Arimidex Tab n / a film about 1mg 28 pc

Description

Composition
Active substance:
1.0 mg anastrozole.
Excipients:
Lactose monohydrate 93.0 mg Povidone 2.0 mg Sodium carboxymethyl starch 3.0 mg Magnesium stearate 1.0 mg membrane shell composition: 1.50 mg of hypromellose, Macrogol 300 0.30 mg titanium dioxide 0.45 mg.
Description:
Round, biconvex tablets of white color, covered with a foil envelope with an engraving.
Product form:
Tablets, coated membrane shell 1 mg. 14 tablets in blister Al / PVC; 2 blisters with instructions for use in a cardboard bundle from the first control opening.
Contraindications
Hypersensitivity to anastrozole or other components of the formulation
Pregnancy and breast-feeding
In premenopausal women
Renal failure (less than 20 ml / min creatinine clearance)
Moderate or severe hepatic insufficiency (safety and efficacy not established)
Concomitant therapy with tamoxifen or medicines that contain estrogen
Children’s age (safety and efficacy in children has not been established)
Precautions: osteoporosis, hypercholesterolemia, coronary heart disease, liver dysfunction, lactase deficiency, glucose-galactose malabsorption.
Dosage
1 mg
Indications
Adjuvant treatment of early breast cancer, hormone receptor-positive postmenopausal women, including after adjuvant tamoxifen therapy for 2-3 years.
First-line treatment of locally advanced or metastatic breast cancer with positive or unknown hormone receptor in postmenopausal women.
Second line therapy for advanced breast cancer progressing after treatment with tamoxifen, in postmenopausal women.
Interaction with other drugs
Research on drug interactions with phenazone (antipyrine) and cimetidine indicate that the combined use of the drug Arimideks® with other drugs is unlikely to result in clinically significant drug interactions mediated by cytochrome P450.
No clinically significant drug interactions when receiving Arimideks® drug simultaneously with other commonly prescribed drugs available.
At the moment, there are no data on the use of Arimideks® drug in combination with other anticancer drugs.
Preparations containing estrogen, reduces the pharmacological action of the drug Arimideks®, and therefore, they should not be administered concurrently with the drug Arimideks®.
Tamoxifen should not be administered concurrently with the drug Arimideks® because it can weaken the pharmacological action of the latter.
Overdose
We describe isolated clinical cases of accidental overdosing. A single dose of the drug Arimideks®, which could lead to the symptoms of life-threatening, is not installed.
There is no specific antidote in case of overdose treatment should be symptomatic. Can induce vomiting, if the patient is conscious. Dialysis can be performed. It recommended general supportive therapy, monitoring of patients and control the function of vital organs and systems.
pharmachologic effect
Pharmacological group:
The antitumor agent, an inhibitor of estrogen synthesis.
Pharmacodynamics:
Arimideks® is highly selective nonsteroidal aromatase inhibitor – an enzyme, whereby in postmenopausal women androstenedione in peripheral tissues is converted into estrone and then to estradiol. Reducing circulating estradiol levels in patients with breast cancer has a therapeutic effect. In postmenopausal women Arimideks® in a daily dose 1 mg of estradiol levels causes a decrease of 80%.
Arimideks® not have progestogenic, androgenic and estrogenic activity.
Arimideks® at daily doses up to 10 mg of an effect on cortisol secretion of aldosterone and hence the application of the preparation does not require Arimideks® substitutive corticosteroids.
Effect on bone mineral density
It has been shown that patients with gormonopozitivnym postmenopausal breast cancer early, which take Arimideks®, bone changes 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 Arimideks® in combination with bisphosphonates (compared to drug therapy only Arimideks®) patients with medium or high risk of fractures has been demonstrated after 12 months on parameters of bone mineral density, structural changes in bone markers and bone resorption. Moreover, in the low risk changes were noted index of bone mineral density in single-drug therapy and supportive treatment Arimideks® vitamin D and calcium.
Lipids
When therapy with Arimideks®, including, at a reception in combination with bisphosphonates have been identified changes in lipid levels in plasma.
Pharmacokinetics:
Anastrozole rapid absorption, the maximum plasma concentration is reached within 2 hours after ingestion (fasting). Food slightly reduces the rate of absorption, but not its extent and does not lead to clinically meaningful effect on the equilibrium concentration of drug in plasma after a single reception Arimideks® daily dose of the drug. After 7-day dosing is achieved approximately 90-95% of the equilibrium concentration in plasma anastrozole. Information about the dependence of anastrozole pharmacokinetic parameters of time or dose not.
The pharmacokinetics of anastrozole is independent of age in postmenopausal women.
Communication with plasma proteins – 40%.
Anastrozole appears slowly, plasma half-life is 40-50 hours. Extensively metabolised in postmenopausal women. Less than 10% of the dose excreted in the urine unchanged within 72 hours after ingestion. Metabolism anastrozole carried N-dealkylation, hydroxylation and glucuronidation. Metabolites derived predominantly in the urine. Triazole, the major metabolite determined in plasma, does not inhibit aromatase.
