NAFARELIN (Systemic)

Some commonly used brand names are:

In the U.S.?

• Synarel

In Canada?

• Synarel

Category

• Antiendometriotic agent
• gonadotropin inhibitor
• gonadotropin-releasinghormone analog

Description

Nafarelin (NAF-a-re-lin) is a hormone similar to the one normally released fromthe hypothalamus gland in the brain. It is used in the treatment of:

• Endometriosis, a painful condition caused by extra tissue similarto the lining of the uterus growing inside and outside of the uterus.
• Central precocious puberty (CPP), puberty developing too early inboys and girls.

When given regularly to boys and girls, this medicine helps to preventthem from continuing to develop the sexual features associated with puberty,slowing down the development of breasts in girls and the development of genitalareas in boys and girls. This medicine delays puberty in a child only as longas the child continues to take it.

Nafarelin prevents the growth of tissue associated with endometriosis inadult women during treatment and for 6 months after treatment is discontinued.Reducing the amount of estrogen in the body is one way of treating endometriosis.

Suppressing estrogen can thin the bones or slow their growth. This is aproblem for adult women whose bones are no longer growing like the bones ofchildren. Slowing the growth of bones is a positive effect for girls and boyswhose bones grow too fast when puberty begins too early. This is why nafarelinis used only for up to 6 months in adult women treated for endometriosis,but often is used for a longer time in girls and boys with pubertal problems.Boys and girls may benefit by adding inches to their adult height when nafarelincauses their bones to grow at a proper rate.

Nafarelin is available only with your doctor's prescription, in the followingdosage form:

Nasal
• Solution (U.S. and Canada)

Before Using This Medicine

In deciding to use a medicine,the risks of taking the medicine must be weighed against the good it willdo. This is a decision you and your doctor will make. For nafarelin, the followingshould be considered:

Allergies?Tell your doctor if you have ever had any unusual orallergic reaction to nafarelin or to gonadotropin-releasing hormone-likemedicines. Also tell your health care professional if you are allergic toany other substances, such as foods, preservatives, or dyes.

Pregnancy?Nafarelin use is not recommended during pregnancy.Nafarelin has not been studied in pregnant women. It has been shown to causeproblems in animals, such as low birth weights and a slight decrease in thenumber of successful pregnancies.

For treatment of endometriosis? Stop taking this medicine immediately and check with your doctorif you suspect that you may have become pregnant.

Breast-feeding?It is not known whether nafarelin passes into thebreast milk. However, use of nafarelin is not recommended during breast-feedingbecause it may cause unwanted effects in nursing babies.

Children?Studies of this medicine for treatment of endometriosishave been done only in adult patients, and there is no specific informationcomparing use of nafarelin to treat this condition in children younger than18 years of age with use in other age groups. Endometriosis is not likelyto occur before puberty.

When used to treat a child for central precocious puberty, nafarelin willstop having an effect soon after the child stops using it, and puberty willadvance normally. It is not known if nafarelin causes:

• Changes in boys' and girls' future abilities to have babies afterhaving used nafarelin around the time of puberty. Their chances of havingchildren later are thought to be normal.
• Problems in the ovaries, such as cysts or a larger than normal ovary.Nafarelin stimulates the ovaries in adult women and has caused these problemsin the ovary. It is not known whether nafarelin can also have these effectsin younger girls treated for central precocious puberty.

Other medicines?Although certain medicines should not be usedtogether at all, in other cases two different medicines may be used togethereven if an interaction might occur. In these cases, your doctor may want tochange the dose, or other precautions may be necessary. When you are takingnafarelin, it is especially important that your health care professional knowif you are taking the following:

• Nasal decongestant sprays?It is not known whether nasal decongestantsprays can decrease the amount of nafarelin that enters the bloodstream throughthe lining of the nose. For this reason, you should wait at least 2 hoursafter using nafarelin before you use a nasal decongestant spray

Other medical problems?The presence of other medicalproblems may affect the use of nafarelin. Make sure you tell your doctor ifyou have any other medical problems, especially:

