Estogel (Estradiol 0.06%)

What is Estogel used for?

Hormone replacement therapy (HRT) is a familiar term when talking about the changes women go through at menopause. They are caused by a lack of the hormone estrogen, and although a natural part of life, menopause can cause severe problems for some women. Various types of HRT are available, and Estogel 0.06% gel is a topical form of HRT that is absorbed through the skin instead of being taken as a tablet.

Estrogen is the female hormone produced by the ovaries that transforms the girl into the woman and plays a central role in all stages of female reproduction, along with other female hormones like progesterone. Estrogen stimulates the development of female sexual characteristics, including breast development and body shape. It regulates the menstrual cycle, triggers ovulation, and stimulates the thickening of the endometrium (lining of the uterus) and thickening of vaginal tissue and its secretions. It also plays other essential roles, including regulating lipid (fat) metabolism, and it supports bone density throughout the fertile years of a woman’s life. As menopause approaches, estrogen production starts to slow down, and eventually, no more is produced by the ovaries. Menstruation ceases, and this lack of estrogen brings with it a host of menopausal symptoms, some mild and some quite severe.

What are the symptoms of menopause?

Symptoms associated with low estrogen in menopause include hot flashes caused by sudden dilation of surface blood vessels. When this happens at night, they cause night sweats.  Vaginal thinning and dryness known as atrophic vaginitis can cause discomfort or pain with sex and recurrent urine infections. Other signs of menopause are headaches, mood swings, lack of concentration and loss of energy.

Loss of bone density is a serious problem related to loss of estrogen, which can lead to osteoporosis. This makes the bones brittle so that they fracture more easily. Estogel gel relieves symptoms of menopause and also helps prevent postmenopausal bone loss, known as osteoporosis, which reduces the risk of fracture.

Transgender hormone therapy

Estrogen is an essential component in transgender hormone therapy for male to female transsexuals as part of a gender reassignment program.  Estogel gel helps stimulate the development of female sexual characteristics, to promote the feminisation process, such as breast development. It also induces metabolic changes such as fat distribution to redefine the general body shape.

How does Estogel work?

Estogel 0.06% is a transdermal gel that contains a synthetic form of estradiol that is chemically and biologically identical to naturally produced Hormone. Estradiol, also known as 17 beta estradiol, is the primary and most active form of the female hormone estrogen.

Estradiol in Estogel gel 0.06% diffuses out of the gel and is absorbed through the skin into the blood. It works by passing through the cell membrane and binding to specific receptors inside the cells of its target tissues.  These include the ovaries, uterus, bone, and breast tissue. Estrogen attached to its receptor then interacts directly with the DNA. This interaction promotes the expression (activation) of specific genes, which then direct the synthesis of proteins needed for estrogen-dependent processes in those tissues. These include breast cell growth, improved lubrication of vaginal cells and increased bone density.

Estradiol in Estogel gel gets into the bloodstream directly through the skin. It does not enter the gastrointestinal system, which means that it is not broken down (metabolised) by the liver, as happens when estrogen is taken orally as a tablet. This results in more of the hormone being available to its target tissues, known as bioavailability.

What does Estogel contain?

Estogel contains the active ingredient 17 beta estradiol 0.06%, which is used for hormone replacement therapy (HRT) to relieve symptoms of estrogen deficiency in menopausal women. It is a clear, colourless gel and also contains ethanol, trolamine and carborner. Each 2.5g dose of Estogel contains 1.5mg estradiol.

What are the side effects of Estogel?

Most medications have some side effects, but they are not experienced by everyone. Some side effects are commonly experienced when taking Estogel, but others are not so common, and you should discuss any problems or concerns with your primary care physician.

Common side effects when taking Estogel include skin irritation where the gel is applied, breast tenderness, breast pain, abdominal pain, nausea, oedema, and headache, breakthrough bleeding and spotting.

What are the health risks of Estogel?

Long-term use of estrogen-only HRT medication like Estogel gel does have risks attached, and it is, therefore, important to consider the risks versus the benefits. There is an increased risk of breast cancer and endometrial cancer; also stroke and blood clot formation, that can result in deep vein thrombosis.

You should only use Estogel gel alone if you have had a hysterectomy or are also taking progesterone as well, because of the health risk of estrogen-only HRT.

When should Estogel not be used?

Have a talk with your primary healthcare physician before using Estogel 0.06% so that you have a full understanding of what this medicine is for and how to use it. There are some reasons for not taking a medication; these are called contraindications, and for Estogel you should consider the following before taking Estogel:

• Have you ever had an unusual reaction or an allergy when using Estogel?
• Are you pregnant or breastfeeding?
• Do you have any problems with your kidneys or your liver?
• Do you have or ever had liver disease?
• Have you had an estrogen-dependent cancer including cancer of the breast or endometrium?
• Have you had any condition caused by a blood clot such as deep vein thrombosis (blood clots in the leg), pulmonary embolism (blood clot in the lungs)?
• Do you have a heart condition like angina, and have you ever had cardiovascular disease, including a heart attack or stroke or uncontrolled high blood pressure?
• Have you had abnormal genital bleeding of unknown cause?

What medications interact with Estogel?

Some medicines interact with Estogel gel 0.06%and may affect the way it works or are affected by Estogel or increase side effects; you should discuss possible interactions with your primary care physician.  These may include medications that increase the metabolism of estrogen, such as anticonvulsants like phenytoin and carbamazepine, anti-infectives like rifampicin, rifabutin, nevirapine, efavirenz or preparations containing St John’s Wort.

If other medications may interact with Estogel, your doctor will discuss these with you.

How should Estogel be used and for how long?

You should apply one spatula of Estogel gel 0.06% once daily for at least 25 days per month, using the measuring spatula provided. Your doctor may adjust the dose you require, and you should use your Estogel gel for as long as your doctor recommends.

You should apply Estogel gel by rubbing into clean, dry, unbroken skin on your abdomen, thighs, arms, and shoulders but not the breasts or face. Use a different site for each application. Do not apply to skin that is red or irritated and avoid contact with your eyes. Allow the gel to dry on your skin for a few minutes and do not wash the skin or apply other skincare products until at least one hour after application. Wash your hands after applying Estogel gel. Avoid using any skin products, particularly strong cosmetics, and soaps on the area of skin you have applied Estogel gel.

Unless you have had your uterus removed, you will probably be taking a form of progesterone as well as Estogel

Missed dose of Estogel?

If you miss a dose of Estogel apply it as soon as you remember, unless it is time to apply the next dose, then skip the missed dose. Do not apply a double dose.

How should Estogel be stored?

You should store your Estogel gel 0.06% below 25°C in a cool dry place, well out of reach of children.