Oestradiol

Registered South African indications:

• Menopause

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Severe renal impairment
• Severe hepatic impairment
• Severe cardiac disease
• Known or suspected cancer of the breast, genital tract or other oestrogen-dependent neoplasia
• History of thrombosis or thromboembolic disorders
• Undiagnosed vaginal bleeding
• Endometrial hyperplasia
• Porphyria

Cautions

• Breastfeeding
• Mild to moderate renal impairment
• Mild to moderate hepatic impairment
• Elderly
• Uterine fibroids
• Risk factors for thromboembolic disorders
• Risk factors for oestrogen-dependent tumours
• Hypertension
• Diabetes mellitus
• Cholelithiasis
• Migraine
• Systemic lupus erythematosus
• History of endometrial hyperplasia
• Epilepsy
• Asthma
• Otosclerosis
• Hereditary angioedema
• Hypertriglyceridaemia
• History of chloasma gravidarum

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

Oestrogen replacement therapy for the relief of symptoms due to natural or surgically induced menopause
- Vasomotor symptoms
- Atrophic vaginitis
- Atrophic urethritis

• Topical (gel): Apply 1.5mg (2.5g gel) to skin of lower trunk or thigh, dly

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2.5g is equivalent to 2 plunges of the pump or one length of the plastic groove rule

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Area of application should be approximately 750cm² or 6 times the size of one hand

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Should not be applied near the breasts or on the vulva

Not indicated for use in children

Pregnancy

• Contraindicated

Breastfeeding

• Caution; no information available

Renal Impairment

• Mild to moderate: Caution; no information available
• Severe: Contraindicated

Hepatic Impairment

• Mild to moderate: Caution; no information available
• Severe: Contraindicated

Elderly

• Caution; no information available 

Porphyria

• Contraindicated

Central Nervous System Disorders

• Headache
• Dizziness
• Migraine
• Paraesthesia
• Tremor
• Depression
• Nervousness
• Lethargy
• Anxiety
• Insomnia
• Apathy
• Emotional lability
• Impaired concentration
• Changes in libido
• Changes in mood
• Euphoria
• Agitation
• Fatigue
• Cerebral ischaemic events

Cardiovascular Disorders

• Palpitations
• Hot flushes
• Hypertension
• Superficial phlebitis
• Purpura
• Venous thromboembolism

Respiratory Disorders

• Dyspnoea
• Rhinitis
• Pulmonary embolism

Gastrointestinal Disorders

• Nausea and vomiting
• Stomach cramps
• Flatulence
• Abdominal pain
• Constipation
• Dyspepsia
• Diarrhoea
• Rectal disorder
• Bloating

Hepatobiliary Disorders

• Alterations in hepatic function and biliary flow
• Cholestatic jaundice

Genitourinary Disorders

• Benign endometrial neoplasm
• Uterine fibroids
• Increased urinary frequency
• Urinary urgency
• Urinary incontinence
• Cystitis
• Discoloured urine
• Haematuria
• Unscheduled vaginal bleeding or spotting
• Vaginal discharge
• Disorders of vulva or vagina
• Menstrual disorder
• Endometrial hyperplasia
• Uterine disorder
• Breast cancer
• Breast pain/tension
• Breast enlargement
• Breast tenderness
• Dysmenorrhea
• Pre-menstrual like syndrome

Endocrine and Metabolic Disorders

• Benign breast neoplasm
• Increased weight
• Decreased weight
• Increased appetite
• Hypercholesterolemia
• Endometrial cancer
• Ovarian cancer

Musculoskeletal Disorders

• Joint disorders
• Muscle cramps

Skin and Subcutaneous Tissue Disorders

• Rash
• Pruritus
• Acne
• Alopecia
• Dry skin
• Nail disorder
• Skin nodule
• Hirsutism
• Erythema nodosum
• Urticaria
• Contact dermatitis
• Eczema
• Skin irritation
• Application site pain
• Increased sweating
• Oedema

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reaction
• Exacerbation of hereditary angioedema
• Fever
• Asthenia
• Flu syndrome
• Malaise

Sensory Disorders

• Impaired vision
• Dry eye  
• Intolerance of contact lenses

• CYP450 inducers
• Anticonvulsants
• Phenobarbital
• Phenytoin
• Carbamazepine
• Anti-infectives
• Rifampicin
• Rifabutin
• Nevirapine
• Efavirenz
• Ritonavir
• Nelfinavir

Others

• St John's wort

• Pelvic examination
• Breast examination
• Mammogram
• Papanicolaou smear
• Blood pressure

Specific cases may require

• Blood glucose
• Hepatic function
• Lipid profile
• Thyroid function
• Endometrial sampling
• Bone density scan
• Ophthalmic examination

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.

Gel (per 2.5g) 1.5mg

• Femigel (Medi-Challenge) originator

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