Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.
Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.
DRUG CLASS AND MECHANISM: Nafarelin is a synthetic (man-made) protein that
blocks the effects of the natural gonadotropin-releasing hormone (GnRH), a
hormone that regulates the output of gonadotropins (a class of hormones) by the
pituitary gland (a small gland located at the base of the brain). Gonadotropins
(follicle stimulating hormone or FSH and luteinizing hormone or LH) are hormones
that cause estrogen production by the ovaries. When nafarelin (known
scientifically as a GnRH analog) is administered continuously to women in their
reproductive years, the pituitary output of FSH, LH, and the production of
estrogen by the ovaries are suppressed. Suppression of estrogen production
causes menstruation to stop, resulting in a temporary (but reversible) state of
"menopause." This temporary state of menopause results in shrinkage of the lining of the
uterus, known as the endometrium.
Endometriosis is a condition whereby the cells
that normally form the endometrium inside of the uterus are instead found
outside of the uterus. These abnormally located cells (called endometrial
implants) are most commonly found on the ovaries, 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 like blood from the uterus can.) 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.
FSH and LH also control the onset of puberty in boys and girls. Therefore,
administration of nafarelin blocks the puberty-promoting effects of FSH and LH,
reducing the development of secondary sexual characteristics (such as pubic
hair) and skeletal development in boys and girls with abnormally early puberty
(central precocious puberty) due to problems in the brain that result in high
levels of FSH and LH. The FDA approved nafarelin in February 1991.
PRESCRIPTION: Yes
GENERIC AVAILABLE: No
PREPARATIONS: Nasal spray: 200µg/spray
STORAGE: Nafarelin should be stored at room temperature, 15 to 30 C (59 to 86
F).
PRESCRIBED FOR: Nafarelin is prescribed for the management of endometriosis,
to relieve pain and shrink endometrial implants. It also is used for managing
central precocious puberty.
DOSING: For treatment of endometriosis nafarelin is given as one spray (200
µg) into one nostril in the morning and one spray in the other nostril in the
evening for 6 months. The first dose of nafarelin should 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 menstruation may stop altogether. For women who continue to experience
normal menstrual cycles after two months of treatment, the daily dose may be
increased to 800 µg daily.
Central precocious puberty is treated with 1600-1800 µg daily administered as
four sprays in alternating nostrils twice daily or three sprays in alternating
nostrils three times daily. Thirty seconds should elapse between sprays.
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 a
diaphragm with
contraceptive jelly, IUD, or condoms) while taking nafarelin.
Endometriosis is the growth of cells similar to those that form the inside of the uterus, but in a location outside of the uterus. Endometriosis 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. They can also be found in the vagina, cervix, and bladder. Treatment of endometriosis can be with medication or surgery.
Premenstrual dysphoric disorder (PMDD) is considered to be a severe form of premenstrual syndrome (PMS). PMDD has also been referred to as late luteal phase dysphoric disorder. The cause of PMDD is unknown. Some of the common symptoms of PMDD (not an inclusive list) include: mood swings, bloating, fatigue, headache, irritability, headache, breast tenderness, acne, hot flashes and more. Treatment for PMDD is with medication to treat the symptoms of PMDD.
Premenstrual dysphoric disorder (PMDD) can be considered to be a severe form
of premenstrual syndrome (PMS). Both PMS and PMDD are characterized by
unpleasant physical and psychological symptoms that occur in the second half of
a woman's menstrual cycle,
most commonly in the days preceding the menstrual period. Fatigue, mood changes, irritability, and abdominal bloating are among the most common symptoms of PMS and PMDD, but numerous other symptoms have been reported. Whereas the symptoms of PMS may be troubling and unpleasant, PMDD may cause severe, debilitating symptoms that interfere with a woman's ability to function.
PMS is much more common than PMDD. PMS may affect to 30% of women with regular menstrual cycles, while only 3% to 8% of these women have true PMDD.
PMDD has been previously medically referred to as late luteal phase dysph...