Gonadotropin-Releasing Hormone Agonist

Aka: Gonadotropin-Releasing Hormone Agonist, Gonadotropin Releasing Hormone Agonist, Gonadotropin-Releasing Hormone Analog, GnRH Agonist, Nafarelin Acetate, Synarel, Leuprolide, Lupron, Goserelin, Zoladex, Histrelin, Vantas, Triptorelin, Trelstar

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II. Indications

  1. Endometriosis
    1. Nafarelin Acetate (Synarel)
    2. Leuprolide (Lupron)
    3. Goserelin (Zoladex)
  2. Central Precocious Puberty
    1. Nafarelin Acetate (Synarel)
    2. Leuprolide (Lupron)
    3. Histrelin (Vantas)
    4. Triptorelin (Trelstar)
  3. Uterine Fibroids
    1. Leuprolide (Lupron)
  4. Prostate Cancer (Men with regionally advanced or metastatic cancer)
    1. Leuprolide (Lupron)
    2. Goserelin (Zoladex)
    3. Histrelin (Vantas)

III. Contraindications

  1. Pregnancy

IV. Mechanism

  1. Gonadotropin-Releasing Hormone (GnRH)
    1. GnRH is generated within hypothalamic Neurons (infundibular nucleus, arcuate nucleus)
    2. GnRH is released typically in pulses in men and women
      1. GnRH is also released in a surge before Ovulation
    3. GnRH binds receptors on the Pituitary Gland triggering release of gonadotropins
      1. Luteinizing Hormone (LH)
      2. Follicle Stimulating Hormone (FSH)
    4. Gonadotropins (LH, FSH) stimulate release of sex Hormones (e.g. Estrogen, Testosterone)
  2. GnRH Agonist
    1. GnRH Agonists are synthetic analogs of GnRH that disrupt normal pulsatile release of GnRH
      1. Hyperstimulates receptors (with initial transient increase in LH and FSH release)
      2. Results in Desensitization and down regulation of GnRH receptors
      3. Ultimately decreases LH and FSH release from the pituitary
    2. Effects
      1. Results in hypoestrogenism or pseudo-Menopause

V. Medications

  1. Leuprolide (Lupron)
  2. Goserelin (Zoladex)
  3. Histrelin (Vantas)
  4. Triptorelin (Trelstar)
  5. Nafarelin Acetate (Synarel)
    1. Endometriosis
      1. Dose 200 mg (1 spray) micro-g intranasally twice daily (alternating nostrils)
      2. Duration: 6 months
    2. Central Precocious Puberty
      1. Dose 2 sprays in each nostril twice daily (800 mcg twice daily)

VI. Dosing

  1. See other references

VII. Efficacy

  1. Endometriosis (Nafarelin)
    1. Effective at regression of lesions and relief of pain
    2. Does not cause the same androgenic effects as Danazol
    3. No proven effect on fertility

VIII. Adverse Effects: Women

  1. Menopausal symptoms
    1. Hot Flashes
    2. Insomnia
    3. Emotional changes (includes Major Depression)
  2. Bone density loss with prolonged use
    1. Consider add-back therapy with Norethindrone to reduce bone loss risk
  3. Ovarian Cysts
    1. May develop in first 2 months of medication use
  4. Other effects
    1. Vaginal Bleeding (initial first 1-2 months)
    2. Weight gain
    3. Fatigue
    4. Hyperglycemia
    5. Dyslipidemia
    6. Cognitive effects (decreased mental sharpness)
    7. QTc Prolongation (Leuprolide)

IX. Adverse Effects: Men (Prostate Cancer)

  1. Prostate Cancer initial flare
    1. Occurs with initial, transient increase in Testosterone
  2. Hot Flashes
  3. Erectile Dysfunction
  4. Testicular atrophy
  5. Gynecomastia
  6. Alopecia
  7. Other effects (similar to women)
    1. Weight gain
    2. Fatigue
    3. Hyperglycemia
    4. Dyslipidemia
    5. Cognitive effects (decreased mental sharpness)

X. Safety

  1. Pregnancy Category X
    1. Use reliable Contraception
  2. Avoid in Lactation

XI. Resources

  1. Nafarelin Acetate (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6
  2. Leuprolide (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=bec9077a-3f04-4887-856d-dde2de24584d
  3. Goserelin (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e4cb3c20-2738-400a-b522-3f36f71fe6c5
  4. Histrelin (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d8fb000e-3cc9-4803-b71d-2cc597661977
  5. Triptorelin (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f41380e7-b830-432d-a5f5-a872932f107e

XII. References

  1. (2022) Presc Lett, Medications to treat Prostate Cancer, Resource #380108
  2. Fairchild (2015) AJR Am J Roentgenol 204(6):W620-30 +PMID: 26001251 [PubMed]

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Related Studies

Cost: Medications

lupron (on 1/14/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
LUPRON DEPOT 11.25 MG 3MO KIT $4,546.75 each
LUPRON DEPOT 22.5 MG 3MO KIT $5,399.92 each
LUPRON DEPOT 3.75 MG KIT $1,505.48 each
LUPRON DEPOT 7.5 MG KIT $1,794.46 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

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