Drug: Climara

Climara®, estradiol transdermal system, is designed to release estradiol continuously upon application to intact skin. Six (6.5, 9.375, 12.5, 15, 18.75 and 25 cm²) systems are available to provide nominal in vivo delivery of 0.025, 0.0375, 0.05, 0.06, 0.075 or 0.1 mg respectively of estradiol per day. The period of use is 7 days. Each system has a contact surface area of either 6.5, 9.375, 12.5, 15, 18.75 or 25 cm², and contains 2, 2.85, 3.8, 4.55, 5.7 or 7.6 mg of estradiol USP respectively. The composition of the systems per unit area is identical. Estradiol USP is a white, crystalline powder, chemically described as estra-1,3,5(10)-triene-3, 17β-diol. It has an empirical formula of C18H24O2 and molecular weight of 272.39. The structural formula is: The Climara (estradiol transdermal) system comprises three layers. Proceeding from the visible surface toward the surface attached to the skin, these layers are (1) a translucent polyethylene film, and (2) an acrylate adhesive matrix containing estradiol USP. A protective liner (3) of siliconized or fluoropolymer-coated polyester film is attached to the adhesive surface and must be removed before the system can be used. The active component of the system is estradiol. The remaining components of the system (acrylate copolymer adhesive, fatty acid esters, and polyethylene backing) are pharmacologically inactive.

Source: http://www.rxlist.com

See BOXED WARNINGS, WARNINGS and PRECAUTIONS. Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The adverse reaction information from clinical trials does, however, provide a basis for identifying the adverse events that appear to be related to drug use and for approximating rates. Summary of Most Frequently Reported Adverse Experiences/Medical Events ( ≥ 5%) by Treatment Groups
AE per Body System Climara Placebo
(N=72) 0.025 mg/day
(N=219) 0.05 mg/day
(N=201) 0.1 mg/day
(N=194) Body as a Whole 21% 39% 37% 29%   Headache 5% 18% 13% 10%   Pain 1% 8% 11% 7%   Back Pain 4% 8% 9% 6%   Edema 0.5% 13% 10% 6% Gastro-Intestinal 9% 21% 29% 18%   Abdominal Pain 0% 11% 16% 8%   Nausea 1% 5% 6% 3%   Flatulence 1% 3% 7% 1% Musculo-Skeletal 7% 9% 11% 4%   Arthralgia 1% 5% 5% 3% Psychiatric 13% 10% 11% 1%   Depression 1% 5% 8% 0% Reproductive 12% 18% 41% 11%   Breast Pain 5% 8% 29% 4%   Leukorrhea 1% 6% 7% 1% Respiratory 15% 26% 29% 14%   URTI 6% 17% 17% 8%   Pharyngitis 0.5% 3% 7% 3%   Sinusitis 4% 4% 5% 3%   Rhinitis 2% 4% 6% 1% Skin and Appendages 19% 12% 12% 15%   Pruritus 0.5% 6% 3% 6% Postmarketing Experience The following adverse reactions have been identified during post approval use of Climara (estradiol transdermal) : a few cases in which there were a combination of the symptoms of generalized hives or rash with swelling of the throat or eyelid edema. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. The following additional adverse reactions have been reported with estrogen and/or progestin therapy.
  1. Genitourinary system
    Changes in vaginal bleeding pattern and abnormal withdrawal bleeding or flow; breakthrough bleeding; spotting; dysmenorrhea; increase in size of uterine leiomyomata; vaginitis, including vaginal candidiasis; change in amount of cervical secretion; changes in cervical ectropion; ovarian cancer; endometrial hyperplasia; endometrial cancer.
  2. Breasts
    Tenderness, enlargement, pain, nipple discharge, galactorrhea; fibrocystic breast changes; breast cancer.
  3. Cardiovascular
    Deep and superficial venous thrombosis; pulmonary embolism; thrombophlebitis; myocardial infarction; stroke; increase in blood pressure.
  4. Gastrointestinal
    Nausea, vomiting; abdominal cramps, bloating; cholestatic jaundice; increased incidence of gall bladder disease; pancreatitis; enlargement of hepatic hemangiomas.
  5. Skin
    Chloasma or melasma, which may persist when drug is discontinued; erythema multiforme; erythema nodosum; hemorrhagic eruption; loss of scalp hair; hirsutism; pruritus, rash.
  6. Eyes
    Retinal vascular thrombosis, intolerance to contact lenses.
  7. Central nervous system
    Headache; migraine; dizziness; mental depression; chorea; nervousness; mood disturbances; irritability; exacerbation of epilepsy, dementia.
  8. Miscellaneous
    Increase or decrease in weight; reduced carbohydrate tolerance; aggravation of porphyria; edema; arthalgias; leg cramps; changes in libido; anaphylactoid/anaphylactic reactions; hypocalcemia; exacerbation of asthma; increased triglycerides.
Read the Climara (estradiol transdermal) Side Effects Center for a complete guide to possible side effectsLearn More »

