A selective nonsteroidal aromatase inhibitor. It has antitumor activity against estrogen-dependent breast tumors in postmenopausal women.
Limits the content of circulating estradiol. It does not have progestogenic, androgenic and estrogenic activity, does not affect the secretion of endogenous glucocorticosteroids (GCS) and mineralocorticoids (MCS).
Absorption is high (after oral administration 83 – 85% of the taken dose is absorbed), maximum concentration (Tcmah) 2 h. Binding to plasma proteins is 40%. About 90 – 95% of the steady plasma concentration is reached after 7 days of drug administration. There is no information about cumulation.
It is well metabolized in postmenopausal women. Metabolism is carried out in the process of N-dealkylation, hydroxylation and conjugation with glucuronic acid.
The main metabolite, triazole, determined in plasma and urine, does not inhibit aromatase. The elimination half-life (T1/2) is 50 hours. Metabolites are excreted mainly by the kidneys, less than 10% of the dose is excreted unchanged in the urine within 72 hours.
The clearance of anastrozole after oral administration in volunteers with stabilized cirrhosis or impaired renal function is not different from that determined in healthy volunteers.
Breast Cancer, Oncology
– Adjuvant therapy for early breast cancer, e hormone receptor positive in postmenopausal women, including after adjuvant therapy with tamoxifen for 2-3 years.
– First-line therapy for locally advanced or metastatic breast cancer with positive or unknown hormone receptors in postmenopausal women.
– Second-line therapy for advanced advanced breast cancer after tamoxifen treatment in postmenopausal women.
Position per tablet:
- Active ingredient:
Anastrozole 1.0 mg
Lactose monohydrate 65,0 mg
Microcrystalline cellulose 25,0 mg
Sodium carboxymethyl starch 5,0 mg
Hypromellose 3,0 mg
Magnesium stearate 1,0 mg
Weight of the tablet-core 100.0 mg
- film coating:
Aquarius Prime VAR218010 white 3.0 mg [hypromellose – 65 %, titanium dioxide -25 %, macrogol (polyethylene glycol) -10 %]
How to take, the dosage
To be taken by mouth at the same time, regardless of meals, 1 mg once a day. The tablet should be swallowed whole with water. The duration of treatment depends on the form and severity of the disease (for adjuvant therapy, the recommended duration of treatment is 5 years). If there are signs of disease progression the drug should be stopped.
Kidney function impairment: Dose adjustment in patients with mild to moderate renal impairment is not required. In patients with severe renal failure the drug should be used with caution.
Hepatic impairment: No dose adjustment is necessary in patients with mild to moderate hepatic impairment.
Studies on drug interactions with phenazone (Antipyrine) and warfarin indicate that co-administration of anastrozole with other drugs is unlikely to result in clinically significant cytochrome P450 (CYP)-mediated drug interactions.
The weak non-specific CYP inhibitor cimetidine has no effect on the plasma concentration of anastrozole. The effect of potent CYP inhibitors on anastrozole concentration is unknown.
The drugs containing estrogens reduce the pharmacological effect of anastrozole, and therefore they should not be administered simultaneously with anastrozole. Tamoxifen should not be prescribed concomitantly with anastrozole, because it may weaken the pharmacological effects of the latter. Currently, there is no information on the use of anastrozole in combination with other anticancer drugs.
In cases of doubt about a patient’s hormonal status, menopause should be confirmed by determination of serum sex hormones.
Oestrogen-containing medications should not be prescribed at the same time as anastrozole, as they would negate the pharmacological effects of anastrozole. The efficacy and safety of anastrozole and tamoxifen when used concomitantly, regardless of hormone receptor status, is comparable to that of tamoxifen alone. The exact mechanism of this phenomenon is not yet known.
In case of persistent uterine bleeding with anastrozole, a gynecologist should be consulted and monitored.
In reducing circulating estradiol levels, anastrozole may cause a decrease in bone mineral density.
In patients with osteoporosis or at risk of osteoporosis, bone mineral density should be evaluated by densitometry (e.g., a DEXA scan – dual-energy X-ray absorptiometry) at the start of treatment and over time. If necessary, treatment or prophylaxis for osteoporosis should be initiated under close medical supervision. To date there is insufficient data regarding the beneficial effects of bisphosphonates on anastrozole-induced loss of bone mineral density or their benefit when used for prophylaxis.
There are no data on concomitant use of anastrozole and gonadotropin-releasing hormone (GnRH) analogues.
It is not known whether anastrozole improves treatment outcomes when used together with chemotherapy.
Some side effects of anastrozole, such as asthenia and drowsiness, may adversely affect the ability to perform potentially hazardous activities requiring increased concentration and rapid psychomotor reactions. In this regard, it is recommended to be cautious while driving vehicles and mechanisms in case of appearance of these symptoms.
Hypersensitivity to anastrozole or other drug components, estrogen-dependent breast tumors in premenopausal women, severe hepatic insufficiency (safety and effectiveness not established), concomitant therapy with tamoxifen or drugs containing estrogens, childhood age (safety and effectiveness not established).
Osteoporosis, hypercholesterolemia, coronary heart disease (CHD), impaired liver function, severe renal failure (creatinine clearance (CK) less than 20 ml/min).
Additionally for dosage forms containing lactose: lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
The frequency of adverse reactions below was determined according to the following criteria: very common (at least 1/10); common (more than 1/100, less than 1/10); infrequent (more than 1/1000, less than 1/100); rare (more than 1/10000, less than 1/1000); very rare (less than 1/10000), including individual reports.
Vascular side: very common – “rushes” of blood to the face.
Skeletal, muscular and connective tissue disorders: very common – arthralgia/joint stiffness, arthritis; common – bone pain, myalgia; infrequent – trigger finger.
Genital organs and mammary glands: often – vaginal mucosal dryness, vaginal bleeding (mainly during the first weeks after cancellation or change of prior hormonal therapy to anastrozole).
Skin and subcutaneous tissue: very common – skin rash; common – thinning of hair, alopecia, allergic reactions; infrequent – urticaria; rare – erythema multiforme, anaphylactoid reaction, cutaneous vasculitis (including individual cases of purpura (Schoenlein-Genoch syndrome)); very rare Stevens-Johnson syndrome, angioedema.
Gastrointestinal tract: very common – nausea; common – diarrhea, vomiting.
Hepatic and biliary tract disorders: frequently – increased alkaline phosphatase, alanine aminotransferase (ALT), aspartate aminotransferase (ACT) activity; infrequently – increased gamma-glutamyl transferase activity and bilirubin concentration, hepatitis.
Nervous system disorders: very common – headache; common – somnolence, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease), sensory disorders (including paresthesia, loss or perversion of taste).
Metabolism and nutrition: often – anorexia, hypercholesterolemia; infrequently – hypercalcemia (e/without reducing the concentration of parathormone). Administration of the drug may cause decrease of bone mineral density due to decrease of circulating estradiol concentration, thereby increasing risk of osteoporosis and bone fractures.
General disorders: very common – mild to moderate asthenia.
Unwanted phenomena noted in clinical studies not related to anastrozole administration: anemia, constipation, dyspepsia, back pain, abdominal pain, increased blood pressure, weight gain, depression, insomnia, dizziness, anxiety, paresthesias.
A single dose of anastrozole that could lead to life-threatening symptoms has not been established.
2 years. Do not use the product after the expiration date printed on the package.
|Conditions of storage|
In a dry place protected from light at a temperature not exceeding 25 ° C. Store out of the reach of children.
Drug Technology, Russia
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