Climara Pro 0.045mg/day Patches 4's

Manufacturer BAYER Active Ingredient Estradiol and Levonorgestrel(es tra DYE ole & LEE voe nor jes trel) Pronunciation Es-tra-DYE-ole & LEE-voe-nor-JES-trel
WARNING: Do not use this drug to prevent heart disease or dementia. A study of women taking an estrogen with a progestin showed a raised chance of heart attack, stroke, blood clot, breast cancer, and dementia. The chance of stroke, blood clot, and dementia was also raised when the estrogen was taken alone. Not all products and doses were studied. It is not known if the same effects may happen with this drug.The chance of endometrial cancer may be raised with the use of estrogen alone in patients with a uterus. Use of a progestin along with estrogen may lower the risk. Call your doctor right away if you have unexplained or long-lasting vaginal bleeding.Use this drug for the shortest time needed at the lowest useful dose. Your doctor will talk with you on a regular basis to see if you need to keep taking this drug. @ COMMON USES: It is used to prevent soft, brittle bones (osteoporosis) after menopause.It is used to treat signs caused by menopause.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Hormone Replacement Therapy (HRT)
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Pharmacologic Class
Estrogen/Progestin Combination
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Pregnancy Category
Category X
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FDA Approved
Oct 2003
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Climara Pro is a skin patch that contains two female hormones, estradiol (an estrogen) and levonorgestrel (a progestin). It is used by women after menopause to help with symptoms like hot flashes and to prevent bone thinning (osteoporosis). The patch is applied to your skin once a week and continuously releases the hormones.
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How to Use This Medicine

Proper Use of Your Medication Patch

To use this medication correctly, follow your doctor's instructions and read all the information provided. Apply the patch to clean, dry, healthy skin on either the lower belly or upper buttocks. Each time you apply a new patch, choose a different site to avoid skin irritation.

Applying the Patch: Important Guidelines

- Do not apply the patch to your breast.
- Avoid placing the patch on your waistline.
- Choose a site where the patch won't be dislodged by sitting.
- Do not apply to irritated, damaged, or sensitive skin.
- Avoid areas with skin folds or where tight clothing may rub against the patch.
- Do not apply the patch to skin that has recently been treated with creams, oils, lotions, powder, or other skin products, as this may affect how well the patch adheres.

Patch Maintenance and Replacement

- If the patch starts to loosen at the edges, press them firmly to secure it.
- If the patch falls off, reapply it. If you're unable to reapply the same patch, use a new one in a different area.
- After removing a patch, fold the sticky sides together and dispose of it in a way that prevents children and pets from accessing it.

Water Exposure and Patch Use

Exposure to water through swimming, bathing, showering, or using a sauna may cause the patch to detach. While it's unclear how water exposure affects the medication's efficacy, it's essential to be aware of this potential issue.

Storage and Disposal

Store your medication patches at room temperature, keeping them in their pouches until you're ready to use them.

Missed Dose

If you miss applying a patch, put on a new one as soon as you remember, after removing the old patch if it's still in place. Do not apply more than one patch at a time.
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Lifestyle & Tips

  • Apply the patch to a clean, dry area of your lower abdomen or buttock. Avoid areas with cuts, rashes, or irritation.
  • Rotate the application site each week to prevent skin irritation.
  • Do not apply the patch to your breasts or waistline.
  • Avoid exposing the patch to direct sunlight or heat for prolonged periods.
  • If a patch falls off, try to reapply it. If it doesn't stick, apply a new patch and continue your regular schedule.
  • Discuss any concerns about diet, exercise, or smoking with your doctor, as these can impact your health while on HRT.
  • Attend all scheduled doctor appointments and screenings (e.g., mammograms, Pap tests).

Dosing & Administration

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Adult Dosing

Standard Dose: Apply one Climara Pro 0.045 mg/day patch transdermally to the lower abdomen or buttock once weekly. Rotate application sites.
Dose Range: 0.045 - 0.045 mg

Condition-Specific Dosing:

postmenopausal_symptoms: For the treatment of moderate to severe vasomotor symptoms associated with menopause and prevention of postmenopausal osteoporosis.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended.
Moderate: No specific dose adjustment recommended.
Severe: Use with caution; monitor for adverse effects. Estrogens and progestins are primarily metabolized by the liver.
Dialysis: Not specifically studied; use with caution.