Clearance anastrozole after oral administration of liver cirrhosis or renal dysfunction is not changed.
Conditions of supply of pharmacies
On prescription.
side effects
The incidence was calculated from the number of adverse events observed in the phase III study in 9,366 women with breast cancer in postmenopausal women with operable cancer treated for 5 years, with the incidence of adverse events in comparison groups, and according to the researchers regarding the relationship of undesirable effects on the test the drug is not taken into account.
Determination of the frequency of adverse reactions: very often (more than or equal to 10%); often (from 1 to less than 10%); infrequently (less than 0.1 to 1%); rare (0.01 to less than 0.1%); very rare (less than 0.01%).
On the part of the vessels: very often – “tides”.
On the part of the musculoskeletal and connective tissue disorders: very often – arthralgia / joint stiffness, arthritis, often – bone pain, myalgia, rarely – trigger finger.
On the part of genitals and mammary gland: often – dry vaginal mucosa; vaginal bleeding (mainly during the first weeks after discontinuation of, or a change in the previous hormonal therapy Arimideks®).
Skin and subcutaneous tissue disorders: very often – skin rash, often – thinning of hair (alopecia), allergic reactions, rarely – urticaria, rarely – erythema multiforme, anaphylactoid reactions, cutaneous vasculitis (including isolated cases of purpura (Henoch-Henoch syndrome)) very rarely – Stevens-Johnson syndrome, angioedema.
Gastro-intestinal tract: often – nausea, often – diarrhea, vomiting.
Of the liver and biliary tract: often – increase in activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, infrequently – increasing the activity of gamma-glutamyltransferase and concentration of bilirubin, hepatitis.
From the nervous system: very often – headache, often – drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease), sensory disturbances (including paraesthesia, loss or distortion of taste).
On the part of metabolism and nutrition: often – anorexia, hypercholesterolemia, rarely – hypercalcemia (with / without an increase in parathyroid hormone concentration). The drug can cause a reduction in bone mineral density due to reduced circulating estradiol concentrations, thereby increasing the risk of osteoporosis and bone fractures.
General disorders: very often – asthenia, mild or moderate in severity.
Adverse events reported in clinical trials, is not associated with taking the drug Arimideks®: anemia, constipation, indigestion, back pain, abdominal pain, increased blood pressure, weight gain, depression, insomnia, dizziness, anxiety, paresthesia.
special instructions
Safety and efficacy in children has not been established.
In women with estrogen retseptorootritsatelnoy tumor efficacy Arimideks® the drug has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen.
In case of doubt in the hormonal status of the patient menopause must be confirmed by the definition of sex hormones in the blood serum.
No data are available for the preparation Arimideks® in patients with moderate to severe hepatic insufficiency and in patients with severe renal failure (creatinine clearance less than 20 mL / min).
In the case of persistent uterine bleeding in patients receiving the drug Arimideks® need advice and supervision of the gynecologist.
Preparations containing estrogens should not be administered concurrently with the drug Arimideks®, as these drugs will neutralize its pharmacological effect.
By reducing the level of circulating oestradiol Arimideks® may cause a reduction in bone mineral density with a consequent increase in fracture risk. Patients with a high risk to be treated according to the Instructions on the treatment of these complications.
In patients suffering from osteoporosis or at risk of osteoporosis, bone mineral density should be evaluated by densitometry, e.g., DEXA scans (Dual-Energy X-ray Absorptiometry – dual energy X-ray absorptiometry), at the beginning of the treatment and in dynamics. If necessary, should start the treatment or prevention of osteoporosis, under the close supervision of a physician.
No data on the concomitant use of anastrozole and LHRH analogues medications.
It is unknown whether anastrozole treatment improves results when used in conjunction with chemotherapy.
Safety data in long-term treatment with anastrozole are not yet available.
In applying the drug Arimideks® more often than tamoxifen, ischemic disease were observed, but no statistical significance observed in this case.
The efficacy and safety of the drug and tamoxifen Arimideks® at their simultaneous use, regardless of hormone receptor status comparable with those using a tamoxifen. The exact mechanism for this phenomenon is not yet known.
Effects on ability to drive and use other mechanisms
Some side effects of the drug Arimideks®, such as fatigue and drowsiness, may adversely affect the ability to perform potentially hazardous activities that require high concentration and psychomotor speed reactions. In this context it recommended for these symptoms to be careful when driving and mechanisms.
Storage conditions
The temperature is not above 30 ° C, out of reach of children.
Dosing and Administration
Inside. Swallow tablet entirely with water. It is recommended to take the drug at the same time.
Adults, including the elderly: 1 mg orally 1 time a day for a long time. If signs of progression of the disease taking the drug should be discontinued.
In the adjuvant treatment of the recommended duration of treatment – 5 years.
Renal impairment: dose adjustment in patients with mild to moderate renal impairment is not required.
Abnormal liver function: a dose adjustment in patients with mild hepatic dysfunction is not required.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist