Estradiol 0.06% vag prep

Indications

Estradiol 0.06% vag prep is used for: Vulvular and vaginal atrophy, Atrophic vaginitis

Adult Dose

Vaginal Vulvular and vaginal atrophy Adult: Insert 2-4 g/day of vag cream intravaginally for 2 wk, then reduce gradually to half the initial dose for 2 wk followed by a maintenance dose of 1 g 1-3 times/wk. Postmenopausal vaginal atrophy Adult: Insert a vag ring containing 2 mg of estradiol and keep in place for 90 days. Urogenital symptoms Adult: Insert a vag ring containing 2 mg of estradiol and keep in place for 90 days. Atrophic vaginitis Adult: Initial: Insert 1 tab (20 mcg) once daily for 2 wk. Maintenance: Insert 1 tab twice wkly. Attempt to discontinue or taper medication at 3-6 mthly intervals.

Child Dose

Renal Dose

Administration

Intravaginal Administration Intravaginal ring Insert in upper third of vaginal vault; the ring is to remain in place continuously for 3 months, after which it is to be removed and, if appropriate, replaced by a new ring Should the ring be removed or fall out at any time during the 90-day treatment period, rinse the ring in lukewarm water and reinsert (by the patient, or, if necessary, by a physician or nurse) Vaginal tablet or cream Use applicator provided with drug to insert vaginal tablet or measure dose of vaginal cream Lay on back with pelvis slightly tilted upward, or stand with one knee bent (ie, foot on seat of chair or toilet), insert the prescribed dose with applicator The applicator should be inserted (without forcing) as far as comfortably possible, or until half of the applicator is inside vagina Note: The vaginal tablet dissolves gradually over several hours, so bedtime application may be desired

Contra Indications

Hypersensitivity; undiagnosed vag bleeding; thrombophloebitis or thromboembolic disorders; breast carcinoma except in selected patients being treated for metastatic disease; oestrogen-dependent tumor; porphyria; pregnancy.

Precautions

Conditions exacerbated by fluid retention; hypercalcaemia, cerebrovascular diorders, coronary artery disease, gall bladder diseases; lipid effects; familial defects of lipoprotein metabolism. May increase BP, risk of venous thromboembolism, breast cancer, benign hepatic adenoma, endometrial cancer and size of preexisting uterine leiomyomata. Dosage should be reduced in hepatic impairment. Lactation. Child. Lactation Should not be used during lactation; estrogen administration to nursing women has been shown to decrease the quantity and quality of the breast milk Caution should be exercised when estrogen is administered to a nursing woman

Pregnancy-Lactation

Pregnancy Therapy not indicated for use in pregnancy; there are no data with use in pregnant women; however, epidemiologic studies and meta-analyses have not found an increased risk of genital or nongenital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to combined hormonal contraceptives (estrogen and progestins) before conception or during early pregnancy Lactation Therapy not indicated for use in females of reproductive potential; estrogens present in human milk and can reduce milk production in breast-feeding females; reduction can occur at any time but is less likely to occur once breast-feeding is well- established

Interactions

CYP1A2 and CYP3A4 inducers e.g. aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together.

Adverse Effects

Side effects of Estradiol 0.06% vag prep : >10% Headache (9-16%) 1-10% Vulvovaginal mycotic infection (5-8%), Vulvovaginal pruritus (8%), Back pain (7%), Abdominal pain (7%), Diarrhea (5%)

Mechanism of Action

Estradiol is a naturally occurring oestrogen. Oestrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. They modulate the pituitary secretion of gonadotrophins, LH and FSH through a negative feedback system.