美国FDA 批准VIVUS公司的雌二醇定量透皮喷雾剂（estradiol，EvaMist）上市，用于治疗绝经后妇女中度至严重的血管舒缩症状。本品是美国FDA批准的首个雌二醇透皮喷雾剂。此快速干燥的美国专利透皮喷雾剂由雌二醇、挥发性溶媒乙醇（溶解药物）和水杨酸乙基己酯（octisalate，一种在一些防晒用品中常用的皮肤渗透促进剂）组成。剂量规格：雌二醇1.53 mg /90 μL/喷。
美国FDA批准本品代表VIVUS公司发展史上的一个重要里程碑：从产品构思至获准上市不到3年。据预测，本品2008年第一季度在美国上市后年销售峰值将达1.25亿美元。

本品为释放天然雌二醇的定量喷雾剂，每日应在相同的时间使用，喷于清洁、干燥和未破损的前臂至肘和手腕间的皮肤上。按一日1次的给药方案，药物被吸收进入血流可持续作用24小时。喷雾后在45秒内干燥形成“看不见的贴片”，但在皮肤上不留痕迹和残留物。临床研究显示，喷雾45秒后再搓擦和清洗不能去除已喷雾的用药剂量。此种透皮喷雾剂给药剂量较口服片低的多，而且较透皮贴片对皮肤无刺激性。本品的生产成本小，故价格低。

本品常见的不良反应是头痛、乳房痛、无规则阴道出血、胃/腹部痉挛、恶心、呕吐、掉发、水潴留及霉菌感染等。

EVAMIST

Indication(s):

Moderate to severe vasomotor symptoms of menopause.

Pharmacology:

The addition of exogenous estrogens helps to alleviate the vasomotor symptoms associated with declining estrogen levels.

Clinical Trials:

In a 12-week, randomized, double-blind, placebo-controlled clinical trial, a total of 454 postmenopausal women were randomized and received at least one dose of Evamist or placebo. Efficacy was determined as a statistically significant and clinically significant (at least two per day or 14 per week difference) reduction in hot flush frequency and a statistically significant reduction in severity for Evamist versus placebo. One, two, or three daily sprays of Evamist were shown to be better than placebo for relief of frequency and severity of moderate to severe vasomotor symptoms at Week 4 and Week 12.

Legal Classification:

Rx

Adults:

Prime pump before 1st use. Apply to clean, dry, unbroken skin on the inside of the forearm between the elbow and wrist. Initially 1 spray daily; may increase to 2–3 sprays if needed; do not spray in the same area. Reevaluate periodically. Allow spray to dry before dressing; do not wash area for at least 30 minutes after application.

Children:

Not applicable.

Contraindication(s):

Breast or estrogen-dependent carcinoma. Undiagnosed abnormal vaginal bleeding. Thromboembolic disorders (eg, stroke or MI within one year, DVT, pulmonary embolism). Thrombophlebitis. Liver dysfunction or disease. Pregnancy (Cat.X).

Warnings/Precautions:

Use shortest duration and lowest dose consistent with treatment goals and risks. Not for prevention of cardiovascular disease (CVD) or dementia. Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Renal dysfunction.Gallbladder disease. Hypertriglyceridemia. Hypothyroidism. Hypercoagulability. Conditions aggravated by fluid retention. Bone disease associated with hypercalcemia. Do initial complete physical; repeat annually (include BP, mammogram, PAP smear). Discontinue if visual disturbances or jaundice occurs, and during immobilization, and at least 4–6 weeks before surgery associated with thromboembolism. Manage risk factors for CVD and VTE appropriately. May aggravate asthma, diabetes, epilepsy, migraine, porphyria, SLE, hepatic hemangiomas. May interfere with lab tests (eg, thyroid, PT, glucose tolerance, HDL-C/LDL-C). Product is flammable.Nursing mothers.

Interaction(s):

Avoid applying sunscreen 1 hr after (decreases estradiol absorption). May need higher doses of thyroid-replacement therapy. May be antagonized by CYP3A4 inducers. May be potentiated by CYP3A4 inhibitors.

Adverse Reaction(s):

Headache, breast/nipple pain, nausea, back pain, nasopharyngitis.

How Supplied:

Pump—8.1mL (56 sprays/pump)

Last Updated:

1/14/2009

Evamist^® is approved by the FDA for use after menopause to reduce moderate-to-severe hot flashes.

Estrogens increase the chance of getting cancer of the uterus (womb). Report any unusual vaginal bleeding right away while you are using Evamist. Vaginal bleeding after menopause may be a warning sign of cancer of the uterus. Your healthcare provider should check any unusual vaginal bleeding to find out the cause.

Do not use estrogens with or without progestins to prevent heart disease, heart attacks, strokes, or dementia. Using estrogens, with or without progestins, may increase your chance of getting heart attacks, strokes, breast cancer, and blood clots. Using estrogen, with or without progestins, may increase your risk of dementia, based on a study of women age 65 years or older. Evamist should not be used if you have unusual vaginal bleeding; currently have or have had certain cancers, including cancer of the breast or uterus; had a stroke or heart attack in the past year; currently have or have had blood clots; currently have or have had liver problems; or think you may be, or know that you are, pregnant.

The most common side effects that may occur with Evamist are headache, breast tenderness, the common cold, nipple pain, back pain, nausea, and joint pain。

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Evamist

Evamist is the first hormone replacement medication that comes in the form of a skin spray. This prescription medication is approved to treat moderate to severe hot flashes or night sweats that are caused by menopause. Evamist is sprayed onto your forearm once daily. Although most women tolerate the medication well, potential side effects can include back pain, headaches, and breast tenderness.

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What Is Evamist?

Evamist® (estradiol transdermal spray) is a prescription hormone replacement medication. It is the first hormone replacement therapy that comes as a skin spray. Evamist is approved for treating moderate to severe hot flashes or night sweats due to menopause.

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(Click Evamist Uses for more information on what Evamist is used for, including possible off-label uses.)

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Who Makes Evamist?

Evamist is manufactured by Ther-Rx Corporation.

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How Does Evamist Work?

Evamist contains estradiol, an estrogen hormone. Estradiol is the predominant estrogen in women prior to menopause. Evamist helps to relieve menopausal symptoms by replacing the estrogen that the ovaries no longer produce. It is readily absorbed through the skin.

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When and How to Use Evamist

Some general considerations for when and how to use Evamist include the following:

•Evamist comes as a spray that is applied to the skin once daily. It comes in an applicator that is specially designed to deliver the exact same dose with each spray.

•Make sure to closely read the directions that come with Evamist. You must prime the pump the first time you use it by pumping three times with the cover on. After this, you do not need to reprime the pump.

•Evamist is sprayed onto an area of clean, dry, unbroken skin on an area of the forearm between the elbow and wrist. If your dosage requires more than one spray, the sprays should be right next to each other but not overlapping. Do not rub Evamist into the skin.

•Evamist dries quickly (within about a minute). Wait at least two minutes before getting dressed, in order to protect your clothing, and wait at least 30 minutes before bathing or showering.

•Never apply Evamist to the breast or vagina.

•For the medication to work properly, it must be taken as prescribed.