Ethinylestradiol/norethisterone acetate

What is Ethinylestradiol/norethisterone acetate?

• Ethinylestradiol/norethisterone acetate is a prescription medicine that contains two kinds of hormones, an estrogen and a progestin.

Ethinylestradiol

Norethisterone acetate

What are the uses of this medicine?

Ethinylestradiol/norethisterone acetate is a prescription medicine that contains two kinds of hormones, an estrogen and a progestin. Norethindrone acetate and ethinyl estradiol tablets are used after menopause to:

• Reduce moderate to severe hot flushes
• Help reduce your chances of getting osteoporosis (thin weak bones)

• If you use norethindrone acetate and ethinyl estradiol tablets only to prevent osteoporosis from menopause, talk with your healthcare provider about whether a different treatment or medicine without estrogens might be better for you. You and your healthcare provider should talk regularly about whether you still need treatment with norethindrone acetate and ethinyl estradiol tablets.

• Estrogens are hormones made by a woman's ovaries. The ovaries normally stop making estrogens when a woman is between 45 and 55 years old. This drop in body estrogen levels causes the "change of life" or menopause, the end of monthly menstrual periods. Sometimes both ovaries are removed during an operation before natural menopause takes place. The sudden drop in estrogen levels causes "surgical menopause".
• When estrogen levels begin dropping, some women get very uncomfortable symptoms, such as feelings of warmth in the face, neck, and chest, or sudden intense episodes of heat and sweating ("hot flashes" or "hot flushes"). In some women the symptoms are mild, and they will not need to take estrogens. In other women, symptoms can be more severe.

How does this medicine work?

• The primary source of estrogen in normally cycling adult women is the ovarian follicle, which secretes 70 to 500 mcg of estradiol daily, depending on the phase of the menstrual cycle.
• After menopause, most endogenous estrogen is produced by conversion of androstenedione, which is secreted by the adrenal cortex, to estrone in the peripheral tissues.
• Thus, estrone and the sulfate conjugated form, estrone sulfate, are the most abundant circulating estrogens in postmenopausal women.
• The pharmacologic effects of ethinyl estradiol are similar to those of endogenous estrogens.
• Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. To date, two estrogen receptors have been identified. These vary in proportion from tissue to tissue.
• Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and FSH through a negative feedback mechanism.
• Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.
• Progestin compounds enhance cellular differentiation and generally oppose the actions of estrogens by decreasing estrogen receptor levels, increasing local metabolism of estrogens to less active metabolites, or inducing gene products that blunt cellular responses to estrogen. Progestins exert their effects in target cells by binding to specific progesterone receptors that interact with progesterone response elements in target genes.
• Progesterone receptors have been identified in the female reproductive tract, breast, pituitary, hypothalamus, bone, skeletal tissue and central nervous system. Progestins produce similar endometrial changes to those of the naturally occurring hormone progesterone.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have unusual vaginal bleeding
• currently have or have had certain cancers
• had a stroke or heart attack
• currently have or have had blood clots
• currently have or have had liver problems
• have been diagnosed with a bleeding disorder
• are allergic to norethindrone acetate and ethinyl estradiol tablets or any of its ingredients
• think you may be pregnant
• have had your uterus (womb) removed (hysterectomy)

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Is this medicine FDA approved?

• Initial U.S. Approval: 1968
• In 2019, it was the 42nd most commonly prescribed medication in the United States, with more than 16 million prescriptions.

How should this medicine be used?

Recommended dosage: Treatment of Moderate to Severe Vasomotor Symptoms due to Menopause:

• Norethindrone acetate and ethinyl estradiol tablet therapy consists of a single tablet to be taken orally once daily.

Prevention of Postmenopausal Osteoporosis:

• Norethindrone acetate and ethinyl estradiol tablets therapy consists of a single tablet taken orally once daily.

Administration:

• Take norethindrone acetate and ethinyl estradiol tablets exactly as your healthcare provider tells you to take it.
• Take 1 norethindrone acetate and ethinyl estradiol tablet at the same time each day.
• You and your healthcare provider should talk regularly (every 3 to 6 months) about the dose you are taking and whether or not you still need treatment with norethindrone acetate and ethinyl estradiol tablets.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Round light yellow tablet contains 0.5 mg norethindrone acetate and 0.0025 mg ethinyl estradiol
• Round white tablet contains 1 mg norethindrone acetate and 0.005 mg ethinyl estradiol

This medicine is available in fallowing brand namesː

• Anovlar, Blisovi, Cumorit, Estrostep, FemHRT, Fyavolv, Gildess, Junel, Larin, Leribane, Loestrin, Lo Loestrin (Lo Lo), Mibelas, Microgestin, Minastrin, Norlestrin, Primodos, Taytulla, and Tri-Legest

• In addition, the combination is sold in the United States under the brand name FemHRT for use in menopausal hormone therapy.

