Cetrotide
Cetrotide: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Cetrotid
ATX code: H01CC02
Active ingredient: cetrorelix (cetrorelix)
Manufacturer: Baxter Oncology (Germany), AEterna Zentaris GmbH (Germany), Abbott Biologicals B. V. (Netherlands), Pierre Fabre Medicament Production (France)
Description and photo update: 2019-31-01
Prices in pharmacies: from 6300 rubles.
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Cetrotide is an antigonadotropic agent.
Release form and composition
The dosage form of Cetrotide is a lyophilisate for the preparation of a solution for subcutaneous administration: powder or mass (in the form of a lozenge) of almost white or white color. The lyophilisate is packaged at 0.25 and 3 mg in colorless glass vials, sealed with a rubber stopper, which is sealed on top with an aluminum cap and an opening plastic flip-off cap. Each vial with a lyophilisate is supplied with a solvent - water for injection: a clear colorless liquid (for a dosage of 0.25 mg - 1 ml, for a dosage of 3 mg - 3 ml) in a pre-filled glass syringe equipped with a polypropylene piston rod with a rubber seal and polypropylene cap. The kit includes: 1 vial of lyophilisate, 1 syringe with solvent, 1 individually wrapped 20G needle, 1 individually wrapped 27G needle,2 nonwoven swabs impregnated with 70% isopropyl alcohol, in a separate double-layer laminated foil bag; 1 or 7 sets are packed in a blister strip packaging made of plastic, sealed with a paper lid, and in a cardboard box.
Composition of 1 bottle of lyophilisate:
- active substance: cetrorelix (in the form of acetate) - 0.25 or 3 mg;
- auxiliary component: mannitol - 54.8 or 164.4 mg.
Pharmacological properties
Pharmacodynamics
Cetrorelix, the active substance of Cetrotide, is an analogue of the gonadotropin-releasing hormone (GnRH). Its mechanism of action is explained by the ability to bind to receptors of pituitary cell membranes and competitively inhibit the binding of endogenous GnRH by these receptors.
The drug dose-dependently inhibits the secretion of gonadotropins by the pituitary gland - luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
In the absence of preliminary stimulation, almost immediately after the introduction of cetrorelix, the onset of inhibition of the secretory function of the pituitary gland begins.
In women, Cetrotide inhibits the rise in LH levels and, as a result, delays ovulation.
The duration of the drug's action depends on the dose administered. After a single dose of 3 mg, the effect persists for at least 4 days (on the fourth day, the inhibition of the secretory function is 70%). The action is maintained with the regular administration of cetrorelix at a dose of 0.25 mg once a day.
After the abolition of Cetrotide, the effect of Cetrorelix is completely reversible.
Pharmacokinetics
Cetrorelix is rapidly absorbed after subcutaneous administration. The volume of distribution is 1.1 l / kg, the absolute bioavailability is 85%.
Pharmacokinetic parameters after administration of a dose of 0.25 mg (respectively, single and multiple - within 14 days):
- C max (maximum plasma concentration) - 4.17-5.92 ng / ml and 5.18-7.96 ng / ml;
- T max (time to reach maximum concentration) - 0.5-1.5 hours and 0.5-2 hours;
- AUC (area under the concentration-time pharmacokinetic curve) - 23.4–42 ng / h / ml and 36.7–54.2 ng / h / ml;
- T 1/2 (half-life) - 2.4-48.8 hours and 4.1-179.3 hours.
With the introduction of single doses of the drug in the range from 0.25 to 3 mg, the pharmacokinetics shows a linear relationship, as with the daily use of cetrorelix for 14 days.
The drug is excreted by the kidneys. The total plasma and renal clearance are 1.2 ml / min · kg and 0.1 ml / min · kg, respectively.
The average terminal half-life after intravenous and subcutaneous administration, respectively, is 12 and 30 hours.
Indications for use
According to the instructions, Cetrotide is prescribed to prevent the premature release of an egg from the follicle in women during the period of controlled stimulation of ovulation for obtaining eggs and further carrying out assisted reproductive technologies.
Contraindications
- moderate to severe hepatic or renal impairment;
- pregnancy and lactation;
- postmenopausal period;
- hypersensitivity to mannitol, cetrorelix, any other structural analogs of GnRH or other exogenous peptide hormones.
Cetrotide should be used with caution in patients with signs and symptoms of an active allergic process or with a history of allergy predisposition.
Instructions for the use of Cetrotide: method and dosage
Cetrotide is used only as directed by a gynecologist.
After the first injection, the woman should be under close medical supervision in order to exclude an allergic or pseudo-allergic reaction to the drug administration. The institution should provide all the necessary drugs and tools for stopping such reactions, if they occur.
A solution for subcutaneous administration is prepared from the lyophilisate by dilution with water for injection.
Cetrotide 0.25 mg
The drug is administered once a day every 24 hours, in the morning or in the evening.
