|Arimidex 1 mg|
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Pharmacological action of Arimidex
Highly selective non-steroidal aromatase inhibitor. Aromatase is an enzyme by which, in postmenopausal women, androstenedione in peripheral tissues is converted into estrone and then into estradiol. A decrease in circulating estradiol levels has a therapeutic effect in breast cancer patients. In postmenopausal women, the drug in a daily dose of 1 mg causes a decrease in estradiol levels by 80%.
Arimidex does not possess progestogenic, androgenic and estrogenic activity.
Arimidex in a daily dose of up to 10 mg has no effect on the secretion of cortisol and aldosterone (therefore, the use of the drug does not require replacement of corticosteroids).
After oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 hours (on an empty stomach). Food decreases the rate, but not the degree of absorption. Small changes in the rate of absorption do not lead to a clinically significant effect on the Css of the drug in plasma with a daily intake of 1 tab. Arimidexa.
Anastrozole binds to plasma proteins by 40%. Approximately 90-95% of Css is achieved after 7 days of taking the drug. There is no information about the cumulation of the drug and the dependence of the pharmacokinetic parameters of anastrozole on time and dose.
Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronidation. Triazole, the main plasma metabolite, does not inhibit aromatase.
Anastrozole is excreted slowly, T1 / 2 - 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 stabilized 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.
Indications of the drug Arimidex
- adjuvant therapy of 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.
Dosage regimen of Arimidex
For adults, including elderly patients, the drug is prescribed 1 mg orally 1 time / day, for a long time. If signs of disease progression appear, the drug should be discontinued. As an adjuvant therapy, the recommended duration of treatment is 5 years.
Patients with mild to moderate renal impairment do not require dose adjustment.
Patients with mild liver dysfunction do not require dose adjustment.
The tablet should be swallowed whole and washed down with water. It is recommended to take the drug at the same time of the day.
Contraindications to the use of Arimidex
- severe renal failure (creatinine clearance less than 20 ml / min);
- moderate to severe hepatic impairment (safety and efficacy have not been established);
- concomitant therapy with tamoxifen;
- childhood (safety and effectiveness have not been established);
- lactation (breastfeeding);
- hypersensitivity to anastrozole and other components of the drug.
Application during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation (breastfeeding).
Application for violations of liver function
Patients with mild violations of liver function do not require dose adjustment.
Contraindicated in moderate to severe hepatic impairment (safety and efficacy have not been established).
Application for impaired renal function
Patients with mild and moderately severe impaired renal function do not require dose adjustment.
Contraindicated in severe renal failure (creatinine clearance less than 20 ml / min).
Use in children
The drug is contraindicated for use in children (safety and effectiveness have not been established).
In women with a receptor-negative tumor to estrogen, the effectiveness of Arimidex has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen.
In case of doubt about the hormonal status of the patient, menopause should be confirmed by the determination of sex hormones in the blood serum.
There is no data on the safety of the use of Arimidex in patients with severe hepatic impairment or in patients with severe renal failure (CC less than 20 ml / min).
In the case of persisting uterine bleeding while taking Arimidex, consultation and supervision of a gynecologist is necessary.
Preparations containing estrogens should not be administered concurrently with Arimidex.
By decreasing circulating estradiol levels, Arimidex can cause a decrease in bone mineral density.
In patients with osteoporosis or at risk of developing osteoporosis, bone mineral density should be assessed by densiometry (for example, DEXA scanning) at the beginning of treatment and over time. If necessary, treatment or prevention of osteoporosis should be started under close medical supervision.
There is no data on the simultaneous use of anastrozole and preparations of GnRH analogues.
It is not known whether anastrozole improves treatment outcomes when used with chemotherapy.
Safety data for long-term treatment with anastrozole have not yet been obtained.
With the use of Arimidex, ischemic diseases were observed more often than with tamoxifen therapy, however, no statistical significance was noted.
The efficacy 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.
Use in pediatrics
The safety and efficacy of the drug in children have not been established.
Impact on the ability to drive vehicles and use mechanisms
Some side effects of Arimidex, such as asthenia and drowsiness, can adversely affect the ability to perform work that requires increased concentration and psychomotor speed. In this regard, it is recommended that when these symptoms appear, be careful when driving or moving machinery.
Single clinical cases of drugare described. A single dose of Arimidex at which life-threatening symptoms develop has not been established.
Treatment: there is no specific antidote. If necessary, symptomatic therapy is carried out: induction of vomiting (if the patient is conscious), general supportive therapy, monitoring the patient and monitoring the function of vital organs and systems. Dialysis is possible.
Drug Interactions of Arimidex
Clinical studies on drug interactions with antipyrine and cimetidine indicate that coadministration of Arimidex with other drugs is unlikely to lead to clinically significant interactions due to 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.
Preparations containing estrogens should not be administered concurrently with Arimidex, because they reduce the pharmacological action of the latter.
Tamoxifen should not be administered concurrently with Arimidex, as it can weaken the pharmacological effect of the latter.
Determination of the frequency of adverse reactions: very often (> 10%); often (1-10%); rarely (0.1-1%); very rare (<0.1%).
From the side of the cardiovascular system: very often - hot flashes.
From the musculoskeletal system: often - arthralgia.
Reproductive system disorders: often - vaginal dryness; rarely - vaginal bleeding (mainly during the first weeks after the cancellation or change of previous hormone therapy to Arimidex).
From the digestive system: often - nausea, diarrhea; rarely - anorexia, vomiting, increased activity of GGT 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 side of metabolism: rarely - hypercholesterolemia. Taking the drug can cause a decrease in bone mineral density due to a decrease in the level of circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures.
Dermatological reactions: often - thinning hair, skin rash; very rarely - erythema multiforme (Stevens-Johnson syndrome).
Allergic reactions: very rarely - angioedema, urticaria, anaphylactic shock.
Others: often - asthenia.