pharmacopeia
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Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Gonadotropin Releasing Hormone Receptor Agonists; Hormone Receptor Agonists.

Gonadotropin Releasing Hormone ReceptorHormone Receptor

Indications

Sourced from openFDA
  • FOR CENTRAL PRECOCIOUS PUBERTY (For Endometriosis, See Reverse Side ) SYNAREL is indicated for treatment of central precocious puberty (CPP) (gonadotropin-dependent precocious puberty) in children of both sexes. The diagnosis of central precocious puberty (CPP) is suspected when premature development of secondary sexual characteristics occurs at or before the age of 8 years in girls and 9 years in boys, and is accompanied by significant advancement of bone age and/or a poor adult height prediction.ICD-10: N80.9

Contraindications

Sourced from openFDA
  • 1. Hypersensitivity to GnRH, GnRH agonist analogs or any of the excipients in SYNAREL; 2.contraindicated

Dosage & administration

Sourced from openFDA

For the treatment of central precocious puberty (CPP), the recommended daily dose of SYNAREL is 1600 µg. The dose can be increased to 1800 µg daily if adequate suppression cannot be achieved at 1600 µg/day. The 1600 µg dose is achieved by two sprays (400 µg) into each nostril in the morning (4 sprays) and two sprays into each nostril in the evening (4 sprays), a total of 8 sprays per day. The 1800 µg dose is achieved by 3 sprays (600 µg) into alternating nostrils three times a day, a total of 9 sprays per day. The patient's head should be tilted back slightly, and 30 seconds should elapse between sprays. If the prescribed therapy has been well tolerated by the patient, treatment of CPP with SYNAREL should continue until resumption of puberty is desired. There appeared to be no significant effect of rhinitis, i.e., nasal congestion, on the systemic bioavailability of SYNAREL; however, if the use of a nasal decongestant for rhinitis is necessary during treatment with SYNAREL, the decongestant should not be used until at least 2 hours following dosing with SYNAREL. Sneezing during or immediately after dosing with SYNAREL should be avoided, if possible, since this may impair drug absorption. At 1600 µg/day, a bottle of SYNAREL provides about a 7-day supply (about 56 sprays). If the daily dose is increased, increase the supply to the patient to ensure uninterrupted treatment for the duration of therapy.

Warnings & precautions

Sourced from openFDA

The diagnosis of central precocious puberty (CPP) must be established before treatment is initiated. Regular monitoring of CPP patients is needed to assess both patient response as well as compliance. This is particularly important during the first 6 to 8 weeks of treatment to assure that suppression of pituitary-gonadal function is rapid. Testing may include LH response to GnRH stimulation and circulating gonadal sex steroid levels. Assessment of growth velocity and bone age velocity should begin within 3 to 6 months of treatment initiation. Some patients may not show suppression of the pituitary-gonadal axis by clinical and/or biochemical parameters. This may be due to lack of compliance with the recommended treatment regimen and may be rectified by recommending that the dosing be done by caregivers. If compliance problems are excluded, the possibility of gonadotropin independent sexual precocity should be reconsidered and appropriate examinations should be conducted. If compliance problems are excluded and if gonadotropin independent sexual precocity is not present, the dose of SYNAREL may be increased to 1800 µg/day administered as 600 µg tid. Psychiatric events have been reported in patients taking GnRH agonists. Postmarketing reports with this class of drugs includes symptoms of emotional lability, such as crying, irritability, impatience, anger, and aggression. Monitor for development or worsening of psychiatric symptoms during treatment with SYNAREL. Post-marketing reports of convulsions have been observed in patients receiving GnRH agonists.

