Some of these cookies are essential to the operation of the site,
while others help to improve your experience by providing insights into how the site is being used.
English to Chinese: Drug label General field: Medical Detailed field: Medical: Pharmaceuticals
Source text - English CETROTIDE - cetrorelix acetate
EMD Serono, Inc.
Cetrotide® (cetrorelix acetate for injection) is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic
activity. Cetrorelix acetate is an analog of native GnRH with substitutions of amino acids at positions 1, 2, 3, 6, and 10. The molecular formula is Acetyl-D-3-(2´-naphtyl)-alanine-D-4-chlorophenylalanine-D-3-(3´-pyridyl)-alanine- L-serine-L-tyrosine-D-citruline-L-leucine-L-arginine-L-proline-D-alanine-amide, and the molecular weight is 1431.06, calculated as the anhydrous free base. The structural formula is as follows:
Cetrotide® (cetrorelix acetate for injection) 0.25 mg or 3 mg is a sterile lyophilized powder intended for subcutaneous injection after
reconstitution with Sterile Water for Injection, USP (pH 5-8), that comes supplied in either a 1.0 mL (for 0.25 mg vial) or 3.0 mL
(for 3 mg vial) pre-filled syringe. Each vial of Cetrotide® 0.25 mg (multiple dose regimen) contains 0.26-0.27 mg cetrorelix acetate,
equivalent to 0.25 mg cetrorelix, and 54.80 mg mannitol. Each vial of Cetrotide® 3 mg (single dose regimen) contains 3.12-3.24 mg
cetrorelix acetate, equivalent to 3 mg cetrorelix, and 164.40 mg mannitol.
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.
Cetrotide® 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 one hour with the 3 mg dose and 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 Cetrotide®, which is consistent with an antagonist effect.
The effects of Cetrotide® on LH and FSH are reversible after discontinuation of treatment. In women, Cetrotide® delays the LHsurge, and consequently ovulation, in a dose-dependent fashion. FSH levels are not affected at the doses used during controlled
ovarian stimulation. Following a single 3 mg dose of Cetrotide®, duration of action of at least 4 days has been established. A dose of
Cetrotide® 0.25 mg every 24 hours has been shown to maintain the effect.