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ospemifene (Osphena)
Indications:
- moderate-to-severe dyspareunia
- painful intercourse due to vulvar & vaginal atrophy during menopause
- moderate to severe genitourinary syndrome of menopause
Contraindications:
- abnormal vaginal bleeding
- pregnancy
- history of thromboembolism, stroke, or myocardial infarction
- history of breast cancer, ovarian cancer, uterine cancer
Dosage:
- 60 mg PO QD
- take with food
Tabs: 60 mg film-coated tablets
Storage: store at room temperature
Pharmacokinetics:
- highly protein-bound
- metabolized by CYP3A4 & CYP2C9, & to a small extent, CYP2C19 [3]
Adverse effects:
- thickening of the endometrium
- vaginal discharge, vaginal bleeding
- hot flashes
- muscle spasms
- excessive sweating
- risks for stroke & deep venous thrombosis are reportedly less than with estrogen therapy
Drug interactions:
- CYP3A4 inhibitors may increase ospemifene levels
- fluconazole can increase ospemifene levels 3-fold
- smaller increases in ospemifene levels occur with ketoconazole & omeprazole
- CYP3A4 inducers may decrease ospemifene levels
- rifampin can decrease ospemifene levels by ~60% [3]
Mechanism of action:
- selective estrogen receptor modulator
- estrogen receptor agonist/antagonist
Notes:
- wholesale average cost (2014) is about $160 for a month supply [3]
General
selective estrogen receptor modulator (SERM)
Database Correlations
PUBCHEM correlations
References
- FDA News Release: Feb. 26, 2013
FDA approves Osphena for postmenopausal women experiencing
pain during sex.
http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm341128.htm
- Rutanen EM, Heikkinen J, Halonen K et al
Effects of ospemifene, a novel SERM, on hormones, genital tract,
climacteric symptoms, and quality of life in postmenopausal
women: a double-blind, randomized trial.
Menopause. 2003 Sep-Oct;10(5):433-9
PMID: 14501605
- Prescriber's Letter 21(3): 2014
Postmenopausal Hormone Therapy
CHART: Postmenopausal Hormone Therapy
COMMENTARY: Nonhormonal Therapy for Hot Flashes
COMMENTARY: New Drug: Osphena (Ospemifene)
SPECIAL REPORT: Natural Medicines in the Clinical Management of
Menopausal Symptoms
Detail-Document#: 300310
(subscription needed) http://www.prescribersletter.com
- Geriatric Review Syllabus, 9th edition (GRS9)
Medinal-Walpole A, Pacala JT, Porter JF (eds)
American Geriatrics Society, 2016
- Geriatric Review Syllabus, 11th edition (GRS11)
Harper GM, Lyons WL, Potter JF (eds)
American Geriatrics Society, 2022