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Cetrotide
Last reviewed: 03.07.2025
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Cetrotide belongs to the group of antigonadotropins and is a liberin.
Indications Cetrotide
It is used to prevent premature onset of female ovulation. It is used in controlled ovarian induction, after which oocytes are extracted. Additional reproductive techniques are also used in the process.
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Release form
It is produced in the form of a lyophilisate for the preparation of injection solutions.
Cetrotide 0.25 mg
Cetrotide 0.25 mg - the blister contains 1 bottle filled with powder, a syringe pre-filled with a special solvent (volume 1 ml), a needle required for dissolution (1 piece), an injection needle (1 piece), and also 2 tampons soaked in alcohol are attached to it. The package contains 1 or 7 blisters.
Cetrotide 3 mg
Cetrotide 3 mg - the blister contains 1 bottle with powder, in addition to it there is a syringe filled with solvent (1 piece; volume 3 ml), a needle for dissolution (1 piece), an injection needle (1 piece), and tampons soaked in alcohol (2 pieces). Inside the package there is 1 such blister.
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Pharmacodynamics
Cetrorelix is a gonadotropin liberin antagonist. It is synthesized with the endings of the pituitary cell membranes and competes in the compound with the internal gonadotropin liberin. This helps the substance control the process of secretion of gonadotropins (LH, as well as FSH) by the pituitary gland. This occurs by slowing down the function (the degree depends on the dose). Suppression begins almost immediately, without providing an initial stimulating effect, and is then maintained in the case of prolonged administration of the solution.
The substance delays the growth of LH in women, which delays ovulation. During ovarian induction, the duration of action of cetrorelix depends on the dose. With a single injection of 3 mg, the effect lasts for at least 4 days. On the 4th day after the injection, the level of suppression is approximately 70%. With injections of 0.25 mg with intervals between procedures lasting 24 hours, the medicinal effect is maintained. At the end of the therapeutic course, the antagonistic hormonal effect of the drug completely disappears.
Pharmacokinetics
When administered subcutaneously, the bioavailability of cetrorelix reaches approximately 85%.
The total renal and plasma clearance is 0.1 ml/min 1x1 kg and 1.2 ml/min 1x1 kg, respectively. The distribution volume is 1.1 l/kg. The average terminal half-life for subcutaneous and intravenous administration is 30 and 12 hours, respectively. This demonstrates the presence of an absorption process at the site of administration.
With subcutaneous injections of single doses of the drug (0.25-3 mg of the substance) and after repeated daily administration of the solution for a period of 14 days, the pharmacokinetic properties of the drug remain linear.
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Dosing and administration
The medicine can only be prescribed by a doctor who has sufficient experience in this field.
Caution is required when prescribing if the patient has symptoms and manifestations of active allergic reactions or if there is a history of a tendency to develop allergies. Cetrotide should not be prescribed for severe forms of allergies.
The first injection should be performed under the supervision of a doctor and in conditions that will allow immediate assistance in the event of pseudoallergic/allergic manifestations. The woman can perform subsequent injections independently until she feels symptoms that may indicate the appearance of signs of hypersensitivity or the development of consequences of these manifestations - in such cases, urgent medical assistance will be needed.
The injection of the solution is performed subcutaneously into the lower part of the peritoneum (it is recommended to choose the area around the navel). To reduce the risk of local reactions, each injection should be done in a different part of the body, without injecting the solution into the same place. In addition, it is recommended to inject slowly to ensure gradual absorption.
After the first injection, the patient should be observed for half an hour to ensure that complications due to the use of Cetrotide do not develop.
The medicine is administered once (use Cetrotide 3 mg) or in the form of a course of daily procedures (0.25 mg medicine) during the middle and early follicular stages. Unless the attending physician has suggested a different scheme for administering the solution, it must be used in accordance with the recommendations described below.
Cetrotide in the form of 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 procedures.
For morning injection: Start using the medication on day 5 or 6 of the ovarian induction cycle (approximately 96-120 hours after ovarian induction with recombinant or human chorionic gonadotropin medications begins) and then continue throughout the entire period of gonadotropin administration (this also includes the day of ovulation stimulation or the day of hCG injection).
For evening injection: the use of the solution should be started on the 5th day of the cycle (approximately 96-108 hours after the start of the ovarian induction course using recombinant or urinary gonadotropin), and then continue administration throughout the entire period of gonadotropin use until the evening (inclusive) before the day when ovulation stimulation will be performed.
Cetrotide in the form of 3 mg.
The solution must be administered after the indicative value of estradiol in the serum (the element responsible for the required response to the induction being performed) has been reached. Often this day is the 7th day of ovarian induction (approximately 132-144 hours after the ovarian induction begins, during which drugs containing recombinant or human chorionic gonadotropin are used).
If the follicular function does not allow ovulation stimulation to be performed on the 5th day after the injection of 3 mg of the drug, then 96 hours after this procedure (the 5th day), it is necessary to additionally administer the drug in the amount of 0.25 mg once a day up to and including the moment of ovarian induction.
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Use Cetrotide during pregnancy
The drug should not be prescribed to pregnant or lactating women.
Animal tests did not reveal any teratogenic effects, but early resorption was observed and an increase in implantation loss was observed (depending on the dose size).
Contraindications
Side effects Cetrotide
The solution may provoke the development of certain side effects:
- immune reactions: occasionally pseudoallergic/allergic manifestations develop, including anaphylactic symptoms that are life-threatening;
- manifestations from the nervous system: in some cases, headaches appear;
- reactions of the gastrointestinal tract: nausea may occasionally develop;
- mammary glands and reproductive function: OHSS often develops (in a moderate or mild form), but this is an inherent risk when performing the ovarian induction procedure. In some cases, this syndrome develops to a severe degree;
- manifestations at the injection site and systemic disorders: local reactions often occur at the injection site - in the form of itching, erythema or swelling. These symptoms are usually transient and mild.
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Overdose
In case of overdose, the effect of the drug may be prolonged, but it is unlikely that this will cause acute poisoning.
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Interactions with other drugs
Formal drug-drug interaction testing has not been performed.
In vitro tests have shown that the probability of interactions of Cetrotide with drugs that are metabolized via hemoprotein P450 or that form conjugates or glucuronides via separate other pathways is extremely low. However, even though there is no information on interactions (especially with commonly used drugs, gonadotropins, and drugs that stimulate histamine release in hypersensitive individuals), the possibility of their development cannot be completely excluded.
Storage conditions
The powder should be stored in a place protected from sunlight and inaccessible to small children. Temperature values are no more than 25°C.
Shelf life
Cetrotide is suitable for use within 2 years from the date of manufacture of the medicine. It should be taken into account that after dilution it should be used immediately. Unused ready solution is prohibited to be administered after some time has passed after dilution.
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Attention!
To simplify the perception of information, this instruction for use of the drug "Cetrotide" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.