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Estradiol and levonorgestrel (Transdermal route)

Pronunciation:

es-tra-DYE-ol, lee-voe-nor-JES-trel

Brand Names:

  • Climara Pro

Dosage Forms:

  • Patch, Extended Release

Warnings:

Transdermal route(Patch, Extended Release)

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 of age) have been reported. An increased risk of developing probable dementia in postmenopausal women 65 years of age or older has also been reported. Estrogens with progestins reduces the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer. Estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman. Postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding should have adequate diagnostic tests, including directed or random endometrial sampling, to rule out malignancy .

Classifications:

Therapeutic

Endocrine-Metabolic Agent

Pharmacologic

Estrogen

Uses of This Medicine:

Estradiol and levonorgestrel combination skin patch is used treat moderate to severe hot flashes and other symptoms of menopause or low amounts of estrogen. It is also used in women to prevent osteoporosis after menopause.

Estradiol is an estrogen hormone. Levonorgestrel is a progesterone. The hormones from the patch are absorbed through your skin into your body. It works by preventing symptoms, such as feelings of warmth in the face, neck, and chest, or sudden strong feelings of heat and sweating (hot flashes) in women during menopause.

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

Use of estradiol and levonorgestrel combination skin patch is not indicated in the pediatric population. Safety and efficacy have not been established.

Older adults

Although appropriate studies on the relationship of age to the effects of estradiol and levonorgestrel combination skin patch have not been performed in the geriatric population, no geriatric-specific problems have been documented to date. However, elderly patients are more likely to have breast cancer, stroke, or dementia, which may require caution in patients receiving estradiol and levonorgestrel combination skin patch.

Pregnancy

Pregnancy CategoryExplanation
All TrimestersXStudies in animals or pregnant women have demonstrated positive evidence of fetal abnormalities. This drug should not be used in women who are or may become pregnant because the risk clearly outweighs any possible benefit.

Breast-feeding

Studies suggest that this medication may alter milk production or composition. If an alternative to this medication is not prescribed, you should monitor the infant for side effects and adequate milk intake.

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 not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Tranexamic Acid

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.

  • Bupropion
  • Carbamazepine
  • Ceritinib
  • Dabrafenib
  • Darunavir
  • Donepezil
  • Eliglustat
  • Idelalisib
  • Isotretinoin
  • Lesinurad
  • Lixisenatide
  • Lumacaftor
  • Pitolisant
  • Pixantrone
  • Sugammadex
  • Theophylline
  • Tizanidine
  • Ulipristal

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.

  • Acitretin
  • Alprazolam
  • Amprenavir
  • Aprepitant
  • Atazanavir
  • Bacampicillin
  • Betamethasone
  • Bexarotene
  • Bosentan
  • Clarithromycin
  • Colesevelam
  • Cyclosporine
  • Delavirdine
  • Efavirenz
  • Eslicarbazepine Acetate
  • Etravirine
  • Fosamprenavir
  • Fosaprepitant
  • Fosphenytoin
  • Ginseng
  • Griseofulvin
  • Ketoconazole
  • Lamotrigine
  • Levothyroxine
  • Licorice
  • Modafinil
  • Mycophenolate Mofetil
  • Mycophenolic Acid
  • Nelfinavir
  • Oxcarbazepine
  • Perampanel
  • Phenobarbital
  • Phenytoin
  • Prednisolone
  • Primidone
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Rosuvastatin
  • Rufinamide
  • Selegiline
  • St John's Wort
  • Tacrine
  • Telaprevir
  • Tipranavir
  • Topiramate
  • Troglitazone
  • Troleandomycin
  • Voriconazole
  • 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. 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 may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

  • Caffeine

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 (eg, deep vein thrombosis, pulmonary embolism), active or history of or
  • Breast cancer, known or suspected, or history of or
  • Heart attack, active or history of or
  • Liver disease or
  • Protein C or protein S deficiency, or other known blood clotting disorders or
  • Stroke, active or history of or
  • Surgery with a long period of inactivity or
  • Tumors (estrogen-dependent), known or suspected Should not be used in patients with these conditions.
  • Angioedema or anaphylaxis Should not be used in patients who have experienced these conditions with prior use of estradiol and levonorgestrel combination skin patch.
  • Asthma or
  • Cancer, history of or
  • Diabetes or
  • Edema (fluid retention or body swelling) or
  • Endometriosis or
  • Epilepsy (seizures) or
  • Gallbladder disease or
  • Heart disease or
  • Hereditary angioedema (swelling of the face, lips, tongue, or throat) or
  • Hypercalcemia (high calcium in the blood) or
  • Hypertension (high blood pressure) or
  • Hypertriglyceridemia (high triglycerides or fats in the blood) or
  • Hypocalcemia (low calcium in the blood), severe or
  • Hypothyroidism (an underactive thyroid) or
  • Jaundice during pregnancy or from using hormonal therapy in the past or
  • Liver tumors or
  • Migraine headache or
  • Porphyria (an enzyme problem) or
  • Systemic lupus erythematosus (SLE) Use with caution. May make these conditions worse.
  • Kidney disease, severe Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of This Medicine:

It is very important that you use this medicine only 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 is for use on the skin only. Do not get it in your eyes, nose, mouth, breast, or vagina. Do not use it on skin areas that have cuts, scrapes, or burns. If it does get on these areas, rinse it off right away with water.

