Anastrozole-TL
Anastrozole-TL: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Anastrozole-TL
ATX code: L02BG03
Active ingredient: anastrozole (Anastrozole)
Manufacturer: Technology of drugs, LLC (Russia); R-Pharm, JSC (Russia)
Description and photo update: 2019-10-07
Anastrozole-TL is an antineoplastic drug used to treat breast cancer in postmenopausal women.
Release form and composition
Dosage form - film-coated tablets: white, round, biconvex, engraved with "H" on one side and "1" - on the other side; the core of the tablet is from almost white to white (28 or 30 tablets in a jar, in a cardboard box 1 can; 7 tablets in a blister, in a cardboard box 1 or 4 packs; 10 tablets in a blister, in a cardboard box 1 or 3 packs, 14 tablets in blisters, in a cardboard box 1 or 2. Each pack also contains instructions for the use of Anastrozole-TL).
Composition of 1 tablet:
- active substance: anastrozole - 1 mg;
- auxiliary components: lactose monohydrate - 65 mg; sodium carboxymethyl starch - 5 mg; microcrystalline cellulose - 25 mg; magnesium stearate - 1 mg; hypromellose - 3 mg;
- film shell: white Aquarius Prime BAP218010 [titanium dioxide - 25%; hypromellose - 65%; polyethylene glycol (macrogol) - 10%] - 3 mg.
Pharmacological properties
Pharmacodynamics
Anastrozole - the active substance of Anastrozole-TL, is a selective non-steroidal aromatase inhibitor. In postmenopausal women, it has antitumor activity against estrogen-dependent breast tumors. Reduces the amount of circulating estradiol. It does not possess androgenic, progestogenic and estrogenic activity, it does not affect the secretion of endogenous glucocorticosteroids and mineralocorticoids.
Pharmacokinetics
Anastrozole is absorbed quickly, the maximum plasma concentration after oral administration on an empty stomach is reached in about 2 hours. Food has an insignificant effect on the rate of absorption, reducing it, but not changing its degree, which does not lead to a clinically significant effect on the equilibrium plasma concentration of anastrozole with a single daily dose. Anastrozole reaches 90–95% of the equilibrium plasma concentration after about 7 days of therapy.
There are no data on the dependence of the pharmacokinetic parameters of the substance on the dose or time of administration. The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women; pharmacokinetic parameters have not been studied in children.
Anastrozole binds to blood plasma proteins at a level of 40%. The elimination of the substance is carried out slowly, the half-life from plasma is in the range from 40 to 50 hours. In postmenopausal women, the substance is extensively metabolized. Less than 10% of the dose is excreted unchanged by the kidneys within 72 hours after taking Anastrozole-TL.
The main metabolic pathways of anastrozole are N-dealkylation, hydroxylation and glucuronidation. Excretion of metabolites is carried out mainly by the kidneys. The main metabolite detected in plasma, triazole, does not inhibit aromatase.
With cirrhosis of the liver or impaired renal function, the clearance of anastrozole after oral administration does not change.
Indications for use
Anastrozole-TL is prescribed for postmenopausal women to treat the following diseases:
- early breast cancer with positive hormone receptors: adjuvant therapy, including after 2–3 years of adjuvant therapy with tamoxifen;
- locally advanced or metastatic breast cancer with unknown or positive hormone receptors: first line of therapy;
- advanced breast cancer that progresses after tamoxifen: second line of therapy.
Contraindications
Absolute:
- severe renal failure (in patients with creatinine clearance <20 ml / min);
- severe liver failure;
- estrogen-dependent breast tumors during premenopause;
- combined use with tamoxifen or estrogen-containing drugs;
- period of premenopause;
- age up to 18 years;
- pregnancy and lactation;
- individual intolerance to the components of the drug.
Relative (Anastrozole-TL tablets are used under medical supervision):
- hypercholesterolemia;
- osteoporosis;
- lactase deficiency, galactose intolerance, glucose-galactose malabsorption;
- cardiac ischemia.
Anastrozole-TL, instructions for use: method and dosage
Anastrozole-TL is taken orally, regardless of food intake, at the same time, once a day. The tablet must be swallowed whole with water.
The recommended daily dose is 1 mg. The duration of the course is determined by the severity and form of the disease (when used as an adjuvant therapy - 5 years).
If signs appear, indicating the progression of the disease, the administration of Anastrozole-TL is canceled.
Side effects
Possible adverse reactions [> 10% - very common; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <0.01% - very rare)]:
- musculoskeletal and connective tissue: very common - arthritis, arthralgia / joint stiffness; often - myalgia, bone pain; infrequently - trigger finger;
- vessels: very often - redness of the face, rush of blood to the head;
- liver and biliary tract: often - increased activity of alkaline phosphatase, aspartate aminotransferase, alanine aminotransferase; infrequently - an increase in the concentration of bilirubin and the activity of gamma-glutamyl transferase, hepatitis;
- nervous system: very often - headache; often - drowsiness, impaired sensitivity (including paresthesia, perversion or loss of taste), carpal tunnel syndrome (observed mainly in the presence of risk factors for the disease);
- digestive system: very often - nausea; often - vomiting, diarrhea;
- skin and subcutaneous tissue: very often - skin rash; often - allergic reactions, alopecia, hair thinning; infrequently - urticaria; rarely - anaphylactoid reactions, erythema multiforme, cutaneous vasculitis (including isolated cases of purpura - Shenlein-Genoch syndrome); very rarely - angioedema, Stevens-Johnson syndrome;
- genitals and mammary gland: often - vaginal bleeding, dryness of the vaginal mucosa (as a rule, during the first weeks after canceling or changing the previous hormonal treatment to Anastrozole-TL);
- metabolism: often - hypercholesterolemia, anorexia; infrequently - hypercalcemia (with or without a decrease in the concentration of parathyroid hormone); a decrease in bone mineral density is possible (associated with a decrease in the concentration of circulating estradiol, against which the likelihood of osteoporosis and bone fractures increases);
- general disorders: very often - mild or moderate asthenia.
