Cetrorelix is indicated for assisted reproductive technologies.
Drugs affecting (inhibiting) gonadotrophin
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.
Cetrorelix Acetate 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. The onset of LH suppression is approximately two hours with the 0.25 mg dose. This suppression is maintained by continuous treatment and there is a more pronounced effect on LH than on FSH. An initial release of endogenous gonadotropins has not been detected with Cetrorelix injection, which is consistent with an antagonist effect.
The effects of Cetrorelix Acetate on LH and FSH are reversible after discontinuation of treatment. In women, Cetrorelix Acetate delays the LH-surge, and consequently ovulation, in a dose dependent fashion. FSH levels are not affected at the doses used during controlled ovarian stimulation. A dose of Cetrorelix Acetate 0.25 mg every 24 hours has been shown to maintain the effect.
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.
No formal drug-drug interaction studies have been performed with Cetrorelix Acetate. In vitro investigations have shown that interactions are unlikely with medicinal products that are metabolized by cytochrome P450 or glucuronised or conjugated in some other way. However, the possibility of interactions with gonadotropins or medicinal products that may induce histamine release in susceptible individuals, cannot be totally excluded.
Hypersensitivity. Moderate to severe renal or hepatic impairment. Women with severe allergic conditions. Pregnancy and lactation. Women with active allergic conditions or a history of allergies; childn; elderly >65 yrs.
Mild and transient reactions at Inj site, nausea, headache, ovarian hyperstimulation syndrome, systemic hypersensitivity reactions.
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.
If you think you have taken too much Cetrorelix Acetate, contact your healthcare professional, hospital emergency department or regional poison control centre immediately, even if there are no symptoms.
To be used immediately after reconstitution. Store in a refrigerator (2°C to 8°C temperature). Do not freeze. Keep away from light & wet place. Keep out of reach of children.
.png&w=384&q=75)