ospemifene

Contraindicated in:

Hypersensitivity;
Undiagnosed abnormal genital bleeding;
History/suspicion of estrogen-dependent cancer;
History of/current thromboembolic disorder, including deep vein thrombosis (DVT), pulmonary embolism (PE), MI, or stroke;
Known or suspected breast cancer;
Severe hepatic impairment;
OB: Pregnancy;
Lactation: Lactation.

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);
Long-term use (>4–5 yr); may ↑ risk of MI, stroke, invasive breast cancer, PE, DVT, and dementia in postmenopausal women;
Women with a uterus (estrogen use without a progestin ↑ risk of endometrial cancer).

Adv. Reactions/Side Effects ⬆ ⬇

CV: DVT, MI

Derm: ↑sweating, hot flush

GU: genital/vaginal discharge

MS: muscle spasms

Neuro: STROKE

Resp: PE

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA), MALIGNANCY (BREAST, ENDOMETRIAL)

Interactions ⬆ ⬇

Drug-drug:

Fluconazole may ↑ levels and risk of toxicity; avoid concurrent use.
CYP3A4 or CYP2C9 inhibitors, including ketoconazole, may ↑ levels and risk of toxicity.
Rifampin may ↓ levels and effectiveness; 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.

Availability ⬆ ⬇

(Generic available)

Tablets: 60 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 60 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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

Therapeutic effects:

Decreased dyspareunia.
Decreased vaginal dryness.

Classifications ⬆ ⬇

Therapeutic Classification: hormones

Pharmacologic Classification: estrogen agonists/antagonists

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration; food enhances absorption 2–3-fold.

Distribution: Extensively distributed to tissues.

Protein Binding: >99%.

Metabolism/Excretion: Mostly metabolized by the liver via the CYP3A4 and CYP2C9 isoenzymes; 75% excreted in feces, 7% in urine as metabolites; minimal amounts excreted unchanged in urine.

Half-Life: 26 hr.

Time/Action Profile ⬆ ⬇

( improvement in symptoms)

ROUTE	ONSET	PEAK	DURATION
PO	within 12 wk	unknown	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of ospemifene to patient. Instruct them to take medication as directed. Do not share medication with others, even if they have similar symptoms; may be harmful. Keep out of children’s reach. Advise patient to read Patient Information sheet before starting therapy and with each Rx refill in case of changes.
Advise patient to discuss dose and need for ospemifene every 3–6 mo as the shortest necessary duration of therapy is recommended.
Advise women to perform monthly self breast exams and yearly breast exams by a health care provider. Mammograms should be scheduled based on patient age, risk factors, and prior mammogram results. Women should also follow yearly pelvic exams to monitor for uterine cancer.
Advise patient to report unusual vaginal bleeding to health care provider immediately.
Advise patient to report 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 provider immediately.
Inform patient that ospemifene may cause hot flashes, vaginal discharge, muscle spasm, and ↑ sweating.
Patients who still have a uterus should discuss addition of progestin with health care provider.
Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications.
Advise patient to notify health care provider of medication regimen before treatment or surgery.
Caution patient that cigarette smoking, ↑ BP, high cholesterol, diabetes, and being overweight during estrogen therapy may ↑ risk of heart disease.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected and to avoid use during breastfeeding.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

50056- Angelini Pharma Italia Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. Spa
- 50056-2021-
  - 50056-2021-5- 50 kg in 1 DRUM (50056-2021-5)

55494- Duchesnay USA, Inc.
- 55494-580- Osphena
  - 55494-580-18- 1 BLISTER PACK in 1 PACKAGE (55494-580-18) / 15 TABLET, FILM COATED in 1 BLISTER PACK

55494- Duchesnay USA, Inc.
- 55494-580- Osphena
  - 55494-580-30- 30 TABLET, FILM COATED in 1 BOTTLE (55494-580-30)

55494- Duchesnay USA, Inc.
- 55494-580- Osphena
  - 55494-580-55- 1 BLISTER PACK in 1 PACKAGE (55494-580-55) / 5 TABLET, FILM COATED in 1 BLISTER PACK

55494- Duchesnay USA, Inc.
- 55494-580- Osphena
  - 55494-580-90- 90 TABLET, FILM COATED in 1 BOTTLE (55494-580-90)

63069- PENN PHARMACEUTICAL SERVICES LTD
- 63069-601-
  - 63069-601-01- 600 BLISTER PACK in 1 CARTON (63069-601-01) / 15 TABLET, FILM COATED in 1 BLISTER PACK

63069- PENN PHARMACEUTICAL SERVICES LTD
- 63069-601-
  - 63069-601-02- 1250 BLISTER PACK in 1 CARTON (63069-601-02) / 5 TABLET, FILM COATED in 1 BLISTER PACK

63069- PENN PHARMACEUTICAL SERVICES LTD
- 63069-601-
  63069-601-03- 1 BAG in 1 CONTAINER (63069-601-03) / 30000 TABLET, FILM COATED in 1 BAG

66039- Glenmark Life Sciences Limited
- 66039-912-
  66039-912-04- 50 kg in 1 DRUM (66039-912-04)

69037- Honour Lab Limited
- 69037-0026-
  69037-0026-1- 25 kg in 1 DRUM (69037-0026-1)

70600- Maithri Drugs Private Limited
- 70600-042-
  70600-042-01- 50 kg in 1 DRUM (70600-042-01)

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Indications ⬇

Contraind./Precautions ⬆ ⬇