Adverse reactions

Sourced from openFDA

In clinical trials of 155 pediatric patients, 2.6% reported symptoms suggestive of drug sensitivity, such as shortness of breath, chest pain, urticaria, rash, and pruritus. In these 155 patients treated for an average of 41 months and as long as 80 months (6.7 years), adverse events most frequently reported (>3% of patients) consisted largely of episodes occurring during the first 6 weeks of treatment as a result of the transient stimulatory action of nafarelin upon the pituitary-gonadal axis: acne (10%) transient breast enlargement (8%) vaginal bleeding (8%) emotional lability (6%) [see Warnings ] transient increase in pubic hair (5%) body odor (4%) seborrhea (3%) Hot flashes, common in adult women treated for endometriosis, occurred in only 3% of treated children and were transient. Other adverse events thought to be drug-related, and occurring in >3% of patients were rhinitis (5%) and white or brownish vaginal discharge (3%). Approximately 3% of patients withdrew from clinical trials due to adverse events. In one male patient with concomitant congenital adrenal hyperplasia, and who had discontinued treatment 8 months previously to resume puberty, adrenal rest tumors were found in the left testis. Relationship to SYNAREL is unlikely. Regular examinations of the pituitary gland by magnetic resonance imaging (MRI) or computer assisted tomography (CT) of children during long-term nafarelin therapy as well as during the post-treatment period has occasionally revealed changes in the shape and size of the pituitary gland.

Use in specific populations

Sourced from openFDA

Pregnancy Teratogenic Effects See Contraindications . Intramuscular SYNAREL was administered to rats during the period of organogenesis at 0.4, 1.6, and 6.4 µg/kg/day (about 0.5, 2, and 7 times the maximum recommended human intranasal dose based on the relative bioavailability by the two routes of administration). An increase in major fetal abnormalities was observed in 4/80 fetuses at the highest dose. A similar, repeat study at the same doses in rats and studies in mice and rabbits at doses up to 600 µg/kg/day and 0.18 µg/kg/day, respectively, failed to demonstrate an increase in fetal abnormalities after administration during the period of organogenesis. In rats and rabbits, there was a dose-related increase in fetal mortality and a decrease in fetal weight with the highest dose.

Overdosage

Sourced from openFDA

In experimental animals, a single subcutaneous administration of up to 60 times the recommended human dose (on a µg/kg basis, not adjusted for bioavailability) had no adverse effects. At present, there is no clinical evidence of adverse effects following overdosage of GnRH analogs. Based on studies in monkeys, SYNAREL is not absorbed after oral administration.

Approval history

Sourced from openFDA
  • Feb 13, 1990NDANDA019886Pfizer

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
271 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Ovarian Hyperstimulation Syndrome4818%
  2. 2Dyspnoea197.0%
  3. 3Ascites186.6%
  4. 4Condition Aggravated134.8%
  5. 5Diarrhoea134.8%
  6. 6Headache134.8%
  7. 7Nausea134.8%
  8. 8Off Label Use134.8%
  9. 9Pain134.8%
  10. 10Abdominal Pain124.4%
  11. 11Drug Ineffective114.1%
  12. 12Malaise114.1%
  13. 13Fatigue103.7%
  14. 14Abdominal Distension93.3%
  15. 15Abortion Spontaneous93.3%

Literature

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Recent PubMed references pinned to Nafarelin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 12 ClinicalTrials.gov registrations naming Nafarelin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Nafarelin work?
Mechanism-of-action classes: Gonadotropin Releasing Hormone Receptor Agonists; Hormone Receptor Agonists.
What is Nafarelin used for?
According to FDA labeling, Nafarelin carries indications including: FOR CENTRAL PRECOCIOUS PUBERTY (For Endometriosis, See Reverse Side ) SYNAREL is indicated for treatment of central precocious puberty (CPP) (gonadotropin-dependent precocious puberty) in children of both sexes. The diagnosis of central precocious puberty (CPP) is suspected when premature development of secondary sexual characteristics occurs at or before the age of 8 years in girls and 9 years in boys, and is accompanied by significant advancement of bone age and/or a poor adult height prediction.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Nafarelin?
Nafarelin is classified as Gonadotropin-releasing hormones, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Hormone Receptor Agonists, Decreased Follicle Stimulating Hormone Secretion, Decreased Luteinizing Hormone Secretion, Decreased Ovarian Estrogen Secretion, Decreased Testosterone Secretion.
What are the brand names for Nafarelin?
Nafarelin is marketed under brand names including Synarel.
What are the contraindications for Nafarelin?
Nafarelin labeling lists contraindications including: 1. Hypersensitivity to GnRH, GnRH agonist analogs or any of the excipients in SYNAREL; 2.. Always consult the full prescribing information and a clinician.
Note. Data for nafarelin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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