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AFIMAREKS

Trade name of the drug: Afimarex

Active ingredient (INN): anastrozole

Pharmaceutical dosage form: coated tablets

Composition

One tablet contains: 
active ingredient: anastrozole – 1 mg,

Excipients: Lactose monohydrate, sodium starch glycolate, povidone, magnesium stearate, macrogol 3350, hypromellose, titanium dioxide, triacetin. 

Description: tablets, round-shaped, biconvex, white film-coated.

Pharmacotherapeutic group: Hormone antagonists and their analogs. Enzyme inhibitors. 

ATC code: L02BG03


Pharmacological properties: Anastrozole is a potent and highly-selective non-steroidal aromatase inhibitor. In postmenopausal women, estradiol is produced mainly in the conversion of androstenedione to estrone through the aromatase enzyme complex in peripheral tissues. Estrone is subsequently transformed into estradiol. The reduction of circulating estradiol levels has a beneficial effect on women with breast cancer. In postmenopausal women, anastrozole at a daily dose of 1 mg caused a suppression of estradiol by more than 80% when using a high-sensitivity analysis.
Anastrozole has no progestogenic, androgenic or estrogenic activity.
Daily doses of anastrozole up to 10 mg do not affect the secretion of cortisol or aldosterone.


Pharmacokinetics: Inhibition of aromatase activity is produced mainly through the anastrozole parent drug. Orally administrated anastrozole is well absorbed by the circulatory system, with 83 - 85% recovered in urine and faeces. Food does not affect the extent of absorption. Anastrozole elimination occurs mainly through hepatic metabolism (approximately 85%) and, to a smaller extent, through renal excretion (about 11%). The average half-life of anastrozole in postmenopausal women is about 50 hours. The main circulating metabolite of anastrozole – triazole - has no pharmacological activity. Pharmacokinetics of anastrozole is linear over a range of doses from 1 mg to 20 mg, and does not change for repeated doses. The half-life is of 2 days, in which the plasma concentration levels approach the established levels after 7 days of dosing once daily. Steady-state levels are three to four times higher than the levels observed after a single dose of anastrozole. In the therapeutic range, about 40% of anastrozole binds with plasma proteins. Anastrozole is extensively metabolized, with about 10% of the dose excreted in the urine as an unchanged drug within 72 hours of dosing, and the remainder (about 60% of the dose) excreted in urine as metabolites.
Metabolism of anastrozole if realized through N-dealkylation, hydroxylation and glucuronidation. In plasma and urine metabolites, three anastrozole metabolites were identified. The identified metabolites are triazole, glucuronide conjugate of hydroxy-anastrozole and anastrozole glucuronide directly.
Since excretion through the kidneys is not the principal elimination method, anastrozole total clearance remains unchanged even in severe (creatinine clearance less than 30 mL / min / 1,73m2) renal insufficiency. Regular dosage for patients with renal dysfunction, as well as those with stable cirrhotic is not required.


Directions for usage
— Breast cancer of advanced stage in postmenopausal period

— Adjuvant Treatment of postmenopausal women with positive receptor status of Breast cancer in the early invasive stages


Early breast cancer in postmenopausal women with positive receptor status, after 2-3 years of adjuvant tamoxifen therapy


Dosage and method of administration:
The drug is administered orally. The tablet is taken with water. The medication is taken always at the same time, regardless of meals.
Adults, including elderly people, take 1 mg orally daily for a long time. If there are signs of progression of the disease, taking the drug should be stopped. As an adjuvant therapy, recommended duration of treatment is of 5 years.
Dose adjustment in patients with impaired renal function is not required. Dose adjustment in patients with mild to moderate liver dysfunction is not required. Maximum single and daily dose -1 mg


Side effects:
Frequently
— hot flashes

— joint pain and stiffness
— vaginal dryness

— vaginal bleeding (mainly during the first weeks after the cancellation or change of previous hormonal therapy anastrozole)

— thinning hair, skin rash

— nausea, diarrhea, anorexia

— increase of ALT, AST, alkaline phosphatase

— hepatitis

— constipation

— headache

— asthenia


Rarely
— vasculitis

— hypercholesterolemia

— increase of GGT activity

— drowsiness


Very rarely
— Erythema multiforme (Stevens-Johnson syndrome)

— Allergic reactions, including angioedema, urticaria and anaphylaxis

 

Contraindications:
— premenopausal period

— Pregnancy and lactation

— Severe renal impairment (creatinine clearance less than 20 mL / min)

— Moderate or severe liver disease

— Hypersensitivity to anastrozole or to any of the excipients

—  Child and adolescence to 18 years

— Concomitant treatment with tamoxifen and / or estrogenic drugs 

 

Drug interactions: Studies on drug interactions with cimetidine and antipyrine indicate that clinically significant drug interactions mediated by cytochrome P450, during the combined use of anastrozole with other drugs is unlikely. Clinically
there are no significant drug interactions when taking anastrozole in conjunction with other frequently prescribed drugs. At the moment, there are no data on the use of anastrozole in combination with other anticancer drugs.
Formulas containing estrogen, reduce pharmacological effect of anastrozole, and therefore they shall not be administered simultaneously.


Special instructions: In case of doubt about the hormonal status of the patient, the menopause must be confirmed through the analysis of the sex hormones in blood serum. When uterine bleeding in patients receiving anastrozole, a gynecologist's consultaion and observation is necessaty.
By reducing the level of circulating estradiol, anastrozole can cause a reduction of bone mineral density.
In patients with osteoporosis or risk of developing osteoporosis, bone mineral density should be assessed by densitometry (eg, DEXA-scan) at the beginning of the treatment and in the dynamics. If necessary, treatment or prevention of osteoporosis under the close supervision of a physician should be started.
Features of drug effects on the ability to drive a vehicle or potentially dangerous machinery. Some Side effects of anastrozole, 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
The drug should be stored out of reach of children and shall not be used after the expiry date.


Overdose: Clinical trials were conducted with various dosages of anastrozole, these dosages were well tolerated, a single doses of anastrozole, which can cause life-threatening symptoms, has not been identified. There is not any specific antidote in case of an overdose therefore the treatment should be symptomatic.
Treatment: in case of an overdose one should take into account that several medications may have been taken by the patient. It can cause vomiting, if the patient is conscious. Dialysis may be helpful because anastrozole is not highly protein bound.


Dosage forms and packaging: 10 tablets in blisters of the aluminum foil.
1,2,3,5,6,9 or 10 blisters with instruction for the medical application in the local and Russian languages are presented in a cardboard box


Storage conditions: Store away from light and moisture, at a temperature no higher than 25 ° C.


Shelf life: 2 years


Dispensing requirements: On prescription


Manufacturer: Codepharm LLC (IE), 30-Gulistan Str, 4th quarter, Gulistan, Sirdaryo Region, The Republic of Uzbekistan.