Estradiol vaginal cream, 0.01% is indicated in the treatment of moderate to severe symptoms of vulvar and vaginal atrophy due to menopause.

Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Although circulating estrogens exist in a dynamic equilibrium of metabolic interconversions, estradiol is the principal intracellular human estrogen and is substantially more potent than its metabolites, estrone and estriol at the receptor level.

The usual dosage range is 2 to 4 g (marked on the applicator) daily for one or two weeks, then gradually reduced to one half the initial dosage for a similar period. A maintenance dosage of 1 g, one to three times a week, may be used after restoration of the vaginal mucosa has been achieved.

Administration

Step 1: Wash hands thoroughly with soapy water.
Step 2: Open the sealed wrapper and remove the applicator.
Step 3: Insert the tip of the applicator into the tube.
Step 4: Press down the tube and squeeze the specified amount of gel (2g - 4g indicated marking) into the applicator tube.
Step 5: Remove the applicator from the tube.
Step 6: Gently insert the rounded tip of the applicator into the vagina.
Step 7: Push the plunger to release the gel.
Step 8: After releasing the gel, remove the applicator, keep the applicator clean and germ-free for later use.

Phenobarbital, carbamazepine, and rifampin may reduce plasma concentrations of estrogens, possibly resulting in a decrease in therapeutic effects and/or changes in the uterine bleeding profile. Erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, and grapefruit juice may increase plasma concentrations of estrogens and may result in side effects.

Estradiol vaginal cream should not be used in women with any of the following conditions:

• Undiagnosed abnormal genital bleeding.

• Known, suspected, or history of cancer of the breast.

• Known or suspected estrogen-dependent neoplasia.

• Active deep vein thrombosis, pulmonary embolism, or history of these conditions.

• Active or recent (e.g., within the past year) arterial thromboembolic disease (e.g., stroke, myocardial infarction).

• Liver dysfunction or disease.

• Estradiol vaginal cream should not be used in patients with known hypersensitivity to its ingredients.

• Known or suspected pregnancy. There is no indication for estradiol vaginal cream in pregnancy. There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins from oral contraceptives inadvertently during early pregnancy

Headache, breast pain, irregular vaginal bleeding or spotting, stomach or abdominal cramps, bloating, nausea and vomiting, hair loss, fluid retention, vaginal yeast infection. Reactions from inserting the vaginal cream, such as vaginal burning, irritation, itching, etc.

This product should not be used during pregnancy. There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins as an oral contraceptive inadvertently during early pregnancy.

Patients taking an additional progestin with this product may have endometrial hyperplasia, which is a precursor to endometrial cancer. These include a possible increased risk of breast cancer. Patients may also face elevated blood pressure, hypertriglyceridemia (if she has pre-existing hypertriglyceridemia). Caution should be taken for patients who have hepatic impairment and/or past history of cholestatic jaundice, hypothyroidism, hypocalcemia. Estrogen may cause exacerbation of endometriosis, asthma, diabetes mellitus, epilepsy, migraine or porphyria, systemic lupus erythematosus, and hepatic hemangiomas. So, this product should be used with caution in women with these conditions.

Overdosage of estrogen may cause nausea, vomiting, breast tenderness, abdominal pain, drowsiness and fatigue, and withdrawal bleeding may occur in women. Treatment of overdose consists of discontinuation of therapy together with institution of appropriate symptomatic care.

Drugs used in Vaginal and Vulval conditions

Do not store above 30°C. Keep away from light and out of the reach of children.