Axastrol

Axastrol is an antitumor drug.

Indications Axastrol

It is used in the following cases:

• therapy for breast carcinoma of a widespread nature in postmenopausal women. In individuals with a negative test result for estrogen endings, no development of the drug effect was observed (excluding situations where a positive drug reaction to tamoxifen was previously detected);
• early stage hormone-positive breast cancer in postmenopausal patients (adjuvant treatment);
• early hormone-positive breast carcinoma in women at the postmenopausal stage, after a therapeutic cycle with the introduction of tamoxifen for 2-3 years (adjuvant treatment).

Release form

The medicine is released in tablet form, in the amount of 14 pieces. Inside a separate box there are 2 blister plates.

Pharmacodynamics

The drug is a selective inhibitor of the aromatase component, which has a non-steroidal nature. At the postmenopausal stage, the main part of estradiol is formed from estrone, produced inside the tissues of a peripheral nature during the transformation from androstenedione (with the help of the aromatase enzyme).

A decrease in circulating estradiol values becomes a catalyst for the development of drug effects in women with breast carcinoma. In postmenopausal women, a daily dose of anastrozole (1 mg) causes a decrease in estradiol values by 80% at once.

Anastrozole does not have androgenic, progestogenic or estrogenic effects. In medicinal doses it does not affect the processes of aldosterone and cortisol secretion.

Pharmacokinetics

Absorption and distribution processes.

Anastrozole has high absorption rates (with oral use, absorption is 83-85% of the dose). Plasma Cmax values are often noted after 2 hours after taking the drug (when taken on an empty stomach). Food slightly reduces the rate of absorption, without affecting its extent. Since the change in the rate of absorption is insignificant, there is no clinically significant effect on obtaining plasma Css values of anastrozole (in the case of using a single daily dose of the drug). When using 7-day doses, the plasma level of anastrozole is equal to 90-95% of the Css values.

Protein synthesis of anastrozole within plasma reaches 40%.

Metabolic processes and excretion.

Anastrozole is extensively metabolized in postmenopausal women. Less than 10% of the administered dose is excreted unchanged in the urine within 72 hours of administration. Metabolism of anastrozole occurs via hydroxylation, N-dealkylation, and glucuronic acid conjugation. The major plasma metabolic product of anastrozole, a triazole, does not inhibit aromatase activity.

Excretion of metabolic products occurs primarily in urine. Anastrozole is eliminated at a low rate, with a plasma half-life of 40-50 hours.

Dosing and administration

The pharmaceutical product should be taken orally, at a dosage of 1 mg, once a day.

The duration of the treatment cycle is determined by the severity and form of the pathology. If symptoms of disease progression occur, the use of the drug should be discontinued.

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Use Axastrol during pregnancy

It is prohibited to prescribe Axastrol during pregnancy or breastfeeding.

Contraindications

Main contraindications:

• the presence of intolerance to the components of the drug;
• premenopausal period;
• use of tamoxifen or medications containing estrogens during therapy with Axastrol;
• severe renal failure (creatinine clearance values are <20 ml/minute);
• severe or moderate liver failure (since there is no information on the safety and medicinal efficacy of the administration of drugs in such conditions).

Side effects Axastrol

The use of a medicinal substance may cause the development of some side effects:

• disorders affecting the functioning of the sensory organs and the nervous system: insomnia, paresthesia, dizziness, as well as a feeling of anxiety or severe drowsiness, severe headaches, depression and asthenic conditions;
• problems associated with hemostasis, hematopoietic processes and the activity of the cardiovascular system: thromboembolism, anemia, thrombophlebitis, and in addition, leukopenia (accompanied by infection or not) and an increase in blood pressure (severe dizziness and long-lasting headaches);
• respiratory disorders: runny nose, pharyngitis, dyspnea, and also bronchitis and sinusitis;
• lesions affecting the gastrointestinal tract: nausea or dry mouth, loss of appetite, diarrhea or constipation, and vomiting are observed;
• manifestations of allergies: rashes, Stevens-Johnson syndrome, as well as erythema multiforme and itching;
• others: vaginal dryness, arthralgia, hot flashes, vaginal bleeding, back or sternum pain, and myalgia. In addition, hyperhidrosis, decreased joint mobility, peripheral swelling, flu-like syndrome, and alopecia or significant thinning of the hair are noted. In addition, the list includes weight gain, the development of hypercholesterolemia, and an increase in AST, ALP, or ALT (in people with liver metastases).

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Overdose

There are only limited data available regarding intoxication testing with anastrozole.

Clinical trials have been performed with a variety of anastrozole doses: up to 60 mg in a single dose given to male volunteers, and up to 10 mg daily given to postmenopausal women with advanced breast cancer. These doses were well tolerated. No single dose of anastrozole has been identified that would be life-threatening.

The drug has no antidote, so in case of poisoning, symptomatic measures must be taken. In this case, it is also necessary to take into account the possible use of another drug or several drugs.

If the person is conscious, vomiting should be induced. Dialysis may help with the excretion of the already absorbed portion of the drug, because anastrozole has a low protein synthesis rate.

General supportive procedures are also required, including regular monitoring of vital systems and organs and close monitoring of the victim.

Interactions with other drugs

Anastrozole significantly weakens the therapeutic properties of estrogens.

Clinical tests have shown that when Axastrol is used in combination with cimetidine or antipyrine, the likelihood of developing drug interactions associated with the induction of liver microsomal enzyme activity is very low.

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Storage conditions

Axastrol should be kept in a place that is inaccessible to small children. Temperature marks - no higher than 25°C.

Shelf life

Axastrol can be used within 4 years from the date of manufacture of the pharmaceutical product.

Application for children

The medication cannot be used in pediatrics - by persons under 18 years of age.

Analogues

The analogs of the drug are Actastrozole, Letrozole, Exemestane with Anastera, Arimidex with Anastrozole, and Lezra with Letrotera. In addition, the list includes Anatero, Femara, Armotraz, Etrusil with Letoraip, Nexazole with Letromara, and also Egistrazole, Mammozole and Femizet with Texol.