Vagifem

What is Vagifem?

• Vagifem (Estradiol insert) is an estrogen used for the treatment of atrophic vaginitis due to menopause.

Estradiol

Estradiol 3D ball

What are the uses of this medicine?

• Vagifem (Estradiol insert) is a medicine that contains estradiol (an estrogen hormone) in a vaginal insert.

Vagifem is used after menopause to:

• Treat menopausal changes in and around the vagina

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, 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.
• 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.

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 Vagifem or any of its ingredients
• think you may be pregnant

What drug interactions can this medicine cause?

• No drug-drug interaction studies have been conducted for Vagifem.
• Inducers and inhibitors of CYP3A4 may affect estrogen drug metabolism.

Is this medicine FDA approved?

• Initial U.S. Approval: 1999

How should this medicine be used?

Recommended dosage:

• Vagifem should be administered intravaginally using the supplied applicator: 1 insert daily for 2 weeks, followed by 1 insert twice weekly (for example, Tuesday and Friday).

Administration:

• Vagifem is an insert that you place in your vagina with an applicator.

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

This medicine is available in fallowing doasage form:

• As vaginal insert contains 10.3 mcg of estradiol hemihydrate equivalent to 10 mcg of estradiol

This medicine is available in fallowing brand namesː

• Vagifem

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
• Nausea and vomiting
• 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
• Enlargement of benign tumors of the uterus (“fibroids”)

What special precautions should I follow?

• Vagifem is intended only for vaginal administration. Systemic absorption occurs with the use of Vagifem.
• Estrogens increase 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. Discontinue estrogen if severe hypercalcemia, loss of vision, severe hypertriglyceridemia or cholestatic jaundice occurs.
• A few cases of local abrasion induced by the Vagifem applicator have been reported, especially in women with severely atrophic vaginal mucosa.
• Estrogen administration leads to increased thyroid-binding globulin (TBG) levels. Women with normal thyroid function can compensate for the increased TBG by making more thyroid hormone, thus maintaining free T4 and T3 serum concentrations in the normal range. Monitor thyroid function in women on thyroid replacement therapy.
• Retinal vascular thrombosis has been reported in women receiving estrogens. Discontinue medication pending examination if there is a sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia, or migraine.
• 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.
• Exogenous estrogens may exacerbate symptoms of angioedema in women with hereditary angioedema.
• For women known to have residual endometriosis post-hysterectomy, the addition of progestin should be considered.
• Estrogens may cause some degree of fluid retention.
• 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.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

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

Management of overdosage:

• Treatment of overdose consists of discontinuation of Vagifem therapy with institution of appropriate symptomatic care.

Can this medicine be used in pregnancy?

• Vagifem should not be used during pregnancy.

Can this medicine be used in children?

• Vagifem is not indicated in children.
• Clinical studies have not been conducted in the pediatric population.

What are the active and inactive ingredients in this medicine?

• Vagifem (estradiol vaginal inserts) are small, white, film-coated inserts containing estradiol.
• Each insert also contains hypromellose, lactose monohydrate, maize starch and magnesium stearate.
• The film coating contains hypromellose and polyethylene glycol.
• Each Vagifem insert is contained in a disposable applicator, packaged in a blister pack. Cartons contain 8 or 18 applicators with inset inserts.

Who manufactures and distributes this medicine?

• Vagifem® is a registered trademark owned by Novo Nordisk Health Care AG.

Manufactured by:

• Novo Nordisk A/S
• Bagsvaerd, Denmark

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

• Store at 25ºC (77ºF); excursions permitted to 15ºC to 30ºC (59ºF to 86ºF).
• Do not refrigerate.

• Dailymed label info on Vagifem
• FDA Vagifem

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