Nafarelin (Nasal)

Nafarelin is a synthetic drug that mimics a hypothalamus-produced hormone; this prescription medication is an effective option for both central precocious puberty in young girls and boys and for the treatment of endometriosis.

Overview

This drug is administered via a nasal spray and is used to treat both central precocious puberty (CPP) in young boys under the age of nine and girls younger than eight, as well as cases of endometriosis in adult women. This drug mimics a hormone that is produced in the hypothalamus gland called GnRH a gonadotropin-releasing hormone. GnRH works by decreasing the production of estrogen in women and girls and the release of the hormone testosterone in boys.

Puberty is considered early if the onset occurs before age nine in boys, and prior to age eight in girls.

By suppressing the production of hormones in boys and girls, testosterone and estrogen, respectively, nafarelin helps to curtail the effects of a medical condition known as central precocious puberty or CPP. This medication is only effective during the time in which it is taken and will not have any hold-over effects if the child stops taking the drug. Nafarelin is successful in thwarting the early development that can be associated with CPP such as early genital development in both genders and the development of breasts in young girls.

The use of nafarelin will prevent not only the early puberty symptoms but can also forestall the growth of bones. By doing this, the child may grow taller in their adolescence.

The condition known as endometriosis causes the production of excessive uterine tissue that can grow either inside, outside of, or in both areas causing a significant amount of pain and discomfort to the women who suffer from this condition. One effective way to minimize the symptoms of endometriosis is the reduction of estrogen in the patient's body. This can be accomplished with a medication such as nafarelin that curtails the production of GnRH which in turn suppresses estrogen production. Nafarelin is effective in curtailing the growth of excess uterine tissue while it is being taken and for six months following the end of the course of treatment.

While suppressing estrogen can cause issues with the bone health of the adult women who take nafarelin to treat their endometriosis, this can be a positive outcome for children suffering from CPP. Nafarelin will help to regulate the bone growth in these children to a healthy rate that may even add inches to their height. Women taking nafarelin as a treatment of endometriosis should discuss the potential ill effects that the drug can have on the health of their bones.

This drug should not be used by pregnant women or women who would like to become pregnant in the near future. If you are seeking treatment for endometriosis and are of childbearing age and are actively trying to become pregnant, you should discuss alternative treatment options with your doctor, as nafarelin will not be safe for use in such a situation. The effects of nafarelin will last for six months following the conclusion of their course of treatment.

A barrier method of contraception must be used by women who are taking this drug as it affects the production of estrogen in their bodies in such a way that hormonal birth control will be ineffective. Patients who are not familiar with such types of birth control should discuss their options before taking this drug. Prior to beginning their nafarelin course of treatment women of childbearing age are encouraged to discuss their contraception method prior to the start of using the drug.

This medication has been reported to cause serious harm to developing fetuses and should not be taken by pregnant women or women who wish to become pregnant in the near future. If you become pregnant while taking this drug, notify your doctor immediately.

Nafarelin is available in the following method of dosage delivery:

  • Spray

Conditions Treated

Type Of Medicine

  • Endocrine-Metabolic Agent
  • Luteinizing Hormone Releasing Hormone Agonist

Side Effects

Similar to most other medications, nafarelin has been reported to also cause unwanted side effects as well as its intended treatment. There are certain side effects that may require additional medical attention and others that will likely dissipate on their own. Patients are encouraged to understand the difference between the different types of symptoms and what action to take should they occur. Discuss any concerns that you may have about how your body and system react to this medication with either your pharmacist or the prescribing physician. If you are unsure if a symptom that you experience is of concern, it is always best practice to seek further medical advice and guidance.

Patients should notify their doctor of any allergies that they may have including those to medications, food, cleaning solutions, and other substances. Certain allergic reactions may increase the likelihood of the patient experiencing some unwanted side effects. Discuss your allergies with your doctor as they may alter the way in which you take nafarelin or offer strategies to implement in order to decrease the chance of experiencing unwanted symptoms.

Patients who experience any of the following side effects should notify their doctors as they may be signs of a more serious problem:

More likely:

[In women]

  • Breast enlargement
  • Heavier than usual menstrual bleeding
  • Spotting, or light bleeding not associated with the menstrual cycle

[In boys]

  • Growth of hair in the pubic region

  • Body odor

[In girls]

  • Body odor
  • Heavier than usual menstrual bleeding
  • Breast enlargement
  • Spotting, or light bleeding not associated with the menstrual cycle
  • The growth of hair in the pubic region

Less likely:

Less likely or rare occurrence:

[In women]

