Mammozole

Mammozol is an insecticidal repellent and enzyme inhibitor. It belongs to the group of hormonal antagonists and other similar drugs.

Indications Mammozole

Shown for:

• a common form of breast cancer in postmenopausal women (except those who have been diagnosed with an estrogen-inactive form of cancer, excluding cases where the patient has shown a positive drug response to the substance tamoxifen);
• adjuvant treatment of invasive estrogen-positive breast cancer (during postmenopause in the early stages of the disease);
• adjunctive treatment of early stage estrogen-positive breast cancer during postmenopause in women who have received adequate treatment with tamoxifen for 2-3 years.

Release form

Available in tablet form, 14 pieces per blister. One package contains 2 such blisters.

Pharmacodynamics

Anastrozole is a potent, highly selective aromatase inhibitor. During postmenopause, estradiol production in women is often carried out in a transformative form - inside peripheral tissues - from androstenedione turning into estrone (the aromatase enzyme is involved in this). Estrone is then converted into the substance estradiol. A decrease in the levels of estradiol circulating in the blood has a medicinal effect on women with breast cancer. The drug in a daily dose of 1 mg causes an 80% decrease in estradiol levels in postmenopausal women.

Anastrozole has no activity against androgens, progestogens, or estrogens.

In a daily dose of up to 10 mg, the drug does not affect the release of aldosterone and cortisol, the level of which was measured before and after standard testing using ACTH stimulation. Therefore, replacement therapy with corticosteroids is not required.

Pharmacokinetics

The drug is absorbed fairly quickly after oral administration, reaching peak plasma levels after 2 hours (if taken on an empty stomach). When taken with food, the absorption rate is slightly reduced, but its extent remains the same. Individual changes in the absorption rate should not have a medicinally significant effect on the steady-state plasma concentration of the drug when taking 1 tablet daily.

About 90-95% of the drug's equilibrium value is achieved 7 days after taking the drug. There is no data that the pharmacokinetics of the active substance depends on the dosage or time of administration. Synthesis of anastrozole with plasma protein is 40%.

Extensive metabolism of the active component is observed in women in the postmenopausal period. The process of metabolism itself occurs through hydroxylation, N-dealkylation, and glucuronidation.

The excretion of the substance is quite slow, the plasma half-life is 40-50 hours. Less than 10% of the dose (unchanged substance) is excreted in the urine – this occurs within 72 hours after taking the drug. The decay products are excreted mostly in the urine. The main decay product (triazole), which can be found in the urine and plasma, is not an aromatase inhibitor.

Dosing and administration

For adults (including elderly women), the dose is equal to a single (daily) oral administration of 1 mg of the drug.

No dosage adjustment is necessary for women with moderate or mild renal impairment or mild hepatic impairment.

When starting treatment at an early stage of the pathology, the duration of the treatment course using Mammozol is usually 5 years.

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Use Mammozole during pregnancy

Mammozol should not be used by pregnant women or during lactation.

Contraindications

Among the contraindications of the drug:

• severe intolerance to anastrozole or other components of the drug;
• premenopausal period;
• severe renal failure (CC values are less than 20 ml/minute);
• liver dysfunction (severe or moderate);
• combination with the substance tamoxifen or with estrogens;
• childhood.

Side effects Mammozole

Frequently, side effects of the drug included hot flashes and asthenia (a less common reaction). Only rarely did allergic reactions develop (urticaria, Quincke's edema, or anaphylaxis).

Other side effects include the following:

• NS organs: in most cases headaches are observed (usually moderate or mild), as well as carpal tunnel syndrome. Occasionally drowsiness may develop (usually also moderate or mild);
• Gastrointestinal organs: nausea (moderate or mild) usually occurs; vomiting, also moderate or mild, is observed less frequently;
• subcutaneous layer with skin: mainly hair thinning (mild or moderate) and skin rash (mild or moderate) can be observed. Stevens-Johnson syndrome or erythema multiforme develops occasionally;
• musculoskeletal system organs: mainly painful sensations in the joints or a decrease in their motor activity are noted (the degree of expression is moderate or weak);
• digestive system and metabolic processes: occasionally, anorexia (in mild form) may develop, as well as moderate or mild hypercholesterolemia;
• Breasts and reproductive organs: vaginal dryness (moderate or mild) was commonly observed. Mild or moderate vaginal bleeding was occasionally observed (usually this type of disorder was observed in women with advanced breast cancer in the first few weeks after changing the form of treatment – from hormone therapy to the use of Mammosol). If bleeding does not stop, further examination is required.

Because anastrozole reduces circulating estrogen levels, it may reduce bone mineral density, which may increase the risk of fracture in some women.

An increase in GGT and alkaline phosphatase values is observed quite rarely.

Overdose

There is limited information regarding clinical cases of accidental overdose. The size of a single dose of the drug that can cause life-threatening disorders has not been established.

The drug has no specific antidote, and symptomatic therapy is required if disorders occur. In the process of eliminating disorders, it is necessary to take into account the possibility that the patient has taken more than just Mammozol. If she is conscious, it is recommended to induce vomiting. In addition, dialysis can be an effective method for overdose, since anastrozole is poorly synthesized with protein. General supportive treatment and constant monitoring of vital systems and organs are also required.

Interactions with other drugs

Clinical interaction tests with the substances cimetidine and antipyrine have shown that when anastrozole is combined with other drugs, it is unlikely that a medicinally significant effect caused by the hemoprotein P450 will occur.

Anastrozole inhibits the action of hemoprotein P450 1A2, as well as 2C8/9 and 3A4 in vitro tests, although clinical trials of combination with warfarin have demonstrated that 1 mg of anastrozole does not significantly inhibit the metabolism of elements metabolized by hemoprotein P450. No significant interactions have been identified between anastrozole and phosphonates.

A review of safety data collected during clinical trials revealed no significant drug interactions in women who combined anastrozole with other commonly prescribed medications.

Estrogens are prohibited to be combined with anastrozole, because these drugs have opposite pharmacological properties.

Also, Mammozole should not be combined with tamoxifen, as this can weaken the medicinal effectiveness of anastrozole.

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Storage conditions

The medicine must be kept in a place inaccessible to small children. The temperature values should not exceed 30°C.

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Shelf life

Mammozol is permitted to be used for a period of 3 years from the date of release of the drug.