Ospemifeno

Ospemifeno Uses, Dosage, Side Effects, Food Interaction and all others data.

Ospemifeno is a new selective non-hormonal estrogen receptor modulator (SERM) that is used for the treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause. FDA approved on February 26, 2013.

The half maximal inhibitory concentration (IC50) for estrogen receptor (ER) alpha and beta are 0.8 μM and 1.7 μM, respectively. Ospemifeno has potential uses in the management of osteoporosis in postmenopausal women. It interacts with osteoblasts and osteoclasts in such a way that it reduces bone turnover. It also has potential uses in the prevention of breast cancer. Studies suggest that ospemifene, in a dose-dependent manner, reduces the incidence of tumours.

Trade Name Ospemifeno
Availability Prescription only
Generic Ospemifene
Ospemifene Other Names Deamino-hydroxytoremifene, Ospemifene, Ospemifeno
Related Drugs estradiol, estradiol topical, Premarin, progesterone, Estrace, Prometrium, Prempro, Vagifem, ethinyl estradiol / norethindrone, Osphena
Type
Formula C24H23ClO2
Weight Average: 378.891
Monoisotopic: 378.138657687
Protein binding

>99% bound to serum proteins

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Ospemifeno
Ospemifeno

Uses

Ospemifeno 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.

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

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

How Ospemifeno works

Ospemifeno 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: Ospemifeno should be taken once daily with food.

Ospemifeno Cholesterol interaction

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

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

Ospemifeno 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

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 Ospemifeno

*** Taking medicines without doctor's advice can cause long-term problems.
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