Mestranol
Mestranol is a potent synthetic estrogen, with actions, uses and adverse effects similar to estrodiol, usually present in combined oral contraceptive steroid preparations. Chemically Mestranol is (17a)-3-methoxy-19-norpregna-1, 3, 5 (10)-trien-20-yn-17-ol.it achieves its estrogenic activity through conversion of ethinyl estradiol by the process of demethylation. it is given by mouth to supress ovulation, in combination with progesterone to reinforcethe contraceptive action and alos for other menstruation disorders.
Primary Characteristics
It is of Synthetic origin and belongs to Steroid.
It belongs to Oestrogen Agonist pharmacological group on the basis of mechanism of action and also classified in Contraceptive Oral pharmacological group. It is also classified under Sex Hormones .
Molecular Weight: 310.4 · Solubility in Water: Insoluble · Solubility in Alcohol: Sparingly soluble · Non-proprietary name: Mestranol.

Pharmacokinetics
Absorption: Mestranol has an oral bioavailability is 94% (±4%), pre-systemic (first-pass) metabolism accounts for 27.5% (±27.5%).
Distribution: Mestranol has a volume of distribution is 3.8±0.8 l/kg. plasma protein binding is 98%.
Elimination: it is metabolised via 70% hepatic, plasma half-life is 8-24hr, renal excretion is 9-36%.
Advertisement
Indications
Mestranol is primarily indicated in conditions like Contraception, Menopausal symptoms, Menstruation disorders.
Contraindications
Mestranol is contraindicated in conditions like Asthma, Depression, Diabetes mellitus, Epilepsy, Gall stones, Hypertension, Migraine, Sickle cell anaemia, Hyperlipidemia, Thromboembolism, Genital bleeding, Thrombophlebitis, Cerebrovascular disease, Chloasma, Cholestatic jaundice, Herpes gestations, Endometriosis, Porphyria, Raynaud's disease, Coronary artery disease, Hepatic tumor, Estrogen-dependent malignant disease.
Dosage
Mestranol's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 50 ug | 50 ug | Every 24h | PO | |
| Paediatric Dosage (20kg) | ||||
| 0 – 0 | — | — | Not recommended for this age group | |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not recommended for 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
Mestranol in overdosage may give rise to further complications which include Chloasma , Sickle crises in sicklers , Porphyria.
Mestranol produces potentially life-threatening effects which include Pulmonary embolism, Hypertension, Endometrial carcinoma, Endometrial hyperplasia, Cerebral thrombosis, Gall bladder disease, Liver tumors, Breast carcinoma, Cervix carcinoma, Coronary thrombosis, Venous thrombosis. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Mestranol are Nausea, Vomiting, Uterine withdrawal bleeding.
Mestranol is known to cause more or less tolerable side effects which are usually transient. These include Breast discomfort, Cervical ectropion, Changes in corneal curvature, dizziness, Fluid retention, Menstrual irregularity, Nausea, Vaginal candidiasis, Vomiting , Weight gain.
Warnings / Precautions
Interference in Pathology
Mestranol may interfere in the diagnosis of Histopathological Tests of Endometrial Biopsies & Uterine Curettings .
Available Brands
None recorded.
Storage Conditions
Drug Classification
- 1.18.3.1 — Hormonal contraceptives