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

To use:

  • Wash your hands with soap and water before and after you use this medicine.
  • Carefully tear open the pouch when you are ready to put the patch on your skin. Do not cut it.
  • Peel off the backing from the patch and apply the patch to a clean, dry, and hair-free area of the lower stomach or upper buttock area. This area must be free of powder, oil, or lotion for the patch to stick on to your skin.
  • Press the patch firmly in place with your hand for about 10 seconds.
  • Do not apply the patch on the breast or over any skin folds. Do not apply the patch on oily, broken, burned, or irritated skin, or areas with skin conditions (such as birth marks, tattoos). Avoid applying the patch on the waistline or other places where tight clothing may rub it off.
  • Wear the patch at all times until it is time to put on a new patch. Do not expose it to the sun for long periods of time.
  • When replacing your patch, make sure to apply the new patch to a different area of your lower abdomen. Wait at least 1 week before applying a patch to the same area.
  • When changing a patch, slowly peel it off from your skin. If you have any patch adhesive left on your skin, allow it to dry for 15 minutes and gently rub the sticky area with oil or lotion to remove it. It is best to change your patch on the same days of each week to help you remember.
  • You may take a bath, shower, or swim while using this medicine. Doing so will not affect the patch.
  • If a patch falls off, just put it back on a different area. If the patch does not stick completely, put on a new patch but continue to follow your original schedule for changing your patch.
  • To throw away a used patch: Fold the patch in half with the sticky side together and place it in a sturdy child-proof container. Throw this container in the trash away from children and pets. Do not flush the patch down the toilet.

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 transdermal dosage form (patch):
    • For hot flashes and other symptoms caused by menopause:
      • Adults At first, apply one patch (0.045 milligrams (mg) of estradiol and 0.015 mg of levonorgestrel) to the lower stomach or upper buttocks area once a week. Your doctor may adjust your dose as needed.
      • Children Use is not recommended.
    • For prevention of osteoporosis after menopause:
      • Adults At first, apply one patch (0.045 milligrams (mg) of estradiol and 0.015 mg of levonorgestrel) to the lower stomach or upper buttocks area once a week. Your doctor may adjust your dose as needed.
      • Children Use is not recommended.

Missed dose

If you forget to wear or change a patch, put one on as soon as you can. If it is almost time to put on your next patch, wait until then to apply a new patch and skip the one you missed. Do not apply extra patches to make up for a missed dose.

Storage

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

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 this medicine is working properly and does not cause unwanted effects. Pelvic exam, breast exam, and mammogram (breast x-ray) may be needed to check for unwanted effects, unless your doctor tells you otherwise.

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 having blood clots, strokes, or heart attacks. This risk may continue even after you stop using the medicine. Your risk for these serious problems is even greater if you have high blood pressure, high cholesterol in your blood, diabetes, or if you are overweight or smoke cigarettes. Contact your doctor immediately if you experience confusion, difficulty speaking, double vision, headaches, an inability to move arms, legs or facial muscle, or an inability to speak.

Using this medicine over a long period of time may increase your risk of breast cancer, endometrial cancer, or uterine cancer. Talk with your doctor about this risk. If you still have your uterus (womb), ask your doctor if you should also use a progestin medicine. Check with your doctor if you have unusual vaginal bleeding.

Using this medicine may increase your risk of dementia, especially in women 65 years of age and older.

Tell the medical doctor or dentist in charge that you are using this medicine before any kind of surgery (including dental surgery) or emergency treatment. Your doctor will decide whether you should continue using this medicine. This medicine may also affect the results of certain medical tests.

Check with your doctor immediately if severe headache or sudden loss of vision or any other change in vision occurs while you are using this medicine. Your doctor may want you to have your eyes checked by an ophthalmologist (eye doctor).

Do not take other medicines or drink grapefruit juice unless you discuss it with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) 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:

Incidence not known
Acid or sour stomach
anxiety
backache
belching
change in vaginal discharge
chest pain or discomfort
clear or bloody discharge from the nipple
confusion
cough
difficulty with speaking
difficulty with swallowing
dimpling of the breast skin
dizziness or lightheadedness
double vision
fainting
fast heartbeat
full or bloated feeling or pressure in the stomach
headache
heartburn
hives, itching, or rash
inability to move the arms, legs, or facial muscles
inability to speak
indigestion
inverted nipple
loss of appetite
lump in the breast or under the arm
nausea
pain or discomfort in the arms, jaw, back, or neck
pain or feeling of pressure in the pelvis
pain, redness, or swelling in the arm or leg
persistent crusting or scaling of the nipple
puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
redness or swelling of the breast
slow speech
sore on the skin of the breast that does not heal
stomach discomfort, upset, or pain
sudden shortness of breath or troubled breathing
sweating
swelling of the abdominal or stomach area
tightness in the chest
unusual tiredness or weakness
vaginal bleeding
vomiting

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
Back pain
body aches or pain
breast pain
burning, itching, redness, skin rash, swelling, or soreness at the application site
chills
discouragement
ear congestion
feeling sad or empty
fever
heavy nonmenstrual vaginal bleeding
irritability
loss of interest or pleasure
loss of voice
nasal congestion
runny nose
sneezing
sore throat
tiredness
trouble concentrating
trouble sleeping
Less common
Bladder pain
bloody or cloudy urine
blurred vision
cough producing mucus
diarrhea
difficult, burning, or painful urination
difficulty with moving
dizziness
excess air or gas in the stomach or intestines
frequent urge to urinate
general feeling of discomfort or illness
itching of the vagina or genital area
joint pain
lower back or side pain
muscle aches and pains
muscle pain or stiffness
pain during sexual intercourse
pain or tenderness around the eyes and cheekbones
passing gas
pounding in the ears
shivering
slow or fast heartbeat
sweating
weight gain
Incidence not known
Hair loss or thinning of the hair
pressure in the stomach
swelling of the abdominal or stomach area

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.


Last Updated: 9/15/2016
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