Drug: Angeliq

ANGELIQ (drospirenone and estradiol) TABLETS provide a hormone regimen consisting of film coated tablets each containing 0.5 mg of drospirenone and 1 mg of estradiol. The inactive ingredients are lactose monohydrate NF, corn starch NF, modified starch NF, povidone 25000 USP, magnesium stearate NF, hydroxylpropylmethyl cellulose USP, macrogol 6000 NF, talc USP, titanium dioxide USP, and ferric oxide pigment NF. Drospirenone, (6R,7R,8R,9S,10R,13S,14S,15S,16S,17S) -1,3´, 4´,6,6a,7,8,9,10,11,12,13,14,15,15a,16-hexadecahydro-10,13- dimethylspiro-[17H-dicyclopropa[6,7:15,16]cyclopenta [a]phenanthrene-17,2´(5H)-furan]-3,5´(2H)-dione (CAS) is a synthetic progestational compound and has a molecular weight of 366.5 and a molecular formula of C24H30O3. Estradiol USP, (Estra–1,3,5(10)–triene–3,17–diol,17β), has a molecular weight of 272.39 and the molecular formula is C18H24O2. The structural formulas are as follows:

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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. The following are adverse events reported with ANGELIQ (drospirenone and estradiol) occurring in > 5% of subjects: Table 4: Adverse Events Regardless of Drug Relationship Reported at a Frequency of > 5% in a 1-year Double-blind Clinical Trial
ADVERSE EVENT E2 1 MG
(N=226)
n (%) ANGELIQ (drospirenone and estradiol)
(N=227)
n (%) BODY AS A WHOLE    Abdominal pain 29 (12.8) 25 (11)    Pain in extremity 15 (6.6) 19 8 ( .4)    Back pain 11 (4.9) 16 (7)    Flu syndrome 15 (6.6) 16 (7)    Accidental injury 15 (6.6) 13 (5 .7)    Abdomen enlarged 17 (7.5) 16 (7)    Surgery 6 (2.7) 12 (5.3) METABOLIC & NUTRITIONAL DISORDERS    Peripheral edema 12 (5.3) 4 (1 .8) NERVOUS SYSTEM    Headache 26 (11.5) 22 (9.7) RESPIR ATORY SYSTEM    Upper respiratory infection 40 (17.7) 43 (18.9)    Sinusitis 8 (3.5) 12 (5.3) SKIN AND APPENDAGES    Breast pain 34 (15) 43 (18.9) UROGENITAL    Vaginal hemorrhage 43 (19) 21 (9.3 )    Endometrial disorder 22 (9.7) 4 (1.8)    Leukorrhea 14 (6.2) 3 (1.3) The following additional adverse reactions have been reported with estrogen and or estrogen/progestin therapy: 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. Breasts Tenderness, enlargement, pain, nipple discharge, galactorrhea, fibrocystic breast changes, breast cancer. Cardiovascular Deep and superficial venous thrombosis, pulmonary embolism, thrombophlebitis, myocardial infarction, stroke, increase in blood pressure. Gastrointestinal Nausea, vomiting, abdominal cramps, bloating, cholestatic jaundice, increased incidence of gall bladder disease, pancreatitis, enlargement of hepatic hemangiomas. Skin Chloasma or melasma, which may persist when drug is discontinued, erythema multiforme, erythema nodosum, hemorrhagic eruption, loss of scalp hair, hirsutism, pruritus, rash. Eyes Retinal vascular thrombosis, intolerance to contact lenses. Central nervous system Headache, migraine, dizziness, mental depression, chorea, nervousness, mood disturbances, irritability, exacerbation of epilepsy, dementia. Miscellaneous Increase or decrease in weight, reduced carbohydrate tolerance, aggravation of porphyria, edema, arthralgias, leg cramps, changes in libido, anaphylactoid/anaphylactic reactions including urticaria and angioedema, hypocalcemia, exacerbation of asthma, increased triglycerides. Read the Angeliq (drospirenone and estradiol) Side Effects Center for a complete guide to possible side effectsLearn More »

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The dosage of ANGELIQ (drospirenone and estradiol) is one tablet daily. Women who are already using a product containing estrogen should stop taking that product before starting ANGELIQ (drospirenone and estradiol) . Use of estrogen, alone or in combination with a progestin, should be limited to the lowest effective dose available 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 sections). 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. The lowest effective dose of ANGELIQ (drospirenone and estradiol) has not been determined.

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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 anti-factor 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, as measured by proteinbound iodine (PBI), T4 levels (by column or by radio immunoassay) or T3 levels by radio immunoassay. 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 circulating corticosteroids and sex steroids, respectively. Free hormone concentrations may be decreased. Other plasma proteins may be increased (angiotensinogen/ renin substrate, alpha-1-antitrypsin, ceruloplasmin).
  4. Increased plasma HDL and HDL-2 subfraction concentrations, reduced LDL cholesterol concentration, increased triglyceride levels.
  5. Impaired glucose tolerance.
  6. Reduced response to metyrapone test.
Read the Angeliq Drug Interactions Center for a complete guide to possible interactions Learn More »

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ANGELIQ (drospirenone and estradiol) is indicated in women who have a uterus for 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.

