Deamino-hydroxytoremifene
Deamino-hydroxytoremifene Uses, Dosage, Side Effects, Food Interaction and all others data.
Deamino-hydroxytoremifene 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. Deamino-hydroxytoremifene 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 | Deamino-hydroxytoremifene |
| 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 |
Uses
Deamino-hydroxytoremifene 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.
Deamino-hydroxytoremifene is used for the treatment of moderate to dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause.
Deamino-hydroxytoremifene is also used to associated treatment for these conditions: Moderate Dyspareunia, Severe Dyspareunia
How Deamino-hydroxytoremifene works
Deamino-hydroxytoremifene 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: Deamino-hydroxytoremifene should be taken once daily with food.
Deamino-hydroxytoremifene Cholesterol interaction
[Major] There is a reported increase of stroke and deep vein thrombosis (DVT) in postmenopausal women receiving oral conjugated estrogens.
Deamino-hydroxytoremifene should be prescribed for the shortest duration consistent with treatment goals, weighting risks and benefits for each woman.
Deamino-hydroxytoremifene 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
Deamino-hydroxytoremifene 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
Deamino-hydroxytoremifene 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 Deamino-hydroxytoremifene
