Nafarelin

Nafarelin (also known as Nafareline, Nafarelina, Nafarelinum, Lhrh, 6(d-nal(2))) is a anti-aging research peptide. Nafarelin is a gonadotropin-releasing hormone receptor agonist used in the management of endometriosis and central precocious puberty.

Nafarelin, also known as Synarel, is an FDA-approved gonadotropin-releasing hormone (GnRH) receptor agonist. It functions by initially stimulating and then desensitizing the GnRH receptor, leading to a reduction in gonadotropin secretion. This mechanism makes it effective for treating central precocious puberty (CPP) in children of both sexes, where it helps to suppress premature sexual development. Additionally, nafarelin is indicated for the management of endometriosis in women aged 18 and older, providing pain relief and reducing endometriotic lesions. Administered via nasal spray, its use has been studied in the context of various treatment strategies for endometriosis and the broader applications of GnRH agonists.

1 Mechanism of action

Gonadotropin-releasing hormone receptor agonist (agonist)

Primary targets: Gonadotropin-releasing hormone receptor

2 Reported effects

Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.

2.1 Indicated / studied for

• Endometriosis
• Central precocious puberty

2.2 Side effects

• Acne
• Transient breast enlargement
• Vaginal bleeding
• Emotional lability
• Transient increase in pubic hair
• Body odor
• Seborrhea
• Rhinitis
• White or brownish vaginal discharge

3 Chemical and physical properties

3.1 Amino acid sequence

4 Research dosages

1600 µg daily, or 1800 µg daily if adequate suppression cannot be achieved; 400 µg daily, or 800 µg daily for persistent regular menstruation after 2 months of treatment

5 Research studies (8)

1. Hereditary Coproporphyria
   (1993) · Review
2. Endometriosis: treatment strategies
   Annals of the New York Academy of Sciences (2003) · Review
3. Transdermal iontophoresis
   Expert opinion on drug delivery (2006) · Review
4. An overview of treatments for endometriosis
   JAMA (2015) · Review
5. Uses of GnRH agonists
   Journal of obstetric, gynecologic, and neonatal nursing : JOGNN (1994) · Review
6. Today's treatments: how do you choose?
   International journal of gynaecology and obstetrics: the official organ of the International Federation of Gynaecology and Obstetrics (1999) · Review
7. Elagolix (Orilissa)--an oral GnRH antagonist for endometriosis pain
   The Medical letter on drugs and therapeutics (2018) · Review
8. Efficacy of nafarelin in assisted reproductive technology: a meta-analysis
   Human reproduction update (2001) · RCT

6 Safety and risk profile

6.1 Regulatory status

Nafarelin is currently classified as FDA approved. Approval applies to specific clinical indications and dosing; research-grade material is not the approved product.

6.2 Contraindications

Conditions and populations in which use is contraindicated:

• Hypersensitivity to GnRH, GnRH agonist analogs, or excipients
• Undiagnosed abnormal vaginal bleeding
• Pregnancy or in women who may become pregnant
• Breast-feeding

6.3 Long-term risks

• psychiatric events (emotional lability, crying, irritability, impatience, anger, aggression)
• convulsions
• severe cutaneous adverse reactions (SJS/TEN, DRESS, acute gen)

6.4 Research best practices

• store upright at 25°C (77°F)
• excursions permitted to 15–30°C (59–86°F)
• protect from light

7 Frequently asked questions

What is nafarelin used for?

Nafarelin is used for the management of endometriosis, including pain relief and reduction of endometriotic lesions. It is also indicated for the treatment of central precocious puberty (CPP) in children, helping to suppress premature development of secondary sexual characteristics.

How does nafarelin work?

Nafarelin works as a gonadotropin-releasing hormone (GnRH) receptor agonist. It initially stimulates the GnRH receptor, but with continuous use, it desensitizes the receptor, leading to a decrease in the secretion of gonadotropins. This action ultimately suppresses the production of sex hormones.

Is nafarelin FDA approved?

Yes, nafarelin is FDA approved. It was first approved in 1990 and is marketed under the brand name Synarel for its indicated uses in endometriosis and central precocious puberty.

What are the side effects of nafarelin?

Common side effects of nafarelin can include acne, transient breast enlargement, vaginal bleeding, emotional lability, and a transient increase in pubic hair. Other reported effects include body odor, seborrhea, rhinitis, and white or brownish vaginal discharge.

How is nafarelin administered?

Nafarelin is administered via the nasal route. It is available as a nasal spray, which is the specified method of delivery for its therapeutic effects.

8 References

1. Nafarelin — compound summary PubChem. View source
2. Nafarelin — molecule record ChEMBL. View source
3. Nafarelin — FDA approved prescribing information U.S. Food and Drug Administration. View source
4. Nafarelin — published literature (270 records) PubMed. View source

9 See also

• Peptide encyclopedia index
• Peptide reconstitution calculator
• Glossary of peptide research terms