PREMARIN VAGINAL CREAM Dosage & Rx Info

Premarin Vaginal Cream Generic Name & Formulations

Legal Class

General Description

Conjugated estrogens 0.625mg/g.

Pharmacological Class

Estrogen.

How Supplied

Tabs 0.3mg, 0.625mg, 1.25mg—100, 1000; 0.45mg, 0.9mg—100; Cream—30g (w. applicator)

Manufacturer

Pfizer Inc.

Mechanism of Action

Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and FSH, through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these gonadotropins seen in postmenopausal women.

Premarin Vaginal Cream Indications

Indications

Atrophic vaginitis. Kraurosis vulvae. Moderate to severe dyspareunia due to menopause.

Premarin Vaginal Cream Dosage and Administration

Adult

Atrophic vaginitis, kraurosis vulvae: 0.5–2g/day intravaginally given cyclically (3 weeks on, 1 week off). Dyspareunia: 0.5g intravaginally twice weekly (eg, Mon. & Thurs.) given continuously or cyclically (3 weeks on, 1 week off).

Children

Not applicable.

Premarin Vaginal Cream Contraindications

Contraindications

Undiagnosed abnormal genital bleeding. Breast cancer (except in select patients being treated for metastatic disease) or other estrogen-dependent neoplasms. Active DVT, PE, or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Hepatic impairment or disease. Protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders. Pregnancy.

Premarin Vaginal Cream Boxed Warnings

Boxed Warning

Endometrial cancer. Breast cancer. Cardiovascular disorders. Probable dementia.

Premarin Vaginal Cream Warnings/Precautions

Warnings/Precautions

Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, MI, stroke, VTE); discontinue if occurs. Manage risk factors for cardiovascular disease and venous thromboembolism appropriately. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of breast or ovarian cancer. Risk of probable dementia in women >65yrs of age. Gallbladder disease. Severe hypercalcemia in breast cancer or bone metastases. Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. Preexisting hypertriglyceridemia. History of cholestatic jaundice. Discontinue if pancreatitis, hypercalcemia, or recurrence of cholestatic jaundice occurs. Monitor thyroid function. Conditions aggravated by fluid retention. Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Reevaluate periodically. Nursing mothers: not recommended.

Premarin Vaginal Cream Pharmacokinetics

Distribution

Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in the blood largely bound to SHBG and albumin.

Metabolism

Hepatic.

Elimination

Renal. Half-life: ~17 hours.

Premarin Vaginal Cream Interactions

Interactions

May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John’s wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

Premarin Vaginal Cream Adverse Reactions

Adverse Reactions

Abdominal pain, asthenia, back pain, headache, flatulence, nausea, depression, insomnia, breast pain, endometrial hyperplasia, leucorrhea, vaginal hemorrhage, vaginitis; thromboembolism, neoplasms, anaphylaxis, angioedema (permanently discontinue if occurs).

Premarin Vaginal Cream Clinical Trials

See Literature

Premarin Vaginal Cream Note

Not Applicable

Premarin Vaginal Cream Patient Counseling