cetrorelix (Cetrotide)
Classes: Gonadotropin Releasing Hormone Agonists; Gonadotropin Releasing Hormone Antagonists
Dosing and uses of Cetrotide (cetrorelix)
Adult dosage forms and strengths
injectable solution
- 0.25mg
- 3mg
Infertility Treatment
Single dose regimen: 3 mg SC when serum estradiol levels show appropriate stimulation response (range days 5-9) usually day 7; if hCG not administered within 4 days, continue dose at 0.25 mg/day until hCG administered
Multiple dose regimen: 0.25 mg SC morning or evening of stimulation day 5 or morning of stimulation day 6; continue until hCG administered
Renal Impairment
Mild-to-moderate impairment: Dose adjustment not described by manufacturer
Severe renal impairment: Contraindicated
Hepatic Impairment
Dose adjustment not described by manufacturer
Pediatric dosage forms and strengths
Not recommended
Cetrotide (cetrorelix) adverse (side) effects
1-10%
Ovarian hyperstimulation syndrome (4%)
Nausea (1%)
Hepatic enzyme elevation (1-2%)
Headache (1%)
<1%
Erythema at injection site
Itching
Pruritus
Swelling
Redness
Hypotension
Rash
Cough
Warnings
Contraindications
Pregnancy
Hypersensitivity
Breastfeeding
Cautions
May cause elevations of hepatic enzymes: ALT, AST, GGT, Ap
Exclude pregnancy before initiating therapy
Monitor closely for hypersensitivity following first injection
Pregnancy and lactation
Pregnancy category: X
Lactation: Excretion in milk unknown/contraindicated
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Cetrotide (cetrorelix)
Mechanism of action
Gonadotropin releasing-hormone (luteinizing hormone-releasing hormone) antagonist; delays luteinizing hormone surge, which in turn prevents ovulation until follicles are of adequate size
Pharmacokinetics
Half-Life: 20-63 hr
Onset: within 12 hr
Peak Plasma Time: 1 hr (0.25mg dose); 1.5 hr (3 mg dose)
Bioavailability: 85% (SC)
Protein Bound: 86%
Duration: 4 days (3 mg dose)
Absorption: Rapid
Vd: 1.2 L/kg
Excretion: Feces; urine