  • Pelvic bloating or tenderness
  • Fast or irregular heartbeat
  • Unexpected or excess milk flow from breasts
  • Numbness or tingling in the hands or feet
  • Unexplained tiredness or weakness
  • Patchy brown or dark brown discoloration of the skin
  • Pain in the eyes or joints

[In both girls and boys]

  • Chest pain
  • Shortness of breath
  • Hives

An unknown incidence of occurrence:

  • Anxiety or mental depression
  • Weakness
  • Changes in vision
  • Slow heart rate
  • Cold, clammy, or pale skin
  • Irregular heartbeats
  • Convulsions
  • Nightmares or unusually vivid dreams
  • Confusion
  • Vomiting
  • Headaches
  • Chest pain or discomfort
  • Coughing
  • Inability to speak
  • Sweating
  • Dizziness or lightheadedness
  • Slow speech
  • Fainting
  • Pain or discomfort in the arms or neck
  • Inability to move the extremities or facial muscles
  • Yellow eyes or skin
  • Nausea
  • Difficulties with speaking
  • Pain, redness, or swelling in the arm or leg
  • Fast heartbeat
  • Sudden shortness of breath or difficulty breathing
  • Double vision
  • Vomiting

As the patient's system adapts to the introduction of nafarelin many of the initial side effects will dissipate on their own and will not require any further medical attention. Patients are advised to contact their doctor in the event that their symptoms become worse or if they linger longer than a few days:

More likely:

[In women]

  • Cessation of the menstrual cycle
  • Hot flashes
  • Rapid weight gain
  • Increased hair growth
  • Oily skin
  • Muscle pain
  • Acne
  • Pain during sexual intercourse
  • Mood swings
  • Reduced breast size
  • Changes in the degree of sexual desire
  • Swelling of the extremities
  • Dandruff
  • Vaginal dryness

[In boys]

  • Oily skin
  • Acne
  • Mood swings
  • Dandruff

[In girls]

  • Acne
  • Oily skin
  • Mood swings
  • Dandruff
  • Hot flashes

Less likely or rare occurrence:

[In women]

  • Mental depression
  • Skin rash
  • An irritated or a runny nose
  • Headaches
  • Breast pain

[In boys]

  • A runny nose or nasal irritation

[In girls]

  • White or brownish vaginal discharge
  • A runny nose or nasal irritation

While this list of side effects is comprehensive in nature, some patients may experience other symptoms that are not included here. If symptoms become a cause for concern, it is always best practice to contact the prescribing physician for further medical advice.

Dosage

The dosage guidelines that are outlined below represent the typical amounts that are prescribed. Patients are advised to always follow the instruction provided with their prescription even when they differ from what is stated here. Do not alter the way in which you take this medication without first discussing any changes with your doctor.

This drug is intended for delivery via a nasal spray and should not be administered in any other manner. Do not spray this medication into the eyes. If you inadvertently get any of this medicine in your eyes wash them thoroughly and contact your doctor for further instruction.

To use nafarelin spray:

At the initial use of the medication spray, the bottle will need to be primed. Simply give the bottle at least five or so pumps until there is a mist of medication that is emitted. Only do this the first time that the bottle is used, otherwise, medication will be wasted. Do not inhale the spray as this can cause you to ingest too much nafarelin.

Prior to administering this medication, lightly blow your nose in order to clear the nasal passages. To administer the spray, simply insert the tip of the spray bottle into a nostril without touching the nose and pump the bottle one time while closing the other nostril. Gently tilt your head back slightly and hold the position for a period of 30 seconds. Repeat the process in the other nostril.

After delivering the medication, thoroughly wipe the tip of the spray bottle with a clean cloth or tissue. Return the safety cap.

When necessary, clean the spray bottle by rinsing the tip with running water; be sure to hold the bottle in such a way that none enters the bottle, as this will dilute the medication.

Speak with your doctor prior to using any nasal decongestants during your course of treatment.

It is of vital importance that this medication is taken as directed in order to be effective. Take each dose at the same time each day in order to maintain the required level of medication in your system at all times.

Always take this medication as instructed and do not make any changes in the way that you take it without first discussing them with your doctor.

For nasal dosage form (spray):

For treatment of central precocious puberty:

  • Children

Administer two sprays in both nostrils twice a day in the evening and the morning, making sure to take the medication at the same time each day. The dosage is equivalent to eight sprays per day. Your doctor will advise if any changes need to be made to your dosage as a higher dose may be necessary in some cases.

For treatment of endometriosis:

  • Adult Women

Treatment is to start on either day 2, 3, or 4 of the menstrual cycle. Administer the medication in one nostril each morning and the next in the alternate nostril in the evening. This course of treatment is typically one that is 6 months in duration.

This drug is not recommended for use in children for this medical condition.