Source: http://www.rxlist.com

When estrogen is prescribed for a postmenopausal woman with a uterus, progestin should also be initiated to reduce the risk of endometrial cancer. A woman without a uterus does not need progestin. Use of estrogen, alone or in combination with a progestin, should be with the lowest effective dose and for the shortest duration consistent with treatment goals and risks for the individual woman. Patients should be reevaluated periodically as clinically appropriate (e.g., 3-month to 6-month intervals) to determine if treatment is still necessary (See BOXED WARNINGS and WARNINGS.) For women who have a uterus, adequate diagnostic measures, such as endometrial sampling, when indicated, should be undertaken to rule out malignancy in cases of undiagnosed persistent or recurring abnormal vaginal bleeding. Patients should be started at the lowest dose. Six (6.5, 9.375, 12.5, 15, 18.75 and 25 cm²) Climara (estradiol transdermal) systems are available. For the treatment of vasomotor symptoms, treatment should be initiated with the 6.5 cm² (0.025 mg/day) Climara (estradiol transdermal) system applied to the skin once weekly. The dose should be adjusted as necessary to control symptoms. Clinical responses (relief of symptoms) at the lowest effective dose should be the guide for establishing administration of the Climara (estradiol transdermal) system, especially in women with an intact uterus. Attempts to taper or discontinue the medication should be made at 3- to 6-month intervals. In women who are not currently taking oral estrogens, treatment with the Climara (estradiol transdermal) system can be initiated at once. In women who are currently taking oral estrogen, treatment with the Climara (estradiol transdermal) system can be initiated 1-week after withdrawal of oral therapy or sooner if symptoms reappear in less than 1-week. For the prevention of postmenopausal osteoporosis, the minimum dose that has been shown to be effective is the 6.5 cm² (0.025 mg/day) Climara (estradiol transdermal) system. Response to therapy can be assessed by biochemical markers and measurement of bone mineral density. Application of the System The adhesive side of the Climara (estradiol transdermal) system should be placed on a clean, dry area of the lower abdomen or the upper quadrant of the buttock. The Climara (estradiol transdermal) system should not be applied to or near the breasts. The sites of application must be rotated, with an interval of at least 1-week allowed between applications to a particular site. The area selected should not be oily, damaged, or irritated. The waistline should be avoided, since tight clothing may rub and remove the system. Application to areas where sitting would dislodge the system should also be avoided. The system should be applied immediately after opening the pouch and removing the protective liner. The system should be pressed firmly in place with the fingers for about 10 seconds, making sure there is good contact, especially around the edges. If the system lifts, apply pressure to maintain adhesion. In the event that a system should fall off, a new system should be applied for the remainder of the 7-day dosing interval. Only one system should be worn at any one time during the 7-day dosing interval. Swimming, bathing, or using a sauna while using the Climara (estradiol transdermal) system has not been studied, and these activities may decrease the adhesion of the system and the delivery of estradiol. Removal of the System Removal of the system should be done carefully and slowly to avoid irritation of the skin. Should any adhesive remain on the skin after removal of the system, allow the area to dry for 15 minutes. Then gently rubbing the area with an oil-based cream or lotion should remove the adhesive residue. Used patches still contain some active hormones. Each patch should be carefully folded in half so that it sticks to itself before throwing it away.

