Ethinyl estradiol Pharmacology

Ethinyl estradiol

About Ethinyl estradiol
Synthetic Estrogen(a derivative of estradiol), In Combined oral contraceptive,Anti neoplastic.
Mechanism of Action of Ethinyl estradiol
The drug exerts it`s pharmacological action by binding to specific nuclear estrogen receptors present in target cells and regulating protein synthesis and thus producing desired therapeutic effects. Estrogen receptors are found in female sex organs, breast, pituitary, liver, bone, blood vessels, heart, CNS, hormone sensitive breast carcinoma cells, hormone responsive prostate carcinoma cells. Agonist binding to ligand binding domain of these receptors results in receptor dimerization and interaction with "estrogen response elements" of target genes and thus promotes gene transcription; through certain coactivator proteins which ultimately leads to modification of protein synthesis.
It causes growth and development of female sex organs, maintains proper female sexual functioning. It exerts week anabolic action, and also maintains bone mass primarily by preventing bone resorption. It inhibits osteoclast pit formation and increases the expression of bone matrix proteins and also improves lipid profile (rises HDL and lowers LDL levels). It inhibits growth of hormone responsive carcinoma cells in prostate cancer and certain breast cancer.
Pharmacokinets of Ethinyl estradiol
Absorption: Well absorbed orally, but substantially inactivated by liver.
Distribution: Extensively distributed in the body with highest levels in the fatty tissue. About 50% to 80% is plasma protein bound.
Metabolism: Metabolized primarily in liver by glucuronide and sulfate conjugation.
Excretion: Excreted through urine as sulfate or glucuronide conjugates.
Onset of Action for Ethinyl estradiol
Duration of Action for Ethinyl estradiol
Half Life of Ethinyl estradiol
Side Effects of Ethinyl estradiol
1. Urticaria
2. Pruritus
3. Irritations of skin
4. Feminization in males
5. Gynaecomastia(male)
6. Breakthrough bleeding
7. Breast tenderness
8. Breast enlargement
9. Gastrointestinal disturbances
10. Nausea
11. Vomiting
12. Pancreatitis
13. Headache
14. Dizziness
15. Seizures
16. Thrombophlebitis
17. Thromboembolism
18. Hypertension
19. Oedema
20. Increased risk of endometrial cancer
21. Increased risk of breast cancer
22. Increased risk of Cerebrovascular accident
23. Pulmonary embolism
24. Myocardial infarction
25. Cholestatic jaundice
26. Hepatic adenoma
Contra-indications of Ethinyl estradiol
1. Thrombophlebitis
2. Thromboembolic disorders
3. Estrogen dependent neoplasia
4. Undiagnosed genital bleeding
5. Estrogen dependent breast carcinoma
6. Hepatic impairment
7. Endometrial hyperplasia
8. Severe hypertension
9. Cholestatic jaundice
10. Dubin Johnson syndrome
11. Rotor syndrome
12. Haemoglobinopathies
13. Porphyria.
Special Precautions while taking Ethinyl estradiol
1. Cerebrovascular diseases
2. Coronary artery diseases
3. Migraine
4. Epilepsy
5. Heart failure
6. Hypertension
7. Diabetes mellitus
8. Renal impairment
9. Fibrocystic disease of breast
10. Abnormal mammographic findings
11. Asthma
Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
Indications for Ethinyl estradiol
1. Female hypogonadism
2. Vasomotor menopausal symptoms
3. Menstrual disturbances
4. Certain cases of amenorrhoea
5. Male hyper sexuality
6. Mammary hypoplasia
7. Palliative treatment of certain breast cancer
8. Palliative treatment of prostatic cancer.
Interactions for Ethinyl estradiol
ACE Inhibitors: Antagonises hypotensive effect.
Anti-coagulants: Efficacy of anticoagulants reduced.
Antidiabetics: Antagonism of hypoglycaemic effect.
TCAs: Pharmacological effects of TCAs altered, increased incidence of toxicity.
Antifungals: Griseofulvin accelerates metabolism of ethinyl oestradiol, reduced contraceptive effect.
Barbiturates, Rifampicin: Efficacy of ethinyloestradiol reduced; failure of contraception.
Beta blockers: Hypotensive action antagonised.
Corticosteroids: Clearance reduced and elimination half-life of corticosteroids increased.
Cyclosporine: Increased plasma cyclosporine concentration.
Dantrolene: Hepatotoxicity, especially in women > 35 yrs of age.
Lab. Tests: With high doses of ethinyloestradiol: Increased Sulfobromophthalein retention. Increased Prothrombin and factors VII, VIII, IX & X; decreased antithrombin III; increased norepinephirine :induced platelet aggregability. Increased thyroid binding globulin (TBG) leading to increased circulating total thyroid hormone, as measured by PBI, T4 by column or T4 by radioimmuno assay. Free T3 resin uptake decreased, reflecting elevated TBG; Free T4 concentration unaltered. Impaired glucose tolerance, decreased pregnanediol excretion, reduced serum folate concentration, increased serum triglyceride and phospholipid concentration.
Typical Dosage for Ethinyl estradiol
Oral : 0.02 to 0.2mg/day
Female hypogonadism: 0.05mg 1 to 3 times daily for two weeks monthly followed by two week progesterone therapy. Continue for 3 to 6month dosing cycles followed by two months off.
Maintenance dosage: 0.025mg/day
Vasomotor menopausal symptoms: 0.025 to 0.05mg/day cyclically as 3 weeks on and 1 week off.
Mammary hypoplasia: 0.05mg/day for 12 days along with progesterone from 16th to 25th day.
Male hyper sexuality: 0.05mg/day
Palliative treatment of breast cancer: 1mg thrice daily for 3 months
Palliative treatment of prostatic cancer: 0.15mg to 2mg/day.
Schedule of Ethinyl estradiol
Storage Requirements for Ethinyl estradiol
Store at controlled room temperature at a range of 20 to 25 degree C.
Effects of Missed Dosage of Ethinyl estradiol
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Ethinyl estradiol
Provide symptomatic treatment and supportive care.

Home Delivery for Ethinyl estradiol in Your City

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However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for ethinyl estradiol and other medicines and health products. Home delivery services for ethinyl estradiol may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take ethinyl estradiol only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for ethinyl estradiol before they complete the sale. You can get this information while placing the order for ethinyl estradiol with the pharmacy.

Ethinyl estradiol is a generic medicine name and there are several brands available for it. Some of the brands for ethinyl estradiol might be better known than ethinyl estradiol itself. If the pharmacy that's willing to deliver medicines to your home doesn't have ethinyl estradiol in stock, you can ask for one of the branded alternatives for ethinyl estradiol.