ospemifene

(redirected from Osphena)

ospemifene

(os- pem-i-feen) ,

Osphena

(trade name)

Classification

Therapeutic: hormones
Pharmacologic: estrogen agonists antagonists
Pregnancy Category: X

Indications

Moderate to severe dyspareunia due to menopausal vulvar/vaginal atrophy.

Action

Has agonist (estrogen-like) effects on the endometrium of the uterus; effects are tissue-specific.

Therapeutic effects

Decreased dyspareunuia.

Pharmacokinetics

Absorption: Well absorbed following oral administration; food enhances absorption 2–3 fold.
Distribution: Unknown.
Protein Binding: >99%.
Metabolism and Excretion: Mostly metabolized by the liver (CYP3A4 and CYP2C9 enzyme systems); 75% exceted in feces, 7% in urine as metabolites; minimal amounts excreted unchanged in urine.
Half-life: 26 hr.

Time/action profile (improvement in symptoms)

ROUTEONSETPEAKDURATION
POwithin 12 wkunknownunknown

Contraindications/Precautions

Contraindicated in: Undiagnosed/abnormal genital bleeding;History/ suspicion of estrogen-dependent cancer;History of/current DVT/PE/MI/cardiovascular/arterial thromboembolic pathology;Concurrent estrogens, estrogen agonist/antagonists, fluconazole, or rifampin; Obstetric: Known/suspected pregnancy (may cause fetal harm); Lactation: Breast feeding should be avoided.
Use Cautiously in: Patients with risk factors for cardiovascular disease, arterial vascular disease or venous thromboembolism (including hypertension, obesity, family history, tobacco use, diabetes mellitus, history of DVT/PE or systemic lupus erythematosus);Known or suspected breast cancer;Severe hepatic impairment.

Adverse Reactions/Side Effects

Cardiovascular

  • stroke (life-threatening)
  • deep vein thrombosis/PE (life-threatening)

Genitourinary

  • endometrial cancer (life-threatening)
  • genital/vaginal discharge

Dermatologic

  • hot flush
  • hyperhydrosis

Musculoskeletal

  • muscle spasms

Interactions

Drug-Drug interaction

Blood levels, effects and risk of adverse reactions ↑ by fluconazole, avoid concurrent use.Blood levels and effects may be ↑ by ketocoanzole or other drugs that inhibit the CYP3A4 or CYP2C9 enzyme systems.Blood levels and beneficial effects ↓ by rifampin, avoid concurrent use.Avoid concurrent use of other estrogens or estrogen agonist/antagonists due to ↑ estrogen effects.May displace or be displaced by other drugs that are highly protein bound.

Route/Dosage

Oral (Adults) 60 mg once daily with food.

Availability

Tablets: 60 mg

Nursing implications

Nursing assessment

  • Assess amount of pain during intercourse prior to and periodically during therapy.
  • Determine methods previously use to treat dyspareunia.
  • Assess BP before and periodically during therapy.

Potential Nursing Diagnoses

Sexual dysfunction (Indications)
Deficient knowledge, related to medication regimen (Patient/Family Teaching)

Implementation

  • Oral: Administer once daily with food.

Patient/Family Teaching

  • Instruct patient to take ospemifene as directed. Advise patient to read Patient Information sheet before starting therapy and with each Rx refill in case of changes.
  • Advise patient to report signs and symptoms of unusual vaginal bleeding, changes in vision or speech, sudden new severe headaches, severe pains in chest or legs with or without shortness of breath, weakness, or fatigue promptly to health care professional.
  • Inform patient that ospemifene may cause hot flashes, vaginal discharge, muscle spasm, and increased sweating.
  • Patients who still have a uterus should discuss addition of progestin with health care professional.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Advise patient to notify health care professional of medication regimen before treatment or surgery.
  • Women should be monitored for breast and uterine cancer (pelvic exam, breast exam, mammogram) at least yearly.
  • Caution patient that cigarette smoking, high BP, high cholesterol, diabetes, and being overweight during estrogen therapy may increase risk of heart disease.
  • Ospemifene should not be taken during pregnancy. Instruct patient to notify health care professional immediately if pregnancy is planned or suspected or if breast feeding.
  • Advise patient to discuss dose and need for ospemifene every 3–6 mo.

Evaluation/Desired Outcomes

  • Decrease in pain during intercourse.
References in periodicals archive ?
The FDA approval of Osphena (TM) was supported by three Phase 3 placebo-controlled clinical trials involving approximately 1,800 postmenopausal women with VVA receiving either Osphena (TM) 60 mg (N=1102) or placebo (N=787).
In the first and second clinical trials, Osphena (TM) demonstrated a statistically significant improvement from Baseline to Week 12 in moderate to severe dyspareunia (1st clinical trial p=0.
In clinical studies, the more commonly reported adverse reactions (greater than or equal to 1 percent) in patients treated with Osphena (TM) 60 mg compared to placebo were: hot flush (7.
The randomized, double-blind, placebo-controlled multicenter study will assess the safety and efficacy of Osphena 60 milligrams (mg) once-daily oral therapy in postmenopausal women with vaginal dryness as the most bothersome symptom (MBS) of VVA due to menopause.
Most Important Information you should know about Osphena
Last year, the Food and Drug Administration approved Osphena (ospemifene) to treat vaginal atrophy related to menopause.
Osphena should not be used in women who have unusual vaginal bleeding, have or have had breast or uterine cancer, blood clots, had a stroke or heart attack, have liver problems, are allergic to Osphena or its ingredients, or are pregnant.
Osphena can actually help improve specific vaginal tissues and provide relief within twelve weeks after starting treatment.
Zerbe co-founded and is chief executive officer of QuatRx Pharmaceuticals Company, a venture-backed drug development company that developed the recently launched product for postmenopausal dyspareunia, Osphena.
Following are the abstracts being presented on Osphena during the NAMS annual conference:
Osphena should be prescribed for the shortest duration consistent with treatment goals for the individual woman.
These are the same women who came of age in the Sexual Revolution, but are now hesitant to talk about painful sex after menopause, even though it is common and there are treatments available, like Osphena (ospemifene)[sup.