Generic
Cetrorelix
2 brands available in the market
At a glance
Cetrorelix is an anti-gonadotropin-releasing hormone medicine used in the treatment of infertility in females by restricting egg release and preventing premature ovulation.
Description
Cetrorelix is an anti-gonadotropin-releasing hormone medicine. It is used in the treatment of infertility in females. It restricts eggs to release directly and prevents premature ovulation. Cetrorelix is injecting directly into the skin under the supervision of a doctor. Do not self administer the injection. Your doctor or nurse may help you to know the best way to inject the medicine at home. The dose and how often you take it depends on what you are taking it for. Your doctor will decide how much you need to improve your symptoms. You should take this medicine for as long as it is prescribed for you. The most common side effects of this medicine include injection site reaction (redness, itching, and irritation), nausea and vomiting. To overcome irritation at the injection site, use a different part of belly every day to inject the medicine. Some side effects may mean you should inform your doctor immediately include dizziness, faint, abdominal pain, and vomiting. Before taking this medicine, tell your doctor if you have ever had liver or kidney disease or if you are breastfeeding to a baby. Your doctor should also know about all other medicines you are taking as many of these may make this medicine less effective or change the way it works.
In females undergoing treatment for infertility, sometimes premature ovulation can lead to the release of eggs which are not ready for fertilisation. Cetrorelix blocks the action of a natural hormone and prevents premature release of the eggs from the ovary.
Indications
- Female infertility
- Prevention of premature ovulation in assisted reproductive technologies
Therapeutic class
Drugs affecting (inhibiting) gonadotrophin
Pharmacological class
Gonadotropin-Releasing Hormone (GnRH) Antagonist
Pharmacology
Cetrorelix Acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. Cetrorelix Acetate blocks the effects of GnRH. GnRH controls the secretion of luteinizing hormone (LH), which induces ovulation during the menstrual cycle. During hormone treatment for ovarian stimulation, premature ovulation may lead to eggs that are not suitable for fertilization. Cetrorelix Acetate blocks such undesirable premature ovulation. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotropic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels.
Mechanism of action
Cetrorelix, a synthetic decapeptide analog of naturally occurring gonadorelin, is a gonadorelin antagonist. It competitively blocks gonadorelin receptors on the anterior pituitary gonadotroph and the subsequent transduction pathway, inducing a rapid, reversible suppression of gonadotrophin secretion.
Dosage
Adult Dose (Subcutaneous): Assisted reproductive technologies: 0.25 mg cetrorelix (as acetate) beginning on day 5 or 6 of ovarian stimulation in the morning or in the evening beginning on day 5, and continued until ovulation induction.
Renal Dose: Severe renal impairment: Contraindicated.
Administration
Your doctor or nurse will give you this medicine. Kindly do not self administer.
Use immediately after reconstitution. Allow the medicine to reach room temperature before injection (remove from refrigerator approximately 30 minutes before use). Inject into the lower abdominal wall, choosing a different site each day.
Missed dose
If you miss a dose of Cetrorelix, please consult your doctor.
Side effects
Common Side Effects:
- Nausea
- Ovarian hyperstimulation syndrome (OHSS)
- Injection site reactions (pain, swelling, redness)
- Itching
- Irritation
- Vomiting
- Lower abdominal pain
Precautions & warnings
- [SAFE] Cetrorelix does not usually affect your ability to drive.
- Cetrorelix helps prevent premature ovulation in women undergoing assisted reproduction treatments such as IVF.
- It is given as an injection under the skin (subcutaneously), preferably of the upper leg.
- Inform your doctor immediately if you get very dizzy, faint, vomit, or have diarrhea while using this medicine. These could be symptoms of ovarian hyperstimulation syndrome (OHSS).
- Do not use this medicine if you are already pregnant or breastfeeding.
Contraindications
- Hypersensitivity
- Moderate to severe renal or hepatic impairment
- Women with severe allergic conditions
- Pregnancy and lactation
Drug interactions
Interactions are unlikely with medications that are metabolised by cytochrome P-450 or glucuronised or conjugated in some other way. However, the possibility of interactions with commonly used medicinal products cannot entirely be excluded. The possibility of interactions with gonadotropins or medicinal products that may induce histamine release in susceptible individuals cannot be totally excluded.
Food interactions
[CAUTION] Caution is advised when consuming alcohol with Cetrorelix. Please consult your doctor.
Use in pregnancy
[UNSAFE] Cetrorelix is highly unsafe to use during pregnancy. Studies on pregnant women and animals have shown significant harmful effects to the developing baby. Seek your doctor's advice.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
[UNSAFE] Cetrorelix is unsafe to use during breastfeeding. Data suggests that the drug may cause toxicity to the baby.
Pediatric use
The safety and effectiveness of Cetrorelix in pediatric patients have not been established.
Geriatric use
Limited information is available on dose adjustment for elderly patients.
Renal / hepatic impairment
[CAUTION] Cetrorelix should be used with caution in patients with kidney disease. Dose adjustment of Cetrorelix may be needed. Please consult your doctor. Use of Cetrorelix is not recommended in patients with severe kidney disease.
[CAUTION] Cetrorelix should be used with caution in patients with liver disease. Dose adjustment of Cetrorelix may be needed. Please consult your doctor.
Overdose effects
If you think you have taken too much Cetrorelix, contact your healthcare professional, hospital emergency department or regional poison control centre immediately, even if there are no symptoms.
Storage conditions
Use immediately after reconstitution. Store in a refrigerator (2°C to 8°C). Do not freeze. Keep away from light & wet place. Keep out of reach of children.
Chemical structure
Cetrorelix Acetate