Estradiol Cream

 

Topical cream of estradiol is used to treat and prevent heat-related suffocation (hot flashes, hot flashes, strong and sudden sensation of heat and perspiration) in women who are in menopause (change of life; Menstruations).

Topical estradiol cream is also used to treat dryness, pruritus (itching), and vaginal burning in women who are in menopause. However, women whose discomfort is only burning, pruritus and vaginal dryness may benefit most by using the topically (local) medication in the vagina. Estradiol belongs to a class of medications called estrogen hormones. It works by replacing the estrogen that is normally produced by the body.

Dosage:

The normal dose is 2.5 g daily. In more severe cases 5 g can be applied in a single daily dose. The treatment is 1 application daily for 30 days. In hysterectomized patients use estrogen alone and in those with intact uterus use the cyclic form (for 12 or 14 days a progestogen can be added). The effective dosage may vary between patients for individual pharmacokinetics or according to residual postmenopausal estrogen production.

Absolute Pharmacy’s non-sterile solutions are compounded under the stringent USP 795 guidelines. The dosage may be readapted after the 2nd or 3rd cycle, depending on the following clinical signs: Excessive dose: breast tension, anxiety, aggression, leucorrhoea, chloasma and hypermenorrhea. In these cases the dose can be applied every 2 days. Insufficient dose: hot flashes, depressive tendency, asthenia. In these cases the dose can be increased to double.

Mechanism of Action:

Estradiol (E2) freely enters the cells and interacts with the cellular receptor. Inside the cytosol, it is first fixed to a receptor protein called 8-S that is unable to traverse the nuclear membrane. But, soon, the hormone is transferred to another 5-S protein that, through the library, puts estradiol in contact with nuclear DNA. Estradiol activates the DNA and, under its influence, it replicates RNA that leaves the nucleus, goes to the ribosomes and there generates the specific metabolic effects, of which, the most important, but not the only one is a protein synthesis.

Use:

It is usually applied once a day. The estradiol cream should be applied in the morning, but should be done around the same time every day. Follow the instructions on the prescription label carefully and ask your doctor or pharmacist for anything you do not understand. Use the medication exactly as directed. Do not use more or less than the indicated dose or more often than prescribed by your doctor. Make sure that the skin where you will apply the medication is clean and dry, and is not red, irritated or injured.

If you take a bath or shower, or use a sauna, apply the cream after you have left the shower, bath or sauna and the skin has completely dried. If you are going to swim, allow as much time as possible between the time you applied the estradiol cream and the time to go swimming. Do not apply sunscreen sooner, at the same time or soon after applying estradiol cream to the skin.

Use of the vaginal cream of estradiol:

Using the annotated applicator provided, measure the dose of prescribed cream. Lie on your back with your knees bent, sit or stay in a comfortable position that allows you access to the vagina area. To administer the medication, gently insert the applicator deep into the vagina and depress the plunger down into its original position.

Clean the applicator by pulling the plunger out of the barrel. Wash with mild soap and warm water. Have annual physicals and examine your breasts monthly for lumps while you are using estradiol.

Pharmacokinetics:

About 10% of the applied dose is absorbed and forms a transient subcutaneous deposit, which allows a slow systemic diffusion, carried out essentially by the lymphatic route. A maximum plasma concentration is obtained after a single dose approximately 12 hours later and then stabilized.

As a natural hormone, estradiol is metabolized as such and is eliminated by the urinary and fecal route. The bioavailability of estradiol cream is 32-50% compared to oral administration; 2.5 g of cream deliver approximately 1.50 mg of estradiol.

Contraindications:

The following are some of the contraindications – Breast cancer, personal history or suspicion of it. Also, there is malignant or suspected dependent estrogen tumors (eg endometrial cancer), undiagnosed vaginal bleeding and untreated endometrial hyperplasia, as well as idiopathic venous thromboembolism (VTE) or antecedents thereof (deep venous thrombosis, pulmonary embolism); known thrombophilic alteration.

Active or recent arterial thromboembolic (eg angina, myocardial infarction); hypersensitivity to estradiol; acute liver disease or history of emph. Liver function tests remain altered; premalignant tumors (eg, untreated atypical endometrial hyperplasia).

Pregnancy: Estradiol may increase your risk of developing a medical condition that can become cancer of the uterus. Call your doctor at once if you have any unusual vaginal bleeding while you are using this medicine.

Breast- Feeding: Debe tenerse precaución durante la lactancia materna y el uso de estradiol; El bebé puede necesitar ser monitoreado para efectos secundarios tales como: agrandamiento de pecho, crecimiento inapropiado, falta de apetito y aumento de peso.

Estradiol cream should not be used to prevent heart disease, stroke, or dementia, because this medicine may increase your risk of developing these conditions. Prolonged use may increase the risk of breast cancer or blood clot.

Interactions:

Efficacy decreased by: carbamazepine, phenytoin, phenobarbital, meprobamate, phenylbutazone, bosentan, rifampicin, rifabutin, nevirapine or efavirenz. Plasma concentrations increased by: ketoconazole, erythromycin, ritonavir or St. John’s wort.

Other drugs may interact with estradiol, including over-the-counter and prescription medicines, vitamins, and herbal products. Tell each of your health care providers about all the medicines you are currently using, and any medicines you start or stop.

Adverse Reactions:

Estradiol increases the risk of getting a medical condition (endometrial hyperplasia) that can become cancer of the walls of the uterus. Taking progestin, another hormonal drug, in combination with estradiol decreases the risk of getting this condition. Therefore, if your uterus has not been removed, your doctor may prescribe a progestin to take at the same time as you use estradiol. Visit your doctor regularly and report any unusual vaginal bleeding immediately.

Long-term treatment with estradiol may increase the risk of having a stroke. Because of this risk, you should contact your doctor or health care professional to discuss your personal risks and benefits before using estradiol for a long time. You should also talk to your doctor or health care professional regularly (for example, every 3 to 6 months) if you should continue with this treatment.

If you experience any of the following serious side effects, stop using estradiol and seek emergency medical attention:

– An allergic reaction (difficulty in breathing, closing of the throat, swelling of the lips, tongue or face, or hives);

– Shortness of breath or chest pain;

– One leg swollen, red, sore;

– Abnormal vaginal bleeding;

– Pain, swelling or tenderness in the abdomen;

– Severe headache or vomiting, dizziness, fainting or changes in vision or speech;

– Yellowing of the skin or eyes; or

– A lump in the breast.

There may also be other side effects not listed here. Talk to your doctor about any side effects that seem unusual or that bother you.

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