end result [18:<18 years of age for uses other than treatment of central precocious puberty. 1 2 12 Common Adverse Effects Women with endometriosis: Hot flushes (flashes), decreased libido, vaginal dryness, headache, emotional lability, acne, myalgia, reduction in breast size, nasal irritation. 2 3 4 5 16 Children with central precocious puberty: Acne, transient breast enlargement, emotional lability, transient increases in pubic hair, body odor, seborrhea, hot flushes (flashes), rhinitis, vaginal bleeding, white or brown vaginal discharge. 1 6 Interactions for Nafarelin Acetate No formal drug interaction studies to date. 1 2 The manufacturer states drug interactions not expected to occur because nafarelin is a peptide mainly degraded by peptidases and not by CYP microsomal enzymes and because of the drug s limited protein binding. 1 2 Specific Drugs and Laboratory Tests Drug or Test Interaction Comments Decongestants (topical nasal) Possible interaction 2 Delay administration of a topical nasal decongestant ≥2 hours after administration of nafarelin 1 2 Tests, diagnostic tests of pituitary gonadotropic and gonadal function Possible erroneous results when diagnostic tests of pituitary gonadotropic and gonadal function obtained during treatment and up to 4 8 weeks after discontinuance of nafarelin 2 Normal function usually restored 4 8 weeks after discontinuance of nafarelin 2 Nafarelin Acetate Pharmacokinetics Absorption Bioavailability Rapidly absorbed into systemic circulation following nasal administration. 1 2 Bioavailability averages 2.8% (range 1.2 5.6%) in adult women. 1 2 Nasal congestion or rhinitis does not appear to affect bioavailability. 1 2 Following intranasal administration in children and adult women, maximum serum concentrations occur at 10 45 minutes and 10 40 minutes, respectively. 1 2 Distribution Extent Not known whether nafarelin is distributed into milk. 1 2 Plasma Protein Binding About 80% at 4 C. 1 2 Elimination Elimination Route Excreted in urine (44 55%) and feces (19 44%) mainly as metabolites. 1 2 Half-life Children: 2.5 hours. 1 Women: 3 hours. 1 2 Stability Storage Intranasal Nasal Solution Upright at 25 C (may be exposed to 15 30 C). 1 2 15 16 Protect from light; 1 2 15 16 do not freeze. 15 16 Actions Potent agonistic analog of GnRH; 1 2 greater activity than naturally occurring GnRH. 1 2 3 Initially produces a transient surge in circulating levels of estradiol, testosterone, LH, and FSH. 1 2 3 Following chronic and continuous administration (generally 4 weeks after therapy initiation), causes a sustained decrease in LH and FSH secretion and a marked reduction of testicular and ovarian steroidogenesis. 1 2 3 In children receiving continuous administration of adequate doses, serum LH, testosterone, and estradiol concentrations return to prepubertal levels, resulting in suppression of secondary sexual characteristics and decreased rate of linear growth and skeletal maturation. 1 6 12 Initial estrogen withdrawal bleeding may occur, generally 6 weeks after therapy initiation; menstruation should cease thereafter. 1 Effects are usually reversible following therapy cessation. 1 In adult women, serum estradiol, FSH, and LH concentrations usually return to pretreatment levels following discontinuance of therapy. 3 4 Advice to Patients Importance of providing patient a copy of manufacturer s patient information. 1 2 15 16 Importance of full compliance with nafarelin dosing for efficacy. 1 2 15 16 If clinician increases the daily dosage, importance of having an adequate supply for uninterrupted treatment. 1 2 15 16 Importance of not sneezing during or immediately after administering nafarelin nasal solution. 1 2 9 15 16 Inform patients to consult clinician in case of rhinitis. 1 2 If a topical nasal decongestant is needed, administer the decongestant at least 2 hours after nafarelin. 1 2 9 15 16 Risk of sensitivity reaction. 1 2 Risk of other adverse effects, including decreased bone mineral density in women. 2 Importance of promptly reporting sudden onset of headache, vomiting, or visual changes to clinician. 1 2 Advise women of childbearing potential to use an effective nonhormonal contraceptive method (e.g., diaphragm with contraceptive jelly, IUD, condoms) instead of a hormonal method during nafarelin therapy. 1 2 16 Advise women to avoid pregnancy and not to breast-feed during therapy. 2 16 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses. 1 2 Importance of informing clinicians of chronic alcohol and/or tobacco use. 2 16 Importance of informing patients of other important precautionary information. (See Cautions.) Central Precocious Puberty Importance of advising patients with precocious puberty that each nasal solution bottle should be used for 7 days unless otherwise directed by a clinician. 15 At the end of 7 days, dispose of bottle and do not reuse. 15 Inform patients and parents/guardians that the suppressive effects of nafarelin in children are reversible and that initial transient increases in the signs of puberty (e.g., vaginal bleeding, breast enlargement) are possible. 1 Advise patients and parents/guardians that menstrual flow may occur during first 6 weeks of treatment, even if not menstruating previously; advise that menstrual flow should stop after first 6 weeks. 