II. Indications
-
Endometriosis
- Nafarelin Acetate (Synarel)
- Leuprolide (Lupron)
- Goserelin (Zoladex)
- Central Precocious Puberty
- Nafarelin Acetate (Synarel)
- Leuprolide (Lupron)
- Histrelin (Vantas)
- Triptorelin (Trelstar)
-
Uterine Fibroids
- Leuprolide (Lupron)
-
Prostate Cancer (Men with regionally advanced or metastatic cancer)
- Leuprolide (Lupron)
- Goserelin (Zoladex)
- Histrelin (Vantas)
III. Contraindications
- Pregnancy
IV. Mechanism
- Gonadotropin-Releasing Hormone (GnRH)
- GnRH is generated within hypothalamic Neurons (infundibular nucleus, arcuate nucleus)
- GnRH is released typically in pulses in men and women
- GnRH binds receptors on the Pituitary Gland triggering release of gonadotropins
- Gonadotropins (LH, FSH) stimulate release of sex Hormones (e.g. Estrogen, Testosterone)
- GnRH Agonist
- GnRH Agonists are synthetic analogs of GnRH
- When GnRH (e.g. Gonadorelin) is given in IV pulses, 90 min apart, they trigger Ovulation
- Pulsatile GnRH release mimics in vivo GnRH release that triggers FSH and LH release
- May be used in Female Infertility due to central Hypogonadism to trigger Ovulation
- When GnRH Agonists are used continuously they disrupt normal pulsatile release of GnRH
- Hyperstimulates receptors (with initial transient increase in LH and FSH release)
- Results in Desensitization and down regulation of GnRH receptors
- Ultimately decreases LH and FSH release from the pituitary
- Results in hypoestrogenism or pseudo-Menopause and is used in Prostate Cancer and Endometriosis
- Images
V. Medications
- Leuprolide (Lupron)
- Goserelin (Zoladex)
- Histrelin (Vantas)
- Triptorelin (Trelstar)
- Nafarelin Acetate (Synarel)
- Endometriosis
- Dose 200 mg (1 spray) micro-g intranasally twice daily (alternating nostrils)
- Duration: 6 months
- Central Precocious Puberty
- Dose 2 sprays in each nostril twice daily (800 mcg twice daily)
- Endometriosis
VI. Dosing
- See other references
VII. Efficacy
-
Endometriosis (Nafarelin)
- Effective at regression of lesions and relief of pain
- Does not cause the same androgenic effects as Danazol
- No proven effect on fertility
VIII. Adverse Effects: Women
- Menopausal symptoms
- Hot Flashes
- Insomnia
- Emotional changes (includes Major Depression)
- Bone density loss with prolonged use
- Consider add-back therapy with Norethindrone to reduce bone loss risk
-
Ovarian Cysts
- May develop in first 2 months of medication use
- Other effects
- Vaginal Bleeding (initial first 1-2 months)
- Weight gain
- Fatigue
- Hyperglycemia
- Dyslipidemia
- Cognitive effects (decreased mental sharpness)
- QTc Prolongation (Leuprolide)
IX. Adverse Effects: Men (Prostate Cancer)
-
Prostate Cancer initial flare
- Occurs with initial, transient increase in Testosterone
- Hot Flashes
- Erectile Dysfunction
- Testicular atrophy
- Gynecomastia
- Alopecia
- Other effects (similar to women)
- Weight gain
- Fatigue
- Hyperglycemia
- Dyslipidemia
- Cognitive effects (decreased mental sharpness)
X. Safety
- Pregnancy Category X
- Use reliable Contraception
- Avoid in Lactation
XI. Resources
- Nafarelin Acetate (DailyMed)
- Leuprolide (DailyMed)
- Goserelin (DailyMed)
- Histrelin (DailyMed)
- Triptorelin (DailyMed)
XII. References
- (2022) Presc Lett, Medications to treat Prostate Cancer, Resource #380108
- Fairchild (2015) AJR Am J Roentgenol 204(6):W620-30 +PMID: 26001251 [PubMed]
Images: Related links to external sites (from Bing)
Related Studies
| 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 | |