definition of equipoise

Definition of equipoise is a highly non-steroidal aromatase inhibitor – an enzyme, whereby in postmenopausal women androstenedione in peripheral tissues is converted into estrone and then to estradiol. Reduced levels of circulating estradiol in breast cancer patients has a therapeutic effect. In postmenopausal women,  in a daily dose 1 mg of estradiol levels causes a decrease of 80%.  Does not have progestogenic, androgenic and estrogenic activity. At daily doses up to 10 mg had no effect on the secretion of aldosterone and cortisol, therefore when using the drug definition of equipoise not required substitution corticosteroids.

Effect on bone mineral density has been shown that in patients with gormonopozitivnym early breast cancer in postmenopausal women who are taking definition of equipoise , changes in bone can be prevented in accordance with the standards established for the treatment of patients with a certain risk of fractures. Thus, the advantage definition of equipoise in combination with bisphosphonates (compared to treatment only drug Arimidex ® ) in patients with moderate and high risk of fractures has been demonstrated after 12 months in terms of bone mineral density, structural changes in the bone tissue and markers of bone resorption. Moreover, in the low risk changes were noted index of bone mineral density with treatment with one drug definition of equipoise and supportive treatment with vitamin D and calcium.

When therapy with definition of equipoise , including, when taken in combination with bisphosphonates, revealed no changes in plasma lipid levels.

Absorption definition of equipoise prompt, the maximum plasma concentration is reached within 2 hours after ingestion (fasting). Food slightly decreases the rate of absorption, but not its extent and does not result in a clinically significant effect on the equilibrium concentration of drug in plasma after a single reception of the daily dose of the drug Arimidex ® . After 7-day dosing is achieved approximately 90-95% of the equilibrium concentration in plasma definition of equipoise. Recorded definition of equipoise pharmacokinetic parameters depending on the time or dose not. The pharmacokinetics of definition of equipoise is independent of age in postmenopausal women.
The connection to plasma proteins -. 40%
of definition of equipoise is displayed slowly from the plasma elimination half-life is 40-50 hours. Extensively metabolized in postmenopausal women. Less than 10% of the dose is excreted in the urine unchanged within 72 hours after dosing.
The metabolism of definition of equipoise is carried out N-dealkylation, hydroxylation and glucuronidation. Metabolites are excreted primarily in the urine. Triazole, the major metabolite, determined in plasma, does not inhibit aromatase.
The clearance of definition of equipoise after oral intake in liver cirrhosis or renal dysfunction does not change.



  • Adjuvant treatment of postmenopausal breast cancer early gormonopolozhitelnogo.
  • Treatment of advanced breast cancer in postmenopausal women.
  • Adjuvant therapy gormonopolozhitelnogo early breast cancer in postmenopausal women after tamoxifen therapy for 2-3 years.Contraindications
  • Hypersensitivity to definition of equipoise or other components of the formulation
  • Pregnancy and lactation
  • In premenopausal women
  • Severe renal impairment (creatinine clearance less than 20 mL / min)
  • Moderate or severe hepatic impairment (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,Dosing and Administration
    Inside. Swallow the tablet whole 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 drug disease should be discontinued. In the adjuvant treatment of the recommended duration of treatment – 5 years. Impaired renal function: No dosage adjustment in patients with mild to moderate renal impairment is not required Violations of liver function: No dosage adjustment in patients with mild disorders liver function is not required.Side effects:
    The incidence was calculated from the number of adverse events observed in the phase III study in 9366 postmenopausal women with operable breast cancer treated for 5 years, with the incidence of adverse events in the control groups and the opinion of the investigator regarding the relationship of undesirable effects on study medication is not taken into account.
    Determination of the frequency of adverse reactions: very often (greater 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 rarely (less than 0.01%)From the circulatory system:
    very often – tides. On the part of the musculoskeletal system: very often – arthralgia / joint stiffness, arthritis often – bone pain infrequently – trigger finger. Reproductive system: often – dry vaginal mucosa;vaginal bleeding (mainly in the first weeks after the cancellation or change of previous hormonal therapy Arimidex ® ). Skin and skin appendages: very often – skin rash, often – thinning 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. On the part of the digestive system: very often – nausea, often – diarrhea, vomiting. On the part of the hepatobiliary system: often – increasing the activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, rarely – increased activity of gamma glutamyltransferase and concentrations 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). On the part of metabolism: often – anorexia, hypercholesterolemia. The drug can cause a reduction in bone mineral density due to snizheniemkontsentratsii circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures. Other: very often.

    describe individual clinical cases of accidental overdose. A single dose of the drug Arimidex ® , which could lead to the symptoms, life-threatening, has not been established.
    The specific antidote does not exist in the case of overdose, treatment should be symptomatic. It is possible to induce vomiting if the patient is conscious. Dialysis can be performed. Recommended general supportive therapy, monitoring patients and control the function of vital organs and systems.

    Interaction with other medicinal products and other forms of drug interaction
    studies for drug interactions with phenazone (antipyrine) and cimetidine indicate that the combined use of the drug Arimidex ® with other drugs are unlikely to bring a clinically significant drug interactions mediated by cytochrome P450.
    Clinically significant drug interaction while taking the drug Arimidex ® in conjunction with other commonly prescribed drugs available.
    at the moment, there are no data on the use of Arimidex drug ® in combination with other anticancer drugs.
    the drugs containing estrogen, reduces the pharmacological effect of Arimidex drug ® , and therefore, they are not shall be appointed at the same time with the drug Arimidex ® .
    it should appoint a drug tamoxifen concurrently with Arimidex ® , as it may weaken the pharmacological action of the latter.

    Special instructions:
    The safety and efficacy in children has not been established.
    Women with retseptorootritsatelnoy tumor estrogen efficacy of Arimidex 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.
    There are no data on the use of Arimidex drug ® in patients with moderate or severe hepatic impairment and in patients with severe renal insufficiency (creatinine clearance less than 20 ml / min).
    in the case of persistent uterine bleeding in patients receiving Arimidex drug ® needed consultation and supervision of the gynecologist.
    preparations containing estrogens should not be administered concurrently with the drug Arimidex ® , since these drugs will neutralize its pharmacological effect.
    By reducing the level of circulating estradiol, Arimidex ® can cause a reduction in bone mineral density with a consequent increase in fracture risk.
    Patients with such a high risk should be treated according to the Instructions on the treatment of data of complications.
    In patients with osteoporosis or with risk of osteoporosis, bone mineral density should be assessed by densitometry eg, DEXA scan (Dual-Energy X-ray absorptiometry – dual-energy X-ray absorptiometry) at the beginning of the treatment and in dynamics. If necessary, must be initiated to treat or prevent osteoporosis, under the close supervision of a physician.
    No data on the concomitant use of definition of equipoise and drug-analogues LHRH.
    Unknown improves whether definition of equipoise treatment results when used in conjunction with chemotherapy.
    The data on the safety of long-term treatment with definition of equipoise are not yet available.
    in applying the drug Arimidex ® more than tamoxifen observed ischemic disease, but the statistical significance is not observed.
    The efficacy and safety Arimidex drug ® and tamoxifen for their simultaneous use, regardless of hormone receptor status are comparable to those using a single tamoxifen. The exact mechanism for this phenomenon is not yet known.

    Effects on ability to drive and other machines
    Some side effects of the drug Arimidex ® , such as fatigue and drowsiness, may adversely affect the ability to perform potentially hazardous activities that require high concentration and speed of psychomotor reactions. In this connection, it is recommended with the appearance of these symptoms to be careful in the management of vehicles and mechanisms.

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