Fazlodex

Fazlodex is an effective antitumor agent possessing an antiestrogenic property, that is, having an effect opposite to the estrogen receptor.

The drug is actively used for the treatment of cancer, especially malignant neoplasms of the breast.

[1], [2]

Indications Fazlodex

Faslodex is prescribed for metastatic and rapidly progressive forms of breast cancer, with oncological diseases that have a positive perception of estrogens (estrogen-dependent cancer ) breast cancer in patients).

Most often it is used in the menopause, when the pathology develops simultaneously or at the end of treatment. antiestrogenic drugs .

Fazlodex is not indicated at a young age: it is usually used to treat adults and elderly women.

[3], [4], [5]

Release form

Medication Fazlodeks is intended for intramuscular injections.

It is manufactured and manufactured in a special disposable syringe made of glass material with a convenient system of use. The syringe contains 5 ml of medicinal product, packed in a clear, transparent, 1-pack, a sterile needle supplied in a protected package. The drug is released in a cardboard box.

The active ingredient of the drug is fulvestrant, in an amount of 0.25 g. Additional substances are represented by ethanol 96% - 0.5 g, benzyl alcohol - 0.5 g, benzyl benzoate - 0.75 g / ml, castor oil, adjusted to 5 ml .

The drug is a clear, perhaps slightly yellowish slightly viscous (due to castor oil) liquid.

[6], [7]

Pharmacodynamics

Farmakodinamika Fazlodeks is determined by the action of the active component of the drug - a substance that has antagonistic properties with the receptor of estrogens. By the strength of interaction with the receptors has a similar effect with estradiol. The active substance stops the trophic effect of estrogens, without revealing at the same time an independent activity, similar to estrogens.

The principle of the drug's effect is based on inhibition of active activity and regression of estrogen receptors.

In addition, the active component of Fazlodex confidently reduces the severity of progesterone receptors. During the reception of the drug there is no stimulation of the endometrium during the postmenopause.

The effect of the drug on endometrial tissue with prolonged course of treatment was not evaluated, as well as possible changes in tissue structure.

There were no studies of the effect of prolonged drug therapy on bone tissue.

[8], [9],

Pharmacokinetics

With intramuscular injection, the drug is absorbed gradually. The maximum amount of active component is detected only after a week. The use of Fazlodex at a dosage of 0.5 g provides optimal balance during the first 4 weeks of use. Equilibrium provides for fluctuating the level of the active substance in the plasma in a fairly narrow range: the readings max and min can differ approximately 3-fold.

With intramuscular injection, the ratio can be proportional to the administered dosage of the drug (in the range of 0.05-0.5 g).

The active substance is distributed in the body fairly quickly, and mainly outside the vessels. With plasma proteins binds to 99%. The main components of the ligament consist of low-density lipoprotein, medium-density and high-density fractions.

The metabolic properties of the active substance of the drug consist of a combination of a large number of possible methods of biological transformation, identical to the metabolic schemes of endogenous steroid hormones. Defined metabolites may be somewhat more passive than the active substance.

The active component of the drug is mostly excreted with calories, about 1% can be excreted through the kidneys. The clearance of the substance implies a high degree of extraction in the liver. The term half-elimination is determined by 50 days.

Pharmacokinetics Fazlodex does not change depending on the age category of the patient, on his weight and belonging to a particular race.

[10], [11], [12]

Dosing and administration

Fazlodex is intended for intramuscular administration. Method of administration: slow (for 2 minutes) injection. If you require the introduction of 2 doses, then the drug is introduced first into one, then into the other buttock muscle.

Adults and elderly patients receive the drug in an amount of 0.25-0.5 g once every 30 days. Perhaps the initial introduction of Fazlodex is 0.5 g twice a month, with an interval of 14-15 days.

In children and adolescents, the drug is not used.

With liver diseases and urinary system, it is not necessary to make changes in the dosage of the medication.

Caution: The needle that comes with the anti-estrogen remedy does not require additional sterilization. Touch the needle during the entire period of drug administration should not be.

Scheme of application:

• we remove the transparent syringe from the packaging cell, inspect for lack of cracks and chips;
• print out the external protection of the needle;
• break off the septum of the white plastic cap of the cannula of the syringe and remove the cap together with the rubber stopper;
• by the method of rotation we attach the needle to the cannula of the syringe;
• we remove the protection of the needle, do it carefully, trying not to hook the end of the needle;
• with a slight push we release excess bubbles from the cavity of the syringe;
• We inject into the outer upper quadrant of the buttocks, inject the drug slowly (up to 2 minutes);
• Remove the needle and press it onto the special lever, moving it to the extremely forward position to close the end of the needle. If this manipulation fails, then simply place the needle in the needle container to prevent possible residues of the drug from getting onto the skin.

The procedure should be carried out as carefully as possible, the injection should be performed with gloves. Do not allow strangers to perform the procedure: the administration of the drug should be controlled by a competent medical specialist.

[13], [14]

Use Fazlodex during pregnancy

The drug is prohibited for use during pregnancy and lactation.

Contraindications

Contraindications for the use of Fazlodex are:

• allergic reactions to the active or any additional substance of the drug;
• severe form of functional disorder of the liver;
• period of pregnancy and breastfeeding;
• children under 18 years of age.

Care should be taken when administering the drug to patients with disorders of the urinary system.

Side effects Fazlodex

Medication Fazlodeks can manifest itself by some side effects, which we give in descending order of frequency:

• bouts of nausea;
• diarrhea, emaciation, loss of appetite, fits of vomiting;
• periodic attacks of "heat", cases of thromboembolism;
• skin rashes;
• signs of an inflammatory reaction at the injection site;
• cystitis, urethritis;
• thrush, discharge from the vagina;
• increased activity of ALT, AST, APF;
• high level of bilirubin;
• pain in the head, swelling.

After the drug is discontinued, side effects tend to disappear.

Overdose

About situations with an overdose of Fazlodex medication was not reported.

When conducting experimental experiments on animals, when large doses of Fazlodex were administered, only direct and indirect signs of oppression of the functional ability of estrogens were seen.

Treatment for overdose is carried out depending on the symptoms detected.

[15], [16], [17]

Interactions with other drugs

Based on the results of the experimental interaction of Fazlodex and Midazolam, cytochrome P450 3A4 activity is not suppressed. The information obtained allows us to conclude that the active substance of the preparation has no effect on cytochrome P450 1A2, 2D6, 2C9 and 2C19. Influence on other cytochromes was not traced.

During the experimental experience of the combined action of Fazlodex with such drugs as Rifampicin and Ketoconazole, no apparent changes in the clearance of the active substance Fazlodex were observed. Hence it can be concluded that the use of Fazlodex concomitantly with drugs inducing or inhibiting cytochrome P450 3A4 does not require a revision of the dosage of the drug.

[18], [19]

Storage conditions

Fazlodex can be stored only in places that are completely inaccessible to children. Optimum temperature performance for the preservation of the drug from +2 to + 8 ° C. The drug should not be frozen and heated.

[20], [21]

Shelf life

The shelf life of the drug under proper storage conditions is up to 4 years. Do not use this medication if its shelf life has expired or the contoured package or glass syringe itself has been damaged.

[22]