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Activella

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Activella

Side Effects
Interactions

SIDE EFFECTS

The following serious adverse reactions are discussed elsewhere in the labeling:

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Adverse reactions reported with Activella 1 mg/0.5 mg by investigators in the Phase 3 studies regardless of causality assessment are shown in Table 1.

TABLE 1 : ALL TREATMENT-EMERGENT ADVERSE REACTIONS REGARDLESS OF RELATIONSHIP REPORTED AT A FREQUENCY OF ≥ 5 PERCENT WITH ACTIVELLA 1 MG/0.5 MG

  Endometrial Hyperplasia Study (12-Months) Vasomotor Symptoms Study (3-Months) Osteoporosis Study (2-Years)
Activella1 mg/0.5 mg
(n=295)
1 mg E2
(n=296)
Activella1 mg/0.5 mg
(n=29)
Placebo
(n=34)
Activella1 mg/0.5 mg
(n=47)
Placebo (n=48)
Body as a Whole
  Back Pain 6% 5% 3% 3% 6% 4%
  Headache 16% 16% 17% 18% 11% 6%
Digestive System
  Nausea 3% 5% 10% 0% 11% 0%
  Gastroenteritis 2% 2% 0% 0% 6% 4%
Nervous System
  Insomnia 6% 4% 3% 3% 0% 8%
  Emotional Lability 1% 1% 0% 0% 6% 0%
Respiratory System
  Upper Respiratory 18% 15% 10% 6% 15% 19%
Tract Infection
  Sinusitis 7% 11% 7% 0% 15% 10%
Metabolic and Nutritional
  Weight Increase 0% 0% 0% 0% 9% 6%
Urogenital System
  Breast Pain 24% 10% 21% 0% 17% 8%
  Post-Menopausal Bleeding 5% 15% 10% 3% 11% 0%
  Uterine Fibroid 5% 4% 0% 0% 4% 8%
  Ovarian Cyst 3% 2% 7% 0% 0% 8%
Resistance Mechanism
  Infection Viral 4% 6% 0% 3% 6% 6%
  Moniliasis Genital 4% 7% 0% 0% 6% 0%
Secondary Terms
  Injury Accidental 4% 3% 3% 0% 17%* 4%*
  Other Events 2% 3% 3% 0% 6% 4%
* including one upper extremity fracture in each group

Adverse reactions reported with Activella 0.5 mg/0.1 mg by investigators during the Phase 3 study regardless of causality assessment are shown in Table 2.

TABLE 2 : ALL TREATMENT-EMERGENT ADVERSE REACTIONS REGARDLESS OF RELATIONSHIP REPORTED AT A FREQUENCY OF ≥ 5 PERCENT WITH ACTIVELLA 0.5 MG/0.1 MG

  Activella 0.5 mg/0.1 mg
(n=194)
Placebo
(n=200)
Body as a Whole
  Back Pain 10% 4%
  Headache 22% 19%
  Pain in extremity 5% 4%
Digestive System
  Nausea 5% 4%
  Diarrhea 6% 6%
Respiratory System
  Nasopharyngitis 21% 18%
  Urogenital System Endometrial thickening 10% 4%
  Vaginal hemorrhage 26% 12%

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of Activella. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Genitourinary System

Changes in vaginal bleeding pattern and abnormal withdrawal bleeding or flow; breakthrough bleeding; spotting; dysmenorrhea, increase in size of uterine leiomyomata; vaginitis, including vaginal candidiasis; change in amount of cervical secretion; changes in cervical ectropion; pre-menstrual-like syndrome; cystitis-like syndrome; ovarian cancer; endometrial hyperplasia; endometrial cancer.

Breast

Tenderness, enlargement, pain, nipple discharge, galactorrhea; fibrocystic breast changes; breast cancer.

Cardiovascular

Deep and superficial venous thrombosis; pulmonary embolism; thrombophlebitis; myocardial infarction, stroke; increase in blood pressure.

Gastrointestinal

Nausea, vomiting; changes in appetite; cholestatic jaundice; abdominal pain/cramps, flatulence, bloating; increased incidence of gallbladder disease and pancreatitis.

Skin

Chloasma or melasma that may persist when drug is discontinued; erythema multiforme; erythema nodosum; hemorrhagic eruption; loss of scalp hair; seborrhea; hirsutism; itching; skin rash; pruritus.

Eyes

Retinal vascular thrombosis, intolerance to contact lenses.

Central Nervous System

Headache; migraine; dizziness; mental depression; chorea; insomnia; nervousness; mood disturbances; irritability; exacerbation of epilepsy; dementia.

Miscellaneous

Increase or decrease in weight; edema; leg cramps; changes in libido; fatigue; exacerbation of asthma; increased triglycerides; hypersensitivity; anaphylactoid/anaphylactic reactions.

Read the Activella (estradiol, norethindrone acetate) Side Effects Center for a complete guide to possible side effects

DRUG INTERACTIONS

Coadministration of estradiol with norethindrone acetate did not elicit any apparent influence on the pharmacokinetics of norethindrone acetate. Similarly, no relevant interaction of norethindrone acetate on the pharmacokinetics of estradiol was found within the NETA dose range investigated in a single dose study.

Metabolic Interactions

Estradiol

In-vitro and in-vivo studies have shown that estrogens are metabolized partially by cytochrome P450 3A4 (CYP3A4). Therefore, inducers or inhibitors of CYP3A4 may affect estrogen drug metabolism. Inducers of CYP3A4 such as St. John's wort (Hypericum perforatum) preparations, phenobarbital, carbamazepine, and rifampin may reduce plasma concentrations of estrogens, possibly resulting in a decrease in therapeutic effects and/or changes in the uterine bleeding profile. Inhibitors of CYP3A4 such as erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir and grapefruit juice may increase plasma concentrations of estrogens and result in side effects.

Norethindrone Acetate

Drugs or herbal products that induce or inhibit cytochrome P-450 enzymes, including CYP3A4, may decrease or increase the serum concentrations of norethindrone.

Read the Activella Drug Interactions Center for a complete guide to possible interactions

Last reviewed on RxList: 11/4/2013
This monograph has been modified to include the generic and brand name in many instances.

Side Effects
Interactions
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Activella - User Reviews

Activella User Reviews

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Report Problems to the Food and Drug Administration

 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


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