Nafarelin
Also known as: Nafarelin, Nafarelin acetate, RS-94991, RS-94991-298, Synarel
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Summary
Nafarelin acetate is a synthetic decapeptide analog of gonadotropin‑releasing hormone used to suppress estrogen or testosterone production in conditions such as endometriosis and prostate cancer.
Mechanism of Action
Continuous stimulation of GnRH receptors leads to down‑regulation of LH/FSH secretion and suppression of sex steroid production.
Routes of Administration
Goals & Uses
- Treatment of endometriosisGynecologyHigh
- Treatment of central precocious pubertyPediatric EndocrinologyHigh
- Uterine fibroids (leiomyomata) managementGynecologyModerate
- Estrogen suppression for endometriosis‑related painGynecologicalHigh
- Ovarian stimulation suppression in assisted reproductionReproductive MedicineModerate
- Testosterone suppression in advanced prostate cancerOncologyHigh
Contraindications
- Known hypersensitivity to Nafarelin or excipientsAllergyHigh
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- BreastfeedingPopulationHighPotential transfer into breast milk or insufficient safety data
- Undiagnosed abnormal vaginal bleedingGynecologyHigh
- Hypersensitivity to GnRH or GnRH analogsAllergy / ImmunologyHigh
- Osteoporosis or significant bone lossMusculoskeletalModerate
Adverse Effects
- Nasal irritation / rhinitisLocal/NasalCommon
- Nasal irritationLocal/NasalCommon
- HeadacheNeurologicCommonPain in the head or upper neck
- Decreased bone mineral densityMusculoskeletalCommon
- Hot flashesEndocrine / VasomotorCommon
- Mood changes / depressionPsychiatricUncommon
- Bone mineral density lossSkeletalRare
- Vaginal drynessGynecologicCommon
Drug Interactions
- Estrogen replacement therapyModerate
- Nasal decongestants (topical)Moderate
- Sex hormone preparations (estrogens, androgens, progestogens)Moderate
- Cytochrome P450 inhibitors (e.g., ketoconazole)Low
Population Constraints
- Pediatric patientsAgeRelative
- Patients with history of osteoporosisMusculoskeletalRelative
- Patients with chronic nasal conditionsENTRelative
- Pediatric patients under 2 yearsAgeAbsolute
- Elderly patients with severe hepatic impairmentOrgan FunctionRelative
- Adolescents with central precocious pubertyPediatricRelative
Regulatory Status
- European UnionApprovedApproved: endometriosis‑related painAvailable as nasal spray; no approved indication for prostate cancer in EU.
- United StatesApprovedApproved: endometriosis‑related pain, palliative treatment of advanced prostate cancerApproved as nasal spray (Synarel) for endometriosis; depot injection approved for prostate cancer.
- United KingdomApprovedApproved: Endometriosis, Central precocious pubertyApproved by MHRA; marketed as Synarel in the UK.
Administered as a nasal spray (Synarel) in the US; depot injection formulations are available in some markets for prostate cancer.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Nafarelin?
Nafarelin acetate is a synthetic decapeptide analog of gonadotropin‑releasing hormone used to suppress estrogen or testosterone production in conditions such as endometriosis and prostate cancer.
What is Nafarelin used for?
Nafarelin is educationally associated with: Treatment of endometriosis, Treatment of central precocious puberty, Uterine fibroids (leiomyomata) management, Estrogen suppression for endometriosis‑related pain, Ovarian stimulation suppression in assisted reproduction, Testosterone suppression in advanced prostate cancer. Educational only — not medical advice.
How is Nafarelin administered?
Recorded routes of administration: Intramuscular, Nasal, Subcutaneous.
What are the potential side effects of Nafarelin?
Reported adverse effects include: Nasal irritation / rhinitis, Nasal irritation, Headache, Decreased bone mineral density, Hot flashes, Mood changes / depression, Bone mineral density loss, Vaginal dryness. This list is not exhaustive — consult a qualified clinician.
Who should avoid Nafarelin?
Recorded contraindications: Known hypersensitivity to Nafarelin or excipients, Pregnancy, Breastfeeding, Undiagnosed abnormal vaginal bleeding, Hypersensitivity to GnRH or GnRH analogs, Osteoporosis or significant bone loss. Consult a qualified clinician before use.