Estradiol Valerate

Indications

Osteoporosis

Estradiol Valerate tablet is used in Hormone Replacement Therapy (HRT) to treat the symptoms of estrogen deficiency in peri- and postmenopausal women. Doctors also prescribe it to prevent osteoporosis in postmenopausal women who are at high risk of fracture in the future.

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Estradiol passes freely into target cells (for example the female organs, breasts, hypothalamus and pituitary) and binds to a receptor inside the cell. Once the estrogen receptor has bound estradiol, it can move into the nucleus of the cell and regulate gene transcription, which leads to the formation of messenger RNA. The mRNA then interacts with ribosomes to make specific proteins, and these proteins produce the effect of estradiol on the cell. Estrogens increase the liver's production of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG) and other serum proteins. They also suppress follicle-stimulating hormone (FSH) from the anterior pituitary. Menopausal symptoms are mainly caused by a loss of estrogenic activity, so increasing the down-stream effects of Estrogen Receptor binding reverses some of them.

Absorption: After oral use, estradiol valerate is absorbed quickly and completely.

Metabolism: Estrogens given from outside the body are metabolized in the same way as the body's own estrogens. They are partly metabolized by cytochrome P450.

Excretion: Estradiol, estrone and estriol leave the body in the urine, together with glucuronide and sulfate conjugates.

Pregnancy & Breastfeeding

Estradiol Valerate is not indicated during pregnancy. If pregnancy occurs while a woman is taking it, the treatment should be stopped immediately. Most epidemiological studies so far, which looked at accidental exposure of the foetus to oestrogens, show no teratogenic or foetotoxic effects. Estradiol Valerate is also not indicated during breast-feeding.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: Estradiol Valerate is an estrogen-only product. The dose is one 1 mg tablet taken daily. The time of day doesn't matter, but once the woman has chosen a time she should keep to it every day. Treatment is continuous, so the next pack follows straight away without a break. To start and to continue treatment of menopausal symptoms, the lowest effective dose should be used for the shortest duration. Treatment should begin with the Estradiol Valerate 1 mg tablet. If it is considered necessary, Estradiol Valerate 2 mg should be used. Once treatment is established, the lowest effective dose needed to relieve the symptoms should be used. In women with an intact uterus, a progestogen should be added to Estradiol Valerate 1 mg for at least 12-14 days each month/28 day cycle. In hysterectomised women, adding a progestogen is not recommended unless there is a previous diagnosis of endometriosis. How to start Estradiol Valerate 1 mg If the woman has an intact uterus and is still menstruating, a combination regimen with Valest and a progestogen, beginning with the oestrogen phase, should start on the first day of bleeding. If her periods are very infrequent, or if amenorrhoea is established, she may start at any time, provided that pregnancy has been excluded where appropriate. Women who are changing from a continuous combined HRT product may start Estradiol Valerate on any day. Women who are changing from cyclic or continuous sequential HRT regimens should complete the cycle first, and then change over without a break in therapy. Missed or lost tablets If the woman forgets a tablet at the usual time, she may take it within the following 12 hours. If she is more than 12 hours late, she should not take the forgotten tablet. She should take the remaining tablets at the usual time on the right days. A missed dose may lead to breakthrough bleeding or spotting. Pediatric population Not recommended for children. Method of administration The tablets can be taken with or without food. Swallow them whole with a glass of water or milk, and take them at the same time each day.