cetrorelix (Cetrotide)

Dosing and uses of Cetrotide (cetrorelix)

• Adult
• Pediatric

 

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