• Bleeding from the vagina (abnormal or of unknown cause)?Foradult women treated for endometriosis or girls treated for central precociouspuberty, using nafarelin when the reason for vaginal bleeding is not knownmay make it harder for the doctor to find the cause of the problem, and maycause a delay in treatment of the condition
• Other conditions that increase the chances of developing thinningbones or osteoporosis (brittle bones)?If you are an adult female beingtreated for endometriosis, it is important that your doctor know if you alreadyhave an increased risk of osteoporosis. Some things that can increase yourrisk for having osteoporosis include cigarette smoking, alcohol abuse, anda family history of osteoporosis or easily broken bones. Some medicines, suchas corticosteroids (cortisone-like medicines) or anticonvulsants (seizuremedicine), can also cause thinning of the bones when used for a long time

Proper Use of This Medicine

You willbe given a fact sheet with your prescription for nafarelin that explains howto use the pump spray bottle. If you have any questions about using the pumpspray, ask your health care professional.

To use nafarelin spray:

• Before you use each new bottle of nafarelin, the spray pump needsto be started. To do this, point the bottle away from you and pump the bottlefirmly about seven times. A spray should come out by the seventh time youpump the spray bottle. This only needs to be done oncefor each new bottle of nafarelin. Be careful not to breathe in thisspray. You could inhale extra doses of nafarelin, since the medicine is dissolvedin the spray.
• Before you take your daily doses of nafarelin, blow your nose gently.Hold your head forward a little. Put the spray tip into one nostril. Aim thetip toward the back and outside of your nostril. You do not need to put thetip too far into your nose.
• Close your other nostril off by pressing on the outside of your nosewith a finger. Then, sniff in the spray as you pump the bottle once.
• Take the spray bottle out of your nose. Tilt your head back for 30seconds, to let the spray get onto the back of your nose.
• Repeat these steps for each dose of medicine.
• Each time you use the spray bottle, wipe off the tip with a cleantissue or cloth. Keep the blue safety clip and plastic cap on the bottle whenyou are not using it.
• Every 3 or 4 days you should clean the tip of the spray bottle. Todo this, hold the bottle sideways. Rinse the tip with warm water, while wipingthe tip with your finger or a soft cloth for about 15 seconds. Dry the tipwith a soft cloth or tissue. Replace the cap right after use. Be careful notto get water into the bottle, since this could dilute the medicine.

It is important to avoid sneezing when spraying and immediately after usingthe medicine. If you sneeze, the medicine may not be absorbed as well.

Use this medicine only as directed by your doctor. Do not use more or lessof it, and do not use it more often than your doctor ordered. The exact amountof medicine you need has been carefully worked out. Using too much may increasethe chance of side effects, while using too little may not improve your condition.

Many boys and girls who have central precocious puberty will not feel sickor will not understand the importance of taking the medicine regularly. Itis very important that the medicine is used exactly as directed and that theproper amount is used at the proper time. It works best when there is a constantamount in the blood. To help keep the amount constant, nafarelin must be givenon a regular schedule.

Dosing?The dose of nafarelin will be different fordifferent patients. Follow your doctor's orders or thedirections on the label. The following information includes only theaverage dose of nafarelin. If your dose is different,do not change it unless your doctor tells you to do so.

• For nasal solution dosage form:
  • For treating central precocious puberty:
    • Children?800 micrograms (mcg) (two sprays into each nostril)two times a day, once in the morning and once in the evening. This providesa total daily dose of eight sprays or 1600 mcg a day. Sometimes a larger dosemay be needed. 1800 mcg a day is provided by using three sprays in alternatingnostrils three times a day to provide a total of nine sprays a day.
  • For treating endometriosis:
    • Adults?200 mcg (one spray) inhaled into one nostril in themorning and one spray inhaled into the other nostril in the evening, for sixmonths. Begin your treatment on Day 2, 3, or 4 of your menstrual period.

Missed dose?If you miss a dose of this medicine, take it assoon as possible. However, if you do not remember until the next day, skipthe missed dose and go back to your regular dosing schedule. Do not doubledoses.

Storage?To store this medicine:

• Keep out of the reach of children.
• The bottle should be stored standing upright, with the tip up.
• Store away from heat and direct light.
• Keep the medicine from freezing. Do not refrigerate.
• Do not keep outdated medicine or medicine no longer needed. Be surethat any discarded medicine is out of the reach of children.

