Nafarelin is an artificially prepared protein. Its main action in the body is to block the effects of GnRH, that is, gonadotropin releasing hormone. GnRH is a hormone that stimulates the pituitary gland to secret gonadotropins. Pituitary gland is a tiny gland found at the base of our brain, and gonadotropins are another class of hormones secreted by it.
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Gonadotropins are of two types - FSH or Follicle Stimulating Hormone and LH or Luteinizing Hormone. Both, FSH and LH, cause the ovaries in women's body to produce estrogen. Continuous administration of nafarelin to women of reproductive ages, blocks the effects of GnRH and stops the secretion of gonadotropins, both FSH and LH. This, in turn, suppresses the production of estrogen in the women's body. Estrogen is instrumental in regulating the menstrual cycle of women, and suppression of its production stops menstruation resulting in a "menopause" like state which is, however, temporary and reversible. This temporary menopausal state gives rise to a condition, called endometrium, in which the linings of the uterus are shrunk or constricted.
Another function of FSH and LH is to regulate the onset of puberty, in girls as well as boys. This they do by promoting the development of secondary sexual characteristics, like pubic hair. Continuous administration of nafarelin delays the onset of puberty by slowing down the development of these secondary sexual characteristics. Increased levels of FSH and LH in the body, that occur sometimes due to some problems in brain, are associated with early puberty, called central precocious puberty. This is characterized by an abnormal skeletal development along with early development of secondary sexual characteristics. Nafarelin also reduces the severity of this abnormal skeletal development.
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Nafarelin received the approval of FDA in February, 1991.
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Nafarelin mainly finds use in relieving pain and discomfort associated with endometriosis, and treating children suffering from early onset of puberty which may or may not be accompanied by abnormal skeletal growth.
Nafarelin is used in the form of a nasal spray.
Before using this spray, read the leaflet containing usage instructions as well as important information for patients, that accompanies the product. Make sure that you understand all the instructions regarding preparation and usage. If you have any doubts, clarify them by talking to your doctor or pharmacist. If you are a first time user, also follow the instructions regarding proper priming of the bottle.
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Before using nafarelin, blow your nose gently. If being given to very young children, clearing the nostrils with a bulb syringe may be required.
Nafarelin is usually used twice daily, that is, at intervals of 12 hours, or as directed by the doctor. If you have been advised more than one spray at a time, wait for 30 seconds after each spray. Take care that the spray does not enter the eyes.
Sneezing may reduce the amount of the medication absorbed by the nostrils, so try not to sneeze during a spray, or immediately after it.
The spray tip should be cleaned after each use. Follow the instructions for cleaning the spray tip, and otherwise using the spray.
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The dosage and duration of nafarelin therapy is determined by the severity of your condition, as well as the response of your body to it. For endometriosis in women, the normal duration of the therapy is 6 months, unless directed otherwise by your health worker. In cases of early puberty in children, the therapy continues till the time is appropriate, in the doctor's opinion, for the onset of puberty to resume.
To derive the optimum benefits of nafarelin therapy, it must be used regularly. Missing even a single dose may reduce the efficacy of the therapy. For ease of remembering, fix a time to use it every day. Obtain refills a few days before required, so that you don't miss a dose if, for some reason, you are unable to get a refill on the last day.
Every bottle of the spray should be used within a certain time period after opening it. Ask your doctor what this time period is and don't use the spray after it, even if there is some medication still left in it. If you use this left-over, you might not be getting full amount of the medication.
Don't increase either the dosage or the frequency of the medication on your own. This will not result in a faster improvement, but will seriously increase the risk of harmful side effects. Conversely, don't reduce the dosage or frequency, or stop use, without first getting the approval of your doctor. This may make your body stubborn to the effects of medication, and render your condition too difficult to improve.
If the use of a nasal decongestant spray is required while you are on nafarelin, use it at a gap of at least two hours after taking nafarelin spray.
Initially, the nafarelin therapy may lead to worsening of symptoms. For example, cases of endometriosis may see increase in vaginal bleeding, or bleeding period. Similarly, cases of early onset of puberty may witness increase in pubic hair or breast size, increased body odour, and oily skin. These symptoms gradually disappear after about a month of treatment. However, if they persist or continue worsening even after two months, inform your doctor immediately.
Continuous administration of nafarelin ultimately causes the ovaries to stop producing estrogen, or reduce its production. Reduced estrogen levels in the blood cause the linings of the uterus, or endometrial tissues, to shrink, thereby easing the flare-ups of endometriosis.
Besides, during treatment and up to six months after discontinuing it, nafarelin hinders the growth of tissues associated with endometriosis in women. This enhances the benefits of reduced estrogen production in the body.
In cases of early onset of puberty, nafarelin acts by decreasing the amount of estrogen production in girls, and testosterone in boys. Therefore, a regular administration helps in preventing the continued development of secondary sexual characteristics associated with puberty, in both. This is manifested in reduced growth of pubic hair and genital areas, as well as bones, in both boys and girls, and slowed down development of breasts in girls. The development of these secondary sexual characteristics is resumed once the medication is stopped.
One handicap in administering nafarelin to women suffering from endometriosis is that prolonged suppression of estrogen production may result in thinning down of the bones or a slowed down bone growth. While this is a desirable effect for boys and girls with early onset of puberty which is often accompanied by an abnormal bone growth, it can cause problems to adult women whose bones may no longer be growing like those of children. This is why the duration of nafarelin therapy for endometriosis in adult women is limited to six months, while it is often much longer for the treatment of problems related to early puberty in young boys and girls. In the latter case, proper bone growth as a result of nafarelin therapy may also result in attaining proper heights by boys and girls later on.
Normal functions of ovaries, that is ovulation, menstruation, and the like, are resumed within 4-8 weeks of discontinuing nafarelin therapy.
The bottle of nafarelin spray should be stored at room temperature, away from light, heat or moisture (so, not near fireplace or in bathroom), in an upright position. The contents of the bottle should not be transferred to any other container, and the bottle itself should be kept tightly closed, away from the reach of children. Medication left in the bottle after the safe period of use should not be used. Ask your pharmacist how to dispose it safely.