Oestradiol Pharmacology

Oestradiol

About Oestradiol
Estrogenic hormone, Estrogen Derivative.
Mechanism of Action of Oestradiol
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 excerts week anabolic action, and also maintain 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 Oestradiol
Absorption: Well absorbed orally; but substantial inactivation by liver limits it`s oral administration and administered parenterally. Well absorbed after topical administration. 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 Oestradiol
N/A
Duration of Action for Oestradiol
N/A
Half Life of Oestradiol
N/A
Side Effects of Oestradiol
1.Urticaria
2.Pruritus
3.Irritations of skin
4.Exanthema
5.Breakthrough bleeding
6.Breast tenderness
7.Breast enlargement
8.Gastrointestinal disturbances
9.Nausea
10.Vomiting
11.Pancreatitis
12.Headache
13.Dizziness
14.Seizures
15.Thrombophlebitis
16.Thromboembolism
17.Hypertension
18.Increased risk of endometrial cancer
19.Increased risk of breast cancer
20.Increased risk of Cerebrovascular accident
21.Cholestatic jaundice
22.Hepatic adenoma
Contra-indications of Oestradiol
1.Thrombophlebitis
2.Thromboembolic disorders
3.Estrogen dependent neoplasia
4.Undiagnosed genital bleeding
5.Hypertension
6.Estrogen dependent breast carcinoma
7.Hepatic impairment
8.Jaundice
9.Thrombosis
10.Porphyria
11.Sickle cell anaemia
12. Hyperlipoprotinaemia
13.Dubin Johnson syndrome
14.Rotor syndrome
15.Endometriosis
16.Endometrial hyperplasia
Special Precautions while taking Oestradiol
1.Migraine
2.Epilepsy
3.Heart failure
4.Hypertension
5.Diabetes mellitus
6.Renal impairment
7.Fibrocystic disease of breast
8.Abnormal mammographic findings
9.Cerebrovascular diseases
10.Coronary artery diseases
11.Asthma
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Oestradiol
1.Menopausal symptoms due to estrogen deficiency
2.Primary ovarian failure
3.Atrophic vaginitis
4.Inoperable breast cancer
5.Female hypogonadism
6.Hyper androgenism in females

Interactions for Oestradiol
1.CYP1A2 and CYP3A4 inducers e.g. aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol.
2.May enhance the effects of hydrocortisone and prednisolone when used together.
Typical Dosage for Oestradiol
Oral: 1 to 2mg/day in cycles of 21days on and 7days off or 23 days on and 5 days off.
Inoperable breast cancer: 10mg 8th hourly for 3 months.
Topical: 1.5mg once daily. Increases the dosage up to 3mg; if required after one month.
(3mg Oestradiol in 5g gel)
Maintenance dosage: 1g gel once to thrice weekly
Transdermal: Place one transdermal patch twice weekly on trunk of the body; preferably the abdomen in cycles of 3 weeks on and 1week off.
Schedule of Oestradiol
H
Storage Requirements for Oestradiol
Store at room temperature at a range of 15 to 30 degree C.
Intramuscular: Store at room temperature.
Oral: Store at room temperature.
Transdermal: Store at room temperature.
Vaginal: Store at room temperature.
Effects of Missed Dosage of Oestradiol
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 Oestradiol
Provide symptomatic treatment and supportive care.

Home Delivery for Oestradiol in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including oestradiol.

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 oestradiol and other medicines and health products. Home delivery services for oestradiol 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 oestradiol 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 oestradiol before they complete the sale. You can get this information while placing the order for oestradiol with the pharmacy.

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