Hepatic Impairment:

Mild: Use with caution; monitor for adverse effects.
Moderate: Use with caution; monitor for adverse effects. Metabolism may be impaired.
Severe: Contraindicated in severe liver disease or liver tumors.

Pharmacology

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Mechanism of Action

Estradiol is an estrogen that replaces the declining endogenous estrogen levels in postmenopausal women, alleviating vasomotor symptoms and preventing bone loss. Levonorgestrel is a progestin that counteracts the estrogen-induced proliferation of the endometrium, thereby reducing the risk of endometrial hyperplasia and carcinoma associated with unopposed estrogen therapy.
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Pharmacokinetics

Absorption:

Bioavailability: High (transdermal bypasses first-pass metabolism)
Tmax: Estradiol: Approximately 1-2 days to reach steady state; Levonorgestrel: Approximately 1-2 days to reach steady state.
FoodEffect: Not applicable for transdermal patch.

Distribution:

Vd: Estradiol: Approximately 9-12 L/kg; Levonorgestrel: Approximately 1.8 L/kg
ProteinBinding: Estradiol: ~98% (primarily to sex hormone-binding globulin (SHBG) and albumin); Levonorgestrel: ~50-60% (primarily to SHBG and albumin)
CnssPenetration: Yes (estrogens and progestins cross the blood-brain barrier)

Elimination:

HalfLife: Estradiol: ~1 hour (systemic, but continuous release from patch); Levonorgestrel: ~24-48 hours
Clearance: Estradiol: High; Levonorgestrel: Moderate
ExcretionRoute: Urine (primarily as glucuronide and sulfate conjugates), Feces (minor)
Unchanged: Minimal
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Pharmacodynamics

OnsetOfAction: Within days to weeks for symptom relief.
PeakEffect: Steady-state concentrations achieved within 1-2 days of patch application.
DurationOfAction: 7 days (due to continuous release from the weekly patch).

Safety & Warnings

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BLACK BOX WARNING

Estrogens and progestins should not be used for the prevention of cardiovascular disease or dementia. The Women's Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 years of age) during 5.6 years of treatment with daily oral conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) relative to placebo. The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with daily oral conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) relative to placebo. These risks should be considered when prescribing Climara Pro.
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Side Effects

Serious Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades, yellow skin or eyes, fever with chills, bloating, or severe upset stomach or vomiting.
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
Breast-related symptoms: lump in the breast, breast pain or soreness, or nipple discharge.
Vaginal symptoms: itching or discharge, or abnormal vaginal bleeding.
Depression or other mood changes, or memory problems or loss.

Fluid Retention and Swelling

This medication may cause fluid retention or swelling in the body. Inform your doctor if you experience swelling, weight gain, or trouble breathing.

Blood Clots and High Calcium Levels

Seek medical help immediately if you experience signs of a blood clot, such as:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, changes in color, or pain in a leg or arm
Trouble speaking or swallowing

High calcium levels have been reported in some people with cancer taking this medication. Contact your doctor right away if you experience:
Weakness
Confusion
Feeling tired
Headache
Upset stomach or vomiting
Constipation
Bone pain

Other Side Effects

Most people do not experience serious side effects, but some may occur. If you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
Headache
Hair loss
Back pain
Upset stomach or vomiting
Cramps
Bloating
Tender breasts
Vaginal bleeding or spotting
Irritation at the site of administration
Signs of a common cold

Reporting Side Effects

This is not an exhaustive list of potential side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Sudden chest pain or shortness of breath (possible blood clot in lungs or heart attack)
  • Sudden severe headache, vision changes, or weakness/numbness on one side of the body (possible stroke)
  • Swelling, redness, or pain in your leg (possible deep vein thrombosis)
  • New breast lump or changes in your breasts
  • Unusual vaginal bleeding or spotting after menopause
  • Yellowing of your skin or eyes (jaundice)
  • Severe abdominal pain
  • Memory loss or confusion (especially if over 65)
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
A history of certain health conditions, such as:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Previous removal of the uterus (hysterectomy)
Pregnancy or suspected pregnancy. Do not take this medication if you are pregnant.

