Dosing & Uses
Dosage Forms & Strengths
nasal spray
- 2mg/mL
Endometriosis
1 spray (200 mcg/spray) in one nostril qAM, 1 spray in the other nostril qPM (total 400 mcg/day) on days 2-4 of menstrual cycle (2 sprays/day)
May increase to 800 mcg/day if still menstruating after 2 month: 1 spray in each nostril twice daily
Maximum treatment duration: 6 months
Dosage Forms & Strengths
nasal spray
- 200mcg/spray
Central Precocious Puberty
<2 years: Safety and efficacy not established
≥2 years: 2 sprays (200 mcg/spray) in each nostril twice daily (total 1600 mcg/day)
May increase to 1800 mcg/day: 3 sprays (200 mcg/spray) into alternating nostrils TID (total 9 sprays/day)
Discontinue when puberty onset is desired
Adverse Effects
1-10%
Acne (10%)
Breast enlargement (8%)
Vaginal bleeding (8%)
Seborrhea (3%)
Emotional lability (6%)
Vaginal discharge (3%)
Rhinitis (5%)
Body odor (4%)
Increase in pubic hair (5%)
Frequency Not Defined
Arthralgia
Breast engorgement
Chloasma
Maculopapular rash
Paresthesia
Weakness
Palpitation
Eye pain
Postmarketing Reports
Liver injury
Pituitary apoplexy
Seizures
Pituitary gland changes
Liver injury (rare)
Ovarian hyperstimulation syndrome
Psychiatric Disorders: Emotional lability, including crying, irritability, impatience, anger, and aggression; depression, including rare reports of suicidal ideation and attempt, in children treated for central precocious puberty
Warnings
Contraindications
Pregnancy, hypersensitivity, lactation, undiagnosed abnormal vaginal bleeding
Cautions
Goal in adult females is to suppress menstruation; max treatment period 6 mth
May cause increase in bone turnover & decrease in bone mineral content
Ovarian cysts may develop within first 2 months of therapy and occur more commonly in women with polycystic ovarian disease
Cases of pituitary apoplexy reported
Use caution in patients with risk factors for decreased bone mineral density
Irregular or incomplete daily doses may result in stimulation of the pituitary-gonadal axis; counsel caregivers to assure full compliance
During first month of treatment, may initially expect some signs of puberty, e.g., vaginal bleeding or breast enlargement, may occur; such changes should resolve soon after first month; if such resolution does not occur within first two months of treatment, this may be due to lack of compliance or presence of gonadotropin independent sexual precocity; if both possibilities excluded, the dose omay be increased to 1800 mcg/day administered as 600 mcg tid
Patients with intercurrent rhinitis should consult their physician for use of topical nasal decongestant; if use of topical nasal decongestant required during treatment decongestant should not be used until at least 2 hr after administering therapy; sneezing during or immediately after administering therapy should be avoided, if possible, since may impair drug absorption
Convulsions reported in patients receiving GnRH agonists; reports with GnRH agonists have included patients with a history of seizures, epilepsy, cerebrovascular disorders, central nervous system anomalies or tumors, and patients on concomitant medications that have been associated with convulsions such as bupropion and SSRIs; convulsions also reported in patients in the absence of any of the conditions listed
Psychiatric events reported in patients taking GnRH agonists; postmarketing reports with this class of drugs include symptoms of emotional lability, such as crying, irritability, impatience, anger, and aggression; monitor for development or worsening of psychiatric symptoms during treatment
Pregnancy & Lactation
Pregnancy Category: X
Lactation: Excretion in milk unknown, contraindicated
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Synthetic decapeptide that is an agonist of LHRH, desensitizes response to endogenous GnRH, which in turn reduces secretion of LH and FSH and subsequently causes decreased ovarian and testicular production
Pharmacokinetics
Peak serum time: 10-45 min
Protein Bound: 78-84%
Metabolism: Degraded by peptidase
Metabolites: Dipeptide, tripeptide, pentapeptide, hexapeptide amide, D-naphthylalanine, 2-naphthylacetic acid (inactive)
Excretion: Urine (44-55%); feces (19-44%)
Half-Life: 3 hr
Bioavailability (1-6%)
Onset: 1 month (initial effect)
Peak effect: 12 wk (endometriosis); 4-8 hr (gonadotropin secretion stimulation)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Synarel nasal - | 2 mg/mL aerosol |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
nafarelin nasal
NAFARELIN ACETATE SPRAY - NASAL
(NAF-a-REL-in AS-e-tate)
COMMON BRAND NAME(S): Synarel
USES: Nafarelin is used in women to treat a condition in which the tissue that normally lines the inside of the uterus grows in the wrong place (endometriosis). This medication helps to decrease the abnormal tissue and also the symptoms of endometriosis (such as pelvic pain, painful menstrual cramps, and pain during/after sex).This medication is also used in children to treat a certain type of early puberty (central precocious puberty, gonadotropin-dependent). It helps to slow the bone aging and height growth rate so that both are near normal, and it helps to stop or reverse signs of early puberty (such as breast growth in girls, growth of sexual organs in boys).Nafarelin is similar to a natural hormone made by the body (gonadotropin-releasing hormone-GnRH). It works by decreasing the testosterone hormones in boys and estrogen hormones in women and girls.
