Estradiol valerate oral
- Drugs List
- Therapeutic Indications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
Tablets containing estradiol valerate.
Secondary prophylaxis of postmenopausal osteoporosis where risk of fracture
Hormone replacement therapy (HRT) to treat oestrogen deficiency symptoms in peri and postmenopausal women.
To prevent osteoporosis in postmenopausal women at high risk of fractures, who cannot take other drugs indicated for the prevention of osteoporosis. (2mg only)
A progestogen should be added for 12 to 14 days each cycle for women with an intact uterus, to oppose the production of an oestrogen-stimulated hyperplasia of the endometrium. It's not recommended to add a progestogen in hysterectomised women, unless there is a previous diagnosis of endometriosis.
Treatment can be started on any convenient day for women who are: hysterectomised; or with established amenorrhoea; or who are experiencing long intervals between spontaneous menses; or those changing from a continuous combined HRT programme.
Women changing from a cyclical or continuous HRT preparation should start treatment the day after completing the previous regimen.
Women who have regular menstrual periods should start treatment on the first day of bleeding.
Treatment of menopausal symptoms:
Initially 1mg daily without interruption. If clinical response is inadequate, increase to 2mg daily but reduce to lowest effective dose for maintenance therapy.
Prevention of osteoporosis:
2mg daily without interruption. Begin treatment as soon as possible after the onset of menopause.
Additional Dosage Information
Tablets should be taken continuously without a break between packs.
If a tablet is forgotten, it should be taken as soon as the patient remembers, therapy should then continue as before. If more than one tablet has been missed, only the most recent tablet should be taken, the patient should not take multiple doses.
If the next tablet is taken more than 12 hours late, the missed tablets should be left in the pack and the next tablet taken at the right time.
Missed tablets may cause breakthrough bleeding and spotting.
Suspected hormone dependent neoplasm
Abnormal liver function test
Acute hepatic disorder
Deep vein thrombosis
Familial conjugated hyperbilirubinaemias
Hereditary fructose intolerance
History of breast cancer
History of hormone dependent neoplasm
History of thromboembolic disorder
History of venous thromboembolism
Hormone dependent neoplasm
Recent arterial thromboembolic disorder
Uncontrolled endometrial hyperplasia
Undiagnosed gynaecological haemorrhage
Precautions and Warnings
Family history of breast cancer
History of recurrent spontaneous abortion
Patients over 65 years
Predisposition to thromboembolic disease
Fibrocystic breast disorder
Gall bladder disorder
Glucose-galactose malabsorption syndrome
History of chloasma
History of endometrial hyperplasia
History of endometriosis
Sickle cell disease
Risk of pancreatitis in individuals with hypertriglyceridaemia
Add progestogen for 12-14 days each cycle for those with an intact uterus
Assess family medical history prior to commencing treatment
Exclude breast cancer before treatment
Exclude oestrogen dependent neoplasm before treatment
Not all available strengths are licensed for all indications
Preparation contains sucrose
Do breast & pelvic exam. before & during treatment if clinically indicated
Exclude pregnancy prior to initiation of treatment
Abnormal and/or irregular bleeding should be investigated
Advise patients of risks/benefits & review need for treatment regularly
Discontinue treatment if patient develops seizures
Monitor hepatic function in patients with history of hepatic disease
Advise patient of thromboembolic symptoms and to report them if they occur
Advise patient that changes in their breasts should be reported to Dr/nurse
Advise patient to contact a doctor if symptoms of thromboembolism develop
Avoid immobilisation-treatment may cause increased risk of thromboembolism
Discontinue at the onset of severe depression
Increased risk of venous thromboembolism
Increased risk of VTE during travel involving >5hr immobilisation
May increase baseline risk of ovarian carcinoma
Uterine fibroids may increase in size
May interfere with certain laboratory measurements
Discontinue 4 - 6 weeks before major surgery
Advise patient to seek advice at first indications of pregnancy
Discontinue at first signs of thrombophlebitis or thromboembolism
Discontinue if abnormal neurological signs develop
Discontinue if cholestasis develops
Discontinue if first occurrence or worsening of migraine/severe headache
Discontinue if jaundice or other evidence of hepatic impairment occurs
Discontinue if significant rise in blood pressure occurs
Discontinue if sudden pain in the chest occurs
Discontinue if sudden, severe pain in stomach occurs
Discontinue if symptoms due to endometriosis are exacerbated
Maintain treatment at the lowest effective dose
Maintain treatment for the shortest possible duration
Advise patient not to take St John's wort concurrently
Advise patient to avoid grapefruit products
Female: Not for contraception.Use non-hormonal contraception, if required
Advise patient of increased risk of breast cancer vs benefits of HRT
HRT should only be considered for patients whose symptoms adversely affect quality of life. An annual careful appraisal of the risks and benefits should be undertaken. When carrying out initial medical examinations of patients, ensure that investigations (including appropriate imaging tools, e.g. mammography) are carried out in accordance with currently accepted screening practices.
