Adult Dosing

Vasomotor symptoms and vulvar and vaginal atrophy due to menopause

• Start 0.3 mg PO qd, adjust dose as per response
• Alt: 0.3 mg PO qd in a cycle of 25 days on and 5 days off

Prevention of postmenopausal osteoporosis

• Start 0.3 mg PO qd, adjust dose as per response
• Alt: 0.3 mg PO qd in a cycle of 25 days on and 5 days off

Hypoestrogenism

Female hypogonadism

• 0.3-0.625 mg PO qd in a cycle of 3 wks on and 1 wk off

Female castration or primary ovarian failure

• 1.25 mg PO in a cycle of 3 wks on and 1 wk off
• May increase or decrease the dose according to severity of symptoms and response of the patient

Palliative treatment of breast cancer

• 10 mg PO tid x 3 months

Palliative treatment of prostate cancer

• 1.25-2.5 mg PO tid

• In postmenopausal women with a uterus, add progestin for at least 12-14 days every 28 day cycle to reduce the risk to the endometrial cancer
• Use lowest effective dose of estrogen/progestin combination for shortest duration

Pediatric Dosing

• Safety and efficacy has not been established in children
• Estrogen therapy has been used for the induction of puberty in adolescents

[Outline]

• Adult Dosing
• Pediatric Dosing

• Treatment of moderate to severe vasomotor symptoms of menopause
• Treatment of moderate to severe symptoms of vulvar and vaginal atrophy of menopause
• Treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure
• Palliative treatment of metastatic breast cancer in women and men
• Treatment of androgen-dependent prostate cancer
• Prevention of postmenopausal osteoporosis

• Hypersensitivity to any of the ingredients of the product
• Undiagnosed abnormal genital bleeding
• Known, suspected, or history of breast cancer except in patients being treated for metastatic disease
• Known or suspected estrogen-dependent neoplasia
• Active or history of deep vein thrombosis, pulmonary embolism
• Active or recent (within 1 yr) arterial thromboembolic disease
• Liver dysfunction or disease
• Known or suspected pregnancy

• Estrogen increases the risk of endometrial cancer. Monitor closely all the women taking estrogen therapy, use adequate diagnostic measures like endometrial sampling to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding
• Do not use estrogens with or without progestins for the prevention of cardiovascular disease. As per the study conducted by Women’s Health Initiative (WHI), daily estrogen 0.625 mg alone therapy increases the risk of stroke and deep vein thrombosis (DVT) in postmenopausal women (50 to 79 years of age) and oral conjugated estrogens 0.625 mg in combination with medroxyprogesterone acetate 2.5 mg, relative to placebo increases risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli and deep vein thrombosis in postmenopausal women (50 to 79 years of age) during 5.6 years of treatment
• It also increases the risk of developing dementia in postmenopausal women 65 years of age or older during 4 years of treatment (WHIMS), other doses or estrogen/progestin combos not studied, but assume similar risk. Use lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman

Renal Dose Adjustment

• Renal impairment: Dose adjustments not defined

Hepatic Dose Adjustment

• Hepatic impairment: Contraindicated

• Estrogen alone or in combination with progestin therapy increases the risk of stroke, DVT, pulmonary embolism, and myocardial infarction [US Black Box Warning]
• Risk factors for arterial vascular disease and/or venous thromboembolism should be managed appropriately
• Estrogen alone or in combination with progestin therapy increases the risk of venous thromboembolism. Discontinue immediately if suspected.
• Discontinue the estrogen therapy 4-6 wks before surgery associated with an increased risk of thromboembolism, or require prolong immobilization
• Unopposed use of estrogens in women with intact uteri increases the risk of endometrial cancer 2-12 times greater than in non-users [US Black Box warning]
• Estrogens and progestins use in postmenopausal women increase the risk of breast cancer. Perform breast examination and mammogram yearly based on patient age, risk factors and prior mammogram results and advise patients to self examine every month
• Estrogen and estrogen/progestin therapy increases the risk of dementia in postmenopausal women 65 years of age and older [US Black Box warning]
• Increases the risk of gallbladder diseases by 2 to 4 fold in postmenopausal women receiving estrogen therapy
• Estrogen therapy causes severe hypercalcemia in patients with breast cancer and bone metastases. Discontinue the therapy and provide appropriate measures, if hypercalcemia occurs
• Retinal vascular thrombosis occurs in patients receiving estrogens. Discontinue the drug if there is sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia or migraine. Permanently discontinue if papilledema or retinal vascular lesions are seen on examination
• Use of progestin with estrogen in continuous regimen lowers the incidence of endometrial hyperplasia, than would be induced by estrogen alone treatment. However there is possible increased risk of breast cancer, adverse effects on lipoprotein metabolism and impairment of glucose tolerance, with the use of progestins along with estrogens compared to estrogen-alone regimens
• Administration of estrogen therapy can exacerbate endometriosis
• Estrogen use causes increases in blood pressure, monitor BP at regular interval
• Estrogen therapy elevates the plasma triglycerides in patients with preexisting hypertriglyceridemia, leading to pancreatitis and other complications
• Use cautiously in patients with a history of cholestatic jaundice associated with past estrogen use or with pregnancy, discontinue the drug in case of recurrence
• Estrogen administration causes increased thyroid-binding globulin (TBG) levels. Patients on thyroid hormone replacement therapy receiving estrogen require increased doses of their thyroid replacement therapy. Monitor thyroid function regularly to maintain free thyroid hormone levels in an acceptable range
• Estrogen causes fluid retention, use cautiously in patients with conditions like asthma, epilepsy, migraine, and cardiac or renal dysfunction
• Use of estrogen alone for 5 or more years increases the risk of ovarian cancer

