Composition, structure and packing
Tablets, coated white, round, biconvex, engraved with "A" on one side and "Adx" and "1" as a fraction - on the other side.
1 tab. anastrozole 1 mg.
Excipients: lactose monohydrate, povidone, sodium karboksimetilenkrahmal, magnesium stearate, purified water.
The composition of the shell tablets: macrogol 300, gipromelloza, titanium dioxide, purified water.
Clinico-pharmacological group: The antitumor drug. Aromatase inhibitors.
Pharmacological action
Highly selective non-steroidal aromatase inhibitor. Aromatase - an enzyme, whereby in postmenopausal women androstenedione in peripheral tissues converted into estrone and further to estradiol. The reduction of circulating estradiol has a therapeutic effect in patients with breast cancer.
In postmenopausal drug in a daily dose of 1 mg causes a decrease in the level of estradiol by 80%. Arimideks not possess progestogenic, androgenic and estrogenic activity. Arimideks a daily dose of 10 mg has no effect on the secretion of cortisol and aldosterone (hence, the use does not require substitution corticosteroids).
Pharmacokinetics
Absorption
After oral anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in the plasma is achieved within 2 h (fasting). Food slightly reduces the rate but not the degree of suction. Small changes in the rate of absorption does not lead to clinically significant effect on the CSS of the drug in plasma at a daily intake of 1 tablet. Arimideksa. Distribution of anastrozole is associated with plasma proteins by 40%. Approximately 90-95% of the CSS is reached after 7 days of treatment. No information about the cumulation of the drug and the pharmacokinetic parameters anastrosol depending on the time and dose.
Metabolism
Anastrozole is metabolized by N-dealkylation, hydroxylation and glyukuronizatsii. Triazole, the main metabolite, determined in plasma, did not inhibit aromatase.
Withdrawal
nastrozol displayed slowly, T1 / 2 - 40-50 hours anastrozole and its metabolites are derived mainly from urine (less than 10% of the derived dose - in an unmodified form) within 72 hours after ingestion.
Pharmacokinetics in special clinical situations
Defined anastrosol clearance after oral administration in volunteers with stable cirrhosis of the liver or kidney dysfunction does not differ from the clearance determined in healthy volunteers. Pharmacokinetics anastrosol not depend on age in postmenopausal women.
Statement
adjuvant therapy for early gormonopolozhitelnogo breast cancer in postmenopausal women;
treatment of disseminated breast cancer in postmenopausal women;
adjuvant therapy for early gormonopolozhitelnogo breast cancer in postmenopausal women after therapy with tamoxifen for 2-3 years.
Dosage regimen
Adults, including elderly patients, a drug prescribed to 1 mg orally 1 time per day, for a long time.
If signs of disease progression receiving the drug should be discontinued. As an adjuvant therapy for the recommended duration of treatment - 5 years. Patients with mild to moderately impaired renal function expressed do not need dose adjustment.
Patients with mild hepatic impairment does not require dose adjustment. Tablets should be swallowed whole and then drink water. It is recommended to take the drug in the same time of day.
Side effect
Determining the frequency of adverse reactions: very common (> 10%), often (1-10%), rarely (0.1-1%), rarely (<0.1%).
Since the cardiovascular system: very often - the tides.
On the part of the reproductive system: often - vaginal dryness; rarely - vaginal bleeding (mainly during the first weeks after the cancellation or change prior hormonal therapy Arimideks).
On the part of the digestive system: frequent - nausea, diarrhea, rarely - anorexia, vomiting, increased activity of GGT and alkaline phosphatase.
On the part of the nervous system: often - headache, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease); rarely - drowsiness.
On the part of metabolism: rare - hypercholesterolemia.
Receiving medication may decrease bone mineral density due to lower levels 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 rare - allergic reactions (including angioedema, urticaria, anaphylactic shock).
Other: often - arthralgia, asthenia.
Contraindications
renal failure, severe (creatinine clearance less than 20 ml / min);
hepatic failure secondary to severe (safety and efficacy not established);
concomitant therapy with tamoxifen;
children's age (safety and efficacy not established);
Pregnancy
lactation (breastfeeding);
Hypersensitivity to anastrozole and other components of the drug. The drug is not indicated in premenopausal women.
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation (breastfeeding).
Application for violations of liver function
Patients with mild hepatic impairment does not require dose adjustment. Contraindicated in moderate or significant hepatic insufficiency (safety and efficacy not established).
Application for violations of renal function
Patients with mild to moderately impaired renal function expressed do not need dose adjustment. Contraindicated in renal failure, severe (creatinine clearance less than 20 ml / min).
Cautions
In women with tumors of estrogen retseptorootritsatelnoy Arimideksa effectiveness 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's menopause must be confirmed by the definition of sex hormones in the blood serum.
