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Mammozol
Mammozol is an insecticidal repellent and an inhibitor of enzymes. It is part of a group of hormonal antagonists and other similar drugs.
Indications of the mammozol
Indicated when:
- a common form of breast cancer in postmenopausal women (except those who have an estrogen-inactive form of cancer, except when the patient has a positive drug response to tamoxifen);
- auxiliary treatment of an invasive form of breast cancer estrogen-positive type (during postmenopause in the early stages of the disease);
- additional treatment of early stages of estrogen-positive breast cancer during postmenopause in women who underwent adequate treatment with tamoxifen for 2-3 years.
Pharmacodynamics
Anastrozole is a strong, highly selective aromatase inhibitor. During postmenopause, the production of estradiol in women is often carried out in a transformative form - inside the peripheral tissues - from androstenedione to estrone (the aromatase enzyme takes part in this). Further, estrone is converted into the substance estradiol. Reduction of the circulating estradiol in the blood has a medicinal effect on women who suffer from breast cancer. The drug in a daily dose of 1 mg causes in women during postmenopause, a decrease in the rates of estradiol by 80%.
Anastrozole has no activity against androgens, progestogens, and estrogens.
In a daily dose of up to 10 mg, the drug does not affect the release of aldosterone with cortisol, the level of which was measured before, and also after standard testing using stimulation of ACTH. Therefore, it is not necessary to carry out substitution treatment with the use of corticosteroids.
Pharmacokinetics
The drug is quickly absorbed after oral administration, reaching peak plasma values after 2 hours (in case of fasting). In the case of reception, along with food, the suction rate decreases slightly, but its degree remains the same. Individual changes in the rates of absorption should not have a drug-significant effect on the equilibrium plasma concentration of drugs in the case of daily use of the 1st pill.
About 90-95% of the equilibrium drug index is reached after 7 days after drug use. There is no evidence that the pharmacokinetics of the active substance depends on the size of the dosage or the time of administration. Synthesis of anastrozole with a plasma protein is 40%.
Extensive metabolism of the active component is observed in women who are in the postmenopausal period. The very process of metabolism occurs by means of hydroxylation, N-dealkylation, and also glucuronization.
The excretion of the substance is rather slow, the plasma half-life is 40-50 hours. Urine excreted less than 10% of the dosage (unchanged substance) - it occurs in the period of 72 hours after taking drugs. The products of decay are mostly excreted in the urine. The main decay product (triazole), which can be found in urine, as well as plasma, is not an aromatase inhibitor.
Contraindications
Among the contraindications of drugs:
- severe intolerance to anastrozole or other components of the drug;
- premenopausal period;
- Kidney failure in severe degree (QC values are less than 20 ml / minute);
- disorders in the work of the liver (severe or moderate degree);
- combination with the substance tamoxifen or estrogen;
- childhood.
Side effects of the mammozol
Often, adverse reactions to the use of the drug were hot flashes, as well as asthenia (less common reaction). Only occasionally developed manifestations of allergies (urticaria, edema Quincke or anaphylaxis).
Among other side effects are the following:
- organs of the National Assembly: in most cases, there are headaches (usually of moderate or mild character), and in addition carpal tunnel syndrome. Occasionally drowsiness may develop (usually also in moderate or mild degree);
- Gastrointestinal organs: usually there is a nausea (moderate or mild); more rarely there is vomiting, also moderate or mild;
- a subcutaneous layer with an integument: basically it is possible to observe thinning of hair (weakly or average expressed) and occurrence on a skin of an eruption (lungs or moderate forms). The Stevens-Johnson syndrome or the erythema multiforme develops singly;
- organs of the ODA: basically pain in the joints or a decrease in their motor activity (degree of expression - moderate or weak);
- digestive system and metabolic processes: occasionally anorexia (in mild form) may develop, and in addition hypercholesterolemia of moderate or mild severity;
- mammary glands and reproductive organs: usually marked dryness of the vaginal mucosa (moderate or mild). Occasionally, slight or moderate bleeding from the vagina was observed (usually this type of disorder was observed in women with a progressive stage of breast cancer in the first few weeks after changing the form of treatment - with hormone therapy for the use of Mammozol). If the bleeding does not stop, an additional examination is required.
Due to the fact that anastrozole lowers the circulating estrogens, it is possible to weaken the mineral density in the bone structure, as a result of which the risk of fracture may increase in some women.
An increase in the GGT values, as well as of the AF, is quite rare.
Dosing and administration
For adults (also elderly women) the dose is equal to a one-time (per day) oral intake of 1 mg of the drug.
Correct the size of the doses for women suffering from mild or mild disorders in the work of the kidneys, as well as mild disorders of the hepatic function, is not necessary.
At the beginning of treatment at an early stage of the pathology, the duration of the treatment course using Mammozol is usually 5 years.
Overdose
There is only limited information regarding clinical cases of development of a random overdose. The size of a single dose of the drug, which is capable of causing life-threatening abnormalities, has not been established.
The drug does not have a specific antidote, in the event of a disorder, symptomatic therapy is required. In the process of elimination of violations it is necessary to take into account the possibility that the patient took not only Mammozol. If it is conscious, it is recommended to induce vomiting. In addition, dialysis can become an effective method for overdose, since anastrozole is poorly synthesized with protein. Also, general supportive treatment and constant monitoring of the work of life-critical systems and organs are required.
Interactions with other drugs
Clinical tests for interaction with cimetidine and antipyrin substances have shown that when anastrozole is combined with other drugs, there is likely to be no medically significant effect caused by the hemoprotein P450.
Anastrozole slows the action of P450 1A2 hemoprotein as well as 2C8 / 9 with 3A4 in in vitro tests, although clinical trials of combining with warfarin have demonstrated that 1 mg of anastrozole hardly interferes with the metabolism of elements that are metabolized by the hemoprotein P450. There is no significant interaction between anastrozole and phosphonates.
A study of the safety data collected during the clinical trials revealed no information about the significant interaction of drugs in women who combined anastrozole with other commonly prescribed drugs.
Estrogens are not allowed to combine with anastrozole, because these drugs have opposite pharmacological properties.
It is also not possible to combine Mammozol with tamoxifen, since it can weaken the drug efficacy of anastrozole.