Evatone 2 Tablet

Evatone 2 is an Estradiol valerate, containing medication which a synthetic form of the female hormone estrogen.  It is used in hormone replacement therapy (HRT) to treat menopausal symptoms like hot flashes, vaginal dryness, and to prevent postmenopausal bone loss.  After taking it, it converts to natural Estradiol in the body and works by replacing estrogen lost during menopause.  If the uterus is intact, it must be taken with a progestin to prevent endometrial cancer.

Key Features

 How does Evatone 2 Tablet work?

Estradiol valerate is a prodrug of 17β-Estradiol, the main natural estrogen.

• After oral intake, it’s hydrolyzed in the liver to Estradiol and valeric acid.
• Estradiol binds to estrogen receptors ER-α and ER-β in target tissues: uterus, breast, bone, brain, liver.
• Replaces estrogen lost in menopause this may reduce hot flashes, prevents bone loss, reverses vaginal atrophy. Also induces proliferative changes in endometrium.
• If uterus is intact: Must be given with progestin for 10-14 days/month or continuously to prevent endometrial hyperplasia/cancer from unopposed estrogen.

Usage

• It is also used in Hormonal Replacement Therapy (HRT).
• It is used in dealing with Menopausal symptoms like moderate-severe vasomotor symptoms, hot flashes, night sweats.
• Managing Vulvar/vaginal atrophy.
• Prevention of postmenopausal osteoporosis.
• Hypoestrogenism: Due to hypogonadism, ovarian failure, oophorectomy.
• Palliative care: Advanced androgen-dependent prostate cancer.

Dosage

• Dosage may depend upon the conditions i.e., in the case of menopausal symptoms it can be taken once a day, in the case of vaginal atrophy it can be taken 1-2 mg once a day, in the condition of osteoporosis it can be taken daily.
• It can be taken daily, with/without food.
• If dose missed, take if less than 12 hrs late, otherwise can skip.

Side effects

• Headache
• Nausea
• Bloating
• Leg cramps
• Breakthrough bleeding
• Mood changes
• Breast tenderness/enlargement

Interactions

• CYP3A4 inducers like Rifampin, carbamazepine, phenytoin, St. John’s Wort may decrease Estradiol levels that may can increase the risk of bleeding.
• CYP3A4 inhibitors like Ketoconazole, clarithromycin, grapefruit juice may increase the level of Estradiol this may lead to side effects.
• Corticosteroids may increase free cortisol due to increase in Capillary Blood glucose (CBG).
• Anticoagulants may alter warfarin effect.
• Lamotrigine, Estrogen may decrease the lamotrigine levels.

Pharmacokinetics

• Absorption: Well absorbed orally. Bioavailability 3-5% due to first-pass metabolism. Peak Estradiol in 4-9 hrs.
• Distribution: 98% bound to sex hormone binding globulin and albumin. Volume of distribution 1 L/kg.
• Metabolism: Liver via CYP3A4, CYP1A2. Converted to estrone, then estriol. Also, sulfation/glucuronidation.
• Half-life: Estradiol valerate is approx. 14 hrs. Terminal half-life of Estradiol 13-20 hrs.
• Excretion: Urine 90% as conjugates, feces approx. 10%.

Precautions

• It can be avoided in Pregnancy.
• It should be avoided in the case of undiagnosed vaginal bleeding, breast cancer, thromboembolic disorder, active liver disease etc.
• The side effects can vary, so prior consult your healthcare provider, to avoid any such unwanted interactions.

Conclusion

Evatone 2 is an Estradiol valerate containing medication which a synthetic form of the female hormone estrogen.  It is used in hormone replacement therapy to treat menopausal symptoms like hot flashes, vaginal dryness, and to prevent postmenopausal bone loss.  After taking it, it converts to natural Estradiol in the body and works by replacing estrogen lost during menopause.  If the uterus is intact, it must be taken with a progestin to prevent endometrial cancer. It may show some side effects like headache, nausea, bloating, leg cramps, mood changes etc, this may can vary from individual to individual and to avoid such unwanted interactions prior consult your healthcare provider.

FAQ’s