15 Endometriosis Importance of advising women with endometriosis to administer the first dose between the second and fourth day after the beginning of menstrual bleeding. 2 16 Inform the patient that each nasal solution bottle should be used for 30 days. 16 At the end of 30 days, a small amount of liquid will be left in the bottle; do not use the remaining amount. 16 Advise women that breakthrough bleeding or ovulation (with potential for conception) may occur if one or more successive doses of the drug are missed. 2 9 16 Importance of contacting clinician to exclude the possibility of pregnancy if this occurs. 16 Advise patients that irregular vaginal spotting or bleeding may occur for the first 2 months of therapy; duration and intensity may vary. 2 16 Importance of informing clinician if regular menstruation persists after 2 months of therapy. 2 16 Advise patients to discuss the possibility of osteoporosis with their clinician before starting therapy. 2 16 Inform patients that repeat treatments increase the risk of bone loss. 2 16 Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Nafarelin Acetate Routes Dosage Forms Strengths Brand Names Manufacturer Nasal Solution 200 mcg (of nafarelin) per metered spray Synarel Searle AHFS DI Essentials. Copyright 2017, Selected Revisions October 16, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. G.D. Searle LLC. Synarel (nafarelin acetate) nasal solution prescribing information for central precocious puberty. New York, NY; 2010 Dec. Available at . Accessed 2011 May 26. 2. G.D. Searle LLC. Synarel (nafarelin acetate) nasal solution prescribing information for endometriosis. New York, NY; 2010 Dec. Available at . Accessed 2011 May 26. 3. Chrisp P, Goa KL. Nafarelin: a review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions. Drugs . 1990; 39:523-51. [PubMed 2140979] 4. Henzl MR. Gonadotropin-releasing hormone (GnRH) agonists in the management of endometriosis: a review. Clin Obstet Gynecol . 1988; 31:840-56. [PubMed 3067932] 5. Henzl M, Corson SL, Moghissi K et al. Administration of nasal nafarelin as compared with oral danazol for endometriosis: a multicenter double-blind comparative clinical trial. N Engl J Med . 1988; 318:485-9. [PubMed 2963213] 6. Lee PA. Central precocious puberty: an overview of diagnosis, treatment, and outcome. Endocrinol Metab Clin North Am . 1999; 28:901-18. [PubMed 10609126] 7. Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414). Rockville, MD; (2002 Feb 3). From FDA web site. 8. Zhao SZ, Kellerman LA, Francisco CA et al. Impact of nafarelin and leuprolide for endometriosis on quality of life and subjective clinical measures. J Reprod Med . 1999; 44:1000-6. [PubMed 10649809] 9. Syntex. Synarel (nafarelin acetate) nasal solution 2 mg/mL (as nafarelin base) information for patients. Palo Alto, CA; 1992 Apr. 10. Lin TH, LePage ME, Henzl M et al. Intranasal nafarelin: an LH-RH analogue treatment of gonadotropin-dependent precocious puberty. J Pediatr . 1986; 109:954-8. [PubMed 2946840] 11. American College of Obstetricians and Gynecologists (ACOG) Committee on Practice Bulletins. Medical management of endometriosis. Practice Bulletin No. 11. Washington, DC: American College of Obstetricians and Gynecologists; 1999 Dec 1999. 12. Pharmacia, Kalamazoo, MI: personal communication. 13. Food and Drug Administration. GnRH agonists: safety review of drug class used to treat prostate cancer (sold under the brand names Lupron, Zoladex, Trelstar, Viadur, Vantas, Eligard, Synarel, and generics). Rockville, MD; 2010 May 3. From FDA web site (http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm210576.htm). 14. Food and Drug Administration. GnRH agonists: label change--increased risk of diabetes and cardiovascular disease (update). Rockville, MD; 2010 Oct 20. From FDA web site (http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm230359.htm). 15. G.D. Searle LLC. Synarel (nafarelin acetate) nasal solution patient instructions for use for central precocious puberty. New York, NY; 2010 Dec. Available at . Accessed 2011 May 26. 16. G.D. Searle LLC. Synarel (nafarelin acetate) nasal solution patient instructions for use for endometriosis. New York, NY; 2010 Dec. Available at . Accessed 2011 May 26. Next Pregnancy Warnings Print this page Add to My Med List More about nafarelin Side Effects During Pregnancy Dosage Information Support Group En Español 2 Reviews Add your own review/rating Drug class: gonadotropin releasing hormones Consumer resources Nafarelin nasal Nafarelin Nafarelin Nasal (Advanced Reading) Professional resources Nafarelin (Wolters Kluwer) Other brands: Synarel Related treatment guides Endometriosis Precocious Puberty> ]} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only X Pregnancy Category Not for use in pregnancy N/A CSA Schedule Not a controlled drug Drug Class Gonadotropin releasing hormones Related Drugs Endometriosis medroxyprogesterone , leuprolide , Provera , Depo-Provera , Lupron Depot , norethindrone , Sprintec , Zoladex , Ortho Tri-Cyclen , danazol , TriNessa , Mononessa , More... Precocious Puberty tamoxifen , Lupron , leuprolide , Nolvadex , triptorelin , histrelin , Vantas , Triptodur , More... Nafarelin Rating 2 User Reviews 6.3 /10 2 User Reviews 6.3 Rate it!} } bargain
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