Source: http://www.rxlist.com

Drug/Laboratory Test Interactions
  1. Accelerated prothrombin time, partial thromboplastin time, and platelet aggregation time; increased platelet count; increased factors II, VII antigen, VIII antigen, VIII coagulant activity, IX, X, XII, VII-X complex, II-VII-X complex, and beta-thromboglobulin; decreased levels of antifactor Xa and antithrombin III, decreased antithrombin III activity; increased levels of fibrinogen and fibrinogen activity; increased plasminogen antigen and activity.
  2. Increased thyroid-binding globulin (TBG) levels leading to increased circulating total thyroid hormone levels as measured by protein-bound iodine (PBI), T4 levels (by column or by radioimmunoassay) or T3 levels by radioimmunoassay. T3 resin uptake is decreased, reflecting the elevated TBG. Free T4 and free T3 concentrations are unaltered. Patients on thyroid replacement therapy may require higher doses of thyroid hormone.
  3. Other binding proteins may be elevated in serum (i.e., corticosteroid binding globulin (CBG), sex hormone-binding globulin (SHBG)) leading to increased total circulating corticosteroids and sex steroids, respectively. Free hormone concentrations may be decreased. Other plasma proteins may be increased (angiotensinogen/renin substrate, alpha-l-antitrypsin, ceruloplasmin).
  4. Increased plasma HDL and HDL2 cholesterol subfraction concentrations, reduced LDL cholesterol concentration, and in oral formulations increased triglyceride levels.
  5. Impaired glucose tolerance.
  6. Reduced response to metyrapone test.
Last reviewed on RxList: 10/2/2008
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

Climara (estradiol transdermal) is indicated in the:
  1. Treatment of moderate to severe vasomotor symptoms associated with the menopause.
  2. Treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with the menopause. When prescribing solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.
  3. Treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure.
  4. Prevention of postmenopausal osteoporosis. When prescribing solely for the prevention of postmenopausal osteoporosis, therapy should only be considered for women at significant risk of osteoporosis and non-estrogen medications should be carefully considered.
The mainstays for decreasing the risk of postmenopausal osteoporosis are weight bearing exercise, adequate calcium and vitamin D intake, and when indicated, pharmacologic therapy. Postmenopausal women require an average of 1500mg/day of elemental calcium. Therefore, when not contraindicated, calcium supplementation may be helpful for women with suboptimal dietary intake. Vitamin D supplementation of 400-800 IU/day may also be required to ensure adequate daily intake in postmenopausal women.

Source: http://www.rxlist.com

Climara (estradiol transdermal) should not be used in women with any of the following conditions:
  1. Undiagnosed abnormal genital bleeding.
  2. Known, suspected, or history of cancer of the breast.
  3. Known or suspected estrogen-dependent neoplasia.
  4. Active deep vein thrombosis, pulmonary embolism or a history of these conditions.
  5. Active or recent (e.g. within the past year) arterial thromboembolic disease (e.g., stroke, myocardial infarction).
  6. Liver dysfunction or disease.
  7. Climara (estradiol transdermal) should not be used in patients with known hypersensitivity to its ingredients.
  8. Known or suspected pregnancy. There is no indication for Climara (estradiol transdermal) in pregnancy. There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins from oral contraceptives inadvertently during early pregnancy (See PRECAUTIONS).
Last reviewed on RxList: 10/2/2008
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

Serious ill effects have not been reported following acute ingestion of large doses of estrogen-containing oral contraceptives by young children. Overdosage of estrogen may cause nausea and vomiting, and withdrawal bleeding may occur in females.