HOW TO USE: Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start using nafarelin and each time you get a refill. Follow the illustrated directions for the proper use of this medication. If you have any questions, ask your doctor or pharmacist.Follow the instructions for test sprays in the air if you are using a bottle for the first time. A fine mist is a sign that the spray is working properly.Gently blow your nose before using this drug. For very young children, it may be necessary to clear the nose with a bulb syringe.Use this medication as directed by your doctor, usually twice daily (about every 12 hours). If you are using more than 1 spray at a time, wait 30 seconds between each spray. Avoid spraying this medication in your eyes. Also, avoid sneezing during or right after using this medication because this may decrease the amount of medication absorbed. Follow the detailed instructions for cleaning the spray tip. It is important to clean the spray tip after each use.The dosage and length of treatment are based on your medical condition and response to treatment.It is very important to continue using this medication exactly as prescribed by your doctor. Do not skip any doses. To help you remember, use it at the same times each day.Ask your doctor or pharmacist to find out how long each bottle of the nasal spray should last. Do not use the nasal spray bottle longer, even if there is medication left over, because you will not get a full dose. Make sure to get your medication refills a few days early so that you will not run out of your medication.Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.If you need to use a nasal decongestant spray while using this medication, wait at least 2 hours after using this medication before using the decongestant.When you first start this medication, worsening of symptoms may occur (such as increased vaginal bleeding for women treating endometriosis, or vaginal bleeding/period, increase in breast size/pubic hair, oily skin, or body odor for children treating early puberty). These symptoms should get better after the first month of treatment. Tell your doctor if your symptoms do not get better or if they get worse after 2 months of treatment.
SIDE EFFECTS: Nasal irritation, hot flashes, or vaginal discharge may occur in children. Nasal irritation, hot flashes, headaches, decreased sexual interest, muscle pain, vaginal dryness, acne, or decrease in breast size may occur in women. If any of these effects last or get worse, tell the doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell the doctor right away if any of these serious side effects occur: mental/mood changes (such as depression, thoughts of suicide, mood swings, aggression).Get medical help right away if any of these very serious side effects occur: seizures.Rarely, a very serious problem with the pituitary gland (pituitary apoplexy) may occur, usually in the first hour to 2 weeks after the first dose of this medication. Get medical help right away if any of these very serious side effects occur: sudden severe headache, sudden severe mental/mood changes (such as severe confusion, difficulty concentrating), vision changes, vomiting.For women using this medication, tell your doctor right away if you have any serious side effects, including: abdominal/lower back pain, bone pain, fast/pounding heartbeat, numbness/tingling of arms/legs, eye pain.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before using nafarelin, tell your doctor or pharmacist if you are allergic to it; or to GnRH or other GnRH-like hormones (such as leuprolide); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: unexplained abnormal vaginal bleeding, smoking, daily alcohol use, bone loss (osteoporosis) or family history of osteoporosis, polycystic ovarian disease, high cholesterol/triglyceride levels, seizures, mental/mood problems (such as depression).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication must not be used during pregnancy. It may harm an unborn baby. Women should start this medication between days 2 and 4 of their period. Although periods and the release of eggs (ovulation) may stop while you are using this drug, this is not a reliable form of birth control. Discuss the use of non-hormonal forms of birth control (such as condoms, diaphragm with spermicide) with your doctor. If you become pregnant or think you may be pregnant, tell your doctor right away.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.This medication may interfere with certain lab tests (such as tests for pituitary gonadotropic and gonadal functions), possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as growth/bone age velocity in children) should be done while you are using this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Use your next dose at the regular time. Do not double the dose to catch up.Vaginal bleeding may occur in girls/women who miss doses of this medication.
STORAGE: Store the bottle upright at room temperature away from light and moisture. Do not freeze. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised August 2017. Copyright(c) 2021 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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