Cetrorelix


Concise Prescribing Info
Indications/Uses
Ovarian stimulation regimens for assisted reproduction in infertility.
Dosage/Direction for Use
Adult : SC In conjunction w/ urinary or recombinant gonadotropins: 0.25 mg once daily, given either in the morning of day 5 or 6 or in the evening of day 5 of ovarian stimulation, and continued until ovulation induction.
Dosage Details
Subcutaneous
Ovarian stimulation regimens for assisted reproduction in infertility
Adult: In conjunction w/ urinary or recombinant gonadotropins: 0.25 mg once daily into the lower abdominal wall, beginning either in the morning of day 5 or 6 of ovarian stimulation, continued throughout gonadotropin treatment period including the day of ovulation induction; or in the evening of day 5, continued throughout gonadotropin treatment period until the evening prior to the day of ovulation induction.
Renal Impairment
Moderate to severe: Contraindicated.
Hepatic Impairment
Moderate to severe: Contraindicated.
Reconstitution
Reconstitute w/ sterile water for inj.
Contraindications
Hypersensitivity to cetrorelix, extrinsic peptide hormones, or GnRH analogues. Postmenopausal women. Moderate to severe renal and hepatic impairment. Pregnancy and lactation.
Special Precautions
Patient w/ active allergic condition, history of allergic predisposition.
Adverse Reactions
Mild to moderate ovarian hyperstimulation syndrome (OHSS); transient reaction at inj site (e.g. erythema, pruritus, swelling); nausea, headache.
Potentially Fatal: Rarely, severe anaphylactoid reactions (associated w/ cough, rash, hypotension).
Parenteral/SC: X
MonitoringParameters
Perform ultrasound to monitor follicle size.
Action
Description: Cetrorelix, a synthetic gonadorelin or gonadotropin releasing hormone (GnRH) analogue, is a competitive antagonist of naturally-occurring GnRH for binding on anterior pituitary receptors. This delays premature luteinising hormone (LH) surge, thereby suppressing ovulation, oocytic meiosis, and luteinisation.
Onset: 2 hr.
Duration: 24 hr.
Pharmacokinetics:
Absorption: Rapidly absorbed. Bioavailability: Approx 85%. Time to peak plasma concentration: 1-2 hr.
Distribution: Volume of distribution: Approx 1 L/kg. Plasma protein binding: 86%.
Metabolism: Metabolised by peptidases, predominantly into (1-4) peptide and into (1-9), (1-7), and (1-6) peptides.
Excretion: Via faeces (5-10% as unchanged drug and metabolites) and urine (2-4% as unchanged drug). Terminal elimination half-life: 30 hr.
Chemical Structure

Chemical Structure Image
Cetrorelix

Source: National Center for Biotechnology Information. PubChem Database. Cetrorelix, CID=25074887, https://pubchem.ncbi.nlm.nih.gov/compound/Cetrorelix (accessed on Jan. 21, 2020)

Storage
Store below 25°C. Protect from light.
ATC Classification
H01CC02 - cetrorelix ; Belongs to the class of anti-gonadotropin-releasing hormones. Used in hypothalamic hormone preparations.
References
Anon. Cetrorelix. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/12/2016.

Buckingham R (ed). Cetrorelix Acetate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/12/2016.

Cetrotide (EMD Serono, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 02/12/2016.

Joint Formulary Committee. Cetrorelix. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/12/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Cetrorelix Acetate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 02/12/2016.

Disclaimer: This information is independently developed by MIMS based on Cetrorelix from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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