Cetrotid

The cetrotide is part of the group of antigonadotropins, is liberin.

Indications of the cetrotid

It is used to prevent premature onset of female ovulation. Used for controlled ovarian induction, after which the extraction of oocytes takes place. In the process, additional reproductive techniques are also used.

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Release form

It is available as a lyophilizate for making injection solutions.

Cetrotide 0.25 mg

Cetrotide 0.25 mg - the blister contains 1 vial filled with powder, a syringe pre-filled with a special solvent (1 ml volume), a needle required for dissolution (1 piece), an injection needle (1 piece) and 2 a tampon soaked in alcohol. Inside the package contains 1 or 7 blisters.

Cetrotide 3 mg

Cetrotide 3 mg - 1 bottle of powder is contained in the blister pack, in addition to it, a syringe filled with a solvent (1 piece, 3 ml volume), a dissolution needle (1 piece), an injection needle (1 piece), and tampons wetted in alcohol (2 pieces). Inside the package contains 1 such blister.

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Pharmacodynamics

Cetrorelix is a gonadotropin antagonist liberin. It is synthesized with the endings of the cell membranes of the pituitary gland and, at the same time, competes in conjunction with the internal gonadotropin liberin. This helps the substance to control the process of pituitary excretion of gonadotropins (LH, as well as FSH). This happens by slowing down the function (the degree depends on the dose). Suppression begins almost immediately, without giving the initial stimulating effect, and then maintained in the case of continuous administration of the solution.

The substance delays the growth of the LH in women, and as a result, ovulation is delayed. During the ovarian induction, the duration of exposure to cetrorelix depends on the size of the dose. When injecting a single dose (3 mg), the effect lasts no less than 4 days. On the 4th day after injection, the suppression level is approximately 70%. When injections with a size of 0.25 mg with intervals between procedures lasting 24 hours, the drug effect is maintained. At the end of the therapeutic course, the antagonistic hormonal effect of the drug completely disappears.

[3], [4]

Pharmacokinetics

With SC injection, the level of bioavailability of cetrorelix reaches about 85%.

The total index of renal and plasma clearance is 0.1 ml / minute 1x1 kg and 1.2 ml / minute 1x1 kg, respectively. The distribution volume is 1.1 l / kg. The average index of the final half-life at n / k and in / in the introductions is 30 and 12 hours respectively. This demonstrates the presence of a suction process at the site of administration.

With n / k injections of single dosages of drugs (0.25-3 mg of substance) and after repeated administration of the solution every 14 days, the pharmacokinetic properties of the drug remain linear.

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Dosing and administration

The medicine can be prescribed only by a doctor who has sufficient experience in this field.

Caution is required to appoint if the patient has symptoms and manifestations of active allergic reactions, or if there is a history of allergies. In severe forms of allergies, Cetrotide should not be prescribed.

The first injection should be carried out under the supervision of the doctor and in such conditions, under which it will be possible to immediately provide assistance in case of pseudoallergic / allergic manifestations. Subsequent injections a woman can perform on her own until she feels symptoms that can indicate the appearance of signs of hypersensitivity or the development of the consequences of these manifestations - in such cases urgent medical care will be needed.

Injection of the solution is performed by the n / k method in the area of the lower part of the peritoneum (it is recommended to choose a site around the navel). To reduce the risk of local reactions, each injection needs to be done in different parts of the body without introducing the solution into the same place. In addition, it is recommended to inject slowly to ensure gradual absorption.

After the first injection, follow the patient for half an hour to ensure that there are no complications due to the use of Cetrotide.

The drug is administered once (use Cetrotide 3 mg) or in the form of a course of everyday procedures (0.25 mg drug) during the middle and early follicular stage. If the attending physician has not proposed a different scheme for administering the solution, it is required to use it in accordance with the recommendations described below.

Cetrotide in the form of release 0.25 mg.

It is necessary to administer the solution once a day (in the morning or in the evening), observing 24-hour intervals between the procedures.

In the morning injection: the medication should be started on the 5th or 6th day of the ovarian induction cycle (approximately 96-120 hours after the ovarian induction begins with the use of the drugs of recombinant or chorionic gonadotropin), and then continue the entire period of gonadotropin administration (this includes also the day of stimulation of ovulation or the day of injection of HC).

In case of evening injection: the solution should be started on the 5th day of the cycle (approximately 96-108 hours after the ovarian induction course begins with the use of recombinant or urinary gonadotropin), and then continue with the entire period of gonadotropin use until evening (inclusive ) before the day when the stimulation of ovulation is performed.

Cetrotide in the form of 3 mg.

It is required to administer the solution after the indicative indicator of estradiol is reached inside the serum (the element responsible for the desired response to the induction being performed). Often this day is the 7th day of ovarian induction (approximately 132-144 hours after ovarian induction begins, during which drugs containing recombinant or chorionic gonadotropin are used).

If the follicular function does not make it possible to perform ovulation stimulation on the 5th day after the injection of 3 mg of the drug, then 96 hours after this procedure (day 5) it is required to additionally administer the drug in the amount of 0.25 mg once a day before the moment ovarian induction inclusive.

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Use of the cetrotid during pregnancy

Do not prescribe medication to pregnant women or lactating women.

Tests performed on animals did not reveal a teratogenic effect, but there were early manifestations of resorption, as well as an increase in implantation losses (depending on the size of the dose).

Contraindications

The main contraindications:

• increased sensitivity with respect to the active component or any structural analogues of the substance Gn-RG, and in addition external peptide hormones and additional elements of the drug;
• postmenopausal period;
• disorders in the work of the liver or kidneys (severe or moderate degree);
• childhood.

[6], [7]

Side effects of the cetrotid

The solution can provoke the development of certain side effects:

• Immunity reactions: pseudoallergic / allergic manifestations occur occasionally, among them anaphylactic symptoms that are life-threatening;
• manifestations from the NA: in some cases there are headaches;
• reactions of the digestive system: occasionally nausea may develop;
• mammary glands and reproductive function: Often develops HSH (in moderate or mild form), but this is an inherent risk when performing the procedure of ovarian induction. In some cases, this syndrome develops to a severe degree;
• manifestations at the site of introduction and systemic disorders: often there are local reactions in the area of injection - in the form of itching, erythema, or swelling. These symptoms are usually transient and have a mild severity.

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Overdose

In case of an overdose, it is possible to prolong the effect of the drug, but it is unlikely that this can provoke acute poisoning.

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Interactions with other drugs

Formal testing for drug interactions with other agents was not performed.

In vitro tests have demonstrated that the likelihood of Cetrotide interactions with drugs metabolized by the hemoprotein P450 or with the formation of conjugates or glucuronides via separate routes is extremely low. But, in any case, even though there is no information on interactions (especially with commonly used drugs, gonadotropins and drugs that stimulate histamine release in people with hypersensitivity), one can not completely exclude the possibility of their development.

Storage conditions

Powder should be stored in a place protected from sunlight, and also inaccessible to small children. Temperature values - no more than 25 ° С.

Shelf life

Cetrotid is suitable for use in the period of 2 years from the date of release of the medicine. In this case, it is necessary to take into account that after dilution it must be used immediately. Unused ready-mixed solution should not be administered after the lapse of time after dilution.

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