Texol

Texol is a hormone antagonist and a drug that inhibits enzyme activity.

Indications Texola

It is used to treat advanced breast cancer in postmenopausal women (except women with estrogen-negative cancer) who have not previously responded positively to tamoxifen.

Release form

The medicine is released in tablets, in the amount of 7 pieces inside a blister pack. The box contains 4 such packs.

Pharmacodynamics

Anastrozole is a selective nonsteroidal element that inhibits aromatase activity. During postmenopause, estradiol formation occurs mainly with the participation of estrone produced by peripheral tissues, through transformation from androstenediol. The enzyme aromatase is involved in this process.

Decreased estradiol levels lead to drug effects in women with breast cancer. During postmenopause, the component anastrozole in a dose of 1 g per day leads to a decrease in estradiol levels by 80%.

The drug does not have androgenic, progestogenic, or estrogenic effects and in therapeutic doses does not affect the release of aldosterone with cortisol.

Pharmacokinetics

When taken orally, the drug is rapidly absorbed in the gastrointestinal tract. Peak values in the blood plasma are noted after 2 hours (when taken on an empty stomach). Food slightly reduces the absorption rate, without affecting its degree. The synthesis of the substance with the protein located in the plasma is 40%. There is no information on the accumulation of the drug.

Metabolic processes of the drug occur with the participation of N-dealkylation, glucuronidation and hydroxylation. The main decay product is triazole, which does not lead to a slowdown in aromatase activity.

Anastrozole, together with its metabolic products, is excreted mostly in urine (less than 10% of which are unchanged) for 72 hours after a single dose. The half-life is approximately 40-50 hours.

Dosing and administration

Texol is prescribed to adult women for oral use at 1 mg once a day.

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Use Texola during pregnancy

Prescribing Texol to pregnant women is contraindicated.

Contraindications

Main contraindications:

• women who have not yet entered menopause;
• severe renal failure (CC level is less than 20 ml/minute);
• breastfeeding women;
• presence of hypersensitivity to anastrozole;
• liver failure.

Side effects Texola

The use of the drug can provoke various side effects that appear with varying frequency.

In most cases, reactions affecting vascular activity develop, such as sudden flushes of blood to the skin of the face, often of mild or moderate severity.

The following signs are often encountered:

• systemic: feeling of fatigue or asthenia;
• disorders affecting the function of the musculoskeletal system: muscle rigidity or pain, and in addition, the risk of bone fractures;
• disorders of the mammary glands or reproductive organs: dryness of the vaginal mucosa (usually moderate);
• lesions of the epidermis or its appendages: moderate form of alopecia;
• problems with the gastrointestinal tract: the appearance of diarrhea or nausea;
• dysfunction of the nervous system: feelings of agitation or anxiety, headaches and carpal tunnel syndrome;
• damage to the visual organs: development of cataracts;
• disorders in the functioning of the cardiovascular system: development of myocardial infarction, coronary heart disease or angina pectoris;
• disorders of the hepatobiliary system: increased levels of liver enzymes, such as ALT with AST and alkaline phosphatase.

The following disorders sometimes occur:

• lesions in the area of the mammary glands or reproductive organs: vaginal bleeding (often in patients with advanced breast cancer - during the first few weeks after changing treatment from hormone therapy to a drug containing anastrozole);
• Metabolic and metabolic disorders: development of anorexia (mostly to a moderate degree). The total cholesterol level may also increase slightly;
• gastrointestinal disorders: vomiting;
• symptoms associated with the work of the nervous system: feeling of drowsiness;
• lesions affecting the hepatobiliary system: development of hepatitis or increased GGT and bilirubin levels;
• dysfunction of the cardiovascular system: any complications of a thromboembolic nature in the veins, and also vascular ischemia in the brain.

The following manifestations are occasionally observed:

• lesions affecting the functioning of the cardiovascular system: ischemia in the myocardium or coronary arteries;
• disorders of the epidermis and its appendages: Stevens-Johnson syndrome or erythema multiforme;
• other disorders: allergy symptoms including urticaria, angioedema and anaphylaxis;
• Disorders of reproductive function and mammary gland function: cancer in the endometrium.

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Interactions with other drugs

The medication weakens the medicinal properties of estrogens when combined with them.

Information from clinical trials shows that when Texol is combined with cimetidine or antipyrine, the likelihood of developing a therapeutic interaction associated with the induction of microsomal liver enzymes is very low.

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Storage conditions

Texol must be kept out of reach of children, at temperatures below 25°C.

Shelf life

Texol can be used for 2 years from the date of manufacture of the therapeutic agent.

Use in children

It is prohibited to use the medicine on children.

Analogues

Analogues of the drug are the following medications: Axastrol, Actastrozole, Anastera, Anastrozole, Anatero, Arimidex, Armotraz, Aromasin, Lezra, Letoraip, Letrozole, Letromara, Letrotera, Mammozole, Nexazole, Femara, Femizet, Egistrazole, Exemestane, Enzamidex, Etrusil.