Estradiol valerate
When ATH:
G03CA03
Pharmacological action
Estrogen, tool for substitution therapy. Estradiol valerate provides specific estrogenic activity: cause endometrial proliferation, stimulates development of the uterus and secondary female sexual characteristics with their underdevelopment, alleviates and eliminates general disorders, It occurs in women on the grounds of lack of gonadal function in menopause or after gynecological surgery.
Estradiol valerate maintains a balance between osteoblasts and osteoclasts, reduces bone resorption and promotes its formation.
Pharmacokinetics
After oral administration of estradiol valerate is rapidly and completely absorbed from the gastrointestinal tract. Plasma protein binding is 50%.
Rapidly metabolized in the liver with the formation of estriol and estrone. When administered at a dose of 1-2 mg maximum plasma concentration is reached after 3-6 no. T1/2 – about 1 no.
Treated effect “first pass” through the liver and to some extent – enterohepatic recycling.
Excreted in the urine as sulphate and glucuronide esters along with a small amount of unchanged substance. Identified and other metabolites.
Testimony
Tides, increased perspiration, sleep disorders, depression, nervousness, irritability, headache, dizziness when you stop menstruating during menopause, after surgical removal of the ovaries or radiation; hypersensitivity of the bladder, degenerative changes in the skin and mucosa, osteoporosis in menopause.
Dosage regimen
When administered daily dose of 1-2 mg. Scheme of treatment depends on the indication.
Side effect
Maybe: stress and breast tenderness, changes in libido, increased production of mucus in the vagina, digestive disorders, flatulence, nausea, vomiting, stomach ache, bile stasis, palpitation, arterial hypertension, headache, dizziness, depressed mood, nose bleed, thrombophlebitis, swelling, decrease glucose tolerance, hives, generalized itching, alopecia.
Contraindications
Serious liver and kidney, liver tumor, violation of thrombosis (incl. history), severe diabetes with vascular changes, drepanocytemia, uterine tumors and mammary hormonal nature and are suspected, endometriosis, inborn errors of metabolism of lipids, hearing loss in otosclerosis, pregnancy, lactation (breast-feeding). The application is also contraindicated, if during a previous pregnancy occurred hepatitis, jaundice or prolonged itching.
Pregnancy and lactation
Contraindicated during pregnancy and lactation (breast-feeding).
Cautions
Estradiol valerate should be abolished, if during the period of treatment there stabbing pain when breathing, cough of unknown etiology, pain and sense of compression in the chest, severe headaches, disorders of the senses, coming elective surgery, prolonged bed rest.
Careful systematic monitoring is required with concomitant diabetes mellitus, hypertension, varicose veins, rasseânnom sclerosis, epilepsy, chorea, porfirii, tetany, previously adjourned phlebitis. The need for regular gynecological examinations.
It can be used in combination with progestins (incl. with dienogest).
Drug Interactions
Regular use of certain drugs (barbiturates, phenylbutazone, gidantoin, rifampicin, ampicillin and others.) may reduce the efficiency. You can change the need for oral hypoglycemic drugs.
