Oestradiol

Registered South African indications:

• Menopause

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy or women who may become pregnant
• Cardiovascular or cerebrovascular disorders, e.g. thrombophlebitis, thrombo-embolic processes or a history of these conditions
• Hypertension
• Migraine
• Liver disease or a history of this condition if the results of the liver function tests have failed to return to normal
• Cholestatic jaundice
• History of jaundice of pregnancy or jaundice due to oestrogen use
• Rotor syndrome and Dubin-Johnson syndrome
• Known or suspected oestrogen-dependant tumours
• Endometrial hyperplasia
• Undiagnosed vaginal bleeding
• Haemoglobinopathies
• Porphyria
• Hyperlipoproteinaemia as well as other risk factors predisposing to cardiovascular disorders
• A history during pregnancy or previous oestrogen use of severe pruritus or herpes gestationis or a deterioration of otosclerosis

Cautions

• Breastfeeding
• Renal impairment
• Dementia
• Endometrial cancer
• Endometriosis
• Pre-existing hypertriglyceridaemia
• Family history of genital cancers
• Asthma
• Diabetes mellitus
• Cardiovascular disease
• Epilepsy
• Gall bladder disease
• Hepatic hemangioma
• Hereditary angioedema
• Hypoparathyroidism
• Systemic lupus erythematosus
• Hyperthyroidism
• Recent surgery
• Risk of osteoporosis

Forms avail. in SA and covered in this monograph: imp

Hormone replacement therapy in menopause

• Subdermal (imp): 20-40mg, every 4-8 months

Frequency of replacement depends on time at which menopausal symptoms return

In women with an intact uterus, oestrogen therapy should be combined with an adequate dosage of a progestational agent at regular intervals, for example for 10-14 days every 1-3 months, to protect the endometrium from oestrogen-induced hyperplasia

Not indicated for use in children

Pregnancy

• Contraindicated
• This product is only approved for use in postmenopausal women and therefore is not appropriate for use in pregnancy

Breastfeeding

• Caution
• Oestrogen is present in breast milk and have been shown to decrease the quantity and quality of human milk

Renal Impairment

• Caution: no information available

Hepatic Impairment

• Contraindicated

Elderly

• No dose adjustment recommended

Porphyria Information

• Possibly porphyrinogenic (PSP)

Drugs in Sport

• Permitted - No warning

Central Nervous System Disorders

• Headache
• Mood changes
• Migraine

Cardiovascular Disorders

• Thrombosis
• Hypertension
• Fluid and salt retention

Gastrointestinal Disorders

• Nausea and vomiting
• Cholelithiasis
• Cholestatic jaundice

Hepatobiliary Disorders

• Benign hepatic tumours

Genitourinary Disorders

• Intermenstrual bleeding
• Endometrial proliferation
• Excessive production of cervical mucous
• Increase in size of uterine fibromyomata
• Aggravation of endometriosis

Endocrine and Metabolic Disorders

• Breast tenderness
• Breast enlargement
• Galactorrhoea
• Changes in bodyweight
• Impaired glucose tolerance

Skin and Subcutaneous Tissue Disorders

• Chloasma
• Erythema nodosum
• Rash

Sensory Disorders

• Contact lens intolerance

• Anastrozole
• Anticoagulants
• CYP3A4 inducers
• Dehydroepiandrosterone
• Exemestane
• Somatropin
• Tizanidine
• Tipranovir

• Gynaecological examination
• Papanicolaou smear
• Mammogram
• Endometrial sampling 
• Blood pressure

Specific cases may require

• Hepatic function
• Blood glucose
• Lipid profile
• Thyroid function
• Bone density measurement

Synthetic 17β-oestradiol is chemically and biologically identical to endogenous human oestradiol. Oestrogen mediates its effects by binding to the oestrogen receptor, which is located in various tissues such as the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. Endogenous 17β-oestradiol induces and maintains the primary and secondary female sexual characteristics. It substitutes for the loss of oestrogen production in menopausal women and alleviates menopausal symptoms.

Implant 20mg

• Oestradiol (Adcock) originator

Also available in the following forms: Transdermal patch, vaginal tablet, gel and oral tablet