Clinical data | |
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Trade names | Synarel, 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 |
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Routes of administration | Nasal spray[1][2] |
Drug class | GnRH analogue; GnRH agonist; antigonadotropin |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Bioavailability | IN : 2.8% (1.2–5.6%)[2] |
Protein binding | 80%[2] |
Metabolism | Peptidases (not CYP450 )[2] |
Elimination half-life | IN: 2.5–3.0 hours[2] SC : 86 hours (metabolites)[2] |
Excretion | Urine: 44–55%[2] Feces: 19–44%[2] |
Identifiers | |
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Chemical and physical data | |
Formula | C66H83N17O13 |
Molar mass | 1322.496 g·mol−1 |
3D model (JSmol) | |
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Nafarelin, sold under the brand name Synarel among others, is a medication used to treat endometriosis and early puberty.[3][2] It is also used for uterine fibroids, as part of in vitro fertilization (IVF), and as part of transgender hormone therapy.[4][5][6] It is used as a nasal spray two to three times per day.[3]
Common side effects in women include hot flushes, vaginal dryness, muscle pain, and sexual dysfunction.[3] Common side effects in children include acne, mood changes, increased pubic hair, and vaginal bleeding.[3] Other side effects may include allergic reactions, osteoporosis, and pituitary apoplexy.[3] Use in pregnancy may harm the baby.[3] It is a gonadotropin-releasing hormone agonist (GnRH agonist) and works by briefly increasing than decreasing the production of sex hormones by the gonads.[2]
Nafarelin was approved for medical use in the United States in 1990.[3] In the United Kingdom 60 doses of 200 mcg cost the NHS about £50 as of 2021.[7] In the United States this amount costs about 2,800 USD.[8] It is available in many countries globally.[9] It is one of two GnRH analogues available as a nasal spray, the other being buserelin.[10]
References
edit- ^ 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): 523–51. doi:10.2165/00003495-199039040-00005. PMID 2140979.
- ^ a b c d e f g h i j k "DailyMed - SYNAREL- nafarelin acetate spray, metered". dailymed.nlm.nih.gov. Archived from the original on 30 March 2021. Retrieved 11 November 2021.
- ^ a b c d e f g h i j "Nafarelin Monograph for Professionals". Drugs.com. Archived from the original on 4 March 2021. Retrieved 11 November 2021.
- ^ Minaguchi H, Wong JM, Snabes MC (June 2000). "Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature". J Reprod Med. 45 (6): 481–9. PMID 10900582.
- ^ Elder, Kay; Dale, Brian (2 December 2010). In-Vitro Fertilization. Cambridge University Press. p. 24. ISBN 978-1-139-49285-0. Archived from the original on 13 November 2021. Retrieved 11 November 2021.
- ^ Olshan J, Eimicke T, Belfort E (June 2016). "Gender Incongruity in Children With and Without Disorders of Sexual Differentiation". Endocrinol. Metab. Clin. North Am. 45 (2): 463–82. doi:10.1016/j.ecl.2016.02.001. PMID 27241976.
- ^ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 782. ISBN 978-0857114105.
- ^ "Nafarelin Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 11 November 2021.
- ^ Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000. pp. 712–. ISBN 978-3-88763-075-1. Archived from the original on 2021-10-28. Retrieved 2021-08-23.
- ^ T. Metin Önerci (17 August 2013). Nasal Physiology and Pathophysiology of Nasal Disorders. Springer Science & Business Media. pp. 208–. ISBN 978-3-642-37250-6. Archived from the original on 28 October 2021. Retrieved 23 August 2021.