For the treatment of menopausal symptoms the benefits of short-term HRT are considered to outweigh the risks in the majority of women.
In all cases, it is good practice to use the lowest effective dose for the shortest possible time and to review the need to continue treatment at least annually.
For postmenopausal women over 50 years who are at an increased risk of bone fracture, HRT should be used to prevent osteoporosis only in those who are intolerant of, or contraindicated for, other osteoporosis therapies.
Physical examination should be guided by this and a knowledge of the contraindications and precautions and warnings for use of the product. Investigations including mammography should be carried out in accordance with currently accepted screening practices, modified according to the clinical needs of the individual.
There is an increased risk of breast cancer in women currently or recently using HRT. The risk of breast cancer increases with the duration of treatment and, after stopping HRT, the risk will decrease with time. When HRT lasts for more than 5 years, the risk may persist for 10 years or more.
Examinations to rule out endometrial abnormalities should be undertaken at regular intervals. Prolonged monotherapy with oestrogens increases the risk of endometrial hyperplasia and carcinoma in postmenopausal women unless supplemented by administration of a progestogen to protect the endometrium. Unless there is a previous diagnosis of endometriosis it is not recommended to add a progestogen in hysterectomised women.
Pregnancy and Lactation
Hormone replacement therapy is contraindicated during pregnancy.
Should pregnancy occur, treatment should be discontinued immediately.
Estradiol has been associated with cardiovascular defects, eye and ear abnormalities and hypospadias in the newborn when having been exposed to these in the womb (Briggs, 2015). However, some studies have failed to find a relationship with cardiovascular defects and non-genital malformations. Down's syndrome has also been associated with oestrogens as a group, but not for estradiol (Schaefer, 2015).
Development alterations in the psychosexual performance of boys have been attributed to exposure to estradiol and progestogen in the womb. Males who have been exposed to estradiol and progestogen have demonstrated a trend to have less heterosexual characteristics and fewer masculine interests than males which have not been exposed to these hormones prenatally.
Hormone replacement therapy is contraindicated during breastfeeding.
Oestrogenic agents demonstrate lower infant weight gain, decreased milk production and decreased composition of nitrogen and protein content of human milk (Briggs, 2015). Even though the extent of these changes is low, the changes in milk production and composition may be of nutritional importance in malnourished mothers. Because of the reasons mentioned above the use of this medication during lactation should be avoided.
Aggravation of porphyria
Allergic skin reactions
Change in amount of cervical secretion
Change in carbohydrate metabolism
Changes in libido
Coronary artery disorder
Deep vein thrombosis (DVT)
Disturbances of appetite
Exacerbation of epilepsy
Increase in plasma triglyceride concentration
Increased risk of breast cancer
Increased risk of endometrial cancer
Increased risk of ovarian cancer
Increased size of uterine fibroids
Intolerance to contact lenses
Peripheral vascular disorders
Steepening of corneal curvature
Effects on Laboratory Tests
Hormone replacement therapy, especially oestrogen-progestogen combined treatment may increase the density of mammographic images and adversely affect the detection of breast cancer.
The use of oestrogen may influence laboratory test results of certain endocrine tests and liver enzymes.
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Last Full Review Date: August 2022.
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 3rd edition (2015) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 10th edition (2015) ed. Briggs, G., Freeman, R. Wolters Kluwer Health, Philadelphia.
Summary of product characteristics: Progynova tablets 1mg. Bayer plc. Revised June 2022
Summary of product characteristics: Progynova tablets 2mg. Bayer plc. Revised June 2022
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 18 August 2022
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Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
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