Patients who inadvertently miss a dose should take it as soon as they realize that it has been skipped. If it is close to the time of the next dose, then skip the dose completely. Do not take a second dose to "make up" for one that was skipped. Patients who have missed a dose and are unsure what to do are encouraged to contact their pharmacist or doctor for further advice.

Major Drug Interactions

Like most drugs and medicines, there are certain drugs that should not be taken together if at all possible. Your doctor may change one of your drugs in order to avoid this contraindication, or in other instances may alter the way that you take one or both of the medications. Prior to starting nafarelin inform your doctor of all medications that you are taking, including both prescription and non-prescription drugs, as well as any herbal remedies or vitamin and mineral supplements.

The use of nafarelin with the following drugs is not advisable and your doctor may opt to treat you with an alternative medication; prior to beginning your course of treatment it is advisable to discuss your use of any of these medications with your doctor:

  • Amifampridine
  • Thioridazine
  • Bepridil
  • Sparfloxacin
  • Dronedarone
  • Piperaquine
  • Pimozide
  • Ziprasidone
  • Saquinavir
  • Mesoridazine
  • Terfenadine
  • Cisapride
  • Amisulpride

Using nafarelin with any of the drugs listed below may increase the risk of certain side effects or cause other complications. Patients may have their prescriptions altered or their doctor may change the way in which they take one or both of the medications:

  • Alfuzosin
  • Voriconazole
  • Amitriptyline
  • Vilanterol
  • Apomorphine
  • Vemurafenib
  • Arsenic Trioxide
  • Vandetanib
  • Astemizole
  • Trazodone
  • Azithromycin
  • Tolterodine
  • Chloroquine
  • Tetrabenazine
  • Ciprofloxacin
  • Telavancin
  • Clarithromycin
  • Tamoxifen
  • Clozapine
  • Sunitinib
  • Cyclobenzaprine
  • Sotalol
  • Dasatinib
  • Solifenacin
  • Desipramine
  • Sodium Phosphate, Dibasic
  • Dofetilide
  • Sevoflurane
  • Domperidone
  • Ritonavir
  • Doxepin
  • Rilpivirine
  • Ebastine
  • Quinine
  • Eribulin
  • Quetiapine
  • Escitalopram
  • Propafenone
  • Felbamate
  • Prochlorperazine
  • Flecainide
  • Probucol
  • Fluoxetine
  • Pitolisant
  • Foscarnet
  • Pimavanserin
  • Galantamine
  • Perflutren Lipid Microsphere
  • Gemifloxacin
  • Pazopanib
  • Halofantrine
  • Paroxetine
  • Hydroquinidine
  • Paliperidone
  • Hydroxyzine
  • Olanzapine
  • Iloperidone
  • Octreotide
  • Pasireotide
  • Itraconazole
  • Nilotinib
  • Ketoconazole
  • Moxifloxacin
  • Levofloxacin
  • Mifepristone
  • Mefloquine
  • Hydroxychloroquine
  • Metronidazole
  • Methadone
  • Mizolastine
  • Lumefantrine
  • Nelfinavir
  • Lapatinib
  • Norfloxacin
  • Ivabradine
  • Ofloxacin
  • Imipramine
  • Ondansetron
  • Ibutilide
  • Panobinostat
  • Haloperidol
  • Pentamidine
  • Granisetron
  • Perphenazine
  • Gatifloxacin
  • Pipamperone
  • Fosphenytoin
  • Posaconazole
  • Formoterol
  • Procainamide
  • Fluconazole
  • Promethazine
  • Fingolimod
  • Protriptyline
  • Famotidine
  • Quinidine
  • Erythromycin
  • Ranolazine
  • Efavirenz
  • Risperidone
  • Droperidol
  • Sertindole
  • Donepezil
  • Sodium Phosphate
  • Dolasetron
  • Sodium Phosphate, Monobasic
  • Disopyramide
  • Sorafenib
  • Delamanid
  • Sulpiride
  • Dabrafenib
  • Tacrolimus
  • Crizotinib
  • Telaprevir
  • Clomipramine
  • Telithromycin
  • Citalopram
  • Tizanidine
  • Chlorpromazine
  • Toremifene
  • Bedaquiline
  • Trimipramine
  • Atazanavir
  • Vardenafil
  • Asenapine
  • Venlafaxine
  • Aripiprazole
  • Vinflunine
  • Anagrelide
  • Vorinostat
  • Amiodarone
  • Zuclopenthixol

Patients who engage in certain lifestyle activities such as the use of tobacco products or the regular intake of alcohol should inform their doctors of such practices as they may affect the way that their system reacts to nafarelin. Let your doctor know all the medications that you are currently taking or have recently stopped taking. Include information about both prescription and non-prescription medications, herbal remedies, and vitamin and mineral supplements.

