DrugInfoSys

Mestranol

Drug #456

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.

Molecular structure of 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%.

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Indications

Mestranol is primarily indicated in conditions like Contraception, Menopausal symptoms, Menstruation disorders.

Contraindications

Dosage

Mestranol's dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
50 ug50 ugEvery 24hPO
Paediatric Dosage (20kg)
0 – 0Not recommended for this age group
Neonatal Dosage (3kg)
0 – 0Not recommended for this age group

Drug Interactions

Unknown3 interactions
6 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

Mestranol should be used with caution in patients with medical history, including family medical history, especially if have asthma, high blood pressure, kidney, liver or heart disease or a history of jaundice (yellowing of skin or eyes) or high blood pressure during pregnancy, excessive weight gain or fluid retention during menstrual cycle, strokes, blood clots, heart attacks, seizures, migraine headaches, breast cancer, high blood level of cholesterol or lipids (fats) or depression. Higher strengths are more likely to cause melasma (darkening of skin), sunlight may intensify this darkening and may need to avoid prolonged sun exposure and sunlamps, consult the doctor regarding use of sunscreens and protective clothing. Oral contraceptives should be stopped at least three months before becoming pregnant. Use another method of birth control during those three months. Consult with doctor before lactation. Avoid smoking. Birth-control pills slightly increase risk of strokes, blood clots, high blood pressure, heart attacks, gallbladder disease, vision problems and liver tumors. Cigarette smoking (especially 15 or more cigarettes daily) and age (women older than 35 or 40 years of age) further increase the risk of stroke, blood clots, high blood pressure and heart attacks. Avoid using contact lenses because it may develop vision problems, consult with eye doctor if these problems occur. Before having surgery, including dental surgery, tell the doctor about the use of the drug.

Interference in Pathology

Mestranol may interfere in the diagnosis of Histopathological Tests of Endometrial Biopsies & Uterine Curettings .

Available Brands

None recorded.

Storage Conditions

Mestranol should be stored Tab.

Drug Classification

  1. 1.18.3.1Hormonal contraceptives