Source: http://www.rxlist.com

Climara (estradiol transdermal system), 0.025 mg/day — each 6.5 cm² system contains 2 mg of estradiol USP Individual Carton of 4 systems………………NDC 50419-454-04 Climara (estradiol transdermal system), 0.0375 mg/day — each 9.375 cm² system contains 2.85 mg of estradiol USP Individual Carton of 4 systems………………NDC 50419-456-04 Climara (estradiol transdermal system), 0.05 mg/day — each 12.5 cm² system contains 3.8 mg of estradiol USP Individual Carton of 4 systems………………NDC 50419-451-04 Climara (estradiol transdermal system), 0.06 mg/day — each 15 cm² system contains 4.55 mg of estradiol USP Individual Carton of 4 systems……………….NDC 50419-459-04 Climara (estradiol transdermal system), 0.075 mg/day — each 18.75 cm² system contains 5.7 mg of estradiol USP Individual Carton of 4 systems……………… NDC 50419-453-04 Climara (estradiol transdermal system), 0.1 mg/day — each 25 cm² system contains 7.6 mg of estradiol USP Individual Carton of 4 systems……………….NDC 50419-452-04 Do not store above 86°F (30°C). Do not store unpouched. Apply immediately upon removal from the protective pouch. Manufactured for: Bayer HealthCare Pharmaceuticals Inc. Wayne, NJ 07470. Manufactured by: 3M Drug Delivery Systems, Northridge, CA 93124. FDA revision date: 1/3/2008 Last reviewed on RxList: 10/2/2008
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

