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
Cetrorelixum
Cetrorelixum

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.

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

*** Taking medicines without doctor's advice can cause long-term problems.
Share