Nafarelin
 | |
| Clinical data | |
|---|---|
| Trade names | Synarel, Nasanyl, others |
| Other names | Nafareline; Nafarelin acetate; RS-94991; RS-94991-298; [6-D-(2-naphthyl)alanine]-GnRH |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a601082 |
| Pregnancy category |
|
GnRH agonist; Antigonadotropin | |
| ATC code | |
| Legal status | |
| Legal status |
|
SC: 86 hours (metabolites)[2] | |
| Excretion | Urine: 44–55%[2] Feces: 19–44%[2] |
| Identifiers | |
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JSmol) | |
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| (verify) | |
Nafarelin, sold under the brand name Synarel among others, is a gonadotropin-releasing hormone agonist (GnRH agonist) medication which is used in the treatment of endometriosis and early puberty.[1][2] It is also used to treat uterine fibroids, to control ovarian stimulation in in vitro fertilization (IVF), and as part of transgender hormone therapy.[3][4][5][6] The medication is used as a nasal spray two to three times per day.[1][2][7]
Nafarelin was introduced for medical use in 1990.[9][1][10] It is available widely throughout the world, including in North America, Europe, and elsewhere throughout the world.[11][12] The medication is one of only two medically used GnRH analogues that are available as nasal sprays, the other being buserelin.[13]
Medical uses
Nafarelin is approved and used in the treatment of
Dosages
Nafarelin is used to treat precocious puberty at a dosage of 1,600 to 1,800 μg per day.[2] The 1,600 μg/day dosage is achieved by two sprays (400 μg total) into each nostril in the morning (four sprays, 800 μg total) and two sprays (400 μg total) into each nostril in the evening (four sprays, 800 μg total).[2] If 1,600 μg/day is insufficient for adequate pubertal suppression, the 1,800 μg/day dosage can be used instead. This is achieved by three sprays (600 μg total) into alternating nostrils three times per day (nine sprays per day total).[2] When administering the sprays, the head should be tilted back slightly and 30 seconds should elapse between each spray.[2] A bottle of nafarelin nasal spray (brand name Synarel) lasts for about 7 days at a dosage of 1,600 μg/day.[2]
Nafarelin is used to treat endometriosis at lower dosages of 400 to 800 μg per day.[2] This is achieved by one or two sprays (200 or 400 μg total) into alternating nostrils once in the morning and once in the evening (two to four sprays per day total).[2] A bottle of nafarelin nasal spray (brand name Synarel) lasts for about 30 days at a dosage of 400 μg/day.[2]
Available forms
Nafarelin is available in the form of a 0.2%
Side effects
Pharmacology
Pharmacodynamics
Nafarelin is a
Pharmacokinetics
The
Chemistry
Nafarelin is a
History
Nafarelin was introduced for medical use in 1990.[9][1][10]
Society and culture
Generic names
Nafarelin is the
Brand names
The major brand names of nafarelin are Synarel and Synarela.[12][11] It has also been marketed under a number of other brand names including Synrelin, Synrelina, Nafarelil 0.2%, and Nasanyl 0.2%.[12][11]
Availability
Nafarelin is available widely throughout the world, including in the United States, Canada, the United Kingdom, Ireland, other European countries, Australia, Israel, Argentina, Brazil, Mexico, and Japan.[12][11]
See also
References
- ^ PMID 2140979.
- ^ a b c d e f g h i j k l m n o p q r s t u v w x y z aa ab ac ad ae af ag ah https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019886s033s035lbl.pdf [bare URL PDF]
- ^ PMID 10900582.
- ^ ISBN 3-8047-1763-2.
- ^ PMID 27241976.
- ^ PMID 23385274.
- PMID 22028996.
- ISBN 978-1-78262-732-6.
- ^ a b "Drugs@FDA: FDA-Approved Drugs".
- ^ PMID 1984190.
- ^ a b c d e f "Nafarelin nasal Uses, Side Effects & Warnings".
- ^ ISBN 978-3-88763-075-1.
- ISBN 978-3-642-37250-6.
- ^ PMID 2533618.
- PMID 8917899.
- ISBN 978-3-319-73781-2.
- PMID 24972421.
- S2CID 73253356.
- PMID 2969835.
- ISBN 978-1-60913-345-0.
- ^ ISBN 978-3-319-52210-4.
- ISBN 978-1-60327-554-5.
- ^ DailyMed: Synarel – nafarelin acetate spray
- ^ S2CID 39987508.
- PMID 8477775.
- ^ ISBN 978-1-4757-2085-3.
- ^ ISBN 978-94-011-4439-1.
Further reading
- Barbieri RL (February 1990). "Comparison of the pharmacology of nafarelin and danazol". American Journal of Obstetrics and Gynecology. 162 (2): 581–585. PMID 2137975.
- Chrisp P, Goa KL (April 1990). "Nafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions". Drugs. 39 (4): 523–551. PMID 2140979.
- Burry KA (February 1992). "Nafarelin in the management of endometriosis: quality of life assessment". American Journal of Obstetrics and Gynecology. 166 (2): 735–739. PMID 1531576.
- Minaguchi H, Wong JM, Snabes MC (June 2000). "Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature". The Journal of Reproductive Medicine. 45 (6): 481–489. PMID 10900582.