Berlex Inc's Angeliq

Monica Holmberg, PharmD
Published Online: Thursday, March 1, 2007
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Berlex Inc has received US FDA approval for Angeliq (0.5 mg drospirenone and 1 mg estradiol) for the treatment of moderate-to-severe vasomotor menopausal symptoms and moderate- to-severe symptoms of vaginal and vulvar atrophy related to menopause in women who have a uterus.1 Up to 85% of menopausal women experience symptoms such as hot flashes, sweating, insomnia, and vaginal dryness or discomfort. Treatment with hormone therapy is a popular option, as estrogen replacement has been shown to control menopausal symptoms and improve patients' quality of life.2

Mechanism of Action

Estrogen supplementation during menopause is believed to relieve menopausal symptoms by replacing the estrogen that the body is no longer able to make. The estradiol form is the primary intracellular human estrogen and is more potent than the estrone or estriol forms.1

In women with a uterus, the use of progestin in conjunction with estrogen has been associated with a lower incidence of endometrial hyperplasia. As a result, hormone therapy in women who have not had a hysterectomy usually includes a progestin component to balance estrogen's effects.1 In addition, the progestin component of Angeliq, drospirenone, exerts an antialdosterone effect and is promoted to counteract estradiol's sodium-and water-retention effect.3

Clinical Trials

The efficacy of treatment with Angeliq was evaluated in a bioequivalence study comparing the combination product Angeliq with estradiol (Estrace) 1 mg, an estradiol product already available. The trial determined the estradiol component of Angeliq to be bioequivelent to Estrace.

The safety of Angeliq on the endometrium was evaluated in a 1-year clinical trial comparing estradiol alone with estradiol with 1, 2, or 3 mg of drospirenone. At the study's end, no patients in the Angeliq group were found to have endometrial hyperplasia.1

Safety

Angeliq is contraindicated in patients with undiagnosed abnormal genital bleeding, a history of or active or suspected breast cancer, estrogen-dependent neoplasia, a history of or active deep vein thrombosis or pulmonary embolism, active or a history of arterial thromboembolic disease within the past year, renal insufficiency, hepatic disease or insufficiency, or adrenal insufficiency.

Angeliq carries a boxed warning against the use of any estrogen or progestin products for the prevention of cardiovascular disease or dementia. Patients using Angeliq may be at a greater risk for developing gallbladder disease, hypercalcemia, or visual abnormalities. An increase in triglycerides was noted in some women with preexisting hypertriglyceridemia. Patients should be monitored for these effects, and treatment with Angeliq should be discontinued if any occur.

Angeliq may cause hyperkalemia as a result of the antialdosterone effect of the drospirenone component. Patients prone to hyperkalemia should not use Angeliq, and caution should be used in patients taking medications known to raise serum potassium levels.

Patients who are pregnant or breast-feeding should not use Angeliq. Angeliq is not approved for use in pediatric patients.1

Patient Education

Patients using Angeliq should tell their doctor about their health history and all concomitant prescription or OTC medications they may be taking.

Rare but serious side effects of Angeliq include breast, ovarian, or uterine cancer, stroke, heart attack, blood clots, dementia, and gallbladder disease. Educate patients about warning signs for these conditions, such as breast lumps, unusual vaginal bleeding, dizziness, changes in speech, severe headache, chest pain, difficulty breathing, pain in the legs, vision changes, or vomiting.

Commonly experienced side effects include headache, breast pain, irregular vaginal bleeding ("spotting"), stomach and/or abdominal cramps, bloating, nausea, vomiting, and hair loss. Less common side effects include hypertension, hepatic problems, increased blood sugar, fluid retention, enlargement of uterine fibroids, and vaginal yeast infection.1

Dr. Holmberg is a pharmacist with Phoenix Children's Hospital, Phoenix, Ariz.


References

1. Angeliq [package insert]. Montville, NJ: Berlex; 2005. Available at: www.berlex.com/html/products/pi/fhc/Angeliq_PI.pdf. Accessed February 2007.

2. American Association of Clinical Endocrinologists medical guidelines for clinical practice for the diagnosis and treatment of menopause. AACE Menopause Guidelines Revision Task Force. Endocrine Pract. 2006;12(3):315-337.

3. Waknine Y. FDA approvals: Humira and Angeliq. Available at: www.medscape.com/viewarticle/514181. Accessed February 2007.




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