Adult Dosing

Moderate to severe vasomotor symptoms of menopause

• 1 tab PO qd. Reevaluate periodically
• Note: Use lowest possible estrogen dose to control symptoms and discontinue medication as soon as possible

Moderate to severe symptoms of vulvar and vaginal atrophy associated with menopause

• 1 tab PO qd. Reevaluate periodically
• Note: Use lowest possible estrogen dose to control symptoms and discontinue medication as soon as possible

Pediatric Dosing

• Safety and effectiveness in pediatric patients have not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

• Moderate to severe vasomotor symptoms of menopause
• Moderate to severe symptoms of vulvar and vaginal atrophy associated with menopause

• Hypersensitivity to any of the components of this preparation
• Undiagnosed abnormal genital bleeding
• Known, suspected, or history of breast CA
• Known or suspected estrogen-dependent neoplasia
• Active deep vein thrombosis, pulmonary embolism or history of these conditions
• Active or recent arterial thromboembolic disease
• Renal insufficiency
• Liver dysfunction or disease
• Adrenal insufficiency
• Known or suspected pregnancy
• Hyperkalemia
• Hysterectomy

• Do not use estrogens with or without progestins to prevent cardiovascular disease or dementia
• Women's Health Initiative (WHI) reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 yrs) during 5 yrs of treatment with daily oral conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (MPA 2.5 mg) relative to placebo
• The Women's Health Initiative Memory Study (WHIMS), a substudy of WHI, reported an increased risk of developing probable dementia in postmenopausal women 65 yrs of age or older during four years of treatment with oral conjugated estrogens combined with medroxyprogresterone acetate, relative to placebo; unknown whether this finding applies to younger postmenopausal women
• In the absence of comparable data, these risks should be assumed to be similar for other oral doses of conjugated estrogens and medroxyprogesterone and other combinations and dosage forms of estrogens and progestins
• Due to these risks, estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals for the individual woman

Renal Dose Adjustment

• Renal impairment: Contraindicated

Hepatic Dose Adjustment

• Hepatic impairment: Contraindicated

See Supplemental Patient Information

• Use for shortest duration and lowest dose consistent with treatment goals and risks [US Black Box Warning]
• Do not use estrogens with or without progestins to prevent cardiovascular disease or dementia [US Black Box Warning]
• Increased risk of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 yrs of age) during five years of treatment with oral conjugated equine estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) relative to placebo [US Black Box Warning]
• Risk of brest CA may occour with the use of estrogens and progestins by postmenopausal women
• Discontinue therapy if visual disturbances or jaundice occurs and during immobilization, or at least 2 weeks before surgery associated with thromboembolism
• Manage risk factors for cardiovascular disease and venous thromboembolism appropriately
• May aggravate asthma, diabetes, epilepsy, migraine, porphyria, SLE, hepatic hemangiomas

Cautions: Use cautiously in

• Hepatic impairment
• Renal impairment
• Breast or estrogen-dependent carcinoma
• Thromboembolic disorders
• Undiagnosed abnormal genital bleeding
• Diabetes mellitus
• Cardiovascular disease
• Obesity
• Gallbladder disease
• HTN
• Sensitive to fluid retention
• Severe hypocalcemia
• Hyponatremia risk
• Hypothyroidism
• Migraine
• Seizure disorder
• Hx. of cholestatic jaundice with estrogens or pregnancy
• Systemic Lupus Erythematosus (SLE)
• Chorea
• Hepatic hemangiomas
• Endometriosis
• Porphyria
• Hypertriglyceridemia
• Asthma
• Surgery or prolonged immobilization
• Patients > 65 yrs

Supplemental Patient Information

• Advise patient not to use estrogens with or without progestins to prevent heart disease, heart attacks, or strokes as it may increase the chances of getting heart attack, strokes, breast cancer, blood clots and dementia
• Advise patients to notify health care provider if breast lumps, changes in speech, changes in vision, chest pain, dizziness, faintness, leg pain, severe headache, shortness of breath, unusual vaginal bleeding, or vomiting is experienced

Pregnancy Category:X

Breastfeeding: Suppresses lactation; not recommended.