Additionally, provide your doctor and pharmacist with a comprehensive list of:

All prescription and over-the-counter medications you are taking
Natural products and vitamins you are using
Any existing health problems

This information is crucial to ensure your safety while taking this medication. Do not start, stop, or modify the dosage of any medication without consulting your doctor first. It is your responsibility to verify that it is safe to take this medication in combination with your other medications and health conditions.
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Precautions & Cautions

Important Warnings and Cautions

When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, about your treatment. Your doctor may advise you to stop taking this medication before certain surgical procedures, and will provide guidance on when to resume treatment after the surgery or procedure.

If you will be immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged inactivity may increase your risk of developing blood clots.

If you have diabetes, closely monitor your blood sugar levels, as this medication may affect them. Additionally, inform your doctor if you have a history of high triglyceride levels, as this medication may cause an increase in triglyceride levels.

Regularly undergo blood tests and bone density checks as directed by your doctor. This medication may also increase your blood pressure, so have your blood pressure checked regularly.

It is crucial to maintain regular breast exams and gynecology check-ups, and perform breast self-exams as instructed by your doctor. This medication may interfere with certain laboratory tests, so inform all your healthcare providers and lab personnel about your treatment.

To minimize the risk of heart disease, refrain from smoking, and limit your alcohol consumption. If you consume grapefruit juice or eat grapefruit regularly, consult your doctor. Protect the patch from sunlight to minimize the risk of side effects.

The risk of certain side effects, such as heart attack, stroke, breast cancer, ovarian cancer, and others, may vary depending on factors like the duration of estrogen treatment, whether it is taken with or without a progestin, and other individual factors. Discuss the benefits and risks of this medication with your doctor.

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.

Osteoporosis

To maximize the effectiveness of this medication, use it in conjunction with calcium and vitamin D supplements, and engage in weight-bearing exercises like walking or physical therapy. Adhere to the diet and exercise plan recommended by your doctor.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Breast tenderness
  • Abdominal pain
  • Drowsiness/fatigue
  • Withdrawal bleeding (in females)

What to Do:

Remove the patch immediately. Seek medical attention or call a poison control center. Call 1-800-222-1222.

Drug Interactions

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Contraindicated Interactions

  • Aromatase inhibitors (e.g., anastrozole, letrozole, exemestane) - concurrent use would counteract the effect of the aromatase inhibitor.
  • Drugs for which estrogen exposure is a contraindication (e.g., certain breast cancers, estrogen-dependent tumors).
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Major Interactions

  • CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital, phenytoin, St. John's Wort) - may decrease estrogen and progestin plasma concentrations, potentially reducing therapeutic effects and increasing risk of breakthrough bleeding.
  • CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin, grapefruit juice) - may increase estrogen and progestin plasma concentrations, potentially increasing adverse effects.
  • Thyroid hormone replacement therapy - estrogens can increase thyroid-binding globulin (TBG), leading to increased circulating TBG and decreased free thyroid hormone. Patients on thyroid hormone replacement may require increased doses of thyroid hormone.
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Moderate Interactions

  • Corticosteroids - estrogens may decrease the clearance of corticosteroids, leading to increased corticosteroid effects.
  • Oral anticoagulants (e.g., warfarin) - estrogens may affect coagulation parameters; close monitoring of INR is recommended.
  • Lamotrigine - estrogens may decrease lamotrigine plasma concentrations, potentially leading to loss of seizure control.
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Minor Interactions

  • Folic acid - may enhance estrogen metabolism.
  • Vitamin C - may inhibit estrogen metabolism.

Monitoring

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Baseline Monitoring

Complete medical history and physical examination

Rationale: To identify contraindications, risk factors for cardiovascular disease, breast cancer, and other conditions.

Timing: Prior to initiation of therapy.

Blood pressure

Rationale: To establish baseline and monitor for hypertension.

Timing: Prior to initiation of therapy.

Breast examination and mammography

Rationale: To screen for breast cancer.

Timing: Prior to initiation of therapy and as clinically indicated.

Pelvic examination and Pap test

Rationale: To screen for gynecological conditions and cervical cancer.

Timing: Prior to initiation of therapy and as clinically indicated.

