Cetrotide (cetrorelix) is a GnRH antagonist that inhibits ovulation by competing with gonadotrophins at receptors present in the pituitary gland. It inhibits the premature surge of LH in females undergoing controlled ovarian stimulation.

Cetrorelix Dose in Adults

For Controlled ovarian stimulation in conjunction with gonadotropins (Follicle stimulating hormone and human menopausal gonadotrophins):

• 0.25 mg as a subcutaneous injection once a day in the morning or evening of stimulation day 5 or morning of stimulation day 6
• continue 0.25 mg once a day until the day human chorionic gonadotrophin is administered.

Cetrorelix Dose in Children

Not applicable

Pregnancy Risk Factor X

• Pregnant females have experienced significant adverse drug reactions, including fetal abnormalities or fetal death.
• It is best to avoid it in pregnant women and those who might become pregnant.
• Before starting Cetrotide therapy, it is important to get rid of any pregnant women.

Cetrorelix use during breastfeeding:

• It is not recommended for lactating mothers.

Cetrorelix Dose in Renal Disease:

It is contraindicated in severe renal dysfunction. Mild to moderate renal dysfunction, has not been studied. Use with caution.

Cetrorelix Dose in Liver Disease:

It has not been studied in patients with liver disease. The manufacturer has not recommended any dose adjustment in patients with liver disease.

Common Side Effects Of Cetrorelix Include:

• Central nervous system:
  • Headache
• Gastrointestinal:
  • Nausea
• Endocrine & metabolic:
  • Ovarian hyperstimulation syndrome
  • Increased gamma-glutamyl transferase
• Hepatic:
  • Increased serum alkaline phosphatase
  • Increased serum ALT
  • Increased serum AST

Contraindications to Cetrotide (Cetrorelix) include:

• Pregnancy
• Breastfeeding
• Moderate to severe liver disease
• Allergy or sensitivity to cetrorelix, other hormones, peptides, gonadotropin-releasing hormone (GnRH), Mannitol, and any other component of the formulation
• Moderate to severe renal impairment

Warnings and Precautions

• After the first or second dose, severe allergic reactions and anaphylactoid reactions can occur (even months later).
• Patients with severe allergies should avoid Cetrotide treatment
• It is not intended for old patients (greater than 65 years of age).

Cetrorelix: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use  

Monitor:

Monitor follicle size (via ultrasound examination)

How to administer Cetrotide (Cetrorelix)?

Administer the drug by subcutaneous injection in the lower part of the abdomen around the nave but not very close to it (at 1-inch distance). Rotate the injection sites

Mechanism of action of Cetrotide (Cetrorelix):

• Cetrotide competes with the naturally-occurring Gonadotrophin-releasing hormone at receptors present in the pituitary. 
• Cetrotide delays the LH (luteinizing hormone) surge, which prevents ovulation.

The start of the action takes 2 hours to complete and 24 hours to complete. 

It works quickly absorbed

It is 86%.protein-bound. 

It is metabolized using peptidases.

Eliminating half-life is possibleAfter a single dose, it takes 5 hours and after multiple doses, 20.6 hours.

Time to get there peak plasma concentrationIt takes one to two hours. 

It isexcretedIn very small amounts in the urine or feces.

International Brands of Cetrorelix:

• Cetrotide
• Shionogi
• Nippon Kayaku

Cetrotide (Cetrorelix) Brands in Pakistan