Brand and Other Names:Premphase, Prempro
- Classes: Estrogens/Progestins-HRT
Dosing & Uses
Dosage Forms & Strengths
- 0.3 mg/1.5mg
- 0.45 mg/1.5mg
- 0.625 mg/2.5mg
- 0.625 mg/5mg
- 0.625 mg/5mg plus conjugated estrogen 0.625 mg (Premphase)
Indicated in women who have a uterus for the treatment of moderate-to-severe vasomotor symptoms or vulvar and vaginal atrophy associated with the menopause
Also indicated for 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 nonestrogen medications should be carefully considered
Premphase (biphasic regimen)
- 1 pure estrogen tablet qDay Days 1-14, THEN
- 1 combo tablet PO qDay on days 15-28 of cycle
- 1 tablet PO qDay
Serious - Use Alternative
Significant - Monitor Closely
Frequency Not Defined
Growth potentiation of benign meningioma
Known anaphylactic reaction or angioedema
Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders
Current/history of DVT/PE, arterial thromboembolic disease, breast cancer, liver disease/tumors
Undiagnosed abnormal vaginal bleeding
Bone mineral density changes, current/history of depression, diabetes mellitus, HTN, hyperlipidemia, hypertriglyceridemia, obesity, endometriosis, family history of breast cancer and/or DVT/PE, smoking, severe hypocalcemia, ovarian cancer
Discontinue if the following develop: jaundice, visual problems, 4 wk before major surgery or prolonged immobilization, any symptoms of VTE, massive BP increase, unusually severe migraines or first-time migraines, depression
Increased risk of post-op thromboembolic complications, MI, stroke, pulmonary emboli, DVT, Alzheimer's disease, cardiovascular disorders, probable dementia, and endometrial cancer
Conditions exacerbated by fluid retention (eg, asthma, migraine, cardiac/renal dysfunction, epilepsy)
Patients on warfarin/oral anticoagulants: estrogens increase thromboembolic risk; increase in anticoagulant dose may be warranted
Exogenous estrogens may exacerbate symptoms of angioedema in women with hereditary angioedema
Pregnancy & Lactation
Pregnancy Category: X
Lactation: controversial; estrogens are excreted into breast milk in small quantities, use caution
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Estradiol: Endogenous estrogen; reduces the release of gonadotropin-releasing hormone from hypothalamus, reduces release of LH and FSH from pituitary gland; increases synthesis of DNA, RNA, and various proteins in target tissues
Medroxyprogestin: Progestin; inhibits secretion of gonadotropins from pituitary gland; prevents follicular maturation and ovulation, stimulates growth of mammary tissues
Bioavailability: Readily absorbed from GI tract (conjugated estrogens)
Onset: 2-4 wk (conjugated estrogens)
Peak Plasma: 8 hr (conjugated estrogens)
Protein Bound: 80% (conjugated estrogens); 90% (medroxyprogesterone)
Conjugated estrogens metabolized in liver to inactive sulfates and glucuronides
Medroxyprogesterone metabolized in liver
Metabolites: Estradiol, estrone, estriol (conjugated estrogens)
Excretion (conjugated estrogens): Urine, most estrogens are also excreted in bile and undergo enterohepatic recycling
Excretion (medroxyprogesterone): Urine
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.
|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
|2||This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.|
|3||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.|
|4||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|5||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|6||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|NC||NOT COVERED – Drugs that are not covered by the plan.|
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
Select a box to add or remove a plan.
Select a class to view formulary status for similar drugs