Cautions: Use cautiously in

• Renal impairment
• Cardiovascular diseases
• Hypertension
• Hypertriglyceridemia
• History of Cholestatic Jaundice
• Hypothyroidism
• Gallbladder disease
• Hyperparathyroidism
• Asthma
• Diabetes mellitus
• Epilepsy
• Migraine
• Severe hypocalcemia
• Surgery or prolonged immobilization
• Porphyria
• Systemic lupus erythematosus
• Hepatic hemangiomas
• Endometriosis

Pregnancy Category:X

Breastfeeding: Estrogen administration during breastfeeding interferes with lactation by decreasing the quantity and quality of the milk. Detectable amount is secreted in breast milk; manufacturer advises to use cautiously in nursing mother.

• CNS: Headache, depression, insomnia, migraine, dizziness, nervousness, mood disturbances, irritability, exacerbation of epilepsy, dementia, exacerbation of chorea
• CV: Deep and superficial venous thrombosis, pulmonary embolism, thrombophlebitis, myocardial infarction, stroke, hypertension, edema, vasodilatation, increased triglycerides
• GU: Abnormal vaginal bleeding, breakthrough bleeding, spotting, dysmenorrhea, vaginal moniliasis, vaginitis, vaginal candidiasis, change in amount of cervical secretion, changes in cervical ectropion, ovarian cancer, endometrial hyperplasia, endometrial cancer, PMS, amenorrhea, cystitis, leukorrhea, breast tenderness, breast enlargement, nipple discharge, galactorrhea, breast cancer, changes in libido
• GI: Nausea, constipation, dyspepsia, vomiting, abdominal pain, bloating, cholestatic jaundice, gallbladder disease, pancreatitis, enlargement of hepatic hemangiomas, diarrhea, flatulence
• DERM: Chloasma or melasma, erythema multiforme, erythema nodosum, hemorrhagic eruption, hirsutism, pruritus, rash, hair loss, urticaria, angioedema
• EENT: Retinal vascular thrombosis, intolerance to contact lenses
• RESP: Sinusitis, URTI, bronchitis, pharyngitis, rhinitis, exacerbation of asthma
• METABOLIC: Hypocalcemia, weight gain, glucose intolerance
• MUSC: Arthralgia, back pain, leg cramps, myalgia
• MISC: Infection, asthenia, accidental injury, flu syndrome, edema, anaphylaxis

• Estrogen; responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. By negative feedback mechanism regulates the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH)
• Metabolized by liver; CYP 450: 3A4. Also undergoes enterohepatic recirculation
• Renally excreted
• Half-life
• Dose of 0.625 mg: 11.4-26.7 hrs
• Dose of 1.25 mg: 12.5-26.5 hrs

US Trade Name(s)

• Premarin

US Availability

Premarin

• TABS: 0.3, 0.45, 0.625, 0.9, 1.25, 2.5 mg

Canadian Trade Name(s)

• Congest
• Premarin

Canadian Availability

Estrogen conjugated (generic)

• TABS: 0.3, 0.625, 0.9, 1.25 mg

C.E.S (generic)

• TABS: 0.3, 0.625, 0.9, 1.25 mg

Congest

• TABS: 0.3, 0.625, 0.9, 1.25, 2.5 mg

Premarin

• TABS: 0.3, 0.625, 1.25 mg

UK Trade Name(s)

• Premarin

UK Availability

Premarin

• TABS: 0.3, 0.625, 1.25 mg

Australian Trade Name(s)

• Premarin

Australian Availability

Premarin

• TABS: 0.3, 0.625 mg

[Outline]

Endocrine/Metabolic

Sex Hormones

Estrogens

Obstetrics/Gynecology

Sex Hormones

Estrogens

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

• Premarin 1.25 MG TABS [Bottle] (WYETH)
  30 mg = $75.99
  90 mg = $209.97
• Premarin 0.45 MG TABS [Bottle] (WYETH)
  30 mg = $75.99
  90 mg = $207.97
• Premarin 0.3 MG TABS [Bottle] (WYETH)
  30 mg = $74.99
  90 mg = $202.97
• Premarin 0.625 MG TABS [Bottle] (WYETH)
  30 mg = $73.99
  90 mg = $199.97
• Premarin 0.9 MG TABS [Bottle] (WYETH)
  30 mg = $76.99
  90 mg = $207.97

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.

• Premarin 0.3 MG Oral Tablet (Physicians Total Care, Inc.)
• Premarin 0.3 MG Oral Tablet (Wyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.)
• Premarin 0.45 MG Oral Tablet (Physicians Total Care, Inc.)
• Premarin 0.45 MG Oral Tablet (Wyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.)
• Premarin 0.625 MG Oral Tablet (Physicians Total Care, Inc.)
• Premarin 0.625 MG Oral Tablet (State of Florida DOH Central Pharmacy)
• Premarin 0.625 MG Oral Tablet (Wyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.)
• Premarin 0.9 MG Oral Tablet (Physicians Total Care, Inc.)
• Premarin 0.9 MG Oral Tablet (Wyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.)
• Premarin 1.25 MG Oral Tablet (Physicians Total Care, Inc.)
• Premarin 1.25 MG Oral Tablet (Wyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.)