Zitazonium

Zitazonium is an antiestrogenic medicine, it is included in the category of antitumor agents and hormonal antagonists.

Indications of the zitazonium

It is used in such cases:

• in the treatment of breast cancer in the late stages of the disease, and beyond this in the postoperative period (as an auxiliary drug in people with breast cancer);
• women who are in the postmenopausal period and who have metastases due to breast cancer. In people who have estrogen-positive tumors, the use of tamoxifen may be an alternative to radiotherapy in the ovaries or ovariectomy;
• to eliminate infertility (anovulatory form of pathology).

[1]

Release form

Release in tablet form - inside the blister packs in the amount of 10 pieces. In a pack it is issued on 3 blister plates.

[2]

Pharmacodynamics

Tamoxifen forms stable complexes with the help of irreversible synthesis with estrogen endings. As a result, the processes of synthesis of estradiol with the nerve ending are suppressed - this is how the active component of drugs often has an anti-estrogenic effect.

Large concentrations of drugs can inhibit the formation of progesterone receptors. As a result, the growth and development of the tumor, stimulated by secreted estrogens, slows down.

Pharmacokinetics

After oral administration, the substance is rapidly absorbed inside the digestive tract. The peak plasma values of the drug reach 4-7 hours later. With the constant use of drugs, its indices inside the blood all the time increase, reaching after 4 weeks of equilibrium.

The drug is subjected to intensive hepatic metabolism. The main substance decomposition product (N-desmethyltamoxifen) has a drug activity. The half-life of tamoxifen ranges from 91-156 hours. Excretion of drugs mainly occurs with feces.

[3]

Dosing and administration

In the treatment of breast cancer at the initial stage, it is required to take 20 mg of medicine per day. Women who are in the late stages of pathology are allowed to take 30-40 mg per day. In this case, auxiliary treatment often lasts about 3-5 years, or until the moment when, due to the progression of the disease, it is required to pass to palliative therapy.

Treatment regimens for the elimination of infertility.

Beforehand, before the beginning of treatment, it is required to be convinced of absence of pregnancy. Duration of the course and the size of the dose can not be prescribed in advance - when selecting, it is necessary to take into account the tolerability of the particular patient.

Scheme # 1: daily intake of 20 mg of the drug (during the 2-5 days of the menstrual cycle). It is necessary to constantly monitor any changes in the function of the ovaries. Women who have an irregular cycle can take medicine on any day. In the absence of ovulation induction as a result of such therapy, it is permitted to increase the dosage in accordance with the rules below.

Scheme 2: if necessary, you can increase the size of the daily dose to 40-80 mg (with a 1-2-dose per day). In the case of the onset of menstruation, a new course should be started from the second day of the new cycle. If there is an irregular cycle and the required medication is not available (and if menstruation does not begin), it is necessary to wait 45 days before starting a re-therapeutic course.

[8], [9]

Use of the zitazonium during pregnancy

Do not use Zitazonium during pregnancy.

Contraindications

The drug should not be prescribed in such cases:

• the presence of intolerance to the active component of drugs (tamoxifen) or all its other constituents;
• the period of breastfeeding;
• problems with the functional activity of the liver in severe form;
• a history of or a current thromboembolic disease.

[4], [5], [6]

Side effects of the zitazonium

The use of tablets can cause such side effects:

• disturbances in the function of the sensory organs and the NC: dizziness, cataracts, headaches, cornea damage, depression, sensation of confusion or fatigue, visual disturbances and development of retinopathy;
• manifestations in the field of CVS, but in addition to a disorder of homeostasis and hematopoiesis: the development of thromboembolism, thrombocytopenia or thrombophlebitis, and also transient leukopenia;
• lesions of the gastrointestinal tract: the emergence of nausea, abdominal pain, vomiting, the development of constipation and severe forms of disorders in the work of the liver (hepatitis or cholestasis), and in addition, loss of appetite and an increase in liver enzymes;
• disturbances in the function of the urogenital system: the appearance of vaginal discharge or bleeding, the development of amenorrhea and a treatable tumor in the ovaries (cystic), fluid retention, as well as the irregularity of the menstrual cycle in premenopausal women;
• allergy symptoms: the appearance of a rash on the skin and itching on the genital area;
• the rest: painful sensations in the site of the tumor or in the bones, the development of alopecia or hypercalcemia, the growth of tumors in the soft tissue region (with noticeable erythema in the affected areas and areas around them). Also, the temperature rises, there is a feeling of fever rolling in the bouts. As a result of prolonged use, endometrial changes can occur (among manifestations - polyps, hyperplasia, as well as uterine fibroids); Single cancer of the uterine body is observed.

[7]

Overdose

Signs of intoxication: transient neurotoxicity in acute form (the appearance of tremors, dizziness, development of hyperreflexia and instability of gait). Similar violations occur several days after the abolition of therapy. Zitazonium does not cause incurable disorders in the body.

The medicine does not have a special antidote. If there is a suspicion that an overdose has occurred, standard procedures for symptomatic and maintenance therapy are required.

Interactions with other drugs

Zitazonium is forbidden to combine with the drug allopurinol (antidotal agent), and in addition to substances that reduce blood viscosity and prevent the appearance of thrombi (eg, coumarin derivatives).

Caution is required when using drugs in combination with bromocriptine - as a result, the serum count of both the active ingredient and the drug decay product may increase. With caution apply and together with cytotoxic agents - this combination increases the risk of complications of thromboembolic type.

[10], [11], [12]

Storage conditions

Zitazonium must be kept in places where sunlight does not penetrate, and also inaccessible to children. Temperature conditions are within 15-25 ° С.

[13], [14]

Shelf life

Zitazonium can be used in the period of 4 years from the date of manufacture of the drug.

[15]