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Progestogens/estrogens should not be used in individuals 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 history of these conditions.
  5. Active or recent (e.g., within the past year) arterial thromboembolic disease (e.g., stroke, myocardial infarction).
  6. Renal insufficiency.
  7. Liver dysfunction or disease.
  8. Adrenal insufficiency.
  9. ANGELIQ (drospirenone and estradiol) should not be used in patients with known hypersensitivity to its ingredients.
  10. Known or suspected pregnancy. There is no indication for ANGELIQ (drospirenone and estradiol) 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: 1/16/2009
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

In cases of ANGELIQ (drospirenone and estradiol) overdose, monitor serum concentrations of potassium and sodium since drospirenone has antimineralocorticoid properties. Serious ill effects have not been reported following acute ingestion of large doses of progestin/estrogen-containing oral contraceptives by young children. Overdosage may cause nausea and withdrawal bleeding may occur in females.

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ANGELIQ TABLETS (drospirenone and estradiol) 0.5 mg/1 mg are available as round, biconvex pink film-coated tablets embossed with “CK” inside a hexagon, and supplied in the following packaging: 3 blisters of 28 tablets NDC 50419-483-03 Storage Conditions Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [See USP Controlled Room Temperature]. Manufactured for: Bayer HealthCare Pharmaceuticals Inc., Wayne, NJ 07470. Manufactured in Germany. FDA revision date: 9/28/2005 Last reviewed on RxList: 1/16/2009
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

General 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 regimens. These include a possible increased risk of breast cancer. 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 estrogen therapy on blood pressure was not seen. Blood pressure should be monitored at regular intervals with estrogen use. Hypertriglyceridemia In patients with pre-existing hypertriglyceridemia, estrogen therapy may be associated with elevations of plasma triglycerides leading to pancreatitis and other complications. 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. The clearance of drospirenone was decreased in patients with moderate hepatic impairment. 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. Fluid retention Because estrogen and estrogen/progestin therapy 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. Hypocalcemia Estrogens should be used with caution in individuals with severe hypocalcemia. Hyponatremia As an aldosterone antagonist, drospirenone may increase the possibility of hyponatremia in high-risk patients. Ovarian cancer The CE/MPA substudy 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 epidemiologic 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. Exacerbation of endometriosis Endometriosismay be exacerbated with administration of estrogens. Exacerbation of other conditions Estrogens may cause an exacerbation of asthma, diabetes mellitus, epilepsy, migraine, 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 ANGELIQ (drospirenone and estradiol) . Laboratory Tests Estrogen administration should be initiated at the lowest dose for the approved indication and then guided by clinical response, rather than by serum hormone levels (e.g., estradiol, FSH). Carcinogenesis, 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. (See BOXED WARNINGS, CONTRAINDICATIONS, and WARNINGS sections.) In a 24 month oral carcinogenicity study in mice dosed with 10 mg/kg/day drospirenone alone or 1 + 0.01, 3 + 0.03 and 10 + 0.1 mg/kg/day of drospirenone and ethinyl estradiol, 0.24 to 10.3 times the exposure (AUC of drospirenone) of women taking a 1 mg dose, there was an increase in carcinomas of the harderian gland in the group that received the high dose of drospirenone alone. In a similar study in rats given 10 mg/kg/day drospirenone alone or 0.3 + 0.003, 3 + 0.03 and 10 + 0.1 mg/kg/day drospirenone and ethinyl estradiol, 2.3 to 51.2 times the exposure of women taking a 1 mg dose, there was an increased incidence of benign and total (benign and malignant) adrenal gland pheochromocytomas in the group receiving the high dose of drospirenone. Drospirenone was not mutagenic in a number of in vitro(Ames, Chinese Hamster Lung gene mutation and chromosomal damage in human lymphocytes) and in vivo (mouse micronucleus) genotoxicity tests. Drospirenone increased unscheduled DNA synthesis in rat hepatocytes and formed adducts with rodent liver DNA but not with human liver DNA. (See WARNINGS section.) Pregnancy ANGELIQ 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 ANGELIQ (drospirenone and estradiol) is administered to a nursing woman. After administration of an oral contraceptive containing drospirenone about 0.02% of the drospirenone dose was excreted into the breast milk of postpartum women within 24 hours. This results in a maximal daily dose of about 3 mcg drospirenone in an infant. Pediatric Use ANGELIQ (drospirenone and estradiol) is not indicated in children. Geriatric Use There have not been sufficient numbers of geriatric patients involved in clinical studies utilizing ANGELIQ (drospirenone and estradiol) to determine whether those over 65 years of age differ from younger subjects in their response to ANGELIQ (drospirenone and estradiol) . 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 who were older than 70. (See WARNINGS, Dementia.) Last reviewed on RxList: 1/16/2009
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

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