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Saturday, August 9, 2025

Gonadotropins


Generic and Brand Names

  • Human chorionic gonadotropin (hCG) — Pregnyl, Novarel, Ovidrel (recombinant form)

  • Human menopausal gonadotropins (hMG; menotropins) — Menopur, Repronex

  • Follitropin alfa (recombinant FSH) — Gonal-F

  • Follitropin beta (recombinant FSH) — Follistim AQ

  • Urofollitropin (purified urinary FSH) — Bravelle

  • Lutropin alfa (recombinant LH) — Luveris

Class

  • Gonadotropins are peptide hormones that regulate reproductive function

  • Include follicle-stimulating hormone (FSH), luteinizing hormone (LH), and human chorionic gonadotropin (hCG)

  • Used therapeutically to stimulate ovarian follicle development, ovulation, and spermatogenesis

Mechanism of Action

  • FSH: Stimulates growth and maturation of ovarian follicles in females; promotes spermatogenesis in males via Sertoli cell stimulation

  • LH: Triggers ovulation and corpus luteum formation in females; stimulates Leydig cells in males to produce testosterone

  • hCG: Mimics LH activity; supports corpus luteum and stimulates testosterone production

  • Exogenous administration induces ovarian stimulation for fertility treatment or testicular stimulation in hypogonadotropic hypogonadism

Indications

  • Female infertility due to anovulation or oligo-ovulation (with or without polycystic ovary syndrome)

  • Controlled ovarian hyperstimulation for assisted reproductive technologies (ART), e.g., in vitro fertilization (IVF)

  • Male infertility due to hypogonadotropic hypogonadism

  • Cryptorchidism in prepubertal boys (hCG)

  • Diagnostic evaluation of Leydig cell function (hCG stimulation test)

Dosage and Administration

  • Route: Intramuscular (IM) or subcutaneous (SC) injection depending on product

  • FSH/hMG (ovarian stimulation):

    • Start 75–150 IU daily for 5–7 days, adjust based on ovarian response (monitored via ultrasound and estradiol)

  • LH (with FSH):

    • Typically 75 IU daily in women with LH deficiency

  • hCG (ovulation trigger):

    • Single injection of 5,000–10,000 IU (urinary) or 250 mcg (recombinant) after adequate follicular development

  • hCG (male hypogonadotropic hypogonadism):

    • 1,000–2,000 IU 2–3 times weekly for several months, often combined with FSH

  • Dosing must be individualized and closely monitored to avoid ovarian hyperstimulation

Monitoring

  • Women: Ovarian follicle growth (ultrasound), serum estradiol levels, signs of ovarian hyperstimulation syndrome (OHSS)

  • Men: Testosterone levels, testicular volume, sperm count

  • General: Monitor for injection site reactions, weight gain, fluid retention

Contraindications

  • Primary ovarian failure (no response to gonadotropin stimulation)

  • Pregnancy or breastfeeding

  • Hormone-sensitive cancers (breast, ovarian, uterine, prostate)

  • Uncontrolled thyroid or adrenal dysfunction

  • Pituitary or hypothalamic tumors

  • Abnormal uterine bleeding of undiagnosed origin

  • Ovarian cysts not due to polycystic ovary syndrome

Precautions

  • High risk of multiple pregnancies with ovarian stimulation — counsel and monitor closely

  • Risk of OHSS, which can be life-threatening — monitor estradiol and ultrasound findings

  • Use only in specialized centers experienced in infertility management

  • Use cautiously in patients with cardiac or renal disease due to fluid retention risk

Adverse Effects

  • Common: Injection site pain/swelling, headache, fatigue, abdominal discomfort, bloating, mood changes

  • Female-specific: OHSS, multiple pregnancies, ovarian torsion

  • Male-specific: Gynecomastia, acne, mood swings

  • Rare: Thromboembolic events, allergic reactions

Drug Interactions

  • Concurrent use with clomiphene citrate or other ovulation-inducing drugs increases risk of OHSS

  • Androgens or estrogen therapy may modify gonadotropin effects

  • No significant CYP450-mediated interactions reported (peptide nature of drugs)

Overdose

  • Manifestations: OHSS, multiple follicle development, abdominal pain, ascites

  • Management: Discontinue therapy, provide supportive care, monitor hemodynamic status, consider hospitalization for severe OHSS

Patient Counselling

  • Explain purpose of therapy and need for frequent monitoring

  • Instruct on proper injection technique (IM or SC as per product)

  • Discuss risk of multiple births and OHSS

  • Advise to report symptoms of OHSS promptly (rapid weight gain, abdominal pain, swelling, shortness of breath)

  • Emphasize importance of adherence to dosing schedule and clinic visits




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