Taking this medication on an empty stomach can affect the way you feel; it may take a few dosages to better understand how your system reacts to nafarelin. Discuss any concerns that you may have while taking this medication with the prescribing physician or another member of your healthcare team.

Certain foods may cause you to experience slight stomach discomfort or other temporary and mild symptoms. Patients are encouraged to actively manage the foods that they eat in order to minimize the occurrence of these symptoms. Discuss any concerns that you may have relating to your reactions to certain foods while taking nafarelin with your doctor.

If you suffer from any of the medical conditions listed here be sure to inform your doctor and also notify them of any significant reactions that you experience while taking nafarelin:

  • Abnormal or unusual vaginal bleeding
  • Ovarian cysts
  • Cigarette smoking
  • Rhinitis
  • Osteoporosis
  • Conditions that increase the chances of developing thinning bones
  • Pituitary gland problem
  • Alcohol abuse

Warnings

While taking this medication your doctor will likely order certain diagnostic testing such as blood and urine tests. It is important to keep all follow-up appointments and undergo all testing as scheduled. These tests will help your healthcare team to monitor the effectiveness of the treatment and also detect and manage any unwanted side effects that may occur.

Children may experience some signs of puberty as they begin their course of treatment. These reactions, such as growing breasts or light bleeding similar to that of a menstrual cycle, should clear up after a few weeks. If the symptoms persist longer than a month or if they worsen, it is advisable to discuss the situation with your doctor right away. Parents of young children should remain in close communication with their child's pediatrician while they are taking nafarelin.

For adult women using nafarelin spray for endometriosis:

Endometriosis symptoms may worsen as you begin your course of treatment but will improve over time. Do not change the way in which you take nafarelin without discussing such changes with your doctor first. Your menstrual cycle may become erratic as your body adjusts to the presence of the medication and is not a sign of a more serious issue. Discuss the situation with your physician if your cycle has not normalized after a period of a few months.

Women who are taking nafarelin should practice effective birth control as this medication should not be taken by pregnant women as it can cause serious harm to the developing fetus. Because nafarelin affects the estrogen production in women who are taking the medication hormonal birth control methods will not be effective. If you become pregnant while taking this medication it is important that you inform your doctor immediately.

Barrier contraception methods should be used during the nafarelin course of treatment. Utilize a condom, spermicide combined with an IUD, cervical cap, or diaphragm. Discuss any contraception concerns that you may have with your doctor, in a thorough manner, prior to beginning your course of treatment.

Storage

Like other medications, this drug should be stored in its original packaging. Patients should store this drug in an area of low moisture and away from direct light. Do not expose to extreme heat or cold. Do not freeze.

Keep this drug out of the reach of small children and pets.

At the conclusion of your course of treatment, it is important to dispose of any unused, excess, or expired medication in a safe and appropriate manner.

Once you have initially primed the bottle of medications, there will be 60 doses remaining. It is important to track the number of doses that you administer and to throw the bottle away following 60 doses, even if there is product remaining.

Summary

This drug is administered via a nasal spray and is used to treat both central precocious puberty (CPP) in young boys under the age of nine and girls younger than eight, as well as cases of endometriosis in adult women. This drug mimics a hormone that is produced in the hypothalamus gland called GnRH a gonadotropin-releasing hormone. GnRH works by decreasing the production of estrogen in women and girls and the release of the hormone testosterone in boys.

Puberty is considered early if the onset occurs before age nine in boys, and prior to age eight in girls.

By suppressing the production of hormones in boys and girls, testosterone and estrogen, respectively, nafarelin helps to curtail the effects of a medical condition known as central precocious puberty or CPP. This medication is only effective during the time in which it is taken and will not have any hold-over effects if the child stops taking the drug. Nafarelin is successful in thwarting the early development that can be associated with CPP such as early genital development in both genders and the development of breasts in young girls.

This drug should not be used by pregnant women or women who would like to become pregnant in the near future. The effects of nafarelin will last for six months following the conclusion of their course of treatment.

A barrier method of contraception must be used by women who are taking this drug as it affects the production of estrogen in their bodies in such a way that hormonal birth control will be ineffective. Prior to beginning their nafarelin course of treatment women of childbearing age are encouraged to discuss their contraception method.

This medication can cause serious harm to developing fetuses and should not be taken by pregnant women or women who wish to become pregnant in the near future. If you become pregnant while taking this drug, notify your doctor immediately.

Patients are advised to actively communicate with their doctor, or child's pediatrician, as this drug can have a significant impact on the future health of patients who are taking it.