Estradiol Vaginal Cream 42.5gm 0.01%

Route: Intravaginal — using calibrated applicator (1–4 gram doses).

• Fill the applicator to the prescribed gram marking (typically 1–4 g per dose for the FDA-approved preparation, though prescriber direction for compounded product may specify a smaller volume).
• Insert the applicator gently into the vagina and depress the plunger to deposit the cream.
• Remain recumbent for several minutes after insertion.
• Wash applicator with mild soap and warm water after each use and allow to air dry.
• The 42.5 g tube with a 1g/dose regimen provides approximately 42 applications.

Dosing is prescriber-determined. Prescribers may specify a dose different from the commercial labeling (e.g., 0.5 g instead of 2–4 g per dose) to further reduce systemic absorption:

• FDA-approved Estrace® cream dosing: 2–4 g/day for 2 weeks initial, then 1 g three times weekly for maintenance (for treatment of vaginal atrophy due to menopause).
• Compounded prescriptions often specify smaller doses (0.5–1 g) to minimize systemic absorption while maintaining local efficacy.
• Confirm the exact gram-per-dose and frequency with Genesis Compounding and the prescribing clinician.

• Estradiol 0.01% (vaginal): Intravaginally applied estradiol diffuses through the vaginal mucosa and binds ERα and ERβ in vaginal epithelial and stromal cells. Estrogen receptor activation restores stratified squamous epithelium, increases glycogen-producing superficial cells, promotes healthy lactobacillus colonization, lowers vaginal pH, and improves tissue elasticity, lubrication, and barrier function. At 0.01% (0.1 mg/g) and low application volumes, systemic absorption is limited; at higher-volume doses (2–4 g), measurable systemic estradiol increases may occur.

Clinical Context: Low-dose local vaginal estradiol is a first-line therapy for genitourinary syndrome of menopause (GSM) — vaginal dryness, dyspareunia, atrophic vaginitis, recurrent UTIs, and urinary urgency. The 0.01%/42.5g compounded formulation mirrors the FDA-approved commercial product in both concentration and supply quantity, enabling patient-specific compounding when commercial preparations are unavailable, contain excipients not tolerated by the patient, or require formulation modifications. Clinical response is typically seen within 4–8 weeks; continued therapy is required for maintained benefit.

Monitoring Considerations:

• Symptom reassessment at 4–8 weeks.
• Vaginal maturation index or pH as objective response markers if desired.
• Progestogen co-administration at prescriber discretion (very-low-dose local vaginal estrogen typically does not mandate routine endometrial protection, but higher-volume applications may warrant it).
• Serum estradiol if systemic exposure is a concern.

Contraindications:

• Known or suspected estrogen-dependent malignancies (breast, endometrial cancer).
• Undiagnosed abnormal genital bleeding.
• Active or history of DVT, PE, arterial thromboembolic events.
• Active liver disease.
• Known hypersensitivity to estradiol or cream components.
• Pregnancy.

Warnings & Precautions:

• Systemic absorption increases with dose volume — higher-volume doses may warrant endometrial monitoring and progestogen consideration.
• Latex contraceptive incompatibility: vaginal cream may degrade latex condoms and diaphragms.
• Use in breast cancer survivors should be guided by oncology in consultation with prescribing clinician and patient preferences.

Drug Interactions:

• Minimal at low-dose local application. At higher volumes, consider CYP3A4 interactions with any systemically absorbed estradiol. Thyroid hormone monitoring if systemic estrogen absorption increases.

Common Side Effects: Vaginal discharge (cream residue), mild vaginal irritation, burning, or pruritus (especially early in therapy), headache. Systemic side effects (nausea, breast tenderness) are more likely at higher application volumes.

Store at controlled room temperature (20–25°C / 68–77°F) in a tightly closed tube, away from heat, moisture, and direct light. Do not freeze. Store out of reach of children. Observe the beyond-use date assigned by Genesis Compounding; do not use after this date. Once the tube is opened, use within the labeled timeframe.

Is this the same as the commercially available Estrace® vaginal cream?

This compounded preparation contains estradiol at the same concentration (0.01% / 0.1 mg per gram) and in a 42.5 g tube — the same as FDA-approved Estrace® vaginal cream (Prasco NDC 66993-002-10). However, this is a 503A compounded preparation from Genesis Compounding, not the branded product. It is not FDA-approved as a finished compounded drug.

How much cream should I use per application?

The prescribing clinician specifies the exact gram amount per dose. For vaginal atrophy, the FDA-approved labeling for this concentration starts at 2–4 grams; however, many clinicians prescribe smaller volumes (0.5–1 g) for maintenance to minimize systemic absorption. Follow your prescriber's instructions and confirm with Genesis Compounding if uncertain.

Do I need a progestogen with this cream?

At low volumes (0.5–1 g/dose), systemic absorption is limited and most guidelines do not require routine progestogen for endometrial protection. At higher volumes (2–4 g/dose), some systemic absorption occurs and progestogen consideration is warranted by the prescriber. Individual clinical assessment is required.

Is this FDA-approved?

This is a patient-specific, prescriber-directed 503A compounded preparation from Genesis Compounding and is not FDA-approved as a finished compounded drug product.

What should I do if I experience irritation?

Mild irritation is common in the first few days as the vaginal tissue adjusts. If irritation is severe, persistent, or associated with unusual discharge, redness, or swelling, contact your prescriber. An excipient sensitivity may rarely occur — Genesis Compounding can reformulate if a specific component is identified as the cause.