Berlex Inc's Angeliq

Berlex Inc has received US FDAapproval for Angeliq (0.5 mg drospirenoneand 1 mg estradiol) for thetreatment of moderate-to-severe vasomotormenopausal symptoms and moderate-to-severe symptoms of vaginal andvulvar atrophy related to menopause inwomen who have a uterus.¹ Up to 85% ofmenopausal women experience symptomssuch as hot flashes, sweating,insomnia, and vaginal dryness or discomfort.Treatment with hormone therapy isa popular option, as estrogen replacementhas been shown to controlmenopausal symptoms and improvepatients' quality of life.²

Mechanism of Action

Estrogen supplementation during menopauseis believed to relieve menopausalsymptoms by replacing the estrogen thatthe body is no longer able to make. Theestradiol form is the primary intracellularhuman estrogen and is more potent thanthe estrone or estriol forms.¹

In women with a uterus, the use ofprogestin in conjunction with estrogenhas been associated with a lower incidenceof endometrial hyperplasia. As aresult, hormone therapy in women whohave not had a hysterectomy usuallyincludes a progestin component to balanceestrogen's effects.¹ In addition, theprogestin component of Angeliq,drospirenone, exerts an antialdosteroneeffect and is promoted to counteractestradiol's sodium-and water-retentioneffect.³

Clinical Trials

The efficacy of treatment with Angeliqwas evaluated in a bioequivalence studycomparing the combinationproduct Angeliqwith estradiol (Estrace)1 mg, an estradiol productalready available.The trial determinedthe estradiol componentof Angeliq to bebioequivelent to Estrace.

The safety of Angeliqon the endometriumwas evaluated in a 1-year clinical trial comparingestradiol alonewith estradiol with 1, 2,or 3 mg of drospirenone. At the study'send, no patients in the Angeliq groupwere found to have endometrial hyperplasia.¹

Safety

Angeliq is contraindicated in patientswith undiagnosed abnormal genitalbleeding, a history of or active or suspectedbreast cancer, estrogen-dependentneoplasia, a history of or activedeep vein thrombosis or pulmonaryembolism, active or a history of arterialthromboembolic disease within the pastyear, renal insufficiency, hepatic diseaseor insufficiency, or adrenal insufficiency.

Angeliq carries a boxed warningagainst the use of any estrogen or progestinproducts for the prevention of cardiovasculardisease or dementia. Patientsusing Angeliq may be at a greaterrisk for developing gallbladder disease,hypercalcemia, or visual abnormalities.An increase in triglycerides was noted insome women with preexisting hypertriglyceridemia.Patients should be monitoredfor these effects, and treatmentwith Angeliq should be discontinued ifany occur.

Angeliq may cause hyperkalemia as aresult of the antialdosterone effect of thedrospirenone component. Patients proneto hyperkalemia should not use Angeliq,and caution should be used in patientstaking medications known to raise serumpotassium levels.

Patients who are pregnant or breast-feedingshould not use Angeliq. Angeliq isnot approved for use in pediatric patients.¹

Patient Education

Patients using Angeliq should tell theirdoctor about their health history and allconcomitant prescription or OTC medicationsthey may be taking.

Rare but serious side effects of Angeliqinclude breast, ovarian, or uterine cancer,stroke, heart attack, blood clots, dementia,and gallbladder disease. Educatepatients about warning signs for theseconditions, such as breast lumps, unusualvaginal bleeding, dizziness, changes inspeech, severe headache, chest pain, difficultybreathing, pain in the legs, visionchanges, or vomiting.

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

Dr. Holmberg is a pharmacist withPhoenix 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 clinicalpractice for the diagnosis and treatment of menopause. AACE Menopause GuidelinesRevision 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.