Estradiol (Valerate)
Also known as: Oestradiol valerate
Estradiol (Valerate) is the most potent naturally occuring ovarian and placental estrogen in mammals. Estradiol (Valerate) is has also been produced semi-synthetically. iteffective for replacement therapy in women who is deficient of hormone and used to treat symptoms associated with menopause and conditions in which hormone levels are low and to prevent osteoporosis (bone loss). itadminstered intramuscularly.
Primary Characteristics
Estradiol (Valerate) is also known as Oestradiol valerate.
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 Estrogen Derivatives pharmacological group. It is also classified under Sex Hormones .
Molecular Weight: 356.5 · Solubility in Water: Insoluble · Solubility in Alcohol: 1 in 28 · Non-proprietary name: Estradiol (Valerate).
Pharmacokinetics
Absorption: Estradiol (Valerate) has an oral bioavailability is 4% (±1%).
Distribution: Estradiol (Valerate) has a volume of distribution is 9-15 litre. plasma protein binding is 97-99%.
Elimination: it is metabolised via Through Liver, plasma half-life is 20-70 min.
Advertisement
Indications
Estradiol (Valerate) is primarily indicated in conditions like Estrogen-responsive prostate carcinoma, Menopausal symptoms, Osteoporosis.
Estradiol (Valerate) is also indicated for secondary conditions like Breast cancer.
Contraindications
Estradiol (Valerate) is contraindicated in conditions like Gall stones, Fibroids, Endometriosis, Estrogen-dependent cancer, Undiagnosed vaginal bleeding, Venous thromboembolic disease.
Dosage
Estradiol (Valerate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 25 – 100 mg | — | — | Implants | For about4 to 8 months |
| 1.5 mg | 1.5 mg | Every 24h | PO | 450 mg may be given as Initial dose. |
| 0.02 mg/ kg | 0.02 mg/ kg | — | Topical | As Required |
| 57 µg | 57 µg | Every 24h | Transdeemal Patches | |
| 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
The signs and symptoms that are produced after acute overdosage of Estradiol (Valerate) are Sudden / Unsual vaginal bleeding, Nausea & vomiting.
Estradiol (Valerate) is known to cause more or less tolerable side effects which are usually transient. These include Breast tenderness, Edema, Gynecomastia, Hypercalcemia, Impotence, Nausea, Nipple tenderness, Skin reactions, Vomiting , Weight gain, Withdrwal bleeding.
Warnings / Precautions
Interference in Pathology
Estradiol (Valerate) may interfere in the diagnosis of Impairment of Glucose Tolerance .
Available Brands
Storage Conditions
Drug Classification
- 1.18.3.1 — Hormonal contraceptives
- 2.18.4 — Estrogens, their combinations and related preparations