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nafarelin, Synarel

GENERIC NAME: nafarelin

BRAND NAME: Synarel

DRUG CLASS AND MECHANISM: Nafarelin is a synthetic protein chemically similar to the natural gonadotropin-releasing hormone (GnRH), a hormone that regulates the output of gonadotropins by the pituitary gland (a small gland located at the base of the brain). Gonadotropins (FSH and LH) are hormones necessary for estrogen production by the ovaries. When nafarelin (known scientifically as a GnRH analog) is administered continuously to a women in her reproductive years, the pituitary output of FSH and LH, along with the ovary output of estrogen are suppressed. Suppression of estrogen production causes menstruation to stop, resulting in a temporary (but reversible) state of " menopause ". This temporary menopause is important in shrinking endometriosis tissue and in relieving pain of endometriosis.

Endometriosis is a condition whereby the cells which normally form the inside of the uterus (endometrium) are instead found outside of the uterus. These abnormally located cells (called endometrial implants) are most commonly found on the ovaries, the fallopian tubes, outer surfaces of the uterus or intestines, and on the surface lining of the pelvic cavity. Like the normal endometrium, implants respond to the hormones of the menstrual cycle, i.e., they build up during the month, then break down and bleed during menstruation. However, unlike normal endometrium, the implants bleed internally (blood from implants cannot exit the body). The internal bleeding, followed by tissue inflammation and subsequent scarring, is believed to be responsible for the symptoms of pain and infertility in women with endometriosis. Nafarelin has been found to be effective in relieving the pain of endometriosis and shrinking the endometrial implants.

Please read the Endometriosis article for further information and different treatment options (medical and surgical) of this condition.

PRESCRIPTION: yes

GENERIC AVAILABLE: no

PREPARATIONS: nasal spray

STORAGE: Store the bottle upright at room temperature. Avoid temperatures above 86 degrees F (30 degrees C), and protect bottle from light.

PRESCRIBED FOR: Nafarelin is prescribed for the management of endometriosis, including pain relief and shrinking of the endometrial implants.

DOSING: Unless the doctor has given special instructions, nafarelin is given twice daily (about every 12 hours) for a total of 6 months. The first dose of nafarelin is to be taken between the second and fourth day after menstrual bleeding begins. After the first two months of nafarelin treatment, most women can expect a decrease in menstrual flow, and periods may stop altogether. Women who continue to experience normal menstrual cycles after two months of treatment should be re-evaluated by their doctors.

For optimal effectiveness and safety, nafarelin has to be given continuously without interruption. Missing one or more doses can cause vaginal bleeding . Missing successive doses can cause release of an egg from the ovary (ovulation) and result in pregnancy, unless proper contraceptive measures have been followed. Since birth control pills cannot be used with nafarelin, it is important to use non-hormonal methods of contraception ( such as diaphragm with contraceptive jelly, IUD, or condoms) while taking nafarelin.

Absorption of nafarelin is not affected by a cold or runny nose. If decongestants nasal spray are needed, they should be taken 30 minutes or more after using nafarelin.

DRUG INTERACTIONS: Nafarelin should not be used by women with undiagnosed abnormal menstrual bleeding.

The low estrogen state and the temporary menopause induced by nafarelin can cause a small amount of bone thinning, which may only partially recover after stopping treatment. During one 6 month treatment period, the amount of bone thinning is usually not significant. Patients should discuss this possibility with their doctors, and alert their doctors to conditions that can increase the risk of bone thinning. These conditions include chronic tobacco use, excessive use of alcohol, family history of osteoporosis , and taking other medications that can cause bone thinning (such as anticonvulsants or corticosteroids).

PREGNANCY: Nafarelin should not be used in pregnancy or in women who may become pregnant while receiving the medication. Safe use of nafarelin in pregnancy has not been established. Pregnancy must be excluded before starting treatment with this medication, and a non-hormonal method of contraception should be used during treatment.

NURSING MOTHERS: Nafarelin should not be used by nursing mothers.

SIDE EFFECTS: Side effects of nafarelin are mostly related to the low estrogen state. Side effects include hot flashes, vaginal dryness, headaches, mood changes, and decreased interest in sex. Some patients may experience acne , muscle pain, reduced breast size, and irritation of the tissue inside the nose. These side effects should disappear after stopping the medication.

Last updated on 05/15/2008

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