Ospemifene

Uses

Ospemifene is a non-hormonal estrogen receptor modulator (SERM) used to treat moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause.

Ospemifene is used for the treatment of moderate to dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause.

Ospemifene is also used to associated treatment for these conditions: Moderate Dyspareunia, Severe Dyspareunia

How Ospemifene works

Ospemifene is a next generation SERM (selective estrogen receptor modulator) that selectively binds to estrogen receptors and either stimulates or blocks estrogen's activity in different tissue types. It has an agonistic effect on the endometrium.

Toxicity

Adverse reactions (≥1 percent) include: hot flush, vaginal discharge, muscle spasms, genital discharge, hyperhidrosis.

Food Interaction

• Take with food.

[Moderate] ADJUST DOSING INTERVAL: Food significantly enhances the oral bioavailability of ospemifene.

In a cross-study comparison, administration of a single 60 mg dose of ospemifene with a high-fat

Elimination half-life and time to maximum concentration (Tmax) were not altered.

In two separate food effect studies where different ospemifene tablet formulations were given to healthy male volunteers, ospemifene Cmax and AUC increased by 2.3- and 1.8-fold, respectively, with a low-fat
MANAGEMENT: Ospemifene should be taken once daily with food.

Ospemifene Cholesterol interaction

[Major] There is a reported increase of stroke and deep vein thrombosis (DVT) in postmenopausal women receiving oral conjugated estrogens.

Ospemifene should be prescribed for the shortest duration consistent with treatment goals, weighting risks and benefits for each woman.

Ospemifene is contraindicated in women with active DVT, pulmonary embolism, active arterial thromboembolic disease (such as stroke or myocardial infarctions), or a history of any of these conditions.

Other risk factors for cardiovascular disorders and

Ospemifene Drug Interaction

Moderate: estradiol, raloxifene, conjugated estrogensUnknown: fexofenadine, lorazepam, aspirin / caffeine, multivitamin with minerals, docusate, rosuvastatin, duloxetine, ferrous sulfate, omega-3 polyunsaturated fatty acids, biotin, hydrocortisone topical, ipratropium, insulin glargine, lurasidone, pregabalin, polyethylene glycol 3350, cholecalciferol

Ospemifene Disease Interaction

Major: breast cancer, cardiovascular disorders, genital bleeding, severe hepatic impairment

Volume of Distribution

448 L

Elimination Route

When a single oral dose of ospemifene 60 mg is given to postmenopausal women under fasted conditions, the pharmacokinetic parameters are as follows: Tmax = 2 hours (range of 1 - 8 hours); Cmax = 533 ng/mL; AUC (0-inf) = 4165 ng•hr/mL. When the same aforementioned dose is given to postmenopausal women under fed conditions, the pharmacokinetic parameters are as follows: Tmax = 2.5 hours (1 - 6 hours); Cmax = 1198 ng/mL; AUC (0-inf) = 7521 ng•hr/mL. Accumulation occurs following repeated doses. Time to steady state = 9 days.
Although the bioavailability of ospemifene has not been formally evaluated, it is expected to have a low bioavailability because of its lipophilic nature.

Half Life

Terminal half-life = 26 hours .

Clearance

Total body clearance = 9.16 L/hr.

Elimination Route

Following an oral administration of ospemifene, approximately 75% and 7% of the dose was excreted in feces and urine, respectively. Less than 0.2% of the ospemifene dose was excreted unchanged in urine.

Innovators Monograph

You find simplified version here Ospemifene