Pronunciation:

os-PEM-i-feen

Brand Names:

• Osphena

Dosage Forms:

• Tablet

Warnings:

Endometrial CancerOspemifene is an estrogen agonist/antagonist with tissue selective effects. In the endometrium, ospemifene has estrogen agonistic effects. There is a potential increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adequate diagnostic measures, including directed and random endometrial sampling when indicated, should be undertaken to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding.Cardiovascular DisordersIn the clinical trials for ospemifene (duration of treatment up to 15 months) the incidence rates of thromboembolic and hemorrhagic stroke were 1.13 and 3.39 per thousand women years, respectively in the ospemifene 60 mg treatment group and 3.15 and 0 with placebo. The incidence of DVT was 2.26 per thousand women years (2 reported cases) in the ospemifene 60 mg treatment group and 3.15 per thousand women years (1 reported case) with placebo. Ospemifene should be prescribed for the shortest duration consistent with treatment goals and risks for the individual woman.There is a reported increased risk of stroke and deep vein thrombosis (DVT) in postmenopausal women (50 to 79 years of age) who received daily oral conjugated estrogens (CE) [0.625 mg]-alone therapy over 7.1 years as a part of the Women's Health Initiative (WHI) .

Classifications:

Therapeutic—

Endocrine-Metabolic Agent

Pharmacologic—

Selective Estrogen Receptor Modulator

Uses of This Medicine:

Ospemifene is used to treat women with moderate to severe dyspareunia (painful intercourse) and moderate to severe vaginal dryness caused by menopause. Low estrogen levels may cause changes in the vulvar and vaginal areas that lead to atrophy (a shrinking of tissues) and dryness. Ospemifene works like natural estrogen in the body.

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Ospemifene is not indicated for use in the pediatric population.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of ospemifene in the elderly.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Abiraterone Acetate
• Amiodarone
• Ceritinib
• Clarithromycin
• Eslicarbazepine Acetate
• Fluconazole
• Fluvoxamine
• Ketoconazole
• Piperaquine
• Regorafenib

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Amobarbital
• Aprobarbital
• Bosentan
• Butabarbital
• Butalbital
• Carbamazepine
• Dexamethasone
• Efavirenz
• Enzalutamide
• Etravirine
• Fosphenytoin
• Mephobarbital
• Methohexital
• Modafinil
• Nafcillin
• Nevirapine
• Oxcarbazepine
• Pentobarbital
• Phenobarbital
• Phenytoin
• Prednisone
• Primidone
• Rifabutin
• Rifampin
• Rifapentine
• Secobarbital
• St John's Wort
• Thiopental

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Abnormal or unusual vaginal bleeding or
• Blood clots, active or history of or
• Breast cancer, known or suspected, or a history of or
• Deep vein thrombosis (blood clot in the leg), active or history of or
• Heart attack, active or history of or
• Liver disease, severe or
• Pulmonary embolism (blood clot in the lung), active or history of or
• Stroke, active or history of or
• Tumors (estrogen-dependent), known or suspected—Should not be used in patients with these conditions.

• Diabetes or
• Heart disease or
• Hypercholesterolemia (high cholesterol or fats in the blood) or
• Hypertension (high blood pressure) or
• Obesity, or history of or
• Systemic lupus erythematosus—Use with caution. May cause side effects to become worse.

Proper Use of This Medicine:

It is very important that you use this medicine exactly as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause unwanted side effects.

This medicine comes with a patient information leaflet. Read and follow the instructions in the leaflet carefully. Ask your doctor if you have any questions.

Take this medicine with food.

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  • For moderate to severe dyspareunia:
    • Adults—60 milligrams (mg) once a day.
    • Children—Use is not recommended.
  • For moderate to severe vaginal dryness:
    • Adults—60 milligrams (mg) once a day.
    • Children—Use is not recommended.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage—

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it. Blood tests may be needed to check for unwanted effects.

It is unlikely that a postmenopausal woman may become pregnant. But you should know that using this medicine while you are pregnant could harm your unborn baby. If you think you have become pregnant while using the medicine, tell your doctor right away.

Using this medicine may increase your risk for blood clots, strokes, or heart attacks. Your risk for these serious problems is even greater if you have high blood pressure, high cholesterol, or diabetes, or if you are overweight or smoke tobacco. Talk to your doctor about this risk. Contact your doctor right away if you have chest pain, confusion, difficulty speaking, double vision, headaches, an inability to move the arms, legs or facial muscle, or an inability to speak.

Using this medicine may increase your risk for endometrial or uterine cancer. Talk to your doctor about this risk. Check with your doctor right away if you have abnormal vaginal bleeding.

Make sure any doctor who treats you knows that you are using this medicine. You may need to stop using this medicine before you have surgery or if you need to stay in bed for a long time.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Less common

Vaginal bleeding

Incidence not known

Anxiety

change in vaginal discharge

chest pain

cough

dizziness or lightheadedness

fainting

fast heartbeat

fever

hives, itching, skin rash

hoarseness

irritation

joint pain, stiffness, or swelling

large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or genitals

pain or feeling of pressure in the pelvis

pain, redness, or swelling in the arm or leg

redness of the skin

swelling of the eyelids, face, lips, hands, or feet

tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over the affected area

tightness in the chest

troubled breathing or swallowing

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Feeling of warmth

redness of the face, neck, arms, and occasionally, upper chest

sudden sweating

white or brownish vaginal discharge

Less common

Headache

increased sweating

muscle spasms

night sweats

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.