Cetrorelixum
Cetrorelixum Uses, Dosage, Side Effects, Food Interaction and all others data.
Cetrorelixum, a synthetic decapeptide analog of naturally occurring gonadorelin, is a gonadorelin antagonist. It competitively blocks gonadorelin receptors on the anterior piyuitary gonadotroph and the subsequent transduction pathway, inducing a rapid, reversible suppression of gonadotrophin secretion.
Cetrorelixum is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic 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. Cetrorelixum competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner.
Trade Name | Cetrorelixum |
Availability | Prescription only |
Generic | Cetrorelix |
Cetrorelix Other Names | Cetrorelix, Cetrorelixum |
Related Drugs | clomiphene, Clomid, chorionic gonadotropin (hcg), Pregnyl, Menopur |
Type | |
Formula | C70H92ClN17O14 |
Weight | Average: 1431.038 Monoisotopic: 1429.669818444 |
Protein binding | 86% |
Groups | Approved, Investigational |
Therapeutic Class | Drugs affecting (inhibiting) gonadotrophin |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Cetrorelixum is used for assisted reproductive technologies
Cetrorelixum is also used to associated treatment for these conditions: Controlled Ovarian Stimulation
How Cetrorelixum works
Cetrorelixum binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner.
Dosage
Cetrorelixum dosage
Adult:250 mcg/day, given either in the morning beginning on the day 5 or 6 of ovarian stimulation or in the evening beginning on day 5, and continued until ovulation induction.
Side Effects
Mild and transient reactions at Inj site, nausea, headache, ovarian hyperstimulation syndrome, systemic hypersensitivity reactions.
Precaution
Women with active allergic conditions or a history of allergies; childn; elderly >65 yrs
Food Interaction
No interactions found.Cetrorelixum Disease Interaction
Major: severe allergies, severe renal impairmentModerate: hepatic impairment
Volume of Distribution
- 1.16 L/kg
Elimination Route
Rapidly absorbed following subcutaneous injection. The mean absolute bioavailability following subcutaneous administration to healthy female subjects is 85%.
Half Life
~62.8 hours
Clearance
- 1.28 ml/min·kg [adult healthy female with 3 mg single SC administration]
Elimination Route
Following subcutaneous administration of 10 mg cetrorelix to males and females, only unchanged cetrorelix was detected in urine.
Pregnancy & Breastfeeding use
Pregnancy Category X. Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Contraindication
Hypersensitivity. Moderate to severe renal or hepatic impairment. Women with severe allergic conditions. Pregnancy and lactation.
Storage Condition
Store cetrorelix acetate at room temperature, between 15 to 30° C
Innovators Monograph
You find simplified version here Cetrorelixum
Cetrorelixum contains Cetrorelix see full prescribing information from innovator Cetrorelixum Monograph, Cetrorelixum MSDS, Cetrorelixum FDA label