• GU: Vaginal hemorrhage, endometrial disorder, leukorrhea, vaginal candidiasis, breast tenderness, breast enlargement, breast pain, nipple discharge, change in amount of cervical secretion, changes in cervical ectropion, galactorrhea, fibrocystic breast changes, breast CA, hyperkalemia, endometrial CA, ovarian CA, increase in size of uterine leiomyomata, endometrial hyperplasia
• GI:Abdominal pain, abdomen enlarged, nausea, vomiting, abdominal cramps, bloating, cholestatic jaundice, increased incidence of gall bladder disease, pancreatitis, enlargement of hepatic hemangiomas
• METABOLIC: Peripheral edema, increase/decrease in weight, reduced carbohydrate tolerance, hypercalcemia
• CV: Deep and superficial venous thrombosis, pulmonary embolism, thrombophlebitis, MI, stroke, increased BP, HTN
• CNS: Headache, migraine, dizziness, mental depression, chorea, nervousness, mood disturbances, irritability, exacerbation of epilepsy, dementia
• RESP: Upper respiratory infection, sinusitis, exacerbation of asthma
• DERM: Chloasma/melasma, erythema multiforme, erythema nodosum, hemorrhagic eruption, loss of scalp hair, hirsutism, pruritus, rash
• EENT: Retinal vascular thrombosis, vision change, intolerance to contact lenses
• MUSC: Back pain, arthralgia
• MISC: Pain in extremity, flu syndrome, accidental injury, surgery, aggravation of porphyria, edema, leg cramps, changes in libido, anaphylactoid/anaphylactic reactions including urticaria and angioedema, hypocalcemia, increased triglycerides

drospirenone

• Progestin; diffuses freely into the target cells in female reproductive tract, mammary gland, hypothalamus, and pituitary, binds to the progesterone receptor and slows frequency of release of gonadotropin releasing hormone from the hypothalamus and blunts pre-ovulatory LH surge
• Metabolized by liver; CYP450: 3A4 (minor) substrate
• Excreted in urine and feces
• Half-life: 30 hrs

estradiol

• Estrogens; binds to nuclear receptors in estrogen-responsive tissues, enhancing DNA, RNA, and protein synthesis. In androgen-dependent prostate cancer, competes for androgen receptor sites, inhibiting androgen activity. Also decreases pituitary release of follicle-stimulating hormone and luteinizing hormone
• Metabolized by liver; CYP450: 3A4 (minor extent) substrate
• Excreted in urine along with glucuronide and sulfate conjugates
• Half-life: 1.75 +/- 2.87 hrs

US Trade Name(s)

• Angeliq

US Availability

Angeliq (drospirenone/estradiol)

• TABS: 0.5 mg/1 mg
• TABS: 0.25 mg/0.5 mg

Canadian Trade Name(s)

• Angeliq

Canadian Availability

Angeliq (drospirenone/estradiol)

• TABS: 1 mg/1 mg

UK Trade Name(s)

• Angeliq

UK Availability

Angeliq (drospirenone/estradiol)

• TABS: 2 mg/1 mg

Australian Trade Name(s)

• Angeliq 1/2

Australian Availability

Angeliq 1/2 (drospirenone/estradiol)

• TABS: 2 mg/1 mg

[Outline]

Endocrine/Metabolic

Sex Hormones

Sex Hormones; Combinations

Obstetrics/Gynecology

Sex Hormones

Sex Hormones; Combinations

Pricing data from www.DrugStore.com in U.S.A.

• Angeliq 0.5-1 MG TABS [Disp Pack] (BAYER HEALTHCARE PHARMA)
  28 mg = $91.99
  84 mg = $260.96

Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

Drug Name: Angeliq 28 Day Pack

Ingredient(s): Drospirenone mixture with Ethinyl Estradiol

Imprint: CK

Color(s): Pink

Shape: Round

Size (mm): 6.00

Score: 1

Inactive Ingredient(s): starch, corn / ferric oxide red / hypromellose / lactose monohydrate / modified corn starch (1-octenyl succinic anhydride) / magnesium stearate / povidone k25 / talc / titanium dioxide

Drug Label Author:
Bayer HealthCare Pharmaceuticals Inc.

DEA Schedule:
Non-Scheduled