AR Estradiol Valerate 40mg/ml

AR Estradiol Valerate general information

What is AR Estradiol Valerate used for?

Menopause is a natural part of a woman’s life and represents the end of her childbearing years and the beginning of her next phase of 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 can cause severe problems for some women.  Hormone replacement therapy (HRT) can help relieve symptoms of menopause.  AR Estradiol Valerate 40mg/mL is an injectable form of HRT. It is recommended for HRT in combination with progesterone, because of the health risk of estrogen-only HRT.  You should only use AR Estradiol Valerate alone if you have had a hysterectomy; or are also taking progesterone. 

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 metabolism and supporting bone density throughout the fertile years of a woman’s life.  As menopause approaches, estrogen production starts to slow down.  Eventually, no more is produced by the ovaries, so that menstruation ceases.   

Symptoms of menopause

Symptoms associated with low estrogen in menopause include hot flashes caused by sudden dilating 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 another problem related to the loss of estrogen.  It can lead to osteoporosis, which makes the bones brittle so that they fracture more easily.  AR Estradiol Valerate relieves symptoms of menopause.  It also helps prevent postmenopausal bone loss (osteoporosis), reducing the risk of fracture. 

Transgender hormone therapy

Estrogen is an essential component in transgender hormone therapy for male to female gender reassignment.  AR Estradiol Valerate helps stimulate the development of female sexual characteristics.  This promotes the feminisation process, such as breast development, and inducing metabolic changes such as fat distribution to redefine the general body shape.

How does AR Estradiol Valerate work?

AR Estradiol Valerate contains estradiol valerate 40mg/mL.  It is used for hormone replacement therapy to substitute for lack of estrogen in postmenopausal women and relieve symptoms of menopause. 

Estradiol valerate is a synthetic form of naturally occurring estradiol, the primary and most active form of the female sex hormone estrogen.  Estradiol is biologically similar to the natural hormone.  Other types of estrogen that exist post-menopause include estrone.  This form of estrogen is produced by conversion from androgens (predominantly a male hormone but found in small amounts in women) in other tissues like fat cells.  Estone does not have much activity, which is why a lack of estradiol is responsible for most menopausal symptoms.

Estradiol in AR Estradiol Valerate works by passing through the cell membrane and binding to specific receptors inside the cells of its target tissues, including the ovaries, uterus, bone, and breast tissue.  Estrogen attaches to its receptor then interacts directly with the DNA to promote the expression (activation) of specific genes that make proteins needed for estrogen-dependent processes in those tissues.  These include breast cell growth, improved lubrication of vaginal cells, and increased bone density. 

AR Estradiol Valerate is formulated for intramuscular injection in an oily solution that slows down absorption.  A single injection of AR Estradiol Valerate is absorbed slowly over several weeks and works for longer, with a prolonged action time

What does AR Estradiol Valerate contain?

AR Estradiol Valerate contains the active ingredient estradiol valerate 40mg/mL that is used for hormone replacement therapy to substitute for lack of estrogen in postmenopausal women.  It also contains 224mg/mL benzyl benzoate, 40mg/mL benzyl alcohol, castor oil.

What are the side effects of AR Estradiol Valerate?

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

Common side effects when taking AR Estradiol Valerate include breast tenderness, breast pain, abdominal pain, nausea, oedema, and headache, breakthrough bleeding, and spotting.

When should AR Estradiol Valerate not be used?

Have a talk with your primary healthcare physician before taking AR Estradiol Valerate 40mg/mLso 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 AR Estradiol Valerate  you should consider the following before taking AR Estradiol Valerate :

• Have you ever had an unusual reaction or an allergy when taking AR Estradiol Valerate?
• Are you pregnant or breastfeeding?
• Do you have any problems with your liver or had a 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 AR Estradiol Valerate?

Some medicines interact with AR Estradiol Valerate 40mg/mL and may affect the way it works, or are affected by AR Estradiol Valerate or increase side effects; you should discuss possible interactions with your primary care physician.  These may include anticonvulsants like phenytoin and carbamazepine, barbiturates, anti-infectives like rifampicin, rifabutin, nevirapine, antibiotics like penicillin.

If other medications may interact with AR Estradiol Valerate, your doctor will discuss these with you. 

How should AR Estradiol Valerate be taken and for how long?

You should take your AR Estradiol Valerate using a clean, dry needle and syringe.  Draw up 1mL Estradiol Valerate and inject deep into the upper, outer area of the gluteal muscle.  The usual dose is one injection every four weeks, depending on your doctor’s recommendation.  You should continue to take Estradiol Valerate Injection injections as long as recommended by your doctor, which may be for several months

Missed dose of AR Estradiol Valerate

If you miss a dose of AR Estradiol Valerate 40mg/mL, take it as soon as you remember, unless it is time to take the next dose, then skip the missed dose.  Do not take a double dose.

How should AR Estradiol Valerate be stored?

You should store your AR Estradiol Valerate 40mg/mL below 25°C in a cool dry place and protect from light.