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Common name
Climara-50 (Estradiol)
Synonyms: Evalon, Prognova, Progynova, Aerodiol, Agofollin, Alora, Altrad, Amnestrogen, Aquadiol, Bardiol, Climaderm, Climara, Combipatch, Compudose, Corpagen, Delestrogen, Dermestril, Dihydrofollicular Hormone, Dihydrofolliculin, Estinyl, Dihydromenformon, Dihydr
Description
Climara, estradiol transdermal system, is designed to provide nominal in vivo delivery of 14 mcg 17b-estradiol per day continuously upon application to intact skin. The period of use is 7 days. The transdermal system has a contact surface area of 3.25 cm2, and contains 1.0 mg of estradiol USP. Estradiol USP (17b-estradiol) is a white, crystalline powder, chemically described as estra-1,3,5(10)-triene-3, 17b-diol. It has an empirical formula of C18 H24 O2 and molecular weight of 272.39
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Active Ingredients:
Estradiol
Therapeutic actions:
The Climara transdermal system provides systemic estrogen therapy by releasing 17b-estradiol, the major estrogenic hormone secreted by the human ovary. Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics.
Although circulating estrogens exist in a dynamic equilibrium of metabolic interconversions, estradiol is the principal intracellular human estrogen and is substantially more potent than its metabolites, estrone and estriol, at the receptor level. The primary source of estrogen in normally cycling adult women is the ovarian follicle, which secretes 70 to 500 mcg of estradiol daily, depending on the phase of the menstrual cycle. After menopause, most endogenous estrogen is produced by conversion of androstenedione, secreted by the adrenal cortex, to estrone by peripheral tissues.
Thus, estrone and the sulfate conjugated form, estrone sulfate, are the most abundant circulating estrogens in postmenopausal women. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues.
To date, two estrogen receptors have been identified. These vary in proportion from tissue to tissue. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.
The decline of ovarian estrogen production that accompanies menopause or oophorectomy results in the acceleration of bone loss and bone resorption. Bone resorption is increased more than bone formation especially in the early years of menopause where bone loss is the greatest.
In some women, these changes will eventually lead to decreased bone mass, osteoporosis and increased risk for fractures, particularly that of the spine, hip, and wrist. Vertebral fractures are the most common type of osteoporotic fracture in postmenopausal women. Postmenopausal women with low serum estradiol concentrations and high serum concentrations of sex hormone binding globulin (SHBG) have an increased risk of hip and vertebral fractures.
Postmenopausal estrogen therapy decreases bone resorption, helping to reestablish balance between resorption and formation. This effect appears to be effective for as long as treatment is continued.
What is it used for?:
(Indications:)
Climara is indicated for the 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 1500 mg/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. Risk factors for osteoporosis include low bone mineral density, low estrogen levels, family history of osteoporosis, previous fracture, small frame (low BMI), light skin color, smoking, and alcohol intake. Response to therapy can be predicted by pre-treatment serum estradiol (see Table 3), and can be assessed during treatment by measuring biochemical markers of bone formation/resorption, and/or bone mineral density.
Contraindications and cautions:
Do not use estradiol transdermal if you have:
• a bleeding or blood-clotting disorder;
• a history of stroke or circulation problems;
• abnormal vaginal bleeding that a doctor has not checked; or
• any type of breast, uterine, or hormone-dependent cancer.
Before using estradiol transdermal, tell your doctor if you have:
• high blood pressure, angina, or heart disease; high Cholesterol or triglycerides;
• liver disease;
• kidney disease;
• asthma;
• epilepsy or other seizure disorder;
• migraines;
• diabetes;
• depression;
• gallbladder disease; or
• if you have had your uterus removed (hysterectomy).
If you have any of these conditions, you may not be able to use estradiol transdermal, or you may need a dosage adjustment or special tests during treatment. Estradiol increases your risk of developing endometrial hyperplasia, a condition that may lead to cancer of the uterus. Taking progestins while using estradiol may lower this risk. If your uterus has not been removed, your doctor may prescribe a progestin for you to take while you are using estradiol transdermal. Long-term estradiol treatment may increase your risk of stroke. Talk with your doctor about your individual risks before using estradiol long-term. Your doctor should check your progress on a regular basis (every 3 to 6 months) to determine whether you should continue this treatment. FDA pregnancy category X. This medication can cause birth defects. Do not use estradiol transdermal if you are pregnant. Tell your doctor right away if you become pregnant during treatment. Use an effective form of birth control while you are using this medication. Estradiol can pass into breast milk and may harm a nursing baby. This medication may also slow breast milk production. Do not use if you are breast-feeding a baby.
Side effects:
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.
Body as a Whole
Abdominal Pain
Accidental Injury
Infection
Pain
Cardiovascular
Digestive System
Constipation
Dyspepsia
Metabolic and Nutritional
Disorders
Musculoskeletal System
Arthralgia
Arthritis
Myalgia
Nervous System
Dizziness
Respiratory System
Bronchitis
Upper Respiratory
Infection
Skin and Appendages
Application Site Reaction
Breast Pain
Urogenital System
Cervical polyps
Leukorrhea
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 gallbladder 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 including urticaria and angioedema; hypocalcemia; exacerbation of asthma; increased triglycerides.
Interactions:
It is important to tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start treatment with this medicine. Similarly, check with your doctor or pharmacist before taking any new medicines while taking this one, to ensure that the combination is safe.
Before using estradiol transdermal, tell your doctor if you are using any of the following drugs:
• St. Johnis wort;
• phenobarbital (Luminal, Solfoton);
• a blood thinner such as warfarin (Coumadin);
• ritonavir (Norvir);
• carbamazepine (Carbatrol, Tegretol);
• rifampin (Rifadin, Rifater, Rifamate, Rimactane); or
• antibiotics such as clarithromycin (Biaxin), erythromycin (E-Mycin, E.E.S., Erythrocin, Ery-Tab), ketoconazole (Nizoral), or itraconazole (Sporanox); If you are using any of these drugs, you may not be able to use estradiol transdermal or you may need dosage adjustments or special tests during treatment.
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