Cetrorelix

Cetrorelix Brand Name– Cetrotide

What is Cetrorelix

Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonist activity similar to ganirelix.

The drug is used to inhibit premature leuteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation followed by insemination or assisted reproductive technology (ART) procedures; cetrorelix has also been used off-label for the treatment of endometriosis and benign prostatic hyperplasia (BPH).

Some data indicate that cetrorelix may also be effective in the treatment of uterine leiomyomata, ovarian cancer, and prostate cancer.

When used in infertility, the main advantage of GnRH antagonists versus GnRH agonists (e.g., leuprolide) is a reduction in the required fertility therapy cycle from several weeks (i.e., 3 weeks) to several days.

Secondarily, the onset of GnRH antagonists occurs rapidly after drug initiation, and the effects reverse rapidly, allowing pituitary function to return to baseline within 1—4 days after drug discontinuation.

Thus, pituitary and hormonal release is essentially normalized at the time of embryo transfer or implantation.

It was theorized that these properties would improve embryo viability and pregnancy success rates; however, results from meta-analyses comparing GnRH antagonists to GnRH agonists do not support this theory. 

FDA approval for cetrorelix was granted in August 2000.

Indications

  1. benign prostatic hyperplasia (BPH)
  2. endometriosis
  3. infertility

For inhibiting premature leuteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation and subsequent in vitro fertilization (IVF) or other assisted reproductive technology (ART) for the treatment of infertility

Side Effects

  1. abdominal pain
  2. anaphylactoid reactions
  3. antibody formation
  4. ecchymosis
  5. elevated hepatic enzymes
  6. erythema
  7. fetal death
  8. headache
  9. hot flashes
  10. hypotension
  11. injection site reaction
  12. menstrual irregularity
  13. nausea
  14. ovarian enlargement
  15. ovarian hyperstimulation syndrome (OHSS)
  16. pelvic pain
  17. pruritus
  18. rash
  19. teratogenesis
  20. vomiting

Monitoring Parameters

  • pelvic exam
  • pelvic ultrasound
  • serum estradiol concentrations
  • serum gonadotropin concentrations
  • weight

Contraindications

  • atopy
  • breast-feeding
  • children
  • geriatric
  • hepatic disease
  • mannitol hypersensitivity
  • obesity
  • ovarian cyst
  • ovarian failure
  • polycystic ovary syndrome
  • pregnancy
  • renal failure
  • renal impairment
  • tobacco smoking

Interactions

  • Aripiprazole
  • Asenapine
  • atypical antipsychotic
  • Brexpiprazole
  • Cariprazine
  • Cimetidine
  • Clozapine
  • Fluoxetine; Olanzapine
  • Haloperidol
  • Iloperidone
  • Loxapine
  • Lumateperone
  • Lurasidone
  • Molindone
  • Olanzapine
  • Paliperidone
  • Phenothiazines
  • Pimozide
  • Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
  • Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
  • Quetiapine
  • Risperidone
  • Tetrabenazine
  • Thiothixene
  • Ziprasidone
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