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Indications and Dosage
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.
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Renal Impairment
Moderate to severe: Contraindicated.
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Hepatic Impairment
Moderate to severe: Contraindicated.
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Reconstitution
Reconstitute w/ sterile water for inj.
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Contraindications
Hypersensitivity to cetrorelix, extrinsic peptide hormones, or GnRH analogues. Postmenopausal women. Moderate to severe renal and hepatic impairment. Pregnancy and lactation.
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Special Precautions
Patient w/ active allergic condition, history of allergic predisposition.
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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). |
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Parenteral/SC: X
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Monitoring Parameters
Perform ultrasound to monitor follicle size.
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Action
Description:
Mechanism of Action: 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. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Cetrorelix, CID=25074887, https://pubchem.ncbi.nlm.nih.gov/compound/Cetrorelix (accessed on Jan. 21, 2020) |
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Storage
Store below 25°C. Protect from light.
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MIMS Class
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ATC Classification
H01CC02 - cetrorelix ; Belongs to the class of anti-gonadotropin-releasing hormones. Used in hypothalamic hormone preparations.
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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.
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