidine indicate that concomitant use of Arimidex with other drugs is unlikely to result in clinically significant drug interactions mediated by 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 anticancer drugs. There is no precise data on the effect of alcohol on the action of Arimidex. Considering the ability of ethyl alcohol to reduce the effectiveness of a number of medications, it is strongly recommended to avoid drinking alcohol during the treatment period.

Drug interactions

According to studies that were carried out using a combination of Arimidex tablets and antipyrine, the drug can be used with most other medications without harm to the body or the occurrence of allergies or adverse reactions.

The only thing you need to be careful with is other anticancer drugs and estrogen-containing ones, which may reduce the effectiveness of Arimidex tablets.

The same prohibition applies to tamoxifen, since taking it together reduces results, can cause allergies and increase the burden on the body.

special instructions

The drug is ineffective for tumors that are insensitive to estrogen (except in cases where there was a positive response to previous therapy with Tamoxifen).

In cases where there are doubts about the patient's hormonal status, the level of female sex hormones should be determined in a laboratory. Arimidex is used only in case of the onset of the postmenopausal period.

It is important to consider that a decrease in estradiol levels during treatment with this drug may lead to osteoporosis and an increased risk of fractures. It is necessary to monitor bone density while taking the drug.

Medicines containing female sex hormones should not be taken simultaneously with Arimidex. Otherwise, you should not count on any effect from treatment with an antitumor drug.

Pharmacokinetics

Suction

After oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is achieved within 2 hours (on an empty stomach). Food slightly reduces the rate, but not the extent of absorption. Small changes in the rate of absorption do not lead to a clinically significant effect on Css of the drug in plasma when taking 1 tablet daily. Arimidex.

Distribution

Anastrozole is 40% bound to plasma proteins. Approximately 90-95% of Css is achieved after 7 days of taking the drug. There is no information about the accumulation of the drug and the dependence of the pharmacokinetic parameters of anastrozole on time and dose.

Metabolism

Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronidation. Triazole, the main metabolite detected in plasma, does not inhibit aromatase.

Removal

Anastrozole is excreted slowly, T1/2 is 40-50 hours.

Anastrozole and its metabolites are excreted mainly in the urine (less than 10% of the excreted dose unchanged) within 72 hours after taking the drug.

Pharmacokinetics in special clinical situations

The determined clearance of anastrozole after oral administration in volunteers with stable liver cirrhosis or impaired renal function does not differ from the clearance determined in healthy volunteers.

The pharmacokinetics of anastrozole does not depend on age in postmenopausal women.

Reviews and recommendations from doctors and patients

Arimidex is an effective and fairly safe drug used for additional therapy for hormone-positive breast cancer. The drug does not have androgenic activity and does not affect the secretion of aldosterone and cortisol, which means that during treatment there is no need for steroid hormone replacement therapy.

The effectiveness of the drug has been proven both by numerous clinical trials and by the experience of specialists actively using Arimidex. In most cases, this drug is well tolerated and has slightly fewer side effects than other drugs used to treat breast cancer.

Attention!

This information does not constitute official instructions for use of the drug. Here, for your information, the main characteristics of the drug "Arimidex" are described. Before purchasing and using the medicine, consult your doctor and read the official instructions.

Analogues of the drug according to ATC codes:

ANASTROZOL-TEVA VERO-ANASTROZOL MAMMOSOL EGISTRAZOL

Before using ARIMIDEX you should consult your doctor. These instructions for use are for informational purposes only. For more complete information, please refer to the manufacturer's instructions.

Features of good stagnation

Zagalni

Arimidex should not be used in premenopausal women. Menopausa MAH BUTI PIDARENENTS BIOKHIMICHY DOSLIDEN (RIVNI LUTHINIIZUUCHOU HRMON [LH], Folikulostimuluyuy Hormone [FSG] TA/Abo ESTRADIOLA) in the time of the Menopausal status of the pathetic. Daily data on the combination of Arimidex with analogues of luteinizing hormone releasing factor (RLH).

A trace of the uniqueness of one-hour administration of tamoxifen or methods that replace estrogen with the drug Arimidex, which may reduce its pharmacological action (section “Interactions with other medicinal agents and other and types of interactions" and "Pharmacological power").

Pouring on the mineral strength of brushes

Arimidex fragments reduce the level of circulating estrogen, which can lead to a decrease in the mineral strength of the brushes with a possible increased risk of fracture (section “Adverse reactions”).

In women suffering from osteoporosis or at risk of osteoporosis, the mineral density of the cysts should be assessed at the beginning of the bath and at regular intervals after bathing. If necessary, treat or prevent osteoporosis and carefully take care of the patient's figure. Ingestion of specific medications, such as bisphosphonates, may further deplete the mineral strength of the brushes caused by Arimidex in postmenopausal women, and then assess the effectiveness of such ingestion (div. or “Adverse reactions”).

