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Cetrorelix

Medically reviewed by Drugs.com. Last updated on Feb 13, 2019.

Pronunciation

(set roe REL iks)

Index Terms

  • Cetrorelix Acetate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Kit, Subcutaneous:

Cetrotide: 0.25 mg [contains mannitol]

Brand Names: U.S.

  • Cetrotide

Pharmacologic Category

  • Gonadotropin Releasing Hormone Antagonist

Pharmacology

Competes with naturally-occurring GnRH for binding on receptors of the pituitary. This delays luteinizing hormone surge, preventing ovulation until the follicles are of adequate size.

Absorption

Rapid

Distribution

Vd: ~1 L/kg

Metabolism

Transformed by peptidases; cetrorelix and peptides (1-9), (1-7), (1-6), and (1-4) are found in the bile; peptide (1-4) is the predominant metabolite

Excretion

Feces (5% to 10% as unchanged drug and metabolites); urine (2% to 4% as unchanged drug)

Onset of Action

0.25 mg dose: 2 hours

Time to Peak

1 to 2 hours

Duration of Action

0.25 mg dose: 24 hours

Half-Life Elimination

0.25 mg dose: 5 hours; 0.25 mg multiple doses: 20.6 hours

Protein Binding

86%

Use: Labeled Indications

Controlled ovarian stimulation: Inhibition of premature luteinizing hormone (LH) surges in women undergoing controlled ovarian stimulation

Contraindications

Hypersensitivity to cetrorelix, extrinsic peptide hormones, gonadotropin releasing hormone (GnRH) or other GnRH analogs, mannitol, or any component of the formulation; severe renal impairment; pregnancy; breast-feeding.

Canadian labeling: Additional contraindications (not in the US labeling): Moderate to severe hepatic function; moderate renal function.

Dosing: Adult

Controlled ovarian stimulation in conjunction with gonadotropins (FSH, hMG): Female: SubQ: 0.25 mg once daily the morning or evening of stimulation day 5, or morning of stimulation day 6; continue 0.25 mg once daily until the day hCG is administered.

Dosing: Geriatric

Not intended for use in women ≥65 years of age

Reconstitution

Reconstitute vial using supplied 1 mL SWFI prefilled syringe (and supplied 20-gauge needle). Inject SWFI slowly into vial. With syringe still in vial, gently swirl vial until solution is clear; avoid forming bubbles. Withdraw entire contents from vial. Replace 20-gauge needle with supplied 27-gauge needle prior to injection.

Administration

SubQ: Administer by SubQ injection following proper aseptic technique procedures. Injections should be to the lower abdomen, preferably around the navel (but staying at least 1 inch from the navel). The injection site should be rotated daily.

Storage

Store refrigerated at 2°C to 8°C (36°F to 46°F). Store in outer carton to protect from light.

Drug Interactions

Indium 111 Capromab Pendetide: Antigonadotropic Agents may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Avoid combination

Adverse Reactions

1% to 10%:

Central nervous system: Headache (1%)

Endocrine & metabolic: Ovarian hyperstimulation syndrome (WHO grade II or III: 4%), increased gamma-glutamyl transferase (≤1% to 2%)

Gastrointestinal: Nausea (1%)

Hepatic: Increased serum alkaline phosphatase (≤1% to 2%), increased serum ALT (≤1% to 2%), increased serum AST (≤1% to 2%)

<1%, postmarketing and/or case reports: Anaphylaxis (includes cough, hypotension, skin rash), injection site reactions (bruising at injection site, erythema at injection site, injection site pruritus, local swelling)

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity: Hypersensitivity reactions, including severe anaphylactoid reactions, have been reported after initial dose and months after starting therapy; use with caution in patients with signs and symptoms of active allergic conditions or known history of allergic predisposition. Treatment is not recommended in patients with severe allergic conditions.

Other warnings/precautions:

• Experienced specialists: Should only be prescribed by fertility specialists.

Monitoring Parameters

Ultrasound to assess follicle size

Pregnancy Considerations

Studies in animals or pregnant women have shown evidence of fetal abnormalities and use is contraindicated in women who are or may become pregnant. Resorption resulting in fetal loss would be expected if used in a pregnant woman. Exclude pregnancy before beginning treatment.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience injection site edema, itching, or redness. Have patient report immediately to prescriber severe dizziness, passing out, cough, or signs of ovarian hyperstimulation syndrome (severe abdominal pain or bloating; severe nausea, vomiting, or diarrhea; excessive weight gain; shortness of breath; or change in amount of urine passed) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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