Disorders, the development of which was noted during the period of clinical trials, but not associated with the use of Anastrozole-TL: insomnia, paresthesia, anxiety, dizziness, constipation, anemia, dyspepsia, abdominal pain, back pain, increased blood pressure, weight gain, depression.
Overdose
The size of a single dose of Anastrozole-TL that could lead to life-threatening symptoms has not been established.
Therapy: symptomatic and supportive (including induction of vomiting, dialysis). Treatment should be carried out under the control of the function of vital organs and systems. There is no specific antidote.
special instructions
The efficacy of Anastrozole-TL in receptor-negative tumors to estrogens has not been demonstrated unless there has been a prior positive response to tamoxifen.
If there is any doubt about the hormonal status of the patient, menopause should be confirmed by determining the sex hormones in the blood serum.
In cases where uterine bleeding persists against the background of therapy, consultation and supervision of a gynecologist is necessary.
Drugs containing estrogens should not be prescribed simultaneously with Anastrozole-TL, since this will result in a significant decrease in the therapeutic effect of the latter. Anastrozole against the background of a decrease in the concentration of circulating estradiol can lead to a decrease in bone mineral density.
In osteoporosis or at risk of osteoporosis, bone mineral density should be assessed by densitometry, for example, using dual-energy X-ray absorptiometry (DEXA scan) at the beginning of therapy and over time.
If necessary, under the close supervision of a physician, treatment or prevention of osteoporosis is carried out. There is currently no sufficient information regarding the positive effect of bisphosphonates on the loss of bone mineral density associated with the intake of anastrozole, or their benefits when used prophylactically.
There is no information on the combined use of Anastrozole-TL with drugs - analogues of gonadotropin-releasing hormone.
It has not been established whether the results of treatment improve against the background of the simultaneous use of Anastrozole-TL and chemotherapy drugs.
Safety data for long-term use of the drug have not yet been obtained.
In cases where anastrozole was used more often than with tamoxifen treatment, the development of ischemic diseases was observed, with no clinical significance. Regardless of the status of hormonal receptors, the safety and efficacy of anastrozole and tamoxifen when used in combination are comparable to those when treated with tamoxifen alone. The exact mechanism of this phenomenon is currently unknown.
Influence on the ability to drive vehicles and complex mechanisms
In the event of some side effects of Anastrozole-TL, including asthenia and drowsiness, caution should be exercised when driving.
Application during pregnancy and lactation
Anastrozole-TL is not prescribed during pregnancy / lactation.
Pediatric use
The efficacy and safety of the use of Anastrozole-TL tablets in pediatric patients has not been established, therefore, the use of the drug is contraindicated under the age of 18 years.
With impaired renal function
Patients with creatinine clearance below 20 ml / min (with severe renal failure) are not prescribed Anastrozole-TL.
For violations of liver function
In severe hepatic impairment, Anastrozole-TL is not prescribed.
Drug interactions
According to the results of a study on drug interactions with warfarin and phenazone (Antipyrin), with the combined use of anastrozole with other drugs, clinically significant drug interactions mediated by cytochrome P 450 should not be expected.
Cimetidine (a weak nonspecific inhibitor of cytochrome P 450) does not change the plasma concentration of anastrozole. The degree of influence of powerful inhibitors of cytochrome P 450 on this indicator has not been established.
Medicines containing estrogens reduce the pharmacological effect of anastrozole, therefore, their simultaneous administration is not recommended. Tamoxifen should not be prescribed in combination with anastrozole, since this may lead to a weakening of the pharmacological action of the latter.
There are currently no data on the use of anastrozole in combination with other anticancer drugs.
Analogs
Anastrozole-TL analogs are Anazalez, AXASTROL, Anamasten, Anastrozole, Anastera, Arimidex, Anastreks, Egistrazole, Selana.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Anastrozole-TL
In reviews of Anastrozole-TL, the patients repeatedly point to the low therapeutic effect of the drug in comparison with analogues. Also, the development of pronounced side effects, such as nausea, vomiting, severe joint pain, is often noted. However, it is impossible to reliably establish the connection between their appearance and the quality of the medicinal product.
Anastrozole-TL is included in the “List of Medicines with Federal Benefit” and can be obtained free of charge, which is its significant advantage.
Price for Anastrozole-TL in pharmacies
Approximate price for Anastrozole-TL, 1 mg film-coated tablets, 28 pcs. in the package is 990 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