Impaired liver function

Arimidex has not been administered to patients with breast cancer and those with death or severely impaired liver function. In patients with impaired liver function, exposure to anastrozole may be increased (section “Pharmacological implications”); Administration of Arimidex to patients with moderate or severely impaired liver function requires caution (section “Method of administration and dosage”). Treatment should be based on an assessment of the joint function of the cortex and the risk of the skin surrounding the patient.

Impaired function of the nirok

The use of Arimidex in patients with breast cancer and severely impaired breast function has not been studied. Exposure to anastrozole does not increase in patients with severely impaired neuronal function (glomerular filtration rate [GFR] < 30 ml/xv, section “Pharmacological influences”); Administration of Arimidex to patients with severely impaired function should be carried out with care (section “Method of administration and dosage”).

Children

Arimidex is not indicated for use in children; however, for this group of patients, safety and effectiveness have not been established.

For boys with growth hormone deficiency, Arimidex should not be used as a supplement to growth hormone treatment. In basic clinical follow-up, efficacy has not been demonstrated and safety has not been established. Since anastrozole reduces estradiol levels, Arimidex should not be used in girls with growth hormone deficiency as a supplement to growth hormone treatment. Every day, daily precautions are taken to ensure the safety of children.

Hypersensitive to lactose

The drug eliminates lactose. Patients with rare seizure disorders, such as galactose intolerance, Lapp lactase deficiency or impaired absorption of glucose-galactose, should not take this medication.

Suspension during pregnancy or breastfeeding.

Data about the use of Arimidex for vaginal women every day. Studies on animals have demonstrated reproductive toxicity. Arimidex contraindications during pregnancy (section “Contraindications”).

Data on the use of Arimidex during lactation every day. Arimidex contraindications during breastfeeding (section “Contraindications”).

Fertility

The effects of Arimidex on human fertility have not been studied. Studies on animals have demonstrated reproductive toxicity.

This is due to the fluidity of the reaction during treatment with vehicles or other mechanisms.

Arimidex does not or may have an insignificant effect on the production of ceruvate by transport means or by other mechanisms. However, if you are aware of episodes of asthenia and drowsiness associated with taking Arimidex, you should be careful when using transport means or using other mechanisms to avoid such symptoms and.

Side effects

Table 3 presents the adverse reactions that were monitored during clinical and follow-up studies or those that appeared to be spontaneous. Unless otherwise specified, frequency categories were allocated based on the number of adverse reactions observed in a large phase III study of 9366 postmenopausal women with operable breast cancer. vines that delayed adjuvant therapy for five years (Arimidex study, Tamoxifen, Alone or in Combination [ATAC]).

The lower adverse reactions are classified according to frequency and organ system classes (OSC). Classification by frequency was carried out according to the following criteria: very often (≥1/10), often (from ≥1/100 to <1/10), infrequently (from ≥1/1000 to <1/100), rarely (from ≥1 /10000 to <1/1000) and even more rarely (<1/10000). The most frequently reported side effects were: headache, hot flashes, tiredness, viscera, arthralgia, loss of joint mobility, arthritis and asthenia.

Table 3

*The incidence of carpal tunnel syndrome was higher in patients weaning off Arimidex during clinical follow-up, equal to that in patients weaning off tamoxifen. However, most of these episodes occurred in patients with significant risk factors for the development of the disease.

**Fragments in the pre-investigated ATAC cases of cutaneous vasculitis and Henoch-Schönlein purpura were not observed, the frequency of these manifestations may be rare (ranging from ≥0.01% to <0.1%) based on the highest point value prices.

***Vaginal bleeding occurred frequently, mainly in patients with advanced breast cancer within the first few hours after replacing hormonal therapy with treatment with the drug Arimidex. If bleeding continues, keep the pads away.

Table 4 presents the frequency of early significant adverse reactions during the ATAS follow-up (follow-up period with a median of 68 months), regardless of the reasons for their occurrence, which were observed in patients who suffered from continue to follow-up therapy for up to 14 days after treatment.

Table 4

Frequency of the most significant adverse reactions in the studied ATAS

At the Groups of ARIMIDEKS, Tamoxifen Taksosten was instructed by the Kilki-fracture: 22 to 1000 Patziynto-Rokriv TA 15 per 1000 Patzindok-Rokіv vidpovo (perioode is the storage of 68 Mysyatsiv). Fracture rates in the Arimidex group were similar to those observed in postmenopausal thyroid cancer patients. The incidence of osteoporosis was 10.5% in patients treated with Arimidex, and 7.3% in patients treated with tamoxifen.

It has not been established whether the incidence of fractures and the incidence of osteoporosis were observed in the study ATAS in patients who took Arimidex, the protective effect of tamoxifen, the specific effect of Arimidex, or the offensive effect.

Information about suspected adverse reactions

Information about suspected adverse reactions after drug registration is important. This makes it possible to continue monitoring the risk of drug withdrawal/congestion. Please contact medical professionals to report any suspected adverse reactions.