Short answer: Cetrorelix has a half-life of about 5 hours after one 0.25 mg dose (20.6 hours with repeated doses). Levels peak about 1 hour after a dose. People vary, so treat these as estimates.
Cetrorelix is a GnRH antagonist, a man-made peptide that blocks the GnRH receptor in the pituitary and quickly lowers LH and FSH. It is sold as Cetrotide (EMD Serono), a daily shot under the skin that stops an early LH surge (early ovulation) during IVF stimulation.
Also known as: Cetrotide, cetrorelix acetate.
Cetrotide comes as a 0.25 mg powder vial with a prefilled syringe of 1 mL sterile water, a 20 gauge needle for mixing and a 27 gauge needle for injecting. The solution is used right after mixing.
The Cetrotide label approves cetrorelix to prevent early LH surges in women having controlled ovarian stimulation. Label dosing is 0.25 mg under the skin of the lower belly once a day, starting on stimulation day 5 (morning or evening) or day 6 (morning), and continued until the day hCG is given; FSH or hMG starts on cycle day 2 or 3. In the studies the median length was 5 days. It is prescribed by fertility specialists, and women can self-inject after training.
The label has no boxed warning. It is not used with allergy to cetrorelix, mannitol or GnRH analogs, in pregnancy or breastfeeding, or with severe kidney impairment. Allergic reactions, including with the first dose, are the main precaution. In 949 women, moderate or severe OHSS was 3.5%, nausea 1.3% and headache 1.1%. Full numbers are on the Cetrotide side effects, Cetrotide dosing schedule and Cetrotide storage pages, and Cetrotide vs ganirelix compares the two antagonists.
The Cetrotide label gives a median time to peak of 1 hour after a 0.25 mg injection under the skin. The half-life was 5.0 hours after a single 0.25 mg dose (range 2.4 to 48.8) and 20.6 hours after repeated daily doses (range 4.1 to 179.3), and 62.8 hours after a single 3 mg dose.
Numbers shown are taken from the source above. Half-life varies from person to person.
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