If Cetrotide is indicated for administration in the morning, treatment is started on day 5 or 6 (approximately 96–120 hours) of ovarian stimulation with recombinant or urinary gonadotropin. Continue therapy throughout the entire period of stimulation, including the day of administration of an ovulatory dose of chorionic gonadotropin (HCG).
If Cetrotide is indicated for administration in the evening, treatment is started on day 5 (after about 96-108 hours) of ovarian stimulation with recombinant or urine-derived gonadotropin. The therapy is continued during the entire period of stimulation, including the evening preceding the administration of the ovulatory dose of hCG.
Cetrotide 3 mg
The drug is administered once on day 7 (approximately after 132-144 hours) of ovarian stimulation with recombinant or urine-derived gonadotropin.
If, on the 5th day after the administration of 3 mg of Cetrotide, the follicle sizes do not correspond to the norm for the appointment of ovulation induction, an additional 0.25 mg of the drug is injected: the first injection - 96 hours after the administration of 3 mg of Cetrorelix, then every 24 hours during the entire period of stimulation, including the day of administration of the ovulatory dose of hCG.
Recommendations for self-administration of Cetrotide
The first injection is always given by a specialist doctor. In the future, independent administration of Cetrotide is possible. The patient should be informed about the symptoms indicating the development of an allergic reaction and their possible consequences, as well as warned about the need to immediately consult a doctor if they occur.
The prepared solution should be injected subcutaneously into the lower part of the anterior abdominal wall, optimally into the area around the navel. It is recommended to change the injection site every day to avoid the appearance of local irritation with repeated injections of the drug.
To dilute the lyophilisate, use only the supplied diluent. During dissolution, the bottle must be gently shaken, it should not be shaken vigorously to avoid the formation of bubbles.
Do not use solution with insoluble particles or cloudiness.
It is necessary to draw the entire contents of the vial into the syringe, this will allow you to enter the required dose: at least 0.23 mg when using the drug at a dosage of 0.25 ml or at least 2.82 mg when using Cetrotide at a dosage of 3 mg. The prepared solution cannot be stored, therefore it should be prepared immediately before administration.
Procedure for self-administration of Cetrotide:
- Wash hands thoroughly.
- Prepare a clean surface and decompose the contents of the Cetrotide kit.
- Open the bottle, wipe the aluminum ring and rubber stopper with one swab with alcohol.
- Take the yellow-marked needle and remove it from the package. Unpack the solvent syringe. Put the needle on the syringe and remove the protective cap from it.
- Insert the needle into the central part of the stopper that closes the bottle, and slowly pushing the plunger, introduce the solution into the bottle.
- Without removing the needle, gently shake the bottle until the lyophilisate is completely dissolved. Do not shake the bottle!
- Draw the entire contents of the vial into the syringe. To collect the rest of the solution in the vial, it is necessary to turn it over and extend the needle so that its end is directly under the stopper.
- Remove the needle from the syringe and place it on a clean surface. Take the gray-marked needle, remove it from the package, put it on the syringe and remove the protective cap.
- Take the syringe so that the needle is a rod. Gently push the plunger to release air from the syringe. Do not touch the needle with your hands, do not allow it to come into contact with any surfaces.
- Choose an injection site (preferably in the navel area). Take a swab soaked in alcohol and wipe it over the skin at the injection site. Set aside the tampon.
- Take the syringe with one hand, with the other - squeeze the skin surrounding the injection site, firmly fixing it between the fingers.
- Place the syringe in your hand like a pencil and at an angle of 45 ° insert the needle completely into the skin, ceasing to squeeze it.
- Gently pull the piston back slightly. If there is no blood, inject the solution by slowly pressing the plunger, then carefully remove the needle, and press the swab soaked in alcohol on the skin at the injection site. If blood appears in the syringe, follow the next step.
- If blood appears in the syringe, it is necessary to remove the needle from the skin and lightly press this place with an alcohol swab. It is forbidden to use this solution for subsequent injection, it should be poured into the sink. Start all actions from point 1.
All needles and syringes are single use only.
Side effects
Most often, local reactions occur in the area of administration of Cetrotide: itching, redness, swelling - they are usually weak and quickly pass. In clinical trials, these phenomena were observed in 9.4% of patients after multiple injections of the drug at a dose of 0.25 mg.
When ovulation is stimulated with gonadotropin, ovarian hyperstimulation syndrome (OHSS) often occurs from mild to moderate severity [I and II degrees in accordance with the classification of the World Health Organization (WHO)]. Symptoms include pain and tension in the abdomen, ovarian enlargement, diarrhea, nausea, vomiting, and weight gain. In severe (III) degree OHSS is rare. In this case, the following symptoms may be added to these symptoms: hemoconcentration, hypovolemia, ascites, electrolyte imbalance, shortness of breath, pleural effusion, oliguria, fluid accumulation in the pericardial cavity, thromboembolic disorders, acute respiratory distress syndrome.