Precautions While Using This Medicine

All scheduledvisits to the doctor should be kept, even if the medicine seems to be workingproperly and you feel well. This is especially important for children usingthe medicine for treatment of central precocious puberty, even if their conditionimproves. Their progress still must be checked by the doctor when they areno longer using the medicine.

For children treated for central precocious puberty?Tell the doctor if nafarelin does not stop puberty from progressingwithin 6 to 8 weeks. You may notice puberty progressing in your child forthe first few weeks of therapy, but you should see signs that puberty is stoppingwithin 4 weeks after your child begins nafarelin therapy.

For adult women treated for endometriosis?

• During the time you are receiving nafarelin, your menstrual periodmay not be regular or you may not have a menstrual period at all. This isto be expected when being treated with this medicine. If regular menstrualperiods do not begin within 2 to 3 months after you stop using this medicine,check with your health care professional.
• To prevent pregnancy if you are sexually active during the time youare using nafarelin, you should use birth control methods that do not containhormones, such as condoms or a diaphragm or a cervical cap with a spermicide.If you have any questions about this, check with your health care professional.
• Use a water-based vaginal lubricant product if dryness of the vaginacauses problems, such as pain during sexual intercourse. Make sure the lubricantyou choose can be used with a latex birth control device if you are usingone. Some lubricants contain oils, which can break down the latex rubber ofcondoms, a cervical cap, or a diaphragm, and cause them to rip or tear.
• If you suspect you are pregnant, stop using thismedicine and check with your doctor immediately. There is a chancethat nafarelin could cause problems to the unborn baby if taken during a pregnancy.

Side Effects of This Medicine

In the first few weeks of therapy, you may notice puberty progressing inyour child, including vaginal bleeding and breast enlargement in girls. Within4 weeks after nafarelin has had time to begin working properly, you shouldsee signs in boys and girls that puberty is stopping. However, pubic hairmay continue to show or grow in either boys or girls.

Along with its needed effects, a medicine may cause some unwanted effects.Although not all of these side effects may occur, if they do occur they mayneed medical attention.

Check with your doctor as soon as possibleif any of the following side effects occur:

More common

For adults (female)

Breast enlargement; light vaginal bleedingbetween regular menstrual periods called spotting; longer or heavier menstrual periods; vaginal bleedingbetween regular menstrual periods called breakthrough bleeding

For children (male)

Body odor; growth of pubic hair

For children (female)

Body odor; breast enlargement; growth of pubic hair; light vaginalbleeding between regular menstrual periods called spotting; longer or heavier menstrual periods; vaginal bleedingbetween regular menstrual periods called breakthrough bleeding

Less common or rare

For adults (female)

Allergic reaction (shortness of breath, chest pain, hives); fast or irregular heartbeat; numbnessor tingling of hands or feet; pain in eyes or joints; patchy brown or dark brown discoloration of skin; pelvic bloating or tenderness; unexpected or excess milk flow from breasts; unusualtiredness or weakness

For children (male and female)

Allergic reaction (shortness of breath, chest pain, hives)

Other side effects may occur that usually do not need medicalattention. Some of these side effects may go away during treatment as yourbody adjusts to the medicine. However, check with your doctor if any of thefollowing side effects continue or are bothersome:

More common

For adults (female)

Acne; dandruff; hot flashes; increase or decrease in sexual desire; increased hair growth, often abnormally distributed; mood swings; muscle pain; oily skin; pain duringsexual intercourse; rapid weight gain; reduced breast size; stopping of menstrualperiods; swelling of feet or lower legs; vaginal dryness

For children (male)

Acne; dandruff; mood swings; oily skin

For children (female)

Acne; dandruff; hot flashes; mood swings; oily skin

Less common or rare

For adults (female)

Breast pain; headache (mild and transient); irritated or runny nose; mental depression (mild and transient); skin rash

For children (male)

Irritated or runny nose

For children (female)

Irritated or runny nose; white or brownishvaginal discharge

Other side effects not listed above may also occur in some patients. Ifyou notice any other effects, check with your doctor.