Cetrorelix

Cetrorelix Uses, Dosage, Side Effects, Food Interaction and all others data.

Cetrorelix, 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.

Cetrorelix 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. Cetrorelix 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.

Cetrorelix
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Cetrorelix
Availability	Prescription only
Generic	Cetrorelix
Cetrorelix Other Names	Cetrorelix, Cetrorelixum
Related Drugs	clomiphene, Clomid, chorionic gonadotropin (hcg), Pregnyl, Menopur
Weight	250mcg/vial, , 0.25mg, 3mg
Type	Sc Injection, Subcutaneous, Subcutaneous Powder For Injection, Injectable
Formula	C₇₀H₉₂ClN₁₇O₁₄
Weight	Average: 1431.038 Monoisotopic: 1429.669818444
Protein binding	86%
Groups	Approved, Investigational
Therapeutic Class	Drugs affecting (inhibiting) gonadotrophin
Manufacturer	Janata Traders
Available Country	Bangladesh, United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Cetrorelix is used for assisted reproductive technologies

Cetrorelix is also used to associated treatment for these conditions: Controlled Ovarian Stimulation

How Cetrorelix works

Cetrorelix 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

Cetrorelix 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.

Cetrorelix 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.