No data on the safety of Arimideksa in patients with severe hepatic impairment or in patients with renal failure severe (CC less than 20 ml / min). In the case of persistent uterine bleeding in the background of reception Arimideksa need advice and supervision by a gynecologist.
Preparations containing estrogens should not be given simultaneously with Arimideksom. By reducing the level of circulating estradiol, Arimideks may decrease bone mineral density.
In patients with osteoporosis or at risk for osteoporosis, bone mineral density should be evaluated by densiometrii (eg, DEXA scan) at the beginning of treatment and in dynamics.
If necessary, should be initiated for treatment or prevention of osteoporosis under the close supervision of a physician. No data on the simultaneous application of anastrosol and preparations of GnRH analogues.
It is not known whether anastrozole improves treatment outcomes when used in conjunction with chemotherapy. Data on safety in the long-term treatment anastrozole has not yet received.
Efficacy and safety Arimideksa and tamoxifen in their simultaneous application, regardless of the status of hormone receptors are comparable with those using a single tamoxifen. The exact mechanism of this phenomenon is not yet known.
Effects on ability to drive vehicles and management mechanisms
Some side effects Arimideksa, such as asthenia and sleepiness, may adversely affect the ability to perform work that requires high concentration and speed of psychomotor reactions. In this connection it is recommended when you encounter these symptoms to be careful when driving or moving machinery.
Overdose
Described sporadic clinical cases of overdosing.
Single dose Arimideksa in which life-threatening symptoms has not been established.
Treatment: There is no specific antidote. If necessary, a symptomatic therapy: induction of vomiting (if the patient is conscious), general supportive therapy, monitoring patients and control function of vital organs and systems. Perhaps dialysis.
Drug Interactions
Clinical studies on drug interactions with cimetidine and antipyrine indicate that coadministration Arimideksa with other drugs is unlikely to lead to a clinically significant interaction caused by cytochrome P450.
Clinically significant drug interactions when taking Arimideksa simultaneously with other prescribers often absent. At the moment there is no information on the application Arimideksa in combination with other anticancer agents.
Preparations containing estrogens should not be given simultaneously with Arimideksom, because they reduce the pharmacological effect of the latter.
You should not assign tamoxifen concurrently with Arimideksom because it can weaken the pharmacological effect of the latter.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children at or above 30 ° C. Shelf life - 5 years.
Tablets, coated white, round, biconvex, engraved with "A" on one side and "Adx" and "1" as a fraction - on the other side.
1 tab. anastrozole 1 mg.
Excipients: lactose monohydrate, povidone, sodium karboksimetilenkrahmal, magnesium stearate, purified water.
The composition of the shell tablets: macrogol 300, gipromelloza, titanium dioxide, purified water.
Clinico-pharmacological group: The antitumor drug. Aromatase inhibitors.
Pharmacological action
Highly selective non-steroidal aromatase inhibitor. Aromatase - an enzyme, whereby in postmenopausal women androstenedione in peripheral tissues converted into estrone and further to estradiol. The reduction of circulating estradiol has a therapeutic effect in patients with breast cancer.
In postmenopausal drug in a daily dose of 1 mg causes a decrease in the level of estradiol by 80%. Arimideks not possess progestogenic, androgenic and estrogenic activity. Arimideks a daily dose of 10 mg has no effect on the secretion of cortisol and aldosterone (hence, the use does not require substitution corticosteroids).
Pharmacokinetics
Absorption
After oral anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in the plasma is achieved within 2 h (fasting). Food slightly reduces the rate but not the degree of suction. Small changes in the rate of absorption does not lead to clinically significant effect on the CSS of the drug in plasma at a daily intake of 1 tablet. Arimideksa. Distribution of anastrozole is associated with plasma proteins by 40%. Approximately 90-95% of the CSS is reached after 7 days of treatment. No information about the cumulation of the drug and the pharmacokinetic parameters anastrosol depending on the time and dose.
Metabolism
Anastrozole is metabolized by N-dealkylation, hydroxylation and glyukuronizatsii. Triazole, the main metabolite, determined in plasma, did not inhibit aromatase.
Withdrawal
nastrozol displayed slowly, T1 / 2 - 40-50 hours anastrozole and its metabolites are derived mainly from urine (less than 10% of the derived dose - in an unmodified form) within 72 hours after ingestion.
Pharmacokinetics in special clinical situations
Defined anastrosol clearance after oral administration in volunteers with stable cirrhosis of the liver or kidney dysfunction does not differ from the clearance determined in healthy volunteers. Pharmacokinetics anastrosol not depend on age in postmenopausal women.
