Nafarelin
Clinical data | |
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Trade names | Synarel |
AHFS/Drugs.com | Monograph |
MedlinePlus | a601082 |
Pregnancy category |
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Routes of administration | Nasal spray |
ATC code | H01CA02 (WHO) |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Biological half-life | 2.6 to 4 hours |
Excretion | renal |
Identifiers | |
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CAS Number | 76932-56-4 |
PubChem (CID) | 25077649 |
IUPHAR/BPS | 3902 |
DrugBank | DB00666 |
ChemSpider | 10482014 |
UNII | 1X0094V6JV |
ChEMBL | CHEMBL1201309 |
ECHA InfoCard | 100.212.186 |
Chemical and physical data | |
Formula | C66H83N17O13 |
Molar mass | 1321.6344 g/mol |
3D model (Jmol) | Interactive image |
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Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist). Its proposed mechanism of action is the desensitization of pituitary GnRH receptors leading to a decrease in gonadotropin release, and ovarian hormone serum concentrations similar to those achieved in postmenopausal women. it decreases pituitary secretion of the gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Nafarelin may be used in the treatment of estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat central precocious puberty, or to control ovarian stimulation in in vitro fertilisation (IVF).[1][2]
Nafarelin acetate is marketed by Searle (now part of Pfizer) under the brand name Synarel. It is delivered via a nasal spray.[3]
Side effects
Side effects of nafarelin are related to the low estrogen state. Side effects include hot flashes, vaginal dryness, headaches, mood changes, and decreased interest in sex. Some patients may experience acne, muscle pain, reduced breast size, and irritation of the tissue inside the nose. These side effects are reversible and should resolve after stopping the medication.[4]
References
- ↑ Mutschler, Ernst; Schäfer-Korting, Monika (2001). Arzneimittelwirkungen (in German) (8 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. pp. 372–3. ISBN 3-8047-1763-2.
- ↑ Wuttke, W; Jarry, H; Feleder, C; Moguilevsky, J; Leonhardt, S; Seong, J. Y.; Kim, K (1996). "The neurochemistry of the GnRH pulse generator". Acta neurobiologiae experimentalis. 56 (3): 707–13. PMID 8917899.
- ↑ Drugs.com: Synarel Monograph
- ↑ DailyMed: Synarel – nafarelin acetate spray