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Cetrorelix

Medically reviewed by Drugs.com. Last updated on May 6, 2020.

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

Reproductive Considerations

Evaluate pregnancy status before beginning treatment.

Pregnancy Considerations

Use is contraindicated in females who are pregnant. Resorption resulting in fetal loss would be expected if used in a pregnant woman.

Patient Education

What is this drug used for?

• It is used to help women get pregnant.

• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Injection site swelling, itching, or redness

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Severe dizziness

• Passing out

• Cough

• Ovarian hyperstimulation syndrome like severe abdominal pain or bloating; severe nausea, vomiting, or diarrhea; excessive weight gain; shortness of breath; or change in amount of urine passed

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

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