aygestin (norethindrone acetate) tablet
[DURAMED PHARMACEUTICALS, INC.]
Revised JULY 2005
Aygestin (norethindrone acetate tablets, USP) - 5 mg oral tablets. Aygestin, (17-hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one acetate), a synthetic, orally active progestin, is the acetic acid ester of norethindrone. It is a white, or creamy white, crystalline powder.
Aygestin Tablets contain the following inactive ingredients: lactose, magnesium stearate, and microcrystalline cellulose.
Norethindrone acetate induces secretory changes in an estrogen-primed endometrium. It acts to inhibit the secretion of pituitary gonadotropins which, in turn, prevent follicular maturation and ovulation. On a weight basis, it is twice as potent as norethindrone.
Aygestin is indicated for the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer.
Known or suspected pregnancy.
Thrombophlebitis, thromboembolic disorders, cerebral apoplexy, or a past history of these conditions.
Markedly impaired liver function or liver disease.
Known or suspected carcinoma of the breast.
Undiagnosed vaginal bleeding.
As a diagnostic test for pregnancy.
Hypersensitivity to norethindrone acetate tablets.
See text which appears at the end of this insert.
Some beagle dogs treated with medroxyprogesterone acetate developed mammary nodules. Although nodules occasionally appeared in control animals, they were intermittent in nature, whereas nodules in treated animals were larger and more numerous, and persisted. There is no general agreement as to whether the nodules are benign or malignant. Their significance with respect to humans has not been established.
Norethindrone acetate is contraindicated during pregnancy as it may cause fetal harm when administered to pregnant women. Several reports suggest an association between intrauterine exposure to progestational drugs in the first trimester of pregnancy and genital abnormalities in male and female fetuses. Hypospadias occurs in about 5 to 8 per 1, 000 male births and is about doubled with exposure to these drugs. Some progestational drugs induce mild virilization of the external genitalia of female fetuses.
Detectable amounts of progestogens have been identified in the milk of mothers receiving them. The effect of this on the nursing infant has not been determined.
Safety and effectiveness in pediatric patients have not been established.
See “WARNINGS” for further information on Retinal vascular thrombosis, Thrombotic and thromboembolism events, and Use in pregnancy.
The following adverse reactions have been observed in women taking progestins:
Change in menstrual flow.
Changes in weight (decreases, increases).
Changes in cervical erosion and cervical secretions.
Rash (allergic) with and without pruritus.
Melasma or chloasma.
Abnormalities of liver tests (i.e., AST, ALT, Bilirubin).
Thrombotic and thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism, retinal vascular thrombosis, cerebral thrombosis and embolism).
Optic neuritis (which may lead to partial or complete loss of vision).
Progestins may alter the result of pregnanediol determinations. The following laboratory results may be altered by the concomitant use of estrogens with progestins:
Coagulation tests - increase in prothrombin, factors VII, VIII, IX, and X.
Increase in PBI, BEI, and a decrease in T3 uptake.
Reduced response to metyrapone test.
The following adverse reactions have been observed in patients receiving estrogen-progestogen combination drugs:
In view of these observations, patients on progestogen therapy should be carefully observed.
Therapy with Aygestin® (norethindrone acetate tablets, USP) must be adapted to the specific indications and therapeutic response of the individual patient. This dosage schedule assumes the interval between menses to be 28 days.
Secondary amenorrhea, abnormal uterine bleeding due to hormonal imbalance in the absenceof organic pathology: 2.5 to 10 mg Aygestin may be given daily for 5 to 10 days during the second half of the theoretical menstrual cycle to produce an optimum secretory transformation of an endometrium that has been adequately primed with either endogenous or exogenous estrogen.
Progestin withdrawal bleeding usually occurs within three to seven days after discontinuing Aygestin therapy. Patients with a past history of recurrent episodes of abnormal uterine bleeding may benefit from planned menstrual cycling with Aygestin.
Endometriosis: Initial daily dosage of 5 mg Aygestin for two weeks. Dosage should be increased by 2.5 mg per day every two weeks until 15 mg per day of Aygestin is reached. Therapy may be held at this level for six to nine months or until annoying breakthrough bleeding demands temporary termination.
Aygestin® (norethindrone acetate tablets, USP) are available as:
5 mg: White, oval, flat-faced, beveled edge, tablet scored on one side. Debossed with 5 Aygestin on the unscored side and stylized b /424 on the scored side.
Available in bottle of:
Store at 20º to 25ºC (68º to 77ºF) [See USP Controlled Room Temperature].
Dispense in a well-closed container.
Your doctor has prescribed Aygestin (norethindrone acetate tablets, USP), a progestin, for you. Aygestin is similar to the progesterone hormones naturally produced by the body. Progestins are used to treat menstrual disorders and to test if the body is producing certain hormones.
AYGESTIN TABLETS SHOULD NOT BE USED IN WOMEN WITH THE FOLLOWING CONDITIONS:
The information below relates only to the risk to the unborn child associated with use of progestin during pregnancy, abnormal blood clotting, and eye abnormalities.
Aygestin tablets should not be used if you are pregnant. Norethindrone acetate is contraindicated during pregnancy as it may cause fetal harm when administered to pregnant women. There is an increased risk of minor birth defects in children whose mothers take this drug during the first 4 months of pregnancy. Several reports suggest an association between mothers who take these drugs in the first trimester of pregnancy and genital abnormalities in male and female babies. The risk to the male baby is the possibility of being born with a condition in which the opening of the penis is on the underside rather than the tip of the penis (hypospadias). Hypospadias occurs in about 5 to 8 per 1,000 male births and is about doubled with exposure to these drugs. There is not enough information to quantify the risk to exposed female fetuses, but enlargement of the clitoris and fusion of the labia may occur, although rarely. Therefore, avoid using the drug during the first trimester of pregnancy.
If you take Aygestin (norethindrone acetate tablets, USP) and later find you were pregnant when you took it, be sure to discuss this with your doctor as soon as possible.
Use of progestational drugs has been associated with changes in the blood-clotting system. These changes allow the blood to clot more easily, possibly allowing clots to form in the bloodstream. If blood clots do form in your bloodstream, they can cut off the blood supply to vital organs, causing serious problems. These problems may include a stroke (by cutting off blood to part of the brain), a heart attack (by cutting off blood to part of the heart), a pulmonary embolus (by cutting off blood to part of the lungs), visual loss or blindness (by cutting off blood vessels in the eye), or other problems. Any of these condition may cause death or serious long-term disability. Call your doctor immediately if you suspect you have any of these conditions. He or she may advise you to stop using the drug.
Discontinue medication and call your physician immediately if you experience sudden partial or complete loss of vision, blurred vision, or sudden onset of bulging eyes, double vision, or migraine.
For further information on the use, side effects and other risks associated with this product, ask your doctor. If you want more information, ask your doctor to show you the professional labeling. The professional labeling is also published in a book called the Physicians’ Desk Reference, which is available in bookstores and public libraries.
DURAMED PHARMACEUTICALS, INC.
A subsidiary of Barr Pharmaceuticals, Inc.
Pomona, New York 10970
Revised JULY 2005
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