Ethinyloestradiol
Ethinyloestradiol is estrogen (hormone). Ethinyloestradiol is used for replacement therapy in women who is deficient of hormone. Ethinyloestradiol is used to treat symptoms associated with menopause and conditions in which hormone levels are low. Ethinyloestradiol is also used to prevent osteoporosis (bone loss).
Primary Characteristics
It is of Synthetic origin and belongs to Oestrogen.
It belongs to Oestrogen Agonist pharmacological group on the basis of mechanism of action and also classified in Estrogen Derivatives, Acne Therapy pharmacological group. It is also classified under Sex Hormones .
Molecular Weight: 296.4 · pKa: 10.34 · Solubility in Water: insoluble · Solubility in Alcohol: 1 in 6 · Non-proprietary name: Ethinyloestradiol.
Pharmacokinetics
Absorption: Ethinyloestradiol has an oral bioavailability is 100%, pre-systemic (first-pass) metabolism accounts for 50%.
Distribution: Ethinyloestradiol has a volume of distribution is 3 l/kg. plasma protein binding is > 95%.
Elimination: it is metabolised via extensive via liver, plasma half-life is 8-24 hr, renal excretion is 60%.
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Indications
Ethinyloestradiol is primarily indicated in conditions like Breast cancer, Breast cancer (unlicensed indication), Dysfunctional uterine bleeding, Gonadal dysgenesis, Heriditary haemorrhagic telangiectasia, Hormone replacement for menopausal symptoms, Hormone replacement therapy, Menopausal symptoms, Oestrogen deficiency, Osteoporosis prophylaxis, Pre-ovulatory mucus, Prostatic cancer.
Ethinyloestradiol is also indicated for secondary conditions like Acne, Contraception, Endometriosis, Hirsutism, Menstruation disorders.
Contraindications
Ethinyloestradiol is contraindicated in conditions like Thromboembolism, Genital bleeding, Jaundice, Thrombophlebitis, Cerebrovascular disease, Hepatic carcinoma, Coronary artery disease, Estrogen-dependent cancer, Untreated endometriosis.
Dosage
Ethinyloestradiol's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 20 – 40 µg | — | Every 24h | PO | |
| 30 µg | 30 µg | Every 24h | PO | Menopausal HRT & fepale hypogonadism on cydical basis |
| 76.5 µg | 76.5 µg | Every 24h | PO | Palliative treatment ofpeostrate cancer |
| Paediatric Dosage (20kg) | ||||
| 0 – 0 | — | — | Not recommended in this age group | |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not recommended in this age group | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Ethinyloestradiol in overdosage may give rise to further complications which include Impotence , Loss of libido , Gynacomastia , Chloasma , MI.
Ethinyloestradiol produces potentially life-threatening effects which include Pulmonary embolism, Hypertension, Venous thromboembolism, Endometrial carcinoma, Endometrial hyperplasia, Cerebral thrombosis, Gall bladder disease, Liver tumors, Breast carcinoma, Venous thromboembolism, Coronary thrombosis. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Ethinyloestradiol are Nausea, Vomiting, Coronary thrombosis, Uterine withdrawal bleeding.
Ethinyloestradiol is known to cause more or less tolerable side effects which are usually transient. These include Chloasma , Cholestatic Jaundice , dizziness, Fluid retention, Intermenstrual bleeding or spotting, Nausea, Vaginal candidiasis, Vomiting , Weight gain.
Warnings / Precautions
Interference in Pathology
Ethinyloestradiol may interfere in the diagnosis of Tests for measuring urinary oestradiol, oestrogens and oestrone , Tests for thyroid + glucose tolerance.
Available Brands
Storage Conditions
Drug Classification
- 1.18.4 — Estrogens, their combinations and related preparations