Pronunciation:

es-TER-i-fide ES-troe-jenz, meth-il-tes-TOS-ter-one

Brand Names:

• Covaryx
• Covaryx HS
• Essian
• Estratest
• Menogen
• Syntest D.S.
• Syntest H.S.

Dosage Forms:

• Tablet

Warnings:

Estrogens increase the risk of endometrial cancer; monitor for abnormal vaginal bleeding. Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. Increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years) have been reported. An increased risk of developing probable dementia in postmenopausal women 65 years or older has also been reported. This product contains an estrogen and androgen, not a progestin. This combination should not be used during a known or suspected pregnancy .

Classifications:

Therapeutic—

Estrogen/Androgen Combination

Pharmacologic—

Estrogen

Uses of This Medicine:

Esterified estrogens and methyltestosterone combination is used to treat the symptoms of menopause in patients who did not get relief after being treated with estrogens alone. These symptoms may include a feeling of heat, sweating, and warmth in the face, neck, or chest ("hot flashes"); and dryness, burning, and itching in the vagina.

Esterified estrogens are a man-made mixture of estrogens. Estrogen is a hormone that is produced by the body in greater amounts in females. It is necessary for normal sexual development of the female and for regulation of the menstrual cycle during the childbearing years. Methyltestosterone is a man-made form of testosterone, a hormone that is produced by the body in greater amounts in males and small amounts in females. Menopause symptoms occur when the hormone balance changes in the female body. This combination of hormones will relieve the symptoms of menopause by adding more hormones to 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—

The use of esterified estrogens and methyltestosterone combination is not recommended in children.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of esterified estrogens and methyltestosterone combination in the elderly. However, elderly patients are more likely to develop dementia and age-related kidney, liver, or heart problems, which may require caution and an adjustment in the dose for patients receiving this medicine.

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.

• Amifampridine
• Anisindione
• Bupropion
• Cosyntropin
• Dicumarol
• Donepezil
• Phenprocoumon
• Somatrogon-ghla

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.

• Ginseng
• Levothyroxine
• Licorice
• Tipranavir
• Warfarin

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 vaginal bleeding, undiagnosed or
• Blood clotting problems (e.g., deep vein thrombosis, pulmonary embolism), history of or
• Breast cancer, or history of or
• Heart attack, recent or history of or
• Liver disease, severe or
• Stroke, recent or history of—Should not be used in patients with these conditions.

• Asthma or
• Cancer (e.g., breast, cervix, liver, vagina) or
• Depression, history of or
• Diabetes or
• Edema (fluid retention) or
• Endometriosis (problem with the lining of the uterus) or
• Epilepsy or
• Eye or vision problems (e.g., retinal vascular thrombosis) or
• Gallbladder disease or
• Hepatitis (including cholestatic jaundice), history of or
• Hypercalcemia (high calcium in the blood) or
• Hypocalcemia (high calcium in the blood) or
• Hypothyroidism (underactive thyroid) or
• Migraine headaches, history of or
• Porphyria (enzyme problem) or
• Systemic lupus erythematosus—Use with caution. May make these conditions worse.

• Heart or blood vessel disease or
• Hypercholesterolemia (high cholesterol in the blood) or
• Hypertension (high blood pressure) or
• Hypertriglyceridemia (high triglycerides or fat in the blood) or
• Venous thromboembolism (clot in the veins), history of—May increase risk for more serious side effects.

Proper Use of This Medicine:

Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

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

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 treatment of menopause symptoms:
    • Adults—One to two tablets 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 to make sure the medicine is working properly and to decide if you should continue to take it. These visits should be every 6 to 12 months or as otherwise directed by your doctor.

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.

Very rarely, this medicine can cause serious side effects such as a heart attack or stroke. You are much more likely to have these side effects if you smoke cigarettes or are overweight, or if you have diabetes, high blood pressure, or a high blood cholesterol. Talk with your doctor if you think you might be at risk.

Using large doses of estrogen alone over a long period of time may increase the risk of some kinds of cancer (e.g., endometrial cancer). Talk with your doctor about this risk. If you have vaginal bleeding with this medicine, call your doctor right away.

This medicine may increase the risk of getting breast cancer. It is very important that you check your breasts on a regular basis for any unusual lumps or discharge, and that you have breast x-rays every year as directed by your doctor. These exams are very important if you have a family member with a history of breast cancer. Talk with your doctor about this risk.

