ospemifene (Osphena)
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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
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
Mechanism of action
Notes
- wholesale average cost (2014) is about $160 for a month supply[3]
More general terms
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: https://www.ncbi.nlm.nih.gov/pubmed/14501605
- ↑ 3.0 3.1 3.2 3.3 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#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=300310&pb=PRL (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