Statement
adjuvant therapy for early gormonopolozhitelnogo breast cancer in postmenopausal women;
treatment of disseminated breast cancer in postmenopausal women;
adjuvant therapy for early gormonopolozhitelnogo breast cancer in postmenopausal women after therapy with tamoxifen for 2-3 years.
Dosage regimen
Adults, including elderly patients, a drug prescribed to 1 mg orally 1 time per day, for a long time.
If signs of disease progression receiving the drug should be discontinued. As an adjuvant therapy for the recommended duration of treatment - 5 years. Patients with mild to moderately impaired renal function expressed do not need dose adjustment.
Patients with mild hepatic impairment does not require dose adjustment. Tablets should be swallowed whole and then drink water. It is recommended to take the drug in the same time of day.
Side effect
Determining the frequency of adverse reactions: very common (> 10%), often (1-10%), rarely (0.1-1%), rarely (<0.1%).
Since the cardiovascular system: very often - the tides.
On the part of the reproductive system: often - vaginal dryness; rarely - vaginal bleeding (mainly during the first weeks after the cancellation or change prior hormonal therapy Arimideks).
On the part of the digestive system: frequent - nausea, diarrhea, rarely - anorexia, vomiting, increased activity of GGT and alkaline phosphatase.
On the part of the nervous system: often - headache, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease); rarely - drowsiness.
On the part of metabolism: rare - hypercholesterolemia.
Receiving medication may decrease bone mineral density due to lower levels 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 rare - allergic reactions (including angioedema, urticaria, anaphylactic shock).
Other: often - arthralgia, asthenia.
Contraindications
renal failure, severe (creatinine clearance less than 20 ml / min);
hepatic failure secondary to severe (safety and efficacy not established);
concomitant therapy with tamoxifen;
children's age (safety and efficacy not established);
Pregnancy
lactation (breastfeeding);
Hypersensitivity to anastrozole and other components of the drug. The drug is not indicated in premenopausal women.
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation (breastfeeding).
Application for violations of liver function
Patients with mild hepatic impairment does not require dose adjustment. Contraindicated in moderate or significant hepatic insufficiency (safety and efficacy not established).
Application for violations of renal function
Patients with mild to moderately impaired renal function expressed do not need dose adjustment. Contraindicated in renal failure, severe (creatinine clearance less than 20 ml / min).
Cautions
In women with tumors of estrogen retseptorootritsatelnoy Arimideksa effectiveness 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's menopause must be confirmed by the definition of sex hormones in the blood serum.
No data on the safety of Arimideksa in patients with severe hepatic impairment or in patients with renal failure severe (CC less than 20 ml / min). In the case of persistent uterine bleeding in the background of reception Arimideksa need advice and supervision by a gynecologist.
Preparations containing estrogens should not be given simultaneously with Arimideksom. By reducing the level of circulating estradiol, Arimideks may decrease bone mineral density.
In patients with osteoporosis or at risk for osteoporosis, bone mineral density should be evaluated by densiometrii (eg, DEXA scan) at the beginning of treatment and in dynamics.
If necessary, should be initiated for treatment or prevention of osteoporosis under the close supervision of a physician. No data on the simultaneous application of anastrosol and preparations of GnRH analogues.
It is not known whether anastrozole improves treatment outcomes when used in conjunction with chemotherapy. Data on safety in the long-term treatment anastrozole has not yet received.
Efficacy and safety Arimideksa and tamoxifen in their simultaneous application, regardless of the status of hormone receptors are comparable with those using a single tamoxifen. The exact mechanism of this phenomenon is not yet known.
Effects on ability to drive vehicles and management mechanisms
Some side effects Arimideksa, such as asthenia and sleepiness, may adversely affect the ability to perform work that requires high concentration and speed of psychomotor reactions. In this connection it is recommended when you encounter these symptoms to be careful when driving or moving machinery.
Overdose
Described sporadic clinical cases of overdosing.
Single dose Arimideksa in which life-threatening symptoms has not been established.
Treatment: There is no specific antidote. If necessary, a symptomatic therapy: induction of vomiting (if the patient is conscious), general supportive therapy, monitoring patients and control function of vital organs and systems. Perhaps dialysis.
Drug Interactions
Clinical studies on drug interactions with cimetidine and antipyrine indicate that coadministration Arimideksa with other drugs is unlikely to lead to a clinically significant interaction caused by cytochrome P450.
Clinically significant drug interactions when taking Arimideksa simultaneously with other prescribers often absent. At the moment there is no information on the application Arimideksa in combination with other anticancer agents.
Preparations containing estrogens should not be given simultaneously with Arimideksom, because they reduce the pharmacological effect of the latter.
You should not assign tamoxifen concurrently with Arimideksom because it can weaken the pharmacological effect of the latter.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children at or above 30 ° C. Shelf life - 5 years.
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