In rare cases, Cetrotide causes hypersensitivity reactions, including anaphylactoid or pseudoallergic. They are similar to the symptoms of allergic reactions, but are characterized by a lack of antibody production and, to one degree or another, usually manifest themselves in the form of headaches, hives, fever, redness of the skin, and difficulty breathing.
Below are listed all the adverse reactions that were observed with the use of Cetrotide, they are divided into frequent (from ≥ 1/100 to <1/10) and infrequent (from ≥ 1/1000 to <1/100):
- on the part of the genitals and mammary gland: often - mild or moderate OHSS (I – II degree according to the WHO classification); infrequently - severe OHSS (grade III according to the WHO classification);
- from the nervous system: infrequently - headache;
- on the part of the immune system: infrequently - systemic allergic or pseudo-allergic reaction, including life-threatening anaphylaxis;
- from the gastrointestinal tract: infrequently - nausea;
- local reactions: often - usually transient and mild redness, itching, swelling at the injection site.
Overdose
In case of exceeding the recommended dose of Cetrotide, an increase in the duration of its action is possible, however, this is not accompanied by symptoms of acute toxicity, therefore, special measures are not required.
special instructions
At a dosage of 0.25 mg, Cetrotide is strongly recommended to be administered every 24 hours. If the injection is missed, the injection should be given at a different time during the same day.
In severe allergic conditions, the use of Cetrotide should be avoided. Caution is required if there is a history of allergy or an active allergic process. It is very important that women inform their doctor about any allergy symptoms.
If OHSS occurs, appropriate therapy is indicated. Luteal phase support is carried out in accordance with the generally accepted practice of assisted reproductive technologies.
OHSS is seen as an inherent risk of gonadotropin stimulation of ovulation. Correlation with a shorter period of stimulation was observed with the use of gonadotropins in combination with GnRH antagonists, as well as with the use of lower doses of gonadotropins and lower concentrations of estradiol. Based on these observations, it can be assumed that the risk of developing OHSS is reduced when using GnRH antagonists.
From mild to severe OHSS can progress rapidly (from days to several days), therefore, after the administration of hCG, the patient should be monitored for at least 2 weeks.
To reduce the risk of developing OHSS, regular ultrasound examination and monitoring of the concentration of estradiol in the blood plasma are indicated. When a severe form of the syndrome develops, the gonadotropins, if they are still used, are immediately canceled.
The experience of repeated stimulation of ovulation with the use of Cetrotide is limited so far, therefore, before prescribing repeated courses, it is necessary to carefully compare the potential risks and expectations from treatment.
Influence on the ability to drive vehicles and complex mechanisms
Taking Cetrotide does not have any negative effect on the ability to concentrate, the speed of motor and mental reactions.
Application during pregnancy and lactation
Cetrotide is contraindicated in pregnancy and lactation. If the use of the drug is required during lactation, breastfeeding should be discontinued.
Pediatric use
In childhood, Cetrotide is not used.
With impaired renal function
Contraindicated in moderate or severe renal failure.
For violations of liver function
Contraindicated in moderate or severe hepatic impairment.
Use in the elderly
In old age, Cetrotide is not used.
Drug interactions
According to in vitro studies, it is unlikely that drug interactions will occur with the simultaneous use of Cetrotide and drugs that are metabolized with the participation of the cytochrome P450 system, undergo a glucuronidation reaction or any other conjugation.
There is no evidence of interactions of cetrorelix with other widely used drugs, in particular with gonadotropins and drugs that potentially induce the release of histamine in allergy-prone patients. Nevertheless, the possibility of interactions cannot be completely ruled out.
Before starting treatment with Cetrotide, a woman should tell her doctor what medications she is currently taking or has taken in the recent past.
Analogs
There is no information on analogues of Cetrotide.
Terms and conditions of storage
Shelf life is 2 years.
Store at temperatures up to 25 ° C out of reach of children.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Cetrotide
Reviews of Cetrotide confirm the high effectiveness of this drug when used according to indications. Additional advantages include the convenience of its use, namely the possibility of self-preparation and administration of the solution, as well as the painlessness of injections.
Almost all patients consider the disadvantage of Cetrotide to be a high cost, some women complain about the development of side effects, the most common of which are redness and itching at the injection site.
Price for Cetrotide in pharmacies
The approximate price for Cetrotide in a dosage of 0.25 mg is 1300-1470 rubles. per package, including 1 bottle, and 8600-10 900 rubles. per package containing 7 bottles. The cost of Cetrotide at a dosage of 3 mg is currently unknown, since the drug is not available commercially.
Cetrotide: prices in online pharmacies
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Drug name Price Pharmacy |
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Cetrotide 0.25 mg lyophilisate for the preparation of a solution for subcutaneous administration 7 pcs. RUB 6300 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