This medicine may increase the risk of getting dementia in elderly women (above 65 years of age). Talk with your doctor if this concerns you.

Check with your doctor right away if blurred vision, difficulty with reading, or any other change in vision occurs during or after treatment. Your doctor may want you to have your eyes checked by an ophthalmologist (eye doctor).

Using large doses of methyltestosterone over a long period of time may increase the risk of serious liver problems (e.g., peliosis hepatis or liver cancer). Talk with your doctor about this risk.

Before you have any medical tests, tell the medical doctor in charge that you are taking this medicine. The results of some tests may be affected by this medicine. Also, you may need to stop using this medicine for a few weeks before and after having surgery, or if you are inactive for a long period of 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:

More common

Absent, missed, or irregular menstrual periods

acne or oily skin

decreased breast size

enlarging clitoris

hoarseness or deepening of the voice

menstrual changes

stopping of menstrual bleeding

unnatural hair growth or loss

Rare

Continuing nausea

cough

dark-colored urine

difficulty with swallowing

dizziness

fast heartbeat

fever

hives

itching

light-colored stools

loss of appetite

puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue

purple or red-colored spots on the body or inside the mouth or nose

shortness of breath

skin rash

sore throat

tightness in the chest

unusual tiredness or weakness

vomiting

wheezing

Incidence not known

Abdominal or stomach bloating, cramps, or pain

anxiety

bleeding from gums or nose

blistering, peeling, or loosening of the skin

bloating

bloody or cloudy urine

burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings

change in vaginal discharge

changes in skin color, pain, or tenderness

chest pain or discomfort

chills

clay-colored stools

clear or bloody discharge from nipple

confusion

constipation

convulsions

darkening of urine

decrease in amount of urine

diarrhea

difficult, burning, or painful urination

difficulty with breathing

difficulty with moving

difficulty with speaking

dimpling of the breast skin

dizziness or lightheadedness

double vision

eye pain

fainting

fever

fluid-filled skin blisters

frequent urge to urinate

headache

heavy bleeding

inability to move the arms, legs, or facial muscles

inability to speak

indigestion

inverted nipple

irregular heartbeats

itching of the vagina or genital area

joint or muscle pain

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

light-colored stools

loss of appetite

lump in the breast or under the arm

mood or mental changes

muscle cramps in the hands, arms, feet, legs, or face

muscle pain or stiffness

nausea

noisy, rattling breathing

numbness and tingling around the mouth, fingertips, or feet

pain

pain during sexual intercourse

pain in the ankles or knees

pain or discomfort in the arms, jaw, back, or neck

pain or feeling of pressure in pelvis

painful, red lumps under the skin, mostly on the legs

pains in the stomach, side, or abdomen, possibly radiating to the back

pelvic pain

persistent crusting or scaling of the nipple

pinpoint red or purple spots on the skin

poor insight and judgment problems with memory or speech

red, irritated eyes

redness or swelling of the breast

ringing in the ears

sensitivity to the sun

shortness of breath

skin thinness

slow speech

sore on the skin of the breast that does not heal

sore throat

sores, ulcers, or white spots in the mouth or on the lips

stomach pain

sudden shortness of breath or troubled breathing

sweating

swelling

swelling of the fingers, hands, feet, or lower legs

tenderness of the breast

thick, white curd-like vaginal discharge without odor or with mild odor

tiredness

tremor

trouble recognizing objects

trouble thinking and planning

trouble walking

troubled breathing at rest

unexpected or excess milk flow from breasts

unpleasant breath odor

vaginal bleeding

vision changes

vomiting of blood

weakness

weight gain

yellow eyes or skin

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:

Incidence not known

Blemishes on the skin

brown, blotchy spots on the exposed skin

decreased interest in sexual intercourse

depression

headache, severe and throbbing

inability to have or keep an erection

increase or decrease in weight

increased hair growth, especially on the face

increased in sexual ability, desire, drive, or performance

increased interest in sexual intercourse

irritability

leg cramps

loss in sexual ability, desire, drive, or performance

loss of hair

mental depression

pimples

redness of the skin

swelling or inflammation of the mouth

twitching, uncontrolled movements of the tongue, lips, face, arms, or legs

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.