Valena Cream

Vulvular and vaginal atrophy, Atrophic vaginitis

Vaginal Prep (Vaginal Cream 0.01%) Vulvular and vaginal atrophy due to menopause Adult The usual dosage range is 2 to 4 g (marked on the applicator) daily for one or two weeks, then gradually reduced to one-half initial dosage for a similar period. A maintenance dosage of 1g, one to three times a week, may be used after restoration of the vaginal mucosa has been achieved. Vaginal Prep (Vaginal Tab) 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.

Intravaginal Administration Instructions for Applicator Use: Step 1. Open the sealed wrapper and remove the applicator. Step 2. Insert the tip of the applicator into the tube. Step 3. Press down the tube and squeeze the specified amount of gel into the applicator tube. Step 4. Remove the applicator from the tube. Step 5. Gently insert the rounded tip of the applicator. Step 6. Push the plunger to release the cream. Step 7. Remove the applicator. (It is normal for a small amount of gel to be left in the applicator. You will still get the right dose of medicine.) Keep the applicator clean and germ free for later use. Vaginal cream or tablet Use the 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 the 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

Undiagnosed abnormal genital bleeding Known, suspected, or history of breast cancer Known or suspected estrogen-dependent neoplasia Active DVT, PE, or history of these conditions Active arterial thromboembolic disease (eg, stroke, MI), or a history of these conditions Known anaphylactic reaction or angioedema to estrogen Known liver impairment or disease Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders Known or suspected pregnancy

Increased risk of endometrial cancer Close clinical surveillance of all women taking estrogens is important Risk of endometrial cancer in women with a uterus increases with use of unopposed estrogens; adding progestin to estrogen therapy may reduce risk of endometrial hyperplasia, a precursor to endometrial cancer Adequate diagnostic measures, including endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding Breast cancer The WHI estrogen plus progestin substudy also demonstrated an increased risk of invasive breast cancer; prescribe estrogens with or without progestins at the lowest doses and for the shortest duration System absorption occurs with intravaginal administration; consider warnings, precautions, and adverse effects associated with systemic estrogen-alone therapy Increased risk of stroke and DVT reported with estrogen-alone therapy; increased risk of PE, DVT, stroke, and MI reported with estrogen plus progestin therapy; discontinue drug immediately if these conditions occur or are suspected The WHI estrogen plus progestin substudy reported a statistically nonsignificant increased risk of ovarian cancer (4 vs 3 cases per 10,000 women-years) Estrogen with or without progesterone may increase risk of dementia Increased risk of gallbladder disease (2- to 4-fold) requiring surgery in postmenopausal women receiving estrogen has been reported Severe hypercalcemia in women with breast cancer and bone metastases reported with estrogen use; if hypercalcemia occurs, discontinue estrogen and initiate appropriate treatment to reduce serum calcium level Retinal vascular thrombosis reported; discontinue estrogen pending examination if there is a sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia, or migraine; if papilledema or retinal vascular lesions diagnosed, permanently discontinue estrogens Rare occurrences reported of

Not Classi Pregnancy 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 (estrogens and progestins) before conception or during early pregnancy Lactation Estrogens are present in human milk and can reduce milk production in breast-feeding females; this reduction can occur at any time but is less likely to occur once breastfeeding is well-established; the clinical need for therapy and any potential adverse effects on breastfed child or from underlying maternal condition. developmental and health benefits of breastfeeding should be considered along with the mother’s

CYP3A4 inducers or inhibitors may affect estrogen drug metabolism CYP3A4 inducers (eg, St. John's wort [Hypericum perforatum] preparations, phenobarbital, carbamazepine, and rifampin) may reduce plasma concentrations of estrogens, possibly resulting in a decrease in therapeutic effects and/or changes in the uterine bleeding profile CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice) may increase plasma concentrations of estrogens and may result in side effects

>10% Headache (5-16%) 1-10% Vulvovaginal mycotic infection (5-8%) Vulvovaginal pruritus (8%) Back pain (7%) Abdominal pain (7%) Diarrhea (5%) Breast pain, Irregular vaginal bleeding or spotting, Abdominal bloating, Nausea and vomiting, Hair loss, Fluid retention, Vaginal yeast infection, Reactions from inserting Vaginal Cream, such as vaginal burning, irritation, itching etc.

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.

Valena 0.01% Cream manufactured by Incepta Pharmaceuticals Ltd.. Its generic name is Estradiol vag prep.