ospemifene

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 ?
Ospemifene is a selective estrogen receptor modulator (SERM), meaning that it acts like estrogen but it contains no estrogen.
Duchesnay USA, a pharmaceutical company that specialises in women's health, has launched its new Osphena (ospemifene) website, it was reported yesterday.
* Neither intravaginal dehydroepiandrosterone (DHEA; prasterone) nor the oral selective estrogen receptor modulator ospemifene has been studied in breast cancer survivors.
Duchesnay USA, a pharmaceutical company specializing in women's health, announced that the Food and Drug Administration has approved its supplemental New Drug Application (sNDA) seeking to add moderate to severe vaginal dryness, a symptom of vulvar and vaginal atrophy (WA), due to menopause, to the indication of Osphena (ospemifene).
Some FDA-approved treatment options for dyspareunia include ospemifene, prasterone.
Global Banking News-October 24, 2018-Duchesnay submits supplemental NDA with the US FDA for Osphena (ospemifene) for treating moderate to severe dyspareunia
But until more robust data are available, doctors should "discuss the benefits and risks of all available treatment options for vaginal symptoms, including over-the-counter lubricants, vaginal moisturizers, and FDA-approved vaginal therapies such as vaginal estrogen and intravaginal dehydroepiandrosterone and oral therapies such as hormone therapy and ospemifene to determine the best treatment for women with GSM." Any discussion of vaginal energy-based therapies, should include the disclosure that these have not been approved for the specific indication, she cautioned.
Ospemifene: a first-in-class, non-hormonal selective estrogen receptor modulator approved for the treatment of dyspareunia associated with vulvar and vaginal atrophy.
will continue to retain its rights to ospemifene in all other countries of the world.
However, therapeutic options have now been increased; after over 20 years in development, ospemifene was approved in early 2013 by the US Food and Drug Administration (FDA) for the treatment of moderate-to-severe dyspareunia associated with vulvar and vaginal atrophy (VVA) due to menopause [9].
In particular, the only SERM indicated for vulvar-vaginal atrophy (VVA) is ospemifene [5].