General
  1. Addition of a progestin when a woman has not had a hysterectomy.
    Studies of the addition of a progestin for 10 or more days of a cycle of estrogen administration, or daily with estrogen in a continuous regimen, have reported a lowered incidence of endometrial hyperplasia than would be induced by estrogen treatment alone. Endometrial hyperplasia may be a precursor to endometrial cancer. There are, however, possible risks that may be associated with the use of progestins with estrogens compared to estrogen-alone treatment. These include a possible increased risk of breast cancer.
  2. Elevated blood pressure
    In a small number of case reports, substantial increases in blood pressure have been attributed to idiosyncratic reactions to estrogens. In a large, randomized, placebo-controlled clinical trial, a generalized effect of estrogens on blood pressure was not seen. Blood pressure should be monitored at regular intervals with estrogen use.
  3. Hypertriglyceridemia
    In patients with pre-existing hypertriglyceridemia, estrogen therapy may be associated with elevations of plasma triglycerides leading to pancreatitis and other complications.
  4. Impaired liver function and past history of cholestatic jaundice
    Estrogens may be poorly metabolized in patients with impaired liver function. For patients with a history of cholestatic jaundice associated with past estrogen use or with pregnancy, caution should be exercised and in the case of recurrence, medication should be discontinued.
  5. Hypothyroidism
    Estrogen administration leads to increased thyroid-binding globulin (TBG) levels. Patients with normal thyroid function can compensate for the increased TBG by making more thyroid hormone, thus maintaining free T4 and T3 serum concentrations in the normal range. Patients dependent on thyroid hormone replacement therapy who are also receiving estrogens may require increased doses of their thyroid replacement therapy. These patients should have their thyroid function monitored in order to maintain their free thyroid hormone levels in an acceptable range.
  6. Fluid retention
    Because estrogens may cause some degree of fluid retention, patients with conditions that might be influenced by this factor, such as a cardiac or renal dysfunction, warrant careful observation when estrogens are prescribed.
  7. Hypocalcemia
    Estrogens should be used with caution in individuals with severe hypocalcemia.
  8. Ovarian cancer
    The CE/MPA sub-study of WHI reported that estrogen plus progestin increased the risk of ovarian cancer. After an average follow-up of 5.6 years, the relative risk for ovarian cancer for CE/MPA versus placebo was 1.58 (95% confidence interval 0.77-3.24) but was not statistically significant. The absolute risk for CE/MPA versus placebo was 4.2 versus 2.7 cases per 10,000 women-years. In some epidemiological studies, the use of estrogen alone, in particular for ten or more years, has been associated with an increased risk of ovarian cancer. Other epidemiologic studies have not found these associations.
  9. Exacerbation of endometriosis
    Endometriosis may be exacerbated with administration of estrogens. A few cases of malignant transformation of residual endometrial implants have been reported in women treated post-hysterectomy with estrogen alone therapy. For patients known to have residual endometriosis post-hysterectomy, the addition of progestin should be considered.
  10. Exacerbation of other conditions
    Estrogens may cause an exacerbation of asthma, diabetes mellitus, epilepsy, migraine or porphyria, systemic lupus erythematosus, and hepatic hemangiomas and should be used with caution in women with these conditions.
Patient information Physicians are advised to discuss the PATIENT INFORMATION leaflet with patients for whom they prescribe Climara (estradiol transdermal) . Laboratory Tests Estrogen administration should be initiated at the lowest dose approved for the indication and then guided by clinical response rather than by serum hormone levels (e.g. estradiol, FSH). Carcinogeneses, Mutagenesis, And Impairment Of Fertility Long-term continuous administration of estrogen, with and without progestin, in women with and without a uterus, has shown an increased risk of endometrial cancer, breast cancer, and ovarian cancer. (See BOXED WARNINGS, WARNINGS and PRECAUTIONS.) Long-term continuous administration of natural and synthetic estrogens in certain animal species increases the frequency of carcinomas of the breast, uterus, cervix, vagina, testis, and liver. Pregnancy Climara (estradiol transdermal) should not be used during pregnancy. (See CONTRAINDICATIONS.) Nursing Mothers Estrogen administration to nursing mothers has been shown to decrease the quantity and quality of the milk. Detectable amounts of estrogens have been identified in the milk of mothers receiving this drug. Caution should be exercised when Climara (estradiol transdermal) is administered to a nursing woman. Pediatric Use Estrogen replacement therapy has been used for the induction of puberty in adolescents with some forms of pubertal delay. Safety and effectiveness in pediatric patients have not otherwise been established. Large and repeated doses of estrogen over an extended time period have been shown to accelerate epiphyseal closure, which could result in short adult stature if treatment is initiated before the completion of physiologic puberty in normally developing children. If estrogen is administered to patients whose bone growth is not complete, periodic monitoring of bone maturation and effects on epiphyseal centers is recommended during estrogen administration. Estrogen treatment of prepubertal girls also induces premature breast development and vaginal cornification, and may induce vaginal bleeding. In boys, estrogen treatment may modify the normal pubertal process and induce gynecomastia. (See INDICATIONS and DOSAGE AND ADMINISTRATION.) Geriatric Use There have not been sufficient numbers of geriatric patients involved in clinical studies utilizing Climara (estradiol transdermal) to determine whether those over 65 years of age differ from younger subjects in their response to Climara (estradiol transdermal) . In the Women's Health Initiative Memory Study, including 4,532 women 65 years of age and older, followed for an average of 4 years, 82% (n=3,729) were 65 to 74 while 18% (n=803) were 75 and over. Most women (80%) had no prior hormone therapy use. Women treated with conjugated estrogens plus medroxyprogesterone acetate were reported to have a two-fold increase in the risk of developing probable dementia. Alzheimer's disease was the most common classification of probable dementia in both the conjugated estrogens plus medroxyprogesterone acetate group and the placebo group. Ninety percent of the cases of probable dementia occurred in the 54% of women that were older than 70. (See BOXED WARNING and WARNINGS, Dementia.)Last reviewed on RxList: 10/2/2008
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

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