Osmifen 60

Osmifen is an estrogen receptor agonist/antagonist used to manage moderate to severe pain during sexual intercourse (dyspareunia) associated with vulvar and vaginal atrophy caused by menopause. It may also help relieve moderate to severe vaginal dryness related to menopausal vulvovaginal atrophy.

Ospemifene is a selective estrogen receptor modulator (SERM). It selectively attaches to estrogen receptors and can either produce estrogen-like effects or block estrogen activity depending on the type of tissue. It has an estrogen-like effect on the endometrium.

Dosage & Administration

For moderate to severe dyspareunia or vaginal dryness associated with menopause, the usual dose is:

Ospemifene 60 mg once daily with food, or as directed by a physician.

রেজিস্টার্ড চিকিৎসকের পরামর্শ মোতাবেক ঔষধ সেবন করুন।

Drug Interactions

Osmifen is mainly metabolized by CYP3A4 and CYP2C9, while CYP2C19 and other pathways also contribute to its metabolism.

• Estrogens and estrogen agonists/antagonists: Concurrent use is not recommended because the safety of combining these medicines has not been adequately established.
• Fluconazole: May significantly increase ospemifene levels in the blood and consequently increase the risk of adverse effects. Concomitant use should be avoided.
• Rifampin: Can substantially lower ospemifene exposure and may reduce its therapeutic effectiveness.
• Ketoconazole: May increase ospemifene exposure and potentially increase the likelihood of adverse reactions.
• Warfarin: Repeated ospemifene administration did not significantly affect the pharmacokinetics of a single warfarin dose. However, its effect on INR and other clotting parameters has not been adequately studied.
• Highly protein-bound medicines: Since ospemifene is more than 99% bound to plasma proteins, it may alter the exposure of other highly protein-bound medicines.
• CYP3A4/CYP2C9 inhibitors: Using Osmifen with medicines that inhibit these enzymes may increase ospemifene exposure and the risk of adverse effects.

Contraindications

Osmifen should not be used in women with:

• Unexplained or undiagnosed abnormal genital bleeding
• Known or suspected estrogen-dependent cancer
• Current or previous deep vein thrombosis (DVT) or pulmonary embolism (PE)
• Current or previous arterial thromboembolic disease, such as stroke or myocardial infarction
• Known allergy or hypersensitivity to ospemifene or any of its ingredients
• Pregnancy or the possibility of becoming pregnant

Ospemifene may cause fetal harm and is therefore contraindicated during pregnancy.

Side Effects

Possible adverse effects include:

• Hot flashes
• Vaginal discharge
• Muscle spasms
• Excessive sweating
• Cardiovascular or vascular disorders
• Malignant neoplasms

Pregnancy & Lactation

Pregnancy: Osmifen should not be used during pregnancy or by women who may become pregnant. Animal studies have demonstrated embryo-fetal death, difficult labor, and increased neonatal mortality. If pregnancy occurs during treatment, the potential risk to the fetus should be discussed with a healthcare professional.

Breastfeeding: It is not known whether ospemifene passes into human breast milk. Its effects on breastfed infants and milk production have not been established. Breastfeeding should therefore be avoided during treatment.

Precautions & Warnings

• Cardiovascular and thromboembolic risk factors such as high blood pressure, diabetes, smoking, high cholesterol, obesity, and personal or family history of blood clots should be appropriately managed.
• Osmifen may increase the risk of stroke and venous thromboembolism (VTE).
• If DVT, pulmonary embolism, or another VTE is suspected or confirmed, treatment should be stopped immediately.
• When possible, treatment should be discontinued 4–6 weeks before surgery associated with an increased risk of blood clots or during prolonged periods of immobilization.
• Osmifen has estrogen-like activity in the endometrium and may cause endometrial thickening, hyperplasia, or polyps. Persistent or recurrent abnormal vaginal bleeding should be investigated promptly.
• Osmifen has not been adequately studied in women with breast cancer and should not be used in women with known or suspected breast cancer.
• It should not be used in women with severe hepatic impairment.
• Patients who develop hypersensitivity reactions such as angioedema, hives, rash, or itching should discontinue the medicine and seek medical advice.
• Osmifen may trigger or worsen hot flashes.
• Appropriate clinical monitoring of postmenopausal women receiving Osmifen is important, particularly when abnormal vaginal bleeding occurs.

Carcinogenicity

Animal studies have shown increases in certain adrenal and ovarian tumors in female mice exposed to high doses of ospemifene. These findings may be associated with its estrogenic and anti-estrogenic activity. The clinical significance of these animal findings in humans is uncertain.

Mutagenicity

Ospemifene did not demonstrate genotoxic effects in the laboratory and animal tests described, including bacterial mutation testing, mouse lymphoma testing, bone marrow micronucleus testing, and assessment of DNA adduct formation.

Effect on Fertility

The direct effect of ospemifene on human fertility has not been established. Animal studies showed changes in reproductive organs and reproductive cycles, including ovarian and uterine changes in females and changes in reproductive tissues in males. These findings are consistent with the drug’s estrogen receptor activity.

Use in Special Populations

Children: Osmifen is not indicated for children because it has not been adequately studied in pediatric patients.

Elderly: Clinical studies have not identified meaningful differences in safety or effectiveness between women aged 65 years and older and younger women.

Renal impairment: No dosage adjustment is generally required in women with renal impairment, including severe renal impairment, based on available pharmacokinetic data.

Hepatic impairment: Osmifen should not be used in women with severe hepatic impairment because its use in this population has not been adequately studied.

Therapeutic Class

Drugs used for vaginal and vulval conditions

Storage

Store below 30°C, away from light and moisture. Keep out of reach of children.