Aksastrol

Aksastrol is an antitumor medication.

Indications Aksastrol

Applicable in the following cases:

• therapy with a breast carcinoma of a widespread nature in women in the postmenopausal period. In individuals with a negative response to the test for estrogen endings, there was no evidence of a drug effect (except when a positive drug response to tamoxifen was previously detected);
• an early stage of breast cancer, which has a hormone-positive nature, in postmenopausal patients (adjuvant treatment);
• early breast carcinoma of a hormone-positive nature in postmenopausal women, after a therapeutic cycle with the introduction of tamoxifen for 2-3 years (adjuvant treatment).

Release form

The drug is produced in tablet form, in a quantity of 14 pieces. Inside the box there are 2 blister plates.

Pharmacodynamics

The drug is a selective inhibitor of the aromatase component, which is non-steroidal. At the postmenopausal stage, the bulk of the estradiol is formed from estrone produced inside the peripheral tissues when converted from androstenedione (using the aromatase enzyme).

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

Anastrozole does not have an androgenic, progestogen, and estrogenic effect. In medicinal portions does not affect the processes of aldosterone release with cortisol.

Pharmacokinetics

Absorption and distribution processes.

Anastrozole has high rates of absorption (when taken orally, the absorption is 83-85% of the dosage). Plasma Cmax values are often noted after 2 hours after drug use (when taken on an empty stomach). Food slightly reduces the rate of absorption, without affecting its degree. Since the change in the rate of absorption is insignificant, the clinically significant effect of obtaining plasma indices of Css anastrozole does not develop (in the case of using a 1-time daily dose of medication). When using 7-day doses, the plasma level of anastrozole is 90-95% of the Css values.

Protein synthesis of anastrozole within the plasma reaches 40%.

Exchange processes and excretion.

Anastrozole undergoes intensive metabolism in postmenopausal women. Less than 10% of the used dosage is excreted in the unchanged state with urine for 72 hours after ingestion. Exchange processes anastrozole carried out through the stages of hydroxylation, N-dealkylation, as well as conjugation with glucuronic acid. The main plasma metabolic product of anastrozole, the triazole substance, does not slow down the activity of the aromatase enzyme.

Excretion of metabolic products mainly occurs in the urine. Excretion of anastrozole is carried out at low speed, and the plasma half-life is 40-50 hours.

Dosing and administration

The pharmaceutical should be taken orally, at a dosage of 1 mg, 1-fold per day.

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

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Use Aksastrol during pregnancy

It is forbidden to prescribe Aksastrol during pregnancy or breastfeeding.

Contraindications

The main contraindications:

• the presence of intolerance relative to the components of the drug;
• premenopausal period;
• The use of tamoxifen on a background of therapy with aksastrol or medicines containing estrogens;
• renal insufficiency, which has a pronounced character (CC values are <20 ml / minute);
• expressed or moderate form of insufficiency of hepatic activity (since there is no information about the safety and drug effectiveness of drug administration under such conditions).

Side effects Aksastrol

The use of medication can cause some side effects:

• disorders affecting the work of the sensory organs and NS: insomnia, paresthesia, dizziness, and in addition a feeling of anxiety or severe drowsiness, severe headaches, depression and asthenic condition;
• problems associated with hemostasis, hematopoiesis and SSS activity: thromboembolism, anemia, thrombophlebitis, and besides this, leukopenia (accompanied by infection or not) and an increase in blood pressure (marked dizziness and long-lasting headaches);
• disturbances of respiratory function: runny nose, pharyngitis, dyspnea, and in addition to bronchitis and sinusitis;
• lesions affecting the intestinal tract: nausea or dryness of the oral mucosa, weakening of appetite, diarrhea or obtapation, as well as vomiting;
• manifestations of allergy: rashes, Stevens-Johnson syndrome, as well as multiform erythema and itching;
• others: dryness of the vaginal mucosa, arthralgia, hot flashes, bleeding from the vagina, pain in the back or sternum and myalgia. In addition, there is hyperhidrosis, decreased joint mobility, peripheral puffiness, flu-like syndrome, and with it alopecia or significant thinning of the hair. In addition, the list of weight gain, the development of hypercholesterolemia and increased indicators of AST, APF or ALT (in people with metastases in the liver).

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Overdose

There are only limited information on the testing of anastrozole intoxication.

Clinical tests were performed with various portions of anastrozole: up to 60 mg in a single dose, which was prescribed for men to volunteers, and also in a dose of up to 10 mg per day given to women at the postmenopausal stage with a common form of breast carcinoma. Such dosages were tolerated without complications. It was not possible to determine a 1-time dose of anastrozole, which could lead to a threat to life.

The medicine does not have an antidote, so when poisoning it is necessary to perform symptomatic measures. It is also necessary to take into account the possible use of another drug or several medications.

If a person is conscious, vomiting should be induced. Carrying out dialysis can help with excretion of an already absorbed part of the drug, because anastrozole has a low protein synthesis value.

It is also necessary to carry out general support procedures, including regular monitoring of the work of life-critical systems and organs, as well as close monitoring of the victim.

Interactions with other drugs

Anastrozole markedly weakens the therapeutic properties of estrogens.

Clinical tests have demonstrated that when combined use of axastrol with cimetidine or antipyrine, the likelihood of developing drug-induced interactions associated with the induction of enzyme activity in the hepatic microsomes is very low.

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Storage conditions

Aksastrol is required to be kept in a place that will not be accessible to young children. Temperature marks - not higher than 25 ° С.

Shelf life

Aksastrol can be used within 4 years of the manufacture of the pharmaceutical.

Application for children

You can not use a medicine in pediatrics - people who have not reached the age of 18.

Analogues

Analogues of the drug are drugs Aktastrozol, Letrozol, Exemestan with Anastora, Arimidex with Anastrozole, as well as Lezra with Letroteroy. In addition, in the list of Anatero, Femar, Armotraz, Etruzil with Lethorup, Nexazol with Letromara, and at the same time Egistrozolum, Mammozolum and Femiset with Texol.