Lipid profile (cholesterol, triglycerides)

Rationale: To assess cardiovascular risk factors.

Timing: Prior to initiation of therapy, if indicated.

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Routine Monitoring

Annual physical examination

Frequency: Annually

Target: N/A

Action Threshold: N/A

Blood pressure

Frequency: Annually or more frequently if indicated

Target: <130/80 mmHg (general guideline)

Action Threshold: Sustained elevation requiring intervention.

Breast examination and mammography

Frequency: Annually (breast exam), biennially or as per guidelines (mammography)

Target: N/A

Action Threshold: New lumps, pain, or suspicious findings requiring further investigation.

Pelvic examination and Pap test

Frequency: As per current screening guidelines (e.g., every 3-5 years for Pap test)

Target: N/A

Action Threshold: Abnormal findings requiring further investigation.

Symptoms of VTE, stroke, MI, breast cancer, endometrial cancer

Frequency: Ongoing patient education and self-monitoring

Target: Absence of symptoms

Action Threshold: Immediate medical attention for new or worsening symptoms (e.g., chest pain, shortness of breath, leg swelling, abnormal vaginal bleeding, breast lump).

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Symptom Monitoring

  • Unusual vaginal bleeding or spotting
  • Breast lumps or changes
  • Chest pain or discomfort
  • Shortness of breath
  • Sudden severe headache
  • Sudden vision changes
  • Weakness or numbness in an arm or leg
  • Speech difficulties
  • Swelling, redness, or pain in a leg (especially calf)
  • Yellowing of skin or eyes (jaundice)
  • Severe abdominal pain

Special Patient Groups

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Pregnancy

Climara Pro is contraindicated during pregnancy. There is no indication for use in pregnancy, and there is evidence of fetal harm.

Trimester-Specific Risks:

First Trimester: Potential for adverse effects on fetal development, including genital abnormalities.
Second Trimester: Potential for adverse effects on fetal development.
Third Trimester: Potential for adverse effects on fetal development.
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Lactation

Climara Pro is contraindicated during lactation. Estrogens and progestins are excreted in breast milk and may reduce the quantity and quality of breast milk. Potential adverse effects on the breastfed infant are also a concern.

Infant Risk: High (potential for adverse effects on infant, reduction in milk supply).
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Pediatric Use

Climara Pro is not indicated for use in pediatric patients. Safety and efficacy have not been established in this population.

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Geriatric Use

Use with caution in women 65 years of age or older. The WHIMS study showed an increased risk of probable dementia in women 65 years of age or older receiving combined estrogen plus progestin therapy. Increased risk of stroke and VTE has also been observed in this age group. Individualize therapy and consider alternative non-hormonal treatments.

Clinical Information

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Clinical Pearls

  • Climara Pro is a continuous combined HRT, meaning both estrogen and progestin are delivered continuously, which typically results in amenorrhea (no monthly bleeding) in most women after several months of use.
  • It is crucial to adhere to the weekly application schedule and rotate patch sites to maintain consistent hormone levels and minimize skin irritation.
  • Patients should be thoroughly counseled on the Black Box Warnings regarding cardiovascular events, breast cancer, and dementia, and the decision to use HRT should be individualized based on symptoms, risk factors, and patient preference.
  • Regular follow-up appointments, including physical exams and screenings (mammograms, Pap tests), are essential to monitor for potential adverse effects.
  • Transdermal delivery bypasses first-pass hepatic metabolism, which may be advantageous for some patients compared to oral HRT, potentially leading to a more favorable lipid profile and less impact on clotting factors, though cardiovascular risks still exist.
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Alternative Therapies

  • Estrogen-only therapy (for women without a uterus, or with progestin separately)
  • Selective Estrogen Receptor Modulators (SERMs) (e.g., bazedoxifene/conjugated estrogens, ospemifene, tamoxifen, raloxifene)
  • Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
  • Lifestyle modifications (e.g., diet, exercise, stress reduction, avoiding triggers for hot flashes)
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Cost & Coverage

Average Cost: $150 - $300 per 4 patches (1 month supply)
Generic Available: Yes
Insurance Coverage: Tier 2 or 3 (Brand-name), Tier 1 (Generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.