Estromarin®

Therapeutic Area:

,

Generic Name:

Conjugated Estrogen

Dosage Form:

cream

Drug Dose

Therapeutic Indications:

Vulvar and vaginal atrophy associated with menopause: Treatment of moderate-to-severe vulvar and vaginal atrophy associated with menopause

Mechanism of Action:

Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism.

Method of Administration:

Usual dosage range: 2 to 4 g daily, intravaginally, depending on the severity of condition.

Notes

-Angioedema or anaphylactic reaction to estrogen conjugated A synthetic or any component of the formulation.

-Undiagnosed abnormal genital bleeding; DVT or PE (current or history of).

-Active or history of arterial thromboembolic disease (eg, stroke, MI)

-Breast cancer (known, suspected or history of).

-Estrogen-dependent tumor (known or suspected)

-Hepatic impairment or disease.

-Antithrombin deficiency or other known thrombophilic disorders;

-Pregnancy

Interactions:

Inducers of CYP3A4, such as St. John’sWort (Hypericumperforatum), phenobarbital, carbamazepine, and rifampin may reduce plasma concentrations of estrogens.

Inhibitors of CYP3A4, such as erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir and grapefruit juice, may increase plasma concentrations of estrogens and may result in side effects.

Pregnancy and Lactation:

Estrogen is contraindicated for use during pregnancy.

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 estrogen is administered to a nursing woman.

Warning and Precaution:

  • Use is contraindicated in patients with known or suspected breast cancer. Estrogen use may also lead to severe hypercalcemia in patients with breast cancer and bone metastases; discontinue estrogen if hypercalcemia occurs.
  • The risk of endometrial cancer appears to be dose and duration dependent; risk appears to be greatest with use ≥5 years and may persist following discontinuation of therapy.
  • Endometriosis: Estrogens may exacerbate endometriosis.
  • Lipid effects: Estrogen compounds are generally associated with lipid effects such as increased HDL-cholesterol and decreased LDL-cholesterol. Triglycerides may also be increased in women with preexisting hypertriglyceridemia; discontinue if pancreatitis occurs.
  • Ovarian cancer: Postmenopausal estrogens with or without progestins may increase the risk of ovarian cancer; however, the absolute risk to an individual woman is small.
  • Use with caution in patients with Hepatic dysfunction, Renal impairment, Migraine, Epilepsy, Asthma, Cardiovascular disease, Gallbladder disease, Hereditary angioedema.
  • Estrogens should be discontinued at least 4 to 6 weeks prior to elective surgery associated with an increased risk of thromboembolism or during periods of prolonged immobilization.

Adverse Reactions:

Incidence>10%:

Headache, paresthesia dizziness, pain, abdominal pain, nausea, mastalgia, endometrial hyperplasia, uterine hemorrhage, Infection, back pain,upper respiratory tract infection.

Storage:

Store below 30ºC and protect from light and moisture.