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]
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%
nasal spray for use one, two, or three times per day.[20][2][1] Each bottle of nafarelin nasal spray (brand name Synarel) contains about 60 sprays delivering approximately 200 μg nafarelin in 100 μL solution per actuation.[2] Nafarelin is not available for use by any other
routes than
intranasal administration.[21]
Nafarelin was introduced for medical use in 1990.[9][1][10]
Society and culture
Generic names
Nafarelin is the
generic name of the drug and its
INNTooltip International Nonproprietary Name and
BANTooltip British Approved Name, while nafaréline is its
DCFTooltip Dénomination Commune Française and nafarelin acetate is its
USANTooltip United States Adopted Name,
BANMTooltip British Approved Name, and
JANTooltip Japanese Accepted Name.[26][12][27][11] It is also known by its former developmental code name RS-94991 or RS-94991-298.[26][12][27][11]
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]
^
abcdefghijklmnopChrisp 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.
doi:
10.2165/00003495-199039040-00005.
PMID2140979.
^
abMinaguchi 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.
PMID10900582.
^
abMutschler E, Schäfer-Korting M (2001). Arzneimittelwirkungen (in German) (8 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. pp. 372–3.
ISBN3-8047-1763-2.
^
abOlshan J, Eimicke T, Belfort E (June 2016). "Gender Incongruity in Children With and Without Disorders of Sexual Differentiation". Endocrinology and Metabolism Clinics of North America. 45 (2): 463–482.
doi:
10.1016/j.ecl.2016.02.001.
PMID27241976.
^
abConn PM, Crowley WF (January 1991). "Gonadotropin-releasing hormone and its analogues". The New England Journal of Medicine. 324 (2): 93–103.
doi:
10.1056/NEJM199101103240205.
PMID1984190.
^
abMonroe SE, Andreyko J (December 1989). "Treatment of uterine leiomyomas and hirsutism with nafarelin". The Journal of Reproductive Medicine. 34 (12 Suppl): 1029–1033.
PMID2533618.
^Kreuser ED, Klingmüller D, Thiel E (1993). "The role of LHRH-analogues in protecting gonadal functions during chemotherapy and irradiation". European Urology. 23 (1): 157–63, discussion 163–4.
doi:
10.1159/000474586.
PMID8477775.
Barbieri RL (February 1990). "Comparison of the pharmacology of nafarelin and danazol". American Journal of Obstetrics and Gynecology. 162 (2): 581–585.
doi:
10.1016/0002-9378(90)90436-B.
PMID2137975.
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.
doi:
10.2165/00003495-199039040-00005.
PMID2140979.
Burry KA (February 1992). "Nafarelin in the management of endometriosis: quality of life assessment". American Journal of Obstetrics and Gynecology. 166 (2): 735–739.
doi:
10.1016/0002-9378(92)91705-F.
PMID1531576.
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.
PMID10900582.