Drospirenone + Estradiol

Drospirenone + Estradiol is a combined oral contraceptive and hormone replacement therapy. Drospirenone is a progestin with antimineralocorticoid and antiandrogenic activity. Estradiol is an endogenous estrogen that reduces gonadotropin-releasing hormone and LH/FSH release. It is used for contraception, treatment of climacteric syndrome (vasomotor symptoms, sleep disorders, depressed mood, nervousness, atrophic urogenital conditions) in postmenopausal women, and prevention of postmenopausal osteoporosis. Contraindicated in pregnancy, undiagnosed abnormal genital bleeding, breast cancer, liver tumors, severe hepatic or renal disease.

• Contraception
• Postmenopausal climacteric syndrome (hot flushes, sweating, sleep disorders, depressed mood, nervousness)
• Atrophic urogenital conditions
• Prevention of postmenopausal osteoporosis

17β-estradiol is chemically and biologically identical to endogenous human E2. Drospirenone is a synthetic progestin with antimineralocorticoid and antiandrogenic activity. Drospirenone opposes estrogen-induced endometrial hyperplasia.

Drospirenone is a progestin with antimineralocorticoid and antiandrogenic activity. Estradiol is an endogenous estrogen that reduces gonadotropin-releasing hormone and LH/FSH release.

Adult Dose (Hormone Replacement Therapy): One tablet orally daily.

Hepatic Dose: Well tolerated in mild/moderate hepatic impairment; contraindicated in severe liver disease.

Renal Dose: Slight increase in DRSP exposure in mild/moderate renal impairment but not clinically relevant; contraindicated in severe renal disease.

Oral tablet. Take in the dose and duration as advised by your doctor. Swallow whole. Do not chew, crush or break. May be taken with or without food, but preferably at a fixed time daily.

If you miss a dose of Drospirenone + Estradiol, take it as soon as possible within 24 hours. If more than 24 hours, no extra tablet needed. If several tablets are missed, bleeding may occur.

Common Side Effects:

• Nausea
• Stomach pain
• Headache
• Weight gain
• Breast pain
• Irregular uterine bleeding

• Consider all risk factors before initiating HRT.
• Venous thromboembolism: Risk increases with personal history, family history, severe obesity and age. Temporarily discontinue with prolonged immobilization, major surgery or trauma.
• Discontinue if migraine, cholestatic jaundice or symptoms of thrombotic event occur.
• Do not use in undiagnosed abnormal genital bleeding, breast cancer, liver tumors or severe liver disease.

• Undiagnosed abnormal genital bleeding
• Known or suspected breast cancer
• Sex steroid-influenced premalignant conditions or malignancies
• Liver tumors (benign or malignant)
• Severe hepatic disease
• Severe renal disease
• Acute arterial thromboembolism (e.g., myocardial infarction, stroke)
• Active deep venous thrombosis or thromboembolic disorders
• Severe hypertriglyceridemia
• Pregnancy and lactation

Pharmacodynamic interaction with antihypertensive medications (ACE inhibitors, angiotensin II receptor antagonists, hydrochlorothiazide) may cause additional decrease in blood pressure. Combined use with NSAIDs may cause a small increase in serum potassium, more pronounced in diabetic women.

Caution is advised when consuming alcohol with Drospirenone + Estradiol. Please consult your doctor.

Highly unsafe during pregnancy. Studies on pregnant women and animals have shown significant harmful effects to the developing baby.

Probably unsafe during breastfeeding. Limited human data suggests drug may pass into breastmilk and harm the baby. Nonhormonal and progestin-only contraceptives preferred, especially during first 4 weeks postpartum.

Not indicated for use in children and adolescents.

No data suggesting a need for dosage adjustment in elderly patients.

Renal impairment: Well tolerated in mild/moderate; contraindicated in severe renal disease.

Hepatic impairment: Well tolerated in mild/moderate; contraindicated in severe hepatic disease.

Acute toxicity studies indicate no acute toxicity risk even with multiple therapeutic doses. Clinical studies up to 100 mg DRSP and 4 mg E2 were well tolerated.

Store below 30°C, away from light & moisture. Keep out of reach of children.

Drospirenone + Estradiol