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache
• breast pain
• irregular vaginal bleeding or spotting
• stomach or abdominal cramps, bloating
• hair loss
• fluid retention
• vaginal yeast infection

Serious, but less common side effects include:

• heart attack
• stroke
• blood clots
• dementia
• breast cancer
• cancer of the lining of the uterus (womb)
• cancer of the ovary
• high blood pressure
• high blood sugar
• gallbladder disease
• liver problems
• changes in your thyroid hormone levels
• enlargement of benign tumors of the uterus ("fibroids")

What special precautions should I follow?

• Inform postmenopausal women of the importance of reporting abnormal vaginal bleeding to their healthcare provider as soon as possible.
• Inform postmenopausal women of possible serious adverse reactions of estrogen plus progestin therapy including Cardiovascular Disorders, Malignant Neoplasms, and Probable Dementia.
• Inform postmenopausal women of possible less serious but common adverse reactions of estrogen plus progestin therapy such as headache, breast pain and tenderness, nausea and vomiting.
• Estrogen plus progestin therapy should not be used for the prevention of cardiovascular disease or dementia.
• The WHI estrogen plus progestin substudy also demonstrated an increased risk of invasive breast cancer. Estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman.
• A 2- to 4-fold increase in the risk of gallbladder disease requiring surgery in postmenopausal women receiving estrogens has been reported.
• Estrogen administration may lead to severe hypercalcemia in women with breast cancer and bone metastases. If hypercalcemia occurs, use of the drug should be stopped and appropriate measures taken to reduce the serum calcium level.
• Retinal vascular thrombosis has been reported in women receiving estrogens. Discontinue medication pending examination if there is sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia, or migraine.
• In a small number of case reports, substantial increases in blood pressure have been attributed to idiosyncratic reactions to estrogens.
• In women with pre-existing hypertriglyceridemia, estrogen therapy may be associated with elevations of plasma triglycerides leading to pancreatitis. Consider discontinuation of treatment if pancreatitis occurs.
• Estrogens may be poorly metabolized in women with impaired liver function. caution should be exercised and in the case of recurrence, medication should be discontinued.
• Estrogen administration leads to increased thyroid-binding globulin (TBG) levels. These women should have their thyroid function monitored in order to maintain their free thyroid hormone levels in an acceptable range.
• Estrogens plus progestins may cause some degree of fluid retention.
• Estrogen therapy should be used with caution in women with hypoparathyroidism as estrogen-induced hypocalcemia may occur.
• Exogenous estrogens may exacerbate symptoms of angioedema in women with hereditary angioedema.
• Estrogen therapy may cause an exacerbation of asthma, diabetes mellitus, epilepsy, migraine, porphyria, systemic lupus erythematosus and hepatic hemangiomas, and should be used with caution in women with these conditions.
• Norethindrone acetate and ethinyl estradiol tablets should not be used during lactation. Detectable amounts of estrogen and progestin have been identified in the breast milk of women receiving estrogen plus progestin therapy. Caution should be exercised when norethindrone acetate and ethinyl estradiol tablets are administered to a nursing woman.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• nausea
• vomiting
• breast tenderness
• abdominal pain
• drowsiness and fatigue
• withdrawal bleeding

Management of overdosage:

• Treatment of overdose consists of discontinuation of norethindrone acetate and ethinyl estradiol tablets with institution of appropriate symptomatic care.

Can this medicine be used in pregnancy?

• Norethindrone acetate and ethinyl estradiol tablets should not be used during pregnancy.

Can this medicine be used in children?

• Norethindrone acetate and ethinyl estradiol tablets are not indicated in children.

What are the active and inactive ingredients in this medicine?

• Active Ingredients: norethindrone acetate and ethinyl estradiol

• Inactive Ingredients: Each white tablet also contains lactose monohydrate, pregelatinized starch, polyethylene glycol, magnesium stearate, ethyl cellulose, vitamin E, titanium dioxide, hypromelloses, macrogol/PEG, triacetin, polydextrose.

• Each light yellow tablet also contains lactose monohydrate, pregelatinized starch, polyethylene glycol, magnesium stearate, ethyl cellulose, vitamin E, iron oxide yellow, iron oxide black, talc, polyvinyl alcohol, titanium dioxide, lecithin (soya).

Who manufactures and distributes this medicine?

Distributed by:

• Nivagen Pharmaceuticals, Inc.
• Sacramento, CA

Manufactured by:

• Novast Laboratories Ltd.
• Nantong, China

What should I know about storage and disposal of this medication?

• Store norethindrone acetate and ethinyl estradiol tablets at room temperature between 68° to 77° F (20° to 25° C).

• Dailymed label info on Ethinylestradiol/norethisterone acetate
• FDA Ethinylestradiol/norethisterone acetate

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